Doxazosin mesylate, a quinazoline compound, selectively inhibits the alpha(1)-subtype of alpha adrenergic receptors, and binds highly to alpha(1A) adrenoceptor. Alpha1 receptor blockade decreases urethral resistance and may relieve symptoms of benign prostatic hyperplasia and increase urine flow. The antihypertensive effect of doxazosin is attributed to a decrease in systemic vascular resistance.
藥動學
Tmax: 8 to 9 hours; Bioavailability, Oral: 54% to 59% of immediate-release; Effect of food: Increases Cmax by 32% and AUC by 18%; Protein binding: 98%; Metabolism -Hepatic: Extensive, CYP3A4 (primary), CYP2D6 and CYP2C19, O-demethylation and hydroxylation. Excretion- Fecal: approximately 63%, 4.8% unchanged; Renal: 9%, trace unchanged; Dialyzable: No (hemodialysis). Elimination Half Life: 15 to 19 hours
禁忌症
Hypersensitivity to quinazolines such as prazosin and terazosin
懷孕分類
C/B in conflict
哺乳分類
Infant risk cannot be ruled out.[MDX]; In animal model, it can be concentrated in milk up to 20 times the serum level.
副作用
Orthostatic hypotension, dizziness, vertigo, and headaches are the most common adverse effects.
劑量和給藥方法
Benign prostatic hyperplasia: initial, 4 mg PO QD with breakfast; may titrate if necessary at 3- to 4-week intervals to 4 to 8 mg PO QD, MAX 8 mg/day
小兒調整劑量
腎功能調整劑量
No dosing adjustments are required in renal failure patients.
肝功能調整劑量
Hepatic impairment (severe, Child-Pugh C): Use not recommended