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18 Cards in this Set

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Drugs used to treat angina
1) Nitrates


2) Beta blockers


3) Calcium channel blockers





4) Sodium channel blockers

Types of nitrates
1) Nitroglycerin (prototype)


2) Isosorbide dinitrate


2) Isosorbide mononitrate
Nitrates – Mechanism of Action
1)


1) A prodrug of nitric oxide that increases NO levels, resulting in smooth muscle relaxation and venodilation


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



3) Decrease O2 demand and increase O2 delivery

Clinical Uses of Nitrates
1) Effective in staable (effort -induced) and variant (rest) angina pectoris





2) Works rapidly to relieve symptoms

(given oral or transdermal)


3) Acute coronary syndrome (given IV)
Side effects of Nitrates
1) Tachycardia


2) Postural hypotension


3) Throbbing headache



4) Facial flushing




NOTE: Contraindicated in patients taking phosphodiesterase V inhibitors

Beta Blockers –Mechanism of Action
1) Acts primarily on the heart


2) Inhibits beta adrenergic receptors


3) Decreases heart rate, cardiac output, and blood pressure



4) Decreases myocardial O2 demand


Clinical Uses of Beta Blockers
Prevent effort angina
Contraindications of Beta Blockers
1) Do not use in patients with asthma, diabetes, COPD, and severe bradycardia



2) When discontinuing drug, dose has to be gradually tapered off in order to prevent rebound angina, MI and hypertension

Types of Calcium Channel Blockers
1) Dihydropyridines (Nifedipine, Amlodipine)


2) Phenylalkylamines (Verapamil)


3) Benzothiazepines (Diltiazem)
Calcium Channel Blockers – Mechanism of Action
1) Blocks L–type calcium channels in heart and blood vessels; results in decreased intracellular calcium



2) Decrease O2 demand and increase O2 delivery

Clinical Uses of Calcium Channel Blockers

Useful for both effort induced angina and vasospastic angina

Ranolazine – Mechanism of Action
1) Blocks late inward sodium current in myocardial cells, resulting in decreased calcium accumulation

2) Improves diastolic function



3) Decreases oxygen demand



Clinical Uses of Ranolazine

Used to treat chronic angina or when other antianginal therapies have failed

Nifedipine

1) Calcium channel blocker




2) Functions mainly as an arteriolar vasodilator; has minimal effects on cardiac conduction or heart rate

Side effects of Nifedipine

1) Flushing, headache, hypotension and peripheral edema (due to vasodilator effect)




2) Constipation




3) Reflex tachycardia

Verapamil

1) Calcium channel blocker




2) Causes greater negative inotropic effect than nifedipine, but is a weaker vasodilator

Types of angina

1) Effort induced (also known as stable, classical or typical angina)




2) Unstable angina




3) Rest angina (also known as Prinzmetal, variant or vasospastic angina)

Tolerance of Nitrates

1) Can occur rapidly after drug administration




2) Drug sensitivity restored after a daily nitrate-free interval (usually ~ 10-12 hours at night)