Description
Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of prostate enlargement (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic. One of the four metabolites identified (piperazine derivative of terazosin) has antihypertensive activity. Route of Elimination: Approximately 10% of an orally administered dose is excreted as parent drug in the urine and approximately 20% is excreted in the feces. Half Life: 12 hours
- Uses/Sources: Terazosin is indicated for the treatment of symptomatic benign prostatic hyperplasia (BPH). There is a rapid response, with approximately 70% of patients experiencing an increase in urinary flow and improvement in symptoms of BPH when treated with terazosin. The long-term effects of terazosin on the incidence of surgery, acute urinary obstruction or other complications of BPH are yet to be determined. Terazosin tablets are also indicated for the treatment of hypertension. Terazosin tablets can be used alone or in combination with other antihypertensive agents such as diuretics or beta-adrenergic blocking agents.
- Health Effects: Hypotension, palpitations, postural hypotension, syncope, peripheral edema, weight gain, dyspnea, nasal congestion/rhinitis, impotence.
- Symptoms: Asthenia, postural hypotension, dizziness, somnolence, nasal congestion/rhinitis.
- Treatment: Should overdosage of Terazosin lead to hypotension, support of the cardiovascular system is of first importance. Restoration of blood pressure and normalization of heart rate may be accomplished by keeping the patient in the supine position. If this measure is inadequate, shock should first be treated with volume expanders. If necessary, vasopressors should then be used and renal function should be monitored and supported as needed. Laboratory data indicate that Terazosin is highly protein bound; therefore, dialysis may not be of benefit. (L1712)
- Route of Exposure: Oral. Essentially completely absorbed in man (90% bioavailability).
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: 259.3mg/kg (parental-intravenous, Mouse) (A308)
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Alpha-1A adrenergic receptor Alpha-1B adrenergic receptor Alpha-1D adrenergic receptor |
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. |
11711348 8736427 1358918 2988814 11752352 10503165 9352700 14767264 9732824 |
Potassium voltage-gated channel subfamily H member 2 Potassium voltage-gated channel subfamily H member 6 Potassium voltage-gated channel subfamily H member 7 |
15098086 |
Terazosin Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Intestinal Neoplasms | 13.18 |
|
Diabetes Mellitus, Experimental | 9.56 |
|
Nerve Degeneration | 7.98 |
|
Intracerebral hemorrhage | 6.79 |
|
Esophageal Neoplasms | 6.76 |
|
Male infertility | 6.74 |
|
Polycystic ovary syndrome | 6.42 |
|
Prostatic Neoplasms | 6.37 |
|
Alzheimer's Disease | 6.21 |
|
Multiple Endocrine Neoplasia, Type IV | 6.17 |
|
Breast carcinoma | 5.94 |
|
Colonic neoplasm | 5.42 |
|
AIDS-related Kaposi sarcoma | 5.31 | |
Ventricular Remodeling | 4.98 |
|
Adenocarcinoma, Clear Cell | 4.97 |
|
Chondrosarcoma, Mesenchymal | 4.86 |
|
Myocardial infarction | 4.86 |
|
Neuroendocrine Tumors | 4.68 |
|
Prostatic Intraepithelial Neoplasia | 4.61 |
|
Rectum cancer | 4.57 |
|