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Alpha BLockers
Question | Answer |
---|---|
Alpha 1 receptors | Vasoconstriction Decreased motility and tone of GI tract Increased renin secretion Gluconeogensis in the liver |
Alpha 2 receptos | Vasoconstriction |
Alpha – Blockers | Alpha -1 blockers Centrally acting alpha – 2 blockers Peripherally acting alpha – 2 blockers |
Alpha – 1 Blockers – Mechanism of Action | Blockage of receptors causes: Dilatation of arterioles and veins Relaxation of smooth muscle in prostate and bladder neck |
Centrally Acting Alpha – 2 Blockers Mechanism of Action | Stimulation of inhibitory alpha receptors in the CNS Leading to: Decreased peripheral vascular resistance Decreased HR Decreased renal vascular resistance |
Peripherally Acting Alpha – 2 Blockers Mechanism of Action | Inhibit the release of norepinephrine from peripheral nerves Vasodilatation |
Alpha – Blockers – Kinetics | Variable bioavailability Most are highly protein bound Alpha – 1 blockers are hepatically metabolized and excreted in bile |
Alpha – Blockers – Adverse Effects | Marked hypotension Especially with first few doses Alpha – 1 blockers Urinary frequency Dry mouth Constipation Headache CNS depression Drowsiness Hallucinations Reserpine |
Alpha – Blockers – Drug Interactions | Increased levels of alpha – blockers by: Alcohol, beta – blockers, cimetidine, verapamil Increased effects of levodopa by methyldopa |
Alpha – Blockers – Cautions | Additive hypotensive effects Rebound hypertension with abrupt withdrawal of clonidine Avoid driving or operating machinery until effects known Warn patient of the possibility of syncope |
Alpha – Blockers - Names | Alpha - 1 blockers Prazosin (Minipress) Terazosin (Hytrin) Doxazosin (Cardura) Alfuzosin (Uroxatral) Tamsulosin (Flomax) Peripherally active alpha – 2 Guanadrel (Hylorel) Reserpine |
Alpha – Blockers – Names | Centrally active alpha – 2 Clonidine (Catapres) Guanabenz (Wytensin) Guanfacine (Tenex) Methyldopa (Aldomet) |
Direct Vasodilators – Mechanism of Action | Relaxation of arteriolar smooth muscle leading to decreased peripheral vascular resistance Causes reflex increase in HR and renin release |
Direct Vasodilators – Kinetics | High first pass effect Liver metabolism Renal excretion |
Direct Vasodilators – Adverse Effects | Tachycardia Headache Constipation Nausea / vomiting Dizziness Angina Minoxidil Hair growth Minoxidil |
Direct Vasodilators | Drug interactions Increased levels of hydralazine by Beta – blockers and indomethacin Names Hydralzine (Apresoline) IV and PO Minoxidil (Loniten |