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MD Cardiology Pharm

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mdunk12's version from 2016-02-29 00:59

1a. Adrenergic mechanisms

Question Answer
Epinephrine (activates what types of receptors?)beta > alpha
Norepinephrine (activates what types of receptors?)Alpha-1 > alpha-2 > beta-1 (NO beta-2)
Isoproterenol (activates what types of receptors?)Beta-1 and beta-2 "pure beta activator"
Dopamine (activates what types of receptors?)Varies relative to its concentration (low activates D1, moderate activates beta, high activates alpha)
Dobutamine (activates what types of receptors?)Preferentially activates beta-1 receptors
Phenylephrine (activates what types of receptors?)Preferentially activates alpha receptors (alpha-1 and alpha-2) "Pure alpha activator"
Metaproterenol, albuterol, salmeterol, terbutaline (MAST; activates what types of receptors?)Preferentially activates beta-2
AmphetamineReleases stored catecholamines
EphedrineReleases stored catecholamines
CocaineCatecholamine reuptake inhibitor
ClonidineAlpha-2 agonist
Alpha-methyldopaAlpha-2 agonist
PhenoxybenzamineIrreversible alpha blocker (for pheochromocytoma, FYI)
PhentolamineReversible alpha blocker
Prazosin (--ZOSIN)Alpha-1 blocker
MirtazapineAlpha-2 blocker
Beta-1 selective blockersBeta-blockers Acting Exclusively at Myocardium (Atenolol, Betaxolol, Esmolol, Acebutolol, Metoprolol
Non-selective antagonists(Please Try Not [being] Picky) Propranolol, Timolol, Nadolol, Pindolol
Partial beta-agonists(PArtial Beta-Agonists) Pindolol and Acebutolol
Nonselective vasodilatory alpha and beta (mixed) blockersCarvediolol and Labetalol
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1b. Adrenergic pharmacokinetics and ADRs

Question Answer
Do not abruptly stop because massive epinephrine release can occurClonidine
Reflex tachycardia, dizziness, and nasal congestionPhentolamine and phenoxybenzamine
Sleepiness, sexual dysfunction, depressionPropranolol
ABCDE Asthma, Block (heart), COPD, Diabetes, Electrolyte (hyperkalemia)Beta blocker major contraindications
Beta blockers affect all the med school blocks - Endo, Repro, Neuro, Cardio and Pulm
(Endo: dyslipidemia, hypoglycemia; Repro: ED; Neuro: seizures, sedation, sleep (vivid dreams); Cardio: AV block, bradycardia; AND Pulm: bronchoconstriction)
Side effects of Beta blockers
Saline, Glucagon, AtropineTreatment of beta blocker toxicity
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2a. Hypertension drug mechanisms

Question Answer
Hydrochlorothiazide (HCTZ)Inhibits sodium reabsorption in the distal tubule by blocking the Na/Cl transporter
TriamptereneDirectly inhibits ENaC channels in the distal tubule (potassium-sparing diuretic)
AliskirenDirect renin inhibitor
Captopril, enalapril (--PRIL)ACE inhibitors, which block conversion of angiotensin-I to angiotensin-II
Losartan (--SARTAN)ARB (angiotensin-receptor blocker), which blocks angiotensin-II at angiotensin-I receptor to decrease vasoconstriction, aldosterone release, and sympathetic activation
EplerenoneAldosterone receptor antagonist (regardless of how aldosterone is produced)
Nifedipine (--DIPINE)Dihydropyridine (DHP) calcium channel blocker (CCB) preferentially acting on the vasculature to vasodilate (vessels > myocardium > nodes)
Verapamil, diltiazamNon-dihydropyridine (DHP) calcium channel blockers (CCBs) that preferentially act on nodes to elicit negative inotropic effects (prevents troponin from moving in myocytes) to slow heart rate
HydralazineIncreases cGMP; relaxes arteriolar smooth muscle (vasodilator)
MinoxidilModulates ATP-activated potassium channels in ARTERIOLAR smooth muscle (reduces likelihood of contraction)
NitroprussideConverted to nitric oxide intravascularly to facilitate vasodilation; works on VENOUS and ARTERIOLAR smooth muscle
Prazosin (--ZOSIN)Block peripheral alpha-1 receptors to induce vasodilation
Metoprolol and atenololLower heart rate (reducing CO) and reduce renin release in the kidney
Labetalol and carvediolol MOALower total peripheral resistance (TPR) without significantly affecting heart rate of cardiac output
AmloridePotassium-sparing diuretic
Name 4 Thiazide diureticsHCTZ, Chlorthalidone, Indapamide, Metolazone
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2b. Hypertension drug pharmacokinetics and ADRs

Question Answer
Activates a PTH-dependent Ca channel (relevant in cardio in that this drug causes calcium reabsorption)Hydrochlorothiazide (HCTZ)
“Hyper GLUC” hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia + HYPOkalemiaHydrochlorothiazide (HCTZ)
Concerns regarding lithium interactions (lithium can block secretion of this drug into the urine)Hydrochlorothiazide (HCTZ)
HyperkalemiaTriampterene
Teratogenic and contraindicated in bilateral renal artery stenosisAliskiren
CoughACE inhibitors (bradykinin effect)
Reflex tachycardia, conduction defects, gingival hyperplasia, peripheral edema (from dilation)Dihydropyridines CCBs (e.g. nifedipine; --PINE) as well as non-DHP CCBs
Drug-induced lupus, fluid retentionInvolves drugs that are ACETYLATED (Hydralazine is one of them)
Hypertrichosis (abnormal amount of hair growth over the body) and tachycardiaMinoxidil
Cyanide toxicity, rebound HTNNitroprusside (administer w/ sodum thiosulfate )
"CATCHH" Cough, Angio, Teratogen, Creatinine elev., Hypotension, HyperkalemiaACEI --prils (Captopril has a CATCHH)
PARK -- Pregnancy, Allergy, Renal artery stenosis (bilateral), K increase (hyperkalemia)ACEI contraindications
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3a. Lipid/Diet Mechanisms, Principles and Normal Values

Question Answer
HMG-CoA reductase inhibitors lovastatin, pravastatin, simvastatin, atorvastatin, rosuvastatin
Statins MOAlower endogenous CHO → increased hepatic LDLR → lower LDL
Choletipol classbile acid resin
Ezetimibe MOAinhibits cholesterol absorption in brush border of duodenum and ilium
Fibrinic acids MOAInhibit an inhibitor of lipoprotein lipase, which increases the efficiency of endothelial lipoprotein lipase (which increases breakdown of fatty acids). Specifically, endothelial lipoprotein lipase activity increases through PPAR-alpha
Colesevelam/cholestyramine MOABind bile salts and prevent bile reabsorption in the ileum, prompting the liver to upregulate LDL receptors for bile synthesis
Name 4 fibratesgemfibrozil, clofibrate, bezafibrate, fenofibrate
What is vitamin B3Niacin
Post MI lipid management protocolHigh intensity statins (Atorvastatin, Rosuvastatin) increase survival post MI
Niacin MOADecreases VLDL secretion by unknown mechanism, decreases adipocyte FFA mobilization by hormone sensitive lipase
Statin effects on lipidsLarge LDL decrease (45-55% - primary effect); Small HDL increase/TG decrease (dose-dependent)
Bile acid resins lipid effectsLDL decrease; slight HDL increase/TG decrease (not main effect)
Ezetimibe lipid effectsLDL decrease only
Fibrates lipid effectsGreatly reduces TAGs (main effect), elevates HDL, but NOT used to lower LDL
Niacin lipid effectsGREATLY increases HDL (main effect - only one with real effect on HDL), decreases TG/LDL modestly
Rule of 30s< 160 for one or fewer risk factors, < 130 two or more risk factors, < 100 CAD or diabetes, < 70 diabetes and CAD
Normal LDL value60-130, 160 is high
Normal HDL value>40 males, >50 females
Normal value for TAG/VLDL<150 (> 200 abnormal)
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3b. ADR/Pharmacokinetics of Lipid/Diet Drugs

Question Answer
ADR of StatinsMyositis, rare hepatotoxicity (elevates enzymes)
P450 liver enzyme inhibitorsAzoles (antifungals), macrolides, HIV protease inhibitors, cyclosporine, grapefruit juice (copious amounts of it), fibrates (IMPORTANT)
Metabolism of statinsAll metabolized by P450 except Pravastatin (thus avoid grapefruit juice ... etc. when taking)
Fibrates ADRMyopathy (risk increased when used with statins), cholesterol gall stones, P450 inhibitor (impairs warfarin clearance)
Niacin ADRFlushing (prostaglandin-mediated vasodilation), increases uric acid, hyperglycemia, can damage the liver (rare liver failure)
Bile acid resins ADRGI upset (constipation and bloating), decreases absorption of anionic drugs (warfarin, fibrates) and fat-soluble vitamins
Contraindications of bile acidsbile acids are contraindicated when triglycerides are high (can have the effect of raising triglycerides)
Which lipid lowering drug is contraindicated in pregnancy?Statins are thought to be teratogenic
Summary of clinical trial benefits of statin use(1) Reduce risk of coronary artery disease (2) Reduce risk of ischemic stroke
Which lipid lowering drug can INCREASE TG/VLDL in someBile acid resins (can increase in familial combined hyperlipidemia)
Effect of EtOH on lipidsIncreased VLDL and triglycerides (with chronic alcohol -- one of the mechanisms for pancreatitis); EtOH can actually increased HDL
Statin hepatotoxicityIncreased AST & ALT
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4a. Anti-Angina Drugs MOA

Question Answer
Nitrate that has a rapid onset, but is quickly metabolizedNitroglycerin
What is the primary action of nitroglycerine in treating stable anginareduces MVO2 by causing VENOdilation -> decreases venous return -> decreases preload
What happens when nitroglycerin is given by IV?Balanced vasodilation (both arteries and veins dilate)
Nitrate that undergoes significant first-pass metabolismIsosorbide dinitrate
Nitrate that is completely bioavailable (no first-pass metabolism)Isosorbide mononitrate
Nitrates and venous capacitanceIncrease venous capacitance, which can pool blood in peripheral veins (this decreases stress on the myocardial wall, which in turn reduces oxygen demand)
Preventing development of nitrate tolerance(1) Nitrate free intervals (IMPORTANT), (2) ACEIs, (3) folic acid, (4) vitamin C, (5) supplemental L-arginine
Tachyphylaxis and nitrates"Monday morning blues" where tolerance to nitrates develops with uninterrupted usage (folks exposed to nitrates throughout their work do not feel the side effects, but when they return on Monday, they feel the ADRs and thus feel "blue") usually presented as a worker in a munition factory (nitrate exposure)
Main ADRs of nitratesHeadache (problematic in that it reduces compliance), tachycardia, orthostatic hypotension
Methemoglobin systemOxidation of Fe2+ to Fe3+, which helps bind nitrate species (like cyanide/CN) and reduce their toxicity
Erectile dysfunction and nitratesDo NOT give Viagra (sildenAFIL; --AFIL), since these drugs inhibit the breakdown of cGMP and can cause hypotensive crisis
Prolongs the QT interval, causes dizziness, and causes headachesRanolazine
Describe the progression of Nytroglycerine metabolism in the liver and smooth muscleNitroglycerine -> dinitrate (less active, remains longer) -> mononitrate (remains longer)
Describe the endogenous production of Nitric OxideArginine is broken down by endothelial Nitric Oxide Synthase (eNOS) to generate NO + citrulline
Verapamil/Diltiazem ADRConstipation, edema/fluid retention, dizziness; at high doses -> cardiac depression/hypotension (diltaizem has lower ADR profile because of shorter duration of action)
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4b. Anti-Anginal pharmacokinetics and ADRs

Question Answer
Nitrate that has a rapid onset, but is quickly metabolizedNitroglycerin
What is the primary action of nitroglycerine in treating stable anginareduces MVO2 by causing VENOdilation -> decreases venous return -> decreases preload
What happens when nitroglycerin is given by IV?Balanced vasodilation (both arteries and veins dilate)
Nitrate that undergoes significant first-pass by liverIsosorbide dinitrate
Nitrate that is completely bioavailable (no first-pass metabolism)Isosorbide mononitrate
Nitrates and venous capacitanceIncrease venous capacitance, which can pool blood in peripheral veins (this decreases stress on the myocardial wall, which in turn reduces oxygen demand)
Preventing development of nitrate tolerance(1) Nitrate free intervals (IMPORTANT), (2) ACEIs, (3) folic acid, (4) vitamin C, (5) supplemental L-arginine
Tachyphylaxis and nitrates"Monday morning blues" where tolerance to nitrates develops with uninterrupted usage (folks exposed to nitrates throughout their work do not feel the side effects, but when they return on Monday, they feel the ADRs and thus feel "blue") usually presented as a worker in a munition factory (nitrate exposure)
Main ADRs of nitratesHeadache (problematic in that it reduces compliance), tachycardia, orthostatic hypotension
Methemoglobin systemOxidation of Fe2+ to Fe3+, which helps bind nitrate species (like cyanide/CN) and reduce their toxicity
Contraindications w/ NitratesDo NOT give Viagra (sindenafil; --AFIL) or other PDE5 inhibitors -> inhibit breakdown of cGMP and can cause fatal hypotension
Prolongs the QT interval, causes dizziness, and causes headachesRanolazine
Describe the progression of Nytroglycerine metabolism in the liver and smooth muscleNitroglycerine -> dinitrate (less active, remains longer) -> mononitrate (remains longer)
Describe the endogenous production of Nitric OxideArginine is broken down by endothelial Nitric Oxide Synthase (eNOS) to generate NO + citrulline
Verapamil/Diltiazem ADRConstipation, edema/fluid retention, dizziness; at high doses -> cardiac depression/hypotension (diltaizem has lower ADR profile because of shorter duration of action)
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