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Drug nameTerazosin
DescriptionTerazosin is a selective alpha 1 antagonist used for treatment of symptoms of prostate enlargement (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
DrugBankPrimary Accession Number: DB01162
DIN02243749
TypeApproved, Small Molecule
IndicationFor the treatment of symptomatic benign prostatic hyperplasia (BPH) and also for hypertension.
Mechanism of ActionTerazosin selectively and competitively inhibits vascular postsynaptic alpha(1)-adrenergic receptors, resulting in peripheral vasodilation and a reduction of vascular resistance and blood pressure. Unlike the nonselective alph-adrenergic blockers phenoxybenzamine and phentolamine, terazosin does not block presynaptic alpha(2)-receptors and, hence, does not cause reflex activation of norepinephrine release to produce reflex tachycardia.
AbsorptionEssentially completely absorbed in man (90% bioavailability).
ToxicityLD50=259.3mg/kg (i.v. in mice)
Protein Binding90-94%