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USMLE Step 1 > Pharmacology > Flashcards

Pharmacology Flashcards

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1
Q

Side effects of ACEI

A

ACEIs dilate afferent arteriole

Hyperkalemia, cough, angioedema (increased bradykinin)

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2
Q

Furosemide

A

Sulfonamide loop diuretic: inhibits Na-K-2Cl symporters in the thick ascending limb of the loop of Henle → increased Na and Cl excretion → increased water excretion

Loop diuretics also stimulate renal prostaglandins which dilate the afferent arteriole → increased renal blood flow → increased GFR → increased drug delivery

Concurrent use of NSAIDs will blunt diuretic response

Indicated for edematous states, HTN, hypercalcemia

SA: ototoxicity, hypokalemia, dehydration, slfa allergies, interstitial nephritis, gout

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3
Q

Spironolactone

A

Competitive aldosterone receptor antagonist in the cortical collecting tubule (K+ sparing diuretic)

Indicated for hyperaldosteronism, K+ depletion, CHF (improves survival)

SA: hyperkalemia → arrhythmias, endocrine effects such as gynecomastia, antiandrogen effects

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4
Q

Eplerenone

A

Competitive aldosterone receptor antagonist in the cortical collecting tubule (K+ sparing diuretic)

Indicated for hyperaldosteronism, K+ depletion, → CHF (improves survival)

SA: hyperkalemia → arrhythmias; fewer side effects than spironolactone

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5
Q

Triamterene

A

Na+ channel blockers in the cortical collecting tubule (K+ sparing diuretic)

Indicated for hyperaldosteronism, K+ depletion, CHF

SA: hyperkalemia → arrhythmias

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6
Q

Amiloride

A

Na+ channel blockers in the cortical collecting tubule (K+ sparing diuretic)

Indicated for hyperaldosteronism, K+ depletion, CHF

SA: hyperkalemia → arrhythmias

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7
Q

Mannitol

A

Osmotic diuretic → increased tubular fluid osmolarity → increased urine flow → decreased intracranial/intraocular pressure

Indicated for drug overdose, increased intracranial/intraocular pressure

SA: pulmonary edema, dehydration

Contraindicated in anuria, CHF

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8
Q

Acetazolamide

A

Carbonic anhydrase inhibitor → NaHCO3 diuresis and decreased total body HCO3- stores

Indicated for glaucoma, urinary alkalinization, metabolic alkalosis, altitute sickness, pseudotumor cerebri

SA: hyperchloremic metabolic acidosis, paresthesias, NH3 toxicity, sulfa allergy

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9
Q

Ethnacrynic acid

A

Phenoxyacetic acid loop diuretic: inhibits Na-K-2Cl symporters in the thick ascending limb of the loop of Henle → increased Na and Cl excretion → increased water excretion

Loop diuretics also stimulate renal prostaglandins which dilate the afferent arteriole → increased renal blood flow → increased GFR → increased drug delivery

Concurrent use of NSAIDs will blunt diuretic response

Indicated for edematous states, HTN, hypercalcemia

SA: ototoxicity, hypokalemia, dehydration, slfa allergies, interstitial nephritis, hyperuricemia → don’t use with gout

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10
Q

Hydrochlorothiazide

A

Thiazide diuretic: inhibits NaCl reabsorption in early distal tubule → decreased diluting capacity of the nephron; decreased calcium excretion

Indicated for HTN, CHF, idiopathic hypercalciuria, nephrogenic DI, osteoporosis

SA: hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia, sulfa allergy

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11
Q

Captopril

A

ACE inhibitor → decreased angiotensin II → dilation of efferent arteriole → decreased GFR

Indicated for HTN, CHF, proteinuria, diabeic nephropathy, prevention of unfavorable remodeling as a result of chronic HTN or MI

SA: cough (ACEI prevent inactivation of bradykinin), angioedema, teratogen, increased creatinine due to decreased GFR, hyperkalemia, hypotension

Contraindicated in bilateral renal stenosis (further decrease in GFR → renal failure)

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12
Q

-sartans

A

Angiotensin II receptor blockers (ARBs)

Decreased risk of cough or angioedema because it does not increase bradykinin

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13
Q

How do diuretics affect serum calcium concentration?

A

Loop diuretics can cause hypocalcemia → hypercalciuria (Loops Loose calcium).

Thiazide diuretics can cause hypercalcemia → hypocalciuria

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14
Q

How do diuretics affect serum potassium concentration?

A

Serum potassium increases with K+ sparing diuretics and decreases with loop and thiazide diuretics.

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15
Q

What effects do diuretics have on acid-base status?

A

Carbonic anhydrase inhibitors and K+ sparing diruetics may cause acidemia.

Loop and thiazide diuretics may cause alkalemia.

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16
Q

Torsemide

A

Sulfonamide loop diuretic: inhibits Na-K-2Cl symporters in the thick ascending limb of the loop of Henle → increased Na and Cl excretion → increased water excretion

Loop diuretics also stimulate renal prostaglandins which dilate the afferent arteriole → increased renal blood flow → increased GFR → increased drug delivery

Concurrent use of NSAIDs will blunt diuretic response

Indicated for edematous states, HTN, hypercalcemia

SA: ototoxicity, hypokalemia, dehydration, slfa allergies, interstitial nephritis, gout

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17
Q

Chlorthalidone

A

Thiazide diuretic: inhibits NaCl reabsorption in early distal tubule → decreased diluting capacity of the nephron; decreased calcium excretion

Indicated for HTN, CHF, idiopathic hypercalciuria, nephrogenic DI, osteoporosis

SA: hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia, sulfa allergy

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18
Q

Bumetanide

A

Sulfonamide loop diuretic: inhibits Na-K-2Cl symporters in the thick ascending limb of the loop of Henle → increased Na and Cl excretion → increased water excretion

Loop diuretics also stimulate renal prostaglandins which dilate the afferent arteriole → increased renal blood flow → increased GFR → increased drug delivery

Concurrent use of NSAIDs will blunt diuretic response

Indicated for edematous states, HTN, hypercalcemia when furosemide is ineffective

SA: ototoxicity, hypokalemia, dehydration, slfa allergies, interstitial nephritis, gout

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19
Q

Metolazone

A

Thiazide-like diuretic

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20
Q

Bethanechol

A

Cholinergic agonist - activates bowel and bladder smooth muscle, resistant to anticholinesterase

Indicated for postoperative ileus, neurogenic ileus, and urinary retention

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21
Q

Carbachol

A

Cholinergic agonist

Indicated for glaucoma (↑ aqueous humor outflow via opening of trabecular meshwork), pupillary constriction, and relief of intraocular pressure

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22
Q

Pilocarpine

A

Cholinergic agonist

I_ndicated for open-angle and closed-angle glaucoma (↑ aqueous humor outflow via opening of trabecular meshwork)_; potent stimulator of sweat, tears, and saliva

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23
Q

Methacholine

A

Muscarinic receptor agonist → stimulates muscarinic receptors in the airway when inhaled causing bronchoconstriction

Used for asthma challenge tests

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24
Q

Neostigmine

A

Anticholinesterase with no CNS penetration

Indicated for postoperative and neurogenic ileus and urinary retention, myasthenia gravis, postoperative reversal of neuromuscular junction blockade

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25
Q

Physostigmine

A

Anticholinesterase with CNS penetration

Indicated for anticholinergic toxicity, glaucoma

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26
Q

Pyridostigmine

A

Anticholinesterase with no CNS penetration

Indicated for myasthenia gravis (long-acting)

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27
Q

Donepezil

A

Acetylcholinesterase inhibitor → ↑ acetylcholine

Indicated for Alzheimer disease

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28
Q

Rivastigmine

A

Acetylcholinesterase inhibitor → ↑ acetylcholine

Indicated for Alzheimer disease

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29
Q

Galantamine

A

Acetylcholinesterase inhibitor → ↑ acetylcholine

Indicated for Alzheimer disease

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30
Q

Edrophonium

A

Anticholinesterase

Historically used to diagnose myasthenia gravis because it is extremely short-acting

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31
Q

Anticholinesterase inhibitor poisoning

A

Commonly caused due to exposure to organophosphates like parathione

Causes diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimation, sweating, and salivation

Treat with atropine (antimuscarinic) and pralidoxime (regenerates acetylecholinesterase)

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32
Q

Atropine

A

Muscarinic antagonist that works on the eye to produce mydriasis/dilation via paralysis of ciliary muscles and to treat bradycardia

Also used to treat organophosphate (cholinesterase inhibitor) poisoning

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33
Q

Homatropine

A

Muscarinic antagonist that works on the eye to produce mydriasis/dilation via paralysis of ciliary muscles

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34
Q

Tropicamide

A

Muscarinic antagonist that works on the eye to produce mydriasis/dilation via paralysis of ciliary muscles

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35
Q

Benztropine

A

Muscarinic antagonist that works in the CNS to treat Parkinson disease

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36
Q

Scopolamine

A

Muscarinic antagonist that works in the CNS to treat motion sickness

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37
Q

Ipratropium

A

Muscarinic antagonist → prevents bronchoconstriction

Indicated for COPD or asthma

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38
Q

Tiotropium

A

Muscarinic antagonist → prevents bronchoconstriction

Indicated for COPD or asthma

Longer-acting than ipratropium

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39
Q

Oxybutynin

A

Muscarinic antagonist that works in the genitourinary system to reduce urgency in mild cystitis and reduce bladder spasms

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40
Q

Darifenacin

A

Muscarinic antagonist that works in the genitourinary system to reduce urgency in mild cystitis and reduce bladder spasms

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41
Q

Solifenacin

A

Muscarinic antagonist that works in the genitourinary system to reduce urgency in mild cystitis and reduce bladder spasms

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42
Q

Tolterodine

A

Muscarinic antagonist that works in the genitourinary system to reduce urgency in mild cystitis and reduce bladder spasms

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43
Q

Fesoterodine

A

Muscarinic antagonist that works in the genitourinary system to reduce urgency in mild cystitis and reduce bladder spasms

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44
Q

Trospium

A

Muscarinic antagonist that works in the genitourinary system to reduce urgency in mild cystitis and reduce bladder spasms

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45
Q

Glycopyrrolate

A

Muscarinic antagonist used in the GI and respiratory systems to reduce airway secretions preoperatively and prevent drooling or peptic ulcers

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46
Q

Anticholinergic toxicity

A

Hot as a hare, dry as a bone, red as a beet, blind as a bad, mad as a hatter

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47
Q

Epinephrine

A

Sympathomimetic (β > α) used to treat anaphylaxis, open angle glaucoma (vasoconstriction → ↓ aqueous humor synthesis), asthma, hypotension

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48
Q

Norepinephrine

A

Sympathomimetic (α1 > α2 > β1)

Indicated for hypotension

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49
Q

Isoproterenol

A

Sympathomimetic (β1 = β2) used in the electophysiologic evaluation of tachyarrythmias

Indicated for tocolysis (relaxation of uterus) via β2 stimulation

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50
Q

Dopamine

A

Sympathomimetic (D1 = D2 > β > α) used to treat unstable bradycardia, heart failure, shock

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51
Q

Dobutamine

A

Sympathomimetic (β1 >> β2, α)

Indicated for refractory systolic heart failure, cardiogenic shock, and cardiac stress testing

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52
Q

Phenylephrine

A

Sympathomimetic (α1 > α2)

Indicated for hypotension, ocular procedures, rhinitis, and nasal decongestion and opening eustachian tubes as it reduces hyperemia and edema

SA: HTN, CNS stimulation/anxiety

Can also be used illicitly to make methamphetamine

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53
Q

Albuterol

A

Sympathomimetic (β2 > β1)

Indicated for acute asthma (short-acting) → relaxes bronchial smooth muscles

SA: tremor, arrythmia

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54
Q

Salmeterol

A

Sympathomimetic (β2 > β1)

Indicated for asthma and COPD (long-acting) prophylaxis

SA: tremor, arrythmia

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55
Q

Terbutaline

A

Sympathomimetic (β2 > β1) used to reduce premature uterine contractions

Indicated for tocolysis (relaxation of uterus) via β2 stimulation

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56
Q

Drugs that have antimuscarinic effects?

A

Atropine, TCAs (e.g. amitriptyline), H1 receptor antagonists (e.g. diphenhydramine), neuroleptics, antiparkinsonian drugs

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57
Q

Describe the pharmokinetic effects of competitive vs. non-competitive inhibitors.

A

Competitive, reversible inhibitors increase Km and decrease potency (increase ED50).

Competitive, irreversible inhibitors and non-competitive inhibitors decrease Vmax and decrease efficacy.

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58
Q

How do you calculate volume of distribution?

A

Vd = amount of drug in the body/plasma drug concentration

High Vd indicates a small molecular weight drug or a highly lipophilic drug that can easily distribute to tissues other than the plasma

A low Vd indicates a large molecular weight drug, a highy hydrophilic drug (highly positively charged), or a drug that is highly protein-bound which is likely to stay in the plasma

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59
Q

How do you calculate half-life?

A

For drugs that follow first-order kinetics:

t1/2 = (0.693 x Vd)/CL

It takes 4-5 half-lives to each steady state (3.3 half-lives to reach 90% steady state)

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60
Q

What is the difference between zero-order and first-order elimination?

A

Zero-order elimination = constant amount of drug eliminated per unit time (Cp decreases linearly with time)

First-order elimination = constant fraction of drug eliminated per unit time (Cp decreases exponentially with time)

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61
Q

How are weak acids and bases eliminated?

A

Ionized apecies are trapped in urine and cleared quickly; neutral forms can be reabsorbed.

Eliminating weak acids → alkalinize with bicarbonate

Eliminating weak bases → acidify with ammonium chloride

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62
Q

Which drugs should you use with caution in the elderly population?

A

Anticholinergics (e.g. first-generation antihistamines), alpha blockers, TCAs, benzodiazepines, antipsychotics, most antiarrhythmics, skeletal muscle relaxants

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63
Q

What medications are appropriate to treat high blood pressure during pregnancy?

A

α-methydopa

Labetaolol

Hydralazine

Nifedipine

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64
Q

Bromocriptine

A

Dopamine agonist

Indicated for prolactinoma, Parkinsons

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65
Q

Desmopressin (DDAVP)

A

ADH analog

Used to treat central diabetes insipidus and von Willibrand factor deficiency

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66
Q

Propylthiouracil (PTU)

A

Inhibits thyroid peroxidase and 5’-doiodinase → decreases T4/T3 production in the thyroid and decreases convertion of T4 to T3 in peripheral tissue

Used to treat hyperthyroidism, esp. in pregnancy

SA: agranulocytosis

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67
Q

Methimazole

A

Inhibits thyroid peroxidase → decreases T4/T3 production in the thyroid

Used to treat hyperthyroidism

SA: agranulocytosis

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68
Q

Cabergoline

A

Dopamine agonist

Indicated for prolactinoma

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69
Q

Octreotide

A

Somatostatin analog

Used to treat excess GH (gigantism, acromegaly), carcinoid tumors, gastrinoma, glucagonoma, VIPomas, acute esophageal variceal bleeding

SA: nausea, cramps, steatorrhea

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70
Q

Lanreotide

A

Somatostatin analog

Used to treat excess GH (gigantism, acromegaly), carcinoid, gastrinoma, glucagonoma, esophagesl varices

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71
Q

Pegvisomant

A

Growth hormone receptor antagonist

Used to treat excess GH (gigantism, acromegaly)

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72
Q

Oxytocin

A

Used to stimulate uterine contractions (starts labor, controls uterine hemorrhage), milk let-down

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73
Q

Demeclocycline

A

ADH antagonist (member of the tetracycline family)

Used to treat SIADH

SA: nephrogenic DI, photosensitivity, abnormalities of the bone and teeth

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74
Q

Adenosine

A

Binds α1 receptors on cardiomyocytes → activates potassium channels and inhibits L-type calcium channels → prolonged depolarization time (phase 4) → ↓ HR, slows AV node conduction

Indicated for termination of SVT (first line)

SA: flushing, hypotension, chest pain, effects blocked by theophylline and caffeine

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75
Q

Verapamil

A

Non-dihydropyridine calcium channel blocker/class IV antiarrhythmics → blocks L-type calcium channels → ↓ contractility, ↑ vasodilation, ↓ conduction velocity

Indicated for HTN, angina, afib/aflutter, prevention of nodal arrhythmias (e.g. SVT)

SA: cardiac depression, AV block, peripheral edema, flushing, dizziness, hyperprolactinemia, constipation

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76
Q

How do calcium channel blockers work?

A

Non-dihydropyridine calcium channel blocker → blocks L-type calcium channels → prevents calcium influx into cardiomyocytes and vascular smooth muscle → vasodilation, slows phase 4 diastolic depolarization and conduction velocity in the SA and AV nodes, ↓ contractility

Dihydropyridines work more on vascular tissue and non-dihydropyridines work more on cardiac tissue

Does not work on skeletal muscle because mechanical coupling of L-type calcium channels and RyR1 channels on the SR allows release of intracellular calcium without significant calcium influx across the plasma membrane

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77
Q

Diltiazem

A

Non-dihydropyridine calcium channel blocker/class IV antiarrhythmics → blocks L-type calcium channels → ↓ contractility, ↑ vasodilation, ↓ conduction velocity

Indicated for HTN, angina, afib/aflutter, prevention of nodal arrhythmias (e.g. SVT)

SA: cardiac depression, AV block, peripheral edema, flushing, dizziness, hyperprolactinemia, constipation

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78
Q

Amlodipine

A

Dihydropyridine calcium channel blocker → blocks L-type calcium channels → ↓ contractility, ↑ vasodilation

Indicated for HTN, angina (including Prinzmetal), Raynaud phenomenon

SA: cardiac depression, AV block, peripheral edema, flushing, dizziness, hyperprolactinemia, constipation

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79
Q

Nimodipine

A

Dihydropyridine calcium channel blocker → blocks L-type calcium channels → ↓ contractility, ↑ vasodilation

Indicated for subarachnoid hemorrhage (prevents cerebral vasospasm)

SA: cardiac depression, AV block, peripheral edema, flushing, dizziness, hyperprolactinemia, constipation

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80
Q

Nifedipine

A

Dihydropyridine calcium channel blocker → blocks L-type calcium channels → ↓ contractility, ↑ vasodilation

Indicated for HTN, angina (including Prinzmetal), Raynaud phenomenon

SA: cardiac depression, AV block, peripheral edema, flushing, dizziness, hyperprolactinemia, constipation

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81
Q

Hydralazine

A

↑ cGMP → smooth muscle relaxation

Vasodilates arterioles > veins (↓ preload, ↓ afterload)

Indicated for severe HTN, esp. in pregnany, CHF

SA: compensatory tachycardia (can co-administer β-blocker), fluid retention, nausea, headache, angina, lupus-like syndrome

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82
Q

Nitroprusside

A

Stimulates release of NO → ↑ cGMP → vasodilation

Indicated for hypertensive emergency

SA: cyanide toxicity

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83
Q

Fenoldopam

A

Dopamine D1 receptor agonist → coronary, peripheral, renal, splanchnic vasodilation

Indicated for hypertensive emergency, esp. in patients with AKI

84
Q

Nitroglycerin

A

↑ NO in smooth muscles → ↑ cGMP → vasodilation

Dilates veins >> arteries (↓ preload)

Indicated for angina, ACS, pulmonary edema

SA: reflex tachycardia (can co-administer β-blocker), hypotension, flushing, headache, “Monday disease” (increase in side effect on Mondays after developing tolerance over the work week)

85
Q

Isosorbide dinitrate

A

↑ NO in smooth muscles → ↑ cGMP → vasodilation

Dilates veins >> arteries (↓ preload)

Indicated for angina, ACS, pulmonary edema

SA: reflex tachycardia (can co-administer β-blocker), hypotension, flushing, headache, “Monday disease” (increase in side effect on Mondays after developing tolerance over the work week)

86
Q

-statins

A

HMG-CoA reductase inhibitors prevents conversion of HMG-CoA to mevalonate, a cholesterol precursor → upregulates LDL receptors in the liver

↓↓↓ LDL

↑ HDL

↓ Triglycerides

SA: hepatotoxicity, myalgias → rhabdomyolysis (esp. when used with fibrates and niacin)

87
Q

Niacin (Vitamin B3)

A

Inhibits lipolysis in adipose tissue, reduces hepatic VLDL synthesis

↓↓ LDL

↑↑ HDL

↓ Triglycerides

SA: facial flushing mediated by prostaglandins (reduced with long-term use or aspirin), hyperglycemia, hyperuricemia (don’t use with gout)

88
Q

Cholestyramine

A

Bile acid resin prevents intestinal absorption of bile acids so liver must use cholesterol to make more

↓↓ LDL

Slight ↑ HDL

Slight ↑ Triglycerides

SA: bad taste, GI discomfort, ↓ absorption of fat-soluble vitamins, cholesterol gallstones

89
Q

Colestipol

A

Bile acid resin prevents intestinal absorption of bile acids so liver must use cholesterol to make more

↓↓ LDL

Slight ↑ HDL

Slight ↑ Triglycerides

SA: bad taste, GI discomfort, ↓ absorption of fat-soluble vitamins, cholesterol gallstones

90
Q

Colesevelam

A

Bile acid resin prevents intestinal absorption of bile acids so liver must use cholesterol to make more

↓↓ LDL

Slight ↑ HDL

Slight ↑ Triglycerides

SA: bad taste, GI discomfort, ↓ absorption of fat-soluble vitamins, cholesterol gallstones

91
Q

Gemfibrozil

A

Fibrate that upregulates lipoprotein lipase → triglyceride clearance, activates PPAR-α in induce HDL synthesis

↓ LDL

↑ HDL

↓↓↓ Triglycerides

SA: myositis, hepatotoxicity, cholesterol gallstones (use with caution because fibrates inhibit 7α-hydroxylase, the rate-limiting step in bile acid synthesis)

92
Q

Clofibrate

A

Fibrate that upregulates lipoprotein lipase → triglyceride clearance, activates PPAR-α in induce HDL synthesis

↓ LDL

↑ HDL

↓↓↓ Triglycerides

SA: myositis, hepatotoxicity, cholesterol gallstones (use with caution because fibrates inhibit 7α-hydroxylase, the rate-limiting step in bile acid synthesis)

93
Q

Bezafibrate

A

Fibrate that upregulates lipoprotein lipase → triglyceride clearance, activates PPAR-α in induce HDL synthesis

↓ LDL

↑ HDL

↓↓↓ Triglycerides

SA: myositis, hepatotoxicity, cholesterol gallstones (use with caution because fibrates inhibit 7α-hydroxylase, the rate-limiting step in bile acid synthesis)

94
Q

Fenofibrate

A

Fibrate that upregulates lipoprotein lipase → triglyceride clearance, activates PPAR-α to induce HDL synthesis

↓ LDL

↑ HDL

↓↓↓ Triglycerides

SA: myositis, hepatotoxicity, cholesterol gallstones (use with caution because fibrates inhibit 7α-hydroxylase, the rate-limiting step in bile acid synthesis)

95
Q

Ezetimibe

A

Prevents cholesterol absorption at the small intestine brush border

↓↓ LDL

SA: ↑ LFTs, diarrhea

96
Q

Which lipid-lowering agents has the greatest effect on increasing HDL?

A

Niacin (vitmain B3) > HMG-CoA reductase inhibitors = fibrates > bile acid resins

97
Q

Which lipid-lowering agents has the greatest effect on lowering LDL?

A

HMG-CoA reductase inhibitors > niacin/vitamin B3 = bile acid resins = cholesterol absoption blockers > fibrates

98
Q

Which lipid-lowering agents has the greatest effect on decreasing triglyceride?

A

Fibrates > HMG-CoA reductase inhibitors = niacin/vitamin B3

Bile acid resins acutally slightly increase triglycerides

99
Q

Quinidine

A

Class IA antiarrhythmic

Sodium channel blocker → ↓ slope of phase 0 depolarization → slows conduction → increased action potential duration

Indicated for atrial and ventricular arrhythmias, esp. re-entrant and ectopic SVT and VT

SA: cinchonism (headache, tinnitus), thrombocytopenia, ↑ QT interval → torsades de pointes

100
Q

Procainamide

A

Class IA antiarrhythmic

Sodium channel blocker → ↓ slope of phase 0 depolarization → slows conduction → increased action potential duration

Indicated for atrial and ventricular arrhythmias, esp. re-entrant and ectopic SVT and VT

SA: SLE-like syndrome, thrombocytopenia, ↑ QT interval → torsades de pointes

101
Q

Disopyramide

A

Class IA antiarrhythmic

Sodium channel blocker → ↓ slope of phase 0 depolarization → slows conduction → increased action potential duration

Indicated for atrial and ventricular arrhythmias, esp. re-entrant and ectopic SVT and VT

SA: heart failure, thrombocytopenia, ↑ QT interval → torsades de pointes

102
Q

Lidocaine

A

Class IB antiarrhythmic

Sodium channel blocker → ↓ slope of phase 0 depolarization + reduced action potential duration

Indicated for acute ventricular arrhythmias (esp. post-MI), digitalis-induced arrhythmias

SA: CNS stimulation/depression, cardiovascular depression

103
Q

Mexiletine

A

Class IB antiarrhythmic

Sodium channel blocker → ↓ slope of phase 0 depolarization + reduced action potential duration

Indicated for acute ventricular arrhythmias (esp. post-MI), digitalis-induced arrhythmias

SA: CNS stimulation/depression, cardiovascular depression

104
Q

Flecainide

A

Class IC antiarrhythmic

Sodium channel blocker → greatly ↓ slope of phase 0 depolarization → prolongs refractory period in AV node (action potential duration unchanged)

Indicated for SVTs, including afib

SA: proarrhythmic, especially post-MI (contraindicated in structural and ischemic heart disease)

105
Q

Propafenone

A

Class IC antiarrhythmic

Sodium channel blocker → greatly ↓ slope of phase 0 depolarization → prolongs refractory period in AV node (action potential duration unchanged)

Indicated for SVTs, including afib

SA: proarrhythmic, especially post-MI (contraindicated in structural and ischemic heart disease)

106
Q

β-blockers (-lol)

A

Class II antiarrhytmic

β-blockers ↓ cAMP → ↓ calcium currents → ↓ slope of phase 4 in AV > SA nodes → ↑ PR interval

Indicated for SVT, slowing ventricular rate during afib and aflutter

SA: impotence, exacerbation of COPD and asthma, bradycardia, AV block, sedation, sleep alterations (treat overdose with glucagon)

Contraindicated in cocaine users 2/2 risk of unopposed α-adrenergic activity)

Esmolol is short acting

Metoprolol can cause dyslipidemia

Propranolol can exacerbate Prinzmetal angina

107
Q

Amiodarone

A

Class III antiarrhythmic

Potassium channel blocker → markedly prolonged repolarization → ↑ action potential duration → ↑ QT interval

Indicated for afib, aflutter, ventricular tachycardia

SA: pulmonary fibrosis, hepatotoxicity, thyroid dysfunction (contains iodine), corneal and skin deposits resulting in photodermatitis, neurologic effects, constipation, bradycardia, heart block, CHF

Check PFTs, LFTs, and TFTs before using!!!

108
Q

Ibutilide

A

Class III antiarrhythmic

Potassium channel blocker → markedly prolonged repolarization → ↑ action potential duration → ↑ QT interval

Indicated for afib, aflutter

SA: prolonged QT interval → torsades de pointes

109
Q

Dofetilide

A

Class III antiarrhythmic

Potassium channel blocker → markedly prolonged repolarization → ↑ action potential duration → ↑ QT interval

Indicated for afib, aflutter

110
Q

Sotalol

A

Class III antiarrhythmic

Potassium channel blocker → markedly prolonged repolarization → ↑ action potential duration → ↑ QT interval

Indicated for afib, aflutter, ventricular tachycardia

SA: prolonged QT interval → torsades de pointes, excessive beta-blockade

111
Q

Digoxin

A

Inhibits Na+/K+ ATPase which indirectly inhibits Na+/Ca2+ exchanger → ↑ intracellular Ca2+ → + inotropy

Stimulates vagus nerve → ↓ HR

Indicated for CHF, afib

SA: cholinergic toxicity, arrhythmias, AV block, hyperkalemia, nausea, vomiting, color vision alterations

112
Q

Clopidogrel

A

Irreversible inhibitor of P2Y12 (component of ADP receptors) on platelets preventing aggregation

113
Q

Fish oil/Omega-3 fatty acids

A

Decrease VLDL and apolipoprotein B synthesis

↑ HDL

↓ Triglycerides

SA: fishy taste

114
Q

What drugs can cause a prolonged QT interval)

A

Class IA antiarrhythmics (e.g. quinidine)

Class III antiarrhythhmics (sotalol)

Antipsychotics (e.g. risperidone)

Atibiotics (e.g.macrolides)

Chloroquine

Protease inhibitors

Thiazides

115
Q

Milrinone

A

Phosphodiesterase 3 inhibitor → ↑ cAMP → ↑ contractility, arterial and venous vasodilation

Indicated for treatment of CHF

SA: hypotension

116
Q

Inamirinone

A

Phosphodiesterase 3 inhibitor → ↑ cAMP → ↑ contractility, arterial and venous vasodilation

Indicated for treatment of CHF

SA: hypotension

117
Q

Which drugs improve survival for CHF?

A

ACEI/ARBs

Aldosterone antagonists

Beta-blockers

118
Q

Cilostazol

A

Phosphodiesterase inhibitor → ↑ cAMP → ↓ platelet activation + vasodilation

Indicated for peripheral artery disease

119
Q

Abciximab

A

Monoclonal antibody targets platelet IIb/IIIa receptors to inhibit platelet aggregation

120
Q

Argatroan

A

Direct thrombin inhibitor

Indicated to treat heparin-induced thrombocytopenia

121
Q

Heparin

A

Potentiates antithrombin III → inactivation of thrombin → anticoagulation

Safe for pregnancy; high water solubility → won’t cross placenta

122
Q

Warfarin

A

Competitive inhibitor of vitamin K epoxide reductase → reduces factors II, VII, IX, X, protein C, protein S → anticoagulation (temporary heparin bridge to prevent hypercoagulation 2/2 shorter half-lives of proteins C and S)

Must monitor PT/INR

Contraindicated during pregnancy; high lipid solubility → will cross placenta

123
Q

Enoxaparin

A

Low molecular weight heparin

Good for anticoagulation during pregnancy (doesn’t cross the placenta, short half-life)

124
Q

Dabigatran

A

Direct thrombin inhibitor

125
Q

Apixaban

A

Factor Xa inhibitor

126
Q

How do β1 agonists work?

A

β1 agonist → GPCR (Gs) → ↑ cAMP → protein kinase A → ↑ intracellular calcium + inhibition of myosin light-chain kinase

↑ HR

↑ contractility

↑ renin release

↑ lipolysis

127
Q

How do β2 agonists work?

A

β1 agonist → GPCR (Gs) → ↑ cAMP → protein kinase A → ↑ intracellular calcium + inhibition of myosin light-chain kinase

Vasodilation (↓ TPR)

Bronchodilation

↑ HR

↑ contractility

↑ lipolysis

↑ insulin release

↑ glycogenolysis

↑ gluconeogenesis

128
Q

How do α1 agonists work?

A

α1 agonist → GPCR (Gq) → Phospholipase C → ↑ IP3 → ↑ intracellular calcium

Vascular smooth muscle contraction

129
Q

How do α2 agonists work?

A

α2 agonist → GPCR (Gi) → ↓ cAMP → ↓ protein kinase A → ↓ intracellular calcium:

↓ sympathetic outflow

↓ insulin release

↓ lipolysis

↑ platelet aggregation

130
Q

Cimetidine

A

Reversible block of H2 receptors → ↓ H+ secretion by parietal cells

Indicated for peptic ulders, gastritis, mild GERD

SA: drug interactions (inhibitor of P-450), antiandrogen effects (prolactin release, gynecomastia, impotence, decreased libido in males), confusion, dizziness, headaches, decreased renal excretion of creatinine

131
Q

Ranitidine

A

Reversible block of H2 receptors → ↓ H+ secretion by parietal cells

Indicated for peptic ulders, gastritis, mild GERD

SA: decreased renal excretion of creatinine

132
Q

Famotidine

A

Reversible block of H2 receptors → ↓ H+ secretion by parietal cells

Indicated for peptic ulders, gastritis, mild GERD

SA: decreased renal excretion of creatinine

133
Q

Nizatidine

A

Reversible block of H2 receptors → ↓ H+ secretion by parietal cells

Indicated for peptic ulders, gastritis, mild GERD

SA: decreased renal excretion of creatinine

134
Q

Omeprazole and other -prazoles

A

Proton pump inhibitor

Irreversibly inhibits H+/K+ ATPase in stomach parietal cells

Indicated for peptic ulcers, gastritis, GERD, Zollinger-Ellison syndrome

SA: increased risk of C. difficile infection, pneumonia, long-term use increases risk of hip fractures and hypomagnesemia

Also includes lansoprazole, esomeprazole, pantoprazole, dexlansoprazole

135
Q

Bismuth, sucralfate

A

Binds to base of ulcer providing physical rotection and allowing HCO3- secretion to reestablish pH gradient in the mucous layer

Indicated for ulcer healing, travelers’ diarrhea

136
Q

Misoprostol

A

PGE1 analog → increases production and secretion of gastric mucous barrier, ↓ acid production

Indicated for NSAID-induced peptic ulcers, maintenance of PDA, ripens cervix

SA: diarrhea

Contraindicated in women of childbearing potential (abortifacient)

137
Q

Aluminum hydroxide

A

Antacid that affects absorption, bioavailability, or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying

SA: hypokalemia

Overuse: constipation, hypophophatemia, proximal muscle weakness, osteodystrophy, seizures

138
Q

Calcium carbonate

A

Antacid that affects absorption, bioavailability, or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying

SA: hypokalemia, can chelate and decrease the effectiveness of other drugs

Overuse: hypercalcemia, rebound acid increase

139
Q

Magnesium hydroxide

A

Antacid that affects absorption, bioavailability, or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying

SA: hypokalemia

Overuse: osmotic diarrhea, hyporeflexia, hypotension, cardiac arrest

140
Q

Infliximab

A

Monoclonal antibody to TNF-α

Indicated for Crohn disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, psoriasis

SA: infection, fever, hypotension

141
Q

Sulfasalazine

A

Colonic bacteria activate sulfapyridine (antibacterial) and 5-aminosalicyclic acid (anti-inflammatory)

Indicated for ulcerative colitis, Chron disease

SA: malaise, nausea, sulfonamide toxicity, reversible oligospermia

142
Q

Ondansetron

A

5-HT3 antagonist → ↓ vagal stimulation → central-acting anti-emetic

Indicated for postoperative and post chemotherapy nausea and vomiting

SA: headache, constipation

143
Q

Metclopramide

A

D2 receptor antagonist → increased resting tone, contractility, LES tone, motility

Indicated for diabetic and post-surgery gastropresis, anti-emetic

SA: Parkinsonian effects (contraindicated in Parkinsons)

144
Q

Rifaximin

A

Binds to DNA-dependent RNA polymerase and inhibits bacterial RNA synthesis

Decreased bacterial flora decreases intetinal production and absorption of ammonia (NH3)

Indicated for hepatic encephalopathy and traveler’s diarrhea

145
Q

Lactulose

A

Catabolized by intetinal bacterial flora to short chain fatty acids, lowering the colonic pH and increasing cconversion of ammonia (NH3) to ammonium (NH4+)

Indicated for hepatic encephalopathy

146
Q

Anti-emetics

A

GI irritation → 5-HT3 antagonists (e.g. odansetron)

Central/Migraines → D2 antagonists (e.g. metoclopramide, prochlorperazine)

Vestibular nausea → H1 antagonists (e.g. diphenhydramine, meclizine) and M1 antagonists (e.g. scopolamine)

147
Q

Hydroxyzine

A

First generation H1 antagonist

Indicated for allergies, motion sickness, sleep aid

SA: sedation, anticholinergic/muscarinic (blurry vision, urine retention, delirium), anti-alpha-adrenergic (orthostatis hypotension), serotonergic (appetite stimulation, weight gain)

148
Q

Diphenhydramine

A

First generation H1 antagonist

Indicated for allergies, motion sickness, sleep aid

SA: sedation, anticholinergic/muscarinic (blurry vision, urine retention, delirium), anti-alpha-adrenergic (orthostatis hypotension), serotonergic (appetite stimulation, weight gain)

149
Q

Promethazine

A

First generation H1 antagonist

Indicated for allergies, motion sickness, sleep aid

SA: sedation, anticholinergic/muscarinic (blurry vision, urine retention, delirium), anti-alpha-adrenergic (orthostatis hypotension), serotonergic (appetite stimulation, weight gain)

150
Q

Chlorpheniramine

A

First generation H1 antagonist

Indicated for allergies, motion sickness, sleep aid

SA: sedation, anticholinergic/muscarinic (blurry vision, urine retention, delirium), anti-alpha-adrenergic (orthostatis hypotension), serotonergic (appetite stimulation, weight gain)

151
Q

Loratadine

A

Second generation H1 antagonist

Indicated for allergies

Fewer side effects than first generation (less lipopholic → less likely to cross BBB and cause sedation)

152
Q

Cetirizine

A

Second generation H1 antagonist

Indicated for allergies

Fewer side effects than first generation (less lipopholic → less likely to cross BBB and cause sedation)

153
Q

Finasteride

A

5α-reductase inhibitors prevents convertion of testosterone to DHT

Indicated for BPH (second line as it takes 6-12 months to see an effect) and androgenetic alopecia (male-pattern hair loss)

154
Q

Succinylcholine

A

Depolarizing NMJ blocker (2 phases)

Binds to nicotinic acetylcholine receptor → continuous depolarization of the neuromuscular endplate (can’t be broken down by acetylcholinesterase) causes inactivation of sodium channels → flaccid paralysis

Indicated for rapid-sequence intubation

SA: malignant hyperthermia (esp. with halothanes), severe hyperkalemia in patients with burns, myopathies, crush injuries, and denervation, bradycardia or tachycardia

155
Q

Dimenhydrinate

A

First generation H1 antagonist

Indicated for allergies, motion sickness, sleep aid

SA: sedation, anticholinergic/muscarinic (blurry vision, urine retention, delirium), anti-alpha-adrenergic (orthostatis hypotension), serotonergic (appetite stimulation, weight gain)

156
Q

Fexofenadine

A

Second generation H1 antagonist

Indicated for allergies

Fewer side effects than first generation (less lipopholic → less likely to cross BBB and cause sedation)

157
Q

Desloratidine

A

Second generation H1 antagonist

Indicated for allergies

Fewer side effects than first generation (less lipopholic → less likely to cross BBB and cause sedation)

158
Q

Guaifenesin

A

Expectorant

Thins respiratory secretions but does not suppress cough

159
Q

Dextromethorphan

A

NMD glutamate receptor antagonist → antitussive

Synthetic codeine analog that has mild opioid effect when used in excess → can give naloxone for overdose

160
Q

N-acetylcystine

A

Mucolytic

Indicated for thinning mucous plugs in CF patients and as antidote for acetaminophen overdose

161
Q

Pseudoephedrine

A

Sympathomimetic α-agonist

OTC indicated for nasal decongestion and opening eustachian tubes as it reduces hyperemia and edema

SA: HTN, CNS stimulation/anxiety

Can also be used illicitly to make methamphetamine

162
Q

Formoterol

A

Sympathomimetic (β2 > β1)

Indicated for asthma and COPD (long-acting) prophylaxis

SA: tremor, arrythmia

163
Q

Theophylline

A

Methylxanthine → inhibits phosphodiesterase → ↑ cAMP → bronchial smooth muscle relaxation

SA: cardiotoxicity, neurotoxicity, blocks actions of adenosine (limited use due to narrow therapeutic index)

164
Q

Beclomethasone

A

Inhibits synthesis of many cytokines, including inactivation of NF-κB (transcription factor) → ↓ TNF-α

Indicated for chronic asthma (first line)

165
Q

Fluticasone

A

Inhibits synthesis of many cytokines, including inactivation of NF-κB (transcription factor) → ↓ TNF-α

Indicated for chronic asthma (first line)

166
Q

Montelukast

A

Leukotriene receptor blocker

Indicated for asthma, especially aspirin-induced

167
Q

Zafirlukast

A

Leukotriene receptor blocker

Indicated for asthma, especially aspirin-induced

168
Q

Zileuton

A

5-lipooxygenase inhibitor blocks converstion of arachidonic acid to leukotrienes

Indicated for asthma

169
Q

Omalizumab

A

Monoclonal anti-IgE antibody → binds to unbound serum IgE and prevents binding to FcεRI

Indicated for allergic asthma resistant to inhaled steroids and long-acting β2-agonists

170
Q

Bosentan

A

Antagonizes endothelin-1 receptors to ↓ pulmonary vascular resistance

Indicated for pulmonary arterial hypertension

171
Q

Vecuronium

A

Nondepolarizing NMJ blocker

Competitive inhibitor of postsynaptic acetycholine receptors at the NMJ

Can be reversed with neostigmine

172
Q

Pancuronium

A

Nondepolarizing NMJ blocker

Competitive inhibitor of postsynaptic acetycholine receptors at the NMJ

Can be reversed with neostigmine

173
Q

Turbocurarine

A

Nondepolarizing NMJ blocker

Competitive inhibitor of postsynaptic acetycholine receptors at the NMJ

Can be reversed with neostigmine

174
Q

Varenicline

A

Partial agonist of nicotinic acetylcholine receptors in the CNS → reduces dopamine release → reduces reward pathway of nicotine

Indicated to reduce cravings and attenuate rewarding effects of nicotine to promote cessation

175
Q

Cromolyn

Nedocromil

A

Inhibits mast cell degranulation

Indicated for prophylaxis for seasonal symptoms, aspirin hypersensitivity, and exercise-induced asthma

176
Q

Latanoprost

A

PGF2α agonist → ↑ outflow of aqueous humor

Indicated for glaucoma

SA: darkens color of iris

177
Q

Opioid analgesics (morphine, fentanyl, codeine, loperamide, methadone, meperidine, dextrmoethorphan, diphenoxylate)

A

Opioid receptor agonist

Binds to post-synaptic receptor → opens K+ channels allowing K+ efflux → hyperpolarizes membrane

Binds to pre-synaptic receptor → closes Ca2+ channels preventing Ca2+ influx → ↓ release of neurotransmitters

Indicated for pain suppression, cough, diarrhea, pulmonary edema

SA: addiction, respiratory depression, constipation, miosis

Toxicity treated with naloxone or naltrexone (opioid receptor antagonist)

178
Q

Butorphanol

A

Mu-opioid receptor partial agonist and kappa-opioid receptor agonist

Indicated for severe pain, less respiratory depression that full opioid agonist

Overdose not easily reversed with naloxone

179
Q

Tramadol

A

Very weak opioid agonist

Indicated for chronic pain

SA: similar to other opioids + decreased seizure threshold, serotonin syndrome

180
Q

Ethnosuximide

A

Blocks thalamic T-type Ca2+ channels

Indicated for absence seizures

181
Q

Phenytoin

A

Increased sodium channel inactivation

Indicated for tonic-clonic seizures (first line)

SA: gingival hyperplasia, hirsutism, megaloblastic anemia, SLE-like syndrome

182
Q

Carbamazepine

A

Increased sodium channel inactivation

Indicated for simple partial, complex partial, and tonic-clonic seizures, trigeminal neuralgia (first line for all)

SA: bone marrow suppression, SIADH

183
Q

Valproic acid

A

Increased sodium channel inactivation, inhibits GABA transaminase → ↑ GABA concentration

Indicated for simple partial, complex partial, tonic-clonic, and absense seizures, bipolar disorder

Contraindicated in pregnancy (neural tube defects)

184
Q

Gabapentin

A

GABA analog → inhibits high-voltage-activated calcium channels

Indicated for partial simple, partial complex, and tonic-clonic seizures, peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis, bipolar disorder

185
Q

Barbiturates (phenobarbital, pentobarbital, thiopental, secobarbital)

A

↑ duration of chloride channel opening → ↑ GABAA action → ↓ neuron firing

SA: respiratory and cardiovascular depression, CNS depression (exacerbated by alcohol)

186
Q

Benzodiazepines

A

↑ frequency of chloride channel opening → ↑ GABAA action → ↓ neuron firing

SA: dependence, additive CNS depression effects with alcohol, less risk of respiratory depression and coma than with barbituates

Avoid taking with other CNS depressants (alcohol, barbituates, neuroleptics, 1st generation antihistamines)

Treat overdose with flumazenil (competitive antagonist at GABA benzodiazepine receptor)

187
Q

Relationship between solubility and induction time and potency for CNS anesthetics

A

↓ solubility in blood = ↓ blood/gas partition coefficient = rapid induction and recovery times (if a gas is not very soluble in the blood, the blood becomes saturated more quickly and the drug can enter the brain more quickly)

↑ tissue solubility = ↑ AV gradients = slow blood saturation = slow brain uptake = slow onset of action

↑ solubility in lipid = ↑ potency = 1/MAC

188
Q

Dantrolene

A

Prevents release of calcium from the sarcoplasmic reticulum of skeletal muscle

Indicated to treat malignant hyperthemia and neuroleptic malignant syndrome

189
Q

Levodopa/carbidopa

A

Levodopa is a dopamine precursor that can cross the BBB and is converted to dopamine by dopa decarboxylase in the CNS

Carbidoba inhibits peripheral dopa decarboxylase

Indicated for Parkinsons

SA: arrythmias (↑ peripheral formation of catecholamines), dyskinesia following administration and akinesia between doses, anxiety, agitation, insomnia, confusion, delusions, hallucinations

190
Q

First line treatment for essential tremor

A

Propranolol

Essential tremor is familial (autosomal dominant) and worsens while maintaining a particular postures and improves with alcohol consumption

191
Q

Where are α1 receptors located?

A

Vascular smooth muscle α1 stimulation = contraction/constriction

Bladder α1 stimulation = contraction of internal urethral sphincter

Eye α1 stimulation = mydriasis (dilation)

192
Q

Where are β2 receptors located?

A

Skeletal muscle vasculature β​2 stimulation = relaxation/vasodilation

Bronchi β​2 stimulation = bronchodilation

Uterus β​2 stimulation = relaxation (tocolysis)

193
Q

Pramipexole

A

Non-ergot dopamine agonist

Indicated for Parkinsons, restless leg syndrome

194
Q

Treatment for status epilepticus

A

Status epilepticus = single seizure lasting > 5 min or multiple discrete seizures with incomplete recovery of consciousness between episodes

IV benzodiazepine (↑ frequency of chloride channel opening) first

IV phenytoin (↓ sodium current in cortical neurons) concurrently to prevent recurrence

195
Q

Remelteon

A

Melatonin agonist

Indicated for insomnia, especially in older adults

Short-term use

196
Q

Sumatriptan

A

5-HTIB/ID agonist → inhibits trigeminal nerve activation →prevents vasoactive peptide release and induces vasocontriction

Indicated for acute migraine (abortive) and cluster headache attachs

SA: coronary vasospasm (contraindicated in CAD and Prinzmetal angina), increased blood pressure

197
Q

Cytochrome P-450 inducers

A

Carbamazepine

Barbiturates

Phenytoin

Rifampin

Griseofulvin

St John’s wort

Modafinil

Cyslophosphamide

OCPs

198
Q

Cytochrome P-450 inhibitors

A

Acetaminophen

NSAIDs

Amiodarone

Cimetidine

Fluoroquinolones

Clarithromycin

Azole antifunals

Grapefruit juice

Isoniazid

Ritonavir

Omeprazole

Thyroid hormone

SSRIs

199
Q

Effects of inhaled anesthetics

A

Myocardial depression

Respiratory depression

Nausea/emesis

Increased cerebral blood flow

Decreased cerebral metabolic demand

Decreased hepatic blood flow

Decrease GFR (increased renal vascular resistance and decrease renal plasma flow)

SA: hepatotoxicity, malignant hyperthermia

200
Q

Anticonvulsants indicated for absence seizures

A

Ethosuximide (first line)

Valproic acid (also indicated for partial smiple, partial complex, and tonic-clonic seizures)

Lamotrigine (also indicated for partial smiple, partial complex, and tonic-clonic seizures)

201
Q

Organophosphate poisoning

A

May organophosphates, often found in pesticides, are irreversible inhibitors of acetylcholinesterase in both nicotinic and muscarinic synapses

Characterized by diarrhea, diaphoresis, urination, miosis, bronchospasm, bradycardia, emesis, lacrimation, salivation

Tx: atropine (muscarinic antagonist) + pralidoxime (restores acetylcholinesterase)

Need both because atropine has no effect on nicotinic receptor overstimulation and patient is still at risk of muscle paralysis

202
Q

Buprenorphine

A

Partial opioid agonist

Can precipitate withdrawal in opioid-tolerant patients

203
Q

Baclofen

A

GABAB receptor agonist

Indicated for treatment of spasticity secondary to brain and spinal cord disease (e.g. MS)

204
Q

Non-benzodiazepine hypnotics (Z drugs)

Zolpidem

Zaleplon

Eszopiclone

A

Binds to BZ1 subtype of the GABAA receptor

Indicated for insomnia

Decreased risk of dependence compared to benzodiazepines

205
Q

Memantine

A

MDA receptor antagonist helps prevent excitotoxicity (mediated by Ca2+)

Indicated for Alzheimers

206
Q

Probenecid

A

Inhibits organic anion transporters in renal tubular cells to inhibit tubular secretion of certain antibiotics (e.g. penicillin)

Also inhibits the urate transporter which increases urinary excretion of uric acid (can be used to treat gout)

207
Q

Retinoids (tretinoin, adapalene, tazarotene, isotretinoin)

A

Vitamin A analogs that bind to intranuclear receptors RAR or RXR that act as transcription factors that decrease sebum production and normalize epidermal differentiation → increased cell turnover and shedding from stratum corneum reduces hyperkeratinization, opens blocked pores, and prevents formation of microcomedones

Indicated for severe, refractory, nodulocystic acne, psoriasis

USMLE Step 1 (20 decks)

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