Pharmacology Year 1991

Drug Charts
Eicosanoids
NSAIDs
Immunopharmacology
Adrenergic Agonists
Adrenergic Antagonists
PsNS Agents
Anti-Hypertensives
Antibiotics
Cancer Drugs
Movement Disorders
Anti-Convulsants
Anxiolytics
Anti-Psychotics
Anti-Depressants
Alcoholism
Opioids
General Anesthetics
Local Anesthetics
GI Drugs
Anti-Virals
Anti-Virals: HIV
Anti-Arrhythmics
Cardiotonics
Diuretics
Alternative Medications
Pituitary Hormones
Estrogens/Progestins
Thyroid/Parathyroid/Adrenal Hormones
Anti-Malarials
Anti-Parasitics
Pulmonary Drugs
Caloric Regulation
Diabetes Drugs
Lipid Drugs
Dermatology Drugs
Gout Drugs
S. Carr
Drug
Eye
Clotting
PGI
PGE1
PGE2
PGF2
plt aggregation
intraocular
pressure
intraocular
pressure
intraocular
pressure
TXA
plt aggregation
plt aggregation
plt aggregation
LTC
LTD
Epoprostenol (PGI)
Treprostinil
Misoprostol
(PGE1)
Alprostadil
(PGE1)
Dinoprostone
(PGE2)
Latanoprost
(PDF2 )
Carboprost
(PGF2 )
Zileuton
(lipoxygenase)
Zafirlukast (LTR)
Montelukast
Indomethacin
(COX inh.)
(Epopro = IV / Trepro = subQ)
Vasculature
Lungs
GI
vasodilation
( cAMP)
vasodilation
( cAMP)
vasodil + vasocx
( IP3 & Ca2+)
vasocx
( IP3 & Ca2+)
vasocx
( IP3 & Ca2+)
permeability
( BP)
permeability
( BP)
vasodilation
( cAMP)
bronchodilation
( cAMP)
bronchodilation
( cAMP)
bronchodilation
( cAMP)
bronchocx
( IP3 & Ca2+)
bronchocx
( IP3 & Ca2+)
bronchocx
( IP3 & Ca2+)
bronchocx
( IP3 & Ca2+)
acid, mucus,
blood
acid, mucus,
blood
acid, mucus,
blood
(male = erection injection)
tone
(+ oxy CX)
CX
( oxytocin)
body temp
NE
body temp
NE
acid, mucus,
blood
Dinoprostone
Kidney: blood
CX
( oxytocin)
(during pregnancy = dinoprostone)
(vasculature = vasodilates to maintain PDA until surgical correction)
bronchodilation
(blocks LT synth)
bronchodilation
(blocks LT synth)
Treats
Primary pulmonary
HTN
Misoprostol
Alprostadil
Latanoprost
Carboprost
CX
( oxytocin)
(stable, long acting, SE: brown pigmentation, dry eyes)
vasocx
( PG synth)
CNS
Zileuton
Zafirlukast
Montelukast
(administered vaginally, uterine contractions & collagenase activity)
(NSAID indole derivative)
tone
CX
(administered vaginally, uterine contractions & collagenase activity)

intraocular
pressure
tone
Organs
Kidney: blood,
diuresis
Kidney: blood,
diuresis, ADH
Kidney: blood,
diuresis, ADH
(vasculature = vasodilates to relieve pulmonary HTN)
(GI = cytoprotective at low doses, acid at high doses)

vasodilation
( cAMP)
Reproductive
CX
( oxytocin)
Primary pulmonary
HTN
NSAID-ulcer
Abortifacient
Impotence
Maintain PDA
Abortifacient
Labor induction
Open angle
glaucoma
Abortifacient
(inhibits leukotrienes)
Asthma
(blocks leukotriene receptors)
Asthma
(vasculature = vasoconstricts to close PDA in premies)
Close PDA
Drug
Inhibits
Aspirin
COX-1
COX-2
Non-acetylated
COX-1
COX-2
salicylates
Ibuprofen
Diclofenac
Etodolac
Indomethacin
Ketoprofen
Naproxen
Sulindac
Celecoxib
Rofecoxib
Valdecoxib
Acetaminophen
NSAID Effects
NSAID Side Effects
Metabolism
Duration
What Makes it Unique
Side Effects
Treats
Low = 15 min
High = 4 h
High = 13 h
1) binds serum proteins (depends on dose)

2) irreversibly acetylates COX-1&2,
3)
irreversibly inhibits platelet aggregation
1) salicylism, respirary alkalosis, met. acid

2) NSAID-asthma
3) Reyes syndome
RA
Chronic inflm
Less effective at COX inhibition than ASA
Less side effects, no renal toxicity,

no NSAID-asthma
RA
Chronic inflm
COX-1
COX-2
Liver
CYP2C8
Short
(2hr)
Low dose = analgesic (no anti-inflam)

High dose = analgesic & anti-inflam
GI, rash, tinnitis, fluid retention

kidney failure, hepatitis
RA
Chronic inflm
COX-1
COX-2
Liver
CYP3A4
CYP2C9
Short
(2hr)
1) serum aminotransferase activity in liver

2) Renal dysfx doesn't impair clearance
Typical NSAID
RA
Chronic inflm
Intermediate
(5 hr)
Affects COX-2 > COX-1 by 10:1
Less GI
RA
Chronic inflm
Very potent indole derivative
30% have to discontinue

(psychosis & hallucination)
RA
Chronic inflm
COX-1
COX-2
COX-1
COX-2
COX-1
COX-2
1) Short (2 hr)
2) Slow release
Also inhibits lipoxygenase
Typical NSAID
RA
Chronic inflm
COX-1
COX-2
Long
(12 hr)
Free fraction is 40% higher in females
Typical NSAID
RA
Chronic inflm
COX-1
COX-2
Long
(12 hr)
1) serum aminotransferases
2) Treats familial intestinal polyposis
Cholestatic liver damage
RA
Chronic inflm
COX-2
1) Least potent of COX-2 inhibitors

2) Does not affect platelet aggregation
Can interfere w/antihypertensive therapy

Still contraindicated in pts w/GI ulcers
RA
Chronic inflm
COX-2
Most COX-2 selective CV problems
Still contraindicated in pts w/GI ulcers
RA
Chronic inflm
COX-1
COX-2
1) COX inhibitory effects primarily in CNS

2) Best anti-pyretic/analgesic in children
3) No anti-inflammatory or anti-coagulant
1) Less GI irritation & bleeding

2) Liver toxicity ( glutathione)
RA
Chronic inflm
Analgesia
(low grade pain)
Anti-pyretic
(PG inhibition)
Anti-inflamatory
(MSK, RA, OA)
Anti-coagulant
(other NSAIDs can block long-lasting ASA)
COX-2 Pro-coagulant
( COX-2 PGI but not COX-1 TXA)
GI irritation
(ASA espclly)
bleeding time
(inhib. TXA)
Kidney effects
Pregnancy
(delayed onset of labor from PGE & PGF)
Hypersensitivity
( COX arachidonate lipoxygenase)
Drug
Cytotoxic
T-cell Inhibitor
Prednisone
Prednisolone
Cyclosporine
Tacrolimus
Sirolimus
Azathioprine
Mycophenolate
FTY720
Antithymocyte Ig
Immunoglobulins
Immune globulin
Anti-CD3 Ig
Basiliximab
Daclizumab
Infliximab
Biological Response Modifiers
Etanercept
Rho Immune Ig
Bacillis CalmetteGuerin
Thymic Factors
Interleukin-2
GM-CSF
G-CSF
Action
Response
Treats
Down-regulate inflammation
Immunosuppression
Anti-inflammatory
Chronic use associated with: infections, ulcers,

hyperglycemia, osteoporosis
Inhibits calcineurin phosphatase

cytokines
Impairs T-cell response to antigen
Tacrolimus is 100x more potent
Inhibits T-cell activation

& proliferation
T-cell response
Renal transplant have surgical complications

May produce an immunosupp tolerance
Converted to thioinosinate
Competitive inhibition of inosinate

S phase inhibitor
Myelosuppression
Coadministration w/allopurinol is toxic
Transplant rejection
Rheumatoid arthritis
Inhibits inosine monophosphate

dehydrogenase
Inhibits T-cell & B-cell cell cycle &

proliferation
Coadminister: cyclosporine & corticosteroids

Do not coadminister: antacids
Sphingosine 1-P receptor agonist
Reversibly sequesters lymphocytes in

2 lymph organs
Graft is protected from T-cell attack

HR in 30% of patients
Ig against T-cells
Removes T-cells from system
Coadminister: azathioprine & corticosteroids
Transplant rejection (kidney)
Human plasma Ig
Replaces missing Ig
Toxicity: autoimmune hemolytic anemia
Immunodeficiencies
Lymphocytic leukemia
Kawasake disease
Ig against CD3 on T-cells
Blocks antigen recognition site
Toxicity: cytokine release syndrome
Ig against IL-2 receptor
Blocks activation of T-cells by IL-2
Coadminister: cyclosporine & corticosteroids

Toxicity: none!
Transplant rejection (kidney)
Ig against TNF-
Blocks immune activation of TNF
Coadminister: methotrexate for RA
Rheumatoid arthritis
Crohn's disease
Ig against anti-D antibodies
Blocks anti-Rh antibodies
Administered to Rh- mother pregnant with Rh+

fetus
Hemolytic disease of the

newborn (prevention)
Strain of myobacterium bovis
Stimulates T-cells & NK cells
Toxicity: severe hypersensitivity & shock
Bladder cancer
Promotes T-cell differentiation
Enhanced T-lymphocytic function
Stem cells rushed through boot camp
SCID
Promotes T & B-cell proliferation,

differentiation
T-cells, B-cells, NK cells
Natural cytokine
AIDS
Cancer
Stimulates clonal expansion
WBC recovery
in pts with hematopoiesis
Natural cytokine
Cancer
Congenital
Autoimmune disease
Transplantation inflm
Hypersensitivity
GVHD (bone marrow trxpnt)
Aplastic anemia (ineligible)
Autoimmune disease
GVHD
Autoimmune disease
Drug
Epinephrine
Phenylephrine
Levarterenol
Norepinephrine
Dopamine
Amphetamine
Arbutamine
-methyl-DOPA
Tyramine
Guanethidine
Ephedrine
Clonidine
Brimonidine
Tizanidine
Isoproterenol
Dobutamine
Metaproterenol
Salmeterol
Formoterol
Terbutaline
Albuterol
Receptors
Heart
Vasculature
1 [high]
2 [high]
1 [low]
2 [low]
1
Reflex bradycardia
DBP ( MSK)
HR, CX, CO
GI
mucus congestion
SBP (indirect)
DBP ( MSK)
Reflex bradycardia
Lungs
Treats
Eye: intraocular
pressure
Metabolism:
Asthma
Anaphylaxis
Cardiac arrest
uterine CX
ACh (2A)
motility
bronchodilation
Organs
Reproductive
motility
uterine CX
DBP & SBP
Nasal deconges.
similar to EPIpotent vasoconstrictor used to treat hypotension & shock
1
2
1
D1 [low]
1 [high]
1 [ high]
Reflex bradycardia
DBP (vasocx)
HR, CX, CO
SBP (indirect)
HR, CX, CO
SBP (indirect)
Shock
Kidney: renin
vasodilation
Kidney: renin
DBP (vasocx)
1) displaces NE from vesicles.2) competitively inhibts NE reuptake.3) inhibits MAO activity NE lingers
1
1
2
1
2
1
1
1
2
1
HR, CX, CO
SBP (indirect)
Narcolepsy
Kidney: renin
some activity, but less effective than NE
1) shock caused by
CO & renal fxn
2) Parkinson's
SE: hepatotoxicity & autoimmune hemolytic anemia
(Experimental)
HTN during
pregnancy
SNS outflow
BP
Reflex bradycardia
DBP (vasocx)
If MAO inhib: 1) displaces NE from vesicles, 2) competes w/NE for reuptake
HR, CX, CO
SBP (indirect)
Initially potentiates NE effects, then eventually depletes NE
Kidney: renin
Depletes NE in the SNS (but does not cross the BBB)
1) displaces NE from vesicles.2) competitively inhibts NE reuptake.3) inhibits MAO activity NE lingers (acts like amphetamine)
2
2
2
1
2
1 [high]
1 [low]
2
2
2
2
2
SNS outflow
SNS outflow
SNS outflow
BP
BP
HTN
humor production & uveoscleral outflow
OA glaucoma
MSK spasticity
HR, CX, CO
SBP (indirect)
cardiac efficiency
DBP vasodilation
cardiac efficiency
DBP (vasocx)
HR, CX, CO
SBP (indirect)
Multiple sclerosis
Kidney: renin
bronchodilation
motility
Kidney: renin
Bronchodilator
Cardiac arrest
Decompensated
heart failure
M = medium
bronchodilation
Medium duration (oral administration)
Bronchospasm
S = steroid & slow
bronchodilation
Long-lasting (inhalation) must be accompanied by steroid
Bronchospasm
Bronchospasm
F = fast
bronchodilation
Long-lasting (inhalation) fast-acting
T = tachycardia
bronchodilation
Minimal tachycardia
Bronchospasm
A = acute
bronchodilation
Short-acting (inhalation) acute relief
Bronchospasm
Drug
Receptors
-methyl-paratyrosine
competitive inhibitor of tyrosine hydroxylase depletes NE, EPI, DA pre-operatively in pheochromocytoma
Reserpine
binds VMAT-2 irreversibly inhibits vesicular concentration of NE & DA transient at receptors SNS depletion
Cocaine
reversibly inhibits NET & DAT (CNS) anesthetic, CNS stimulant, sympathomimetic
Phenoxybenzamine
Carvedilol
Heart
Anti 1
Reflex tachycardia
Anti 2
SNS outflow
Vasculature
Lungs
GI
Reproductive
Organs
vasocx
Treats
Pheochromocytoma
Anti 1
Anti 1
Heart failure
Anti 2
Prazosin
Tamsulosin
Anti 1
Reflex tachycardia
vasocx
Anti 2B
Reflex tachycardia
vasocx
Anti 1A
Reflex tachycardia
vasocx
Alfuzosin
Anti 1
Yohimbine
Anti 2
Propranolol
Anti 1
Anti 1 [low]
Hypertension
HR, CX, CO
SBP
Kidney: renin
bronchocx
HR, CX, CO
SBP
Kidney: renin
Anti 1
HR, CX, CO
SBP
Long-lasting, specific, reduced CNS activity, no bronchocx
Acebutolol
Anti 1
HR, CX, CO
SBP
1 specific, partial agonist less exercise intolerance
Timolol
Anti 1
HR, CX, CO
SBP
intraocular pressure w/o affecting pupil or ciliary body
Anti 2
Anti 1
Kidney: renin
Hypertension
HR, CX, CO
SBP
Hypertension
Hypertension
Kidney: renin
bronchocx
Anti 2
Sotalol
Hypertension
Migraine
bronchocx
Atenolol
Anti 1
BPH
Male impotence
Anti 2 [high]
Labetalol
Hypertension
BPH
smooth muscle RX
Anti 2
Metoprolol
smooth muscle RX
Kidney: renin
Open angle
glaucoma
Hypertension
bronchocx
HR, CX, CO
SBP
Anti 2
anti-arrhythmic, anti-atrial fibrillation

bronchocx
Kidney: renin
Arrhythmia
Atrial fibrillation
Carbachol
ACh musc Ciliary muscle CX widens trabecular network drainage of aqueous humor
OA glaucoma
Pilocarpine
ACh musc Ciliary muscle CX widens trabecular network drainage of aqueous humor
OA glaucoma
Physostigmine
AChE inhib Ciliary muscle CX widens trabecular network drainage of aqueous humor
OA glaucoma
Echothiophate
AChE inhib Ciliary muscle CX widens trabecular network drainage of aqueous humor
OA glaucoma
Brimonidine
Latanoprost
2
PDF2
Inhibits aqueous humor production
OA glaucoma
Enhance uveoscleral outflow
OA glaucoma
Cholinomimetics
Drug
Bethanechol
Carbachol
Pilocarpine
Parasympathetic Antagonists
Atropine
Scopalamine
Heart
Vasculature
Lungs
GI
GU
Organs
Treats
Choline Ester
PsNS agonist
M1, M2, M3
M2
[Lo] = reflx tach
[Hi] = AV block
M3
vasodil (B & C)
secretions
bronchoCX
M1
motility (B)
secretions
M1
Detrussor CX
(B & C)
Eye : M1
Circular M. CX
Ciliary M. CX
C: OA glaucma
B: GI/GU retentn
Natural alkaloid
M1, M2, M3
Muscarinic blockade
(M1, M2, M3)
Muscarinic blockade
(M1, M2, M3)
Pirenzepine
M1 antagonist
Tolterodine
Trospium
Oxybutynin
Anti-muscarinic
Ipratropium
Tiotropium
Edrophonium
Physostigmine
Neostigmine
Cholinesterase Inhibitors
Mechanism
M3 (ant)
vasocx
secretions
bronchodil
M1 (ant)
motility
secretions
M1 (ant)
Detrussor RX
Urine retention
Eye: M1 (ant)
Circular M. RX
Ciliary M. RX
Used w/H-2 blockers to reduce gastric acid secretion to promote gastric ulcer healing
Reversible ChE
inhibitor (competitive)
Physo : block nACh?
DFP
Irreversible ChE
inhibitor
(phosphorylate ChE)
GI spasms
Eye exams
ChEI toxicity
Anesth adjunct
Motion sickness
Overax bladder
Gastric ulcer
Overactive
bladder
secretions
bronchodil
COPD
Reversible ChE
inhibitor
Diagnosis of MG
PAT
Direct:
M2
HR
Indirect:
M3
vasodil
reflex tachy
M3
NO-cGMP
vasodil
secretions
bronchoCX
M1
motility
secretions
M1
Detrussor CX
Trigone RX
Ex. sphincter RX
micturition
Parathion
Eye : M1
Circular M. CX
Ciliary M. CX
~
Skel Muscle :
Nm
fasciculations
~
CNS :
Stimulation
depression
Atropine toxicity
(crosses BBB)
Paralytic ileus
Treatment of MG
Xerostomia
Caused by
exposure to
toxins
*Atropine can
reverse
*Pralidoxime can
reverse
Soman
Tacrine
Donepezil
Tubocurarine
Mivacurium
Vecuronium
Rocuronium
Succinylcholine
Ganglion blockers
Botulinum toxin
Varenicline
Reverses ChEI
toxicity
Splits covalent bond forming oxime-phosphonate splits off leaves regenerated ChE
Pralidoxime
Neuromuscular Junction Blockers (nAChR)
M2 (ant)
[Lo] = brady
[Normal] = HR
M2 (ant)
[Lo] = brady
[Hi] = HR
Muscarinic blockade
(M1, M2, M3)
[No cilia motility]
Echothiophate
Malathion
Treats OA glaucoma: (1) pupillary CX, (2) spasm of accom., (3) transient IOP persistent IOP, (4) impaired night vision
Non-competitive
reversible ChE inhib.
(centrally-acting)
Steroid nucleus
competitive NMJ
blocker (NmX)
Isoquinoline
competitive NMJ
blocker (NmX)
Depolarizing NMJ
blocker
( open freq. & dur.)
Competitive /
Depolarizing Nn
blockers
Prevent ACh release
from the motor nerve
terminal
Partial nicotine agonist
at 42 Nn
Also: (1) blocks DA, NE, 5-HT uptake (2) MAO inhibitor (3) block Na+ & K+ channelshepatotoxicity
Alzheimer's
disease
AChE selectivity in CNS (minimal peripheral activity)no hepatotoxicity
Nm (ant)
HR
(PsNS + rx tach)
Nm (ant)
BP
(SNS + hstmne)
Resp. paralysis
BronchoCX
(histamine)
Drug intrx: aminoglycosides & tetracyclines

Contraind.: asthma, MG
cardiac effects (less tachycardia)... histamine release (more bronchoCX)
Used during
procedures that
require muscle
paralysis
cardiac effects (more tachycardia)... histamine release (less bronchoCX)

Nn
HR
(PsNS + rx brad)
Nn (ant)
HR (PsNS)
CX (SNS)
Nn
BP
(SNS)
Nn (ant)
BP
Resp. paralysis
Slight histamine
w/halothane + RyR defect malig. Hyperthermia

(give sodium dantrolene)
Nn (ant)
motility secr
(PsNS)
Nn (ant)
Urinary reten
impotence
Eye : mydriasis
Skin : sweat
Surg: bleeding
SCI: reflexia
Cleaves synaptobrevin & SNAP to prevent ACh vesicle fusion & release
Dystonia
Spasticity
Hyperhidrosis
May help prevent rewarding aspects of nicotine administration
Nicotine addiction
Drug
SNS Inhibitors
Guanethidine
Reserpine
-methyl DOPA
Clonidine
Blockers
K+
Thiazide
Sparing
Diuretic
Diuretic
Direct on VSM
Hydralazine
Minoxidil
Sodium
nitroprusside
Hydrochlorothiazide
Chlorthalidone
Amiloride
Spironolactone
Proproanolol
Atenolol
Acebutolol
ReninPDE5
1
Ca2+ Channel Blockers Angiotensin
inhib
Antag
Inhibitors
Labetalol
Prazosin
Captopril
Enalapril
Losartan
Nifedipine
Verapamil
Diltiazem
Sildenafil
Mechanism
Duration
Renin
Side Effects
Treats
Depletes NE
SNS
Long lasting
w/residual
Initial:
Eventual:
Reserpine: central depletion of 5-HT, DA,

NEParkinsonism & depression
Nasal cong, ortho hypo, miosis, brady,

diarrhea, cramps, imp
HTN (?)
Stimulate NTS
2 receptors
Post-syn 2A
NTS SNS
Initial:
Eventual: ?
Metabolized to -methyl NE (false NT) and

acts mostly 2, little 1 centrally
Common+...hemolytic anemia,
sedation, imp, lactation, EP signs
Moderate HTN
(LVH)
Stimulate NTS
2 receptors
Initial:
Eventual: ~
No DA problems ( lactation, EP signs)
Less ortho hypo, rebound W/D HTN
HTN (?)
NO
K+ permeability
Initial:
Eventual: ?
Can produce a lupus-like syndrome
Tachycardia, fluid retention, edema,

headache, nausea
Severe HTN
K+ permeability
Initial:
Eventual: ?
Preference for resistance (over capacitance)

vessels. venous pooling
Same as hydralazine
(should use w/-blocker & diuretic)
Severe HTN
w/ renal disease
Initial:
Eventual: ?
Unstable: degrades thiocyanate & CN

IV only: moment to moment control
Nausea & headache
HTN Crisis!
Na+ reabsorption
in DCT urine
Initial:
Eventual: ~
Ceiling effect of 15 mmHg
Hypokalemia, hyperglycemia,
hyperuricemia, chol & TAG
Mild HTN
Aldosterone
antagonist
Initial: ?
Eventual: ?
Used with thiazide diuretic to avoid

hypokalemia
Hyperkalemia (in renal disease)

Gynecomastia
Not anti-HTN by
themselves
Metabolized to NO
cGMP
Very short
Mild-Moderate
HTN
Initial:
CX, CO, renin
pre-syn. (+) fdbk
Recommended use: w/ CHF or angina

NSAIDs interfere w/anti-HTN effect
Initial:
Same as above
(+ partial agonist)
Initial:
1/1/2 blocker
Initial:
Partial agonist activity:

less HDL & less exercise intolerance
Heart, bronchial CX, hypoglycemia,

W/D rebound, exercise intol.
TAG & HDL
t1/2 = 3-4 hr
Initial:
Could cause cardiac events
Prevent A1 A2
conversion
(ACE inhibitors)
Short
Long (prodrug)
Initial: ?
Eventual: ?
Also inhibit bradykinin metabolism

leads to PGI2 production cough
Good in diabetics (renal)/CHF
Vasculature A-2
receptor blocker
Initial: ?
Eventual: ?
Similar to ACE inhib. but no cough
DHP Ca2+
channel blocker
Initial: ?
Eventual: ?
Good vasodilation w/ less cardiodepression
Reflex tachycardia
Adverse cardiac events
Initial: ?
Eventual: ?
Cardiodepression: HR & CO
Little reflex tachycardia

Initial: ?
Eventual: ?
Similar to Verapamilbut less HR & CO
Little reflex tachycardia

Initial: ?
Eventual: ?
Requires ACh to initiate process:

M3 NOS GMP cyclase cGMP
Rx interaction: (in cardiac pts)

Nitrates NO hypotension
PDE-5 inhibitor
cGMP
Mild-Moderate
HTN
HTN Crisis!
Block 1
(& some 2B)
Should use
long-acting
L-type Ca2+ channel
(short acting
blocker
toxicities)
Ca2+ channel
blocker
Mild-Moderate
HTN
Syncope (initial trx), ortho hypo,

tachycardia, headache, depression
Mild-Moderate
HTN
Cough, rash, leukopenia, renal,

ageusia, fetal ab, no ortho hypo,
K+ diuretic, BC, NSAID, lithium intaxn
Hypotension in volume-depleted pts
Less effective in Afr.Americans
Moderate HTN
(LVH)
HTN (?)
HTN (?)
(Not first-line)
impotence
Pulm. Art. HTN
Fluoro
quinolones
Resistance
Pharmacodynamics
Adverse Reactions
Inhibit DNA gyrase & topo IV

(Bactericidal)
1) Target modification
2) Altered uptake/efflux
3) Plasmid-mediated modification by
quinolone transacetylase
Administer: oral or IV
Drug Intrxn: antacids oral avail.
Arthopathy (no preg or children)

QT interval prolongation
Inhibit RNA polymerase

(Bactericidal)
Target site mutation in rpoB subunit
Distribution: great, CNS, intracellular
Liver problems, induces cyt p450

(HIV meds), turns fluids orange
Metronidazole
Produces compounds
toxic to DNA
(Rare, unknown mechanisms)
Distribution: great, CNS
elimination of lithium & ergot

derivatives...(no alcohol!)
Sulfanilamide
PABA analog that binds DHP

synthetase folic acid
Target site mutation, up-regulation,
new genes, altered uptake/efflux
(Plasmid/Chromosomal)
Sulfa & trimethoprim given together
(TMX-SMX = Bactrim)
Sulfa given w/silver ions in cream
Allergy
Not given to: G6P or folic acid
deficiency, or pregnant
HIV: prophylaxis neutropenia &
exfoliative dermatitis
1) Altered transpeptidases
2) permeability
3) -lactamases
Distribution: good bioavailability
Crosses BBB
Allergy
(Can be desensitized)
1) Altered transpeptidases
2) permeability
3) -lactamases
Distribution: good bioavailability
Crosses BBB
Allergy
(Can be desensitized)
Transposon: enzymes use D-serine or

D-lactate to make cell wall
Administer: IV
Distribution: good, CNS (inflam.)
Red man syndrome: histamine

mediated w/rapid IV admin.
Administer: topical
(often w/neomycin & polymyxin B)
Allergy (rare)
Ciprofloxacin
Levofloxacin
Sulfa
Drugs
Trimethoprim
Dapsone
Penicillins
w/-lactamase
inhibitors
Poly Glyco
peptide peptide
DHF acid analog that binds DNF

acid reductase folic acid
PABA analog that binds DHP
synthetase folic acid
Penicillin G/V
Artificial penicillin
Bind transpeptidase & prevent

cross-linking
TicaricillinClavulanic Acid
Amoxicillin1) Bind transpeptidase & prevent
Clavulanic Acid
cross-linking
Piperacillin2) Bind & inhibit -lactamase
Tazobactam
Ampicillin-Sulbactam
Vancomycin
Bacitracin
Binds D-alanine dimer in crosslinking peptide in peptidoglycan

Binds membrane lipid carrier
molecule cell wall comp.
Cephalosporins
Cephalexin
Carba Mono
penem bactam
Inhibitors of the Bacterial Cell Wall
Action
Rifampin
Penicillins
Inhibitors of Nucleic Acid Synthesis
Drug
Cefotaxime
cross-linking
Allergy
(5-10% PCN-allergy crosshypersensitivity)
Aztreonam

cross-linking
No PCN-allergy crosshypersensitivity
Imipenem-Cilastatin
Ertapenem

cross-linking
Ceftazidime
Ceftriaxone
Cilastatin = inhibits renal

dihydropeptidase I to prolong t1/2
Allergy
(PCN-allergy cross-hypersen.)
Drug
Action
Resistance
Pharmacodynamics
Adverse Reactions
1) Block protein synthesis by

bacterial ribosomes
2) Disrupt magnesium bridges in
LPS
1) Modifying enzymes (most com .)

2) Efflux pumping
3) Altered ribosome binding
Administer: IM or IV
Post-ABX Effect: persistent
suppression after drug removal
Conc.-Dependent Killing:
concentrations better killing
Nephrotoxicity
Ototoxicity
(Particularly Streptomycin)
Distribution: good, including CNS
Drug Intx: food absorption
Antagonizes -lactams
Nausea
Photosensitivity
Can discolor teeth
(not given to children or pregnant)
Tetracyclines
Inhibitors of Bacterial Protein Synthesis
Aminoglycosides
Streptomycin
Neomycin
Gentamycin
Tobramycin
Tetracycline
Doxycycline
Block protein synthesis by bacterial

ribosomes
Tigecycline
1) Efflux pumping (most common )

2) Altered ribosome binding
Not affected by resistance
Macrolides
Erythromycin
More nausea & QT prolongation
Azithromycin
Clarithromycin

ribosomes
1) Methylation of ribosomes
(most common )
2) Efflux pumping
Distribution: good
Azithromycin: long intracellular
half-life, given to children, pregnant
Miscellaneous
Strepto
gramin
Oxazoli Linco
dinone samide
Telithromycin
Severe hepatotoxicity
Clindamycin

ribosomes
Linezolid

ribosomes
Chloramphenicol

ribosomes
QuinupristinDalfopristin
Polymyxins

Occurs if only one of the two is given
ribosomes
Daptomycin
Nitrofurantoin
Mupirocin
Administer: oral or IV or topical

Distribution: good, but no CNS
Allergy
Distribution: good
Thrombocytopenia
Contraindication: SSRI
Aplastic anemia, BM suppression

Gray syndrome (shock, coma)
Administer: IV
Arthralgias
Myalgias
Disrupts bacterial membranes
Administer: Topical or IM or IV
(often w/neomycin & bacitracin)
Few
Cyclic lipopeptide: interferes

w/bacterial membrane
Administer: IV
liver fx tests
muscle weakness & pain (CPK)
Administer: oral
(drug concentrated in urine)
Turns urine brown

Lung problems w/chronic use
Radiomimetic
(IC enzymatic redctn required)
Disrupts protein synthesis
1) rRNA methylation/adenylation
2) altered ribosomal proteins
1) acetylation (most common )

2) efflux pumping
Altered levels of reduction enzymes
Drug
MOA
Treats
Toxicity
Hodgkin lymphoma
Bone marrow
GI
Interesting N-(CH2-CH2-Cl)2
structure activates to ring
Non-Hodgkin Lymphoma
Breast/Ovary Carcinoma
Bone marrow (immunosupp)

Alopecia
Hemorrhagic cystitis
Acrolein byproduct toxic but

rescued by MESNA
lipophilic crosses BBB
Brain tumors

Nephrotoxicity (long-term trx)
Inhibits DNA synthesis
Pancreatic islet cell

carcinoma
Insulin shock
Nephrotoxicity
Hepatotoxicity
CML
Pulmonary fibrosis
Mechlorethamine
Cyclophosphamide
Monofx: modify DNA base

Bifx: DNA cross-link or DNA-protein
Alkylating Agents
(Phase non-specific)
Ifosfamide
Carmustine
Lomustine
Streptozocin
Dacarbazine
Temozolomide
Procarbazine
Cis-platinum
Carboplatin
Oxaliplatin
Methotrexate
6-Mercaptopurine
Antimetabolites
(S phase specific)
6-Thioguanine
Fludarabine
We must preserve the brain

to maintain life!
Retained in cells of islets of
Langerhans
Active metabolite monomethyl triazeno Dcarb: Hodgkin lymphoma

Temozo: malignant glioma
methylates DNA

Nausea
Forms intrastrand & interstrand DNA

cross-links DNA/RNA synthesis
Produces DNA breaks
Hodgkin/Non lymphoma
SCLC, Melanoma
Brain tumors
CURES: testicular tumor
Ovarian cancer
Also: SCLC & bladder CA

Neurotoxic & leukemia
Contraindx: EtOH/Drugs
Ototoxicity
Nephrotoxicity
Electrolyte disturbances
Nausea/diarrhea/fatigue
Neurotoxicity (glutathione helps)
GI
Nephro & Hepatotoxicity
Forms platinum-DNA cross-links

DNA synthesis
Colorectal cancer (malig.)

Ovarian cancer (adv.)
Inhibits DHFR thymidylate,

purines, methionine, serine
CURES: osteosarcoma &

choriocarcinoma
ALL, Burkitt's, Non-H, Blad
Converted to 6-MPRP by HGPRT

purine synthesis
ALL

6-MP can gout (give Allopurinol)
Unnatureal purine incorporated into

DNA & RNA synthesis & function
Leukemia
Converted to 5FdUMP
thymidylate synthetase
TMP DNA synthesis
Breast cancer
Colorectal cancer
Basal cell carcinoma

GI
Mod: Cispt/IFN/Luke/MTX/PALA/Uridine
Converted to AraCTP incoporated

into DNA terminates elongation
Acute leukemia
(w/6-TG)
Drinking, driving, & drugs

don't mix!
Testes & ovaries are
precious, & platinum is a
precious metal!
CRC: w/5-FU & Leucovorin
Ovary C: w/Cisplatin & Paclitaxel
Good for ovaries & your

o-ring
Develops resistance via DHFR ,

transport, MPs
Also treats RA & psoriasis
Luke to the rescue

(meth lab)!
Thiopurine methyltransferase
mutation 6-MP metabolism
MP controls ALL
Converted to nucleotide inhibits

PRPP amidotrx DNA synthesis
Pentostatin
5-Fluorouracil
Cytarabine
Gemcitabine
Converted to dFdCTP incorporated Pancreatic cancer (1st line)

into DNA terminates elongation
Non-SC lung cancer
Vincristine
Vinblastine
Binds tubulin to polymerization into

microtubules
Vinorelbine
Antimitotics
Tall lean cyclist has bladder

problems & needs a mens
room!
Busulfan
Inhibits DNA/RNA/protein synthesis
Paclitaxel
ALL (1st line)

Hodgkin/Non-H lymphoma
Acute myelo leukemia
CURES: testicular tumor
Choriocarcinoma

Flu-like syndrome
Elevated liver enzymes (transaminases)
Patients on Cimetidine have

survival rate
Not S-phase specific

Vinocristine = treats
children
Vinocristine = Christ PN
Peripheral neuropathy
Vinoblastine = bone marrow

supp.
Non-SC lung cancer (adv.)

Breast cancer (adv.)
Promotes microtubule formation &
stabilizes the polymer
Etoposide
Teniposide
Inhibit topoisomerase II
DNA replication
Ovarian cancer (met.)

Breast cancer (met.)
Testicular cancer
Prostate cancer
Oat cell lung cancer
Vinorelbine = bone marrow

supp.
Neutropenia (give G-CSF)
Hypersensitivity (give
dexameth/diphen/H2)
Abraxane = albumin-bound Taxol

(give doses)
Etoposide = topoisomerase
II
Teniposide =
topoisomerase II
Teniposide = ten year-olds
Topotecan =
topoisomerase I
Both "tecans" do the same
ALL
Topotecan
Irinotecan
Actinomycin D
Inhibit topoisomerase I
DNA replication
Doxorubicin
Daunorubicin
Antibiotics
Mnemonic
Intercalates between GC bp binds

DNA DNA/RNA synthesis
Colorectal cancer (met.)

Ovarian cancer (met.)
Alopecia & skin bronzing & cholinergic sx
SC lung cancer (adv.)
Nausea/vomiting/diarrhea/mucositis
CURES: Wilm's tumor
& rhabdomyosarcoma
MTX-res. Choriocarcinoma
Myeloma
Sarcoma
Lymphoma
Alopecia
Acute leukemia
Cardiotoxicity
Flat ring structure
Of the Rubicin sisters, Epi is

less likely to break your
heart (she is "above"
that.Epi)!
Epirubicin
Plicamycin
Bleomycin
Inhibits RNA synthesis
Bone cancer (met.)
Glycopeptides that bind DNA

produce free radicals strand breaks
Inhibits DNA ligase DNA repair
CURES: testicular cancer

Squamous carcinoma
Lymphoma
Cervical cancer
GI cancer (stomach/anus)
Lung cancer
Mitomycin
Cross-links DNA DNA synthesis

Hepatotoxicity
Nephrotoxicity
Specific to osteoclasts
[Ca2+] in hypercalcemic
patients
Pneumonitis & Pulmonary fibrosis

Hyperpigmentation, alopecia, stomatitis
Bleomycin = DNA breaks

Least myelosuppressive
activity

Nephrotoxicity
Interstitial pneumonia
Mighty Mitomycin is the one

treating cervical cancer!
Protea
some
Inhib.
Tyrosine Kinase Inhibitors Miscellaneous
Drug
L-asparaginase
Tretinoin
Gefitinib
Specialty Antibodies
Metabolizes L-asparagine required by

tumor cells with asparagine
synthetase
ALL
Stimulate transcription of retinoic acid

receptor genes
CURES: Prostate cancer

Leukemia
Binds to Bcr-Abl kinase activity
CML
Nausea, diarrhea, edema, cramps, rash

Neutropenia, thrombocytopenia
Inhibits EGFR tyrosine kinase

cell proliferation & survival
Non-SC lung cancer
(Well tolerated!)
Diarrhea, acne-like rash
Inhibits VEGFR & PDGFR kinase
RCC (adv.)
GI stromal tumors
Fatigue, anorexia
Nausea, diarrhea, mucositis, stomatitis
Inhibits cell surface & intracellular

kinases
RCC (adv.)
Fatigue, diarrhea, dermatologic

Hypertension, neutropenia, bleeding
Reversible 26S proteasome inhibitor

activation of NFB
Multiple myeloma
Antibody that blocks (amplified)

HER2/neu receptor growth signal
Breast cancer (met.)
Antibody that blocks CD20 antigen on

B-cells B-cells in blood
Non-H B-cell lymphoma
Fever & chills

Nausea w/first infusion
Does not deplete stem cells

(which lack CD20)
Ritu has 20 CD's which will

be selled.
Antibody that blocks (amplified)

EGF receptor growth signal
Colorectal cancer
Acne-like skin rash
EGFR is overexpressed in
colorectal cancer
Can see (C) Colorectal

cancer in situ (Cetu)
Colorectal cancer (met.)
Nausea, constipation, GI bleed, abd. pain

Hypertension, wound healing
In combo w/ 5-FU & leucovorin
The color of a very good

beverage
Antiviral activity
Harry interferes and should

mellow out.
Sunitinib
Sorafenib
Bortezomib
Rituximab
Cetuximab
Bevacizumab
Interferons
Biological Response
Modifiers
Treats
Imatinib mesylate
Trastuzumab
Interleukin-2
G-CSF
GM-CSF
Diethylstilbesterol
Ethinyl Estradiol
Tamoxifen
Toremifene
Fulvestrant
Aminoglutethimide
Hormones
MOA
Antibody that blocks VEGF prevents

binding to endothelium
angiogenesis
1) Stim. 5-oligoadenylate synthetase
2) c-myc
3) protein synthesis
4) Activates nuclease degrades dsRNA
Prednisone
Leuprolide
Goserelin
Flutamide
Hypersensitivity, hyperglycemia,
Coagulation defects, hypoalbuminemia
due to normal protein
Nasty drug.retinoic acid syndrome:
fever, wt gain, SOB, heart, photosens.,
skin, hearing, diarrhea, liver enzymes,
Nausea, diarrhea, anorexia, fever, weak

Neuropathy, neutropenia,
thrombocytopenia
Fever & chills
Cardiotoxic (if given w/Adriamycin)
Respiratory problems

Fever & chills
Neurotoxicity
Nausea, diarrhea, fever, liver function
Anemia, hypotension, edema, arrhythmia
Thrombocytopenia
Mnemonic
Sometimes interferes w/other

drugs activity
ALL disparaging
Can become resistant

[Warfarin]
Itraconz & Erythro [IM]
Phenytoin [IM]
EGFR mutations correlate with
drug's efficacy
Works best in Asian nonKetoconz [Sunitinib]
Rifampin [Sunitinib]
Sunni are vegetarians &

pretty darn good
HER2/neu is overexpressed in Adam Trask's wife broke his

breast cancer
heart with her new pistol
Melanoma (malig.)
RCC
Induce neutrophil & granulocyte

precursor formation
Chemotherapy-induced
neutropenia
Bone pain
Rescue bone marrow graft failure

Speed bone marrow graft recovery
Bone marrow
transplantation
Fever
Bone pain
Block production of LH
testosterone
Prostate cancer (met.)
Hypercalcemia
Vaginal carcinomas in offsprings
Binds ER estrogen antagonist

Depletes ER, EGF, IGF-1
Breast cancer
(Post-men; in ER+ tumors)
Nausea, hot flash, rash, vag bleed, Ca

May cause endometrial cancer
osteoporosis
serum & LDL cholesterol
apolipoprotein A1
Binds ER prevents dimerization
Breast cancer
(Pre-men; in ER+ tumors)
Nausea, hot flashes, pain, headaches
Indicated for pre-menopausal

breast cancer
Inhibits aromatase & desmolase

estradiol
Breast cancer
CNS depression
(drowsiness, blurry vision, ataxia)
Breast cancer
GI, weakness, headaches, bone/back

pain
Breast cancer
Nausea
Musculoskeletal pain
Converted to prednisolone binds

receptor
ALL, CLL
Breast cancer
Cushing's syndrome
Immunosuppression
LHRH analog that initially FSH & LH

secretion desensitization FSH &
LH testosterone/estrogen
Prostate cancer
Sexual dysfunction
Converted to dihydroxyflutamide
blocks DHT binding to receptors
Prostate cancer
GI distress
Inhibits aromatase estradiol
Asian non-smokers Get fit

without lung cancer
My llama is a bore, I've had

enough (NF)!
Induce T-cell response kill tumor

cells
Anastrozole
Letrozole
Hairy cell leukemia

Kaposi's sarcoma
Melanoma (malig.)
Toxicity
Doesn't treat cancer
Prostate cancer is still the

best.
The breast way to treat

Post-menopause women
Tammy, Ethyl, Anna, and
produce estrogen in adrenal
Lenny is by aromatherapy.
cortex.. Medical
Reduced incidence of blood clots
& vaginal bleeding compared to
Tamoxifen
ALL pretty girls should get

phone CaLLs
Transient flare w/initial dose
(give flutamide)
A goose named Lou was

sick with the flu, but still
showed flare at the pro state
Dwight (DHT) plays the
flute but he's still a man
Drug
Metabolism
Toxicity
What makes it unique
Dopamine agonist ( DA)

L-DOPA (AADC) DA
DA in striatum
C-DOPA: peripheral AADC
L-DOPA DA (AADC)
DA (MAO-B, DBH, COMT)
Periph: N/V, OH, arrhythmia

CNS: On-off, wear-off, dyskin
Psych: hallucin, delusion, sleep
Peak-Dose: grimace/writhe
Neuroleptic malignant syndrome
SNS tone peripherally

N/V/anorexia via CTZ stimulation
Tubero-infund DA prolactin
Dopamine agonist
Bromocriptine
Pergolide
B: D2 agonist / D1 antagonist
P: D2 agonist / D1 agonist
Used in "frozen" cases

(Reverses "off" state)
Advanced PD on dose L-DOPA
B: short half-life
P: better w/L-DOPA (D1 & lipophilic)
Nausea, somnolence, dry mouth, edema,

insomnia, postural/OH
Peak-dose, on-off,
depr., anxiety, hallucinations
Bromo only works in L-DOPA Pergolide

allows L-DOPA dose
D2 agonist
Reduce on-off in late PD

Pramipexole can delay L-DOPA by 2
years
Selegiline
Deprenyl
Inhibits MAO-B striatal DA
Used when L-DOPA effects are starting to

decline
Anticholinergic
Apomorphine
Treats
Amantadine
Treats influenza A & hepatits C

May: alter DA release/reuptake
Block NMDA receptors
Block mACh receptors
COMT
Inhibitors
Dopamine Agonists
Levodopa
Carbidopa
Mechanism
Tolcapone
Entacapone
Inhibits COMT DA in cleft
Anti
Anti
Psychotics Depressant
MAO
Inhibitors
Pramipexole
Ropinirole
Produce 2x in bioavailability & half-life

of L-DOPA
Tolcapone: fatal hepatoxicity
No effect on tremor
Competes w/L-DOPA BBB

cause "wear-off" / "on-off"
May
SSRI
Block 5-HT reuptake
Anxiolytics
Fatigue, restlessness, hyperexcitability,

tardive dyskinesia
Huntington's Disease
Butyrophenone
Block DA receptors (D2)
Help with tics
Phenothiazine
Reserpine
Clonidine
Guanfacine
Miscellaneous
Restlessness, agitation, insomnia,

confusion, hallucinations, OH
Parkinson's Disease
Antipsychotics
Bromocriptine
Primidone
Baclofen
Riluzole
Deplete DA vesicles chorea
Hypotension, depression, sedation, GI
2 agonists
Tachycardia, sweating, restlessness
Don't w/d suddenly

Improve tics in 50% of children
Tourette's Syndrome
Block DA receptors (D2)

Some 5-HT receptor block
Neuroleptic malignant syndrome
dose APD helps

Balancing DA agonist helps
Tardive Dyskinesia
Anticonvulsant
Abuse potential
Congener of phenobarbital
Benign Essential Tremor
GABA-B receptor agonist
Drowsiness, loss of coordination,

confusion, nausea, seizures
Prolong time before tracheostomy
Amyotrophic Lateral
Sclerosis
Reduces glutamate release
Dizziness, GI, pain, diarrhea, weakness
Miscellaneous
Generalized
Seizures
Partial & Generalized Tonic-Clonic Seizures
Drug
Mechanism
Metabolism
Toxicity
Treats
Phenytoin
Block Na+ channel

(prolong inactive state)
Admin: oral / IV (status epilepticus)

90% protein bound
First order (low) Zero order (high)
Displaced by other protein-bound Rx
Acute: nystagmus, diplopia, ataxia, GI, conf.

Chronic: Gingival hyperplasia, hirsutism,
osteomalacia, rash, agranulocytosis,
megaloblastic anemia
High IV: arrhythmia, CNS depression
Congeners (mepheny/etho-toin) more toxic

Phenacemide very toxic (refractory partial)
Fosphenytoin = more soluble (injection)
BC effectiveness & birth defects
Partial seizures
Gen. tonic-clonic seizures
Status epilepticus
(not absence)
Carbamazepine
Block Na+ channel

Enhance GABA activity
Induces liver microsomes

Produces active 10,11 epoxide metabolite
Acute: stupor, coma, convulsions, irritability

Chronic: diplopia, ataxia, GI, sedation, fluid reten
Major: aplastic anemia, agranulocytosis
Accelerates metabolism: phenytoin,

primadone, ethosuximide, valproate, BC
Congener (oxcarb) less toxic, less potent
Partial seizures
Trigeminal neuralgia
Bipolar Disorder
(not absence)
Sedation, ataxia, respiratory depression, rash,

nystagmus, porphyria, tolerance, withdrawal
Congeners (mephobarbital & primidone)
Partial seizures
(not absence)
Block Na+ channel

May block Ca2+ channel
Headache, diplopia, rash, nausea, dizziness, ataxia
Life-threatening rash in 1-2% of patients
Partial seizures
Generalized seizures
Absence seizures
Myoclonic seizures
Felbamate
NMDA antagonist
Enhance GABA
Aplastic anemia
Severe hepatitis
Gabapentin
GABA analog
( release of GABA?)
Topiramate
Block Na+ channel

Enhance GABA activity
Tiagabine
GABA reuptake inhibitor
Pregabalin
GABA analog
Phenobarbital
Vigabatrin
Lamotrigine
Block Na+ channel

Prolongs GABA-A channel activity
Block AMPA receptor
Enhance GABA
Ethosuximide
Block T-type Ca2+ channel ( threshold)

rhythmic thalamic activity
Valproic Acid
Block Na+ channel

GABA ( GAD) GABA-T activity
Block T-type Ca2+ channel
Renal excretion of unchanged drug
Somnolence, dizziness, ataxia
No liver involvement!
Partial seizures
Neuropathic pain
Alcoholism
Somnolence, dizziness, fatigue, cognitive slowing,

weight loss
Used for weight loss
Partial seizures
Can produce euphoria

Neuropathic pain: post-herpetic neuralgia &
diabetic neuropathy
Partial seizures
Neuropathic pain
Phensuximide & methsuximide not as good
Absence seizures
Preferred over ethosuximide if absence +

generalized tonic-clonic seizures
Absence seizures
Myoclonic seizures
Atonic seizures
Partial seizures
Good absorption orally (stomach irritation)

GI, lethargy, fatigue, rash, bone marrow suppression
75% liver metabolized
Well absorbed
90% protein bound
Liver metabolized
Nausea, vomiting, GI, hepatotoxicity, birth defects,

Sedation (w/phenobarbital)
Diazepam
Clonazepam
Partial seizures
(poorly controlled)
Status epilepticus
Sedation, tolerance, withdrawal
Absence seizures
Myoclonic seizures
Infantile spasms
Drug
Mechanism
Alprazolam
Chlordiazepoxide
Benzodiazepines
Oxazepam
Lorazepam
Bind 12 on GABA-A receptor

GABA binding freq.
Cl- conductance
neuron hyperpolarizaiton
neuron activity
~
Anxiolytic-sedative
Hypnotic
Anesthesia
Anticonvulsant
Muscle relaxation
Alcohol withdrawal
Anxiolytics
(Non-Benzo/Non-Barb)
Barbiturates
Anxiety
Alcohol withdrawal
Rapidly absorbed
Long acting
Slowly absorbed
Short acting
Slowly absorbed
Short acting
Midazolam
Steep dose-response curve

Short acting
Water soluble
Meprobamate
Carisiprodol
Slowly developing anxiolysis
Acts just like Benzos (BZ-1) but

structually unrelated
Short acting
Long acting
Thiopental
Methohexital
Ultra short acting
Act at GABA-A receptor prolong

Cl channel opening inhibition
Phenobarbital
Ramelteon
Don't induce their own metabolism

(MDOS)
Difficult to produce respiratory arrest
alone
~
King Midas and Lora found a tricolor ox on their short trip to the
Alps
~
Flur Diaz longed to be a clown
Anxiety
Status epilepticus
Anxiety
Anxiety
Insomnia
Status epilepticus
Palpitations, tachycardia
GI distress
Miosis, BP
No sedation, dependence, abuse,

W/D, amnesia, CNS interx, motor
(w/MAOIs)
Generalized anxiety D/O

Anxiety w/MDD
Muscle relaxant
Short acting
Eszoplicone
Pentobarbital
Secobarbital
Insomnia
Propanediols indistinguishable from barbiturates in their drawbacks
Zolpidem
Zaleplon
REM suppression
REM rebound upon W/D
Tolerance
~
Sedation, lethargy, fatigue, mental
clouding, fine motor incoord, ataxia,
W/D, convulsions
~
Physio/Psycho dependence
~
Anterograde amnesia
Paradoxical hostility
~
Toxicity reversed by flumazenil
-BZ-1 & BZ-2 antagonist
-Not effective w/other agents
-Short acting
-Must be given IV
Long acting
?: 5-HT1A or DA receptor
Major metabolite blocks 2
(Not GABA receptor)
Treats
Rapidly absorbed
Short acting
Long acting
Buspirone
Anxiety
Depression
Flurazepam
Clonazepam
Toxicity
Short acting
Rapidly absorbed
Short acting (very )
Triazolam
Diazepam
Metabolism
Short-intermediate acting
Long acting
Melatonin-1 & 2 agonist

sleep onset
Bizarre night-time behavior

Less SE than benzos/barbs
Reversed by flumazenil
Induce own metabolism (MDOS)

Excessive sedation, confusion,
lethargy, motor incoordination
Tolerance
Phys/Psych dependence W/D
Respiratory arrest
ALA synthase AIP
Get some ZZZ's.

E-long-ate
Insomnia
Thio huxtable was ultra short
Anesthesia adjuct
Drugs of abuse
Fennel seeds are long
Anticonvulsant
Insomnia
(sleep onset problems)
Atypical Antipsychotics
Typical
Antipsychotics
Drug
Chlorpromazine
Haloperidol
Fluphenazine
Clozapine
Metabolism
Toxicity
Treats
Blocks: 1=5-HT2A > D2

mAChR, histamine receptors
High dose, low potency

Liver metabolized
Interax: produce sedation
DA: EPS, prolactin, wt gain

mACh: "anti-cholinergic effects"
1: orthostatic hypotension
Jaundice, photosensitivity,
Parkinsonism, NMS, TD
Blocks: D2 > 5HT2A
Low dose, high potency
Less CV & anti-cholinergic effects
IM preparation
Schizophrenia
Schizoaffective D/O
Bipolar D/O
Mania
Tourette's syndrome
Ortho hypotension, ~EPS

seizure threshold
Agranulocytosis
Causes sialorrhea
Have to keep their mouth clozed
Blocks: D4=1 > 5-HT2A > D2

Weak agonist at M4 ACh receptor
Risperidone
Blocks: 5-HT2A > D2

(potent @ D2looks typical)
Olanzapine
Blocks: 5-HT2A > D2 >
Low doses EPS

Therapeutic doses EPS &
prolactin
DA: EPS, prolactin, wt gain
Weight gain prominent

(Metabolic syndrome)
Especially good for negative SX of

schizophrenia
Schizophrenia
Schizoaffective D/O
Bipolar D/O
Mania
Tourette's syndrome
Less SE's
Aripiprazole
Lithium
Mood Stabilizers
Mechanism
Partial agonist at: D2 & 5-HT2A

Na+ or Mg2+ replacement
IP3/DAG, cAMP
NT release
Valproic Acid
Anti-convulsant
Block Na+, enhance GABA
Carbamazepine
Lamotrigine
Anti-convulsant
Block Na+
Clonazepam
Benzodiazepine
Minimal or no weight gain

Oral absorption
Kidney excretion ( in preggo)
Narrow therapeutic window
Acute: fatigue, weakness, tremor

Chronic: thyroid, diabetes insipidus,
nephritis, edema
Only drug that suicide

Breast milk (Ebstein anomaly)
dietary sodium can effect
Mania
Used for early mania

Used as lithium adjunct
Sedation, GI
Hepatotoxicity
Birth defects
As effective as lithium in early mania
Mania
(early)
Use anti-convulsant dose

Used if lithium inadequate
Diplopia, ataxia, GI
Aplastic anemia, birth defects
Agranulocytosis
Mania
Used as lithium adjunct

Sedation
Amnesia
Abuse, dependence
Miscellaneous
MAO Inhibitors
SSRIs
2nd & 3rd Generation
Tricycic Antidepressants
Drug
Mechanism
Metabolism
Imipramine
Inhibits NE & 5-HT reuptake

Blocks: 1, mAChR, histamine
Metabolized to desipramine
Amitriptyline

(5-HT>NE)
Blocks: 1, mAChR, histamine
Metabolized to nortriptyline
Desipramine
Inhibits NE reuptake
Nortriptyline

(NE>5-HT)
Buproprion
Inhibits DA reuptake (?)
CV SE's
sexual complications
seizure threshold
Venlafaxine
CV SE's
BP
Trazodone
Nefazodone
Phenelzine
Tranylcypromine
Moclobemide
St. John's Wort
Sedation
Orthostasis
Cardiotoxicity
Anti-cholinergic effects
Hypomania
Rash, photosensitivity
seizure threshold
1: hypotension reflex SNS
Tachycardia
Arrhythmia
Angina, infarct
Suicide
Impotence
Trazodone: Sedation (in a tranz)

Nefazodone: Hypnotic
Fluoxetine
Sertraline
Paroxetine
Fluvoxamine
Toxicity
Inhibition of 5-HT reuptake
Long acting
Active metabolite
Inhibits P450 system
Shorter acting (than fluox)
No active metabolites (like fluox)
No inhibition of P450 system
Irreversibly inhibit MAO-A & B

NE & 5-HT & DA
Inhibit SIF ganglion cells BP

Headache
Sexual dysfunction
Hypertension/hypotension
Reversibly inhibit MAO-A

NE & 5-HT
Partially inhibit NE & 5-HT reuptake
Bind GABA receptors
Akathisia
Behaviorally activating
Nervousness, insomnia, N/V
Headache, anorgasmia
Suicide
MAOI Interax: serotonin syndrome
Interax: levels ofcyclosporine,

warfarin, indinavir, digoxin,
amitriptyline
Photosensitivity
Induces liver enzymes
Treats
Pronounced anti-ACh visual effects:

mydriasis & accom.
Depression
~
Enuresis
(anti-ACh)
Pain
ADHD
Sudden death in children
Psychomotor activation
Depression
Nicotine withdrawal
Depression
Trazodone can cause priapism &

orgasms w/yawning
food intake weight loss
Interax: tyramine-containing foods

hypertensive crisis
~
Mood elevations in depressed &
normal individuals
Depression
(Nef>Traz)
Depression
OCD
Bulimia
Depression
Narcolepsy
Phobia anxiety D/O
OCD
Depression?
Substance P
antagonist
Needs confirmation
Depression?
Mifepristone
Glucocorticoid receptor antagonist
Psychotic major
depression
Alcoholism Treatment
Drug
Mechanism
Metabolism
Toxicity
Disulfiram
Irreversibly inhibit ALDH

acetaldehyde
Converted to active metabolites

(which inhibit ALDH)
Acetaldehyde syndrome
alcohol flush reaction
Naltrexone
Opiate OR antagonist
Blocks alcohol reinforcement
Acamprosate
Topiramate
Tiapride
Toxic Alcohols
Ondansetron
Methanol
Ethylene glycol
Interacts with NMDA & GABA-A

receptors
Treats
Reduces craving
Reduces relapse rates by 50%
Reduces hyperexcitability during
withdrawal
Taurine derivative
Alcoholism
Facilitates GABA-A function

Blocks AMPA & kainate receptors
D2 dopamine antagonist
Alcoholism
(early-onset)
5-HT effects
Methanol ADH formaldehyde

ALDH formic acid
Headache, vertigo, vomiting,

abd/back pain, dyspnea, met.
Acidosis, coma, resp. failure
Can cause blindness (15mL)
Toxic
Ethgly ADH glycoaldehyde

ALDH glycolic acid
glyoxylic & oxalic acid
Metabolic acidosis
Renal failure (oxalate deposits)
Treat with EtOH

Treat w/fomepizole: ADH inhibitor
Antifreeze
Mixed Opioid
Agonist-Antagonists
Moderate Opioid
Agonists
Strong Opioid Agonists
Drug
Mechanism
Morphine
Fentanyl
Su & Alfentanil
Toxicity
Treats
30% absorbed in gut

90% first pass metabolism
Analgesia, sedation, euphoria,

dysphoria, miosis, N/V, OH,
resp. & cough suppression
Pinpoint pupils = opioid OD

Constipation
Mod-severe pain
Myocardial infarction
Dyspnea, anxiety
80x morphine potency
Less nausea
Sufentanyl = fentanyl
Alfentanyl = fentanyl
Post-op pain
Anesthetic (w/droperidol)
Potent MOR agonist
Meperidine
1/5 morphine potency

1/4 morphine duration
No cough suppression
Less constipation
No labor prolongation
OB/Surg analgesia
Mod-severe pain
Methadone
Same potency as morphine

bioavailability than morphine
Long acting
No euphoria
Prevents W/D signs
Mod-severe pain
Opioid addiction
Metabolized in part to morphine

Excellent bioavailability
Codeine
Propoxyphene
Weaker MOR agonist
Given w/aspirin or acetaminophen
Pentazocine
Given w/naloxone IV to avoid

analgesic & euphoric effects
Butorphanol
30x pentazocine antagonism

20x pentazocine analgesia
KOR agonist
MOR antagonist
Same potency as morphine

5x pentazocine potency
Nalbuphine
Mild-moderate pain
Cough
Few SE
1/2 codeine potency

Given w/acetaminophen
Interax: alcohol/sedatives (fatal)
Oxycodone
Mild-moderate pain
Abuse
Combined w/tripelennamine
("T's & blues") heroin-like
Sedation (KOR)
Sweating, dizziness
Psychotomimetic effects
Anxiety, nausea, vomiting
Moderate pain
Mod-severe pain
(acute)
Less psychotomimetic effects
Less MOR antagonist activity
Mod-severe pain
Buprenorphine
Opioid
Antagonists
Metabolism
25-50x morphine potency (pain)
Naloxone
Fast onset
Competitive opioid antagonist
(MOR)
Naltrexone
Tramadol
Worse sedation & resp. depression

than morphine
Binds MOR w/high affinity
Weak MOR agonist

T-REX is bigger than an OX, and a

T-REX is more orally active!
Precipitates opioid W/D
3-5x naloxone potency

Long acting
Orally active (moreso)
1/10 codeine MOR affinity
6000x less morphine MOR affinity
Opioid overdose
Opioid addiction
(highly motivated)
Less potential for abuse &
respiratory depression
Dual mechanism of action
Dental pain
Acute MSK pain
Cancer pain
Drug
Mechanism
General Anesthetics
(Inhalation)
Halothane
Enflurane
Nonspecific interactions w/ lipid bilayer

Block K+ channels hyperpolarization
Activate or facilitate GABA
Toxicity
Slow induction ( blood:gas)

Most potent (MAC)
Hepatotoxicity (free radicals)

Sensitizes myocardium to NE/EPI
cerebral blood flow
Halo = Heart
Intermediate induction
Intermediate potency
Fluranes (fluoride) can be nephrotoxic

minute volume
Muscle relaxation
Fluranes fluoride floppy

muscles
Isoflurane
Thiopental
Diazepam
Loraz/Midaz
Morphine
Fentanyl
Mnemonic
NO potency
Ultra short acting

Rapid onset, short anesthesia
Diffuses out of brain
May produce "hangover"

Myocardial/Respiratory depression
cerebral/renal blood flow, GFR
Benzodiazepines
Slower onset
Long acting
Prolonged post-op. recovery

Anterograde amnesia
High potency opioid
Can be reversed w/naloxone
Respiratory depression
Analgesic
Only anesthetic @ doses
Rapid onset
Rapid recovery
Anti-emetic
Respiratory depression
Hypotension
Most popular IV anesthetic
Be proper, don't puke
CV stimulation: HR, BP, CO

cerebral blood flow, ICP
Disorientation, illusions, vivid dreams
Analgesic
Amnesia
Catatonia
Ketamine = catatonic
Analgesia
Pt. can respond to commands
(no loss of consciousness)
Can talk to the patient from

behind the drape
Not analgesic
He tummy ache
Barbiturate
Propofol
Ketamine
Blocks NMDA receptors
Droperidol
Antipsychotic
Etomidate
Fast induction ( blood:gas)

Least potent (MAC)
Nitrous oxide
General Anesthetics (IV)
Metabolism
Given w/opioid (fentanyl)
Rapid onset
Rapid recovery
Nausea & vomiting

Pain
(Minimal CV/repspiratory Depression)
Thio huxtable is ultra short

Not analgesic
Local Anesthetics (Esters)
Drug
Cocaine
Procaine
Tetracaine
Benzocaine
Mechanism
Block V-G Na+ channels
in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
~
Quickly metabolized by PChE
Local Anesthetics
(Amides)
Lidocaine
Mepivacaine
Bupivacaine
Procainamide
Block V-G Na+ channels

in high frequency pain fibers
(spend lots of time "open")
~
Weak bases (pKa=8-9)
1) uncharged into axoplasm
2) ionized & trapped inside
3) binds open Na+ channel
Metabolism
Toxicity
Use
Absorb via mucous membranes

Topical use
CNS stimulation & euphoria (abuse)
Produces vasoconstriction
(All other LA's produce vasodilation)
Topical LA
Short acting
(metabolized by plasma ChE)
Given w/EPI
Aunt Ester had allergies

but she was a peach! (PChE)
Infiltration
Nerve block
Spinal anesthesia
More lipophilic than Pro/Coke:

Rapider onset, potenter
Longer acting
Most commonly used drug for Spinals
Spinal anesthesia
Topical LA
Poorly water soluble
So poorly water soluble that systemic toxicity

potential is zero.
Dusting powder
Ointment
(burns/ulcerations)
Used in ester-allergic individuals
LA
Cardiac arrhythmias
More lipophilic than Pro/Coke:

Rapider onset, potenter
(Intermediate) Longer acting
More lipophilic than Mep/Lido:
Long acting
Highly plasma protein bound
Drowsiness
Lassitude in neonate
Cardiotoxic
OB LA
Particularly long acting
(some nerve blocks last 24+ hrs!)
Analgesia + abdominal muscle control
Epidural anesthesia (OB)

Nerve blocks
Cardiac arrhythmias
Inflammatory Bowel Disease
Cyto
Protect
Mucosal
Protectants
Proton
Pump
Inhibitor
H2 Receptor Antagonists
Second Generation
First Generation
Degranulation
Inhibitors
Drug
Mechanism
Metabolism
Toxicity
Treats
Ineffective after asthma attack has started
Bronchial asthma
(prophylaxis)
Ineffective in bronchial asthma (mediated by

more than just ol' histamine)
Seasonal allergic rhinitis

Urticaria
Cromolyn Sodium
Inhibit immunologically triggered mast
cell degranulation
Nedocromil
Chlorpheniramine
Diphenhydramine
Promethazine
Terfenadine
Block H1 receptor histamine ax

Allergies
Motion sickness
Sedation
Antiparkinsonian effects
Anti-cholinergic effects
Anti-serotonergic effects
receptor blocking
Local anesthetic effects
Rapidly absorbed orally

Metabolized by CYP3A4
Strong sedation!
Ototoxicity
(newborns or ABX)
Drug interax: cardiotoxic w/ conazoles or
macrolides
Metabolized to fexofenadine (not cardiotoxic),

if CYP3A4 inhibited, terfenadine accumulates
Fexofenadine
Loratadine
Allergies
Motion sickness
Sedation
Allergies
Lower risk of arrhythmia
Block H1 receptor histamine ax
Long acting
Little to NO sedation
Cyproheptadine
No significant side effects
Allergies
Strong 5-HT blocking
Cimetidine
Ranitidine
Competitive inhibitor of histamine (H2)stimulated gastric HCl secretion
Famotidine
Inhibits P450 system

Drug interax: chlordiazepoxide, EtOH,
propranolol, theophylline, warfarin
Diarrhea, muscle pain

Headache, dizziness
Gynecomastia, impotence
4-10x more effective than cimetidine

Does not interfere with P450
Less side effects than cimetidine

No antiandrogenic effects
Not metabolized by P450
Nizatidine
Ci me, I ran ti dine with my family & my nizce
Gastric/duodenal ulcers
ZE syndrome
GERD
Don't use in renal disease
Don't use with salicylates
Active form irreversibly binds & inhibits

proton pump in parietal cells
Absorbed in alkaline SI pH
Use >2 months not advisable
Diarrhea, nausea
Dizziness, headache
Heals duodenal ulcers more rapidly than H2

blockers
ZE syndrome
GERD
Sucralfate
Aluminum salt of sucrose sulfate

binds plasma proteins in crater
protective barrier
Short acting
Drug interax: blocks tetracycline & PO4
absorption
Constipation
Nausea
Additionally: inhibits pepsin & bile aciton

Also: prostaglandin release
Duodenal ulcer
Colloidal bismuth
React w/proteins in acid medium

protective barrier in ulcer crater
Black stools, black tongue

Don't use in renal disease
May have ABX activity against H. pylori
Prostaglandin E1 analog H+
mucus & bicarbonate secretion
Nausea, diarrhea
Abortion in preggos
Omeprazole
Misoprostol
Sulfasalazine
Hydrocortisone
Azathioprine
Mercaptopurine
Bacteria split azo bond 5-ASA (&

sulfapyridine) inflammation
75% reaches colon

5-ASA = active metabolite
Sulfapyridine = SEs
Nausea, vomiting
Headache
Allergy
Can cause folate absorption
Corticosteroid inflammation
Ulcerative colitis (85%)

Colonic Crohn's Dz
Acute episodes
Ulcerative colitis
Crohn's disease
Cytotoxins
Low dose used for prophylaxis
Toxicity may limit chronic use
Cyclosporine
Infliximab
NSAID-induced damage
Used in nonresponsive cases

Severe refractory IBD
Monoclonal antibody against TNF-

inflammatory action
Single IV infusion remission
Nausea
Serum sickness
Infections, autoimmunity, cancer
Crohn's disease
Drug
Acyclovir
Valacyclovir
Ganciclovir
Valganciclovir
Herpes / Varicella / CMV
Famciclovir
Penciclovir
Guanine nucleoside analog

Viral thymidine kinase produces analog
binds viral DNA polymerase & inactivates
Guanine nucleoside analog

Inhibits viral DNA synthesis
Metabolism
Valacyclovir (rapidly) acyclovir
Famciclovir is a prodrug metabolized to

active penciclovir
Toxicity
Nausea, vomiting, diarrhea

Headache, renal dysfx
Resistance: altered/deficient viral

thymidine kinase or
viral DNA polymerase
Myelosuppression, neutropenia vision

disturbances, carcinogenic
CNS effects
More toxic than acyclovir
Inorganic pyrophosphate analog

Reversibly inhibits viral DNA & RNA polymerases
Nausea, fever, headaches, hypocalcemia,

hypomagnesemia, nephrotoxicity, anemia,
genital ulcer
Trifluridine
Pyrimidine analog
Cornea inflammation
Fomivirsen
Antisense oligonucleotide
Docosanol
Prevents viral fusion viral entry
Idoxuridine
Iodinated thymidine analog

Incorporated into viral & cellular DNA
susceptible to breaks & error in trx
Inhibits viral uncoating & blocks influenza A M2

protein ( dissociation of RNP complex in
replication)
Iritis, vitritis, intraocular pressure

Vision changes
CMVertables are fos

cars, cid so you ganci
the road fomi
CMV (retinitis)
HSV
(acyclovir resist.)
More toxic than gancyclovir
Tri flurting w/Kera's

tits & HSV
Don't give to patients who have taken

cidofovir in past month
CMV (retinitis)
(in HIV patients unresp)
For herpes, tri giving
acyclovir, doc (or
dox)!
Inhibits neuraminidase release of virus

viral aggregates & viral spread
Orally inhaled
Used once taily to prevent flu
Oseltamivir
HSV
(keratitis)
Reduces duration & severity of influenza
infection
90% of influenza is resistant!
Influenza A
Parkinson's disease
Nasal/throat discomfort, headache,

bronchospasm (asthmatics)
If taken within ~30 hrs of SX onset

duration & respiratory complications
Influenza A & B
Nausea, vomiting, headache
Viral Hepatitis Infection
Dexamethasone
Interferons
Croup
Inhibits viral reverse transcriptase

IFN & IFN bind cellular receptors activate JAKSTAT 2,5-oligoadenylate synthetase & kinase
protein syn
Imquimod
Nephrotoxicity
IM or SC injection
Ade for viruses

makes me hep B!
Flu-like symptoms, bone marrow

suppression, fatigue, infections, anorexia,
diarrhea, depr, anxiety
Hepatitis B
(chronic)
HPV
Hepatits B & C
Kaposi's sarcoma, MS
Renal dysfunction
Myopathy ( CK)
Tell bi he's a dead

hepatitis..
Hepatitis B
Synthetic guanosine nucleoside analog

Alters nucleotide pool viral mRNA syn
Conjunctiva irritation, wheezing, rash

Anemia, bone marrow suppression
Teratogenic
Ribavirin blocks RNA

of virin
Hepatitis C
RSV , Influenza, HIV
Parainflu, Paramyxo
Induces IFN & TNF

(and other cytokines)
Local erythema, flaking, itching

(topical)
I'm quiet about warts
HPV
Telbivudine
Ribavirin
HSV
Metabolized by liver
Zanamivir
Adefovir
HSV
(Keratoconjunctivitis)
(Epithelial keratitis)
CMV (retinitis)
Pain, inflammation, edema

of eyes or eyelids
Anorexia, nausea, peripheral edema
CNS effects
(in renal failure dz)
CMV
(retinitis)
Acute herpes zoster
Only effective if given at first symptoms

(ineffective at papule stage)
Metabolized by kidney
Treats
HSV
VZV
Nephrotoxicity, neutropenia, metabolic

acidosis
Cidofovir
Rimantadine
Mnemonic
Nausea, diarrhea
Headache
Tumors, testicular toxicity
Foscarnet
Amantadine
Viral Respiratory Infections
Mechanism
Drug
Mechanism
Metabolism
Toxicity
Converted via human thymidine kinase AZT-TP

incorporated into viral DNA terminates chain
elongation
toxicity w: probenecid, tylenol,

lorazepam, indomethacin, cimetidine
Anemia, leukopenia, headaches, lactic

acidosis, hepatic steatosis, lipoatropy,
central fat, lipids
Protects fetuses from infection

Resistance: mutated RT w/ affinity for
AZT-TP
Didanosine
Orally in buffered tablets

toxicity w: stavudine
Pancreatitis, peripheral neuropathy
Zalcitabine
Given w/AZT or alone

(if can't tolerate AZT)
Stomatitis, peripheral neuropathy, rash
Non-Nucleoside
RT Inhibitors
Nucleoside Reverse Transcriptase Inhibitors
Zidovudine
Mnemonic
Treats
HIV
HIV
(AZT resistant)
Resistance: mutated RT
Peripheral neuropathy
Lactic acidosis, hepatic steatosis,
lipoatropy, central fat, lipids
Stavudine
Lamivudine
Inhibits viral reverse transcriptase terminates

DNA chain elongation
Pancreatitis (pediatric patients)
Emtricitabine
HIV
Zitty Zal went nuclear

& did stab a baby
lamb he tends.
Resistance to AZT develops more slowly
if you add lamivudine
HIV
HIV
Hepatitis B
Hyperpigmentation
Abacavir
Given w/AZT or Lamivudine or

protease inhibitor
Hypersensitivity, fever, GI, malaise, rash
HIV
Tenofovir
Do not give w/didanosine, lamivudine,

abacavir
Flatulence
Renal toxicity
HIV
Hepatitis B
Efavirenz
Given w/AZT & lamivudine
Dizziness, headache, insomnia, rash

Nightmares, hallucinations
Given w/AZT & didanosine

Least potent
Rash
Given w/didanosine & stavudine
Rash, fever, nausea, hepatotoxicity
Delavirdine
Binds next to RT activation site change

conformation inhibit RT activity
Nevirapine
[phenobarb, phenytoin, carbmzpne,

methadone, rifabutin]
Rifampin efav
[rifampin, rigabutin, ergot, triazolam,
midazolam, cisapride]
Efavirenz Rx & SJW dela
[rifampin, ketoconazole, ethinyl
estradiol (BC)]
SJW nevir
Never ever tell a nun

a lie.
HIV
Nel is a LIAR. She is

a professional tease
and will inhibit or slow
your fost progress
HIV
Binds enfulope
HIV
Indinavir
Diarrhea, nausea, vomiting, lipodystrophy,
hyperglycemia
Protease Inhibitors
Saquinavir
SJW lowers concentration
Ritonavir
Diarrhea, nausea, fatigue, headache,

hyperlipidemia, hyperglycemia, altered
body fat
Lopinavir
Administered together:
Ritonavir inhibits CYP3A4
Lopinavir
Interferes w/proteolysis of gag-pol viral protein

precursor nonfunctional virions
Nelfinavir
Inhibits CYP34A (Rx toxicity)
Rifampin induces CYP3A4
Amprenavir
Diarrhea, nausea, vomiting, lipodystrophy,

hyperglycemia
Although HIV cross-resistance occurs,

most likely to still be Amprenavir
susceptible
Atazanavir
Fusion
Inh.
Fosamprenavir
Enfuvirtide
Binds viral envelope glycoprotein to prevent

conformational change when binding host cell
membrane
Pain, erythema, nodules, cysts

(at injection site)
Injected twice a day
Metabolism
Toxicity
Treats
Quinidine
Blocks V-G Na+ channels

& K+ channels
Blocks -adren. & vagus
automaticity, prolonged QT, widened

QRS, SA & AV node conduction velocity
GI, hepatic granulomas, torsades, ventricular

rate w/A flutter, cinchonism, lupus-like
syndrome
Can cause paradoxical in heart rate in

atrial flutter
Chronic SVT
Procainamide
Blocks V-G Na+ channels

& K+ channels
(no ANS effects)
automaticity
refractory period
conduction velocity
GI, hypotension, torsades,

heart block, agranulocytosis, lupus-like
syndrome
Converted to active metabolite NAPA

no Na+ channel activity but blocks K+
channels
Ventricular tachycardia
SVT
IV use only ( first pass metab)

automaticity, action potential,
conduction velocity
Seizures
Nystagmus, tremor, dysarthria, altered
sernsorium
Same, but orally effective
Nausea, tremor, CNS effects
Lidocaine
Flecainide
Blocks Na+ channels

Blocks K+ channels
Blocks Ca2+ channels
Propafenone
Blocks Na+ channels

Blocks K+ channels
Blocks -adrenergic
Class II - Blockers
Class 1B
Na+ blocker
(Rapid )
Mechanism
Class 1C
Na+ blocker
(Very long )
Class 1A
Na+ blocker
(Intermediate )
Drug
Blocks Na+ channels, gK in fast

fibers during phase 3 & 4
Mexiletine
Propranolol
Non-selective blocker
Na+ blocker at dose
(membrane stabilization)
Metoprolol
1 blocker
Carvedilol
blocker
Proarrhythmic (after MI)

Exacerbate CHF by LV fxn
Heart block (in AV node dz), torsades
AV conduction velocity, prolonged PR,

automaticity in ectopic foci
Amiodarone
Atrial arrhythmia
(if no other strx disease)
Bradycardia & bronchospasm ( block)
Atrial arrhythmia
Antioxidant properties
Atrial flutter
Atrial fibrilliation
Ventricular arrhythmia (post-MI)
Angina
Myocardial depression, heart block,

bronchospasm, insulin hypoglycemia,
depression, rebound SNS if w/d
Intrinsic SNS activity, but no membrane

stabilizing effects
Less polar less CNS effects
Longer acting
Used IV when immediate block is needed

Cleared quickly
Esmolol
Class IV Miscellaneous Ca2+ channel Class III - K+ channel blockers
blockers
conduction velocity, widened QRS,

action potential,
prolonged QT, prolonged PR
Lupus-like syndrome
1 blocker
Orally active
Proarrhythmic (after MI)

Exacerbate CHF by LV fxn
Heart block (in AV node dz)
Acebutolol
Atenolol
Ventricular fibrillation
Blocks K+ channels
Blocks Na+ & Ca2+ channels
Non-competitive SNS blocker
Prolonged QT, automaticity,

conduction velocity,
widened QRS, prolonged PR
Corneal deposits (100%), liver dz, hypo &

hyperthyroidism, pulmonary fibrosis,
vasodilation, photosensitivity/skin color
First line agent in ACLS code

Active metabolite: desethyl-amio
Atrial tachycardia
Sotalol
Blocks K+ channels
action potential, automaticity,

conduction velocity (AV only), prolongs
AV refractory period
Torsades (especially in hypokalemia)

blocker SE's
Ibutilide
Blocks K+ channels
IV use only
Delays repolarization,
action potential
Torsades
Contraindicated in hypokalemia
IV use only
Atrial arrhythmias
(acute)
Blocks K+ channels
(rapid delayed rectifier K+ current)
Greater effect on atria than ventricles
Torsades
Rx Interax: [Dofetilide]
Interfere w/cation trx in kidney, prolong QT
interval, use liver metab.
Atrial arrhythmias
(chronic)
Blocks L-type Ca2+ channels
HR, CX, conduction velocity (AV),

prolongs AV refractory period
Hypotension reflex tachy, neg. inotropy,

heart block (AV conduction dz), bradycardia
(SA conduction dz), GI
Dofetilide
Verapamil
Diltiazem
Digoxin
Adenosine
Direct: Blocks Na+/K+ ATPase

Indirect: vagal stimulation
CX ( Ca2+)
Vagal: atrial AP & AV refractory
Binds adenosine receptors opens

ACh-sens. K+ channels
(in
SA/AV/atria)
Shortens atrial AP, automaticity,

AV refractory period,
AV conduction velocity
Arrhythmias
Nausea
CNS effects
Transient: asystole, dyspnea, bronchoCX
Atrial fibrillation
Flushing
Renal excretion of unchanged drug

blocker w/Class III effects
Given orally but IV is better

More active L-isomer first pass met.
Less negative inotropic effects
(less CX)
Rx Interax: [Digoxin]
quinidine & verapamil
IV use only
Rx Interax: theophylline & caffeine block
adenosine receptors
Atrial arrhythmias
(chronic)
SVT
(acute or chronic)
SVT
(acute or chronic)
CHF ( CO)
Atrial tachycardia
Atrial fibrillation
Produce controlled hypotension
Miscellaneous
Inotropes
Digitalis
Glycosides
Drug
Toxicity
Treats
Fatigue, malaise, dizziness, confusion,

delirium, anorexia, N/V, abdominal pain,
color vision, halos, bradycardia, AV
block, ectopic beats, SA arrest,
ventricular arrhythmias, EKG changes
Aglycone portion = for cardiac activity

Monosaccharide chain = metab.
Eubacterium lentum in gut inactivates
Heart failure
Simulate 1 receptors CX
Dopamine: tachycardia, arrhymthia

Dobutamine: tolerance, vasodilation (via
2 receptors)
Dopamine vasodilates renal vasculature via

D1 receptors
Inhibits phosphodiesterase-III
vasodilation & CX
PDE-III selectively found in cardiac & smooth

muscle
Nausea, vomiting
Thrombocytopenia, liver damage
Arrhythmia
Does more harm than good when used longterm
Diuresis & peripheral vasodilation

cardiac workload
Short acting
Very potent
Hyponatremia, hypokalemia,
hypocalcemia, hypomagnesemia,
hypophosphatemia
Hyrdochlorothiazide
Chlorothiazide
Diuresis
Synergistic with loop diuretics
Hyponatremia, hypokalemia,
hypocalcemia, hypophosphatemia
Kidneys can adapt

Ineffective at GFR < 30 ml/min
Heart failure
(mild)
Spironolactone
Diuresis
Add to other diuretics

(to help w/diuresis & to spare K+)
Hyperkalemia, anti-androgenic effects

(gynecomastia)
Avoids K+ wasting
Heart failure
Digoxin
Digitoxin
Dopamine
Dobutamine
Amrinone
Diuretics
Furosemide
Bumetamide
Captopril
Enalapril
Lisinopril
Mechanism
Metabolism
Inhibit Na+/K+ ATPase binding

extracellularly on subunit
Prefers E1-P form stabilize to E2-P
form
Na & Mg favor binding
K favors release
25% plasma protein bound

Renal elimination
2 day half-life
>90% plasma protein bound
Hepatic elimination
7 day half-life
Venous & arterial vasodilation

preload & afterload
(+ bradykinin)
Vasodilators
Isosorbide dinitrate
Nitroglycerin
Isosorbide 5-mononitrate
Hydralazine
Carvedilol
Metoprolol
Bisoprolol
Verapamil
Diltiazem
Nifedipine
Metabolized to NO venous & arterial

vasodilation preload & afterload
Arterial vasodilation afterload

CX
renal dilation renal blood flow
Blocks receptors in heart counteracts May allow gradual up-regulation of receptors
SNS input to heart
to occur in the heart
Blocks L-type Ca2+ channel
vasodilation & HR & CX
Heart failure
Abrupt in BP w/first dose (vol dep)

Rash, loss of taste, cough
Sodium nitroprusside
Highly protein bound (~90%)

Liver metabolized
Heart failure
(serious)
Heart failure
Hypotension, coronary steal, angina,

cyanide toxicity, thiocyanate toxicity
Cyanide thiocyanate
(eliminated kidneys)
No tolerance (different NOS from NG)
Heart failure
Angina
Flushing, headache, hypotension, reflex

tachycardia,
Fast first pass metabolism

Tolerance develops rapidly
CHF (acute & chronic)

Vasospastic Angina
(w/Ca2+ blockers)
Hypotension
Reflex SNS activity
Heart failure
Myocardial depression, bronchoCX,

hypoglycemia, fatigue, depression,
impotence, rebound SNS if W/D
Heart failure
Worsening angina, worsening HF, heart

block (in AV dz), bradycardia,
hypotension, edema, resp, GI
Not helpful for systolic dysfx

Helpful for diastolic dysfx (cardiac filling)
Heart failure / HTN

Reentry arrhythmia
Angina (vasospastic/exer)
Carbonic
Anhydrase
Inhibitors
Drug
Acetazolamide
Dorzolamide
Mechanism
Metabolism
Toxicity
Inhibits CA in the PCT

Na & HCO3- reabsorption
Secreted into lumen via OA trx

Inhibits 85% of PCT HCO3 reabs
Inhibits 45% of total HCO3 reabs
Metabolic acidosis, renal CaPO4 stones,

hypokalemia, CNS, allergy
Contraind: cirrhosis (encephalopathy)
Inhibits CA in the eye
Topical application
Minimal

Eliminated via kidney
Loop Diuretics
Furosemide
Bumetanide
Inhibits Na+/K+/2Cl- trx in TAL

Na & K & 2Cl reabsorption
Shorter acting
50% liver elimination
(50% kidney elimination)
Longer acting
Faster absorption
80% liver elimination
Torasemide
Hyponatremia/dehydration
Hypocalcemia
Hypokalemia
Metabolic alkalosis
Hypomagnesemia
Hyperuricemia
Ototoxicity
Allergy
Thiazide Diuretics
Shorter acting
Inhibits NaCl cotrx in DCT

Na & Cl reabsorption
Potassium-Sparing Diuretics
Chlorthalidone
Hyponatremia/dehydration
Hypokalemia
Metabolic alkalosis
Hypercalcemia
Hyperglycemia
Hyperuricemia
Allergy
Weakness
Competitive aldosterone receptor in DCT &

CT in Na+ channels &
out K+ channels (Princ.)
Na+ reabsorption & K+ secretion

in Principal cells
H+ secretion Intercalated cells
Hyperkalemia, metabolic acidosis, gynecomastia,

impotence, libido, GI, CNS effects
Epoxy-spironolactone derivative
Blocks Na+ channels in Principal cells in

DT & CT
Na+ reabs & K+ secretion
40x more potent
Filtered & excreted exerting osmotic pull in

PCT & loop of henle
10x less potent than HCT
10x more potent than HCT

Different structure from thiazides
Lithium
Also inhibits DHT receptor

testosterone
Only diuretic not acting in lumen
Cirrhosis (ascites)
Hyperaldosteronism
Hypertension
Less anti-androgenic effects (less DHT &

progesterone receptor binding)
Heart failure
Hyperkalemia (NSAIDs likelihood)

Nausea, vomiting, diarrhea, leg cramps, headache,
dizziness
Shorter acting
Metabolized in liver into kidney lumen
insoluble & ppts out
Photosensitivity
10x less potent than amiloride
Must be given IV
flow urea excretion
ability to concentrate urine
Headache, nausea, vomiting,

hypernatremia/dehydration, pulmonary edema
Initial rapid expansion of plamsa volume
Intracranial pressure
Renal excretion of toxins
Nephrotoxic
Tetracycline antibiotic
SIADH
Usually used to treat mania
Bipolar disorder
(~SIADH)
Not very good
Nesiritide
Recombinant form of ANF

Na+ excretion
Tolvaptan
ADH V2 receptor antagonist

free H2O excretion &
urea & Na+ reabsorption
ADH V1a antagonist
vasocx & smooth muscle growth
Hypertension
CHF
Idiopathic hypercalciuria
(renal stones)
Nephrogenic diabetes insipidus
20x more potent than HCT

Edema
Hypertension
Blocks ADH action in the CT

aquaporins
Miscellaneous
Pulmonary edema
Edema (CH, renal, cirrhosis)
Hypercalcemia
Hyperkalemia
Secreted unchanged into lumen via

organic base transporter
Eliminated unchanged via kidney
Demeclocycline
Conivaptan
Glaucoma
Same potency as HCT

Longer acting
Triamterene
Mannitol
Longer acting
Longer acting
Excellent oral absorption
Eliminated via liver
Indapamide
Amiloride
Used more often for glaucoma than

acetazolamide
Low Na in cell sucks Na through basolateral

Na/Ca exchanger
Ca2+
reabsorption

Absorbed orally
Chlorothiazide
Eplerenone
CHF edema, Glaucoma

Urine alkalinization
Mountain sickness
No sulfur group in its structure

Only if allergic to other loops
Worst ototoxicity
Hydrochlorothiazide
Spironolactone
Treats
Decrease luminal (+) potential

( K+ pushed out) Ca2+ & Mg2+ reabs
Ethacrynic Acid
Metolazone
Hypotension
CHF
Heart failure
ADH V2 receptor antagonist
free H2O excretion &
urea & Na+ reabsorption
Drug
Toxicity
Treats
Proposed immune stimulant
Flu-like, hepatitis, asthma, rash,

nausea, urticaria, anaphyaxis
May contain organocholine

pesticides
URI or "Colds"
Ephedra
Contains ephedrine
(sympathomimetic)
Stroke, arrhythmias, hypertension
16x risk of hemorrhagic stroke

(w/phenylpropanolamine)
Weight loss
Energy
Feverfew
May inhibit PLA2 arachadonic

acid
Dizziness, nausea, indigestion,

heartburn, oral ulcer, rash
Contains melatonin
Does work, but not better than
traditional treatment
Migraines
Arthritis
GI distress, allergy, dermatitis,

bleeding, odor
Culture media for C. botulinum
Hypertension
As effective as antihistaminics in
nausea
Motion sickness
Morning sickness
Herbal medications & Nutrient supplements
Echinacea
Mechanism
Metabolism
Contraind: anti-coagulants
(may inhibit platelet aggregation)
Garlic
Lowers blood pressure

Lowers cholesterol
(small & brief)
Ginger
Effective anti-nausea
Inhibit thromboxane synthase
Ginseng
Many have NO donor capability
Phenelzine
Ginseng abuse syndrome:

CNS, arousal, HTN, nervous,
insomnia, vaginal bleeding
Dementia
Ginko biloba
ACh activity
Effects 5-HT & NE
VasoRX.Antioxidant...coag
GI, headache, allergy, bleeding
Dementia
Circulatory disorders
Kava
Saw Palmetto
St. John's Wort
Valerian
Glucosamine
Creatine
Androstenedione
Dry flaking skin, puffy face, red eyes,

Can cause serious cirrhosis & liver
weakness, oral tingling, GI, SOB,
failure!
EKG abnormalities
Enhances GABA activty
Inhibit 5-reductase DHT

Block 1 receptors
Contains hyperforin activates
PXR CYP450
Headache, GI, hypertension, libido

metabolism of: cyclosporine,
indinavir, digoxin, phenobarbital,
tamoxifen, BC
Trad. > Saw palmetto > placebo
Anxiety
Insomnia
BPH
Photosensitivity
Depression
Small hypnotic effect
Morning drowsiness, headache,

excitability, cardiac, odor
Insomnia
Stimulate cartilage cells GAG &

proteoglycans
Gi discomfort, nausea,
photosensitivity, systolic HTN,
proteinuria
Osteoarthritis
Wound healing
DHEA androstenedione &

testosterone & androsterone
Creatine phosphocreatine
Rash, dyspnea, N/V, diarrhea,

nervousness, fatigue, migraine,
myopathy, seizures, a-fib, testo
Athletic performance
Weight loss
Drug
HPA Axis
Growth Hormone Associated Agents
Growth Hormone
Somatropin
Somatotropin
IGF
Mecasermin
GHRH
Sermorelin
Hexa/Capromorelin
Somatostatin
Octreotide
Pegvisomant
Bromocriptine
Cabergoline
Pergolide
ACTH
Cosyntropin
CRH
HPT Axis
Corticorelin
TSH
Thyrotropin-
TRH
Protirelin
hCG
Choriogonadotropin-
hMG
Gonadotropins
Menotropin
FSH
Urofollitropin
rFSH
Clomiphene
GnRH
Gonadorelin
Leuprolide, Goserelin
Post.
Pituitar
y
Ganirelix
Cetrorelix
Vasopressin
Desmopressin
Mechanism
Metabolism
Toxicity
IGF-1, ECM, muscle, soft

tissue, urinary retention of nitrogen,
PO4, K+, anti-insulin
Administered daily in evening

(mimics normal pattern)
Children: few
Adults: per. edema, arthralgia,
myalgia, carpal tunnel syndrome
Mitogenic & anti-apoptotic

Skeletal, muscle, organ growth
Should not be used after closure of

epiphyses or in neoplasia
May induce hypoglycemia
Binds GHRH receptor cAMP

GH synthesis & release
40-80% of GH deficienct children

respond normally to GHRH
Binds SRIF receptor cAMP

GH release (synthesis intact)
Also inhibits TSH secretion
Synthetic SRIF is resistant to

enzymes (t1/2: 3min2hr)
Selective for GH (vs. insulin)
GH lysine replaced by glycine GH

antagonist
Paradoxical inhibitory effect on
somatroph adenomas (GH)
Childhood deficiency
Adult deficiency
SPIGFD: mutations in GH receptor,
post GHR defect, IGF-1 defects
Severe primary IGF

deficiency
Hexorelin: cardiac performance

(dilated cardiomyopathy)
Dx pituitary defect
Hypothalamic GH deficiency
GI motility & secretions, bile

production, gallbladder CX
PVR of hypothalamus = 14 AAs

cells of pancreas = 28 AAs
Acromegaly
Carcinoid tumors
VIPomas
PEGylated to t1/2,
immunogenicitybut affinity
(8 AA substitutions fix that)
hepatic aminotransferase
(otherwise well-tolerated)
Does not reduce size of GH tumor or

lower GH levels
Acromegaly
Cabergoline > bromocriptine
Headache, N/V, dizziness, postural

hypotension, insomnia
Most useful in GH & prolactin
Somatroph adenomas
CRH (hypothalamus) ACTH (ant.

pituitary) cortisol & aldosterone &
sex hormones
Binds CRH receptor cAMP
POMC ACTH
Dx adrenal insufficiency
Ovine CRH = t1/2 & potency

(over synthetic)
Flushing, SOB, tachycardia,

hypotension
Blood drawn from inferior petrosal

sinus after CRH stimulation
Binds TSH receptor cAMP

iodide uptake & TH syn/secr'n
Binds TRH receptor Ca2+
TSH & prolactin
Treats
Dx ACTH-secreting tumor
location
Dx residual thyroid
carcinoma
Admin: IV over 15-30 seconds

(TSH 2-5x basal in 30 min)
Transient nausea, hypo/HTN,

flushing, palpitations
Dx 2 hypothyroidism
Measure PRL reserves
Male infertility
Cryptorchidism
Dx Leydig cell failure
Used for LH activity (acts at same

receptor as LH, but longer t1/2)
Derived from urine of
postmenopausal women
Male infertility
Female infertility
Used for LH & FSH activity
IM
Used for FSH activity (merotropin

w/LH component removed)
Urofollitropin: IM/subQ
rFSH: subQ
Multiple births, ovarian

hyperstimulation syndrome, fluid
accumulation in cavities
Partial estrogen agonist (competitive

inhibitor of ER)
Admin: oral x5 days
Ovarian enlargement, vasomotor

flushing, OHSS
amplitude (not frequency) of

pulsatile LH & FSH secretion
Induce ovulation
Dx gonadotropin secr'n
Hypogonadism, bone
mineralization, lipids
Pulsatile: LH & FSH release

Continuous: LH & FSH release
GnRH deficiency
Delayed/precoc. Puberty
Gn-depen. Disease
No transient rise in gonadotropin

secretion as with continuous GnRH
administration
Inhibit premature LH surge

in ovary stim.
Long-acting agents (leuprolide,

Binds GnRH receptor Ca2+
histrelin, nafarelin, goserelin) have DPLC FSH & LH
AA's at cleavage site
Competitive antagonists binding
GnRH receptor LH > FSH
subQ
Binds V1a receptors GI/vasoCX

Binds V1b receptors ACTH
Binds V2 receptors aquaporins
Nasal spray, subQ
VasoCX
GI muscle, uterine muscle
Female infertility
Desmopressin challenge: urine Osm Central diabetes insipidus

should 50% w/central DI
Dx central/nephro DI
SIADH: Rx w/loop/demeclocycline Post-op ileus...eso varices
Drug
Mechanism
Estrogens
Conjugated & esterified natural

steroids
Ethinyl estradiol
Mestranol
Admin: IM
Admin: PO
first pass metabolism (ethinyl)
Synthetic steroidal estrogens
Admin: IM (x1/month)
Insoluble in water
Estradiol cypionate
Diethylstilbesterol
Methallenestril
Toxicity
Endometrial hyperplasia
Endometrial cancer
Breast tenderness
Feminization in males
Cholestasis (GB disease)
Hepatic adenomas
plasma TAG
Thromboembolic disease/MI
Headache, migraine
BC Interax: ABX, phenytoin,
barbiturates
Ethinyl estradiol = #1 estrogen

Norethidrone = #1 progestin
Low-dose mono-triphasic = #1
~
Suppress ovulation by negative
feedback on gonadotropin release
~
Progestins = thicken cervical mucus
~
Thin endometrium
ovum transport
~
hormone binding proteins
insulin secretion & resistance
Admin: transdermal patch

Most potent natural steroid
Extensive first pass metabolism
17 -estradiol
Esterified estradiol
Metabolism
Synthetic non-steroidal estrogens
Admin: PO
As potent as estradiol
Longer t1/2 than estradiol
Treats
Hormone replacement
(Primary hyogonadism)
Prostate cancer
Oral contraceptive
Hormone replacement
(Primary hypogonadism)
Advanced prostate
carcinoma
Anti
Progestin
Estrogen
Synthesis
Inhibitors
Estrogen Receptor
Modulators
Progestins
Progesterone
Admin: IM
>oral activity than progesterone
Medroxyprogesterone
Norethindrone
Norgestrel
Levonorgestrel
fat deposition & weight gain

Acne
Menstrual abnormalities
Uterine cramps
Hirsutism (androgenic preps)
risk of breast cancer
The only role of the progestin

component of combination oral
contraceptives is to protect
endometrium from estrogen-induced
hyperplasia & cancer
Endometriosis
Dys/amenorrhea
Oral contraceptive
Suppress gonadotropins
Fulvestrant
Pure estrogen receptor antagonist

ER downregulation
Tamoxifen
Breast: estrogen antagonist

Lipids, bones, uterus: agonist
ER+ breast cancer
Raloxifene
total cholesterol
risk of breast cancer
Osteoporosis
(in post-menopausal)
Exemestane
Binds irreversibly to aromatase

inhibiting conversion to estrogen
Anastrozole
Nonsteroidal aromatase inhibitor
Mifepristone
Admin: IM (x1/month)
As effective as anastrozole
ER+ metastatic breast

cancer
Structure similar to androstenedione
Competitive binding to progesterone

Inh. prog receptor & PG uteroCX
receptor & prostaglandin
Given w/misoprostol 2 days later
dehydrogenase
Breast cancer
(unresponsive to
tamoxifen)
Also blocks glucocorticoid receptor
Abortifacient
Cushing syndrome
Thyroid
Drug
Mechanism
Metabolism
Levothyroxine
Identical to endogenous T4
Converted to T3
Intrx: steroids, tmxfn, opioid, 5-FU,

phenytoin, CPZ, salicylate, benzos
Contraind: adrenal insufficiency
Propylthiouracil
Methimazole
Inhibit thyroid peroxidase

TH synthesis
Selectively destroys thyroid tissue
Radioactive iodine
Sodium Iodide
Calcium Homeostasis
PTH
Teriparatide acetate
Vitamin D
Calcitriol
Binds VitD receptor + RXR

calbindins & osteocalcin &
osteoclast formation & Ca2+
Etidronate
Alendronate
Risedronate
Bisphosphonates (pyroPO4 analogs)

Bind OH-apatite osteoclasts
bone mass
Glucocorticoids
Hydrocortisone
Cortisone
Dexamethasone
Bind glucocorticoid receptors

gluconeogenesis
glycogenesis
hormone-sensitive lipase
blood glucose
cytokines
vasoCX
demarginalized PMNs
vitamin D Ca2+ absorption &
Ca2+ clearance & bone resorption
ACTH
Corticosteroid Antagonists
ACTH analog w/complete biological

activity
Fludrocortisone
Binds mineralocorticoid receptor

Na+ reabs. & K+ secretion
Ketoconazole
Spironolactone
Drospirenone
TBG in children & preggos

doses required
Thyroid hormone replacement
Propyl: Preggos
Methim: longer duration
Rash, agranulocytosis, arthralgia,

myalgia, hepatic necrosis (P),
cholestatic jaundice (M)
Propylthiouracil T4T3 conversion
Graves disease
Thyrotoxicosis
Coadmin: -blockers or Ca2+

channel blockers for Sx
Contraind: preggo
Hypothyroidism
Doesn't increase cancer risk or

fertility or effect offspring
Hyperthyroidism
Thyrotoxic crisis
Stored for prolonged periods in fat
Not used to treat hypocalcemia
Nausea, facial flushing, hand

swelling, urticaria, resistance
Absorbed IV much better than PO
PO: take w/full glass of water
Hypocalcemia, hypophosphatemia
Upper GI distress
Hypoparathyroidism
Dx pseudohyperPTH
Osteoporosis
HypoPTH, pseudohypoPTH
Rickets, osteomalacia
Osteoporosis
Hypervitaminosis D: hypercalcemia
Short-acting
4x anti-inflammatory
Intermediate-acting
5x topical
Long-acting
10x topical
susceptibility to infx
Inhibits growth in kids
Myopathy
Osteoporosis
Cataracts
Adrenocortical atrophy
Iatrogenic Cushing's
Inhaled
Cosyntropin
Aminoglutethimide
Nervousness, arrhythmia, HTN,

SOB, N/V, diarrhea, heat intolerance,
reproductive fx
Salmon CT is potent and t1/2

20% develop resistance
Hypercalcemia
HyperPTH, VitD, Bone mets
Osteoporosis, Paget's Dz
Paget's Dz
Osteoporosis
Malignancy Ca2+
Short-acting
Betamethasone
Metyrapone
Treats
Binds PTH receptors Ca2+ bone Daily intermittent admin osteoblasts

mobilization & renal Mg & Ca (PO4)
& bone formation
reabsorption & vit.D production
(not bone resorption!)
Binds calcitonin receptors cAMP

osteoclast-mediated Ca2+
mobilization & excretion
Triamcinolone
Traps thyroid iodide & blocks thyroid Coadmin: -blockers & Ca2+ channel
hormone release
blockers & thionamide
Calcitonin
Prednisone
Prednisolone
Toxicity
Addison's disease
Dx of hypercortisolism
Congenital adrenal
hyperplasia
Asthma
Plasma cortisol measured 30-60 min Replaced therapeutically with steroid

after IM/IV administration
hormones
Hypernatremia, hypokalemia
Metabolic alkalosis, hypervolemia
Hypertension
Dx of adrenal insufficiency
Primary adrenocortical
deficiency
Blocks cortisol synthesis
Blocks conversion of cholesterol

pregnenalone
Cushing's syndrome
Inhibit P450 enzymes required for

steroid synthesis
Competitive mineralocorticoid receptor
antagonist
Primary hyperaldosteronism
Drug
Miscellaneous
ABX
Folate
Inhib.
Main Drugs
Chloroquine
Quinine
Quinidine
Mechanism
Metabolism
Toxicity
Schizonticide terminates fever &

parasitemia
Buildup of free heme
Resistance: mutant PfCRT trx

(reversed by verapamil & desipramine)
Pruritus, nausea, anorexia, blurring

Hemolysis in G6PD, Wide QRS
Agranulocytosis, oto/retinopathy
Unknown
Metabolized by liver, excreted by kidney

Cardiotoxicity, hematologic
Coadmin: doxycycline
Cinchonism, hypersensitivity
Only used in chloroquin-resistant
Blackwater fever, glucose, uteroCX
Mefloquine
Schizonticide
Used as prophylaxis
Long half-life (~20 days)
GI
Neuropsychiatric
Cardiac & blood dyscrasias
Primaquine
Synthetic 8-aminiquinoline
Absorbed GI
Half-life: 3-8 hours
GI, methemoglobinemia
Hemolysis in G6PD
Cardiac & blood dyscrasias
Active against RBC forms

Inhibit DHF reductase folate
Coadmin: sulfa drugs

(inh. DHP synthase = synergy)
GI
Pruritus
Pyrimethamine
Proguanil
Tetracycline
Doxycycline
Clindamycin
Atovaquone
Combined w/proguanil (malarone)
GI
Treats
PF malaria
Hepatic amebic abscess
Does not eliminate liver forms

(P. vivax & P. ovale)
No P. falciparum gametocyte kill
PF malaria
PF malaria
(chloroquine resistant)
Only agent active against dormant
hypnozoite liver form
(P. vivax & P. ovale)
Doxycycline added to quinine trx

Clindamycin instead of doxy for
preggos
Action is too slow to be used as

monotherapy
Active against RBC forms
Malaria
Not to be used alone

(Resistance & toxicity)
Halofantrine
Artemisin
Sesquiterpene lactone peroxide

dihydroartemisin
PF malaria
(drug-resistant)
Trypanosomiasis & Leishmaniasis
Drug
Mechanism
Suramin
Melarsoprol
Eflornithine
Nifurtimox
Stibogluconate
Metronidazole
Trivalent arsenical compound
Other Protozoa
Anti-Helminths
Toxicity
Treats
Admin: IV
Does not cross BBB
GI
Neurological
Cardiovascular, blood dyscrasias
Adding pentamidine may increase

efficacy
Early hemolymphatic
African trypanosomiasis
Admin: IV
Does cross BBB
Reactive encephalopathy
Renal & cardiac toxicity
Hypersensitivity
Inhibits ornithine decarboxylase blocks

conversion of ornithine putrescine
Admin: IV
GI
Blood dyscrasias
Nitrofuran structure
Admin: oral
GI
CNS
Decreases severity of acute disease,

but many times fails to eradicate the
parasite
Acute American
trypanosomiasis
Pentavalent antimonial
Admin: IM or IV
(daily)
GI
Fever, arthralgias
T wave changes, QT prolong
First line therapy
Cutaneous & visceral

leishmaniasis
Causes multiple-strand breaks, disruption of

DNA replication & trx & inhibits DNA repair
Admin: oral
Nausea, headache, metallic taste

GI, CNS, hematologic
Disulfiram-like reaction
May potentiate oral anticoagulants
Giardiasis
Entamebiasis
Trichomoniasis
Coadmin: metronidazole
GI
Pruritis
Contraind: Optic neuropathy

Renal or thyroid disease
Iodine intolerance
Little GI absorption
Renal excretion
GI
Effective against intraluminal E. hystolytica

(not tissue)
Paromomycin
Emetine
CNS advanced
African trypanosomiasis
Mammalian OC enzyme very short

half-lifetrypanosome OC enzyme
much more stable
Iodoquinol
Anti-Trematodes
Metabolism
Effective against tissue E. hystolytica

trophozoites
Entamebiasis
Heart failure
Hypotension
Use limited to severe amebiasis

when metronidazole unavailable
Cardiovascular
Pancreatic, hepatic, renal, blood
Bronchospasm, dyspnea
Injectable (trypanosomatid)
Inhalation (pneumocystis)
Trypanosomes
P. carinii
Useful in trx metro-resistant protozoa

& tapeworms
Giardiasis
Cryptosporidiasis
(+ tapeworms)
Pentamidine
Effective against trypanosoma & P. carinii
Admin: IM or IV
Half-life: ~6 hr
Accumulates in tissues (12 days)
Nitazoxanide
Blocks pyruvate:ferredoxin oxidoreductase

pathway
Converted to active tizoxanide
Piperazine
Direct GABA agonist

Blocks ACh at NMJ to produce nematode
flacid paralysis
Admin: oral
Excretion: w/in 24 hrs
GI
Cure rate of ascariasis (>90%)
Ascariasis
Pyrantel pamoate
Tetrahydropyrimidine derivative
NMJ blocking agent paralyzes & expels
Admin: oral
Poorly absorbed from GI (good!)
GI
Insomnia
ACh release & AChE inhibition

Cure rates >90%
Ascariasis
Pinworm
Hookworm
Mebendazole
Inhibits microtubule synthesis
Admin: oral
Poorly absorbed from GI
(effect w/fatty meal)
Hypersensitivity reactions
Alopecia
Wide-spectrum
Ascariasis
Trichuriasis
Pin & Hookworm
Albendazole
Active albendazole sulfoxide
Admin: oral
Metabolized in liver to active form
Mild GI
Long-term use (hydatid):
liver enzyme & blood dyscrasia
Admin fasting: luminal parasite

Admin fatty meal: tissue parasite
Coadmin: corticosteroids (cyst)
Cysticercosis
Hydatid disease
Round, Pin, Hook
Niclosamide
Salicylamide derivative
Inhibits oxidative phosphorylation
Admin: oral
Mild GI
Praziquantel
Isoquinoline-pyrazine derivative
cell membrane permeability to Ca2+
paralysis
Admin: oral
[]: cimetidine or carbs
[]: steroids or antiepileptics
Mild: headache, dizziness, GI,

myalgia, pruritis, fever
Admin: oral
GI
Skin rash
Admin: oral
Half-life: 2-3 hrs (acidic urine)
10 hrs (alkaline urine)
Mild: headache, dizziness, GI, fever,

rash, blood dyscrasias
Bithionol
Diethylcarbamazepine
Synthetic piperazine derivative

Immobilizes & alters microfilament surface
structure
Tapeworm
Bitter taste (don't chew)
Schistosomiasis
Hydatid disease
Neurocysticercosis
Trematodes & Cestodes
Fascioliasis
Give w/antihistaminics
(allergic reactions)
Filariasis
Noradrenergic Targets
Drug
Phentermine
Diethylproprion
Phendimetrazine
Benzphetamine
Phenylpropanolamine
Mixed
Fat
Target
Metab.
s
Ephedra
Sibutramine
Orlistat
Mechanism
Amphetamine derivative
Inhibits NE reuptake
Inhibit NE reuptake
Metabolism
Coadmin: fenfluramine
(Pulmonary HTN & valve problems)
Interax: MAOI, guaneth, stim, EtOH,
sibutramine, TCA
NE target
Toxicity
Fenfluramine releases 5-HT &

Drug mouth, insomnia, constipation,
inhibits 5-HT reputake
BP, HR, abuse
Contraind: hyperthyroid, HTN, CVD,
glaucoma, anxiety
Withdrawn in 2000 due to

hemorrhagic strokes in women
Only approved OTC appetite

suppressant
Appetite suppressant & weight loss
weight loss w/: caffeine & aspirin
Cardiac arrest, HTN, arrhythmia,

stroke, seizure, MI
Found in the herb Ma Huang
Inhibits NE, 5-HT, DA reuptake
Interax: MAOI, SSRI, triptans,

ergotamines, dextromethorphan,
opioids, lithium, tryptophan
Drug mouth, insomnia, constipation,

BP, HR, abuse
Lose 10-15% of weight

Contraind: HTN, renal/liver impair,
addx, CAD, CHF, arrhythmia, stroke
Interax: cyclosporine
Gas, oily stools, defecation

absorption of ADEK & -carotene
Lose 8-10% of weight

Improves H1Ac & sulfonylurea dose
Contraind: malabsorption, cholestitis
Inhibits GI lipases dietary fat

absorption
Treats
Obesity
Obesity
Asthma
URI
Obesity
Drug
Lispro insulin
Insulin
Regular insulin
Mechanism
Metabolism
Able to stay as monomer, because

proline & lysine AA's are swapped
Ultra-fast & short-acting
Zinc insulin crystals in a neutral,

unbuffered suspension
Short-acting
Admin: IV or subQ
(30-60 min before meal)
NPH insulin
Insulin(-) complexed w/protamine(+)

& zinc
Lente insulin
30% semilente insulin + 70%

ultralente insulin crystals in acetate
buffer
Intermediate-acting
Peptides
Insulin requirements during 2nd

half of pregnancy
~
If impaired renal fx: insulin
clearance
Type 1 diabetes
Peakless recombinant insulin that

precipitates in neutral subQ tissues
Ultra-long-acting
Delayed onset of action
Pramlintide
Amylin analog gastric emptying

& satiety & post-pran glucagon
Admin: subQ w/mealtime insulin

Don't use w/acarbose
Insulin-induced severe
hypoglycemia
Glucagon-like peptide agonist

gastric emptying & post-pran
glucagon & insulin secretion
GLP-1 secreted in response to food

to potentiate glucose-stim insulin
release
N/V, diarrhea
Glipizide
First generation:
Longest acting (60 hours)
Intermediate potency
Bind SUR receptors associated w/
ATP-sensitive K+ channels
K+ current insulin secretion
Second generation:
Glimepiride
Highest potency
Once daily dosing
Meglitinides
Once daily dosing
Biguanides
Glyburide
Repaglinide
Phenformin
Nateglinide
Metformin
TZDs
Rosiglitazone
Pioglitazone
Contraind: hypersensitivity,
gastroparesis, hypoglycemia
unawareness
Type 1 diabetes
Type 2 diabetes
Type 2 diabetes
First generation:
Shortest acting
Least potent
Chlorpropamide
Sulfonylureas
Hypoglycemia
(Counter-reg. often impaired)
Mild: juice/glucose
Severe: glucagon
~
Allergy
(insulin or protamine)
~
Insulin resistance (IgG)
~
Lipohypertrophy
Glargine insulin
Exenatide
inhib.
Treats
Long-acting
Tolbutamide
Dipep
Excess zinc (produces large

crystals) in acetate buffer
Ultralente insulin
Hyperglycemic
Pptdase glcsdase
s
4 inhib
Toxicity
Bind SUR receptors associated w/

ATP-sensitive K+ channels (diff. site
from sulfonylureas) K+ current
insulin secretion
gluconeogenesis
insulin-stimulated GLUT4
trafficking to membrane
cAMP-act. protein kinase
(Increase tissue sensitivity to
insulin)
Bind PPAR- receptor + RXR

GLUT1 & GLUT4
lipoprotein lipase, FABPaP2
TNF, leptin
Half-life: 1 hour
Severe hypoglycemia
(chlorpropamide & glyburide)
Weight gain
Skin reactions & erythema
Blood dyscrasias
Hepatic dysfunction
(All are liver metabolized)
GI disturbances
May induce SIADH

or alcohol flush reaction
Recurring hypoglycemia
Extended release form does not
induce weight gain!
Type 2 diabetes
Does not cross placenta

(can use for gestational diabetes)
Binds a site on K+ channel different
from all other sulfonylureas
muscle insulin sensitivity
Hypoglycemia
Weight gain
Used for post-pran hyperglycemia
Type 2 diabetes
Lactic acidosis
(Even less with 2nd generation)
Cardiovascular disorders
Do not cause hypoglycemia

(even at high doses)
TAG, cholesterol, LDL, HDL
Weight loss & BP
Type 2 diabetes
(obese)
Troglitazone: hepatotoxicity
Heart failure
Angina, MI
Do not cause hypoglycemia

Current TZD's do not cause
hepatotoxicity
Type 2 diabetes
Flatulence, nausea, diarrhea

Contraind: IBS, obstruction, ulcer
Do not cause hypoglycemia, lactic

acidosis, or weight gain
Type 2 diabetes
Half-life: even shorter & rapider
Not significantly metabolized

90% oral dose gone in 24 hours
Half-life: 2 hours
Low potency
Metabolized to inactive metabolites

albumin bound
Metabolized to weak metabolites
albumin bound
Acarbose
Miglitol
Competitive -glucosidase inhibitors

carbohydrate digestion/absorb
Blunted post-prandial glucose
Low systemic bioavailability

Taken with a meal
Sitagliptin
Blocks dipeptidyl peptidase IV

GLP-1 & GIP post-pran insulin
With: diet & exercise

With: metformin or TZD
Diazoxide
open time of ATP-sensitive K+

channel insulin release
Metabolized in liver
Half-life: 48 hours
Nausea/vomiting
Fluid & salt retention
Does not inhibit the synthesis of

insulin, only the release
Insulinoma
Glucagon
Binds glucagon receptor cAMP

(P) glycogen phosphorylase &
synthase
Admin: subQ, IM, IV

Half-life: 3-6 minutes
Metabolism: 25% first-pass
Nausea & vomiting
Inotropic & chronotropic

RX of GI smooth muscle
Release catecholamines & CT
Severe hypoglycemia
Shock & GI RX
Dx pheochr-cytoma
Type 2 diabetes
Drug
Mechanism
Metabolism
Toxicity
Treats
Vitamin B3 hepatic TAG

synthesis & lipoprotein lipase
apoB VLDL LDL
Half-life: 1 hour
Used w/: bile acid binding resin
Used w/: HMG CoA reductase inh.
Flushing, pruritis
Nausea, diarrhea, peptic ulcer
Hepatotoxic, glucose intol., gout
Most effective agent to HDL

Only agnet to Lp(a)
HyperTAG
Familial hyperTAG
FC hyperTAG
Gemfibrozil
Fenofibrate
Clofibrate
Bind PPAR-+ RXR apoC-III &

apoB & lipoprotein lipase VLDL
LDL & apoA
Half-life: 1.5 hours

Highly albumin bound
GI disturbances
Rash, myopathy, arrhythmia
Fatigue
Cholestipol
Cholestyramine
(+) charged resins that bind bile

acids reabsorption of bile acids
cholesterol & LDL receptors
Taken with meals PO
HyperTAG
GI (constipation)
Negligible systemic bioavailability

Approved for use in children
Familial HyperTAG
FC hyperTAG
Statins
Inhibit HMG CoA reductase (HMG

CoA mevalonate) cholesterol
& LDL receptors
First pass metabolism

Cytochrome P450 metabolized
Extensively protein bound
Myopathy (CK)
Renal dysfx (myoglobinuria)
Rhabdomyolysis (w/gemfribrozil)
BMP-2 osteoblasts
fracture risk
Hypercholesterolemia
(& familial)
cholesterol transport at brush

border in small intestine lumen
cholesterol & LDL-C & HDL
Enterohepatic recycling
Half-life: 22 hours
Low systemic bioavailability
Cholesterol lowering effect limited

by liver cholesterol synthesis
Hypercholesterolemia
Triglycerides
Niacin
Cholesterol
Ezetimibe
Estrogen
replacement
lipid oxidation
TAG, HDL
LDL, cholesterol
Plant stanol
esters
absorption of dietary cholesterol
Omega-3 fatty
acids
Ethanol
HyperTAG
Dysbetalipoproteinemia
FC hyperTAG
Progestins have undesirable effects

on plasma lipids
(CAD & stroke)
endothelial inflammation
LDL & TAG
Monosaturated fatty acids (oleic):

LDL but not HDL
HDL & LDL
No association with beverage types
Drug
Mechanism
Metabolism
Toxicity
Ointment
Used w/neomycin or polymyxin
Absorbed through skin
Allergic contact dermatitis
Gram (+) bacteria

Anaerobes (cocci)
Effective against most gram (+)
Intranasal preparation
PEG vehicle can irritate nasal

mucosa
Impetigo
(S. aureus & S. pyogenes)
Effective against most gram (-)
Topical
Bacterial Infections
Bacitracin
Mupirocin
Treats
P. aeruginosa
E. coli, enterobacter
Klebsiella
Polymyxin B
Sensitization
Cross-sensitivity to streptomycin,
kanamycin, gentamycin
Neomycin
Gentamycin
10% of topical application is
absorbed
Clindamycin
Bloody diarrhea
Pseudomembranous colitis
Acne Vulgaris
Acne vulgaris
Erythromycin
Naftifine
Terbinafine
Effective against dermatophyte

infection
Allylamines
Inhibit ergosterol synthesis
Oral
Antifungals
Effective against growing cells

Inhibits fungal cell wall synthesis
Ketoconazole
Pencyclovir
Dermatophytes
Fine microcystal suspension
Diarrhea
Photosensitivity
Headaches
Interax: benzos sedation

statins rhabdomyolysis
Gynecomastia
Hepatitis
Ventricular dysfx
Tinea infections
Chronic gen. MC candidiasis

Dermatophytes
Cream
Applied at first sign of infection
Recurrent orolabial HSV
Shampoo or lotion
~Absorbed via skin, in fatty tissue,
excreted in urine in 5 days
Skin staining
Unpleasant odor
Inhibit tyrosinase melanin
skin hyperpigmentation
Hydroquinone = temporary
Monobenzone = permanent
Lack of systemic effects

(good for kids and preggos)
Scabies
Local irritation
Allergy
Retinoic acid
Tretinoin (ATRA)
epidermis cohesion
cell turnover
Erythema
Dryness
Sunlight sensitivity
Adapalene
Naphtoic acid analog
Admin: topical
Applied to dry skin only
Pediculosis capitis
Pediculosis pubis
Scabies
Hematotoxicity
Neurotoxicity
Skin cancer
Cataracts
Synthetic retinoid-like drug

Decreases sebaceous gland function
Admin: oral
Similar to hypervitaminosis A:
dryness, itching, IBS
IBS, muscle pain, teratogen
Converted to benzoic acid

Effective against P. acnes
Admin: topical
Skin irritation
Vitiligo
May appear worse in the first month,
as quiescent comedones emerge &
rupture
Acne vulgaris (comedones)

Light-damaged skin
Similar to retinoic acid but less

irritation
Mild to moderate acne
Severe cystic acne
Acne vulgaris
Admin: oral
Anti-inflammatory
Antiproliferative
Extreme caution in young women
Synthetic vitamin D3
Skin dryness
Itching
Corticosteroids
Anti-inflammatory
Antimitotic
Skin atrophy, rosacea

IO pressure
Cushing's syndrome, growth
Tar compounds
Byproducts of petrol distillation

Antipruritic
Irritant folliculitis
Solubilize cell surface protein debris
Anaphylactic shock
Irritation & inflammation
Salicylism
Salicylic acid
Contraind: porphyria, liver dysfx
Decreases viral shedding (time) &

time to healing
Produce repigmentation of
depigmented macules
Psoralens intercalate w/DNA
Calcipotriene
Superficial candidiasis
Primary cutaneous HSV

Limited MC HSV
Trioxsalen
Methoxsalen
Tazarotene
Cessation of therapy generally

followed by infection recurrence
Ointment
Sulfur
Hydroquinone
Monobenzone
Dermatophytes
Candida
P. obiculare
Decreases viral shedding
Lindane
Acne
Psoriasis
Seborrheic dermatitis
Candidiasis
Use in onychomycosis only effective
in ~10% of patients
Acitretin
Antiinflammatory
Cream, shampoo, lotion, vagial

tablets, suppositories
Well tolerated
Benzoyl peroxide
Keratolytics
Acne rosacea
Amphotericin B
Nystatin
Isotretinoin
Pruritis
Possible carcinogen
Contraind: pregnancy & lactation
Well tolerated
Acyclovir
Tricogenics
Acne vulgaris
Acne rosacea
Tolfnaftate
Griseofulvin
Antiparasites
Effective against Dermodex brevis

Anti-inflammatory
Contraind: sulfa allergy
Ciclopiroxolamine
Topical
Antivirals
Topical Antifungals
Azoles
Burning
Irritation
Topical
Alone or with sulfur preparation
Sulfacetamine
Metronidazole
Skin
Pigmentation
Effective against
Propionibacterium acnes
Propylene glycol
Used for elimination of keratolytic

debris
Urea
prekeratin & keratin solubility

elimination
Alone or with: salicylic acid
Psoriasis
Keloids, cystic acne, alopecia areata

= triamcinolone injection
Psoriasis
Chronic lichenified dermatitis

Xerosis
Hyperkeratosis
(palms & soles)
Doxepin
Potent histamine receptor (H1 & H2)

antagonist
Admin: oral or topical
Minoxidil
Reverses progressive of terminal

scalp hairs
Admin: topical
Finasteride
Blocks 5-reductase inhibits

conversion of testosterone DHT
Admin: oral
SE's & contraindications similar to

anticholinergics
Atopic dermatitis
Lichen simplex chronicus
Discontinuation causes continued hair

loss in 4-6 months
Androgenic alopecia
libido
Ejaculation disorders
Eretctile dysfunction
Pregnant women should not be

exposed (hypospadias)
Drug
Misc.
Colchicine
Urate
Inhib.
Uricosuric
Agents
Indomethacin
Mechanism
Metabolism
Toxicity
Binds microtubule tubulin

polymerization WBC migration
& urate phagocytosis
Admin: oral
Accumulates in WBCs
Deacetylated in liver
GI
Blood dyscrasias
CNS depression, shock
Admin: oral
Interax: PCN, ASA, sulfa, allopurinol
Inhibits proximal tubule reabsorption

of urate
Sulfinpyrazone
Inhibits proximal tubule reabsorption

of urate
No anti-inflammatory or analgesia
Very highly plasma protein bound
Comp. inhibits xanthine oxidase

conversion of hypoxanthine
xanthine uric acid
Metabolized to oxipurinol (active)

Depletes purine precursors
(5'-PRPP)
GI
Dermatitis
Nephrotic syndrome
Treats
Gouty arthritis attacks
Pseudogout
Familial Med. fever
Not to be used in chronic gout or

prophylaxis
Anti-inflammatory
Probenecid
Allopurinol
Acute gouty attacks
Not to be used in acute gout attacks

Hyperuricemia control
Potentiates insulin & oral
hypoglycemics
Maculopapular rash (pruritus)

GI, hepatotoxicity
Fever, hypersensitivity
Not useful for acute gout attacks

Inhibits kidney reperfusion injury
Chronic tophaceus gout
Drug
Albuterol
Terbutaline
Metaproterenol
Salmeterol
Formoterol
Mechanism
2-agonists Gs cAMP
bronchoRX
Metabolism
Toxicity
Treats
Admin: Metered dose inhaler

Nebulizers
Anxiety, tremor, restlessness, HR,

hypokalemia
Albuterol is the most used

Metered dose inhaler is most
common
Acute asthma attack
Salmeterol is not useful in acute

asthma attacks!
(Slow onset of action)
Severe refract asthma

COPD
Chronic bronchitis
Long-acting
Salmeterol = slow-acting
Formoterol = fast-acting
Theophylline
Antagonist at adenosine A1 receptor

Gi cAMP & PLC
bronchoRX
Admin: IV
Low therapeutic index
Ipratropium
Tiotropium
mACh receptor antagonist Gi

cAMP & PLC bronchoRX
Admin: dry powder inhalation
Prevents mast cell degranulation

(asthma prophylaxis)
Admin: metered dose inhaler

Spinhaler
4x day regimen
Cromolyn
Nedocromil
Prednisone
Methylprednisone
Methylprednisone
Hydrocortisone
Beclomethasone
Flunisolide
Triamcinolone
Troleandomycin
Gold salts
Methotrexate
Admin: oral
Inhibit late-phase reactions of
inflammation
Decrease bronchial reactivity
Most potent anti-asthma agents
available
Admin: IV
Admin: inhalation
TAO = macrolide antibiotic inhibit

corticosteroid metabolism
Headache, CNS stimulation

N/V, epigastric pain
Arrhythmias, seizures
Nocturnal asthma
Chronic bronchitis
Limited in asthma
No role in acute asthma!

Virtually no side effects
Greater potency than cromolyn
Additive therapeutic effects with
corticosteroids
Systemic corticosteroid effects

Hoarseness
Oropharyngeal candidiasis
Coughing, wheezing
HPA axis suppression
Long-term therapy (>3weeks) only if
refractory to other trx
Asthma
(maintenance)
Acute asthma
Reformulated as HFA inhaler

systems (+MDI)
Steroid-sparing therapy
Asthma
(maintenance)
Montelukast
Weak anti-inflammatory &

bronchodilator actions
Best if added to ICS therapy

(allows lower doses)
Omalizumab
Monoclonal anti-IgE antibody
Allowed lower doses of ICS &

hospitalizations & ER visits
Iodinated glycerol
Mucolytic that improves

expectoration, cough, chest
discomfort, duration of attack
Tumorigenicity forced removal from

the market
Chronic bronchitis

Pharmacology Year 1991

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Pharmacology Year 1991

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Drug Charts

(Epopro = IV / Trepro = subQ)

(male = erection injection)

(during pregnancy = dinoprostone)

(vasculature = vasodilates to maintain PDA until surgical correction)

(stable, long acting, SE: brown pigmentation, dry eyes)

(administered vaginally, uterine contractions & collagenase activity)

(NSAID indole derivative)

(administered vaginally, uterine contractions & collagenase activity)

(vasculature = vasodilates to relieve pulmonary HTN)

(GI = cytoprotective at low doses, acid at high doses)

(blocks leukotriene receptors)

(vasculature = vasoconstricts to close PDA in premies)

What Makes it Unique

1) binds serum proteins (depends on dose)

1) salicylism, respirary alkalosis, met. acid

Less effective at COX inhibition than ASA

Less side effects, no renal toxicity,

Low dose = analgesic (no anti-inflam)

GI, rash, tinnitis, fluid retention

1) serum aminotransferase activity in liver

Affects COX-2 > COX-1 by 10:1

Very potent indole derivative

30% have to discontinue

Also inhibits lipoxygenase

Free fraction is 40% higher in females

Cholestatic liver damage

1) Least potent of COX-2 inhibitors

Can interfere w/antihypertensive therapy

Most COX-2 selective CV problems

Still contraindicated in pts w/GI ulcers

1) COX inhibitory effects primarily in CNS

1) Less GI irritation & bleeding

Biological Response Modifiers

What Makes it Unique

Chronic use associated with: infections, ulcers,

Inhibits calcineurin phosphatase

Impairs T-cell response to antigen

Tacrolimus is 100x more potent

Inhibits T-cell activation

Renal transplant have surgical complications

Competitive inhibition of inosinate

Inhibits inosine monophosphate

Inhibits T-cell & B-cell cell cycle &

Coadminister: cyclosporine & corticosteroids

Sphingosine 1-P receptor agonist

Reversibly sequesters lymphocytes in

Graft is protected from T-cell attack

Removes T-cells from system

Coadminister: azathioprine & corticosteroids

Transplant rejection (kidney)

Toxicity: autoimmune hemolytic anemia

Ig against CD3 on T-cells

Blocks antigen recognition site

Toxicity: cytokine release syndrome

Ig against IL-2 receptor

Blocks activation of T-cells by IL-2

Coadminister: cyclosporine & corticosteroids

Transplant rejection (kidney)

Blocks immune activation of TNF

Coadminister: methotrexate for RA

Ig against anti-D antibodies

Blocks anti-Rh antibodies