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USMLE Step 1 Pharmacology

Subjects : health-sciences, usmle-step-1

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Answer 50 questions in 15 minutes.
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1. List the mechanism - clinical use - & toxicity of Methotrexate.
- S- phase anti - metabolite folate analogue - Luk - Lymp - sarc - RA - & psoriasis / - Reversible myelosuppression
- Alkalates DNA - CML - Pulmonary fibrosis hyperpigmentation
- Class III antiarrhythmics (sotalol) - class IA (quinidine)
Tetracycline - Doxycycline - Demeclocycline - Minocycline

2. What enzymes are inhibited by NSAIDs - acetaminophen and COX II inhibitors?
Chronic gout.
Ceftriaxone
decrease the slope of phase 4 - increase PR interval (the AV node is particularly sensitive)
Cyclooxygenases (COX I - COX II).

3. Mg+- clinical use?
effective in torsade de pointes and digoxin toxicity
Only in limited amounts
GI upset
- Vitamin K & fresh frozen plasma

4. What are three toxicities of Propylthiouracil?
Inhibits reabsorption of uric acid.
1. Skin rash 2. Agranulocytosis (rare) 3. Aplastic anemia
check PFTs - LFTs - and TFTs
Sucralfate cannot work in the presence of antacids or H2 blockers because it requires an acidic environment to polymerize.

5. K+- clinical use?
Staphlococcus aureus and Clostridium difficile (pseudomembranous colitis)
depresses ectopic pacemakers - especially in digoxin toxicity
Diarrhea
Nifedipine - Verapamil - Diltiazem

6. List the specific antidote for this toxin: TPA & Streptokinase
- Aminocaproic acid
- Tricyclic antidepressants
Chronic gout.
Norepinephrine

7. What are three clinical uses of the Leuprolide?
1. Infertility (pulsatile) 2. Prostate cancer (continuous: use with flutamide) 3. Uterine fibroids
Chronic gout.
Giant Roundworm (Ascaris) - Hookworm (Necator/Ancylostoma) - Pinworm (Enterobius)
constipation - flushing - edema - CV effects (CHF - AV block - sinus node depression) - and torsade de pointes (Bepridil)

8. What is a mnemonic to remember Amantadine's function?
Blocks Influenza A and RubellA; causes problems with the cerebellA
Hormone synthesis inhibition (Gynecomastia) - Liver dysfunction (Inhibits CYP450) - Fever - Chills
- Flumazenil
- Phenytoin

9. Which H2 Blocker has the most toxic effects and What are they?
Prevention of NSAID- induced peptic ulcers - maintains a PDA.
Cimetidine is a potent inhibitor of P450; it also has an antiandrogenic effect and decreases renal excretion of creatinine. Other H2 blockers are relatively free of these effects.
- EDTA - dimercaprol - succimer - & penicillamine
Same as penicillin. Act as narrow spectrum antibiotics

10. What is treated with Chloroquine - Quinine - Mefloquine?
Non - Nucleosides
Inhibits CMV DNA polymerase
They activate the ciliary muscle of the eye (open angle) and pupillary sphincter (narrow angle).
Malaria (P. falciparum)

11. What are the indications for using amphetamine?

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12. Dobutamine used for the tx of shock acts on Which receptors
Same as penicillin. Act as narrow spectrum antibiotics
Beta1 more than B2
No - it inhibits the release of Nor Epi
Due to the presence of a bulkier R group

13. What are the clinical indications for Azole therapy?
Aplastic anemia (dose independent) - Gray Baby Syndrome
Systemic mycoses
Cephalosporins
Corticosteroids; prevent production of leukotrienes from arachodonic acid by blocking phospholipase A2. Drugs of choice in a patient with status asthmaticus (in combination with albuterol.)

14. Which Aminoglycoside is used for Bowel Surgery ?
Norepinephrine
Post - op and neurogenic ileus and urinary retention - myasthenia gravis - and reversal of neuromuscular junction blockade (post - op) through anticholinesterase activity.
Stimulates beta adrenergic receptors
Neomycin

15. What are the clinical uses for Imipenem/cilastatin?
Gram + cocci - Gram - rods - and Anerobes
- MT polymerization stabilizer - Ovarian & breast CA - Myelosupperession & hypersensitivity.
TCA
Glycoproteins from leukocytes that block various stages of viral RNA and DNA synthesis

16. What are the classic symptoms of cholinesterase inhibitor poisoning (parathion or other organophosphates)?
constipation - flushing - edema - CV effects (CHF - AV block - sinus node depression) - and torsade de pointes (Bepridil)
Lovastatin - Pravastatin - Simvastatin - Atorvastatin
very short acting
Diarrhea - Urination - Miosis - Bronchospasm - Bradycardia - Excitation of skeletal muscle and CNS - Lacrimation - Sweating - and Salivation = DUMBBELS; also abdominal cramping

17. Spironolactone - mechanism?
Hemolytic anemia
Give an antichloinesterase - neostigmine - edrophonium - etc
physostigmine
competitive inhibirot of aldosterone in the cortical collecting tubule

18. Which drug(s) cause this reaction: Hepatitis?
- Isoniazid
PT
Ototoxicity - Hypokalemia - Dehydration - Allergy (sulfa) - Nephritis (interstitial) - Gout
Inhibit intestinal bursh border Alpha - glucosidases; delayed hydrolysis of sugars and absorption of sugars leading to decresed postprandial hyperglycemia.

19. List the specific antidote for this toxin: Acetaminophen
- N- acetylcystine
Yes - it does not cross the placenta.
- Disulfram & also sulfonylureas - metronidazole
1. Tolbutamide 2. Chlorpropamide 3. Glyburide 4. Glipizide

20. What are three toxicities of Leuprolied?
- Sulfonamides - INH - ASA - Ibuprofen - primaquine - nitrofurantoin /- pyrimethamine - chloramphenicol
Triple Therapy' 2 Nucleoside RT Inhibitors with a Protease Inhibitor
1. Antiandrogen 2. Nausea 3. Vomiting
anuria - CHF

21. What is the mechanism of action of Warfarin (Coumadin)?
Directly of indirectly aid conversion of plasminogen to plasmin Which cleaves thrombin and fibrin clots. (It is claimed that tPA specifically converts fibrin - bound plasminogen to plasmin.)
Warfarin interferes with the normal synthesis and gamma - carboxylation of vitamin K- dependent clotting factors II - VII - IX - and X - Protein C and S via vitamin K antagonism.
Increases mean - systolic - and diastolic bp - while there is little change in pulse pressure.
dry mouth - sedation - severe rebound hypertension

22. Beta Blockers - BP?
decrease
Decreased uptake or Increased transport out of cell
Hemolytic anemia
depresses ectopic pacemakers - especially in digoxin toxicity

23. While at a tail gait party - you bite into a sandwich that a yellow jacket is also enjoying. Knowing your allergy to this creature - What should you do?
- Estrogen receptor antagonist - Breast CA - increased endometrial CA risk
Epinephrine to treat anaphylaxis. Also useful if you have open angle glaucoma - asthma - or hypotension.
- B51Naloxone / naltrexone (Narcan)
Acetylcholinesterase; ACh is broken down into choline and acetate.

24. Which antimicrobial classes inhibit protein synthesis at the 30S subunit? (2)
K+ wasting - metabolic alkalosis - hypotension - ototoxicity
1) Aminoglycosides = bactericidal 2) Tetracyclines = bacteriostatic
Penicillin.
Activates antithrombin III

25. How do the Protease Inhibitors work?
Antibiotic - protein synthesis inhibitor.
1. Antipyretic 2. Analgesic 3. Anti - inflammatory
Inhibt Assembly of new virus by Blocking Protease Enzyme
Heparin catalyzes the activation of antithrombin III.

26. What is the category of drug names ending in - cycline (e.g. Tetracycline)
Antibiotic - protein synthesis inhibitor.
Blood
Pentamidine
Hemicholinium inhibits the transport of choline into the nerve - thus inhibiting formation of ACh.

27. What is the clinical use for Sucralfate?
Peptic ulcer disease.
- Methotrexate - 5 FU - 6 mercaptopurine
vascular sm. Mus.: Nifedipine>Diltiazem>Verapamil
Recurrent UTIs - Shigella - Salmonella - Pneumocystis carinii pneumonia

28. What is the mechanism of action of Misoprostol?
Suramin
Acute gout.
Misoprostol is a PGE1 analog that increases the production and secretion of the gastic mucous barrier.
BM suppression (neutropenia - anemia) - Peripheral neuropathy

29. List the specific antidote for this toxin: Beta Blockers
Mycobacterium tuberculosis - the only agent used as solo prophylaxis against TB
- Glucagon
hypertension - CHF - diabetic renal disease
Indirect agonist - uptake inhibitor

30. How do spare receptors effect the Km?
Small lipid - soluble molecule
Cimetidine is a potent inhibitor of P450; it also has an antiandrogenic effect and decreases renal excretion of creatinine. Other H2 blockers are relatively free of these effects.
Cilastatin
- ED 50 is less than the Km (less than 50% of receptors)

31. What are three possible toxicities of NSAID usage?
Antibiotic - protein synthesis inhibitor.
Prevention of NSAID- induced peptic ulcers - maintains a PDA.
1. Renal damage 2. Aplastic anemia 3. GI distress
Inhibits xanthine oxidase - decresing conversion of xanthine to uric acid.

32. Mannitol - mechanism?
Sulfonamide Loop Diuretic. Inhibits ion co - transport system of thick ascending loop. Abolishes hypertonicity of the medulla - thereby preventing concentration of the urine.
decrease myocardial O2 consumption by: 1- decreasing end diastolic volume 2- decreasing BP 3- decreasing HR 4- decreasing contractility 5- decreasing ejection time
severe orthostatic hypotension - blurred vision - constipation - sexual dysfunction
osmotic diuretic - increase tubular fluid osmolarity - thereby increasing urine flow

33. What is the main clinical use for the thrombolytics?
Early myocardial infarction.
As PABA antimetabolites that inhibit Dihydropteroate Synthase - Bacteriostatic
Reversibly inhibit cyclooxygenase (COX I and COX II). Block prostaglandin synthesis.
atropine - homatropine - tropicamide

34. Mannitol - contraindications?
- Corticosteroids - heparin
anuria - CHF
1) Serious Gram - infections resistant to other Beta lactams 2) Meningitis (most penetrate the BBB)
Warfarin interferes with the normal synthesis and gamma - carboxylation of vitamin K- dependent clotting factors II - VII - IX - and X - Protein C and S via vitamin K antagonism.

35. What is the MOA of Ganciclovir?
Gram + cocci - Gram - rods - and Anerobes
Inhibits CMV DNA polymerase
- Dimercaprol - succimer
Reversibly inhibits cyclooxygenase - mostly in CNS. Inactivated peripherally.

36. How is Acyclovir used clinically?
HSV - VZV - EBV - Mucocutaneous and Genital Herpes Lesions - Prophylaxis in Immunocompromised pts
cardiac muscle: Verapamil>Diltiazem>Nifedipine
Ceftriaxone
Receptors = D1=D2>beta>alpha - thus increasing heart rate (beta) and blood pressure (alpha vasoconstriction) while maintaining kidney perfusion (dopamine receptors)

37. What are common side effects of RT Inhibitors?
BM suppression (neutropenia - anemia) - Peripheral neuropathy
Due to the presence of a bulkier R group
Irreversibly inhibits H+/K+ ATPase in stomach parietal cells.
1. Gastric ulceration 2. Bleeding 3. Hyperventilation 4. Reye's syndrome 5. Tinnitus (CN VIII)

38. What is the effect of epinephrine infusion on bp and pulse pressure?
Mechanism unknown; possibly inhibits gluconeogenesis and increases glycolysis; effect is to decrease serum glucose levels
Increased systolic and pulse pressure - decreased diastolic pressure - and little change in mean pressure.
Megaloblastic anemia - Leukopenia - Granulocytopenia
Beta antagonist.

39. What would be the effect on blood pressure with infusion of the alpha -2 agonist clonidine?
Beta - lactamase cleavage of Beta - lactam ring
- Tetracycline
Initially vasoconstriction would increase bp - but then it acts on central alpha -2 receptors to decrease adrenergic outflow resulting in decreased bp.
It affects beta receptors equally and is used in AV heart block (rare).

40. Name the Protease Inhibitors (4)
Digoxin=urinary Digitoxin=biliary
- Tetracycline - amiodarone - sulfonamides
Saquinavir - Ritonavir - Indinavir - Nelfinavir
YES

41. What is the effect of the Glitazones in diabetes treatment?
Ld= (CpxVd)/F Cp=plasma conc. F= Bioaval.
ARF - shock - drug overdose - decrease intracranial/intraocular pressure
Chronic anticoagulation.
Increase target cell response to insulin.

42. What are three possible complications of Heparin therapy?
Altered bacterial Dihydropteroate Synthetase - Decreased uptake - or Increased PABA synthesis
1. Better bioavailability 2. 2 to 4 times longer half life 3. Can be administered subcutaneously 4. Does not require laboratory monitoring
Flutamide is a nonsteroidal competitive inhibitor of androgens at the testosterone receptor - used in prostate carcinoma.
1. Bleeding 2. Thrombocytopenia 3. Drug - drug interactions

43. The COX-2 inhibitors (celecoxib - rofecoxib) have similar side effects to the NSAIDs with What one exception?
No. Atropine is used to reduce urgency in mild cystitis. So it would aggravate the urinary retention.
The COX-2 inhibitors should not have the corrosive effects of other NSAIDs on the gastrointestinal lining.
Neostigmine - pyridostigmine edrophonium - physostigmine echothiophate
Blocks viral penetration/uncoating; may act to buffer the pH of the endosome

44. Which drug(s) cause this reaction: Focal to massive hepatic necrosis (4)?
- Fluoroquinolones
Methylxanthine.
- Constant AMOUNT eliminated per unit time. - Etoh & ASA
- Halothane - Valproic acid - acetaminophen - Amantia phalloides

45. What Sulfonamides are used for simple UTIs?
carbonic anhydrase inhibitors - K+ sparing diuretics
Triple sulfas or SMZ
Lidocaine - Mexiletine - Tocainide
Initially vasoconstriction would increase bp - but then it acts on central alpha -2 receptors to decrease adrenergic outflow resulting in decreased bp.

46. What cholinergic inhibitor acts by directly inhibiting Ach release at the presynaptic terminal
loop diuretics - thiazides
Cardiac glycoside (inotropic agent).
- Shifts the curve down - reduces Vmax
Botulinum

47. Hydralazine - clinical use?
- Chlorpromazine - thioridazine - haloperidol
severe hypertension - CHF
Increase target cell response to insulin.
1. Buffalo hump 2. Moon facies 3. Truncal obesity 4. Muscle wasting 5. Thin skin 6. Easy bruisability 7. Osteoporosis 8. Adrenocortical atrophy 9. Peptic ulcers

48. Which drug(s) cause this reaction: Atropine - like side effects?
1. Predisposes to viral infections and lymphoma 2. Nephrotoxic (preventable with mannitol diuresis)
- Metronidazole - certain cephalosporins - procarbazine - sulfonylureas
- Act on same receptor - Full has greater efficacy
- Tricyclic antidepressants

49. ACE inhibitors - clinical use?
hypertension - CHF - diabetic renal disease
Malaria (P. falciparum)
Interstitial nephritis
GI disturbances.

50. What is the major toxic side effect of Penicillin?
Minor hepatotoxicity - Drug interactions (activates P450)
- Flumazenil
- reduction - oxy - & hydrolysis - H2O sol. Polar product - P450
Hypersensitivity reactions

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USMLE Step 1 Pharmacology

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