ANTI-ANGINAL DRUGS

NITRATES AND NITRITES Amyl Nitrite Nitroglycerin (duration depends on

administration) Isosorbide mononitrate (long duration,

great bioavailability)

NITRATES AND NITRITES MoA: denitrated by glutathione releasing

free nitrites which are converted to NO which increase cGMP dephosphorylation of MLCK and decrease in [Ca] in cell

ActionsDecrease O2 demand by decreasing preload

(relaxation of large veins - VENODILATOR) Increase O2 delivery by relieving coronary

spasm Tolerance appears rapidly but disappears

rapidly too DO NOT WITHDRAW FROM PTS WHO

ARE ON THEM FOR YEARS

NITRATES AND NITRITES Adverse

Reflex tachycardia and postural hypotension with high doses

Increased cGMP = decreased platelet aggregation

Nitrites = methemoglobin formationThrobbing HA, dizziness, flushing

(prevent with NSAIDS)Hypotension w/ sildenafil (viagara)Contraindicated in hypertrophic

cardiomyopathy (preload is already reduced)

NITRATES AND NITRITES USES Tx and prevention of acute attack

(sublingual) Chronic prophylaxis Relieve pulmonary congestion Cyanide poisoning (amyl nitrite

produces methemoglobin which complexes with cyanide)

B-BLOCKERS Propranolol; Metoprolol MoA: decrease O2 demand by

decreasing contractility and heart rate Actions

Decrease cardiac O2 demand Increase myocardial perfusion because

of increased diastolic perfusion time

B-BLOCKERS Adverse

Increased EDV increased Ejection timeWithdrawal effects Interact with calcium channel blockers

which act on the heart or P450 inducers/inhibitors

UsesMyocardial InfarctionChronic prophylaxis of exertional angina

(not effective in variant angina)

CA-CHANNEL BLOCKERS Nifedipine & Nimodipine

selectivity for vessels only Diltiazem & Verapamil

selectivity for heart and vessels MoA:

Decrease O2 demand by decreasing afterload, contractility, and heart rate

Increase O2 delivery by relieving coronary spasm

Diltiazem and verapamil: decrease automaticity

vasodilation

CA-CHANNEL BLOCKERS Adverse

HA and dizziness Flushing and peripheral edema Profound hypotension (coronary steal phenomenon

with nifidepine!), tachycardia Verapamil = constipation & gingival hyperplasia Adverse effects with B-blockers

Uses Good for exertional angina by decreasing O2

demand Variant angina because they increase myocardial

O2 supply Hypertension DOC for Raynaud’s Phenomenon

VARIANT ANGINA Aka prinzmetal or vasospastic angina is

due to large vessel spasmOccurs regularly or certain times of the day

and there is pain at rest

COMBINATION THERAPY B-blockers and nitrates work because B-

blockers can prevent reflex tachycardia and increased tachycardia while the nitrates prevent increased EDV and ejection time

Nitrates and Ca-channel blockers work because of similar reasoning

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