Peringatan Keamanan

In the event of overdose, patients may experience hypotension and should lie down in a supine position to maintain blood pressure and heart rate.Label If further measures are required intravenous fluids should be considered.Label If further progression is required, vasopressors may be used and renal function should be monitored.Label Dialysis is unlikely to assist in treating overdose because tamsulosin is extensively protein bound.Label

The oral LD50 in rats is 650mg/kg.MSDS

Tamsulosin is not indicated for use in women and no studies have been performed in pregnancy, though animal studies have not shown fetal harm.Label Tamsulosin is excreted in the milk of rats but there is no available data on what the effect of this tamsulosin exposure may be.Label Animal studies have shown male and female rat fertility is affected by tamsulosin due to impairment of ejaculation and fertilization.Label In men, tamsulosin is associated with abnormal ejaculation.Label Tamsulosin is not mutagenic but may be carcinogenic at levels above the maximum recommended human dose.Label Female rats experience a slight increase in the rates of mammary gland fibroadenomas and adenocarcinomas.Label

Tamsulosin

DB00706

small molecule approved investigational

Deskripsi

Tamsulosin is a selective alpha-1A and alpha-1B adrenoceptor antagonist that exerts its greatest effect in the prostate and bladder, where these receptors are most common.Label It is indicated for the treatment of signs and symptoms of benign prostatic hypertrophy.Label Antagonism of these receptors leads to relaxation of smooth muscle in the prostate and detrusor muscles in the bladder, allowing for better urinary flow.Label Other alpha-1 adrenoceptor antagonists developed in the 1980s were less selective and more likely to act on the smooth muscle of blood vessels, resulting in hypotension.A178351

Tamsulosin was first approved by the FDA on April 15, 1997.L6238

Struktur Molekul 2D

Berat 408.512
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life in fasted patients is 14.9±3.9 hours.[Label] The elimination half life is 5-7 hours and the apparent half life is 9 to 13 hours in healthy subjects.[Label] In patients who require tamsulosin, the apparent half life is 14-15 hours.[Label]
Volume Distribusi 16L after intravenous administration.[Label]
Klirens (Clearance) 2.88L/h.[Label]

Absorpsi

Oral tamsulosin is 90% absorbed in fasted patients.Label The area under the curve is 151-199ng/mL\*hr for a 0.4mg oral dose and 440-557ng/mL*hr for a 0.8mg oral dose.Label The maximum plasma concentration is 3.1-5.3ng/mL for a 0.4mg oral dose and 2.5-3.6ng/mL for a 0.8mg oral dose.Label Taking tamsulosin with food increases the time to maximum concentration from 4-5 hours to 6-7 hours but increases bioavailability by 30% and maximum plasma concentration by 40-70%.Label

Metabolisme

Tamsulosin is mostly metabolized in the liver by cytochrome P450 (CYP) 3A4 and 2D6, with some metabolism by other CYPs.Label,A1078 CYP3A4 is responsible for the deethylation of tamsulosin to the M-1 metabolite and the oxidative deamination to the AM-1 metabolite,A178276,A178321 while CYP2D6 is responsible for the hydroxylation of tamsulosin to the M-3 metabolite and the demethylation of tamsulosin to the M-4 metabolite.A178276 In addition, tamsulosin can be hydroxylated at a different position by an unknown enzyme to form the M-2 metabolite.A178276 The M-1, M-2, M-3, and M-4 metabolites can be glucuronidated, and the M-1 and M-3 metabolites can undergo sulfate conjugation to form other metabolites before excretion.A178321

Rute Eliminasi

97% of an orally administered does is recovered in studies, which 76% in the urine and 21% in the feces after 168 hours.Label 8.7% of the dose is excreted as unmetabolized tamsulosin.Label,A1078

Interaksi Makanan

1 Data
  • 1. Take after a meal. Take 30 minutes after the same meal each day to reduce plasma level variations.

Interaksi Obat

1438 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Tamsulosin is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Tamsulosin is combined with Levodopa.
Risperidone Tamsulosin may increase the hypotensive activities of Risperidone.
Nicotine The risk or severity of adverse effects can be increased when Tamsulosin is combined with Nicotine.
Mecamylamine The risk or severity of adverse effects can be increased when Tamsulosin is combined with Mecamylamine.
Pentolinium The risk or severity of adverse effects can be increased when Tamsulosin is combined with Pentolinium.
Trimethaphan The risk or severity of adverse effects can be increased when Tamsulosin is combined with Trimethaphan.
Hexamethonium The risk or severity of adverse effects can be increased when Tamsulosin is combined with Hexamethonium.
Cyclopentamine The risk or severity of adverse effects can be increased when Tamsulosin is combined with Cyclopentamine.
Dapoxetine Dapoxetine may increase the orthostatic hypotensive activities of Tamsulosin.
Methotrexate The protein binding of Methotrexate can be increased when combined with Tamsulosin.
Cimetidine The serum concentration of Tamsulosin can be increased when it is combined with Cimetidine.
Lurasidone Tamsulosin may increase the hypotensive activities of Lurasidone.
Mirabegron The serum concentration of Tamsulosin can be increased when it is combined with Mirabegron.
Nicorandil Nicorandil may increase the hypotensive activities of Tamsulosin.
Ketoprofen The risk or severity of adverse effects can be increased when Ketoprofen is combined with Tamsulosin.
Dexketoprofen The risk or severity of adverse effects can be increased when Dexketoprofen is combined with Tamsulosin.
Bethanidine The therapeutic efficacy of Bethanidine can be decreased when used in combination with Tamsulosin.
Isoetharine The therapeutic efficacy of Isoetharine can be decreased when used in combination with Tamsulosin.
Etomidate The therapeutic efficacy of Etomidate can be decreased when used in combination with Tamsulosin.
Phenylpropanolamine The therapeutic efficacy of Phenylpropanolamine can be decreased when used in combination with Tamsulosin.
Guanabenz The therapeutic efficacy of Guanabenz can be decreased when used in combination with Tamsulosin.
Dexmedetomidine The therapeutic efficacy of Dexmedetomidine can be decreased when used in combination with Tamsulosin.
Tizanidine The therapeutic efficacy of Tizanidine can be decreased when used in combination with Tamsulosin.
Orciprenaline The therapeutic efficacy of Orciprenaline can be decreased when used in combination with Tamsulosin.
Ritodrine The therapeutic efficacy of Ritodrine can be decreased when used in combination with Tamsulosin.
Terbutaline The therapeutic efficacy of Terbutaline can be decreased when used in combination with Tamsulosin.
Bitolterol The therapeutic efficacy of Bitolterol can be decreased when used in combination with Tamsulosin.
Salmeterol The therapeutic efficacy of Salmeterol can be decreased when used in combination with Tamsulosin.
Formoterol The therapeutic efficacy of Formoterol can be decreased when used in combination with Tamsulosin.
Albuterol The therapeutic efficacy of Salbutamol can be decreased when used in combination with Tamsulosin.
Guanfacine The therapeutic efficacy of Guanfacine can be decreased when used in combination with Tamsulosin.
Isoprenaline The therapeutic efficacy of Isoprenaline can be decreased when used in combination with Tamsulosin.
Arbutamine The therapeutic efficacy of Arbutamine can be decreased when used in combination with Tamsulosin.
Arformoterol The therapeutic efficacy of Arformoterol can be decreased when used in combination with Tamsulosin.
Fenoterol The therapeutic efficacy of Fenoterol can be decreased when used in combination with Tamsulosin.
Pirbuterol The therapeutic efficacy of Pirbuterol can be decreased when used in combination with Tamsulosin.
Ephedra sinica root The therapeutic efficacy of Ephedra sinica root can be decreased when used in combination with Tamsulosin.
Ephedrine The therapeutic efficacy of Ephedrine can be decreased when used in combination with Tamsulosin.
Procaterol The therapeutic efficacy of Procaterol can be decreased when used in combination with Tamsulosin.
Clenbuterol The therapeutic efficacy of Clenbuterol can be decreased when used in combination with Tamsulosin.
Bambuterol The therapeutic efficacy of Bambuterol can be decreased when used in combination with Tamsulosin.
4-Bromo-2,5-dimethoxyphenethylamine The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Tamsulosin.
Lofexidine The therapeutic efficacy of Lofexidine can be decreased when used in combination with Tamsulosin.
Indacaterol The therapeutic efficacy of Indacaterol can be decreased when used in combination with Tamsulosin.
Amibegron The therapeutic efficacy of Amibegron can be decreased when used in combination with Tamsulosin.
Solabegron The therapeutic efficacy of Solabegron can be decreased when used in combination with Tamsulosin.
Xylometazoline The therapeutic efficacy of Xylometazoline can be decreased when used in combination with Tamsulosin.
Naphazoline The therapeutic efficacy of Naphazoline can be decreased when used in combination with Tamsulosin.
Protokylol The therapeutic efficacy of Protokylol can be decreased when used in combination with Tamsulosin.
Adrafinil The therapeutic efficacy of Adrafinil can be decreased when used in combination with Tamsulosin.
Isoxsuprine The therapeutic efficacy of Isoxsuprine can be decreased when used in combination with Tamsulosin.
Hexoprenaline The therapeutic efficacy of Hexoprenaline can be decreased when used in combination with Tamsulosin.
Etilefrine The therapeutic efficacy of Etilefrine can be decreased when used in combination with Tamsulosin.
Olodaterol The therapeutic efficacy of Olodaterol can be decreased when used in combination with Tamsulosin.
Vilanterol The therapeutic efficacy of Vilanterol can be decreased when used in combination with Tamsulosin.
Synephrine The therapeutic efficacy of Synephrine can be decreased when used in combination with Tamsulosin.
Moxonidine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Tamsulosin.
Doxofylline The therapeutic efficacy of Doxofylline can be decreased when used in combination with Tamsulosin.
DL-Methylephedrine The therapeutic efficacy of DL-Methylephedrine can be decreased when used in combination with Tamsulosin.
Amitraz The therapeutic efficacy of Amitraz can be decreased when used in combination with Tamsulosin.
Medetomidine The therapeutic efficacy of Medetomidine can be decreased when used in combination with Tamsulosin.
Xylazine The therapeutic efficacy of Xylazine can be decreased when used in combination with Tamsulosin.
Ractopamine The therapeutic efficacy of Ractopamine can be decreased when used in combination with Tamsulosin.
Romifidine The therapeutic efficacy of Romifidine can be decreased when used in combination with Tamsulosin.
Detomidine The therapeutic efficacy of Detomidine can be decreased when used in combination with Tamsulosin.
Etafedrine The therapeutic efficacy of Etafedrine can be decreased when used in combination with Tamsulosin.
Rilmenidine The therapeutic efficacy of Rilmenidine can be decreased when used in combination with Tamsulosin.
PF-00610355 The therapeutic efficacy of PF-00610355 can be decreased when used in combination with Tamsulosin.
Abediterol The therapeutic efficacy of Abediterol can be decreased when used in combination with Tamsulosin.
Tulobuterol The therapeutic efficacy of Tulobuterol can be decreased when used in combination with Tamsulosin.
Dopexamine The therapeutic efficacy of Dopexamine can be decreased when used in combination with Tamsulosin.
Batefenterol The therapeutic efficacy of Batefenterol can be decreased when used in combination with Tamsulosin.
Higenamine The therapeutic efficacy of Higenamine can be decreased when used in combination with Tamsulosin.
Reproterol The therapeutic efficacy of Reproterol can be decreased when used in combination with Tamsulosin.
Levosalbutamol The therapeutic efficacy of Levosalbutamol can be decreased when used in combination with Tamsulosin.
Octopamine The therapeutic efficacy of Octopamine can be decreased when used in combination with Tamsulosin.
Norfenefrine The therapeutic efficacy of Norfenefrine can be decreased when used in combination with Tamsulosin.
Oxyfedrine The therapeutic efficacy of Oxyfedrine can be decreased when used in combination with Tamsulosin.
Rimiterol The therapeutic efficacy of Rimiterol can be decreased when used in combination with Tamsulosin.
Tretoquinol The therapeutic efficacy of Tretoquinol can be decreased when used in combination with Tamsulosin.
Prenalterol The therapeutic efficacy of Prenalterol can be decreased when used in combination with Tamsulosin.
Xamoterol The therapeutic efficacy of Xamoterol can be decreased when used in combination with Tamsulosin.
Racephedrine The therapeutic efficacy of Racephedrine can be decreased when used in combination with Tamsulosin.
Methyldopa The therapeutic efficacy of Methyldopa can be decreased when used in combination with Tamsulosin.
Amidephrine The therapeutic efficacy of Amidephrine can be decreased when used in combination with Tamsulosin.
Esmolol Esmolol may increase the orthostatic hypotensive activities of Tamsulosin.
Betaxolol Betaxolol may increase the orthostatic hypotensive activities of Tamsulosin.
Atenolol Atenolol may increase the orthostatic hypotensive activities of Tamsulosin.
Timolol Timolol may increase the orthostatic hypotensive activities of Tamsulosin.
Propranolol Propranolol may increase the orthostatic hypotensive activities of Tamsulosin.
Bisoprolol Bisoprolol may increase the orthostatic hypotensive activities of Tamsulosin.
Alprenolol Alprenolol may increase the orthostatic hypotensive activities of Tamsulosin.
Pindolol Pindolol may increase the orthostatic hypotensive activities of Tamsulosin.
Acebutolol Acebutolol may increase the orthostatic hypotensive activities of Tamsulosin.
Nadolol Nadolol may increase the orthostatic hypotensive activities of Tamsulosin.
Practolol Practolol may increase the orthostatic hypotensive activities of Tamsulosin.
Penbutolol Penbutolol may increase the orthostatic hypotensive activities of Tamsulosin.
Oxprenolol Oxprenolol may increase the orthostatic hypotensive activities of Tamsulosin.
Dexpropranolol Dexpropranolol may increase the orthostatic hypotensive activities of Tamsulosin.

Target Protein

Alpha-1A adrenergic receptor ADRA1A
Alpha-1D adrenergic receptor ADRA1D
Alpha-1B adrenergic receptor ADRA1B

Referensi & Sumber

Synthesis reference: Hun Wang, Jun Park, Min Kwon, Ji Shim, Bong Lee, Hong Jeon, "Controlled release formulation of tamsulosin hydrochloride and preparation process thereof." U.S. Patent US20050100606, issued May 12, 2005.
Artikel (PubMed)
  • PMID: 11950378
    Dunn CJ, Matheson A, Faulds DM: Tamsulosin: a review of its pharmacology and therapeutic efficacy in the management of lower urinary tract symptoms. Drugs Aging. 2002;19(2):135-61.
  • PMID: 9492387
    Matsushima H, Kamimura H, Soeishi Y, Watanabe T, Higuchi S, Tsunoo M: Pharmacokinetics and plasma protein binding of tamsulosin hydrochloride in rats, dogs, and humans. Drug Metab Dispos. 1998 Mar;26(3):240-5.
  • PMID: 8810034
    Soeishi Y, Matsushima H, Watanabe T, Higuchi S, Cornelissen K, Ward J: Absorption, metabolism and excretion of tamsulosin hydrochloride in man. Xenobiotica. 1996 Jun;26(6):637-45.
  • PMID: 25684798
    Rivard R: Tamsulosin: ureteral stones (distal). Hosp Pharm. 2015 Jan;50(1):31-3. doi: 10.1310/hjp5001-031.
  • PMID: -
    Lepor H, Roehrborn C: Historical Overview of Medical Therapy for Benign Prostatic Hyperplasia Reviews in Urology.

Contoh Produk & Brand

Produk: 206 • International brands: 19
Produk
  • Apo-tamsulosin CR
    Tablet, extended release • 0.4 mg • Oral • Canada • Generic • Approved
  • Auro-tamsulosin CR
    Tablet, extended release • 0.4 mg • Oral • Canada • Generic • Approved
  • Ava-tamsulosin CR
    Tablet, extended release • 0.4 mg • Oral • Canada • Generic • Approved
  • Dutasteride and tamsulosin hydrochloride
    Capsule • - • Oral • US • Generic • Approved
  • Dutasteride and Tamsulosin Hydrochloride
    Capsule • - • Oral • US • Generic • Approved
  • Dutasteride and tamsulosin hydrochloride
    Capsule • - • Oral • US • Generic • Approved
  • Dutasteride and tamsulosin hydrochloride
    Capsule • - • Oral • US • Generic • Approved
  • Dutasteride and Tamsulosin Hydrochloride
    Capsule • - • Oral • US • Generic • Approved
Menampilkan 8 dari 206 produk.
International Brands
  • Betamsal — Hemofarm
  • Contiflo XL — Ranbaxy
  • Flomaxtra — Astellas
  • Harnal D — Astellas
  • Maxrin — Square
  • Mecir — Boehringer Ingelheim
  • Omexel — Astellas
  • Omipro — Jelfa
  • Omix — Astellas
  • Omnic — Astellas Pharma Europe

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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