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Pronunciation |
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(ter
AY zoe
sin) |
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U.S. Brand
Names |
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Hytrin® |
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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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Management of mild to moderate hypertension; alone or in combination with
other agents such as diuretics or beta-blockers; benign prostate
hypertrophy |
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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.
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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Asthenia, postural hypotension, dizziness, somnolence, nasal
congestion/rhinitis, and impotence were the only events noted in clinical trials
to occur at a frequency significantly greater than placebo (p<0.05).
1% to 10%:
Cardiovascular: Edema, palpitations, chest pain, peripheral edema (3%),
orthostatic hypotension (2.7% to 3.9%), tachycardia
Central nervous system: Fatigue, nervousness, drowsiness
Gastrointestinal: Dry mouth
Genitourinary: Urinary incontinence
Ocular: Blurred vision
Respiratory: Dyspnea, nasal congestion
<1% (Limited to important or life-threatening symptoms): Sexual
dysfunction, priapism, syncope (0.8%) |
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Overdosage/Toxicology |
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Symptoms of overdose include hypotension, drowsiness, shock (but very
unusual)
Hypotension usually responds to I.V. fluids or Trendelenburg positioning; if
unresponsive to these measures, the use of a parenteral vasoconstrictor may be
required; 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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Alpha1-specific blocking agent with minimal alpha2
effects; this allows peripheral postsynaptic blockade, with the resultant
decrease in arterial tone, while preserving the negative feedback loop which is
mediated by the peripheral presynaptic alpha2-receptors; terazosin
relaxes the smooth muscle of the bladder neck, thus reducing bladder outlet
obstruction |
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Pharmacodynamics/Kinetics |
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Onset of effect: 1-2 hours
Absorption: Oral: Rapid
Protein binding: 90% to 95%
Metabolism: Extensively in the liver
Half-life: 9.2-12 hours
Time to peak serum concentration: Within 1 hour
Elimination: Principally in feces (60%) and in urine (40%)
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Usual Dosage |
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Adults: Oral:
Dosage reduction may be needed when adding a diuretic or other
antihypertensive agent; if drug is discontinued for greater than several days,
consider beginning with initial dose and retitrate as needed; dosage may be
given on a twice daily regimen if response is diminished at 24 hours and
hypotensive is observed at 2-4 hours following a dose
Benign prostatic hypertrophy: Initial: 1 mg at bedtime, increasing as needed;
most patients require 10 mg day; if no response after 4-6 weeks of 10 mg/day,
may increase to 20 mg/day |
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Dietary
Considerations |
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May be administered without regard to meals at the same time each
day |
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Monitoring
Parameters |
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Standing and sitting/supine blood pressure, especially following the initial
dose at 2-4 hours following the dose and thereafter at the trough point to
ensure adequate control throughout the dosing interval; urinary
symptoms |
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Cardiovascular
Considerations |
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Terazosin 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 drowsiness or nervousness; may rarely cause
insomnia or depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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None reported |
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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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Up to 10% of patients could experience dry mouth |
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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
alcohol or OTC medications which may affect blood pressure (eg, cough or cold
remedies, diet pills, "stay-awake" medications) without consulting physician.
You may experience 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); dry mouth or nausea (frequent mouth care or
sucking lozenges may help); urinary incontinence (void before taking
medication); or sexual dysfunction (reversible, may resolve with continued use).
Report altered CNS status (eg, fatigue, lethargy, confusion, nervousness);
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; difficulty breathing; muscle weakness; 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; administer
initial dose at bedtime
Monitor blood pressure, standing and sitting/supine |
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Dosage Forms |
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Capsule: 1 mg, 2 mg, 5 mg, 10 mg
Tablet: 1 mg, 2 mg, 5 mg, 10 mg |
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References |
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Alver JE, Mooppan UM, Kester RR, et al,
"The Effects of the Alpha 1-Adrenergic Antagonists Terazosin and Phentolamine on Prostastatic Adenoma and Urethra In Vitro,"
Proc West Pharmacol Soc, 1989, 32:317-25.
Appell RA,
"Pathogenesis and Medical Management of Benign Prostatic Hyperplasia," Semin
Nephrol, 1994, 14(6):531-43.
Kim J, Gazarian M, Verjee Z, et al,
"Acute Renal Insufficiency in Ibuprofen Overdose," Pediatr Emerg Care,
1995, 11(2):107-8.
Lowe FC,
"Safety Assessment of Terazosin in the Treatment of Patients With Symptomatic Benign Prostatic Hyperplasia: A Combined Analysis,"
Urology, 1994, 44(1):46-51.
Luther RR,
"Terazosin: A New Antihypertensive Agent With Favorable Effects on Lipids,"
Int J Clin Pharmacol Ther Toxicol, 1989, 27(7):313-9.
Petrovich Z, Ameye F, Baert L, et al,
"New Trends in the Treatment of Benign Prostatic Hyperplasia and Carcinoma of the Prostate,"
Am J Clin Oncol, 1993, 16(3):187-200.
Sonders RC, "Pharmacokinetics of Terazosin," Am J Med, 1986, 80(Suppl
5B):20-4.
Titmarsh S and Monk JP,
"Terazosin: A Review of Its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Efficacy in Essential Hypertension,"
Drugs, 1987, 33(5):461-77. |
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