Indications
Hypertension (alone or with other agents) (immediaterelease
only). Symptomatic benign prostatic hyperplasia
(BPH).
Action
Dilates both arteries and veins by blocking postsynaptic
alpha1-adrenergic receptors. Therapeutic Effects:
Lowering of BP. Increased urine flow and decreased
symptoms of BPH.
Pharmacokinetics
Absorption: Well absorbed following oral administration.
Distribution: Probably enters breast milk; rest of
distribution unknown.
Protein Binding: 98–99%.
Metabolism and Excretion: Extensively metabolized
by the liver.
Half-life: 22 hr.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
PO† 1–2 hr 2–6 hr 24 hr
PO-XL‡ 5 wk unknown unknown
† Antihypertensive effect.
‡ Improved urinary flow and BPH symptoms.
Contraindications/Precautions
Contraindicated in: Hypersensitivity.
Use Cautiously in: Hepatic dysfunction; Gastrointestinal
narrowing (XL only); Geri: Appears on Beers
list. Geriatric patients are atqrisk for hypotension; OB,
Lactation, Pedi: Safety not established; Patients undergoing
cataract surgery (qrisk of intraoperative floppy
iris syndrome).
Adverse Reactions/Side Effects
CNS: dizziness, headache, depression, drowsiness, fatigue,
nervousness, weakness . EENT: abnormal vision,
blurred vision, conjunctivitis, epistaxis, intraoperative floppy iris syndrome. Resp: dyspnea. CV:
first-dose orthostatic hypotension, arrhythmias, chest
pain, edema, palpitations. GI: abdominal discomfort,
constipation, diarrhea, dry mouth, flatulence, nausea,
vomiting. GU:plibido, priapism, sexual dysfunction.
Derm: flushing, rash, urticaria. MS: arthralgia, arthritis,
gout, myalgia.
Interactions
Drug-Drug:qrisk of hypotension with sildenafil,
tadalafil, vardenafil, other antihypertensives, nitrates,
or acute ingestion of alcohol. NSAIDs, sympathomimetics,
or estrogens maypeffects of antihypertensive
therapy.
Route/Dosage
Hypertension
PO (Adults): —1 mg once daily, may be graduallyq
at 2-wk intervals to 2–16 mg/day; incidence of postural
hypotension greatlyqat doses 4 mg/day. BPH—1 mg
once daily, may be gradually increased to 8 mg/day.
Benign Prostatic Hyperplasia
PO (Adults): Immediate release—1 mg once daily,
may beqevery 1–2 wk up to 8 mg/day; Extended release—
4 mg once daily (with breakfast), may beqin
3–4 wk to 8 mg/day.
Availability (generic available)
Tablets: 1 mg, 2 mg, 4 mg, 8 mg. Cost: Generic—1
mg $60.00/100, 2 mg $79.89/100, 4 mg $85.34/100, 8
mg $60.41/100. Extended-release tablets: 4 mg, 8
mg. Cost: 4 mg $84.62/30, 8 mg $88.90/30.
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