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.



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.


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:

  • Dizziness
  • headache
  • Insomnia
  • nausea
  • blurred vision
  • sexual dysfunction

Other less common side effects may include dizziness when standing and angioedema.

Toxicological data

LD50, rat, oral: 650 mg/kg

Chemical & physical properties

ATC Code G04CA02
Formula C20H28N2O5S
Molar Mass (g·mol−1) 408,51
Physical State solid
Melting Point (°C) 228–230
CAS Number 106133-20-4
PUB Number 129211
Drugbank ID DB00706

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All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.


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