Tulosin^® (Capsules) Instructions for Use

Marketing Authorization Holder

Egis Pharmaceuticals PLC (Hungary)

ATC Code

G04CA02 (Tamsulosin)

Active Substance

Tamsulosin (Rec.INN registered by WHO)

Dosage Form

Tulosin®

Modified-release capsules 400 mcg: 10 or 30 pcs.

Dosage Form, Packaging, and Composition

Modified-release capsules hard gelatin, self-locking, with a transparent green body and an opaque green cap; the capsule contents are white pellets, odorless or almost odorless.

Excipients : microcrystalline cellulose, methacrylic acid and ethyl acrylate copolymer (1:1) (in the form of a 30% aqueous dispersion), calcium stearate, talc, triethyl citrate, tween 80 (polysorbate 80).

Gelatin capsule composition: indigo carmine, quinoline yellow, gelatin, titanium dioxide.

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

Clinical-Pharmacological Group

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

Pharmacotherapeutic Group

Alpha1-adrenergic blocker

Pharmacological Action

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

It selectively blocks postsynaptic α_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, and urine outflow is facilitated. Simultaneously, the 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 α_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%. 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 α_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 capsuleorallyonce daily.

Administer the dose at the same time each day, approximately 30 minutes after the same meal every day to ensure consistent absorption.

Swallow the capsule whole with a sufficient amount of water; do not chew or crush the capsule or the pellets inside, as this will damage the modified-release properties.

The therapeutic effect on urinary 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).

Contraindicated in patients with severe hepatic impairment.

If a dose is missed, take it as soon as remembered on the same day; if a full day has passed, skip the missed dose and continue the regular schedule. Do not double the dose to make up for a forgotten one.

Inform your surgeon and ophthalmologist about current or past use of this medication prior to any cataract or glaucoma surgery due to the risk of intraoperative floppy iris syndrome.

Be aware of the potential for orthostatic hypotension (dizziness, lightheadedness) when rising quickly from a sitting or lying position, especially during initial treatment.

Seek immediate medical attention in the event of a persistent, painful erection (priapism) lasting more than 4 hours.

Adverse Reactions

From the cardiovascular system palpitations, atrial fibrillation, arrhythmia, tachycardia, shortness of breath, orthostatic hypotension.

From the central nervous system headache, dizziness, fainting.

From the digestive system: constipation, diarrhea, nausea, vomiting.

From the skin and subcutaneous tissues: skin rash, skin itching, urticaria, angioedema, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis.

From the reproductive system ejaculation disorders, priapism.

Other rhinitis, asthenia. Cases of intraoperative floppy iris syndrome during cataract and glaucoma surgery in patients taking Tamsulosin have been described.

Contraindications

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

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

Use in Pregnancy and Lactation

Not applicable.

Use in Hepatic Impairment

Contraindicated in severe hepatic insufficiency.

Use in Renal Impairment

Should be used with caution in severe renal failure (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 can 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 the prostate-specific antigen. In patients with impaired renal function, no change in the dosage regimen is required.

There have been reports of cases of prolonged erection and priapism during therapy with α₁-adrenergic blockers. If an erection persists for more than 4 hours, immediate medical attention should be sought. If therapy for priapism is not carried out immediately, it can lead to damage to penile tissues and irreversible loss of potency.

In some patients taking or having previously taken Tamsulosin, during surgical interventions for cataract or glaucoma, the development of intraoperative floppy iris syndrome is possible, which can lead to complications during surgery or in the postoperative period. It is not recommended to start tamsulosin therapy in patients who are 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 possibility of intraoperative floppy iris syndrome during surgery.

Effect on the ability to drive vehicles and machinery

During the use of tamsulosin, patients should exercise caution when driving vehicles and 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 the blood plasma was noted, and with furosemide – a decrease in concentration; with other α₁-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 α₁-adrenergic blockers, acetylcholinesterase inhibitors, alprostadil, anesthetics, diuretics, levodopa, antidepressants, beta-adrenergic blockers, slow calcium channel blockers, muscle relaxants, nitrates and ethanol may increase 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.