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Pharma Final 2012
Qs&As from Review Sheet for Pharmacology Final Nov 2012
| Question | Answer |
|---|---|
| MOA for ACE inhibitors | They block the Enzyme needed to Convert Angiotensin I into angiotensin II |
| Well-known side effect of ACE inhibitors | annoying, dry cough |
| MOA for thiazide diuretics | They inhibit Na+ and Cl- reabsorption in ascending loop and distal tubule |
| MOA for loop diuretics | They inhibit Cl- reabsorption in LOOP of Henle |
| Side effect of loop diuretics | OTOTOXICITY, increase in blood sugar, decrease in everything else: Na, K, Ca, Mg, uric acid |
| MOA for cardiac glycosides | They inhibit Na-K-ATPase which results in INCREASED SODIUM IONS (and thus dereased CALCIUM IONS) in heart muscle cells (myocytes). So force of myocardial contraction increases. |
| Example of cardiac glycosides | Digoxin |
| Precaution when taking cardiac glycosides | (they have a very low therapeutics index/narrow therapeutic window) |
| List potential toxic effects of cardiac glycosides | Arrhythmias, anorexia, nausea, diarrhea, visual disturbances |
| MOA for class I antiarrhythmics | Na+ channel blockers. They block Na+ entry into the cell during depolarization. |
| MOA for class II antiarrhythmics | Beta blockers. They prevent sympathetic stimulation of the heart, causing decreased heart rate. |
| MOA for class IV antiarrhythmics | Ca+ channel blockers. They slow the inward flow of Ca+ and thus prolong the refractory period (especially in AV node). |
| Bolded example of class I antiarrhythmics | Procainamide (1a), Lidocaine (1b) |
| Bolded example of class II antiarrhythmics | Propranolol (Inderal) |
| Bolded example of class IV antiarrhythmics | (but none of them is?are BOLDED!) |
| MOA for organic nitrates | They cause DILATION of large myocardial arteries (this lowers BP but somehow increases blood supply to the heart) |
| Drug of choice for acute coronary spasm | nitrogylcerine |
| "Routes" of administration for organic nitrates to treat angina | Sublingual for rapid onset. Transdermal patch for long-term use. |
| MOA for beta blockers (for rx of angina) | duh... they block (down regulate) the sympathetic nervous system (thereby decreasing O2 demand of heart) |
| Contraindications for beta blockers (for rx of angina)? Hint: think BBCI--> A-B-C-D-PVD | Asthma. (severe) Bradycardia. COPD. Diabetes. Peripheral Vascular Disease. |
| How to taper off beta blockers (for rx of angina) | Gradually reduce dose over 5-10 day period |
| Antihypertensive class of choice for use in diabetic patients | ACE inhibitors!! |
| Antihypertensive class of choice for use in AA | Ca+ channel blockers!! |
| Antihypertensive class of choice for use in angina patients (and migraine pts.) | Beta blockers! |
| Antihypertensive class of choice for use in pregnant women | the Central Acting ones. (e.g., methyldopa) |
| List bolded antiplatelet drugs | aspirin and Plavix (clopidrogel) |
| MOA for aspirin | (antiplatelet drug) blocks platelet aggreg. by "inhibiting thromboxane A2 synthesis, and thus prolonging bleeding time" |
| MOA for clopidogrel (Plavix) | (antiplatelet drug) blocks platelet aggreg. by inhibiting binding of ADP |
| Important side effect of heparin | hemorrhage |
| Drug used to heparin-induced hemorrhage | protamine sulfate |
| List bolded oral anticoagulants meds | warfarin and something called argatroban (!!) |
| Definition of thrombolytic drugs | lyse (already formed) clots |
| MOA for thrombolytic drugs | they activate plasminogen into plasmin (plasmin eats up fibrin) |
| Example of thrombolytic drugs | streptokinase and TPA |
| List bolded drug(s) used to treat end-stage renal failure | erythropoietin and the 2 human recombinant erythropoietins "alpha": epo alpha and darb epo alph |
| List bolded drug(s) used to treat megaloblastic anemia | vitamin B12 (cynaocobalamin) |
| MOA for statins (aka HMG-CoA reductase inhibitors) | HMG-CoA reductase is the rate limiting step in cholesterol synthesis, so inhibiting this enzyme inhibits cholesterol production |
| Side effects of statins | LFT abnormalities, myopathies, rhabdomyolysis (rapid disintegration of muscle tissue --> myoglobin inundates kidney --> kidney damage) |
| List bolded statins (aka HMG-CoA reductase inhibitors) | Zocor, Lipitor, Crestor: simvastatin, atorvastatin, rosuvastatin |
| MOA for niacin | strongly inhibits lipolysis (in adipose tissue) |
| MOA for ezetimibe (Zetia) | inhibits intestinal absorption of BOTH dietary and biliary cholesterol |
| Notable/possible side effect of (high-dose) niacin | flushing, pruritus |
| List bolded drugs used to treat hyperthyroidism (MIPP) | methimazole, propylthyuriacil, iodine/iodide, propranolol |
| MOA for methimazole | inhibits iodization of tyrosine groups and coupling of these groups to form thyroid hormones |
| MOA for propylthiuracil | the same as methimazole (inhibits iodization of tyrosine group, and coupling), plus inhibits peripheral conversion of T4 to T3 |
| Possible complications of glucocorticoid use | long-term use increases risk of osteoporosis |
| (Endocrine) use of spiranolactone | antagonist of both aldosterone (so useful in HTN, water retention, hypokalemia) AND testosterone (so useful in teenage acne) |
| (Endocrine) use of ketoconazole | an antifungal that crushes not just your balls but also your adrenals!! ("strongly inhibits ALL GONADAL and ADRENAL STEROID HORMONE SYNTHESIS"!!) |
| Use of raloxifene | (a SERM) is an estrogen AGONIST in bone and estrogen ANTAGONIST in breat and uterus, so useful in BOTH preventing & treating osteoporosis |
| Use(s) of clomiphene | (a SERM) is an estrogen receptor antagonist (in hypothalamus), so interferes with negative feedback loop and results in INCREASE RELEASE of GnRH and other gonadotropins-- thus useful in treating female infertility |
| Use of medroxyprogesterone | aka Depo-Provera, used for amenorrhea and abnormal vaginal bleeding |
| Use(s) of mifespristone | terminate pregnancy (causes shedding of uterine lining) |
| Major side effects of oral contraceptives | breast tenderness ("fullness"), n/v (fm estrogen), depression, edema (fm progesterone) |
| "Special risk" of OC in smokers and women over 35 yo | increased risk of abnormal clotting |
| Two major groups of androgens | testosterone based and anabolic steroids |
| Use of finasteride | male pattern baldness (1 mg QD, as Propecia); BPH (5 mg QD, as Proscar) |
| Use of flutamide | aka Eulexin, it is an oral nonsteroidal antiandrogen drug used to treat prostate cancer |
| MOA for alpha-glucosidase inhibitors (for rx of diabetes) | they slow carb digestion by inhibiting this alpha-glucosidase in "brush border" of intestine. (They are also said to inhibit amylase production.) |
| MOA for glitazones (for rx of diabetes) | they re-sensitize cells to endogenous insulin |
| List bolded alpha-glucosidase inhibitors (for rx of diabetes) | acarbose (cute name: they slow carb digestion!) |
| List bolded glitazones (for rx of diabetes) | Avandia (rosiglitazone). Removed fm mkt in EU. As of January 2011, Glaxo had set aside $6.4 billion to cover expected expenses from 13,000 heart attack lawsuits over the drug. |
| Hypoglycemic med that "has been proven to decrease cardiovascular mortality" | metformin (Glucophage) |
| Group of drugs most effective for rx of acute bronchospasm | beta-2 adrenergic agonists |
| Group of drugs most effective for rx of exercise-induced asthma | beta-2 adrenergic agonists |
| List bolded drugs for rx of acute bronchospasm | albuterol is the DRUG OF CHOICE for acute bronchospasm. also terbutaline |
| List bolded drugs for rx of exercise-induced asthma (EIA) | (the beta-2 adrenergic agonists): albuterol, terbutaline, salmeterol (long-acting; used, as is albuterol, for prevention of EIA) |
| "In which condition" are inhaled corticosteroids the "choice" for an asthma patient? | long-term control in patients who require beta-2 agonists >2x per week |
| Potential side effect of inhaled corticosteroids | increased risk of oral candidiasis ("thrush") |
| List bolded examples of inhaled corticosteroid drugs | beclomethasone (Beclovent) |
| MOA for cromolyn | inflammatory cell stabilizer (prevents release of histamine from mast cells, macrophages, neutrophils, eosinophils |
| Use of cromolyn | prophylaxis of asthma attacks |
| MOA for montelucast | leukotriene modifier (blocks binding of cysteinyl leukotrienes) |
| Use of montelucast | prevention and chronic treatment of asthma |
| Use of omalizumab | monoclonal Ab specific for IgE (used for allergic asthma) |
| Use of surfactant | infants with infant respiratory distress syndrome (administered "endotracheally") |
| Use of dornase-alfa | (one of the "Miscellaneous" respiratory drugs) Used in CYSTIC FIBROSIS (inhaled) to decrease viscosity of bronchial secreations |
| MOA for sildenafil (for rx of ED) | Inhibits phosphodiesterase-5 (PDE5), the enzyme that "unrelaxes" the smooth muscle relaxation of the penis (via cyclic adenosine monophosphate (cAMP) & cyclic guanosine monophosphate (cGMP)) |
| Danger of combining sildenafil (tadalafil, vardenafil) & nitrates | sudden & life-threatening drop in BP |
| MOA for biphosphonates | They inhibit osteoclastic activity (and decrease bone t/o and resorption) |
| Use(s) of biphosphonates | "established" osteoporosis. Also Paget's disease |
| List bolded examples of biphosphonates | Fosamax (alendronate) |
| Other than biphosphonates, what groups of drugs are used to treat osteoporosis? (think of dry ("secC") bones) | Estrogens, calcitonin, vit D/calcium and SERMs (e.g., raloxifene). Remember that raloxifene is agonist in bone but ANTAGONIST in breast & uterus! |
| List classes of anti-obesity drugs | anoreixiants (remember FenPhen??!!) and lipase inhibitors (orlisat) |
| MOA for orlisat | It's a lipase inhibitor (from pancreas). Decreases intestinal digestion of fats |
| Difference between bacteriostatic and bacteriocidal antibiotics | Bacteriostatic stop growth and reproduction and bactericidal kill bacteria |
| List bolded antibiotics that prevent cell wall synthesis | Penicillin, cephalosporins, clavulanic acid |
| "What do meant by" beta-lactam antibiotics? | They contain a B-lactamase ring in their structure (not SI beyond that) |
| How do some bacteria inactivate beta-lactam antibiotics? | Some bacteria contain an enzyme, beta-lactamase , that can "open" the beta-lactam ring of the beta-lactam ABX and inactivate them |
| Drug of choice for rx of syphilis | penicillin-G |
| Which penicillins are effective against Pseudomonas aeruginosa? | carbenicillin and pipericillin |
| MOA for clavulanic acid (as part of Augmentin combo) | it inhibits penicillinases |
| What are the uses of 3rd generation cephalosporins (e.g. cefriaxone (Rocephin))? | 1st line rx for gonorrhea; also for (H. flu) meningitis in kids |
| Potential side effects of aminoglycoside drugs | Nephrotoxicity, ototoxicty, neuromuscular toxicity |
| What is the synergy between penicillin and aminoglycoside? | Penicillin causes cell wall abnormalities to let in the aminoglycosides. |
| What is oral neomycin used for? | Hepatic coma (mostly used TOPCIALLY for skin infections) Not for kids....slows cartilage growth. (Due to the inherent oto- & nephrotoxicity of the aminoglycoside antibiotics, systemic use is rare.) |
| Use(s) of tetracyclines | (ricketts), chlamydia (mycoplasma, borrelia) |
| MOA for class III antiarrhythmics | The K+ channel blockers. They prolong REpolarization. |
| Give an example of a class III antiarrhythmic | Amiodarone |
| What is special about macrolide antibiotics? | Safe in pregnancy! |
| Use of macrolide antibiotics | Drug (class) of choice for Legionella pneumonia as well as mycoplasma infections |
| List bolded examples of macrolide antibiotics | erythromycin, azithromycin, clarithromycin |
| Potential side effects of chloramphenicol | BONE MARROW SUPPRESSION & APLASTIC ANEMIA. "GRAY BABY SYNDROME" |
| Potential adverse effect of clindamycin | C. dificile |
| MOA for TMP-SMX (aka cotrimoxazole) | folate antagonist |
| Use(s) of TMP-SMX (aka cotrimoxazole) | UTI and PCP pneumonia |
| MOA for quinolone antibiotics | They inhibit DNA gyrase & topoisomerase (bacterial DNA replication) |
| Potential adverse effects of quinolone antibiotics | damage to cartilage growth |
| List bolded examples of quinolone antibiotics | all the "floxacins": ciprofloxacin, norfloxacin, moxifloxacin |
| What are 2 uses of metronidazole? | giardia and "antibiotic-associated enterocolitis" (e.g., pseudomembranous colitis caused by C. dificile) |
| Why is TB necessarily treated with combo rx? | to prevent development of drug resistance |
| Potential side effects of isoniazid | hepatotoxicity, PERIPHERAL NEUROPATHY |
| Recommended vitamin supplementation to prevent peripheral neuropathy from isoniazid | B6 |
| How might rifampin affect the liver? | rifampin is potent INDUCER of cytochrome p450 enzyme |
| Potential side effect of ethambutol | liver toxicity (hepatitis), also red-orange secretions!! |
| "Mainstay" treatment of leprosy | dapsone |
| What drug has might be used in leprosy and TB? | RIFAMPIN! |
| Most commonly used antifungal drug for DISSEMINATED (fungal) infections | amphotericin |
| Most common toxicity/side effect of amphotericin | KIDNEY DAMAGE (nephrotoxicity) |
| MOA for HIV RT inhibitors | they inhibit the synthesis of viral DNA from viral RNA by stopping RT enzyme |
| "Name 3 subgroups" of RT inhibitors (in HIV infection) | nuke, nonnuke, nucleoTIDE |
| List bolded examples of nucleoside RT inhibitors (for tx of HIV infection) | lamivudine, zidovudine, efavirenz |
| Post-exposure prophylaxis combo (old) for HIV needle stick | AZT+3TC (lamivudine) |
| MOA for protease inhibitors (for tx of HIV and HCV infection) | foils the assembly of newly formed viral particles |
| List bolded examples of protease inhibitors (for tx of HIV infection) | amprenavir, indinavir |
| Potential side effects of HIV protease inhibitors | (not in handout) I would said GI stuff, hyperlipidemias, and fat redistribution abnormalities |
| List bolded examples of meds used to treat flu (influenza) | amantadine, zanamivir |
| MOA of neuraminidase inhibitors (e.g., zanamivir) to treat influenza | block release of baby flu viruses from infected cells |
| Use of amantidine | handout says "rx and prevention of influenza-A infections" |
| List bolded drugs used to treat HSV (1 or 2) | ACV |
| List bolded drugs used to treat CMV | gancyclovir is DRUG OF CHOICE. foscarnet also used, but very toxic |
| An odd use of ribavirin | Respiratory Syncytial Virus (RSV) infections!! |
| List bolded drugs used to treat HBV | interferon-alpha, peg interferon-alpha, lamivudine |
| List bolded drugs used to treat HCV | peg interferon + RIBAVIRIN |
| MOA for interferon-alpha | induces cellular enzymes (host) that inhibit viral RNA TRANSLATION |
| MOA for methotrexate | binds & competitively inhibits DIHYDROFOLATE REDUCTASE |
| Use(s) of methotrexate | a "whole variety of cancers" plus PSORIASIS and severe RA |
| MOA for doxorubicin | disrupts S and G2 phases of cell cycling ("DNA function") |
| Potential side effects of doxorubicin | CARDIOTOXICITY, hair loss, BM suppression |
| Potential side effects of bleomycin | can cause FATAL PULMONARY FIBROSIS (use with extreme caution in pts. with pre-existing lung disease) |
| MOA of vincristine | mitotic inhibitor |
| MOA of vinblastine | antimicrotubule drug |
| Potential side effects of vincristine | neurologic toxicity |
| Potential side effects of vinblastine | BM toxicity (vinBlastine, Bone marrow tox) |
| Classify hormonal agents used to treat cancers | glucocorticoids, aromatase inhibitors, antiestrogens, antiandrogens (androgen receptor antagonists), GnRH analogs |
| List bolded drugs from glucocorticoid group of anti-cancer hormonal agents | prednisone!! |
| List bolded drugs from aromatase group of anti-cancer hormonal agents | anastrozole |
| List bolded drugs from antiestrogen group of anti-cancer hormonal agents | tamoxifen |
| List bolded drugs from antiandrogen group of anti-cancer hormonal agents | flutamide (remember this one?) |
| List bolded drugs from GnRH analog group of anti-cancer hormonal agents | leuprolide (how to remember this? leuPROlide... metastatic PROstatic cancer) |
| Use of imatinib | CML (@ $90,000 a year) |
| Use of etoposide | small cell lung cancer |
| Use of cisplatin | testicular cancer ("cure rate" 10-85%) |
| Use of procarbazine | Hodgkin's lymphoma (and glioblastoma multiforme) |
| Use of L-asperginase | Useful in treatment of leukemia |
| Use of BCG vaccine in cancer | This Euro vaccine against TB has shown effectiveness in treating bladder cancer! |
| MOA for NSAIDs | they inhibit COX-1 and COX-2 (cyclo-oxygenase) enzymes (first step in prostaglandin synthesis) |
| "What serious adverse effect can happen when using aspirin in viral infections?" | can cause Reye syndrome (especially in children) |
| Special use of indomethacin | patent ductus arteriosus (PDA) in newborn babies |
| What is special about COX-2 inhibitors? | they do not inhibit platelet aggregation (so lower risk of GI bleed) |
| Use of COX-2 inhibitors | "chronic use" (but LT use of COX-2s may increase MI risk/stroke!!) |
| List bolded examples of COX-2 inhibitors | (they end in COXib): celocoxib, rofecoxib |
| MOA of acetominophen | inhibits prostaglandin synthesis in CNS!! (thus its fever & pain power. less good at inflammation) |
| "Action" of acetominophen | fever, pain. less effect on inflammation |
| Limitations of use of acetominophen | weak anti-inflammatory activity |
| Use of methotrexate | was mostly a cancer drug. also used in bad cases of psoriasis and severe RA |
| Use of D-penicillamine | "arthritis" and also as chelating agent in heavy metal poisoning. also Wilson's disease!!? |
| Use of infliximab | monoclonal Ab used in arthritis as well as Crohn's!! |
| MOA for infliximab | binds and inactivates TNF-alpha |
| MOA for cyclosporine | stops IL-2 production by binding something called calcineurin |
| Use(s) of cyclosporine | agent of choice for prev/treat transplant rejection (but needs azathiprione in order to give low dose) |
| Potential side effects/toxicities of cyclosporine | KD toxicity, neuro toxcity, THROMBOEMBOLISM, seizure!! |
| MOA for allopurinol (in gout) | inhibits xanthine oxidase (and thus uric acid formation) |
| MOA for colchicine (in gout) | stops the migration of neutrophils to site of inflammation!! (for ACUTE ATTACKS) |
| MOA for probenacid (in gout) | increases uric acid excretion in kidneys (PRO-ben-ACID) |
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mrbarr
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