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49 Cards in this Set

  • Front
  • Back

Three groups of vasoactive peptides

1) Vasoconstrictors




2) Vasodilators




3) Peptides with mixed effects

ACE Inhibitors

1) Captopril




2) Enalapril




3) Lisinopril

Angiotensin II Receptor Blockers (ARBs)

1) Saralasin




2) Losartan




3) Valsartan




4) Telmisartan

Renin Inhibitors

Aliskiren

Drugs that block renin release

1) Clonidine




2) Propranolol

ACE Inhibitors - Mechanism of Action

1) Block angiotensin converting enzyme (ACE), resulting in decreased ANG II formation




2) Decrease systemic vascular resistance (arteriolar and venous); promote natriuresis




3) Prevents bradykinin degradation

Side effects of ACE Inhibitors

1) Cough




2) Angioedema




3) Hyperkalemia




NOTE: Contraindicated in pregnancy

Therapeutic use of ACE Inhibitors

1) Mild to moderate hypertension




2) Diabetic renal failure




3) Congestive heart failure

Saralasin

1) A partial AT receptor agonist that functions as a peptide angiontensin II receptor blocker (ARB)




2) used to treat renin-dependent hypertension

Nonpeptide ARBs

1) Losartan




2) Valsartan




3) Telmisartan

Nonpeptide ARBs - Mechanism of action

1) Competitive antagonists of AT1 receptor




2) Do not interfere with bradykinin degradation

Clinical Uses of Nonpeptide ARBs

1) Hypertension




2) Congestive Heart Failure




3) Prevention of diabetic nephropathy

Side effects of Nonpeptide ARBs

1) Lower incidence of cough




2) Contraindicated in pregnancy and patients with nondiabetic renal disease

Aliskiren - Mechanism of Action

1) Inhibits action of renin, which results in decreased ANG I, ANG II, and aldosterone levels




2) Does not interfere with bradykinin degradation

Clinical Uses of Aliskiren

Hypertension

Side effects of aliskiren

1) Hyperkalemia




2) Renal impairment





3) Headache





4) Diarrhea




5) Contraindicated in pregnancy

Vasodilators

1) Hydralazine




2) Minoxidil




3) Diazoxide




4) Sodium Nitroprusside

Hydralazine - Mechanism of Action

1) Release of nitric oxide from endothelial cells




2) Relaxes smooth muscle (more effective on arterioles)

Clinical Uses of Hydralazine

1) Severe hypertension (long term outpatient therapy)




2) Heart failure

Side effects of Hydralazine

1) Headache


2) Nausea and anorexia


3) Palpitations


4) Sweating and flushing


5) Lupus like syndrome (high doses)


6) Peripheral neuropathy (not common)

Minoxidil- Mechanism of action

1) Opens potassium channels, resulting in hyperpolarization of smooth muscle




2) Promotes arteriolar vasodilation

Clinical Uses of Minoxidil

1) Severe hypertension




2) Baldness (topical application)

Side effects of Minoxidil

1) Hypertrichosis




2) Headache




3) Sweating

Diazoxide - Mechanism of action

1) Opens potassium channels, resulting in smooth muscle hyperpolarization




2) Produces arteriolar vasodilation




3) Reduces insulin release

Clinical Uses of Diazoxide

Hypertensive emergencies

Side effects of Diazoxide

1) Hypotension




2) Hyperglycemia




3) Edema




4) Reflex tachycardia

Sodium Nitroprusside - Mechanism of Action

1) Stimulates release of nitric oxide and increases cGMP




2) Decreases total peripheral resistance by dilation of arterioles and venules

Clinical Uses of Sodium Nitroprusside

1) Hypertensive emergencies




2) Severe heart failure

Side Effects of Sodium Nitroprusside

1) Excessive hypotension




2) Shock




3) Cyanide toxicity

Drugs used to treat angina

1) Nitrates




2) Beta blockers




3) Calcium channel blockers

Types of nitrates

1) Nitroglycerin (prototype)




2) Isosorbide dinitrate




2) Isosorbide mononitrate

Nitrates - Mechanism of Action

1) A prodrug of nitric oxide




2) Increases NO levels, resulting in smooth muscle relaxation and venodilation




3) primarily works on arteries and veins; no direct effects on cardiac muscle

Clinical Uses of Nitrates

1) Acute angina episodes (given sublingual)




2) Prophylaxis of angina


(given oral or transdermal)




3) Acute coronary syndrome (given IV)

Side effects of Nitrates

1) Tachycardia




2) Orthostatic hypotension




3) Throbbing headache

Monday Disease

1) Syndrome experienced by workers exposed to nitrate contaminants in the workplace




2) Workers develop tolerance to nitrates during the work week that disappears over the weekend

Amyl nitrate

1) Rapid acting drug taken via inhalation




2) Acts by releasing NO, resulting in increased cGMP and vasodilation

Clinical Uses of Amyl Nitrate

1) Rarely prescribed to prevent angina




2) Cyanide poisoning

Side effects of Amyl Nitrate

Methemoglobinemia


(at high concentrations)

Beta Blockers -Mechanism of Action

1) Acts primarily on the heart




2) Inhibits beta adrenergic receptors




3) Decreases heart rate, cardiac force and pressure




4) Increases heart size and injection time

Clinical Uses of Beta Blockers

Prevent effort angina

Side effects of Beta Blockers

1) Cardiovascular effects


(bradycardia, atrioventricular blockade, heart failure)




2) Severe asthma attacks




3) CNS effects (sedation, fatigue, sleep alterations)




4) Sexual dysfunction

Types of Calcium Channel Blockers

1) Dihydropyridines (Nifedipine, Amlodipine)




2) Phenylalkylamines (Verapamil)




3) Benzothiazepines (Diltiazem)

Calcium Channel Blockers - Mechanism of Action

Blocks L-type calcium channels in heart and blood vessels; results in decreased intracellular calcium

Clinical Uses of Calcium Channel Blockers

1) Treatment of AV node arrythmias (verapamil and diltiazem only)




2) Hypertension




3) Prophylatic therapy for effort and vasospastic angina




4) Moderately effective in hypertrophic cardiomyopathy, migraine and Raynaud's phenomenon

Side Effects of Calcium Channel Blockers

1) Constipation


2) Pretibial edema


3) Nausea


4) Flushing


5) Dizziness


6) Heart failure


7) AV blockade


8) Sinus node depression

Ranolazine - Mechanism of Action

1) Blocks late inward sodium current in myocardial cells, resulting in decreased calcium accumulation




2) Decreases end diastolic pressure and improves diastolic coronary flow




3) Thought to inhibit fatty acid oxidase

Clinical Uses of Ranolazine

Prevent angina

Side effects of Ranolazine

1) Constipation


2) Nausea


3) Dizziness


4) Prolongs QT interval

Ivabradine

1) Drug that inhibits If sodium channel in SA node; produces a reduction in heart rate and reduced myocardial O2 demand




2) Approved in U.S. for treatment of chronic heart failure




3) Also used in Europe to treat stable angina