Terazosin

387.43

387.43

613-265-8

DTXSID3023639

G04CA03|G - Genito urinary system and sex hormones

103

1

white to off-white powder

1.332 g/cm3

273 °C

664.5ºC at 760 mmHg

355.7ºC

H2O: 29.7mg/mL

-20°C Freezer

NONH for all modes of transport

3

22-36/37/38

26-36

TK8044925

Xn,Xi

P264, P270, P301+P312, P330, P501

H302

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 42 companies from 2 notifications to the ECHA C&L Inventory.

In the event of an overdose, patients may experience hypotension. Blood pressure and heart rate should be controlled by having the patient lie down or by treating with volume expanders or if necessary vasopressors. Patients should be monitored for renal function. Because terazosin is highly protein bound, dialysis is unlikely to provide benefit to overdosing patients. The oral LD50 in mice is 5500mg/kg[MSDS].

Terazosin has been associated with a low rate of serum aminotransferase elevations that in controlled trials was no higher than with placebo therapy. These elevations were transient and did not require dose modification. Instances of serum enzyme elevations, but no instances of clinically apparent acute liver injury with jaundice due to terazosin, have been published. Furthermore, product labels do not include discussion of hepatic toxicity. Cholestatic hepatitis and jaundice have been reported with other alpha-adrenergic blockers. Thus, acute symptomatic liver injury due to terazosin must be exceedingly rare if it occurs at all.

90-94%.

Terazosin is indicated for use in treating symptomatic benign prostatic hyperplasia and hypertension.|FDA Label

Terazosin is a nonselective alpha-1 adrenergic antagonist used in the therapy of hypertension and benign prostatic hypertrophy. Terazosin therapy is associated with a low rate of transient serum aminotransferase elevations and to rare instances of clinically apparent acute liver injury.

Antihypertensive Agents

Terazosin is a quinazoline derivative alpha-1-selective adrenergic blocker.

Drugs used in the treatment of urogenital conditions and diseases such as URINARY INCONTINENCE; PROSTATIC HYPERPLASIA; and ERECTILE DYSFUNCTION. (See all compounds classified as Urological Agents.)|Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS. (See all compounds classified as Adrenergic alpha-1 Receptor Antagonists.)

Approximately 90%.|Approximately 10% of the oral dose is excreted unchanged in the urine and approximately 20% is excreted in the feces. 40% of the total dose is eliminated in urine and 60% of the total dose is eliminated in the feces.|25L to 30L.|Plasma clearance is 80mL/min and renal clearance is 10mL/min.

The majority of terazosin is hepatically metabolized. The metabolites recovered include 6-O-demethyl terazosin, 7-O-methyl terazosin, a piperozine derivative, and a diamine derivative.

Terazosin has a mean half life 12 hours though this can be as high as 14 hours in patients over 70 years and as low as 11.4 hours in patients 20 to 39 years old.

Terazosin is selective for alpha-1-adrenoceptors but not their individual subtypes. Inhibition of these alpha-1-adrenoceptors results in relaxation of smooth muscle in blood vessels and the prostate, lowering blood pressure and improving urinary flow. Smooth muscle cells accounts for roughly 40% of the volume of the prostate and so their relaxation reduces pressure on the urethra. It has also been shown that catecholamines induce factors responsible for mitogenesis and alpha-1-adrenergic receptor blockers inhibit this effect. A final long term mechanism of terazosin and other alpha-1-adrenergic receptor blockers is the induction of apoptosis of prostate cells. Treatment with terazosin enhances the expression of transforming growth factor beta-1 (TGF-beta1), which upregulates p27kip1, and the caspase cascade.

A 45975

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals