Tamsulosin


Description

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 prost...

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Pharmacology

Indication

Tamsulosin is indicated for the treatment of signs and symptoms of benign prostatic hyperplasia.[Lab... Read more

Pharmacodynamic

Tamsulosin is an alpha adrenoceptor blocker with specificity for the alpha-1A and alpha-1D subtypes,... Read more

Mechanism of action

Tamsulosin is a blocker of alpha-1A and alpha-1D adrenoceptors.[Label, Read more

Absorption

Oral tamsulosin is 90% absorbed in fasted patients.[Label] The area under the curve is 151-199ng/mL\... Read more

Protein binding

Tamsulosin is 94%-99% protein bound, mostly to alpha-1-acid glycoprotein.[Label]

Volume of distribution

16L after intravenous administration.[Label]

Clearance

2.88L/h.[Label]

Half life

The half life in fasted patients is 14.9±3.9 hours.[Label] The elimination half life is 5-7 hours an... Read more

Route of elimination

97% of an orally administered does is recovered in studies, which 76% in the urine and 21% in the fe... Read more

Toxicity

In the event of overdose, patients may experience hypotension and should lie down in a supine positi... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 19.3-21.1%
  • Kind: placebo
    • Percent: 20.1%
  • Clinical Trial
    Positive orthostatic test result US
  • Kind: experimental
    • Percent: 16-19%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Abnormal ejaculation US
  • Kind: experimental
    • Percent: 8.4-18.1%
  • Kind: placebo
    • Percent: 0.2%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 13.1-17.9%
  • Kind: placebo
    • Percent: 8.3%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 14.9-17.1%
  • Kind: placebo
    • Percent: 10.1%
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 9.0-10.8%
  • Kind: placebo
    • Percent: 7.5%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 7.8-8.5%
  • Kind: placebo
    • Percent: 5.5%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: 7.0-8.3%
  • Kind: placebo
    • Percent: 5.5%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 4.3-6.2%
  • Kind: placebo
    • Percent: 4.5%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 5.1-5.8%
  • Kind: placebo
    • Percent: 4.7%
  • Clinical Trial
    Increased cough US
  • Kind: experimental
    • Percent: 3.4-4.5%
  • Kind: placebo
    • Percent: 2.4%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 3.0-4.3%
  • Kind: placebo
    • Percent: 1.6%
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: 4.0-4.1%
  • Kind: placebo
    • Percent: 3.7%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 2.6-3.9%
  • Kind: placebo
    • Percent: 3.2%
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 2.2-3.7%
  • Kind: placebo
    • Percent: 1.6%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 1.4-2.4%
  • Kind: placebo
    • Percent: 0.6%
  • Clinical Trial
    Decreased libido US
  • Kind: experimental
    • Percent: 1.0-2.0%
  • Kind: placebo
    • Percent: 1.2%
  • Clinical Trial
    Tooth disorder US
  • Kind: experimental
    • Percent: 1.2-2.0%
  • Kind: placebo
    • Percent: 1.4%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 0.2-2.0%
  • Kind: placebo
    • Percent: 0.4%
  • Clinical Trial
    Postural Hypotension US
  • Kind: experimental
    • Percent: 0.2-0.4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Palpitations US
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    Hypotension US
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    Atrial Fibrillation US
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    Arrhythmia US
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    Tachycardia US
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    Skin desquamation US
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    Stevens-Johnson Syndrome US
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    Erythema multiforme US
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    Dermatitis exfoliative US
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    Constipation US
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    Vomiting US
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    Dry Mouth US
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    Visual Impairment US
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    Epistaxis US
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    Intaoperative floppy iris syndrome US
    Post Marketing
    Skin Rash US
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    Pruritus US
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    Urticaria US
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    Allergic-type respiratory symptoms US
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    Angioedema US
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    Dyspnea US
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    Priapism US
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    Intaoperative floppy iris syndrome US
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    Contraindications

    • Route:
      • Oral
    • Dose Form:
      • Capsule
    • Hypersensitivity:
      • true
    • Sex Group: all
    • Regions: US

    Food Interactions

    • Take 30 minutes after a meal (always after the same meal). Taking the drug with food minimizes plasma levels variations.

    Interactions

    Type in a drug name to check for interaction with Tamsulosin

    The metabolism of (R)-warfarin can be decreased when combined with Tamsulosin.
    The metabolism of (S)-Warfarin can be decreased when combined with Tamsulosin.
    The metabolism of Tamsulosin can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
    The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Tamsulosin.
    The therapeutic efficacy of Tamsulosin can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
    The therapeutic efficacy of Tamsulosin can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Tamsulosin.
    The therapeutic efficacy of Tamsulosin can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
    The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Tamsulosin.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Tamsulosin.
    The therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Tamsulosin.
    The metabolism of 5-androstenedione can be decreased when combined with Tamsulosin.
    The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Tamsulosin.
    The metabolism of Tamsulosin can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Tamsulosin.
    The metabolism of Tamsulosin can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Tamsulosin.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Tamsulosin.
    Tamsulosin may decrease the excretion rate of Abacavir which could result in a higher serum level.
    The metabolism of Tamsulosin can be increased when combined with Abatacept.

    References

    • 1 . 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. [PubMed: 11950378]
    • 2 . 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. [PubMed: 9492387]
    • 3 . 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. [PubMed: 8810034]
    • 4 . Rivard R: Tamsulosin: ureteral stones (distal). Hosp Pharm. 2015 Jan;50(1):31-3. doi: 10.1310/hjp5001-031. [PubMed: 25684798]
    • 5 . Lepor H, Roehrborn C: Historical Overview of Medical Therapy for Benign Prostatic Hyperplasia Reviews in Urology. [PubMed: ]
    • 6 . FDA Approved Drug Products: Flomax [Link]
    • 7 . Urology Times: Urologists no longer primary initiator of tamsulosin [Link]

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