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Butorphanol
Opioid analgesic Mixed opioid agonist-antagonist Partial agonist or antagonist @ opioid receptors Agonist @ receptors @ spinal & supraspinal sites Inhibits spinothalamic pain neurotransmission
Moderate-severe pain Admin intranasally respiratory depression, constipation, dependence than full receptor agonists Dysphoria Nightmares w/drawal in pts dependent on full opioid agonists AVOID MAOI
Potentially fatal
Dihydroergotamine
Antimigraine Ergot alkaloid 5-HT 1B/1D receptor agonist Activates 5-HT 1B/1D receptors
Pial & dural vessel constriction N, V Stiff neck, shoulder, extremities Leg weakness Numbness & tingling in fingers & toes
Presynaptic inhibition of trigeminal peptide neurotransmitter release Inhibitions brainstem activation of trigeminal neurons
Vascular HA
Migraine & cluster
Fentanyl
Opioid analgesic Phenylpiperidine Activates opioid receptors
Inhibits pain transmission @ spinal & supraspinal sites Chronic pain Breakthrough for cancer pain Transdermal patch Sedation Confusion Respiratory depression Anorexia N, V Constipation AVOID MAOI in past 14d
Meperidine
Opioid analgesic Strong opioid agonist Activates opioid receptors
Inhibits pain transmission Generalized CNS depression Moderate-severe pain Analgesia during labor Preoperative sedation Lacks antitussive activity Confusion Sedation Constipation N, V Dependence Toxic metabolite CNS excitation, convulsions, tremors AVOID MAOI
Potentially fatal
Methadone
Opioid analgesic Strong opioid agonist Activates opioid receptors
Inhibits pain transmission Suppresses opioid w/drawl Sx w/ euphoria or dependence Moderate-severe pain Prevention of opioid abuse Orally, once per day Respiratory depression Constipation Confusion Sedation AVOID MAOI
Morphine
Opioid analgesic Strong opioid receptor agonist Activates receptors
cAMP
Opens K & closes Ca channels release substance P
Naloxone
Opioid antagonist Opioid receptor antagonist Blocks opioid , , receptors Rapidly reverses effects of opioid agonists
Propoxyphene
Opioid analgesic Weak opioid agonist Activates opioid receptors
Inhibits pain transmission Mid-moderate pain Combined w/ acetaminophen or aspirin Dizziness Weakness N dependence
Sumatriptan
Antimigraine 5-HT 1B/1D receptor agonist Activates 5-HT 1B/1D receptors
Pial & dural vessel constriction Dizziness Vertigo Tingling Warm sensation Tight feeling head & chest Coronary vasospasm AVOID
MAOI SSRI
Presynaptic inhibition of trigeminal peptide neurotransmitter release Inhibitions brainstem activation of trigeminal neurons
Vascular HA
Migraine & cluster
Tramadol
Analgesic Dual action Activates opioid receptors
Inhibits neuronal reuptake 5-HT & NE inhibition of pain Moderate pain Chronic pain Naloxone reverses some but NOT all Sx Dizziness HA Constipation Lowers seizure threshold AVOID MAOI risk seizures w/ high doses
Penicillins Phenothiazines
Anesthetics
Benzocaine
Local anesthetic Ester-type Blocks Na channels & nerve conduction
Topical anesthetic
Pain Itching Inflammation
Burns Insect bites Contact dermatitis Wounds Irritates skin when 1st applied Use caution w/ sunburn & large areas of skin
Bupivacaine
Local anesthetic Amide-type Blocks Na channels & nerve conduction
Local or regional anesthetic
Surgical Diagnostic Obstetrical therapeutic
Halothane
General anesthetic Inhalational, halogenated hydrocarbon Potentiates GABA binding to GABA-A Cl ion channel
Suppresses sensory processing in thalamus General anesthetic High blood:gas partition coefficient Slow rate of induction & recovery Sensitizes heart to catecholamine-induced cardiac arrhythmia Hepatotoxic
Fluoride metabolites
Ketamine
IV anesthetic Glutamate antagonist Blocks glutamate NMDA receptors
Dissociate anesthesia Analgesia Immobility Amnesia Does NOT depression respiration or cause LOC Anesthesia Minor surgical & diagnostic procedures Children
Lidocaine
Local anesthetic Amide-type Blocks Na channels & nerve conduction
Topical Infiltration Nerve block Epidural Spinal anesthesia Eutectic mixture
Lidocaine & prilocaine Anesthetize intact skin for venipuncture IV cannulation Circumcism
Midazolam
Sedative-hypnotic-anxiolytic Short-acting BZDP Potentiates GABA binding to GABA-A Cl ion channel
Sedation Hypnosis Amnesia Preoperative sedation & anxiolysis Sedation of mechanically vented pts
Nitrous Oxide
Inhalation general anesthetic Anesthetic gas Potentiates GABA binding to GABA-A Cl ion channel
Suppresses sensory processing in thalamus Minor surgery & dental procedures
Propofol
General anesthesia IV anesthetic Diisopropyl phenol Potentiates GABA binding GABA-A Cl ion channel
Hypnosis Anesthesia Amnesia NO analgesic effect Intubation & maintenance of general anesthesia Sedation of intubated pts in ICU Bradycardia Hypotension
Sevoflurane
General anesthetic Inhalation anesthetic Potentiates GABA binding to GABA-A Cl channel
Suppresses sensory processing in thalamus Causes LOC General anesthesia
Anti-infective
Foscarnet Fosfomycin Ganciclovir Gentamicin Griseofulvin Imipenem-cilastatin Isoniazid Itraconazole Ivermectin Levofloxacin
Acyclovir
Antiviral Nucleoside analogue Converted to acyclovir triphosphate by viral & host cell kinases Incorporated into DNA by viral DNA polymerase causing DNA chain termination
HSV2 Herpes zoster
Shingles Chickenpox varicella
Albendazole
Antihelmintic Benzimidazole Binds & inhibits polymerization of tubulin dimmers to form cytoplasmic microtubules
Impairs glucose uptake & deplete glycogen stores Intestinal nematode infections
Hookworm Pinworm Whipworm Ascariasis Capillariasis
Trichinosis
Use w/ corticosteroid
Amantadine
Anti-influenza, antiparkinson Tricyclic amine Inhibits influenza-A M2 proton channel & acidification of virus particle
Prevents viral proteinprotein dissociation & uncoating of viral particles Influenza A Ataxia Dizziness Insomnia Skin mottling & livedo reticularis Blurred vision Dry mouth
Amoxicillin-clavulanate
-lactam ABX Extended spectrum aminopenicillin & -lactamase inhibitor Amoxicillin
Binds PBP
Inhibits cross-linking of cell wall peptidoglycan
Clavulanate
Inhibits class-A -lactamase
Protects amoxicillin from destruction
Amphotericin B
Antifungal Polyene ABX Binds ergosterol & membrane permeability
Leakage of cell contents Candidiasis Cryptococcal meningitis Aspergillosis Blastomycosis Coccidioidomycosis Histoplasmosis Mucormycosis Chills Fever Diarrhea N, V Nephrotoxicity Hypokalemia toxicity w/ cyclosporine, antineoplastics Thiazides, & corticosteroids hypokalemia
Azithromycin
Macrolide Protein synthesis inhibitor Binds 50s ribosome Prevents peptide elongation & translocation from acceptor site to peptidyl site
Respiratory infections d/t strep, pneumo, H. influenzae, Legionella
Otitis media, sinusitis
Aztreonam
-lactam ABX Monobactam Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Drug resistant gram (-) infections including Pseudomonas aeruginosa & Enterobacteriaceae Thrombophlebitis Allergic rxn
Caspofungin
Antifungal Echinocandin Inhibits synthesis of cell wall component
-1,3-D-glucan Candida albicans Invasive aspergillosis IV admin
Not absorbed well by gut
Cefazolin
-lactam ABX 2nd generation cephalosporin Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Surgical wound infections Infections d/t
Staph, strep, E. coli, Klebsiella pneumoniae, Proteus mirabilis
Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels
Cefepime
-lactam ABX 4th generation cephalosporin Binds multiple PBP Inhibits cross-linking of cell wall peptidoglycan Resistant to many lactamases
Drug-resistant gram (-) bacteria
Citrobacter Enterobacter
Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels
Ceftazidime
-lactam ABX 3rd generation cephalosporin Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Gram (+), gram (-), & anaerobics Pseudomonas aeruginosa Pneumonia, meningitis, UTI, skin structures, bones, jts Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels
Cetriaxone
-lactam ABX 3rd generation cephalosporin Binds PBP including transpeptidase Inhibits cross-linking of cell wall peptidoglycan
Infection d/t
Pneumococci, gonococci, meningococci, H. influenzae, Moraxella catarrhalis, Borrelia burgdorferi
Rash Diarrhea Pseudomembranous colitis Superinfection Probenecid inhibits excretion & serum levels
Ciprofloxacin
Antibacterial Fluoroquinolone Inhibits bacterial DNA topoisomerase type II (DNA gyrase) & type IV Prevents DNA replication & separation of chromosomes
Urinary tract, prostate, intraabdominal w/ metronidazole, bone or jt, skin Inhalational anthrax Gonorrhea Infectious diarrhea Gram (+), gram (-), Pseudomonas aeruginosa Insomnia Diarrhea N Absorption by cations
Antacids Iron Zinc bismuth
Clindamycin
Aminosugar ABX Protein synthesis inhibitor Binds 50s ribosome Prevents translocation of nascent peptide from acceptor site to peptidyl site
Strep, staph, gram (+) Acne vulgaris Anaerobes including Bacteroides C. difficile superinfection Diarrhea Pseudomembranous colitis
Doxycycline
Tetracycline ABX Protein synthesis inhibitor Binds 30s ribosome Reversibly inhibits binding of transfer RNA to acceptor site
Rickettsia, Chlamydia, Mycoplasma, Borrelia Acne Cholera Gonorrhea & syphilis in PCN allergic pts Brucellosis & ehrlichiosis AVOID
Pregnancy & children > 8 y/o Outdated preparations are nephrotoxic
Efavirenz
Antiretroviral Non-nucleoside reverse transcriptase inhibitor Binds reverse transcriptase & disrupts catalytic site
HIV in combo w/ nucleoside reverse transcriptase inhibitor synergistic High fat meal absorption N Rash Drowsiness Depression
Enfuvirtide
Antiretroviral HIV fusion inhibitor Binds HIV virus gp41 & blocks fusion of HIV w/ host cells CD4 Thelper lymphocytes
Drug-resistant HIV Injection site rxn
Rotate sites daily
Erythromycin
Macrolide ABX Protein synthesis inhibitor Binds 50s ribosome Prevents peptide elongation & translocation from acceptor site to peptidyl site
Pharyngitis, otitis media, sinusitis, pneumonia d/t
Strep, pneumococci, Mycoplasma, Chlamydia, Legionella, MAI
Ethambutol
Antitubercular Synthetic butanol derivative Bacteriostatic against mycobacteria Inhibits RNA synthesis
M. tuberculosis MAI Dose-related retrobulbar optic neuritis Impaired red-green color discrimination
Monitor pts color discrimination regularly
Gouty arthritis
Foscarnet
Antiviral Pyrophosphate Blocks pyrophosphatebinding site on viral DNA polymerase
Prevents attachment of nucleotide precursors to DNA CMV retinitis in HIV pts Acyclovir-resistant HSV in immunocompromised HA Diarrhea V Renal failure Hypocalcemia Hypokalemia Hypomagnesemia Anemia Arthralgia Myalgia Pentamidine causes lifethreatening hypocalcemia
Fosfomycin
ABX Cell wall synthesis inhibitor Inhibits enopyruvyl transferase & addition of phosphenolpyruvate to Nacetylglucosamine to form N-acetylmuramic acid
Cystitis d/t E. coli or Enterococcus faecalis Single dose Tx for UTI
Ganciclovir
Antiviral Nucleoside analogue Converted to ganciclovir triphosphate
Inhibits viral DNA polymerase CMV infection in immunocompromise d & transplants visual acuity Neutropenia Thrombocytopenia Anemia
Gentamicin
Aminoglycoside ABX Protein synthesis inhibitor Binds 30s ribosome Prevents initiation of protein synthesis
Misreading of genetic code Gram (-) bacilli including Enterobacteriaceace & P. aeruginosa Strep, enterococcal, & staph infections Monitor serum levels Nephrotoxicity Ototoxicity
Vestibular & cochlear w/ loop diuretics
Griseofulvin
Antifungal Fungistatic ABX Deposits in keratin precursor cells of skin, hair, & nails Disrupts microtubules & mitotis of dermatophytes
Dermatophyte infections NOT Candida HA Induces CYP450
Reduces plasma levels warfarin & OCP
Imipenem-cilastatin
-lactam ABX Carbapenem ABX & dehydropeptidase inhibitor Imipenem
Binds PBP & inhibits crosslinking cell wall peptidoglycan Allergic rxns Diarrhea V Seizures
risk w/ ganciclovir or cyclosporine
Cilastatin
Inhibits renal dehydropeptidase & degradation of imipenem Endocarditis, pneumonia, UTI, pelvic, abdominal d/t aerobic & anaerobic
Isoniazid
Antitubercular Nicotinic acid derivative Reduces catalaseperoxidase
Inhibits synthesis of mycolic acid component of cell wall TB Bimodal distribution d/t fast & slow acetylation Inactivates vit. B6 Hepatitis
Toxic metabolite acetylhydrazine
Peripheral neuropathy
Vit. B6 deficiency
Itraconazole
Antifunal Synthetic triazole Inhibits 14--demethylase
CYP450 enzyme that converts lanosterol ergosterol Blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis Onychomycosis nail beds GI distress Rash Hepatitis
Ivermectin
Antiparasitic Antihelmintic ABX Activates glutamate-gated Cl ion channel
Pharyngeal m. hyperpolarization & paralysis Strongyloidiasis Cutaneous larva migrans Onchocerciasis filiariasis
W. bancrofti
Vertigo Sedation
Levofloxacin
Antibacterial Fluoroquinolone Inhibits bacterial DNA topoisomerase type II (DNA gyrase) & type IV Prevents DNA replication & separation of chromosomes
Community-acquired pneumonia UTI Gynecologic & skin infections Gram (+), gram (-), P. aeruginosa, Mycoplasma, Mycobacterium
Linezolid
Antibacterial Oxazolidinone protein synthesis inhibitor Binds 23s ribosomal RNA of 50S subunit
Prevents formation of 70s initiation complex VRE, MS/MRSA, PCNsensitive pneumococci Inhibits MAO
Mefloquine
Antimalarial 4-quinolone methanol derivative Inhibits erythrocytic schizogony Inhibit nucleic acid synthesis
Malaria Chloroquinesusceptible/resistant trains of P. falciparum & P. vivax Perform CBC during chronic prophylactic Tx Neuropsychiatric syn
Hallucination Anxiety Confusion Seizure Coma
Metronidazole
Antiprotozoal Nitroimidazole Reduced by pyruvate:ferredoxin to form nitro-free radicals that attack DNA & proteins
Amebiasis, giardiasis, trichomoniasis Balantidium coli, C. difficile, B. fragilis GI pain Anorexia N Dizziness Alcohol causes disulfiram-like effect
Mupirocin
ABX Protein synthesis inhibitor Competes w/ isoleucine for binding bacterial isoleucyl tRNA synthetase Prevents addition of isoleucine during protein synthesis
Impetigo by staph or strep Eradicate nasal colonization of MRSA Infected traumatic skin lesions
Nafcillin
-lactam ABX Antistaphylococcal, penicillinase-resistant penicillin Binds PBP
Inhibits cross-linking of cell wall peptidoglycan Methicillin-sensitive penicillinase producing staph
Bone, jt, UTI, respiratory, skin, endocarditis, meningitis
Nitrofurantoin
Urinary tract antibacterial Nitrofuran Inhibits bacterial enzymes
UTI
E. coli, S. saprophyticus
Oseltamivir
Antiviral Neuraminidase inhibitor Inhibits influenza A & B neuraminidase
Prevents release & spreading of viral particles Influenza A & B
Paromomycin
Antiprotozoal Aminoglycoside ABX Inhibits protein synthesis
Intestinal amebiasis Cryptosporidiosis in immunocompromised pts Nephrotoxic & ototoxic if given IV
Penicillin G
-lactam ABX Narrow-spectrum penicillin Binds PBP
Inhibits cross-linking of cell wall peptidoglycan Strep, pneumococcal, meningococcal Syphilis Diarrhea Superinfection Pseudomembranous colitis Allergic rxn
Rash Serum sickness Anaphylaxis
Pentamidine
Antiprotozoal Amidino-pentane derivative Disrupts nucleic acid synthesis in protozoa
P. carinii Early stage African trypanosimiasis sleeping sickness Nephrotoxic Hematologic toxicity Hypoglycemia Allergic rxn
Anaphylaxis
Piperacillin-tazobactam
-lactam ABX Antipseudomonal penicillin & lactamase inhibitor Piperacillin
Binds PBP
Inhibits cross-linking of cell wall peptidoglycan
Tazobactam
Inhibits class A -lactamases Gram (-) bacilli, P. aeruginosa
Praziquantel
Antihelmintic Isoquinoline derivative Ca permeability of schistosome tegument
Contraction & exposing antigens to host immunity Schistosomiasis Chinese liver fluke Lung fluke Cestodes tapeworms Malaise Anorexia Drowsiness dizziness
Primaquine
Antimalarial 8-aminoquinoline Converted to oxidizing quinoline-quinone intermediates
Eradicate exo-erythrocytic forms of P. vivax & P. ovale Hemolytic anemia in G6PD deficiency methemoglobinemia
Pyrimethamine
Antiprotozoal Folate reductase inhibitor Inhibits folate reductase Folate deficiency in protozoa
Malaria in combo w/ sulfadoxine Toxoplasmosis in combo w/ sulfadoxine NOT effective against P. vivax N Anorexia Hypersensitivity rxn
Pyrantel
Antihelmintic Pyrimidine analogue Activates cholinergic nicotinic receptors in somatic m. of nematodes Produces depolarizing NM blockade
Ascariasis Hookworm & pinworm Abdominal cramps Anorexia Diarrhea V
Quinine
Antimalarial 4-aminoquinoline Binds plasmodial DNA & prevents replication & transcription during erythrocytic schizogony
Chloroquine-resistant malaria Admin w/ doxycycline or pyrimethamine-sulfadoxine Abdominal cramps Diarrhea V Cinchonism
Tinnitus Blurred vision
Metabolism
Cimetidine inhibits Rifampin induce
Quinupristin-dalfopristin
Streptogramin ABX Protein synthesis inhibitor Binds 50s ribosomal subunit Quinupristin
Inhibits aminoacyl tRNA synthesis & addition of AA Infusion site rxn
Dalfopristin
Inhibits peptidyl transferase VRE, MS/MRSA
Ribavirin
Broad-spectrum antiviral Guanosine analogue Converted to ribavirin triphosphate Depletes guanosine triphosphate Inhibits viral RNA & protein synthesis
RSV in infants or children Chronic hepatitis C Viral hemorrhagic fever Lass fever Anemia Hypotension Cardiac arrest
Rifampin
Antitubercular Rifampin derivative Inhibits DNA-dependent RNA polymerase
TB Leprosy Prophylaxis meningococcal meningitis & H. flu B infections Red discoloration of tears, urine, saliva, sweat Abdominal pain V Diarrhea Hepatitis Induces CYP450 levels
Warfarin Theophylline Itraconazole Steroids Opioids Phenytoin Verapamil
Ritonavir-lopinavir
Antiretroviral HIV protease inhibitor Inhibits HIV protease & conversion of gag-pol polyprotein to functional proteins Ritonavir
lopinavir levels HIV in combo w/ nucleoside reverse transcriptase inhibitor Anorexia V Altered taste Abnormal thinking Hyperlipidemia Hyperlgycemia
Streptomycin
Aminoglycoside Protein synthesis inhibitor Binds 30s ribosome Prevents initiation of protein synthesis
Misreading of genetic code Drug-resistant TB Plague Tularemia IV admin Nephrotoxic Ototoxic
w/ loop diuretics
Terbinafine
Antifungal Allylamine Inhibits squalene oxygenase & formation of squalene epoxide during fungal membrane ergosterol synthesis
Topical
Tinea corporis, cruris, pedis, versicolor
Oral
Onychomycosis fungal nail infection
Trifluridine
Antiviral Thymidine analogue Inhibits HSV DNA polymerase
Herpetic keratitis Keratoconjunctivitis Topical ocular admin Ocular irritation
Redness Itching
Trimethoprim-sulfamethoxazole
Antibacterial Folate antagonist Sulfamethoxazole
Inhibits folate synthesis N, V Rash Stevens-Johnson syn Allergic rxn Anemia
Hemolytic anemia Megalobalstic anemia
Trimethoprim
Inhibits folate reduction UTI, travelers diarrhea Shigella enteritis P. carinii & Nocardia pneumonia
Vancomycin
Glycopeptide ABX Cell wall synthesis inhibitor Binds D-alanyl-D-alanine portion of peptidoglycan Prevents cross-linking of D-alanine & pentaglycine chain
MRSA, penicillin-resistant enterococci, C. difficile Red man syn
Extensive rate of infusion Erythematous rash on face & upper body
Ototoxicity
Vestibular & cochlear
Zidovudine
Antiretroviral Nucleoside reverse transcriptase inhibitor Activated nucleotide triphosphate incorporated into DNA causing chain termination
HIV Prevent maternal-fetal HIV transmission 1st line Tx for HIV infections
Zidovudine w/ lamivudine or emtricitabine & efavirenz or lapinavir-ritonavir
Anemia
Antineoplastic
Anastrozole Bleomycin Busulfan Carmustine Cisplatin Cyclophosphamide Doxorubicin Etoposide Fluorouracil Gemtuzumab ozogamicin
Anastrozole
Estrogen antagonist Nonsteroidal aromatase inhibitor Inhibits aromatase & conversion to estrone precursor to estradiol Lowers estrogen levels Halts progression of estrogen-sensitive breast cancers
Breast cancer in postmenopausal women
Bleomycin
Antitumor DNA intercalating Complexes ironforming oxygen free radicals that cause single strand breaks G2 phase specific
Lymphomas SCC Testicular carcinoma Choriocarcinoma
Pneumonitis & pulmonary fibrosis Hyperpigmentation Mucocutaneous toxicity Hematology toxicity
Busulfan
Antineoplastic Alkyl sulfonate bifunctional alkylating agent Cross-links DNA strands by covalently bonding guanine residues Prevents DNA replication & transcription
CML Use w/ cyclophosphamide prior allogenic hematopoietic progenitor cell transplant for CML
Carmustine
Antineoplastic Nitrosurea bifunctional akylating agent Cross-links DNA strands by covalently bonding guanine residues Prevents DNA replication & transcription
Brain tumors Myeloma Lymphoma Causes prolonged myelosuppression
Cisplatin
Antineoplastic Platinum compound Forms reactive metabolites that covalently bond DNA bases & cross-link DNA strands
Testicular, ovarian, cervical, bladder, lung, head/neck cancers Less bone marrow suppression
Cyclophosphamide
Antineoplastic Nitrogen mustard bifunctional akylating agent Cross-links DNA strands by covalently bonding guanine residues Prevents DNA replication & transcription
Hodgkins ds Lymphomas, myeloma Leukemia Ovarian & breast tumors RA Converted to active metabolites by CYP enzymes Anorexia N, V Hemorrhagic cystitis & hematuria Alopecia Thrombocytopenia Leukopenia Anemia Rifampin induces CYP & toxicity
Doxorubicin
Antitumor DNA intercalating agent Inserts b/w DNA bases
Causes deformation & uncoupling
Colors urine red Cardiomyopathy doselimiting Anemia Leukopenia Thrombocytopenia Diarrhea V Stomatitis Alopecia
Complexes iron forming hydroxyl free radicals that cause strand breaks Inhibits topoisomerase II
Causes strand breaks
S phase specific
Breast, ovarian, bladder tumors Bronchogenic carcinoma Lymphoma & leukemia
Etoposide
Antineoplastic Podophyllotoxin, topoisomerase inhibitor Inhibits mammalian topoisomerase II & prevents resealing of nicked DNA strands G2 phase specific
Testicular, small cell lung carcinoma Lymphoma Leukemia
Fluorouracil
Antineoplastic Pyrimidine antimetabolite Converted to active nucleotide form
Inhibits thymidylate synthetase
S phase specific
Colon, breast, rectal, gastric, pancreatic cancer Topical for basal cell carcinoma & actinic keratosis
Gemtuzumab ozogamicin
Antineoplastic Monoclonal Ab & cytotoxic ABX calicheamicin Gemtuzumab
Binds CD33 Ag on hematopoietic cells & sequesters lysosomes where calicheamicin is released
Calicheamicin
Causes DNA dbl strand breaks CD33 (+) AML
Imatinib
Antineoplastic Tyrosine kinase inhibitor Inhibits oncoprotein bcr-abl tyrosine kinase expressed by Philadelphia chromosome Inhibits leukemic cell proliferation & induced apoptosis
CML
Cause hematologic & cytogenetic remission
Cough Dyspnea Pharyngitis Pneumonia Abdominal pain V Petechiae Pruritis Rash Night sweats Myalgia Arthralgia Thrombocytopenia Neutropenia
Leuprolide
Antineoplastic, agent for precocious puberty GnRH analogue Pulsatile admin FSH & LH release Continuous admin downregulates GnRH receptors & FSH & LH
Central precocious puberty Advanced prostate cancer Endometriosis Uterine fibroids IM depot & implants for prostate cancer Transient in testosterone w/ 1st dose
Use flutamide or other androgen antagonist
Hot flashes
Mercaptopurine
Antineoplastic Purine antimetabolite Converted to nucleotide triphosphate by phosphoribosyl transferase Inhibits purine biosynthesis & salvage pathways S phase specific
Acute leukemia CML Lymphomas Tumors that delete phosphoribosyl-transferase acquire resistance Cross-react w/ thioguanine Myelosuppression Hyperuricemia Hepatotoxicity Allopurinol inhibits degradation
Methotrexate
Antineoplastic Folate reductase inhibitor Inhibits dihydrofolate reductase Prevents formation of active folate & addition of single carbon units to DNA base precursors S phase specific
Choriocarcinoma, trophoblastic tumors Leukemia Breast, head, neck, lung cancers Severe psoriasis RA Mycosis fungoides Leucovorin used to minimized hematologic toxicity & Tx OD
Paclitaxel
Antineoplastic Mitotic inhibitor Binds tubulin & prevents depolymerization of microtubules of mitotic spindle M phase specific
Advanced ovarian cancer w/ cisplatin Non-small-cell lung cancer Metastatic ovarian or breast cancer
Tamoxifen
Antineoplastic Estrogen receptor antagonist & partial agonist Competes w/ estrogen for receptors in breast & other tissues Suppresses breast tumor growth
Breast cancer & ductal carcinoma following surgery & radiation Advanced breast cancer
Trastuzumab
Antineoplastic Monoclonal Ab Binds human epidermal growth factor-2 (HER2) receptor on breast cancer cells Prevents receptor stim. & cell proliferation Regression of breast cancer metastases
Metastatic breast cancer w/ overexpression HER2 Combined w/ paclitaxel
blood levels
Abdominal pain Anorexia Diarrhea V Back pain Chills Fever Allergic rxns Doxorubicin risk of cardiotoxicity
Vincristine
Antineoplastic Vinca alkaloid, mitotic inhibitor Binds tubulin & prevents polymerization of tubulin dimers forming microtubules of mitotic spindle M phase specific
Hodgkins ds Lymphoma Leukemia Neuroblastoma Rhabdomyosarcoma Wilms tumor
Atenolol
Sympatholytic, antihypertensive 1 receptor antagonist 1 receptor antagonist
Angina Post MI Hypertension
Atropine
Anticholinergic Muscarinic receptor antagonist Muscarinic receptor blocker
Bradycardia IBS Anticholinesterase poisoning Antisecretory agent
Mydriasis & cycloplegia Warm, dry, flushed skin Tachycardia Delirium Hallucinations
Dobutamine
Sympathomimetic, cardiac stimulant 1 receptor agonist Selective 1 receptor agonist
1 > 2 > 1 Cardiac contractility & output Acute heart failure Cardiogenic shock Synergistic on cardiac output w/ nitroprusside Tachycardia Arrhythmia
Edrophonium
Diagnostic agent Cholinesterase inhibitor Reversible cholinesterase inhibitor
Dx myasthenia gravis Muscarinic effects
Miosis Salivation
Epinephrine
Sympathomimetic, bronchodilator, vasopressor Nonselective adrenergic agonist Activates & receptors
IP3 & cAMP 1 vasoconstrict & BP 1 HR, conduction, & contractility 2 vasodilate, BP, bronchodilate Cardiac arrest, V fib Shock, asthma COPD
Phenoxybenzamine
Vasodilator Irreversible receptor antagonist receptor antagonist
1 > 2
Presurgical Tx of HTN d/t pheochromocytoma
Phentolamine
Vasodilator receptor antagonist Blocks 1 & 2 receptors
Control BP during surgical removal of pheochromocytoma IV admin only Hypotension Severe hypotension w/ Epi
Phenylephrine
Vasocontrictor, decongestant Selective 1 receptor
Rebound nasal congestion HTN MAOI cause severe HTN
agonist
Activates 1 receptor
Increase IP3 causing contraction of vascular smooth m. Nasal & ocular decongestant Dilate pupil for opthalmoscopy Mydriasis w/o cycloplegia
Paralysis of accommodation
Pilocarpine
Antiglaucoma, sialogogue Muscarinic receptor agonist Activates muscarinic receptors in ciliary m. & salivary gland
Sjogrens syn
Glaucoma
Ciliary m. aqueous humor
Xerostomia
Salivary gland salivation
Pralidoxime
Organophosphate antidote Cholinesterase reactivator Binds phosphorous & breaks organophosphate bond w/ cholinesterase
Organophosphate toxicity Reverses muscle weakness
Propranolol
Sympatholytic, antihypertensive Nonselective receptor antagonist Blocks 1 & 2 receptors
Angina HTN Benign tremor Migraine prophylaxis thyrotoxicosis Post-MI Highly lipophilic effects CNS Bronchoconstriction Inhibits glycogenolysis Nightmares & depression
Pseudoephedrine
Decongestant Indirect/direct-acting adrenergic receptor agonist release NE directly activates adrenergic receptors causing vasoconstriction & cardiac stim.
Allergic & viral rhinitis Tachycardia CNS stim. BP MAOI cause severe HTN
Pyridostigmine
Antimyasthenic Cholinesterase inhibitor, cholinergic agonist Reversibly inhibits cholinesterase
Tx myasthenia gravis Reverse nondepolarizing NM blockers Muscarinic effects
Miosis Salivation
Rocuronium
Paralytic agent Nondepolarizing NM blockade Blocks nicotinic receptors in skeletal m.
Skeletal m. relaxation for intubation, surgery, ECT Effects reversed by neostigmine & edrophonium
Sildenafil
Vasodilator Phosphodiesterase inhibitor Inhibits type 5 phosphodiesterase & degradation of cGMP
vasodilation in corpus cavernosum d/t Ach release from sacral PNS neurons Erectile dysfunction HA Nasal congestion Back pain Visual disturbances
Succinylcholine
Paralytic agent Depolarizing NM blockade Binds nicotinic receptors causing prolonged depolarization of skeletal m. & paralysis
Skeletal m. relaxation for intubation & surgery Transient m. fasciculations
Tamsulosin
Urologic agent Uroselective 1 receptor antagonist Blocks 1A receptors in prostate
Tx urinary outflow obstruction d/t prostatic hyperplasia Dizziness HA Postural hypotension Cimetidine increases blood levels & effects
Terazosin
Antihypertensive, urologic agent Selective 1 receptor antagonist Blocks 1 receptors
HTN Outflow obstruction d/t prostate hyperplasia 1st dose syncope
Cardiovascular
Acetazolamide Adenosine Amiloride Amiodarone Amlodipine Carvedilol Clonidine Digoxin Diltiazem Dofetilide Enalapril Esmolol Fenoldopam Furosemide Hydralazine
Hydrochlorothiazide Labetalol Mannitol Methyldopa Minoxidil Nesiritide Nitroglycerin Nitroprusside Propafenone Quinidine Sotalol Spironolactone Valsartan verapamil
Acetazolamide
Diuretic Carbonic anhydrase inhibitor Inhibits interconversion of carbonic acid & bicarbonate NaHCO3 excretion Inhibit aqueous humor formation Hyperchloremic metabolic acidosis
Tx open-angle glaucoma Mtn sickness Metabolic alkalosis
Adenosine
Antiarrhythmic Purine nucleoside, cardiac node membrane stabilizer Opens K channels & blocks Ca influx in SA & AV nodes Slows AV conduction AV refractory period
Terminate SVT
Transient asystole
Amiloride
K-sparring diuretic Epithelial Na channel blocker Blocks Na Channel distal tubule & collecting duct
Inhibits Na reabsorption & K excretion Prevent & Tx hypokalemia Hyperkalemia
Amidarone
Antiarrhythmic Cardiac ion channel blocker Blocks K, Na, Ca channels & receptors
Prolongs repolarization refractory period Slows HR PR & QT intervals SVT, VT, VF Hypo/hyperthyroidism Photosensitivity Blue-gray skin Corneal microdeposits Pulmonary fibrosis
Amlodipine
Antihypertensive, antianginal Dihydropyridine Ca channel blocker Ca channel blocker in vascular smooth m. Arteriolar vasodilation & coronary blood flow
HTN Angina pectoris HA Edema Hypotension Effects w/ grapefruit juice
Carvedilol
Antihypertensive & heart failure Tx Nonselective adrenergic receptor agonist Blocks 1, 2, 1 receptors Cause vasodilation
HTN Heart failure
remodeling
Clonidine
Antihypertensive 2 receptor agonist Central 2 receptor agonist
sympathetic outflow from vasomotor center Inhibits pain neurotransmission in spinal cord HTN Opioid w/drawal
Digoxin
Cardiac stimulant Digitalis glycoside Inhibits Na/K ATPase
IC Ca & cardiac contractility AV conduction AV refractory period Heart failure Serum levels assess dosage & toxicity Arrhythmias N, V Blurred vision Yellow vision
Diltiazem
Vasodilator, antiarrhythmic Non-dihydropyridine Ca channel blocker Block Ca channels in cardiac tissue & vascular smooth m.
Vasodilation HR & conduction contractility HTN Angina pectoris SVT
Dizziness Hypotension Peripheral edema Constipation Gingival hyperplasia Grapefruit juice serum levels
Dofetilide
Antiarrhythmic K channel blocker Blocks delayed K channels in cardiac tissue
Slows repolarization & prolongs refractory period QT interval AF, A flutter Monitor QT interval during initial dose titration
Enalapril
Antihypertensive ACE inhibitor Inhibits ACE & formation of AT II
Vasodilation aldosterone secretion CO V remodeling survival in heart failure HTN Heart failure Post-MI progression of diabetic nephropathy
Esmolol
Antiarrhythmic Class II Selective 1 blocker Blocks SNS stim. SA & AV nodes
HR AV conduction AV refractory period Sinus tachycardia & SVT during/after surgery Rapidly metabolized by plasma esterase
Hypotension Bradycardia
Fenoldopam
Antihypertensive D1-like receptor agonist D1 receptor agonist
Arteriolar vasodilation
Afferent & efferent renal arterioles
serum K levels
Monitor for hypokalemia
Furosemide
Loop-acting diuretic Membrane ion transport inhibitor Inhibits Na/K/2Cl cotransporter in ascending loop of Henle
Blocks NaCl reabsorption Edema Heart failure HTN Hypercalcemia Ca excretion Na/K exchange in collecting duct
Hydralazine
Antihypertensive. heart failure Vasodilator Alters IC Ca metabolism
Relaxes arteriolar smooth m.
vasodilation
Moderate-severe HTN
Hydrochlorothiazide
Antihypertensive Thiazide diuretic Inhibits NaCl transporter in distal tubule
excretion Na, K, Cl Ca excretion HTN Nephrogenic DI Nephrolithiasis Hypokalemia Metabolic alkalosis Hyperuricemia & gout excretion of lithium
Labetolol
Antihypertensive Adrenergic & receptor antagonist Selective 1 & nonselective 1, 2 blockers
HTN Postural hypotension Abrupt w/drawal cause life-threatening HTN, arrhythmias, or MI
Mannitol
Diuretic Osmotic Diuretic Osmotic attraction of edematous & ocular fluid
Filtered by glomerulus
electrolyte excretion Oliguric renal failure Cerebral edema ICP Acute glaucoma
Methyldopa
Antihypertensive Adrenergic 2 receptor agonist Converted to active form methylnorepinephrine which activates central 2 receptor agonist
SNS outflow from vasomotor center HTN HTN in pregnancy Positive direct Coombs test
Minoxidil
Antihypertensive, hair growth stimulant Vasodilator, K channel opener Opens K channels in vascular smooth m.
Hyperpolarization m. relaxation vasodilation
Systemic admin.
Reflex tachycardia Angina pericarditis Pulmonary HTN hypertrichosis
Nesiritide
Heart failure Tx Recombinant human B-type natriuretic peptide Activate guanylate cyclase cGaMP
Dilates venous & arterial smooth m. venous pressure, cardiac preload, vascular congestion, & dyspnea Decompensated heart failure
Hypotension
Nitroglycerin
Antianginal Organic nitrate
Nitroprusside
Antihypertensive Vasodilator Relaxes venous & arteriolar smooth m.
Metabolized to CN & thiocyanate
Tx toxicity w/ sodium nitrite & sodium thiosulfate
CN toxicity Hypotension HA
HTN crisis Acute heart failure or cardiogenic shock Controlled hypotension during pregnancy
Propafenone
Antiarrhythmic Class IC Na channel blocker Blocks Na channel in cardiac tissue conduction & prevent re-entry PR, QRS, & QT duration
SVT & life-threatening V arrhythmias
Proarrhythmic 1st 2 wks
Monitor ECG when starting Tx
Quinidine
Antiarrhythmic Class IA Na channel blocker Blocks Na & K channels in cardiac tissue conduction QRS & QT duration
SVT & VT D-isomer = quinine, used to treat malaria pts
Cinchonism
Blurred vision Tinnitus Photophobia
levels w/
Amiodarone Cimetidine Diltiazem Verapamil Grapefruit juice
Sotalol
Antiarrhythmic Class III K channel blocker Blocks K channels in cardiac tissue
Prolongs repol. refractory period & QT interval
Torsades de pointes
Spironolactone
K-sparring diuretic Aldosterone antagonist Blocks aldosterone receptors Na excretion K excretion
Primary hyperaldosteronism HTN hypokalemia Gynecomastia Impotence Hyperkalemia
Valsartan
Antihypertensive Angiotensin receptor antagonist Blocks AT II receptor in vascular smooth m. & adrenal cortex
Vasodilation & aldosterone secretion HTN Nephropathy Less cough & angioedema than ACEI
Verapamil
Antihypertensive, antianginal Non-dihydropyridine Ca channel blocker Blocks Ca channels in cardiac m. & vascular smooth m.
Vasodilation HR & conduction contractility
Suppress contractility more than other Ca channel blockers
CNS Depressants
Busprione
Antianxiety 5-HT1A partial agonist Activates presynaptic 5-HT1A receptors in dorsal raphe nucleus
firing serotonergic neurons Generalized anxiety disorder NO
Drug dependence Significant sedation Muscle relaxation Anticonvulsant effects
Dizziness Drowsiness Fatigue HA Excitement Nervousness Blurred vision Tachycardia N Rash Myalgia Sweating levels by
Erythromycin Itraconazole Grapefruit juice
Carbamazepine
Anticonvulsant Neuronal Na channel blocker Blocks Na channels in CNS
firing of ectopic foci & spread of epileptic seizures Partial seizures & generalized tonic-clonic seizures Bipolar disorders Trigeminal neuralgia Neuropathic pain Ataxia Drowsiness Blurred vision Agranulocytosis Aplastic anemia Thrombocytopenia Induces its own metabolism
Diazepam
Antianxiety Benzodiazepine Binds receptors on GABA operated Cl ion channel
channel affinity for GABA & frequency of channel opening Potentiates inhibitory effects of GABA Anxiety Status epilepticus Muscle spasm Alcohol w/drawal Anterograde amnesia Long-lasting active metabolites Drowsiness Lethargy Physical/psychological dependence Tolerance
Disulfiram
Alcohol abuse Tx Acetaldehyde dehydrogenase inhibitor Inhibits acetaldehyde degradation following alcohol ingestion
Blurred vision Chest pain Dizziness Palpitations N, V HA Weakness Reinforcement of alcohol abstinence Drowsiness
Ethosuximide
Anticonvulsant Succimide Binds T-type Ca channels in thalamic neurons Suppresses nerve transmissions to motor cortex
Generalized absence seizures
Petit mal epilepsy
Flumazenil
Antidote Benzodiazepine receptor antagonist Blocks benzodiazepine receptors
Counteract adverse effects of benzodiazepines
Respiratory depression d/t IV OD
CI in status epilepticus
Gabapentin
Anticonvulsant GABA analogue GABA release from central neurons
Inhibits neuronal discharges from seizure foci Inhibits pain neurotransmission Partial seizures Chronic pain Migraine prophylaxis Ataxia Dizziness Drowsiness Nystagmus Tremor
Lamotrigine
Anticonvulsant Phenyltriazine Blocks voltagesensitive Na channels
Release of glutamate Prevents spread of seizure foci discharges Adjunct/monotherapy for partial seizures in adults Skin rash in 1st 8 wk of Tx
Can progress to Stevens-Johnson syn
Lorazepam
Sedative-hypnotic, anxiolytic Benzodiazepine Binds benzodiazepine receptors on GABA operate Cl ion channel
channel affinity for GABA & frequency of channel opening Potentiates inhibitory effects of GABA Anxiety Insomnia Preoperative sedation Light anesthesia Anterograde amnesia Flumazenil used to counteract severe OD
Dizziness Drowsiness Apnea & cardiac arrest w/ rapid IV admin Additive depression w/ alcohol & other depressants
Phenobarbital
Sedative-hypnotic, anticonvulsant Barbiturate Binds GABA operated Cl ion channel increasing duration of channel opening
Cl influx in absence of GABA Tonic-clonic & partial seizures Febrile seizures in children Preoperative sedation Short-term hypnotic folate requirement during long-term Tx
Drowsiness Lethargy Delirium Hangover Physical & psychological dependence Induces CYP P450 metabolism of drugs
Phenytoin
Anticonvulsant Hydantoin Blocks voltage-sensitive Na channels
Release glutamate Prevents spread of seizure foci discharges Partial seizures Generalized tonic-clone seizures Status epilepticus following IV diazepam Zero-order @ high doses Fosphenytoin for IV use Ataxia Diplopia Nystagmus Gingival hyperplasia
Topiramate
Anticonvulsant Monosaccharide derivative Block voltage-sensitive Na channels
Augments GABA activation of GABA receptors
Blocks glutamate receptors
Ataxia Dizziness Drowsiness Fatigue Impaired concentration & memory Psychomotor slowing Speech problems Diplopia Nystagmus
Valproate
Anticonvulsant Branched-chain FA GABA levels by release or metabolism or reuptake
Reduced Na dependent action potentials Simple & complex absence seizures Complex partial seizures Tonic-clonic seizures Myoclonic seizures Migraine prevention Manic phase of bipolar Indigestion N, V Dizziness Sedation Hepatotoxicity
Zolpidem
Non-benzodiazepine hypnotic Imidazopyridine Activates BZBP receptors on GABA operated Cl ion channel
channel affinity for GABA & frequency of channel opening
Neuronal hyperpolarization
Insomnia
Endocrine
Acarbose Alendronate Calcitonin Danazol Desmopressin Ergocalciferol Ethinyl estradiol & drospirenone Ethinyl estradiol & norethindrone Finasteride Fludrocortisone Glyburide Hydrocortisone
Insulin Levothyroxine Medroxyprogesterone Metformin Methimazole Mifepristone Octreotide Oxytocin Pioglitazone Prednisone Raloxifene Repaglinide Somatropin Testosterone
Acarbose
Antidiabetic -glucosidase inhibitor Inhibits intestinal enzyme that converts oligosaccharides & disaccharides to glucose digestion of starch & sucrose postprandial blood glucose & HbA1c
Type II DM
Alendronate
Bone resorption inhibitor Bisphosphonate Prevents attachment of osteoclast precursor cells to bone metabolic activity of osteoclasts & ability to resorb bone
Prevent/Tx
Osteoporosis Corticosteroid-induced osteoporosis Pagets ds of bone hypercalcemia
Calcitonin
Ca hormone Thyroid gland hormone Binds calcitonin receptor on osteoclasts
cAMP & inhibits osteoclast activity
Danazol
Ovarian inhibitor Synthetic androgen, antiestrogen Feedback inhibits pituitary FSH & LH secretion ovarian estrogen secretion & stim. endometrial & breast tissue.
Endometriosis Fibrocystic breast ds Hereditary angioedema
C1 esterase inhibitor & C4 complement component
CI in pregnancy androgenic effects on female fetus Emotional lability Deepening voice Acne Hirsutism Amenorrhea breast size
Desmopressin
Posterior pituitary hormone Vasopressin, ADH analogue Mimics natural vasopression
Increases water reabsorption in kidneys Vasoconstriction DI Nocturnal enuresis Control bleeding in hemophilia & wWFs ds Intranasal, oral, or IV
Ergocalciferol
Vit. D Fat-soluble Activated in liver & kidneys to form calcitriol
Ca & phosphorus absorption from gut Vit. D deficiency
Rickets, osteomalacia
Chronic renal failure Familial hypophosphatemia Hypocalcemia d/t hypoparathyroidism Postoperative & idiopathic tetany
Thromboembolism
risk w/ smoking
Progesterone
Inhibits midcycle LH surge & ovulation
Edema Efficacy w/
ABX Carbamazepine phenytoin
Norethidrone
Slightly androgenic Thromboembolism Edema Depression Gallbladder ds
Progesterone
Inhibits midcycle LH surge & ovulation
Finasteride
Androgen synthesis inhibitor 5--reductase inhibitor Inhibits conversion testosterone dihydrotestosterone & androgenic stimulation of prostate & skin prostate size & promotes hair growth
BPH Male pattern baldness
CI pregnancy
Risk to male fetus Do NOT handle tablets
Impotence
Fludrocortisone
Corticosteroid Mineralocorticoid Activates aldosterone receptors in renal distal tubule
Na reabsorption K & H excretion Adrenal insufficiency
Addisons ds
Hypokalemia
by thiazide & loop diuretics
Glyburide
Antidiabetic Sulfonylurea hypoglycemia Closes ATP-sensitive K channels preventing K efflux & depolarizing pancreas B cells
Influx Ca & relaxing insulin
Photosensitivity Hypoglycemia
Hydrocortisone
Short-acting corticosteroid, low-potency topical corticosteroid Glucocorticoid Replaces endogenous cortisol in deficiency states Suppresses inflammation & immune response topical
Adrenocortical insufficiency Topical
Insect bites Contact dermatitis
Insulin
Antidiabetic Pancreatic hormone Replaces endogenous insulin
DM Rapid acting lispro Intermediate acting lente Long acting ultralente
Levothyroxine
Thyroid hormone Tetraiodothyronine Binds nuclear receptors & gene transcription
metabolic rate, protein synthesis, gluconeogenesis, cell growth & differentiation, & CNS development
Converted to T3 in tissues
Hypothyroidism
Medroxyprogesterone
Progestin, contraceptive Progesterone analogue endometrial hyperplasia in women receiving estrogen Prevents conception by thickening cervical mucus
Estrogen-progestin HRT Injectable contraceptive Progestin-only injectable contraceptive IM depot injection lasts 3mo
Metformin
Antidiabetic Biguanide, antihyperglycemic # & affinity of insulin receptors in peripheral tissues hepatic glucose output glucose absorption from gut glucose uptake & utilization in skeletal m. & adipose tissue
Type II DM Used in combo w/ sulfonylureas
N, V, D Abdominal bloating
Methimazole
Antithyroid Thiourea, thyroid hormone synthesis inhibitor Inhibits peroxidase & iodination & coupling of tyrosine residue of thyroglobulin thyroxine secretion
Hyperthyroidism Graves ds
Rash Agranulocytosis
Mifepristone
Abortificient Progesterone antagonist Partial agonist or antagonist progesterone receptors
Medical termination of pregnancy through 49d gestation Single dose + prostaglandin for 48hr stim. uterine contractions
Octreotide
GH inhibitor, antidiarrheal Somatostatin analogue w/ greater effects on GH than insulin secretion Suppresses secretion of GH, insulin-like growth factors, 5-HT & GI peptides gastrin, motilin, secretin, & VIP
Acromegaly Severe diarrhea & flushing d/t carcinoid tumors & VIP tumors Bleeding GE varices Complications of pancreatic surgery
Oxytocin
Oxytocic Posterior pituitary hormone Stim. Uterine smooth m. & induce labor Stim. mammary gland smooth m. & lactation
Induce labor @ term Facilitate uterine contractions Postpartum control of uterine bleeding Promote milk let-down IV for uterine stim. Nasal for milk let-down
Pioglitazone
Antidiabetic Thiazolidinedione antihyperglycemic Activates peroxisome proliferator-activated receptor- in adipose tissue, skeletal m., & liver gene transcription, insulin sensitivity, & glucose transports in muscle & adipose tissue Suppresses hepatic glucose output
Type II DM Used w/ metformin
Prednisone
Anti-inflammatory Corticosteroid Suppresses inflammation & immune response
Inflammatory, allergic, autoimmune, & neoplastic ds Prevent organ transplant rejection Asthma Depression or euphoria HTN Acne Impaired wound healing Adrenal suppression Muscle wasting Osteoporosis Cushingoid appearance
Moon facies Buffalo hump
susceptibility to infection
Raloxifene
Bone resorption inhibitor Selective estrogen receptor modulator SERM Estrogen-like effect on bone & lipid metabolism Estrogen antagonist in breast & uterine tissue bone mineral density & vertebral fractures
Osteoporosis in postmenopausal women Used in woman @ risk for breast cancer
Repaglinide
Antidiabetic Meglitinide hypoglycemic Closes ATP-sensitive K channels & insulin secretion postprandial blood glucose & [HbA1c]
Taken before meals to control postprandial hyerglycemia Used w/ metformin NOT sulfonylureas
Hypoglycemia
Somatropin
GH Recombinant somatotropin release of insulin-like growth factors in liver & cartilage
Stim. skeletal growth, AA transport, protein synthesis, nucleic acid synthesis & cell prolif. Short stature in children d/t GH deficiency Turner syn Chronic renal failure Prader-Will syn
Testosterone
Androgen Gonadal steroid Activated gene transcription & development of male sex organs & secondary sex characteristics lean body mass Stim. skeletal growth Accelerates epiphyseal closure sebaceous gland sebum production EPO secretion HDL levels
Hypogonadism in androgen-deficient men Delayed puberty in males
Gastrointestinal
Bisacodyl
Stimulant laxative Inhibits GI fluid reabsorption & stimulates peristalsis
Bowel evacuation prior colonoscopy or surgery Acute constipation Cramping N Fluid & electrolyte depletion
Hypokalemia
Calcium carbonate
Antacid, Ca supplement Ca salt Neutralizes gastric acid Provides Ca supplementation
Dyspepsia Hypocalcemia Prevention of osteoporosis Admin 1-1.5hr after meals & @ bedtime Constipation absorption of drugs
Tetracyclines Fluoroquinolones Phenytoin Iron salts
Dicyclomine
Antispasmodic Muscarinic receptor antagonist Blocks PNS stim. intrinsic nervous system & GI tone & motility
Directly relaxes GI smooth m. IBS cramping & pain Constipation Dyspepsia Dry mouth Urinary retention Blurred vision Decreased sweating
Docusate
Stool softener, laxative Surface-active agent Facilitates hydration of fecal material & softens feces
Constipation Fecal impaction rectal enema
Lactulose
Laxative Osmotic agent water content & softens feces Lowers pH of colon
Converts ammonia ammonium ion & ammonia absorption & blood levels Chronic constipation Hepatic encephalopathy
Improves mental status
Loperamide
Antidiarrheal Opioid analogue Activates opioid receptors in GI smooth m.
Segmental contraction & inhibits peristalsis Mild-moderate acute diarrhea Chronic diarrhea d/t IBD volume of ileostomy drainage AVOID
Pregnancy Lactation Children < 2 y/o
Mesalamine
GI anti-inflammatory Salicylate 5-ASA Inhibits prostaglandin synthesis & migration of inflammatory cells into bowel wall Scavenges superoxide-free radicals
IBD UC Proctitis Sulfasalazine sulfapyridine mesalamine &
Metoclopramide
Promotility & antiemetic D2 receptor antagonist Blocks relaxant effect of D on GI smooth m. Blocks presynaptic D receptors & Ach release & stim. smooth m. Blocks D2 receptors in chemoreceptor trigger zone & vomiting center
Chemotherapy-induced emesis Gastric stasis postsurgical & diabetic GE reflux CI in Parkinsons ds & seizure disorders Drowsiness EPS rxns restlessness
Misoprostol
Cytoprotective Synthetic PGE1 analogue gastric mucosal secretion & secretion of bicarbonate & mucus
Prevent gastric mucosal injury from NSAIDs Abortificient in combo w/ mifepristone CI in pregnancy Abdominal pain D Miscarriage
Omeprazole
Antiulcer Proton pump inhibitor Irreversibly inhibits H/K ATP pump in gastric parietal cells
Prevents gastric acid secretion Peptic ulcer ds GE reflux Zollinger-Ellison syn dyspepsia Abdominal pain Inhibits metabolism
Diazepam Cyclosporine Phenytoin
Ondansetron
Antiemetic 5-HT3 receptor antagonist Blocks 5-HT3 receptors in GI vagal afferent nerves, solitary tract nucleus, & chemoreceptor trigger zone
Prevent N, V from chemotherapy & radiation therapy Postoperative N, V HA Constipation D
Promethazine
Antiemetic, antihistamine, sedative H1 receptor antagonist, phenothiazine Blocks H1 & M1 receptors Inhibits stim. chemoreceptor trigger zone & vomiting center
N, V Preoperative sedation Allergic rxns Neuroleptic malignant syn Sedation Confusion Disorientation
Ranitidine
Antiulcer H2 receptor antagonist Blocks H2 receptors in gastric parietal cells
gastric acid secretion Peptic ulcer ds GE reflux Dyspepsia
Sucralfate
Antiulcer Cytoprotective, sulfated polysaccharide Adheres ulcer crater & forms protective barrier Prevents acid secretion & pepsin hydrolysis of mucosal proteins Stim. prostaglandin synthesis
Peptic ulcer ds GE reflux Prevent NSAID-induced gastric injury Constipation absorption
Fat soluble vitamins fluoroquinolones
Tegaserod
GI motility agent Partial agonist @ 5-HT4 receptors Activates 5-HT4 receptors on sensory neurons in enteric nervous system
Release neurotransmitters & peristalsis IBS in women w/ constipation Diarrhea Ischemic colitis
Hematologic
Abciximab Alteplase Aspirin Atorvastatin Bivalirudin Cholestyramine Cilostazol Clopidogrel Cyclosporine Enoxaparin
Epoetin Eptifibatide Ezetimibe Filgrastim Folic acid Gemfibrozil Heparin Niacin Sirolimus Warfarin
Abciximab
Antithrombotic Monoclonal Ab Inactivates platelet gp llb/llla receptors
Prevents platelet aggregation Prevent thrombosis during coronary angioplasty & stent placement Bleeding Thrombocytopenia
Alteplase
Thrombolytic Plasminogen activator Converts plasminogen plasmin
Degrades fibrin & fibrinogen AMI Acute ischemic stroke Occluded central venous access devices Streptokinase & urokinase for pulmonary embolism Reperfusion arrhythmia Contraindications
Internal bleeding Recent CNS surgery or trauma
Atorvastatin
Cholesterol lowering agent HMG-CoA reductase inhibitor HMG-CoA reductase, ratelimiting enzyme for cholesterol
hepatic cholesterol uptake LDL levels Hypercholesterolemia Cholesterol-lowering effects w/ ezetimibe & bile acidbinding agents Myalgia Myositis Rhabdomyolysis Hepatitis GI distress Effects w/
Grapefruit juice Azole antifungals cyclosporine
Bivalirudin
Anticoagulant Hirudin analogue Inhibits thrombin
Prevents blood coagulation Thrombosis in unstable angina AMI Stent insertion Used in pts w/ heparininduced thrombocytopenia
Bleeding
Cholestyramine
Cholesterol-lowering agent Bile-acid binding resin Binds intestinal bile acids
Prevents reabsorption cholesterol utilization
LDL levels
Cilostazol
Antiplatelet Platelet aggregation inhibitor Inhibits phosphodiesterase III & cAMP in platelet & blood vessels
Inhibit platelet aggregation Causes vasodilation Intermittent claudication
Improves blood flow & walking distance
Clopidogrel
Antiplatelet Platelet aggregation inhibitor Irreversibly inhibits binding of ADP to platelet receptors
gp IIb/IIIa mediated aggregation Stroke MI Peripheral vascular ds Additive effects w/ aspirin Hypersensitivity reaction
Cyclosprine
Immunosuppressant IL2 expression inhibitor Bind immunophilins
Complex binds calcineurin inhibits transcription of IL2 gene Prevent rejection of renal, cardiac or hepatic allografts Severe RA & psoriasis HTN Nephrotoxic Gingival hyperplasia Hirsutism Tremor Induce metabolism
Rifampin Barbiturates Carbamazepine
Inhibits metabolism
Grapefruit juice
Enoxaparin
Parenteral anticoagulant LMWH Binds/potentiates antithrombin III on factor Xa
Prevent
DVT Pulmonary embolism after knee, hip, or abdominal surgery Thrombosis in unstable angina & non Q-wave MI
Thrombocytopenia
Epoetin
Hematopoietic growth factor Recombinant human EPO Binds receptors on erythroid progenitor cells & stim. cell maturation & prolif.
Reticulocytosis & Hct Anemia d/t
CRF Chemotherapy Zidovudine therapy Hematologic malignancy
lymphoma
HTN
Eptifibatide
Antiplatelet GP IIb/IIIa receptor antagonist Reversibly inhibits fibrinogen binding to gp IIb/IIIa receptors
Prevents platelet aggregation Prevent coronary thrombosis in
Unstable angina or non-ST segment elevation MI Coronary angioplasty or stent placement
Bleeding
Ezetimibe
Cholesterol-lowering agent Cholesterol absorption inhibitor Disrupts annexin-caveolin complex mediating cholesterol transport intestinal brush border Inhibits absorption of biliary dietary cholesterol
Pro-drug converted to active glucuronide metabolite Hypercholesterolemia Additive effect w/ statins
Filgrastim
Hematopoietic growth factor Recombinant human GCSF Binds receptors on myeloid progenitor cells & stim. maturation & prolif. Accelerates neutrophil recovery after myelosuppressive chemotherapy
infection incidence Neutropenia assoc/ w/ chemotherapy & bone marrow transplants Avoid 24 hrs prior & after chemotherapy Bone pain
Folic acid
Vitamin, hematologic agent Metabolic cofactor for DNA synthesis Activated folate transfer one-carbon units to purine & pyrimidine precursors
Megaloblastic anemia Fetal neural tube defects Coronary artery ds Pregnant woman have requirements Absorption by
Phenytoin Cholestyramine
Gemfibrozil
Lipid-lowering agent Fibric acid derivative Activates peroxisome proliferator activated receptor-
Oxidizes FA & apo-AI & AII plasma triglycerides HDL Hypertriglyceridemia HDL levels Monitor LFTs throughout Tx GI distress Myositis Statins risk rhabdomyolisys
Heparin
Parenteral anticoagulant Antithrombotic Binds/potentiates antithrombin III
inactivation factor Xa & thrombin Venous thromboembolism Pulmonary embolism AF w/ embolism Consumptive coagulopathies In vitro & catheter coagulation Monitor PTT Protamine sulfate for OD Thrombocytopenia
Niacin
Vitamin, lipid-lowering agent G-protein coupled receptor ligand Activates G-protein coupled receptor
Inhibits lipolysis & release of FA hepatic triglyceride synthesis & VLDL secretion Hypertriglyceridemia HDL Hypercholesterolemia Pellagra Flushing Pruritis GI distress, peptic ulcer Hyperglycemia Hepatotoxicity Statins risk rhabdomyolysis
Sirolimus
Immunosuppressant T-lymphocyte inhibitor Inhibits regulatory kinase in cytokinedriven T-cell prolif.
Combo w/ corticosteroid & cyclosporine Prevent
Rejection renal allograph Coronary stent restenosis
Warfarin
Oral anticoagulant Coumarin vit. K antagonist Inhibits reduction of oxidized vit. K
Prevents vit. K dependent carboxylation of glutamate residues of factors II, VII, IX, X, proteins C & S Delayed onset d/t circulating coagulation factors Monitor INR Give vit. K if bleeding Fetal malformations Abnormal bone development
Musculoskeletal
Acetaminophen
Analgesic, antipyretic COX-3 inhibitor Inhibits COX-3 selectively Inhibits synthesis of PG causing pain & fever
Mild-moderate pain Fever Lacks anti-inflammatory & antiplatelet activity OD cause fatal hepatic failure hepatotoxicity w/ alcohol renal toxicity w/ salicylates & NSAIDs
Allopurinol
Antigout Xanthine oxidase inhibitor Inhibits xanthine oxidase & catabolism of purines xanthine & uric acid
uric acid levels Prevent hyperuricemia & gout Rash Inhibits metabolism
Mercaptopurine
Celecoxib
NSAID COX-2 inhibitor Inhibits COX-2 & synthesis of PG causing pain, fever, & inflammation
OA RA Inflammatory jt ds GI bleeding risk stroke & MI
Cyclobenzaprine
Skeletal m. relaxant Tricyclic central-acting m. relaxant Acts on brainstem & spinal cord to reduce tonic somatic m. activity via & motor neurons
Acute muscle spasm Dizziness Drowsiness Dry mouth AVOID MAOI
Etanercept
Antirheumatic agent, antitumor necrosis factor Antitumor necrosis factor p57 combined w/ Fc of IgG Binds TNF- & jt inflammation & pain Slows progression of RA
RA URI HA Ab response to live virus vaccines
Ibuprofen
NSAID Nonselective COX inhibitor Inhibits COX-1 & COX-2 & synthesis of PG causing pain, fever, & inflammation
Mild-moderate pain or dysmenorrhea Inflammatory disorders
OA RA
Indomethacin
NSAID Nonselective COX inhibitor Inhibits COX-1 & COX-2
Inflammatory disorders
Gouty arthritis OA RA Ankylosing spondylitis
Infliximab
Ds modifying antirheumatic Monoclonal Ab to TNF Inactivates TNF- & jt inflammation, pain, & destruction Sx of Crohns ds
RA Crohns ds Fatigue N, V URI
Ketorolac
NSAID Nonselective COX inhibitor Inhibits COX-1 & COX-2 & synthesis of PG causing pain, fever, & inflammation
Short-term pain management Prolongs bleeding time
Limit use to < 5d
Probenecid
Inhibits renal tubular secretion of Penicillins
Used to penicillin serum levels
Colchicine
D N, V Agranulocytosis & aplastic anemia
Colchicine
Inhibits leukocyte response to monosodium urate crystals in jt Acute gouty arthritis Prevent gouty arthritis
Neurodegenerative
Baclofen
Antispasticity GABA-B receptor agonist neuronal cAMP & Ca influx
K influx motor neuron excitability & inhibits spinal reflexes Spasticity
MS Spinal cord injury ALS
Benztropine
Anti-Parkinson Central anticholinergic Blocks cholinergic receptors & restores neurotransmitter balance in basal ganglia
Parkinsons ds Drug-induced EPS tremor > bradykinesia & rigidity Blurred vision Dry eyes Constipation Dry mouth Urinary retention
Donepezil
Anti-Alzheimer Cholinesterase inhibitor Inhibits cholinesterase in CNS
Ach neurotransmission Slows decline in cognitive function Alzheimers ds Does NOT prevent ds progression N, D HA
Entacapone
Anti-Parkinson Catechol-Omethyltransferase inhibitor Inhibits catechol-omethyltransferase inactivation of levodopa
levodopa in CNS Prolongs response to levodopa & S/Sx Parkinsons ds Adjunct to levodopa/carbidopa for Parkinsons ds AVOID nonselective MAOI Rhabdomyolysis Neuroleptic malignant syndrome
Interferon-beta-1b
Anti-multiple sclerosis Interferon Binds cell surface receptors producing immuno-suppressive effects
relapse & slows physical disability in MS Relapsing-remitting MS SubQ daily HA Weakness GI distress Sweating Neutropenia Myalgia Chills Fever
Levodopa-carbidopa
Anti-Parkinson Dopamine precursor, decarboxylase inhibitor Levodopa
Converted to D in CNS
Augments neurotransmission in basal ganglia
Carbidopa
Inhibits peripheral dopadecarboxylase
levodopa availability in CNS
Memantine
Anti-Alzheimer Glutamate antagonist Glutamate NMDA receptor antagonist
Prevent excitotoxic effects of glutamate causing neuronal loss Slows decline in cognitive function Alzheimers ds
Pergolide
Anti-Parkinson Dopamine receptor agonist Activates D receptors in basal ganglia
Parkinsons ds in conjunction w/ levodopa/carbidopa Dyskinesia Hallucination Orthostatic hypotension Constipation
Selegiline
Anti-Parkinson Type B MAOI
Converted to active form by MAO Irreversibly inhibits D degradation by MAO
response to levodopa/carbidopa Tx Parkinsons ds w/ levodopa/carbidopa Slows progression of Parkinsons ds
AVOID Meperidine & opioids
Fatal rxn Excitation Rigidity HTN coma Serotonin syn Asystole HTN Syncope Rigidity seizures
SSRI
Tricyclics
Other Drugs
Alprostadil
Vasodilator Prostaglandin E1 Activates PG EP receptors
Vascular smooth m. relaxation & vasodilation Maintain PDA in neonates awaiting surgery
IV infusion
IV infusion
Apnea Hypotension Arrhythmia
Local products
Prolonged/painful erection lightheadedness
Bosentan
Vasodilator Endothelin-1 receptor antagonist Blocks endothelin A & B receptors pulmonary vascular resistance & dyspnea Improves walking distance
Pulmonary arterial HTN CI in pregnancy
Causes birth defects
Epoprostenol
Vasodilator Naturally occurring prostacyclin (PGI2) Activated prostaglandin IP receptors
Vascular smooth m. relaxation Flushing Hypotension Tachycardia Diarrhea N, V
Latanoprost
Ocular hypotensive agent Prostaglandin F2 analogue Activates prostaglandin FP receptors aqueous humor outflow via uveoscleral pathways Lowers intraocular pressure
Chronic open-angle glaucoma Topical ocular admin Alters color of iris causing permanent eye color change by amount of melanin in melanocytes
Mesna
Antidote Sulfhydryl compound Detoxifies urotoxic metabolites acrolein of ifosfamide & cyclophosphamide
Hemorrhagic cystitis d/t ifosfamide & cyclophosphamide
Succimer
Antidote Metal chelating agent dimercaptosuccinic acid Chelates lead
Water-soluble chelates to excreted in urine
Psychotherapeutics
Amitriptyline Amphetamine & dextroamphetamine Atomoxetine Buproprion Desipramine Fluoxetine Haloperidol Lithium
Amitriptyline
Antidepressant Tricyclic Blocks neuronal reuptake of serotonin > norepinephrine Blocks muscarinic & adrenergic receptors
Chronic pain Depression Delayed onset of antidepressant effect >4 wks AVOID
MAOI SSRI
Lethargy Sedation Blurred vision Constipation Urinary retention appetite & wt gain OD wide QRS complex VT Altered effects by drugs that inhibit/induce CYP450
Carbamazepine Quinidine Rifampin
Amphetamine
CNS stimulant Sympathomimetic amine neuronal release of norepinephrine
ADHD
attention span motor restlessness
Tachycardia HTN Anorexia Irritability Insomnia Tremor Growth inhibition Drug dependence HTN crisis w/ MAOI
Narcolepsy
mental alertness drowsiness & fatigue
Atomoxetine
ADHD agent Selective NE reuptake inhibitor Inhibits neuronal reuptake of NE in CNS
ADHD in children/adults levels & effect in slow metabolizers CYP2D6 appetite Insomnia Levels & effects altered by drugs that inhibit/induce CYP2D6
Bupropion
Antidepressant Neuronal reuptake inhibitor Inhibits neuronal reuptake of DA > 5-HT & NE
Depression Smoking cessation Delayed onset for antidepressant effects Agitation HA Dry mouth N Tremor Impaired motor & cognitive skills MAOI adverse effects Seizure risks w/ phenothiazines
Desipramine
Antidepressant Tricyclic Blocks neuronal reuptake NE > 5-HT Blocks muscarinic & adrenergic receptors
Depression Chronic pain Delayed onset for antidepressant effects AVOID
MAOI SSRI
Lethargy Sedation Blurred vision Constipation Urinary retention appetite & wt gain OD wide QRS complex VT
Fluoxetine
Antidepressant SSRI Inhibits neuronal reuptake of serotonin
Depression OCD Bulimia nervosa Anorexia nervosa Fibromyalgia Panic attacks Phobias Prementsrual dysmorphic disorder Active metabolite 5-7d half-life AVOID MAOI Anxiety Drowsiness Insomnia Nervousness Sexual dysfunction Sweating Tremor levels metabolized by CYP2D6
Haloperidol
Typical antipsychotic Butyrophenone Blocks D2 receptors in mesolimbic area, chemoreceptor trigger zone, solitary tract, & basal ganglia Blocks muscarinic & adrenergic receptors
Psychotic disorders
Schizophrenia
Extrapyramidal rxns Tardive dyskinesia Blurred vision Constipation Dry mouth Urinary retention Hypotension
Tourettes syn
Lithium
Mood stabilizer, antimanic Inorganic cation noradrenergic neurotransmission or effects b/c of cAMP Inhibition of inositol-1phosphatase
Depletion of inositol & IP3
Polyuria Impaired memory Acne Tremor ECG changes GI distress Hypothyroidism Leukocytosis NM toxicity w/ haloperidol toxicity
Diuretics NSAIDS Fluoxetine
Methyphenidate
CNS stimulant Sympathomimetic amine neuronal release NE
ADHD
attention span motor restlessness
Tachycardia HTN Anorexia Irritability Insomnia Tremor Growth inhibition Dependence HTN crisis w/ MAOI
Narcolepsy
mental alertness drowsiness & fatigue
Mirtazapine
Antidepressant Tetracyclic Inhibits presynaptic 2 autoreceptors & heteroreceptors
NE & 5-HT release Depression Appetite stimulation AVOID MAOI
HTN, seizure, death
Olanzapine
Atypical antipsychotic Thienobenzodiazepine Blocks D2 & 5-HT2 receptors in CNS Blocks H1, muscarinic, & adrenergic receptors
Schizophrenia Manic episodes of biploar Anorexia nervosa Oral tablets contain aspartame
Avoid in phenylketonuria
Agitation Dizziness Restlessness Sedation Amblyopia Orthostatic hypotension Tachycardia Constipation Dry mouth Wt gain Tremor
Phenelzine
Antidepressant MAOI Inhibits MAO & CNS levels of NE & 5-HT
Neurotic & atypical depression Avoid
Fluoxetine Tyramine
Dizziness Insomnia Restlessness Blurred vision Orthostatic hypotension Diarrhea Potentially fatal
SSRI Tricyclics
HTN crisis
Tyramine Amphetamines Methyldopa Levodopa
Risperidone
Atypical antipsychotic Benzisoxazole Blocks 5-HT2 > D2 receptors in CNS Blocks H1 & -adrenergic receptors
Schizophrenia Psychotic disorders Monitor pt for neuroleptic malignant syn Aggressive behavior Extrapyramidal rxns Sleep disturbances Insomnia Sedation Constipation or diarrhea Wt gain
Thioridazine
Typical antipsychotic Phenothiazine Blocks D2 receptors in mesolimbic area, chemoreceptor trigger zone, solitary tract, & basal ganglia Blocks muscarinic receptors
Psychotic disorders Schizophrenia Extrapyramidal rxns Tardive dyskinesia Photosensitivity Potential for V arrhythmias & sudden death Retinal pigmentation w/ high doses
melanosis
Venlafaxine
Antidepressant Phenethylamine Inhibits neuronal reuptake 5-HT & NE
Depression Generalized anxiety disorder AVOID MAOI Sexual dysfunction GI distress Dizziness Insomnia Nervousness
Respiratory
Albuterol
Bonchodilator 2 receptor agonist Activates 2 receptors in bronchial smooth m.
cAMP activating kinases Inhibiting myosin phosphorylase m. relaxation Asthma
Acute bronchospasm Prevent exercise-induced asthma
Cromolyn
Antiasthmatic & antiallergy Mast cell stabilizer Prevents Ca influx & stabilizes mast cell & eosinophil membranes
Prevents degranulation & release of histamine, leukotrienes Asthma prophylaxis Exercise-induced bronchospasm Allergic disorders Oral or nasal inhalation Nasal & throat irritation
Diphenhydramine
Antihistamine, sedative, antiemetic H1 receptor antagonist Blocks H1 & muscarinic receptors
Prevents histamineinduced allergic rxns Prevents vestibular stim. of vomiting center Sedation Allergic rxns Prevent motion sickness Insomnia Drowsiness Blurred vision Dry mouth Urinary retention Anorexia
Fluticasone
Anti-inflammatory Corticosteroid Inhibits cytokine production by Thelper cells Prevents mediator release from mast cells, basophils, eosinophils Stabilizes lysosomal membranes Vasoconstriction & capillary permeability
Allergic rhinitis Chronic nasal inflammation Chronic asthma
Ipratropium
Bronchodilator Muscarinic receptor antagonist Blocks muscarinic receptors in bronchial smooth m. & nasal mucosa Prevents vagal-stimulated bronchoconstriction
COPD Rhinitis Asthma Inhalation admin
Loratadine
Antihistamine H1 receptor antagonist Blocks H1 receptors in nasal mucosa Prevents allergic rxns
Seasonal rhinitis Chronic idiopathic urticaria Less sedating than diphenhydramine
Montelukast
Antiasthmatic Leukotriene antagonist Blocks cysteinyl leukotriene1 receptor for leukotrienes C4, D4, E4 Prevent airway inflammation, edema, bronchoconstriction, & secretion viscous mucus Inhibits early/late phase bronchoconstriction
Long-term asthma control Oral admin
Omalizumab
Antiasthmatic IgE antagonist Blocks IgE
Severe asthma in combo w/ corticosteroid therapy SubQ every 2-4 wks Allergic rxns
anaphylaxis
Salmeterol
Bronchodilator 2 agonist cAMP Relaxes bronchial smooth m. Inhibits late phase allergeninduced bronchoconstriction
Asthma
Prevent nocturnal attacks Exercise-induced asthma NOT acute bronchospasm
Tachycardia Nervousness HA
Inhalation admin
Theophylline
Bronchodilator Methylxanthine Inhibits phosphodiesterase isoenzymes & cAMP Relaxes bronchial smooth m. Inhibits T-lymphocyte proliferation & cytokine production
Chronic asthma Obstructive pulmonary ds Neonatal apnea respiratory stim. Half-life
Shorter in smokers & children Longer in elderly Monitor blood levels
Zileuton
Antiasthmatic Leukotriene synthesis inhibitor Inhibits 5-lipoxygenase & leukotriene synthesis
Prevents airway inflammation & bronchoconstriction Long-term asthma control
Flu-like syn HA Drowsiness Dyspepsia serum aminotransferase levels & hepatitis Inhibits CYP450 & 3A4
theophylline & warfarin levels