Pharmacology Flashcards by Kristin Wertin

Q

Side effects of ACEI

A

ACEIs dilate afferent arteriole

Hyperkalemia, cough, angioedema (increased bradykinin)

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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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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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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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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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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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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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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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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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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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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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Q

-sartans

A

Angiotensin II receptor blockers (ARBs)

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

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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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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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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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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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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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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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Q

Metolazone

A

Thiazide-like diuretic

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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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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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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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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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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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Physostigmine

Anticholinesterase _with_ CNS penetration Indicated for anticholinergic toxicity, glaucoma

Pyridostigmine

Anticholinesterase with no CNS penetration Indicated for myasthenia gravis (long-acting)

Donepezil

Acetylcholinesterase inhibitor → ↑ acetylcholine Indicated for Alzheimer disease

Rivastigmine

Acetylcholinesterase inhibitor → ↑ acetylcholine Indicated for Alzheimer disease

Galantamine

Acetylcholinesterase inhibitor → ↑ acetylcholine Indicated for Alzheimer disease

Edrophonium

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

Anticholinesterase inhibitor poisoning

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)

Atropine

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

Homatropine

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

Tropicamide

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

Benztropine

Muscarinic antagonist that works in the CNS to treat Parkinson disease

Scopolamine

Muscarinic antagonist that works in the CNS to treat motion sickness

Ipratropium

Muscarinic antagonist → prevents bronchoconstriction Indicated for COPD or asthma

Tiotropium

Muscarinic antagonist → prevents bronchoconstriction Indicated for COPD or asthma Longer-acting than ipratropium

Oxybutynin

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

Darifenacin

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

Solifenacin

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

Tolterodine

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

Fesoterodine

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

Trospium

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

Glycopyrrolate

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

Anticholinergic toxicity

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

Epinephrine

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

Norepinephrine

Sympathomimetic (α1 \> α2 \> β1) Indicated for hypotension

Isoproterenol

Sympathomimetic (β1 = β2) used in the electophysiologic evaluation of tachyarrythmias Indicated for tocolysis (relaxation of uterus) via β2 stimulation

Dopamine

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

Dobutamine

Sympathomimetic (β1 \>\> β2, α) Indicated for refractory systolic heart failure, cardiogenic shock, and cardiac stress testing

Phenylephrine

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

Albuterol

Sympathomimetic (β2 \> β1) Indicated for acute asthma (short-acting) → relaxes bronchial smooth muscles SA: tremor, arrythmia

Salmeterol

Sympathomimetic (β2 \> β1) Indicated for asthma and COPD (long-acting) prophylaxis SA: tremor, arrythmia

Terbutaline

Sympathomimetic (β2 \> β1) used to reduce premature uterine contractions Indicated for tocolysis (relaxation of uterus) via β2 stimulation

Drugs that have antimuscarinic effects?

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

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

Competitive, reversible inhibitors increase K_m and decrease potency (increase ED₅₀). Competitive, irreversible inhibitors and non-competitive inhibitors decrease V_max and decrease efficacy.

How do you calculate volume of distribution?

V_d = amount of drug in the body/plasma drug concentration High V_d indicates a small molecular weight drug or a highly lipophilic drug that can easily distribute to tissues other than the plasma A low V_d 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

How do you calculate half-life?

For drugs that follow first-order kinetics: t_1/2 = (0.693 x V_d)/CL It takes 4-5 half-lives to each steady state (3.3 half-lives to reach 90% steady state)

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

Zero-order elimination = constant _amount_ of drug eliminated per unit time (C_p decreases linearly with time) First-order elimination = constant _fraction_ of drug eliminated per unit time (C_p decreases exponentially with time)

How are weak acids and bases eliminated?

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

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

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

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

α-methydopa Labetaolol Hydralazine Nifedipine

Bromocriptine

Dopamine agonist Indicated for prolactinoma, Parkinsons

Desmopressin (DDAVP)

ADH analog Used to treat central diabetes insipidus and von Willibrand factor deficiency

Propylthiouracil (PTU)

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

Methimazole

Inhibits thyroid peroxidase → decreases T4/T3 production in the thyroid Used to treat hyperthyroidism SA: agranulocytosis

Cabergoline

Dopamine agonist Indicated for prolactinoma

Octreotide

Somatostatin analog Used to treat excess GH (gigantism, acromegaly), carcinoid tumors, gastrinoma, glucagonoma, VIPomas, _acute esophageal variceal bleeding_ SA: nausea, cramps, steatorrhea

Lanreotide

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

Pegvisomant

Growth hormone receptor antagonist Used to treat excess GH (gigantism, acromegaly)

Oxytocin

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

Demeclocycline

ADH antagonist (member of the tetracycline family) Used to treat SIADH SA: nephrogenic DI, photosensitivity, abnormalities of the bone and teeth

Adenosine

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

Verapamil

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

How do calcium channel blockers work?

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

Diltiazem

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

Amlodipine

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

Nimodipine

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

Nifedipine

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

Hydralazine

↑ 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

Nitroprusside

Stimulates release of NO → ↑ cGMP → vasodilation Indicated for hypertensive emergency SA: cyanide toxicity

Fenoldopam

Dopamine D1 receptor agonist → coronary, peripheral, renal, splanchnic vasodilation Indicated for hypertensive emergency, esp. in patients with AKI

Nitroglycerin

↑ 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)

Isosorbide dinitrate

↑ 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)

-statins

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)

Niacin (Vitamin B3)

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)

Cholestyramine

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

Colestipol

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

Colesevelam

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

Gemfibrozil

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)

Clofibrate

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)

Bezafibrate

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)

Fenofibrate

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)

Ezetimibe

Prevents cholesterol absorption at the small intestine brush border ↓↓ LDL SA: ↑ LFTs, diarrhea

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

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

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

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

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

Fibrates \> HMG-CoA reductase inhibitors = niacin/vitamin B3 Bile acid resins acutally slightly increase triglycerides

Quinidine

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

Procainamide

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

Disopyramide

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

Lidocaine

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

Mexiletine

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

Flecainide

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)

Propafenone

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)

β-blockers (-lol)

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

Amiodarone

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!!!

Ibutilide

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

Dofetilide

Class III antiarrhythmic Potassium channel blocker → markedly prolonged repolarization → ↑ action potential duration → ↑ QT interval Indicated for afib, aflutter

Sotalol

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

Digoxin

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_

Clopidogrel

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

Fish oil/Omega-3 fatty acids

Decrease VLDL and apolipoprotein B synthesis ↑ HDL ↓ Triglycerides SA: fishy taste

What drugs can cause a prolonged QT interval)

Class IA antiarrhythmics (e.g. quinidine) Class III antiarrhythhmics (sotalol) Antipsychotics (e.g. risperidone) Atibiotics (e.g.macrolides) Chloroquine Protease inhibitors Thiazides

Milrinone

Phosphodiesterase 3 inhibitor → ↑ cAMP → ↑ contractility, arterial and venous vasodilation Indicated for treatment of CHF SA: hypotension

Inamirinone

Phosphodiesterase 3 inhibitor → ↑ cAMP → ↑ contractility, arterial and venous vasodilation Indicated for treatment of CHF SA: hypotension

Which drugs improve survival for CHF?

ACEI/ARBs Aldosterone antagonists Beta-blockers

Cilostazol

Phosphodiesterase inhibitor → ↑ cAMP → ↓ platelet activation + vasodilation Indicated for peripheral artery disease

Abciximab

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

Argatroan

Direct thrombin inhibitor Indicated to treat heparin-induced thrombocytopenia

Heparin

Potentiates antithrombin III → inactivation of thrombin → anticoagulation Safe for pregnancy; high water solubility → won't cross placenta

Warfarin

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

Enoxaparin

Low molecular weight heparin Good for anticoagulation during pregnancy (doesn't cross the placenta, short half-life)

Dabigatran

Direct thrombin inhibitor

Apixaban

Factor Xa inhibitor

How do β1 agonists work?

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

How do β2 agonists work?

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

How do α1 agonists work?

α1 agonist → GPCR (Gq) → Phospholipase C → ↑ IP3 → ↑ intracellular calcium Vascular smooth muscle contraction

How do α2 agonists work?

α2 agonist → GPCR (Gi) → ↓ cAMP → ↓ protein kinase A → ↓ intracellular calcium: ↓ sympathetic outflow ↓ insulin release ↓ lipolysis ↑ platelet aggregation

Cimetidine

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

Ranitidine

Reversible block of H2 receptors → ↓ H+ secretion by parietal cells Indicated for peptic ulders, gastritis, mild GERD SA: decreased renal excretion of creatinine

Famotidine

Reversible block of H2 receptors → ↓ H+ secretion by parietal cells Indicated for peptic ulders, gastritis, mild GERD SA: decreased renal excretion of creatinine

Nizatidine

Reversible block of H2 receptors → ↓ H+ secretion by parietal cells Indicated for peptic ulders, gastritis, mild GERD SA: decreased renal excretion of creatinine

Omeprazole and other -prazoles

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

Bismuth, sucralfate

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

Misoprostol

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)

Aluminum hydroxide

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

Calcium carbonate

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

Magnesium hydroxide

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

Infliximab

Monoclonal antibody to TNF-α Indicated for Crohn disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, psoriasis SA: infection, fever, hypotension

Sulfasalazine

Colonic bacteria activate sulfapyridine (antibacterial) and 5-aminosalicyclic acid (anti-inflammatory) Indicated for ulcerative colitis, Chron disease SA: malaise, nausea, sulfonamide toxicity, reversible oligospermia

Ondansetron

5-HT3 antagonist → ↓ vagal stimulation → central-acting anti-emetic Indicated for postoperative and post chemotherapy nausea and vomiting SA: headache, constipation

Metclopramide

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)

Rifaximin

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

Lactulose

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

Anti-emetics

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)

Hydroxyzine

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)

Diphenhydramine

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)

Promethazine

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)

Chlorpheniramine

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)

Loratadine

Second generation H1 antagonist Indicated for allergies Fewer side effects than first generation (less lipopholic → less likely to cross BBB and cause sedation)

Cetirizine

Second generation H1 antagonist Indicated for allergies Fewer side effects than first generation (less lipopholic → less likely to cross BBB and cause sedation)

Finasteride

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)

Succinylcholine

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

Dimenhydrinate

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)

Fexofenadine

Second generation H1 antagonist Indicated for allergies Fewer side effects than first generation (less lipopholic → less likely to cross BBB and cause sedation)

Desloratidine

Second generation H1 antagonist Indicated for allergies Fewer side effects than first generation (less lipopholic → less likely to cross BBB and cause sedation)

Guaifenesin

Expectorant Thins respiratory secretions but does not suppress cough

Dextromethorphan

NMD glutamate receptor antagonist → antitussive Synthetic codeine analog that has mild opioid effect when used in excess → can give naloxone for overdose

N-acetylcystine

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

Pseudoephedrine

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

Formoterol

Sympathomimetic (β2 \> β1) Indicated for asthma and COPD (long-acting) prophylaxis SA: tremor, arrythmia

Theophylline

Methylxanthine → inhibits phosphodiesterase → ↑ cAMP → bronchial smooth muscle relaxation SA: cardiotoxicity, neurotoxicity, blocks actions of adenosine (limited use due to narrow therapeutic index)

Beclomethasone

Inhibits synthesis of many cytokines, including inactivation of NF-κB (transcription factor) → ↓ TNF-α Indicated for chronic asthma (first line)

Fluticasone

Inhibits synthesis of many cytokines, including inactivation of NF-κB (transcription factor) → ↓ TNF-α Indicated for chronic asthma (first line)

Montelukast

Leukotriene receptor blocker Indicated for asthma, especially aspirin-induced

Zafirlukast

Leukotriene receptor blocker Indicated for asthma, especially aspirin-induced

Zileuton

5-lipooxygenase inhibitor blocks converstion of arachidonic acid to leukotrienes Indicated for asthma

Omalizumab

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

Bosentan

Antagonizes endothelin-1 receptors to ↓ pulmonary vascular resistance Indicated for pulmonary arterial hypertension

Vecuronium

Nondepolarizing NMJ blocker Competitive inhibitor of postsynaptic acetycholine receptors at the NMJ Can be reversed with neostigmine

Pancuronium

Nondepolarizing NMJ blocker Competitive inhibitor of postsynaptic acetycholine receptors at the NMJ Can be reversed with neostigmine

Turbocurarine

Nondepolarizing NMJ blocker Competitive inhibitor of postsynaptic acetycholine receptors at the NMJ Can be reversed with neostigmine

Varenicline

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

Cromolyn Nedocromil

Inhibits mast cell degranulation Indicated for prophylaxis for seasonal symptoms, aspirin hypersensitivity, and exercise-induced asthma

Latanoprost

PGF2α agonist → ↑ outflow of aqueous humor Indicated for glaucoma SA: darkens color of iris

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

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)

Butorphanol

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

Tramadol

Very weak opioid agonist Indicated for chronic pain SA: similar to other opioids + decreased seizure threshold, serotonin syndrome

Ethnosuximide

Blocks thalamic T-type Ca2+ channels Indicated for absence seizures

Phenytoin

Increased sodium channel inactivation Indicated for tonic-clonic seizures (first line) SA: gingival hyperplasia, hirsutism, megaloblastic anemia, SLE-like syndrome

Carbamazepine

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

Valproic acid

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)_

Gabapentin

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

Barbiturates (phenobarbital, pentobarbital, thiopental, secobarbital)

↑ _duration_ of chloride channel opening → ↑ GABA_A action → ↓ neuron firing SA: respiratory and cardiovascular depression, CNS depression (exacerbated by alcohol)

Benzodiazepines

↑ _frequency_ of chloride channel opening → ↑ GABA_A 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)

Relationship between solubility and induction time and potency for CNS anesthetics

↓ 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

Dantrolene

Prevents release of calcium from the sarcoplasmic reticulum of skeletal muscle Indicated to treat malignant hyperthemia and neuroleptic malignant syndrome

Levodopa/carbidopa

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

First line treatment for essential tremor

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

Where are α1 receptors located?

Vascular smooth muscle α1 stimulation = contraction/constriction Bladder α1 stimulation = contraction of internal urethral sphincter Eye α1 stimulation = mydriasis (dilation)

Where are β2 receptors located?

Skeletal muscle vasculature β2 stimulation = relaxation/vasodilation Bronchi β2 stimulation = bronchodilation Uterus β2 stimulation = relaxation (tocolysis)

Pramipexole

Non-ergot dopamine agonist Indicated for Parkinsons, restless leg syndrome

Treatment for status epilepticus

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

Remelteon

Melatonin agonist Indicated for insomnia, especially in older adults Short-term use

Sumatriptan

5-HT_IB/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

Cytochrome P-450 inducers

Carbamazepine Barbiturates Phenytoin Rifampin Griseofulvin St John's wort Modafinil Cyslophosphamide OCPs

Cytochrome P-450 inhibitors

Acetaminophen NSAIDs Amiodarone Cimetidine Fluoroquinolones Clarithromycin Azole antifunals Grapefruit juice Isoniazid Ritonavir Omeprazole Thyroid hormone SSRIs

Effects of inhaled anesthetics

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

Anticonvulsants indicated for absence seizures

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)

Organophosphate poisoning

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

Buprenorphine

Partial opioid agonist Can precipitate withdrawal in opioid-tolerant patients

Baclofen

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

Non-benzodiazepine hypnotics (Z drugs) Zolpidem Zaleplon Eszopiclone

Binds to BZ1 subtype of the GABA_A receptor Indicated for insomnia Decreased risk of dependence compared to benzodiazepines

Memantine

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

Probenecid

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)

Retinoids (tretinoin, adapalene, tazarotene, isotretinoin)

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