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System
CNS
Brain and Spinal Cord
Acts as control for regulating physical and mental
processes
Neurons are the brains functional units
Neurotransmitters
Receptors
Drugs
affecting
Central Nervous
System Drugs
6
Depressants
Stimulants
11
12
Opioids:
Examples of opioids:
Opium
Morphine sulfate
Meperidine
Hydromorphone
Butorphanol
Hydrocodone
Fentanyl
Etorphine
Buprenorphine
Pentazocine
14
Opioid antagonists:
Block the binding of opioids to their receptors
Used to treat respiratory and CNS depression of
opioid use
Examples include naloxone and naltrexone
15
Neuroleptanalgesics:
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1.
2.
3.
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22
25
4. Muscle relaxation
relax contracted muscle in joint disease
or muscle spasm.
5. Other effects
lead to temporary amnesia
decrease the dosage of anesthetic;
depress respiratory and cardiovascular
function.
26
27
28
29
Short-acting compounds:
triazolam, oxazepam(15-30min,
t1/2 2-3 h)
Medium-acting compounds:
estazolam, nitrazepam (40min,
t1/2 5-8 h)
Long-acting compounds:
diazepam, flurazepam(50h)
30
Acute
toxicity:
Benzodiazepines in
acute overdose are considerably less
dangerous than other sedative-hypnotic
drugs. Cause prolonged sleep,without
serious depression of respiration or
cardiovascular. The availability of an
effective antagonist, flumazenil.
31
Side-effects
during
therapeutic use: drowsiness,
confusion, amnesia, impaired
coordination. Main disadvantages are
interaction with alcohol, long-lasting
hangover and the development of
dependence.
Tolerance
and dependence:
Classification
(1)Ultra-short-acting barbiturates: act
within seconds, and their duration of
action is 30min. Therapeutic use of
Thiopental: anesthesia
(2)Short-acting barbiturates: have a
duration of action of about 2h. The
principal use of Secobarbital : sleepinducing hypnotics.
33
Classification
(3)Intermediate-acting barbiturates: have
and effect lasting 3-5h. The principal use
of Amobarbital is as hypnotics.
(4)Long-acting barbiturates: have a
duration of action greater than 6h. Such
as Barbital and Phenobarbital.
Therapeutic uses: hypnotics and
sedative, and antiepileptic agents at low
doses.
34
35
Reasons:
(1) have a narrow therapeutic-to-toxic
dosage range.
(2) suppress REM sleep.
(3) Tolerance develops relatively quickly.
(4) have a high potential for physical
dependence and abuse.
(5) potent inducers of hepatic drugmetabolizing enzymes.
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39
Sedative-hypnotic agents
Be used in the emergency treatment of
convulsions as in status epilepticus.
Anesthetic (or be given before
anesthetic)
Combination with antipyretic-analgesic
Treatment of hyperbilirubinemia and
kernicterus in the neonate.
40
41
42
Phenothiazines
(Tranquilizers)
Indications
Good sedation for healthy
animals undergoing elective
procedures
Anti-emetic
43
Phenothiazines
Contraindications
Phenothiazines
Other effects
Antiarrhythmic effect
May cause excitement rather than
sedation
Personality changes that usually
subside within 48 hours
45
Benzodiazepines (Benzodiazepines)
Indications
Convulsing/epileptic patients
Patients with a history of seizure
CSF taps or myelogram procedures
Minimal cardiovascular or respiratory
depression
Useful in geriatric or pediatric
Ideal for older, depressed or anxious
patients
Works effectively as an induction agent
when used with ketamine
46
Benzodiazepines (Benzodiazepines)
Contraindications
47
Benzodiazepines (Benzodiazepines)
48
Benzodiazepines (Benzodiazepines)
Other points
Midazolam is water soluble and
readily combines with opioids
(oxymorphone, butorphanol)
Effects are reversed with
flumazenil if adverse effects are
seen
49
2-Agonists
50
2-Agonists
51
2-Agonists
52
2-Agonists
Contraindications
Considerable potential for side
effects especially if administered IV
Profound cardiovascular effects
include bradycardia, profound
hypotension, decreased
contractility and stroke volume and
second degree heart block
Contraindicated when concerned
about respiratory function, hepatic
and renal function
53
2-Agonists
Contraindications
Associated with temporary
behavior and personality changes
Reduces pancreatic secretions
causing transient hyperglycemia
(exacerbates dehydration)
Opioids will exacerbate these side
effects
54
Opioids
Commonly used:
Morphine
Oxymorphone (Numorphan)
Butorphanol (Torbugesic, Torbutrol)
Hydromorphone
Meperidine (Demerol, Pethidine)
Fentanyl
55
Opioids
56
Opioids
Opioids
58
Opioids
Fentanyl patches
59
Opioids
Reversible by use of pure antagonists such as
naloxone or nalmefene
60
Opioids
Other effects in addition to analgesia
61
Opioids
Cardiopulmonary effects
Bradycardia
Possible hypotension with release of
histamine
Especially if given IV
Morphine and meperidine
Increased muscle contraction in low
doses
Inotropic effect
morphine
62
Opioids
Other effects in addition to analgesia
63
Opioids
Contraindications
64
Definition
Stimulants
are a substance
which tends to increase
behavioral activity when
administered
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70
MOAs :
Block the reuptake of norepinephrine
and dopamine into the presynaptic neuron
and increase the release of these
monoamines into the extraneuronal space.
- Clinical use:
1. Narcolepsy.
2. Attention-deficit hyperactivity disorder
71
Adverse effects:
- Cardiovascular: Hypertension
- Endocrine metabolic: Weight loss
- Gastrointestinal: Abdominal pain , Loss
of appetite, Xerostomia
- Neurologic: Headache , Insomnia
- Psychiatric: Feeling nervous
72
73
MOA:
Non-competitive antagonist of GABA
receptors.
After injecting the mice with picrotoxin you
wellnotice:
- Clonic convulsion characterized by :
1. Asymmetric
2. Intermittent
3. Spontaneous
4. Coordinated
74
MOA:
Competitive antagonist of the glycin
receptors.
75
Methylphenidate
Brand Name: Ritalin
Classification Therapeutic: CNS stimulant
Action: Produces CNS and respiratory
stimulation with weak sympathomimetic
activity.
Therapeutic Effects: Increased attention
span in ADHD. Increased motor activity,
mental alertness, and diminished fatigue
in narcoleptic patients.
76
Drug
List
carbamazepine (Epitol, Tegretol)
clonazepam (Klonopin)
diazepam (Valium)
divalproex (Depakote)
ethosuximide (Zarontin)
Fosphyenytoin (Cerebyx)
gabapentin (Neurontin)
77
Drug
List
lamotrigine (Lamictal)
levetiracetam (Keppra)
lorazepam (Ativan)
oxcarbazepine (Trileptal)
phenobarbital (Luminal Sodium)
phenytoin (Dilantin)
78
Drug
List
primidone (Mysoline)
topiramate (Topamax)
valproic acid (Depakene)
zonisamide (Zonegran)
79
Drug
List
amantadine (Symmetrel)
benztropine (Cogentin)
bromocriptine (Parlodel)
entacapone (Comtan)
levodopa (Dopar)
levodopa-carbidopa (Sinemet)
80
Drug
List
levodopa-carbidopa-entacapone (Stalevo)
pergolide (Permax)
pramipexole (Mirapex)
ropinirole (ReQuip)
selegiline (Eldepryl)
tolcapone (Tasmar)
81
Drug
List
azathioprine (Imuran)
cyclophosphamide (Cytoxan)
edrophonium (Enlon, Reversol)
neostigmine (Prostigmin)
pyridostigmine (Mestinon)
82
Drug
List
atomoxetine (Strattera)
clonidine (Catapres, Catapres-TTS)
desipramine (Norpramin)
dexmethylphenidate (Focalin), C-II
dextroamphetamine-amphetamine
(Adderall), C-II
83
Drug
List
imipramine (Tofranil)
methylphenidate (Concerta, Metadate,
Ritalin, Ritalin-SR), C-II
nortriptyline (Aventyl, Pamelor)
pemoline (Cylert), C-IV
84
Drug
List
riluzole (Rilutek)
85
Drug
List
baclofen (Lioresal)
glatiramer acetate (Copaxone)
interferon beta-1a (Avonex, Rebif)
interferon beta-1b (Betaseron)
mitoxantrone (Novantrone)
tizanidine (Zanaflex)
86
Drug
List
donepezil (Aricept)
galantamine (Reminyl)
ginkgo
memantine (Namenda)
rivastigmine (Exelon)
tacrine (Cognex)
87
Drugs
affecting
Peripheral
Nervous System
Drugs
88
Sympathetic:
(Adrenergic)
Activators
Sympthomimetics
Agonists
Blockers
Sympatholytic
Antagonists
Receptors
Alpha 1 & 2
Beta 1 & 2
Dopamine
Parasympathetic
(Cholinergic)
Activators
Parasympathomimetics
Agonists
Blockers
Anticholinergics
Antimuscarinics
Parasympatholytics
Antagonists
Receptors
Muscarinic
Nicotinic N & M
89
90
Neostigmine (Prostigmine)
(anticholinesterase) prototype
Pyridostimine (Mestinon)
Myasthenia Gravis
Donepezil (Aricept)
91
Limited uses:
Urinary retention
Increase GI peristalsis
Glaucoma, eye surgery
Adverse effects
Bradycardia, hypotension
Excess saliva, cramps, diarrhea
Urinary (contra: bladder obstruction &surgery)
Asthma exacerbation
93
Sources
Muscarinic agonists
Cholinesterase inhibitors
Mushrooms
Symptoms
Profuse salivation, tearing, bronchospasm,
diarrhea, bradycardia, hypotension
Treatment: atropine
94
Anticholinergics
Agents to know forever
95
96
Pharmacologic
effects:
heart rate
secretions (GI, tear,
salivary)
smooth muscle
(peristalsis, urination)
Dilate eye (mydriasis)
CNS excitability
Therapeutic Uses
Preanesthesia (make
sure heart doesnt stop)
Eye surgery: (dilate
eye)
Bradycardia: heart
rate
Intestinal hypertonicity,
hypermotility (slows GI
tract)
Muscarinic Agonist
Poisoning (antidote)
97
98
Dry as a bone
Red as a beat
Hot as a hare
Blind as a bat
Mad as a hatter
Treatment:
Minimize absorption
Cholinesterase inhibitor
99
Competitive antagonists
Sites of action
10
0
EXAMPLES
Acetylcholine antagonist
Antidysrhythmic
Antispasmotic
Antisecretory
10
1
USES
10
2
OXYBUTYNIN (DITROPAN)
Synthetic antimuscarinic
INCREASES BLADDER CAPACITY
DECREASES FREQUENCY OF VOIDING
10
3
Dose
dependent
Low dose
Glands: sweat,
salivary, bronchial
Heart
Eye
Bladder
Intestine motility
Lung
High dose
Stomach
10
4
Antihistamines
Phenothiazine antipsychotics
Tricyclic antidepressants
Furosemide (Lasix)
10
5
10
6
10
7
Treatment
Side effects cont
Muscarinic effects
Neuromuscular blockade (toxicity)
10
8
Neuromuscular Blockers
Paralyze muscle
10
9
11
0
Catecholamines:
Broken down by MAO
and COMT in liver and
intestine
Parenteral only
Cannot be given orally,
short half-life
Colorless solutions; color
is sign of oxidation
Natural catecholamines:
epi, norepi, dopamine
Synthetic: dobutamine
(others we dont need to
know)
Non-catecholamines
Can be given PO
Last longer in body
11
1
Noncatecholamines
Phenylephrine: (alpha1) nasal congestion,
inotropic support (rare now)
Pseudoephedrine (all alpha and beta):
Nasal congestion
Can be used to make amphetamines
11
2
-1
-2
-1
-2
Epinephrine
Dopamine
Dobutamine
Norepinephrine
dopa
+
+
11
3
Therapeutic effects
Vasoconstriction
BP (intensive care, last resort)
Hemostasis
local anesthesia absorption
Nasal decongestion
Mydriasis
Adverse effects
Hypertension
Necrosis
Bradycardia
11
4
Therapeutic Uses
Cardiac arrest (make heart beat again)
Heart Failure: inotropic support
Shock: inotropic and chronotropic support
A-V heart block (speed conductivity)
Adverse effects
HR
Angina pectoris
dysrhythmia
11
5
Therapeutic use
Asthma: bronchodilate
Preterm labor: stop contraction
Adverse effects
Hyperglycemia
Tremor
11
6
Therapeutic uses:
absorption of local
anesthetics
Control superficial
bleeding
BP
Mydriasis
AV block, V. fib,
Asystole
Status Asthmaticus
Anaphylactic shock
Reduce nasal
congestion
Adverse events
Hypertensive crisis
Dysrythmias
Angina pectoris
Necrosis
Hyperglycemia
11
7
Absorption
Inhalation: minimal
Injection
Preparations
SC, IM, IV, Intracardiac, intraspinal, inhalation,
Lidocaine with epi
No fingers, nose, penis, and toes
11
8
Interactions
MAO inhibitors (why oh why?)
Alpha-adrenergic blocking agents
Beta-adrenergic blocking agents
11
9
Adverse Effects
Dysrhythmias, angina pectoris
12
0
Short acting
Albuterol
Levalbuterol
Long acting
Salmeterol
Formoterol
12
1
12
2
Hypotensive state
Cardiac arrest (last resort)
12
3
12
4
Therapeutic uses
Hypertension
BPH
Reverse toxicity of
epinephrine
Pheochromocytoma
(what is it?)
Raynauds disease
Adverse effects
Orthostatic
hypotension
Reflex tachycardia
Nasal Congestion
Inhibition of
ejaculation
Na+ & H2O retention
12
5
Prazosin - HTN
Doxazosin HTN, BPH
Terazosin HTN, BPH
Tamsulosin BPH
Phentolamine Pheochromocytoma, tissue
necrosis
12
6
Therapeutic Uses
MI
HF
Angina Pectoris
Dysrhythmias
HTN
Other
Hyperthyroid
Migraine
Stage Fright
Pheochromocytoma
Glaucoma
12
7
Beta1, Beta2
Propanolol*
Nadolol
Pindolol
Labetalol
Carvedilol*
Selective
Metoprolol*
Atenolol*
Bisoprolol
Beta1,beta2,
alpha1
Used for HF
Metoprolol*
Carvedilol*
Clonidine
activates alpha-2 receptors in CNS
norepinephrine release
Uses
Hypertension
Pain relief in cancer (epdidural use only)
Adverse effects
Drowsiness, dry mouth, rebound HTN, bradycardia
Preparations
Oral: at least twice a day
Transdermal: seven days
12
9
Reserpine
Suppresses NE synthesis and promotes MAOmediated destruction
Crosses BBB
Effects
Hypotension
Adverse effects
Depression, sedation, apathy
Bradycardia, hypotension
13
0
Methyldopa, Methyldopate
Similar to clonidine, but are taken up in brain
stem neurons and converted to active alpha2
agonist
Use: HTN
Adverse effects
10 20% Positive Coombs test (5%) will go on to
have hemolytic anemia
Hepatotoxicity
Drowsiness, dry mouth, hypotension, etc.
13
1