Terazosin_Hydrochloride: profile and news






Drug Makers Cleared on Delaying Generic  Apr 21, 2006
...in which Geneva -- now Sandoz Inc., a subsidiary of Novartis AG -- delayed marketing its generic version of Abbott's terazosin hydrochloride drug, Hytrin. ... - Texas Lawyer (subscription),


Other information


Indication
For the treatment of symptomatic benign prostatic hyperplasia (BPH) and also for hypertension.

Pharmacology
Terazosin, classified as a quinazoline, is similar to doxazosin and prazosin. As an alpha-adrenergic blocking agent, terazosin is used to treat hypertension and benign prostatic hypertrophy (BPH). Terazosin produces vasodilation and reduces peripheral resistance but in general has slight effect on cardiac output. Antihypertensive effect with chronic dosing is usually not accompanied by reflex tachycardia.

Mechanism Of Action
Terazosin selectively and competitively inhibits vascular postsynaptic alpha(1)-adrenergic receptors, resulting in peripheral vasodilation and a reduction of vascular resistance and blood pressure. Unlike the nonselective alph-adrenergic blockers phenoxybenzamine and phentolamine, terazosin does not block presynaptic alpha(2)-receptors and, hence, does not cause reflex activation of norepinephrine release to produce reflex tachycardia.

Drug Category
Antineoplastic Agents; Adrenergic alpha-Antagonists; Platelet Aggregation Inhibitors; ATC:G04CA03

Brand Names/Synonyms
Abbott 45975; Blavin; CHEMBANK1722; Flumarc; Fosfomic; Heitrin; Hytracin; Hytrin; Hytrinex; Itrin; Terazosin; Terazosin Hcl; Terazosin Hydrochloride; Terazosina [Inn-Spanish]; Terazosine; Terazosine [Inn-French]; Terazosinum [Inn-Latin]; Trazosin Hcl; Urodie; Vasocard; Vasomet; Vicard

Dosage Forms
TABLET

Absorption
Essentially completely absorbed in man (90% bioavailability).

Interactions
-->Interactions for Terazosin:

In controlled trials, terazosin has been added to diuretics, and several beta-adrenergic blockers; no unexpected interactions were observed. Terazosin has also been used in patients on a variety of concomitant therapies; while these were not formal interaction studies, no interactions were observed. Terazosin has been used concomitantly in at least 50 patients on the following drugs or drug classes: 1) analgesic/anti-inflammatory (e.g., acetaminophen, aspirin, codeine, ibuprofen, indomethacin); 2) antibiotics (e.g., erythromycin, trimethoprim and sulfamethoxazole); 3) anticholinergic/sympathomimetics (e.g., phenylephrine hydrochloride, phenylpropanolamine hydrochloride, pseudoephedrine hydrochloride); 4) antigout (e.g., allopurinol); 5) antihistamines (e.g., chlorpheniramine); 6) cardiovascular agents (e.g., atenolol, hydrochlorothiazide, methyclothiazide, propranolol); 7) corti-costeroids; 8) gastrointestinal agents (e.g., antacids); 9) hypoglycemics; 10) sedatives and tranquilizers (e.g., diazepam).

Use with Other Drugs

In a study (n=24) where terazosin and verapamil were administered concomitantly, terazosin’s mean AUC0-24 increased 11% after the first verapamil dose and after 3 weeks of verapamil treatment it increased by 24% with associated increases in Cmax (25%) and Cmin (32%) means. Terazosin mean Tmax decreased from 1.3 hours to 0.8 hours after 3 weeks of verapamil treatment. Statistically significant differences were not found in the verapamil level with and without terazosin. In a study (n=6) where terazosin and captopril were administered concomitantly, plasma disposition of captopril was not influenced by concomitant administration of terazosin and terazosin maximum plasma concentrations increased linearly with dose at steady-state after administration of ter-azosin plus captopril.

 


Chemical IUPAC Name
[4-(4-amino-6,7-dimethoxy-quinazolin-2-yl)piperazin-1-yl]-tetrahydrofuran-2-yl-methanone

Chemical Formula
C19H25N5O4

Half Life
12 hours

Drug Type
Approved Drug

# Accession No
APRD00667

CAS Registry Number
63590-64-7


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