drugs affecting the vasculature and blood pressure Flashcards
what classes of drugs are used to relax vascular smooth muscle?
- organic nitrates = used to treat angina, as prophylaxsis, pulmonary oedema
- calcium channel blockers = to treat hyertension, stable angina
what is angina?
pain that occurs when the O2 supply to the myocardium is insufficient to meet its metabolic demand
what are the 3 types of angina?
stable, unstable, variant
what causes stable angina?
a fixed narrowing (stenosis) of coronary vessels as a consequence of atherosclerosis
- characterised by predictable pain upon exertion
what causes unstable angina?
- due to platelet-fibrin thrombus in association with an atheromatous plaqur
- characterised by pain to less and less exertion
- danger of MI
what causes variant angina?
- associated with coronary artery spasm
what do organic nitrates do?
- relax all types of smooth muscles
- they act upon vasculature causing:
1. venorelaxation
2. arteriolar dilation
3. increased coronary blood flow
how do organic nitrates effect coronary circulation?
the nitrate dilates collateral and causes the blood flow to the ischaemic myocardium to increase
what are the clinical uses of organic nitrates in angina?
GTN
what does GTN do?
- short acting
- undergoes extensive first-pass metabolism
- administered sublingually
what is first pass metabolism?
- drugs that are swallowed are carried from the gut to the liver by the portal circulation
- they undergo variable metabolism by the liver before reaching the systemic circulation
- some drugs (GTN) are almost completely inactivated by the liver
what are the adverse effects of organic nitrates?
- headaches
- hypotension and fainting
- reflex tachycardia
- formation of mathaemoglobin
how are organic nitrates tolerated?
- repeat administration of organic nitrates may be associated with a diminished effect
what are they 3 main types of calcium channel blockers?
- verapamil
- amlodipine
- diltiazem
how do calcium blockers help hypertension?
- reduced Ca+ entry int vascular smooth muscle cells causes generalised arteriolar dilation, reducing TPR and MABP. the major effect is on the arteries
- drugs with selectivity for smooth muscle L-type channels are preferred to minimise unwanted effects upon cardiac muscle
- Ca+ channel blockers cause coronary vasodilation and are useful in angina and hypertension at the same time