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Pharmacology > Final Review... > Flashcards

Final Review... Flashcards

1
Q

What is the mechanism of action of ACE inhibitors? What is its well-known side effect?

A
  • Block Synthesis of Angiotensin II to prevent vasoconstriction.
  • Reduce Aldosterone secretion from adrenal cortex resulting in net water loss.
  • Cause DRY IRRITATING COUGH, H/A, Dizziness, Abd pain, confusion, renal failure & impotence
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2
Q

What are the mechanisms of actions of Thiazide diuretics, and of loop diuretics? What are the undesirable effects of loop diuretics?

A
  • Thiazide Diuretics - Inhibit Na+ & Chloride reabsorption in thick ascending tubule & early distal tubule.
  • Loop Diurectics - Inhibit Chloride reabsorption in ascending loop of Henle (Effects can include OTOTOXICITY, HYPOnatremia, Hypokalemia, Hypocalcemia, Hypomanesemia, HYPERglycemia, HYPERuricemia.
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3
Q

What is the mechanism of action of cardiac glycosides? Give an example. What precaution is to be taken when using these drugs? List their toxicities.

A
  • Inhibit NA+, K+, ATPase. Cause increase in level of NA+ in myocytes which lead to rise in level of intracellular calcium ions.
  • Digoxin/Lanoxin/Digitoxin - Cardiac Glycoside
  • Low therapeutic index - can cause Arrythmias, Anorexia, Nausea, Diarrhea, drowsiness, fatigue & visual disturbances.
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4
Q

What are the mechanisms of actions of class I, class III, and class IV antiarrhythmic drugs? Give important examples of each group.

A
  • Class I - NA+ channel blockers QUINIDINE, Procainamide, LIDOCAINE - block NA+ entry into cell during depolarization. Decreases rate of rise of Phase 0 of action potential. -
  • Class III - K+ channel blockers AMIODARONE, Sotalol - prolong repolarization, useful in treating intractable ventricular arrythmias. -
  • Class IV - CA+ channel blockers VERAPAMIL, Diltiazem - slow inward CA+ current, slow conduction & prolong effective refractory period, esp in AV Node. (Effectvice against Atrial Ventricular arrythmias)
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5
Q

What is the mechanism of action of organic nitrates in relieving angina? What is the drug of choice for acute coronary spasm? What are its routes of administration?

A
  • Dilate the large myocardial arteries to increase the blood supply of the heart; also reduce cardiac preload by reducing venous tone.
  • NITROGLYCERINE - Rx. of choice,
  • given SUBlingually for rapid onset and applied transdermally for longer duration of action.
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6
Q

What is the mechanism of action of β-blockers in relieving angina? What are their contraindications? How these drugs should be tapered off?

A
  • β-blockers Lower rate & force of contraction in order to decrease Oxygen demands of MYOcardium. Block B1 receptors.
  • C/I - Px. w. Asthma, Diabetes, Severe Bradycardia, peripheral vascular disease or COPD
  • NOT abrubtly. Should be tapered off over 2-3 weeks to avoid rebound angina or Hypotension.
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7
Q

List group of antihypertensive drugs useful in treating diabetes patients, African-Americans, patients with angina, and pregnant women.

A
  • Diabetes - ACE Inhibitors
  • Af-Am’s - Calcium Channel blockers, 55+ too
  • Angina Px. - Sodium Nitroprusside?
  • Pregnant Women - Methyldopa - Central/CNS acting
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8
Q

List important antiplatelet drugs. What are the mechanisms of actions of aspirin and clopidegrol?

A
  • Aspirin - Inhibits platelet aggregation, thomboxane A2 synthesis, prolongs bleeding time.
  • Clopidegrol - Blocks by irreversibly inhibiting binding of ADP, inhibits activation of GPIIb/IIIa
  • GPIIb/IIIa receptor ANTAGONISTs - Abciximab
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9
Q

What is the action of heparin? What is its important side effect? What drug is used to treat that side effect?

A
  • Anticoagulant - binds to Antithrombin III, blocks thrombin & Xa.
  • A/E - hemorrhage
  • Protamine - is heparin antagonist used to treat heparin-induced hemorrage.
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10
Q

What is the mechanism of action of oral anticoagulants? Give an example.

A
  • Antagonize Vitamin K, interfere with synthesis of Vit. K dependent clotting factors - II, VII, IX, X
  • Warferin/Coumadin - prevents clot formation (avoid cranberry juice)
  • Dicumarol

* Antidote = Vitamin K, helps overcome anticoagulant effects of oral a’s.

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11
Q

Define thrombolytic drugs? What is their mechanism of action? Give an example.

A
  • Used to Lyse already formed clots - work better w/in shorter period of injury.
  • Activates plasminogen to plasmin which digests fibrin forming degradation products
  • Examples:
  1. Streptokinase; Reteplase; Alteplase
  2. Tissue Plasminogen Activator t-PA
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12
Q

List the drugs used to treat anemia of end-stage renal failure and megaloblastic anemia?

A
  • Erythropoieitin - stimulates erythropoieisis in KD
  • Cyanocobalamin ( Vit. B12) - treats megaloblastic anemia
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13
Q

What is the mechanism of action of HMG- CoA reductase inhibitors? What are their side effects? List important drugs of this group

A
  • Inhibit HMG-CoA reductase (enzyme controls rate-limiting step in cholesterol synthesis) — Decreases LDL, VLDL & TG — INcreases HDL
  • Can cause myopathy, rhabdomyolysis & LV Fx. abnormalities. STOP if muscle pain.
  • Should not be taken with Grapefruit
  • Lovastatin, Simvastatin, Most potent are = Atrovastatin & Rosuvastatin
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14
Q

What are the mechanisms of actions of Niacin and Ezetimibe (Zetia)? What are the adverse effects of Niacin?

A
  • Niacin - Strongly inhibits Lipolysis in adipose tissue – Decreases LDL, VLDL, TG & INcreases HDL
  • Adverse effect = Flushing & Pruritis - does not allow LV to produce Tryglycerides
  • Ezetimibe/Zetia - Cholesterol Absorption INhibitor - inhibit intestinal absorption of dietary & biliary cholesterol. Decreases LDL, TG & INcreases HDL.
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15
Q

List important drugs used to treat hyperthyroidism. What are the mechanisms of actions of Methimazole and Propylthiouracil?

A
  • Hyperthyroidism treated by Methimazole/Tapazole; Propylthiouracil/PTU; Iodine/Iodide; Propranolol b-blockers
  • Methimazole - Inhibits Iodide & Thyrosene coupling & prevents forming of thyroid hormone.
  • Propylthiouracil - Inhibits peripheral conversion of T3 & T4
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16
Q

What are the complications of using Glucocorticoids? What are the uses of Spiranolactone and Ketoconazole?

A
  • Glucocorticoids need to be tapered off; otherwise can cause acute adrenal insufficiency syndrome

​* Inhibitors of Adrenal Hormone Synthesis & action:

  • Spiranolactone - Antihypertensive drug, competes for aldosterone receptor inhibiting sodium reabsorption in KD’s; antagonizes aldosterone & testosterone synthesis. Used for hirsutism
  • Ketoconazole - antifungal agent; Inhibits gonadal & adrenal steroid hormone synthesis - Tx Cushing’s
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17
Q

What are the uses of Raloxifene, Clomiphene, and Medroxyprogesterone, and Mifepristone?

A
  • Raloxifene - SERMS - Agonist activity in bone & Antagonist activity in breast & endometrial tissue - used to Prevent OSTEOPOROSIS
  • Clomiphene - SERMS - Estrogen Receptor agonist in Hypothalamus, used to increase GnRH & gonadotropins to stim ovulation. Used to treat infertility in Women.
  • Medroxyprogesterone - PROGESTINS - in oral contraceptives, HRT & Tx of Uterine bleeding/DUB, Dysmenorrhea & Endometriosis.
  • Mifepristone - Antiprogestins - works to terminate pregnancy, breaks down uterine lining.
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18
Q

What are the major side effects of oral contraceptives? What is special risk in smokers and more than 35 year of age group?

A
  • Side effects = breast fullness, nausea & vomiting (estrogen), depression, & edema (progestin)
  • Abnormal clotting in women who smoke & 35+
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19
Q

What are the two groups of Antiandrogens? What are the uses of Finasteride and Flutamide?

A
  1. 5-a-reductase inhibitors: Testosterone/DHT inhibited – FINASTERIDE - treats BPH & male pattern baldness
  2. Androgen receptor antagonists:** competitive inhibitor – **FLUTAMIDE - treats Prostate carcinoma
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20
Q

What are the mechanisms of actions of lowering blood glucose by α-glucosidase inhibitors and Glitazones? List important drugs of each group? Which hypoglycemic drug has been proven to decrease cardiovascular mortality?

A
  • α-glucosidase inhibitors - slows carb digestion by inhibiting and lowering serum levels after meals, creates gas & Hypoglycemia
  1. Acarbose
  2. Miglitol
  • Glitazones/Thiazolidinediones - improves insulin resistence by enhancing response of target cells. can cause ovulation in PCOS. *Needs LV monitoring.
    1. Rosiglitazone/Avandia
  • Metformin - Biguanides- can decrease Cardio mortality, diagnosed for type 2 DM & PCOS
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21
Q

Which group of drugs are the most effective drugs available for the treatment of acute bronchospasm and for prevention of exercise-induced asthma? Give examples.

A

B2 -adrenergic agonists: cause bronchodilation by activation of B2 adrenergic receptors on bronchial smooth muscle

  • Albuterol, drug of choice
  • Terbutaline
  • Salmeterol - for long lasting
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22
Q

In which condition inhaled corticosteroids are the drugs of choice for asthma patients? What may be their side effect? Give an example

A
  • Preferred for patients who require B2 agonists more than 2x a week
  • Increase risk of oral candidiasis (Thrush) infections
  • Rx include BECLOMETHASONE & PREDNISONE
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23
Q

What is the mechanism of action and use of Cromolyn?

A
  • Cromolyn is an Inflammatory cell stabilizer & prevents release of histamine from mast cells, macrophages, neutrophils & Eosinophils
  • Used for Prophylaxis of asthma attacks
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24
Q

What is the mechanism of action and use of Montelukast?

A
  • Montelukast is a Leukotriene modifier which blocks binding of Leukotriene D4 (LTD4) to its receptor.
  • Used as prophylaxis & chronic asthma tx.
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25
Q

What are the uses of Surfactant, and Dornase alfa?

A
  • Surfactant - given endotracheally in infant respiratory distress, esp premature babies
  • Dornase Alfa - administered via inhalation to patients w. Cystic fibrosis to decrease viscosity of bronchial secretions.
26
Q

What is the mechanism of action of Sildenafil in treating erectile dysfunction? What is the danger of using it with nitrates?

A
  • Sildenafil/Viagra - potentiate the hypotensive action of nitrates.
  • Could result in a fatal drop in BP when used together with nitrates.
27
Q

What are the mechanisms of actions and uses of biphosphonates? Give an example. What are the other groups of drugs used in the treating osteoporosis?

A
  • Biphophonates - inhibit osteoclast destruction activity & decrease bone turnover & resorption, used in Paget’s disease.
  • Alendronate/Fosamax, must be taken 1st thing in AM w. Full glass of water on empty ST & patient must sit upright for at least an hour.
  • Other types:
  1. SERMS - selective Estrogen Receptor Modulators - Raloxifene
  2. Estrogens - enhance calcium retention & retard bone loss
  3. Calcitonin - regulates calcium by inhibiting osteoclast activity
  4. Vitamin D & Calcium supplements - LV & KD produce to increase absorption - lack of sunlight can cause Rickets in kids & Osteomalasia in adults
28
Q

Classify anti-obesity drugs. What is the mechanism of action of Orlisat?

A
  • Anorexiants - note - FenPhen removed, Phentermine & Sibutramine still used
  • Lipase Inhibitors - Orlisat, is a reversible pancreatic lipase inhibitor approved for management of patients with body mass index greater than 30kg/m2
29
Q

What is the difference between Bacteriostatic and bactericidal antibiotics?

A
  • Bacteriostatic - stop the growth & replication of bacteria
  • Bacteriocidal - kill bacteria
30
Q

List the antibiotics which act by inhibiting bacterial cell wall synthesis.

A
  • B-Lactam antibiotics:
  1. Penicilins
  2. Cephalosporins
  • Others:
  1. Vancomycin
  2. Bacitracin
  • B-Lactamase Inhibitors:
    1. Clavulanic Acid
31
Q

What is the best drug for treating syphilis patients? Which penicillins are effective against Pseudomonas aeruginosa?

A
  • Benzathine Penicillin G = Syphillis
  • Pseudonomas Aeruginosa = Piperacillin & Carbenicillin (after Sx. or severe burn)
32
Q

What is the action of Clavulanic acid in Augmentin?

A
  • Clavulanic Acid kills Penicillinase while the Amoxicillen kills the bacteria
33
Q

What are the uses of third generation cephalosporin—Ceftriaxone?

A
  • Ceftriaxone - Gonorrhea & used for tx. of meningitis in children (Hemophyllus Influenzae)
34
Q

What are side effects of Aminoglycosides?

How are Penicillins & Aminoglycosides synergistic?

What is the use of oral neomycin?

A
  • Aminoglycosides - inhibit 30s protein synthesis - can cause nephrotoxicity, ototoxicity & neuromuscular toxicity.
  • Work well together because Penicillin causes cell wall abnormalities that allow aminoglycosides to get into the bacteria.
  • Neomycin used orally in hepatic coma to decrease coliform flora thus decreasing production of ammonia.
35
Q

What are the uses and side effects of Tetracyclines?

A
  • Tetracyclin used for Chlamydia & specific infections: C/I in pregnancy & children. Can’t give with milk/chelates.
  • Stain teeth, retardation of bone growth & photosensitivity.
36
Q

What are the uses of Macrolides? Give examples.

A
  • Macrolides - bind to 50s & inhibit translocation steps of protein synthesis
  • Used in Px. with Mycoplasma, Pneumonia, Legionnaire’s Disease, Chlamydial infections, Diphtheria & Pertussis
  • Safe to use during pregnancy*
  • Erythromycin
  • Azithromycin
37
Q

What are the adverse effects of chloramphenicol?

A
  • Not used often; Can cause Bone Marrow depression and aplastic anemia.
  • Can also cause Gray baby syndrome in infants
38
Q

What is the use of Clindamycin? What adverse effect can be caused by its use?

A
  • Clindamycin - used for anaerobic GI infections.
  • Can cause Pseudomembranous colitis bc C. Deficile is resistent to it. Antibiotic Associated Diarrhea.
39
Q

What is the mechanism of action of Trimethoprim-Sulfamethoxazole (Cotrimoxazole)? What are its uses?

A
  • Trimethoprim-Sulfamethoxazole/Cotrimoxazole - combo of Sulfonamide & Trimethoprim are Synergystic for affecting PABA/folate de novo for bacteria that is impermiable to folic acid.
  • Used for UTI & Pneumocystitis Carinii Pneumonia
40
Q

What are mechanisms of actions and adverse effects of Quinolones? List important drugs of this group

A
  • Quinolones - inhibit DNA gryase & topoisomerase IV thereby inhibiting Bacterial DNA replication. (BROAD-SPECTRUM antimicrobial agents)
  1. Norfloxacin
  2. Ciprofloxacin
  3. Levofloxacin
41
Q

What are the uses of Metronidazole?

A
  • Metronidazole - used for trichomoniasis (STD), Amebiasis (Dysentery) & Gardiasis (Dysentery)
  • Drug of choice for Pseudomembranous Colitis caused by C. Deficile
  • Inhibits DNA synthesis
42
Q

Why anti-tubercular drugs are given as a combination therapy? What are the adverse effects of Isoniazid? How peripheral neuropathy can be prevented?

A
  • Combo therapy used to prevent the emergence of resistent strains - 6-8 months of tweeking.
  • Isoniazid has been assoc. w. Hepatotoxicity & Peripheral Neuropathy
  • Peripheral neurpoathy prevented by Vitamin B6
43
Q

What are the effects of Rifampin on liver? What is the adverse effect of Ethambutol?

A
  • Rifampin - is a potent inducer of C-P450 enzymes. Can cause heptaitis & may color secretions red-orange.
  • Ethambutol - can cause retrobulbar Optic Neuritis.
44
Q

What is mainstay of treatment of leprosy? Which drug is both an antileprosy and anti-TB drug?

A
  • Dapsone - mainstay Tx. of leprosy
  • Rifampin - is both an antileprosy & Anti-TB Rx.
45
Q

What is the most commonly used antifungal drug to treat serious disseminated infections? What is its most common toxicity?

A
  • Amphotericin B
  • Can cause Nephrotoxicity
46
Q

What is the mechanism of action of Reverse Transcriptase Inhibitors used in the treatment of HIV infection? Name its three subgroups. Give examples of Nucleosides. What combination of drugs is given to healthcare providers after accidental needle sticks?

A
  • Inhibit formation of viral DNA from RNA by Reverse Transcriptase enzyme which is very rapid.
  1. Nucleosides (NRTI’s) - **Zidovudin, *Lamivudine*, Zalcitabine
  2. Nucleotides - Tenofovir
  3. Nonnucleosides (NNRTI’s) - Efavirenz, Nevirapine
  • ​Combivir - combo of Zidovidine + Lamivudine - is given for accidental needle stick.
47
Q

What is the mechanism of action of Protease inhibitors? Give examples. What are their side effects?

A
  • Protease Inhibitors - Atazanavir; Fosamprenavir; Amprenavir - all interfere with processing of viral protein thus preventing formation of new viral particles. Used in HIV - inhibit HIV protease.
  • Can cause lipid abnormalities. Parethesias, Diarrhea, Nausea/Vomiting, Hyperglycemia, Hypertriglyceridemia, Hypercholesterolemia. Accum of fat at back of neck.
48
Q

What are the drugs used to treat influenza? What are their mechanisms of action?

A
  • Amantadine - inhibits virus uncoating @ ENTRY- used for prevention of type A infections.
  • Neurominidase Inhibitors - Block the release of influenza virus from infected cell @ EXIT - used in tx. of both type A & B influenza. Example - ZANAMIVIR; Oseltamivir
49
Q

List important drugs used to treat herpes and cytomegalovirus infections.

A

All inhibit DNA synthesis

  1. ACYclovir** - HSV1, 2 & VZV, EBV & CMV - used topically, IV & orally
  2. GANCYCLOVIR - best choice for CMV infections
  3. Famcyclovir
  4. Vidarabine
  5. Cidofovir
  6. Valacyclovir
  7. Valgancyclovir
  8. FOSCARNET
  9. Fomivirsen
  10. Pencyclovir
50
Q

What is the use of Ribavirin? List important drugs used to treat Hepatitis B and Hepatitis C. What is the mechanism of action of interferons?

A
  • Ribavirin - used for HEP C & tx. of Resp. Syncytial Viral infections (RSV). Interfere w. viral messenger RNA.
  • HEP B is treated by: Aedefovir; Tenofovir, Interferon-a 2a; Pegylated Interferon; & Lamivudine
  • HEP C is treated by: Pegylated Interferon-a 2a & Ribavirin
51
Q

What are the mechanism of action and adverse effect of Cyclophosphamide?

A

Cyclophosphamide - an Alkylating agent works by adding an akyl group to components of DNA aka Alkylation of DNA - prone to cause local tissue necrosis & damage.

  • This drug most commonly used for this process - can cause HEMORRHAGIC CYSTITIS
52
Q

What are the mechanism of action and uses of Methotrexate?

A
  • Methotrexate - it’s an Antimetabolite - binds & competitively inhibits the enzyme, dihydrofolate reductase. (interfere w. Purine or Pyrimidine synthesis)
  • Used to treat: Psoirasis; Rheumatoid Arthritis & variety of Cancers.
  • Leucovorin is given for toxicity, reverses all A/E except neurotoxicity.
53
Q

What are the mechanism of action and adverse effect of Doxorubicin? What is the adverse effect of Bleomycin?

A
  • Doxorubicin - causes Cardiotoxicity; Alopecia & Bone Marrow depression
  • Bleomycin - Can cause fatal Pulmonary fibrosis. Caution w. px. history of pre-exisitng LU disease.
  • Both are ANTIBIOTICS that disrupt DNA Fx. of S & G2 phase
54
Q

What are the mechanism of action and adverse effects of Vinca Alkaloids—Vincristine and Vinblastine?

A
  • Vinca Alkaloids: microtubule- inhibitors, bind to tubules & disrupt spindle apparatus during cell divison
  • Vincristine - has Neurologic toxicity
  • Vinblastine - has Bone Marrow toxicity
55
Q

Classify hormonal agents used to treat cancers. List a drug of each group

A
  • Glucocorticoids - Prednisone - inhibit cell growth & proliferation, leukemia; Hodgkin’s.
  • Aromatase Inhibit - Anastrozole - estrogen-resisitent breast cancer resistent to tamoxifen.
  • Antiestrogens - Tamoxifen - competitive antagonists of estrogen receptor, breast cancer
  • Androgen receptor antagonists - Flutamide - used in prostate cancer
  • GnRH Analogs - Leuprolide - used in metastatic prostatic cancer
56
Q

What are the uses of Imatinib, Cisplatin, and Bacille Calmette-Guerin (BCG) vaccine in cancer?

A
  • Imatinib - used to Tx. Chronic Myeloid Leukemia
  • Cisplatin - used to Tx. testicular carcinoma, ovarian carcinoma & bladder carcinoma
  • Bacille Calmette-Guerin (BCG) - TB vaccine used to tx. small localized superficial UB carcinoma - intravesicular use - early stage only
57
Q

What is the mechanism of action of NSAIDs? What serious adverse effect can happen when using aspirin in viral infections? What is a special use of Indomethacin?

A
  • NSAIDS - inhibit cyclooxygenase enzymes that catalyze 1st step of prostaglandin biosynthesis.
  • Aspirin can cause Reye Syndrome if given in viral infections, esp in children.
  • Indomethacin - used in Patent Ductus Arteriosus (PDA) in newborn babies.
58
Q

What is the use of and advantage of using COX-2 inhibitors? Give an example.

A
  • COX-2 inhibitors - don’t inhibit platelet aggregation & has a lower risk for GI bleeding, good for chronic use.
  • CELOCOXIB/Celebrex
  • May cause hypertension
59
Q

What are the actions, mechanism of action, and limitations of using Acetomenophen?

A
  • Acetomenophen - Inhibits prostaglandins synthesis in CNS.
  • Has less effect on cyclooxygenase in peripheral tissues - weak anti-inflamm. activity.
60
Q

What are the uses of methotrexate, D-penicillamine, and inflliximab? What is the mechanism of action of Infliximab?

A
  • Methotrexate - DMARD - Arthritis, more widely used.
  • D-penicillamine - DMARD - Arthritis, also chelating agent in heavy metal poisoning & Wilson’s Disease.
  • Infliximab - Rx. for Arthritis - binds to TNF-a & neutralizes cytokines - used in Crohn’s disease
61
Q

What are the mechanisms of actions of Allopurinol, Colchicine and Probanacid in Gout?

A
  • Allopurinol - inhibits Xanthine Oxidase, reduces Uric Acid formation.
  • Colchicine - decrease migration of neutrophils to inflamm. site; inhibits synthesis of leukotries - used in acute attack of gout
  • Probanacid - increases uric acid excretion by the KD’s (Uricosuric Rx.)
62
Q

What are the mechanism of action, uses and toxic effects of Cyclosporine?

A
  • Cyclosporine - inhibits rejection of transplanted tissue. Specific T-Cell inhibitor. Inhibits synthesis of IL-2 responsible for T Cell growth & Fx.
  • Toxic effects: Nephrotoxicity, thrombo-embolism, neurotoxicity, Seizure, etc.
  • used in conjunction w. Azathioprine bc of A/E

Pharmacology (4 decks)

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