Cardio - Pharm (Part 1: Antihypertensives & Antianginal therapies) Flashcards
Pg. 298-299 in First Aid 2014 Pg. 279-280 in First Aid 2013 Sections include: -Antihypertensive therapy -Calcium channel blockers -Hydralazine -Hypertensive emergency (In FA2013, Malignant hypertension treatment) -Nitroglycerin, isosorbide dinitrate -Antianginal therapy
What are the 3 major conditions treated by antihypertensive therapy?
(1) Primary (essential) hypertension (2) Hypertension with CHF (3) Hypertension with Diabetes mellitus
What 4 drugs are used as antihypertensive therapy in Primary (Essential) hypertension?
(1) Diuretics, (2) ACE inhibitors, (3) angiotensin II receptor blocks (ARBs), (4) calcium channel blockers
What 4 drugs are used as antihypertensive therapy in CHF?
(1) Diuretics, (2) ACE inhibitors/ARBs, (3) Beta-blockers (compensated CHF), (4) Aldosterone antagonists
What 5 drugs are used as antihypertensive therapy in Diabetes mellitus?
(1) ACE inhibitors/ARBs, (2) calcium channel blockers, (3) diuretics, (4) B-blockers, (5) alpha-blockers
When must Beta-blockers be used cautiously with regard to CHF, and when are they contraindicated?
In decompensated CHF; in cardiogenic shock
What should you remember about the potential effects of ACE inhibitors/ARBs in diabetic patients?
ACE inhibitors/ARBs are protective against diabetic neuropathy
For what condition are the following drugs used: Diuretics, ACE inhibitors, angiotensin II receptor blockers (ARBs), calcium channel blockers?
Primary (Essential) hypertension
For what condition are the following drugs used: Diuretics, ACE inhibitors/Angiotensin II receptor blockers (ARBs), beta-blockers (compensated CHF), aldosterone antagonists?
Hypertension with CHF
For what condition are the following drugs used: ACE inhibitors/ARBs, calcium channel blockers, diuretics, beta-blockers, alpha-blockers?
Hypertension with Diabetes mellitus
What are 3 examples of dihydropyridine calcium channel blockers? What are 2 examples of non-dihydropyridine calcium channel blockers?
Amlodipine, Nimodipine, Nifedipine (Dihydropyridine); Diltiazem, Verapamil (Non-Dihydropyridine)
What is the mechanism of calcium channel blockers, and what effect does this have?
Block voltage-dependent L-type calcium channels of cardiac and smooth muscle & thereby reduce muscle contractility
In terms of their effects on vascular smooth muscle, how do the following calcium channel blockers compare: amlodipine, diltiazem, nifedipine, verapamil?
Vascular smooth muscle - amlodipine = nifedipine > diltiazem > verapamil
In terms of their effects on heart, how do the following calcium channel blockers compare: amlodipine, diltiazem, nifedipine, verapamil?
Heart - verapamil > diltiazem > amlodipine = nifedipine; Think: “Verapamil = Ventricle”
For what 3 conditions are dihydropyridine calcium channel blockers used clinically? Which dihydropyridine calcium channel blocker is the exception? For what is that particular one used, and why?
Dihydropyridine (except Nimodipine): Hypertension, Angina (including Prinzmetal), Raynaud’s phenomenon; Nimodipine: Subarachnoid hemorrhage (prevents cerebral vasospasm)
What are 7 toxicities associated with calcium channel blockers (i.e., amlodipine, nimodipine, nifedipine, diltiazem, and verapamil)?
(1) Cardiac depression, (2) AV block, (3) peripheral edema, (4) flushing, (5) dizziness, (6) hyperprolactinemia, & (7) constipation
What is the mechanism of hydralazine? What effects does it have on arterioles versus veins? What effect does this have on afterload?
Increases cGMP –> smooth muscle relaxation. Vasodilates arterioles > veins; afterload reduction
In what 3 conditions/settings is hydralazine used clinically? How is it frequently administered, and why?
(1) Severe hypertension, (2) CHF; (3) First-line therapy for hypertension in pregnancy, with methyldopa; Frequently coadministered with Beta-blocker to prevent reflex tachycardia
What is the first-line therapy for hypertension in pregnancy?
Hydralazine - First-line therapy for hypertension in pregnancy, with methyldopa;
What are 6 toxicities of hydralazine?
(1) Compensatory tachycardia (contraindicated in angina/CAD), (2) fluid retention, (3) nausea, (4) headache, (5) angina. (6) Lupus-like syndrome
What are 5 drugs commonly used in hypertensive emergency?
Commonly used drugs include (1) Nitroprusside, (2) Nicardipine, (3) Clevidipine, (4) Labetalol, and (5) Fenoldopam
What condition is Nitroprusside used to treat clinically? What is its length of action?
Hypertensive emergency; Short acting
What is the mechanism of Nitroprusside? What is a potential toxicity associated with this drug?
Increase cGMP via direct release of NO; Can cause cyanide toxicity (releases cyanide)
What condition is Fenoldopam used to treat clinically? What is its mechanism? What 3 major effects does it have?
Hypertensive emergency; Dopamine D1 receptor agonist - (1) coronary, peripheral, renal, and splanchnic vasodilation; (2) Decreased BP and (3) Increased natriuresis
What other drug shares the same mechanism as nitroglycerin? What is their mechanism?
Isosorbide dinitrate; Vasodilate by increasing nitric oxide in smooth muscle, causing increase in cGMP & smooth muscle relaxation
Again, what is the mechanism of nitroglycerin and isosorbide dinitrate? What effect does this have on arteries versus veins? What effect does this have on preload?
Vasodilate by increasing nitric oxide in smooth muscle, causing increase in cGMP & smooth muscle relaxation; Dilate veins»_space; arteries; Decrease preload
For what 3 conditions are nitroglycerin and isosorbide dinitrate used clinically?
(1) Angina, (2) Acute coronary artery syndrome, (3) Pulmonary edema
What are 5 toxicities associated with nitroglycerin and isosorbide dinitrate?
(1) Reflex tachycardia (treat with Beta-blockers), (2) hypotension, (3) flushing, (4) headache, (5) “Monday disease” in industrial exposure: development of tolerance for the vasodilating action during the work week and loss of tolerance over the weekend results in tachycardia, dizziness, and headache upon reexposure
What is the goal of antianginal therapy? What are the factors involved in achieving this goal?
Reduction of myocardial O2 consumption (MVO2) by decreasing 1 or more of the determinants of MVO2: end-diastolic volume, blood pressure, heart rate, contractility
Do nitrates versus Beta-blockers affect afterload or preload?
Nitrates - Preload; Beta-blockers - Afterload
What affect do nitrates have on the following factors associated with myocardial O2 consumption: (1) End-diastolic volume (2) Blood pressure (3) Contractility (4) Heart rate (5) Ejection time (6) MVO2?
(1) Decrease (2) Decrease (3) Increase (reflex response) (4) Increase (reflex response) (5) Decrease (6) Decrease
What affect do beta-blockers have on the following factors associated with myocardial O2 consumption: (1) End-diastolic volume (2) Blood pressure (3) Contractility (4) Heart rate (5) Ejection time (6) MVO2?
(1) Increase (2) Decrease (3) Decrease (4) Decrease (5) Increase (6) Decrease
What affect do nitrates and beta-blockers combined have on the following factors associated with myocardial O2 consumption: (1) End-diastolic volume (2) Blood pressure (3) Contractility (4) Heart rate (5) Ejection time (6) MVO2?
(1) No effect or decrease (2) Decrease (3) Little/no effect (4) Decrease (5) Little/no effect (6) Significant Decrease
How do calcium channel blockers compare to nitrates and beta-blockers in terms of effect? Give a specific calcium channel blockers that relates to each.
Nifedipine is similar to Nitrates in effect; Verapamil is similar to Beta-blockers in effect
What are 2 examples of partial Beta-agonists? In what clinical condition are they contraindicated?
Pindolol and acebutolol; angina
What are 3 conditions for which non-dihydropyridine calcium channel blockers are used clinically?
Non-dihydropyridine: (1) Hypertension (2) Angina (3) Atrial fibrillation/flutter
In what condition(s) is Hydralazine contraindicated, and why?
Toxicity: Compensatory tachycardia (contraindicated in angina/CAD)
What adverse effect can nitroglycerin and Isosorbide dinitrate have on the heart? How is this treated?
Reflex tachycardia (treat with Beta-blockers)
What 2 drugs are associated with “Monday disease” as a toxicity? Describe the disease and give its 3 symptoms.
Nitroglycerin, Isosorbide dinitrate; “Monday disease” in industrial exposure: development of tolerance for the vasodilating action during the work week and loss of tolerance over the weekend results in tachycardia, dizziness, and headache upon reexposure
What are 4 determinants of myocardial O2 consumption (MVO2)?
Determinants of MVO2: end-diastolic volume, blood pressure, heart rate, contractility
Give 2 examples of non-dihydropyridine calcium channel blockers. For which 3 conditions are non-dihydropyridine calcium channel blockers used clinically?
(1) Diltiazem (2) Verapamil; Non-dihydropyridine: (1) Hypertension, (2) Angina, (3) Atrial fibrillation/flutter