Omsulosin (Capsules) Instructions for Use

Marketing Authorization Holder

Sun Pharmaceutical Industries, Ltd. (India)

ATC Code

G04CA02 (Tamsulosin)

Active Substance

Tamsulosin (Rec.INN registered by WHO)

Dosage Form

Omsulosin

Prolonged-release enteric-coated capsules 400 mcg: 10, 30, or 100 pcs.

Dosage Form, Packaging, and Composition

Prolonged-release enteric-coated capsules hard gelatin, size #2, with an orange body and a brown cap, printed with black ink "R" on the cap and "TSN 400" on the body; capsule contents are white or almost white granules.

Excipients: microcrystalline cellulose PH101 – 194.4 mg, magnesium stearate – 5.7 mg, methacrylic acid and ethyl acrylate copolymer (1:1) dispersion – 75 mg.

Enteric coating composition: methacrylic acid and ethyl acrylate copolymer (1:1) dispersion – 6.888 mg, sodium hydroxide – 0.088 mg, triacetin – 1.035 mg, purified talc – 1.648 mg, titanium dioxide – 0.117 mg.
Capsule shell composition: body – gelatin – q.s. to 100%, sunset yellow FCF – 0.098%, ponceau 4R – 0.0036%, brilliant blue FCF – 0.0021%, quinoline yellow – 0.0202%, titanium dioxide – 2.23%; cap – gelatin – q.s. to 100%, yellow iron oxide – 0.6825%, brilliant blue FCF – 0.0045%, azorubine – 0.008%, titanium dioxide – 1.1%.
Printing ink composition: shellac – 24-27%, black iron oxide – 24-28%, potassium hydroxide – 0.05-0.1%.

10 pcs. – blisters (1) – cardboard packs.
10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (10) – cardboard packs.

Clinical-Pharmacological Group

Drug used for urination disorders associated with benign prostatic hyperplasia. Alpha₁-adrenergic blocker

Pharmacotherapeutic Group

Drugs used in urology; drugs for the treatment of benign prostatic hyperplasia; alpha-adrenergic blockers

Pharmacological Action

Alpha₁-adrenergic receptor blocker; an agent for the symptomatic treatment of benign prostatic hyperplasia.

It selectively blocks postsynaptic alpha_1A-adrenergic receptors of the smooth muscles of the prostate gland, bladder neck, and prostatic part of the urethra. As a result, the tone of the smooth muscles of these structures decreases, facilitating urine outflow. Simultaneously, symptoms of obstruction and irritation associated with benign prostatic hyperplasia are reduced. The therapeutic effect appears approximately 2 weeks after the start of treatment.

Tamsulosin has a significantly lesser ability to block alpha_1B-adrenergic receptors of vascular smooth muscles, therefore its effect on systemic blood pressure is insignificant.

Pharmacokinetics

After oral administration, Tamsulosin is rapidly and almost completely absorbed from the gastrointestinal tract. After a single oral dose of 400 mcg, the C_max of the active substance in plasma is reached after 6 hours.

Plasma protein binding is 99%. The V_d is insignificant and amounts to 0.2 l/kg.

Tamsulosin is slowly metabolized in the liver to form pharmacologically active metabolites that retain high selectivity for alpha_1A-adrenergic receptors. Most of the active substance is present in the blood unchanged.

The T_1/2 of tamsulosin after a single dose is 10 hours, the terminal T_1/2 is 22 hours. It is excreted by the kidneys, 9% unchanged.

Indications

Treatment of dysuric disorders in benign prostatic hyperplasia.

ICD codes

Dosage Regimen

Take one 400 mcg capsuleorally once daily.

Take the capsule at the same time every day, approximately 30 minutes after the same meal.

Do not chew or crush the capsules; swallow them whole with a glass of water.

If you miss a dose, take it as soon as you remember on the same day. If you remember the next day, skip the missed dose and continue your regular schedule. Do not take a double dose to make up for a forgotten one.

The therapeutic effect on urination symptoms typically begins after 2 to 4 weeks of continuous treatment.

No dosage adjustment is required for elderly patients or for patients with mild to moderate renal impairment.

Use with caution in patients with severe renal impairment (creatinine clearance less than 10 ml/min).

This medication is contraindicated in patients with severe hepatic impairment.

Inform your surgeon and ophthalmologist that you are taking or have taken this medication prior to any cataract or glaucoma surgery.

Discontinue therapy and seek immediate medical attention if you experience an erection lasting more than 4 hours (priapism).

Be aware of potential symptoms of orthostatic hypotension, such as dizziness or lightheadedness when rising from a sitting or lying position.

Exercise caution when driving or operating machinery until you know how this medication affects you.

Adverse Reactions

Cardiovascular system: palpitations, atrial fibrillation, arrhythmia, tachycardia, dyspnea, orthostatic hypotension.

Central nervous system: headache, dizziness, syncope.

Digestive system: constipation, diarrhea, nausea, vomiting.

Skin and subcutaneous tissues: skin rash, pruritus, urticaria, angioedema, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis.

Reproductive system: ejaculation disorders, priapism.

Other: rhinitis, asthenia. Cases of intraoperative floppy iris syndrome (IFIS) during cataract and glaucoma surgery in patients taking Tamsulosin have been reported.

Contraindications

Hypersensitivity to tamsulosin; orthostatic hypotension (including history), severe hepatic impairment; children and adolescents under 18 years of age.

With caution severe renal impairment (creatinine clearance less than 10 ml/min); arterial hypotension.

Use in Pregnancy and Lactation

Not applicable.

Use in Hepatic Impairment

Contraindicated in severe hepatic impairment.

Use in Renal Impairment

Should be used with caution in severe renal impairment (creatinine clearance < 10 ml/min).

Pediatric Use

Contraindicated in children and adolescents under 18 years of age.

Special Precautions

Before starting therapy with tamsulosin, the patient should be examined for the presence of other diseases that may cause the same symptoms as benign prostatic hyperplasia. Before starting treatment and regularly during therapy, a digital rectal examination should be performed and, if required, determination of prostate-specific antigen. In patients with impaired renal function, no dosage adjustment is required.

There have been reports of cases of prolonged erection and priapism during therapy with alpha₁-adrenergic blockers. If an erection persists for more than 4 hours, immediate medical attention should be sought. If therapy for priapism is not administered immediately, it may lead to penile tissue damage and irreversible loss of potency.

In some patients taking or having previously taken Tamsulosin, during cataract or glaucoma surgery, the development of intraoperative floppy iris syndrome (IFIS) is possible, which may lead to complications during surgery or in the postoperative period. It is not recommended to start tamsulosin therapy in patients scheduled for cataract or glaucoma surgery. During the preoperative examination of patients, the surgeon and ophthalmologist should take into account whether the patient is taking or has taken Tamsulosin. This is necessary to prepare for the possible development of intraoperative floppy iris syndrome during surgery.

Effect on ability to drive vehicles and operate machinery

During the use of tamsulosin, patients should exercise caution when driving vehicles and operating machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use of tamsulosin with cimetidine, some increase in the concentration of tamsulosin in blood plasma was noted, and with furosemide – a decrease in concentration; with other alpha₁-adrenergic blockers – a pronounced enhancement of the hypotensive effect is possible.

Diclofenac and indirect anticoagulants somewhat increase the elimination rate of tamsulosin.

Diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin, and warfarin do not change the free fraction of tamsulosin in human plasma in vitro. In turn, Tamsulosin also does not change the free fractions of diazepam, propranolol, trichlormethiazide, and chlormadinone.

In vitro studies, no interaction at the level of hepatic metabolism with amitriptyline, salbutamol, glibenclamide, and finasteride was found.

Other alpha₁-adrenergic blockers, acetylcholinesterase inhibitors, alprostadil, anesthetics, diuretics, levodopa, antidepressants, beta-blockers, slow calcium channel blockers, muscle relaxants, nitrates, and ethanol may enhance the severity of the hypotensive effect.

Concomitant administration of tamsulosin with potent inhibitors of the CYP3A4 isoenzyme may lead to an increase in the concentration of tamsulosin. Concomitant administration with ketoconazole led to an increase in the AUC and C_max of tamsulosin by 2.8 and 2.2 times, respectively.

Tamsulosin should not be used in combination with potent CYP3A4 inhibitors in patients with impaired metabolism of the CYP2D6 isoenzyme. Tamsulosin should be used with caution in combination with potent and moderate CYP3A4 inhibitors.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.