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Pronunciation |
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(doks
AYE zoe
sin) |
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U.S. Brand
Names |
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Cardura® |
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Generic
Available |
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No |
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Pharmacological Index |
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Alpha1 Blockers |
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Use |
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Treatment of hypertension alone or in conjunction with diuretics, cardiac
glycosides, ACE inhibitors, or calcium antagonists (particularly appropriate for
those with hypertension and other cardiovascular risk factors such as
hypercholesterolemia and diabetes mellitus); treatment of urinary outflow
obstruction and/or obstructive and irritative symptoms associated with benign
prostatic hyperplasia (particularly useful in patients with troublesome symptoms
who are unable or unwilling to undergo invasive procedures, but who require
rapid symptomatic relief) |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to quinazolines (doxazosin, prazosin, terazosin) or any
component |
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Warnings/Precautions |
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Can cause significant orthostatic hypotension and syncope, especially with
first dose. Prostate cancer should be ruled out before starting for BPH. May
need dosage adjustment in severe hepatic dysfunction. Anticipate a similar
effect if therapy is interrupted for a few days, if dosage is rapidly increased,
or if another antihypertensive drug is introduced. |
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Adverse
Reactions |
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>10%: Central nervous system: Dizziness (16% to 19%), headache (10% to
14%)
1% to 10%:
Cardiovascular: Orthostatic hypotension (dose-related; 0.3% up to 10%), edema
(2.7% to 4%), hypotension (1.7%), palpitation (1.2% to 2%), chest pain (1.2% to
2%), arrhythmia (1%), syncope (2%), flushing (1%)
Central nervous system: Fatigue (8% to 12%), somnolence (3% to 5%),
nervousness (2%), pain (2%), vertigo (2%), insomnia (1% to 1.2%), anxiety
(1.1%), paresthesia (1%), movement disorder (1%), ataxia (1%), hypertonia (1%),
depression (1%), weakness (1%)
Dermatologic: Rash (1%), pruritus (1%)
Endocrine & metabolic: Sexual dysfunction (2%)
Gastrointestinal: Abdominal pain (2.4%), diarrhea (2% to 2.3%), dyspepsia (1%
to 1.7%), nausea (1.5% to 3%) xerostomia (1.4% to 2%), constipation (1%),
flatulence (1%)
Genitourinary: Urinary tract infection (1.4%), impotence (1.1%), polyuria
(2%), incontinence (1%)
Neuromuscular & skeletal: Back pain (1.8%), arthritis (1%), muscle
weakness (1%), myalgia (1%), muscle cramps (1%)
Ocular: Abnormal vision (1.4% to 2%), conjunctivitis (1%)
Otic: Tinnitus (1%)
Respiratory: Rhinitis (3%), dyspnea (1% to 2.6%), respiratory disorder
(1.1%), epistaxis (1%)
Miscellaneous: Flu-like syndrome (1.1%), increased sweating (1.1%)
<1% (Limited to important or life-threatening symptoms): Tachycardia,
bradycardia, peripheral ischemia, syncope, hypoesthesia, increased sweating,
agitation, weight gain, angina, myocardial infarction, stroke, pallor, thirst,
gout, hypokalemia, lymphadenopathy, purpura, breast pain, alopecia, dry skin,
eczema, paresis, twitching, confusion, migraine, impaired concentration,
paranoia, amnesia, emotional lability, abnormal thinking, depersonalization,
parosmia, earache, taste perversion, photophobia, abnormal lacrimation,
increased appetite, anorexia, fecal incontinence, gastroenteritis, bronchospasm,
sinusitis, coughing, pharyngitis, renal calculus, hot flashes, infection, fever,
rigors, weight loss
Case reports: Leukopenia, cataplexy, enuresis, systemic lupus erythematosus
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Overdosage/Toxicology |
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Symptoms of overdose include severe hypotension, drowsiness, tachycardia
Hypotension usually responds to I.V. fluids, Trendelenburg positioning, or
parenteral vasoconstrictor; treatment is primarily supportive and symptomatic.
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Drug
Interactions |
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NSAIDs may reduce antihypertensive efficacy.
ACE inhibitors: Hypotensive effect may be increased.
Beta-blockers: Hypotensive effect may be increased.
Calcium channel blockers: Hypotensive effect may be increased.
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Mechanism of
Action |
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Competitively inhibits postsynaptic alpha-adrenergic receptors which results
in vasodilation of veins and arterioles and a decrease in total peripheral
resistance and blood pressure; approximately 50% as potent on a weight by weight
basis as prazosin |
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Pharmacodynamics/Kinetics |
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Increased age does not significantly affect pharmacokinetics of doxazosin
Duration: >24 hours
Half-life: 22 hours
Time to peak serum concentration: 2-3 hours |
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Usual Dosage |
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Oral:
Hypertension: Maximum dose: 16 mg/day
BPH: Maximum dose: 8 mg/day.
Elderly: Initial: 0.5 mg once daily |
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Monitoring
Parameters |
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Blood pressure, standing and sitting/supine |
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Test
Interactions |
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Increased urinary VMA 17%, norepinephrine metabolite 42% |
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Cardiovascular
Considerations |
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Doxazosin can be used alone or in combination as an antihypertensive.
Patients with BPH may derive an extra benefit from therapy. |
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Mental Health: Effects
on Mental Status |
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Dizziness is common; may cause anxiety, nervousness, or sedation; rarely may
cause depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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Psychotropics may potentiate the hypotensive effects of
doxazosin |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take as directed, at bedtime. Do not skip dose or discontinue without
consulting prescriber. Follow recommended diet and exercise program. Do not use
OTC medications which may affect blood pressure (eg, cough or cold remedies,
diet pills, stay-awake medications) without consulting prescriber. This
medication may cause drowsiness, dizziness, or impaired judgment (use caution
when driving or engaging in tasks that require alertness until response to drug
is known); postural hypotension (use caution when rising from sitting or lying
position or when climbing stairs); or dry mouth or nausea (frequent mouth care
or sucking lozenges may help). Report increased nervousness or depression;
sudden weight gain (weigh yourself in the same clothes at the same time of day
once a week); unusual or persistent swelling of ankles, feet, or extremities;
palpitations or rapid heartbeat; muscle weakness, fatigue, or pain; or other
persistent side effects. Pregnancy/breast-feeding precautions: Inform
prescriber if you are or intend to be pregnant. Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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Syncope may occur usually within 90 minutes of the initial
dose |
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Dosage Forms |
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Tablet: 1 mg, 2 mg, 4 mg, 8 mg |
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References |
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Boston D and Collins C,
"Safety, Efficacy, and Lipid Profile of Doxazosin at a VA Medical Center,"
Hosp Formul, 1995, 30(4):233-6.
Carlson RV, Bailey RR, Begg EJ, et al,
"Pharmacokinetics and Effect on Blood Pressure of Doxazosin in Normal Subjects and Patients With Renal Failure,"
Clin Pharmacol Ther, 1986, 40(5):561-6.
Cubeddu LX, Fuenmayor N, Caplan N, et al,
"Clinical Pharmacology of Doxazosin in Patients With Essential Hypertension,"
Clin Pharmacol Ther, 1987, 41(4):439-49.
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