Pronunciation: dox-AZ-oh-sin MES-i-late
Class: Alpha-1 adrenergic blocker
- Tablets 1 mg
- Tablets 2 mg
- Tablets 4 mg
- Tablets 8 mg
- Tablets, extended-release 4 mg
- Tablets, extended-release 8 mg
Selectively blocks postsynaptic alpha-1 adrenergic receptors, resulting in dilation of arterioles and veins.
AbsorptionExtended-release (ER) tablets
Relative bioavailability of 4 and 8 mg dose is 54% and 59%, respectively, compared with immediate-release (IR) product. C max for 4 and 8 mg dose is 10.1 and 25.8 ng/mL, respectively. T max for 4 and 8 mg dose is 8 and 9 h, respectively. Food increases C max and AUC approximately 32% and 18%, respectively.IR tablets
T max is 2 to 3 h. Bioavailability is approximately 65%. Enterohepatic recycling. Food decreases C max 18% and AUC 12%.
Approximately 98% bound to plasma proteins (IR and ER).
First-pass metabolism; extensively metabolized by O-demethylation or hydroxylation to several active metabolites.
The t ½ is approximately 22 h.Feces
63% of dose; 4.8% as unchanged drug.Urine
9% of dose; trace amount as unchanged drug.
Elimination is biphasic.ER
Apparent elimination t ½ is 15 to 19 h.
Special PopulationsHepatic Function Impairment
40% increase in exposure.
Indications and Usage
Treatment of benign prostatic hyperplasia (BPH); treatment of hypertension, alone or in combination with other agents (IR only).
Hypersensitivity to doxazosin, prazosin, or terazosin.
Dosage and AdministrationBPH
4 mg once daily with breakfast. Dose may be increased to 8 mg after 3 to 4 wk (max, 8 mg once daily). If treatment is stopped for several days, restart therapy at 4 mg once daily.IR Initial dose
Increase to 2 mg, and thereafter to 4 and 8 mg every day, which is the max dose for BPH. Recommended titration interval is 1 to 2 wk.Hypertension
1 mg every day.Maintenance
Based on standing BP response, may increase to 2 mg and thereafter to 4, 8, and 16 mg.
- Patients should swallow ER tablets whole and not chew, divide, cut, or crush them.
- Administer ER tablets with breakfast.
Store at 59° to 86°F.
10% increase in mean AUC of doxazosin.Tadalafil, vardenafil
BP-lowering effect of doxazosin may be increased. Alpha-1 adrenergic blockers (including doxazosin) are contraindicated in patients receiving tadalafil or vardenafil.
Laboratory Test Interactions
None well documented.
Hypotension, palpitation, postural hypotension (2%); arrhythmia (1%); palpitations, peripheral ischemia, syncope, tachycardia (less than 1%); bradycardia, cerebral vascular accidents, MI (postmarketing).
Dizziness (19%); headache (16%); fatigue/malaise (12%); asthenia (7%); somnolence (5%); vertigo (4%); nervousness (2%); anxiety, ataxia, depression, hypertonia, insomnia, kinetic disorder, paresthesia (1%); agitation, anorexia, hypesthesia (postmarketing).
Increased sweating, pruritus, rash (1%); alopecia, urticaria (postmarketing).
Rhinitis (3%); abnormal vision (2%); conjunctivitis/eye pain, epistaxis, tinnitus (1%); blurred vision, floppy iris syndrome (postmarketing).
Nausea (3%); abdominal pain, diarrhea, dry mouth, dyspepsia (2%); constipation, flatulence (1%); GI irritation and bleeding, vomiting (postmarketing).
Polyuria, sexual dysfunction (2%); impotence, urinary incontinence, UTI (1%); gynecomastia, hematuria, micturition disorder, micturition frequency, nocturia, priapism (postmarketing).
Leukopenia, purpura, thrombocytopenia (postmarketing).
Abnormal LFTs, cholestatic hepatitis, hepatitis, jaundice (postmarketing).
Back pain (3%); arthralgia/arthritis, muscle cramps, muscle weakness, myalgia (1%).
Respiratory tract infection (5%); dyspnea (3%); respiratory disorder (1%); aggravated bronchospasm (postmarketing).
Chest pain, pain (2%); face edema, flushing, influenza-like symptoms (1%); allergic reaction, hot flashes (postmarketing).
Monitor BP and pulse. Assess changes in urinary symptoms, such as dribbling, frequency, hesitancy, nocturia, volume, weak stream.
Category C .
Safety and efficacy not established.
Use of ER tablets in severe hepatic function impairment is not recommended.
Intraoperative floppy iris syndrome has occurred during cataract surgery in patients on or previously treated with alpha-1 blockers.
Marked hypotension (especially orthostatic) and syncope may occur 2 to 6 h after the first few doses, after reintroduction with rapid increase in dosing, or after addition of another antihypertensive.
Administer ER product with caution in patients with preexisting severe GI narrowing. Obstructive symptoms have occurred in patients with known strictures in association with ingestion of nondeformable ER formulations.
Mean WBC and neutrophil counts decreased 2.4% and 1%, respectively. No patients became symptomatic as a result of the low WBC or neutrophil count.
Slight decrease in total serum cholesterol and LDL may occur as well as increase in HDL.
Occurs rarely; may lead to permanent impotence if not promptly treated.
Rule out before starting therapy.
- Advise patient to take prescribed dose every day, morning or evening, without regard to meals but to take with food if stomach upset occurs.
- Advise patient that medication will be started at a low dose and then gradually increased as tolerated until max benefit is obtained.
- Inform patient to swallow the ER formulation whole and not to chew, divide, cut, or crush tablets.
- Instruct patient to take the ER formulation with breakfast.
- Caution patient not to change the dose or stop taking unless advised by health care provider.
- Inform hypertensive patient that drug controls, but does not cure, hypertension and to continue taking drug as prescribed even when BP is not elevated.
- Instruct hypertensive patient to continue taking other BP medications as prescribed by health care provider.
- Emphasize to hypertensive patient importance of the following modalities on BP: weight control, regular exercise, smoking cessation, and moderate intake of alcohol and salt.
- Instruct hypertensive patient in BP and pulse measurement skills.
- Advise hypertensive patient to monitor and record BP and pulse at home and to inform health care provider if abnormal measurements are noted. Also advise patient to take record of BP and pulse to each follow-up visit.
- Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
- Caution patient that drug may cause dizziness or fainting and to avoid driving or performing hazardous tasks for 24 h after the first dose, after a dosage increase, and after interruptions of therapy when treatment is resumed.
- Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
- Advise patient with BPH to contact health care provider if urinary symptoms do not improve or if they worsen while taking this medication.
- Instruct patient to report the following symptoms to health care provider: dizziness, fainting, prolonged or painful erection, other adverse reactions.
Copyright © 2009 Wolters Kluwer Health.
More Doxazosin Mesylate resources
- Doxazosin Mesylate Monograph (AHFS DI)
- Doxazosin Prescribing Information (FDA)
- Cardura Prescribing Information (FDA)
- Cardura Advanced Consumer (Micromedex) - Includes Dosage Information
- Cardura Consumer Overview
- Cardura MedFacts Consumer Leaflet (Wolters Kluwer)
- Cardura XL extended-release tablets MedFacts Consumer Leaflet (Wolters Kluwer)
- Cardura XL Prescribing Information (FDA)