Pharmacology of Doxazosin (Cardura) ; Pharmacokinetics, Mechanism of Action, Uses, Effects

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Doxazosin (brand name: Cardura) is a selective alpha-1 adrenergic receptor antagonist commonly used to treat hypertension and benign prostatic hyperplasia (BPH). Below is an overview of its pharmacology:

Mechanism of Action
Selective Alpha-1 Adrenergic Blockade:

Doxazosin selectively inhibits alpha-1 adrenergic receptors located in the vascular smooth muscle and the smooth muscle of the bladder neck and prostate.

This results in:

Vasodilation: Reduces peripheral vascular resistance and decreases blood pressure.

Smooth Muscle Relaxation in BPH: Improves urinary flow by relaxing the bladder neck and prostate.

Pharmacokinetics
Administration:

Administered orally, often as a once-daily dose due to its long duration of action.

Absorption:

Well-absorbed after oral administration, with peak plasma concentrations achieved within 2–3 hours.

Metabolism:

Metabolized in the liver by cytochrome P450 enzymes (CYP3A4, CYP2D6, CYP2C9).

Excretion:

Excreted primarily in the feces (63%) and urine (9%) as inactive metabolites.

Half-Life:

The elimination half-life is approximately 16–22 hours, allowing for once-daily dosing.

Indications
Hypertension:

Lowers blood pressure by reducing arterial resistance.

Typically used as an adjunct or second-line therapy for resistant hypertension.

Benign Prostatic Hyperplasia (BPH):

Alleviates urinary obstruction and associated symptoms, such as hesitancy, weak stream, and incomplete bladder emptying.

Adverse Effects
Common Side Effects:

Postural Hypotension: Often occurs with the first dose or dose increases ("first-dose effect").

Dizziness and headache.

Fatigue or somnolence.

Palpitations and mild tachycardia.

Gastrointestinal:

Nausea and abdominal pain.

Other Effects:

Nasal congestion due to vasodilation.

Rarely, priapism (prolonged erection).

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