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75 Cards in this Set
- Front
- Back
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Alprostadil
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a. Class: PGE1 analog
b. Therapeutic uses: keep a patent Ductus arteriosis or for ED (on nitrates can't use viagra) c. Mechanisms: PGE1 analog, IV, topical, or subcutaneous d. Side effects: NA |
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Epoprostenol
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a. PGI2 analog
b. Treatment for pulmonary hypertension c. Vasodilator and decreased platelet agg. via Gs d. NEED CONTINUOUS IV infusion b/c half-life is 6min very expensive |
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Treprostinil
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a. PGI2 analog (epoprostenol)
b. same as epoprostenol c. same as epoprostenol d. LONGER HALF LIFE |
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Latanoprost
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a. PGF2 analog
b. Treatment for OPEN ANGLE GLAUCOMA c. INCREASES outflow of aqueous humor, combination therapy with B blockers that decrease production of aq. humor d. DARKENS IRIS COLOR and EYELASHES |
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Misoprostol
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a. PGE1 analog
b. Used to PREVENT STOMACH ulcers in high risk patients taking NSAIDS, treat miscarriage - postpartum hemorrhage, abortion c. Inhibits cAMP which increases mucin and decreases proton pump activity d. ORAL administered, used to expel blastocyst post methotrexate (RU486) uterine contraction, cervix ripening |
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Dinoprostone
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a. PGE2 analog
b. Contraction of pregnant uterus, abortion/postpartum hemorrhage, cervical ripening c. PGE2 analog d. Vaginal suppository |
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Carboprost
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a. PGF2 analog (15 methyl PGF)
b. induces contraction of pregnant uterus (abortion, induced labor, hemorrhage) c. IM injection d. increases incidence of arrythmias (not commonly used) |
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Zafirlukast
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a. LT inhibitor
b. Antagonizes smooth muscle contraction (relieves bronchoconstriction - asthma) c. Competitive inhibitor of LT receptor type 1 ( PO BID - takes 3 d to start working, hepatic p450 metabolism) d. Drug interaction with WARFARIN/PHENTANYL, GI complaints CHURG-STRAUSS synddrome (eiosinophilic granulomatosis - allergic granulomatosis) |
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Montelukast
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a. LT inhibitor
b. relieves BRONCHOCONSTRICTION (asthma) c. LT competitive inhibitor of LT receptor. PO (1 week max effect) - p450 and excreted in bile d. OKAY in CHILDREN greater than 1 week - rare incidence of side effects |
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Zileuton
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a. LT inhibitor
b. Asthama (bronchoconstriction reliefe), antiinflamatory (RA and IBD) c. 5-lipoxygenase inhibitor, PO QID, few hours effective (renal excretion p450 metabolism) d. HEPATITIS, drug interaction with WARFARIN, theophylline |
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Aspirin (acetylsalicyclic acid - ASA)
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a. NSAID
b. inhibits platelet aggregation at LOW DOSE (thromboemoblism or atherosclerosis) and decreases PG mediated potentiation of pain (analgesia and antipyretic) c. IRREVERSIBLE COX inhibitor, PO, ZERO ORDER d. HEMORRHAGE, peptic ulcers, GI BLEEDING, aspirin sensitivity |
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Reyes Syndrome
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Aspirin with viral infection AEs
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Ibuprofen
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a. NSAID (proprionic acids)
b. close patent ductus arteriosis, prototype aspirin c. REVERSIBLE COX inhibitor d. COMMON AEs but lower incidence of bleeding |
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Naproxen
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a. NSAID (proprionic acid)
b. LONGER half life BID QD c. REVERSIBLE COX inhibitor d. common AEs but longer HALF LIFE |
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Common AEs of NSAIDS
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Premature closing of DA
COMBOS of NSAIDS NOT SAFE acute renal failure, interstitial nephritis FLUID RETENTION HEADACHE TINNITUS ULCERS PRURITUS |
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Celecoxib
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a. COX2 specific inhibitors
b. prevent the GI BLEEDS with NSAIDS c. specifically inhibits COX2 d. LESS PEPTIC ULCERATION but increased risk of MI |
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Acetaminophen
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a. Antipyretic analgesics
b. NOT ANTI-INFLAMMATORY or ANTIPLATELET (weak PG synth inhibitor) but for ANALGESIA and FEVER c. inhibits COX3 d. TOXICITY - ACUTE hepatic failure, renal failure, pancreatitis CHRONIC nephropathy SAFEST for KIDS (liquid) |
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OVERDOSE TX for ACETOMINOPHEN
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USE N-acetylcysteine which WORKS as a substitute for HEPATIC GLUTATHIONE which promotes the METABOLISM (IV administer) of paracetamol (a toxic metabolite for acetaminophen)
ALSO MUCOMYST because it is used as a Mucolytic therapy |
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Indomethacin
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a. NSAID
b. analgesic, antiinflam, antipyretic, USED for GOUT, close DA c. REVERSIBLY inhibits COX and PLA2 d. common AEs for NSAIDs |
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Diclofenac Sodium
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a. NSAID
b. arthritis, analgesia, fever c. CONCENTRATES in SYNOLVIAL FLUID, reversible COX inhibitor |
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Keterolac
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a. NSAID
b. analgesia, POST OP PAIN c. COX inhibitor reversible d. PO, IM, IV, or SC |
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Piroxicam
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a. NSAID
b. USED for RA (analgesia, fever, antiinflam) c. DECREASES PMN migration and lmpho activation COX INHIBITOR d. Once DAILY ADMIN |
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Methotrexate
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a. Disease Modifying AntiRheumatic Drug (immunosupressant - delays disease progression)
b. RA treatment, anti metabolite and immunosuppressant c. BINDS dihydrofolate reductase - reduces folate and interferes with DE NOVO SYNTH OF THYMIDINE therfore inhibits DNA, RNA, and protein synth - INCREASES ADENOSINE RELASE decreases lymphocytes d. LOW DOSE PO for RA and Psoriasis, HIGH DOSE for chemotherapy NAUSEA, mucosal ulcers, bone marrow suppression and TERATOGEN HEPATOTOXICITY |
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Leflunomide
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a. DMARD (nucleic acid inhib)
b. Immunosupressant for RA c. Pyrimidine SYNTH inhibitor, reduces rUMP levels in LYMPHOCYTES blocks CELL CYCLE d. RASH, bone marrow suppression, hepatotoxicity |
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Azathioprine
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a. DMARD (MERCAPTOPURINE)
b. Immunosupressant (RA SEVERE or transplant, AUTOIMMUNE HEPATITIS) c. converted to 6-mercaptopurin - INHIBITS PURINE SYNTH and SALVAGE pathway - d. BONE MARROW SUPPRESSION, malignancy - ALLOPURINOL interactions, RISK of infection |
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Prednisone
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a. CORTISOL analog (3x more potent than it)
b. Antiinflammatory, immunosuppressant (RA acute attacks only, ASTHMA, leukemia, HODGKIN LYMPHOMA, GOUT, PROPHYLAxIS for Transplant c. Binds to the glucocorticoid receptor d. reduces action of proinflammatory cytokines (AP1) induces expression of antiinflammatory genes (iKB) LYMPHOLYTIC PO withe HEPATIC CONVERSION to ACTIVE AE: adrenal insufficiency, HYPERGLYCEMIA, CATARACTS, ULCERS |
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Hydroxycloroquine
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a. DMARD (RA and antimalaria)
b. UNK anti inflammatory, NOT SLOW PROGRESSION c. TAKES 12-24 weeks to WORK NO BONE MARROW SUPPRESSION d. AEs - retinopathy (rarere with chloroquine) |
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Sulfasalazine
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a. DMARD (RA and IBD)
b. UNK anti inflammatory c. AE - hypersensitive to SULFA ALLERGY |
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Anakinra
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a. ANTI IL1B (prototype)
b. RA c. RECEPTOR antagonist d. AE same as ANT TNF - lymphoma or bad infection, SC injection |
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Rilonacept
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a. Ankinra is prototype (ANTI IL1B)
b. SOLUBLE IL1B receptor (binds up IL1B) |
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Infliximab
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a. DMARD - ANTI TNF antibody
b.RA and CHRON's c. HUMANIZED monoclonal AB to TNF -single dose infusion d. AE- infusion rxn -chest pain nausea fever dyspnea, HYPOTENSION, incre risk of infection LYMPHOMA |
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Adalimumab
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a. DMARD, anti TNF ANTIBODY
b. RA, CHRONS, ANKYLOSING SPONDYLITIS, psoriatic arthritis c. SC injection - humanized MONOCLONAL ANTIBODY against TNF |
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Etanercept
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a. DMARD (refractory) - ANTI TNF
b. RA, ANkylosing spondylitis c. SC 2x per week - FUSION protein- TNF Receptor ligand BINDING DOMAIN with an IgG Fc |
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Abatacept
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a. DMARD (RA) - ETANERCEPT prototype
b. CTLA4 IG it is a recombinatn FUSION PROTEIN - inhibits the Cd28 - CD80/86 costimulation of TCELLS c. IV infusion |
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Rituximab
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a. ANTI NEOPLASTIC
b. RA and B CELL LYMPHOMA c. ANTI CD20 monoclonal AB block B CELL COSTIMULATION (IV infusion) d. AEs- hypersensitivity TUMOR LYSIS SYNDROME |
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Ondansetron
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a. ANTIEMETIC
b. for MIGRAINES symptomss c. BLOCKS 5-HT type 3 receptors d. PO or IV - 3-4 hr halflife - AEs headache and diziness constapation |
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Sumatriptan
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a. 5 HT1 receptor AGONIST (vasoconstrictor)
b. MIGRAINES c. SC, PO, NASAL d. AEs hypertension ISCHEMIA DRUG INTERAcTIONS with MAO-A inhibitors |
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Zolmitriptan
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a. Sumatriptan is the PROTOTYPE
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Ergotamine
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a. 5 HT1 receptor AGONIST - VASOCONSTRICTOR - uterine STIMULANT and Alpha adrenergic ANTAGONIS
b.MIGRANES c. RECEPTOR AGONIST d. AEs: NAUSEA vomiting CONTRA INDI for PERIPHERAL VASCULAR disease, CORONARY artery DISEASE or HYPERTENSION |
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Propranolol
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a. BETA BLOCKER (prototype) attenuate the NERUOTRIGGER PHASE
b. MIgraines prophyl- decreases HR, Decreases LV contractility, REDUCES myocardial oxyg. demand c. LOTS of AEs |
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Verampamil
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a. Ca2+ channel ANTAGONIST (prototype) - decreases Ca2+ influx and dilates the vasculature
b. MIGRAINE prophylaxis - ATTENUATE NEUROTRIGGER AND VASOCONSTRICTIVE PHASE c. PO and IV - bound plasma proteins d. AEs EXCESSIVE VASODILATION, Bradycardia |
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Topiramate
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a. Ca and Na channel blocker, GABA channel activator (Cl-) GLu receptor antagonist (AMPA and KAINATE but NOT NMDA)
b. Prophylaxis for MIGRAINES, also for SEIZURES c. REnal excretion, AEs - dizziness, ataxia, fatigue, kidney stones |
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Amitriptyline
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a. Tricyclic ANTI DEPRESSANT BLOCKS 5-HT reuptake (PROTOTYPE is imipramine)
b. ANti depressant and migraine prophylaxis c. 4 weeks for efficacy - very lipid soluble large VD - bind plasma protein difficult to dialyze and get out - BLOCKS reuptake of 5HT d. TOxicity - SEDATION tremor ANTICHOLINERGIC SIDE EFFECTS (DRY MOUTH, BLURRED VISION, urinary RETENTION) |
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Methysergide
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a. 5-HT receptor ANTAGONIST/partiol agonist
b. migraine prophylaxis c. vasoconstrictor and ERGOT DERIVATIVE d. RETROPERITONEAL FIBROSIS |
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Colchicine
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a. MT inhibitor - decreases NEUTRO migration into joint
b. SPECIFIC for GOUT and Prophylaxis d. AEs include NAUSEA, diarrhea, vomiting and abdominal pain |
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Prednisone and indomethacin
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Prednisone - cortisol analog and indomethacin is an NSAID -- GOUT and GOUT prophylaxis - AVOIDASA b/c compete with URATE secretion by KIDNEY and will RAISE SERUM URATE LEVELS
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Allopurinol
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a. Xanthine oxidase inhibitor (prototype)
b. DECREASES uric acid SYNTH (gout PROPHYLAXIS) c. SUICIDE SUBSTRATE decreases synth of uric acid d. AEs severe drug reaction with azathioprine |
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Febuxostat
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a. Xanthine oxidase inhibitor
b. HYPERURICEMIA or GOUT c. NON PURINE INHIBITOR d. Better tolerated than allopurinol |
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Rasburicase
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a. Urate oxidase (prototype)
b. recombinant urate oxidase enzyme from aspergillus converts urate into allantoin (more soluble) - for patients with TUMOR LYSIS SYNDROME NOT USED FOR GOUT c. PREVENTS renal failure with massive loading of urate into serum from tumor lysis d. AEs can only use ONCE b/c dev. AB against |
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Prednisone
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a. Glucocorticoids - prototype
b. Prophylaxis immunosuppressive before transplant c. Bind GR (displace HSP/immunophilin), Activates anti inflam gnes IKB and inhibiits Jun fos (AP1 pro inflamm genes) |
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Daclizumab
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a. Immunosuppressant - humanized MURINE (CDR/humang IG1 chimeric monoclonal Ab)
b. Cd25 ab (ANTI IL2 receptor) - immunosupressant c. IL2 binding, prevents activation of T cells d. Prophylaxis for GRAFT REJECTION |
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Sirolimus (rapamycin)
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a. Immunosuppressant (prototype)
b. organ transplant prophylaxis c. inhibition of TOR protein kinase and signaling d PO and rapid metabolism by P450 and excreted in BILE DOSE DEPENDENT THROMBOCYTOPENIA and incr. infections NO RENAL TOXICITY ALONE, LEUKOPENIA |
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Mycophenolate mofetil
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a. Immunosuppressant
b. ORgan transplant prophylaxis c. Converted to Mycophenolic acid by plasma esterases- INHIBITS IMP - dehydrogenase - BLOCKS DE NOVO PURINE SYNTH important in lymphos - inhibits recruitment of leuks via blocking glycosylation of cell adhesion molecules (loss of GTP) d.GI hematologic toxicity (incr risk of infections) |
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Azathioprine
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a. immunosuppressant
b. converted to 6 mercaptorpurine, suppression of ORGAN rejections c. HIGH INCIDENCE of malignancies and infections |
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Cyclosporine
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a. DMARD (prototype)
b. RA (severe) and organ transplant and psoriasis atopic - chronic dry eyes c. BINDS to cyclosporine inhibits NFAT and IL2 - signal transduction of TNFa and IL2 PO or IV d AEs - nephrotoxicity and HYPERTENSION, infection, diabetes, DO NOT SUPRESS BONE MARROW ACCELERATED clearance of cyclosporin (induce p450) with RIFAMPIN, phenobarbital, phenhytoin, methoxazole. DECREASED CL with erythomyacin, etc. |
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Tacrolimus (FK506)
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a. immunosuppressant (prototype is cyclosporine)
b. 100X more potent same efficacy c. BINDS FKBP same mech as cyclosporine inhibit calcineurin d. PO or IV - ORGAN TRANSPLAT rescue - AEs inclue diabeteis neurologic toxicity, increased risk of malignancy, NEPHROTOXICITY |
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Enfuvirtide
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a. viral FUSION INHIBITOR (not 1st line)
b. anti HIV c. binds to gp41 prevents the hairpin unfolding that catalyzes fusion w/host cell d. IV - called FUZEON |
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Ritonavir Boost
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a. antiviral HIV PROTEASE inhibitor
b. HIV c. mimics transition state during proteolysis of HIV recursors - inhibits the METABOLISM of protease inhibitors by inhibiting the CYP3A (boosting other protease inhibitors) d. PO hepatic metabolism, fecal excretion - LIPODYSTROPHY, HYPERcholesterolemia drug ingteractions with P450 INHIBITION - multiple ddugs |
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Saquinavir
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a. ANTI VIRAL HIV - PROTEASE inhibitor
b. HIV protease inhibitor c. mimics transition state d. SIMILAR as RITONAVIR - PO EXTENSIVE 1st PASS HEPATIC metabolism - CRYSTALIZES in KIDNEYS and LIVER - mUST DRINK LOTS oF WATER fewer side effects than ininavir |
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Nevirapine
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a. nNRTIs
b.HIV childbirth anti viral c. ALLOSTERIC RTI - combo with a NRTI to decrease resistance d. RASH, hepatotoxicity |
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Efanvirenz
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a. ANTI VIRAL nNRTI
b. HIV c. SAME ase NEVIRAPINE d. CNS effects dizziness insomina, hallucinations -- LONG HALF LIFE only 1x d dose INDUCES CYP3A4 p450s (increase metabolism) |
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Maraviroc
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a. Co receptor blocker - Prototype (not 1st line)
b. HIV c. monoclonal Ab binds CCR5 |
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Raltegavir
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a. Integrase inhibitor
b. HIV c. interefere with integration of viral DNA into HOST |
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Zidovudine (AZT)
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a. antiviral NRTI
b. HIV c. nucleoside RT inhibitor - PRODRUG - SUICIDE chain termination d. PO - TOXIC, bone marrow supression, hepatotoxicity, CNS toxicity, renal excretion, GLUCURONIDATION metabolism DRUG RESISTANCE - drug interactions with PROBENECID and INHIBITS liver METABOLYZING ENZYMES STAVUDINE competes with it for PHOSPHORYLATION |
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Lamivudine (3TC)
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a. NRTI
b. HIV and HEP B c. SAME MEcH as AZT and SYNERGIZES d. dev of HEP B strains |
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Ematricitabine (FTC)
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a. NRTI
b. HIV c. SAME MECH as AZT d. LOW SIDE EFFECTS |
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Tenofovir
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a. NRTI
b. HIV and HEP B c. PRO DRUG - disoproxil fumarate is converted to tenofovir - BLOCKS chain elongation - NO DIFFUSE OUT conc. are HIGH AMP analog d. 1 day dose PO well absorbed AES include GI and PANCREATITIS lactic acid and renal insufficiency |
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Acyclovir
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a. ANTIVIRAL for HERPES (HSV, conronic supress HSV and varicella)
c. INITIAL phospho via VIRAL THYMADINE KINASE then by host kinase - inhibits viral DNA polymerase (guan) d. PO fair absorption (IV in serious cases) - RARE AE but nephrotoxicity and encephalopathy |
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Valacyclovir
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a. antiviral (herpes zoster)
c. SAME MECH as acyclovir (L-valyl ester of acyclovir) d. HAS MUCH BETTER ABSORBED than acyclovir since valyl ester of it |
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Ganciclovir
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a. CMV anti viral
c. SAME as acyclovir d. PO for chronic and IV for INTRAOCULAR IMPLANTS for RETINITIS AE - myelosuppression (IV) , teratogen and CARCINOGENIC |
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Foscarnet
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a. ANTIVIRAL (CMV and HIV)
c. NOT a PRODRUG - binds to PYROPHOSPHATE on viral DNA polymerase prevents its release inhibits activity d. RENAL dysfunction, HYPOCALCEMIA, chromosomal damage, and bone marrow toxicity |
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Zanamivir
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a. ANTI viral (INFLUENZA A&B)
C. inhibits NEURAMINIDASE (needed for maturation and release) d. inhaled - AE - cough nasal throat pain, bronchospasm |
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Oseltamivir
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a. ANti viral (inflenza)
c. SAME mech as Zanamivir (safer though) d. PO |
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Pegylated INTERFERON ALPHA
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a. ANTI VIRAL (HEP B and C and other viruses)
c. ACTivates RIbonuclease that degrades VIRAL mRNA (endogenous interpheron alpha is natural response) - INHIBITS protein synthesis elongation step of virally infected cells d. pegylated - has LONGER HALFLIFE so given weekly SC or IM hepatic and renal metabolism - AES - FLU LIKE SYMPTOMS, psych problems, myelosuppression |
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Ribavirin
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a. ANti viral (hep C and respiratory syncictial virus)
c. NUCLEOSIDE ANALOG prodrug - phosphorylated in CELL to active form inhibits viral RNA polymerase d. INHALED FORMULATION for RSV penumonia in CHILDREN (take PO w/ interfereon alpha) AES - TERATOGEN!!!! , MYELOSUPPRESSIOn (IV) and HEMOLYSIS |
