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ANTI ANGINA THERAPY

Angina Pectoris : Mismatch between myocardial oxygen supply


and demand.
Symptom: Retrosternal discomfort, pressure like, occurs with exertion, relieved by rest, may radiate down arm or into neck.

Drug Mech of action/ indication Metabolism/ drug Side effect/ contraindication Clinical use
interaction
Organic nitrates: decompose to NO  activate A)Tolerance -Headache, = stable angina
guanylate cyclase, so  =continue exposure to - hypotension, = unstable angina
1)nitorglycerin cGMP, cGMP activate nitrates leads to decrease -transiet of hypotension worsen = MI
2)isosorbide dinitrate protein kinase, lead to  magnitude of with alcohol
= HF
3)isosorbide-5- intracellular Ca. in smooth pharmacological effect.
mononitrate =due to decrease in free – = hypertensive
muscle, reduced
phosphorylation of myosin SH group
light chain, reduced calcium, require nitrate free 24-h
Method of and relaxation.
administration : B) Interaction with
At concentration, nitrates Phosphodiesterase 5
a)sublingual= decrease preload, so reduce inhibitors:
nitoglycerin workload on heart. - sildenafil (viagra)
At  concentration, nitrate -taldalafil (cialis)
b)oral = isosorbide cause vasodilaton of coronary -vardenafil (levitra)
dinitrate A and blood supply to combination of nitrates
myometrium with this drug causes
c)cutaneous = I – angina, MI, heart failure extreme hypotension
transdermal patch

d)IV
-blocker: - block action of NA n -bronchoconstriction (block = angina stable
Adrenaline at beta adrenergic beta 2 mediated smooth muscle = MI
receptor relaxation) = HF
Non selective: -reduce mortaliti and -mask symptom of = arrythmias
1) propanolol, infarction hypoglycemia
2) timolol -reduce myocardial O2 -HF
demand by: -bradycardia
Cardioselective: a) HR -somnolence(induce sleep)
1)Metaprolol b) BP (afterload) -depression
2)Atenolol c) contarctility -impotence

Alpha 1 antagonist xtvt:


1)carvedilol Result =
1-heart ratecontractility
2- contract SM (blood vessel
and bronchi)
1- smooth muscle relaxation
Ca channel blocker - Block L-type calcium Headache, dizziness =arrythmias
channels, so Ca entry, so Flushing = hypertension
Dihydropyridine: intracellular Ca Oedema = chronic stable angina,
1)nifedipine Tachycardia
not used in unstable
2)amlodipine - In SMOOTH muscle = Constipation
=affect vasculature Hypotension angina
vascular smooth muscle
(decrease BP) relaxation
- in HEART = contractility
Non Dihydropyridine;
1)verapramil -can alter ratio of O2
2)diltiazem supply/demand in CHRONIC
=affect heart (decrease STABLE ANGINA:
HR) a) arteriolar Pressure
b) myocardial contractility
c) HR
Gene therapy  new vessel formation
(eg:VGEF)

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