Terazosin (terazosin HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Terazosin hydrochloride is a alpha1-adrenergic blocking agent.
Terazosin hydrochloride is a quinazoline-derivative postsynaptic alpha1-adrenergic blocking agent. The drug is chemically and pharmacologically related to prazosin and doxazosin. On a molar basis, the postsynaptic alpha1-adrenergic receptor affinity of terazosin is one-third that of prazosin when tested in rat liver, and the alpha1-receptor selectivity is 4 times that of doxazosin when tested in human prostate adenoma.
Terazosin reduces peripheral vascular resistance and blood pressure as a result of its vasodilating effects; the drug produces both arterial and venous dilation. Terazosin reduces blood pressure in both supine and standing patients; the effect is most pronounced on standing blood pressure, and postural hypotension can occur. Terazosin generally causes no change in heart rate or cardiac output in the supine position.
Cardiovascular responses to exercise (e.g., increased heart rate and cardiac output) are maintained during terazosin therapy.
Effects of terazosin on the cardiovascular system are mediated by the drug's activity at alpha1-receptor sites in vascular smooth muscle. alpha1-Adrenergic receptors also are located in nonvascular smooth muscle (e.g., bladder trigone and sphincters, GI tract and sphincters, prostate adenoma and capsule, ureters, uterus) and in nonmuscular tissues (e.g., CNS, liver, kidneys). Because of the prevalence of alpha-receptors in the prostate capsule, prostate adenoma, and the bladder trigone and the relative absence of these receptors on the bladder body, alpha-blockers decrease urinary outflow resistance in men.
Terazosin may improve to a limited extent the serum lipid profile (e.g., small increases in high-density lipoprotein cholesterol concentrations (HDL)/total cholesterol ratio, small decreases in low-density lipoprotein (LDL) cholesterol, total cholesterol, and triglyceride concentrations). In addition, such potential effects of terazosin may counteract the negative effects of thiazide diuretics on serum lipoprotein concentrations.
SumMon(R)(see Users Guide). For additional information on this drug until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the labeling be consulted for information on the usual cautions, precautions, and contraindications concerning potential drug interactions and/or laboratory test interferences and for information on acute toxicity.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Terazosin belongs to a class of drugs known as alpha blockers.
It works by relaxing blood vessels so blood can flow more easily. Terazosin is also used in men to treat the symptoms of an enlarged prostate (benign prostatic hyperplasia-BPH). It does not shrink the prostate, but it works by relaxing the muscles in the prostate and part of the bladder.
This helps to relieve symptoms of BPH such as difficulty in beginning the flow of urine, weak stream, and the need to urinate often or urgently (including during the middle of the night).
Generic name: terazosin HCl
Pronunciation: (ter-AY-zoe-sin)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Terazosin
Indications
The following indications are listed for Terazosin:
- Benign Prostatic Hyperplasia With Lower Urinary Tract Symptom
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Symptomatic Benign Prostatic Hyperplasia, Symptomatic Benign Prostatic Hypertrophy, Symptomatic Bph, Symptomatic Prostatic Hypertrophy, Systemic Arterial Hypertension.
Dosing
Dosage of terazosin hydrochloride is expressed in terms of terazosin and must be individualized according to the patient's response and tolerance.
While the manufacturer makes no specific recommendations for titration of terazosin dosage in geriatric patients, patients in this age group generally are less tolerant of the postural hypotensive effects of alpha1-adrenergic blocking agents because of impaired cardiovascular reflexes, and caution should be exercised. Therefore, dosage escalation in elderly patients generally should be slower than in younger adults. In addition, the elimination half-life may be prolonged and plasma clearance of the drug decreased in patients 70 years of age and older.
Clinically important alterations in the pharmacokinetics of terazosin in patients with impaired renal function have not been observed to date, and modification of dosage in such patients generally does not appear to be necessary. In addition, administration of supplemental doses of the drug following hemodialysis does not appear to be necessary.
The effects, if any, of hepatic impairment on the pharmacokinetics of terazosin have not been elucidated, and the manufacturer makes no specific recommendations for modification of terazosin dosage in patients with hepatic impairment.
Terazosin hydrochloride is administered orally. Food has little, if any, effect on the extent of absorption of terazosin but may delay achievement of peak plasma concentrations by about 1 hour.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
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There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
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There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
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There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Terazosin was not teratogenic in rats or rabbits at oral dosages up to 1330 or 165 times the maximum recommended human dosage, respectively. Fetal resorptions occurred in rats at an oral dosage of 480 mg/kg daily, which is approximately 1330 times the maximum recommended human dosage. Increased fetal resorptions, decreased fetal weight, and increased supernumerary ribs were observed in offspring of rabbits that received 165 times the maximum recommended human dosage. These fetal findings were most likely secondary to maternal toxicity. There are no adequate and controlled studies in pregnant women, and safety of terazosin during pregnancy has not been established. The drug should be used during pregnancy only when potential benefits justify the possible risks to the mother and fetus.
In a perinatal and postnatal development study in rats, there was an increased frequency of deaths in the offspring during the first 3 weeks postpartum at a maternal oral terazosin dosage of 120 mg/kg daily (more than 300 times the maximum recommended human dosage).
Since it is not known whether terazosin is distributed into milk, the drug should be used with caution in nursing women.
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ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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