Pharmacology Part 1 Flashcards by roxanne massoumi

What is the therapy for essential hypertension?

Diuretics
ACE I
ARB
CCB

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What is the therapy for CHF?

Diuretics
ACE I
ARB
Beta Blocker (compensated CHF)
K+ sparing diuretics

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Beta blockers must be used cautiously in __________ and are contraindicated in ________

decompensated CHF, cardiogenic shock

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What is the therapy for Diabetes Mellitus?

Diruetics
ACE I
ARB
CCB
Beta Blocker
Alpha Blocker

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ACE Inhibitors are protective against what?

Diabetic nephropathy

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What are the CCBs?

Nifedipine, verapamil, diltiazem, amlodipine

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What is the mechanism of CCBs

Block voltage dependent L-type Ca Channels of Cardiac and smooth muscle and therby reduce muscle contractility

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Name the order of Vascular smooth muscle CCBs

AND Vascular

A=N>D>V

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Name the order of heart CCBs

AND Vascular backwards

V>D>N=A

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What are the clinical uses of CCBs?

Hypertension
Angina
Arrythmia (not nifedipine)
Prinzmetal's angina
Raynauds

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What is the side effects of CCBs?

Cardiac depression
AV block
peripheral edema
flushing
dizziness
constipation

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What is the mechanism behind hydralazine?

Increased cGMP causes smooth muscle relaxation

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Hydralazine vasodilates ______>_______ and thus causes _______ reduction

arterioles, veins, afterload

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Hydralazine is used for what?

Severe hypertension

CHF

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hydralazine is the first line therapy for ___________ with _______

hypertension in pregnancy, methyldopa

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Hydralazine is coadministered with a ________ to prevent _______

Beta blocker

reflex tachycardia

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Hydralazine side effects are what?

Compensatory tachycardia
Fluid retention
Nausea
headache
angina
lupus-like syndrome

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hydralazine is contraindicated in what?

Angina/CAD

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What are the most common used drugs in malifnant hypertension?

Nitroprusside
nicardipine
clevidipine
labetalol
fenoldopam

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What is the mechanism of nitroprusside? and is it short or long acting?

Short acting and increases cGMP via direct release of NO

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Nitroprusside can cause what and why?

Cyanide toxicity because it releases cyanide

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What is the mechanism of fenoldopam?

Dopamine D1 agonist

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Fenoldopam causes vasodilation where?

Coronary
peripheral
renal
splanchnic

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Fenoldopam decreases ________ and increases ________

Blood Pressure, Natiuresis

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What is the mechanism of nitroglycerin and isosorbide dinitrate?

Vasodilate by releasing NO in smooth muscle causing increase in cGMP and smooth muscle relaxation

Nitroglycerin and isosorbide dinitrate dilate ____ more than ______ and decrease______

veins, arteries, preload

What is the clinical use of nitroglycerin and isosorbide dinitrate

Angina, Pulmonary edema

What is the toxicity of nitroglycerin and isosorbide dinitrate?

Reflex tachycardia, hypotension, flushing, headache

What is Monday disease?

development of tolerance for the vasodilating action of nitroglycerin and isosorbide dinitrate during the work week and loss of tolerance over the weekend

What does Monday disease results in upon reexposure to nitroglycerin and isosorbide dinitrate?

Tachycardia Dizziness Headache

What is the goal of anti-anginal therapy?

Reduction go MVO2 by decreasing 1 or more of the determinants of MVO2

What are the determinants of MVO2?

EDV, BP, HR, Contractility, Ejection Time

Name the effects of nitrates on EDV, BP, Contractility, HR, ET, and MVO2

``` Decrease EDV Decrease BP Increase Contractility (reflex) Increase HR (reflex) Decrease ET Decrease MVO2 ```

Name the effects of Beta Blockers on EDV, BP, Contractility, HR, ET, and MVO2

``` Increase EDV Decrease BP Decrease Contractility Decrease HR Increase ET Decrease MVO2 ```

What is the effect of Nitrates + Beta blockers on EDV, BP, Contractility, HR, ET, and MVO2

``` No effect/decrease EDV Decrease BP Little/no effect contractility Decrease HR Little/no effect ET Very decrease MVO2 ```

CCB ______ is similar to nitrates in effect

Nifedipine

CCB _______ is similar to Beta blockers in effect

Verapamil

What are 2 partial beta agonists contradindicated in angina?

Pindolol | Acebutolol

What type of drugs are the statins?

HMG-CoA reductase inhibitors

What is the mechanism of action of the HMG-CoA reductase inhibitors?

Inhibit conversion of HMG-CoA to mevalonate (cholesterol precursor)

What are the side effects of HMG-CoA reductase inhibitors?

Hepatotoxicity (increase LFTs) | Rhabdomyolysis

Name the effects of HMG-CoA reductase inhibitors on LDL, HDL, and TG

3 times decease LDL 1 times increase HDL 1 times decrease TG

What is the mechanism of action of Niacin (vitamin B3)?

Inhibits lipolysis in adipose tissue | Reduces hepatic VLDL secretion into circulation

What are the side effects of Niacin?

Red flushed face hyperglycemia hyperuricemia

With niacin, the red flushed face is decreased by what two things?

Aspirin | long-term use

How does the hyperglycemia caused by Niacin present?

Acanthosis Nigricans

How does the hyperuricemia caused by Niacin present?

Exacerbates gout

Name the effects on LDL, HDL, and TG of Niacin

2 times decreases LDL 2 times increases HDL 1 time decreases TG

Name 3 Bile acid resings

Cholestyramine Colestipol Colesevelam

What is the mechanism of action of Bile acid resins?

Prevent intestinal absorption of BA and liver must use cholesterol to make more

What are the side effects of bile acid resins that makes patients hate it?

- Tastes bad - GI discomfort - Decreased absorption of fat-soluble vitamins - Cholesterol gallstones

Name the effects on LDL, HDL, and TG of bile acid resins

2 times decrease in LDL slight 1 times increase in HDL slight 1 times increase in TG

Name one cholesterol absorption blocker

Ezetimibe

What is the mechanism of cholesterol absorption blockers?

Prevent cholesterol reabsorption at small intestine brush border

What are the side effects of cholesterol absorption blockers?

increase in LFTs (rare) | Diarrhea

Name the effects on LDL, HDL, and TG of Cholesterol absorption blockers

2 times decrease in LDL | no effect in HDL or TG

Name 4 fibrates

Gemfibrozil Clofibrate Bezafibrate fenofibrate

What is the mechanism of action of Fibrates?

Upregulate LPL to increase TG clearance

What are the side effects of fibrates?

Myositis Hepatotoxicity (increased LFTs) cholesterol gallstones

Name the effects on LDL, HDL, and TG of fibrates

1 times decrease LDL 1 times increase HDL 3 times decrease TG

What is the bioavailability, protein bound percent, and half life of Digoxin?

75% bioavailable 20-40% protein bound 40 hours

How is digoxin excreted?

Urine

What are the mechanisms of digoxin?

1. Direct inhibition of Na/K ATPase leads to indirect inhibition of Na/Ca exchanger increasing intracellular Ca and having a positive ionotropic effect 2. Stimulates vagus nerve and decreases HR

What is the clinical use of Digoxin?

CHF | Atrial Fibrilation

Why is digoxin used in CHF?

Incrases contractility

Why is digoxin used in Atrial Fibrillation?

Decreases conduction at the AV node and depresses SA node

What are the cholinergic side effects of Digoxin?

Nausea Vomitting Diarrhea Blurry yellow vision

What are the ECG toxicities of Digoxin?

``` Increased PR Decreased QT ST scooping T wave inversion Arrhythmia AV block ```

What is another toxicities of Digoxin?

Hyperkalemia, a poor prognostic indicator

What are the factors predisposing to toxicity of Digoxin and why?

- Renal Failure (decreased excretion) - Hypokalemia (permissive for digoxin binding at K site of NaK ATPase) - Quinidine (decreased Digoxin clearance and replaces digoxin from tissue binding sites)

What is the antidote for Digoxin toxicity?

- Slowly normalize K - Lidocaine - Cardiac pacer - Anti-digoxin Fab Fragments - Mg2+