| ATC Code | G04CA02 |
| CAS number | 106133-20-4 |
| PUB number | 129211 |
| Drugbank ID | DB00706 |
| Empirical formula | C20H28N2O5S |
| Molar mass (g·mol−1) | 408,51 |
| Physical state | solid |
| Melting point (°C) | 228–230 |
Tamsulosin is a drug used to treat symptomatic benign prostatic hyperplasia (BPH) and chronic prostatitis, as well as to aid in the passage of kidney stones. Strictly speaking, the drug is an alpha-1A and alpha-1D adrenoreceptor antagonist. Tamsulosin is taken by mouth.
Tamsulosin was approved for medical use in the United States in 1997.
Pharmacodynamics
Tamsulosin is an alpha-adrenoceptor blocker with high specificity for the alpha-1A and alpha-1D subtypes, which are particularly abundant in the prostate and submaxillary tissues. Blockade of these adrenoceptors relaxes smooth muscle in the prostate and improves urinary flow. Blockade of alpha-1D adrenoceptors relaxes the detrusor muscles of the bladder, preventing symptoms of congestion. The specificity of tamsulosin concentrates the effect in the target area and minimizes effects in areas such as the aorta.
Pharmacokinetics
Orally ingested tamsulosin is 90% absorbed. Time from ingestion to maximum plasma concentration is 4-7 hours. Tamsulosin is 94%-99% bound to proteins, mainly to the acidic alpha-1-glycoprotein. Tamsulosin is metabolized primarily in the liver by cytochrome P450 enzymes, mainly CYP-3A4 and -2D6. The plasma half-life in fasting patients is approximately 14 hours.
Side effects
Common side effects are:
Other less common side effects may include dizziness when standing and angioedema.
Toxicological data
LD50, rat, oral: 650 mg/kg
Markus Falkenstätter, BSc
Mag. pharm. Stefanie Lehenauer
Browse our extensive database of medications from A-Z, including effects, side effects, and dosage.
All active ingredients with their effects, applications, and side effects, as well as the medications they are contained in.
Symptoms, causes, and treatments for common diseases and injuries.
The presented content does not replace the original package insert of the medication, especially regarding the dosage and effects of individual products. We cannot assume liability for the accuracy of the data, as the data has been partially converted automatically. Always consult a doctor for diagnoses and other health-related questions.
© medikamio