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Pharma Final 2012

Qs&As from Review Sheet for Pharmacology Final Nov 2012

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)
Created by: mrbarr