Tamsulosin

Indications
 Oral
Benign prostatic hyperplasia
Adult: As HCl: As modified-release preparation: 400 mcg once daily. May increase to 800 mcg once daily after 2-4 wk if necessary. If therapy is interrupted for several days, restart with 400 mcg once daily. Dose to be taken 30 minutes after the same meal each day.
CrCl (ml/min)Dosage Recommendation
≥10No dose adjustment needed.
<10Not studied.
Hepatic impairment: Moderate hepatic impairment (Child-Pugh classification A and B): No dose adjustment needed. Severe hepatic impairment: Avoid.
Contraindications
 Hypersensitivity to sulfonamide, severe hepatic impairment, lactation.
Warnings / Precautions
 Prostate carcinoma should be ruled out before starting the therapy. Risk of intraoperative floppy iris syndrome in patients who undergo cataract surgery. May cause orthostatic hypotension or syncope especially with first dose, if dosage is increased or an antihypertensive drug or a phosphodiesterase-5 inhibitor is added to the treatment regimen. Caution when used in patients with sulfa allergy. May cause priapism (rare); immediate medical attention is recommended. Pregnancy.
Adverse Reactions
 Postural hypotension, dizziness and vertigo, malaise, headache, rhinitis, pharyngitis, cough, sinusitis, diarrhoea, nausea, infection, asthenia, back pain, tooth disorder, chest pain, somnolence, insomnia, decreased libido, abnormal ejaculation, priapism, blurred vision. Risk of intraoperative floppy iris syndrome during phacoemulsification surgery.
Overdose Reactions
 Hypotension, headache. Keep in supine position to restore BP and heart rate. If needed, admin of IV fluid and vasopressors. Dialysis unlikely to be of benefit.
Drug Interactions
 Concomitant admin with moderate or strong inhibitors of CYP2D6 (eg. fluoxetine) or CYP34A (eg. ketoconazole, cimetidine) increases serum concentration.
See Below for More tamsulosin Drug Interactions
Food Interactions
 Food reduced extent and rate of absorption.
Mechanism of Actions
 Tamsulosin is a selective α1 adrenoreceptor-blocking agent. Smooth muscle tone is mediated by the sympathetic nervous stimulation of α1 adrenoreceptors, which are abundant in the prostate, prostatic capsule, prostatic urethra, and bladder neck. Blockade of these adrenoceptors can cause smooth muscles in the bladder neck and prostate to relax, resulting in an improvement in urine flow rate and reduction in symptoms in BPH.
Absorption: Completely absorbed from the GI tract. Peak plasma concentrations after 1 hr; 6 hr (modified-release preparation).
Distribution: Protein-binding: 99%.
Metabolism: Metabolised slowly in the liver primarily by CYP2D6 and CYP3A4.
Excretion: Excreted in urine (76%) and faeces (21%). Plasma elimination half life: 4-5.5 hr; as modified-release preparation : 10-13 hr.
Administration
 Cap: Should be taken with food. (Take ½ hr following the same meal daily. Swallow whole, do not open/chew/crush.)
Orodispersible extended release tab: Should be taken with food. (Take after meals. Place on the tongue & allow to dissolve. Then, swallow w/ saliva or water. )
Prolonged release tab: May be taken with or without food. (Swallow whole, do not chew/crush.)
Storage Conditions
 Oral: Store at 25°C.
ATC Classification
 G04CA02 - tamsulosin ; Belongs to the class of alpha-adrenoreceptor antagonists. Used in the treatment of benign prostatic hypertrophy.
Storage
 Oral: Store at 25°C.
Available As
  • Tamsulosin 0.2 mg
  • Tamsulosin 0.4 mg
  • Tamsulosin 0.5 mg
  • Tamsulosin 200 mcg

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