| Indication | For treatment and management of mild to moderate hypertension and urinary obstruction symptoms caused by BPH. |
| Pharmacodynamics | Doxazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Doxazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Doxazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that Doxazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Doxazosin results from a decrease in systemic vascular resistance and the parent compound Doxazosin is primarily responsible for the antihypertensive activity. |
| Mechanism of action | Doxazosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation. |
| Absorption | 65% |
| Volume of distribution | Not Available |
| Protein binding | 98% |
| Metabolism | Hepatic. |
| Route of elimination | On average only 4.8% of the dose was excreted as unchanged drug in the feces and only a trace of the total radioactivity in the urine was attributed to unchanged drug. |
| Half life | 22 hours |
| Clearance | Not Available |
| Toxicity | Symptoms of overdose include hypotension. Oral LD50 is greater than 1000 mg/kg in mice and rats. |