Lecture 11 - Alpha blockers and calcium channel blockers Flashcards
What is the mechanism of action for alpha blockers?
These drugs block the effects of sympathetic nerves on blood vessels by binding to alpha-adrenoreceptors located on vascular smooth muscle. Basically these drugs stop the contraction of smooth muscle on the blood vessels, hence causing dilation (not contraction which normally happens).
List alpha blockers?
- Doxazosin.
- Proazosin.
- Terazosin.
- Phenoxybenzamine.
- Phentolamine.
- Labetalol.
- Carvedilol.
- Tamsulosin.
What are alpha blockers used for?
- Hypertension.
- Vasoconstriction.
- Raynaud’s disease.
- Pheochromocytoma.
- Erectile dysfunction.
Describe doxazosin?
Selective oral reversible alpha-1 blocker that acts on post-sympathetic receptors. It is mainly a vasodilator.
What is doxazosin used for?
- Hypertension.
2. Benign prostatic hyperplasia.
Why do patients not take doxazosin?
- History of postural hypotension.
- Pulmonary oedema due to aortic or mitral stenosis.
- Heart failure.
What are the adverse effects of doxazosin?
- Dry mouth.
- GI disturbances.
- Hypotension.
- Oedema.
- Syncope.
- Tachycardia.
- SOB.
- Drowsiness.
- Sleep disturbances.
- Headache.
- Lassitude - mental or physical weariness.
- Nasal stuffiness.
- Urinary incontinence in women.
Describe phenoxybenzamine?
Non-selective oral irreversible alpha blocker that is a H1, ACh, 5HT antagonist as well.
What is phenoxybenzamine used for?
- Phaeochromocytoma.
2. Hypertension.
Why do patients not take phenoxybenzamine?
They do not take if they have the following:
- History of cerebrovascular accident.
- Conditions where sudden drop in BP is undesirable (e.g. stroke or MI).
- Congestive heart failure.
- Severe ischaemic heart disease.
- Cerebrovascular disease.
- Renal impairment.
What are the adverse effects of phenoxybenzamine?
- Postural hypotension.
- Dizziness.
- Compensatory tachycardia.
- Lassitude.
- Nasal congestion.
- Miosis.
- Impotence - inhibition to ejaculate.
Describe phentolamine?
It is an intravenous alpha blocker that cannot be absorbed orally. It is a competitive antagonist for both alpha receptors (causes an increase in NE release) and it is also a: 5Ht, muscarinic H1 and H2 antagonist.
What is phentolamine used for?
Hypertensive episodes due to pheochromocytoma.
Why do patients not take phentolamine?
They do not take if they have the following:
- Hypotension.
- History of MI.
- Coronary insufficiency.
- Angina.
- Coronary artery disease.
What are the adverse effects of phentolamine?
- Postural hypotension.
- Tachycardia.
- Dizziness.
- Flushing.
- Nausea.
- Vomiting.
- Diarrhoea.
- Nasal congestion.
- Angina.
- Chest pain.
Describe labetalol?
It is both an alpha and beta blocker.
What is labetalol used for?
- Hypertension (even in pregnancy).
2. Angina following acute MI.