Drug Treatment for Cardiovascular Disease Flashcards
b receptors molecular action
Gs-protein dependent activation of AC –> increases cAMP –> activates pKA –> increases/decreases intracellular calcium –> increases contractility of cardiac muscle and decreases the contractility of arterial smooth muscle and bronchial smooth muscle
examples of beta blocker drug and their indications
propnol- non selective beta blocker- effective for angina, HTN, arrhthymias, migraine, tremor
bisoprolol-commonly in the UK- selective b1 blocker
heart: decreases force and rate of contraction-> reduces BP
lungs: bronchoconstriction
arterioles: decreases blood supply to muscles, skin, penis
side effects of beta blockers
heart: fatigue, bradycardia
lungs: breathlessness, exacerbations of asthma
arterioles: fatigue, claudication, cold hands/feet, erectile dysfunction
contraindication of beta blockers
hypoglycaemia and beta blockers
- low blood glucose activates Adr release (mobilises glucose from the liver-gluconeogenesis)
- causes tremor, palpitations, sweat
- symptoms blocked by beta blockers
- patients need to be able to recognise hypoglycaemia
- beta blockers contraindicated in diabetic pts with recurrent hypoglycaemia
Mechanism of action of thiazide diuretics
BENDROFLUMETHIAZIDE-blocks Na+/Cl- symporter on the lumenal side of the epithelial cells
-inhibits reabsorption of Na and Cl and increases excretion of Na+/Cl- and water which lowers BP
INDAPAMIDE-arterioles (K-ATP): decreases BP
side effects of thiazides
kidney: hyponatraemia, hypokalaemia, alkalosis, hypercalcaemia, hypermagnesaemia, increase in urate
insulin resistance: increase in glucose (diabetes)
liver: increase in lipids (arterial disease)
other indications of thiazide diuretics
oedema, UT stones, nephrogenic diabetes insipidus
core thiazide drug
bendroflumethiazide
alpha blockers mechanism of action
a1 receptors acts via the Gq protein to increase IPA levels and further release of Ca2+ from the sarcoplasmic reticulum
a-blocker drug
doxazosin- decreases Ca2+ release in arteriolar smooth muscle
other indications of a-blockers
prostatic hypertrophy to relax bladder outflow sphincter
side effects of alpha blockers
palpitations (reflex tachycardia), postural hypotension
calcium channel blocker mechanism of action
- blocks the L-type voltage gates Ca2+ channel
- decreases intracellular Ca2+
- arterioles: smooth muscle relaxation
- heart: decreased force of contraction
- SA and AV node: decreased heart rate
other indications of calcium channel blocker
Raynaud’s syndrome, angina, arrhythmias
core calcium channel blockers
amlodipine, ditiazem, verapamil