Tamsulosin retard (Tablets) Instructions for Use

Marketing Authorization Holder

Aliym, JSC (Russia)

ATC Code

G04CA02 (Tamsulosin)

Active Substance

Tamsulosin (Rec.INN registered by WHO)

Dosage Form

Tamsulosin retard

Prolonged-release film-coated tablets 0.4 mg: 10, 14, 15, 20, 28, 30, 40, 42, 45, or 60 pcs.

Dosage Form, Packaging, and Composition

Prolonged-release film-coated tablets from yellow to brownish-yellow in color, round, biconvex; a cross-section shows two layers.

Excipients: hypromellose (hydroxymethylcellulose) 41.25 mg, colloidal silicon dioxide (aerosil) 0.625 mg, microcrystalline cellulose 82.1 mg, magnesium stearate 0.625 mg.

Shell composition Opadry II – series 85 (partially hydrolyzed polyvinyl alcohol, macrogol 3350, talc, titanium dioxide, yellow iron oxide, red iron oxide, black iron oxide) 3 mg.

10 pcs. – blisters (1) – carton packs.
10 pcs. – blisters (2) – carton packs.
10 pcs. – blisters (3) – carton packs.
14 pcs. – blisters (1) – carton packs.
14 pcs. – blisters (2) – carton packs.
14 pcs. – blisters (3) – carton packs.
15 pcs. – blisters (1) – carton packs.
15 pcs. – blisters (2) – carton packs.
15 pcs. – blisters (3) – carton packs.
20 pcs. – blisters (1) – carton packs.
20 pcs. – blisters (2) – carton packs.
20 pcs. – blisters (3) – carton packs.

Clinical-Pharmacological Group

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

Pharmacotherapeutic Group

Alpha1-adrenergic blocker

Pharmacological Action

Tamsulosin is a specific blocker of postsynaptic alpha-adrenergic receptors located in the smooth muscle of the prostate gland, bladder neck, and prostatic part of the urethra.

The blockade of alpha-adrenergic receptors by tamsulosin leads to a decrease in the tone of the smooth muscle of the prostate gland, bladder neck, and prostatic part of the urethra and improves urine outflow.

Simultaneously, both voiding symptoms and filling symptoms caused by increased smooth muscle tone and detrusor hyperactivity in benign prostatic hyperplasia (BPH) are reduced.

Tamsulosin’s ability to act on the alpha A subtype of adrenergic receptors is 20 times greater than its ability to interact with the alpha B subtype of adrenergic receptors, which are located in the smooth muscles of blood vessels.

Due to its high selectivity, Tamsulosin does not cause a clinically significant decrease in systemic blood pressure in either patients with arterial hypertension or patients with normal baseline blood pressure.

Pharmacokinetics

Tamsulosin is well absorbed in the intestine and has almost 100% bioavailability.

The absorption of tamsulosin is somewhat slowed down after food intake.

A consistent level of absorption can be achieved if the patient always takes the drug after a regular breakfast.

Tamsulosin is characterized by linear kinetics.

After a single oral dose of 0.4 mg, its C_max is reached after 6 hours.

After multiple oral doses of 0.4 mg per day, C_ss is reached by day 5, with its value being approximately two-thirds higher than the value of this parameter after a single dose.

Plasma protein binding is 99%, V_d is small (about 0.2 l/kg).

Tamsulosin is slowly metabolized in the liver to form less active metabolites.

Most of the tamsulosin is present in the blood plasma in unchanged form.

Experiments have revealed the ability of tamsulosin to slightly induce the activity of liver microsomal enzymes.

In cases of mild to moderate hepatic impairment, no dose adjustment is required.

Tamsulosin and its metabolites are mainly excreted in the urine, with approximately 9% of the drug excreted unchanged.

T_1/2 of the drug after a single dose of 0.4 mg after a meal is 10 hours, after multiple doses it is 13 hours.

No dose reduction is required in renal impairment; if the patient has severe renal impairment (creatinine clearance (CrCl) less than 10 ml/min), tamsulosin should be prescribed with caution.

Indications

• Treatment of dysuric disorders in benign prostatic hyperplasia.

ICD codes

Dosage Regimen

Take one 0.4 mg prolonged-release film-coated tabletorally once daily.

Administer the dose after the same meal each day, preferably after breakfast, to ensure consistent absorption.

Swallow the tablet whole with a full glass of water; do not chew, crush, or split the tablet as this damages the prolonged-release properties.

The recommended initial and maintenance dose is 0.4 mg once daily.

No dose adjustment is typically required for elderly patients or those with mild to moderate renal impairment.

Exercise caution in patients with severe renal impairment (creatinine clearance below 10 mL/min).

This medication is 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 resume the normal schedule the next day. Do not double the dose to make up for a missed one.

Therapeutic effect on urinary symptoms may be observed after 2-4 weeks of treatment.

Regular follow-up with a physician is necessary to monitor treatment efficacy and tolerability.

Adverse Reactions

The frequency of side effects developing with tamsulosin intake is classified according to WHO recommendations: very common – not less than 10%; common – not less than 1%, but less than 10%; uncommon – not less than 0.1%, but less than 1%; rare – not less than 0.01%, but less than 0.1%; very rare – less than 0.01%, including isolated reports.

Rare – dizziness, retrograde ejaculation; very rare – orthostatic hypotension, tachycardia/palpitations, asthenia, headache, nausea, vomiting, diarrhea, constipation, hypersensitivity reactions – skin rash, itching, angioedema.

Contraindications

• Orthostatic hypotension (including history);
• Severe hepatic impairment;
• Hypersensitivity to tamsulosin or any other component of the drug.

With caution: chronic renal failure (CrCl below 10 ml/min).

Use in Hepatic Impairment

Contraindicated in severe hepatic impairment.

Use in Renal Impairment

With caution: chronic renal failure (CrCl below 10 ml/min).

Special Precautions

As with the use of other alpha-blockers, in some cases, a decrease in blood pressure may be observed during treatment with Tamsulosin retard, which can sometimes lead to fainting.

At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down and remain in this position until the signs disappear.

During cataract surgery while taking the drug, the development of intraoperative floppy iris syndrome (IFIS) is possible, which the surgeon must take into account for preoperative patient preparation and during the operation.

Before starting therapy with Tamsulosin retard, the patient should be examined to rule out the presence of other diseases that may cause the same symptoms as BPH.

Before starting treatment and regularly during therapy, a digital rectal examination should be performed and, if required, determination of prostate-specific antigen.

Effect on ability to drive vehicles and operate machinery

Caution should be exercised when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions, due to the possible development of dizziness.

Overdose

There are no reports of acute overdose with tamsulosin.

However, theoretically, an overdose may lead to an acute decrease in blood pressure and compensatory tachycardia, in which case symptomatic therapy should be administered.

Blood pressure and heart rate may recover when the person assumes a horizontal position.

If there is no effect, agents that increase the volume of circulating blood and, if necessary, vasoconstrictors can be used.

Renal function should be monitored.

It is unlikely that dialysis will be effective, as Tamsulosin is highly bound to plasma proteins.

To prevent further absorption of the drug, gastric lavage, administration of activated charcoal or an osmotic laxative, such as sodium sulfate, is advisable.

Drug Interactions

No interactions were detected when tamsulosin was prescribed together with atenolol, enalapril, or nifedipine.

With simultaneous use of tamsulosin with cimetidine, a slight increase in the plasma concentration of tamsulosin was noted, and with furosemide – a decrease in concentration; however, this does not require a change in the dose of Tamsulosin retard, since the drug concentration remains within the normal range.

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.

Diclofenac and warfarin may increase the elimination rate of tamsulosin.

Concomitant administration of other alpha₁-adrenergic receptor antagonists may lead to a decrease in blood pressure.

Storage Conditions

Store the drug in a dry place, protected from light, at a temperature not exceeding 25°C (77°F).

Keep out of reach of children.

Shelf Life

Shelf life 2 years.

Do not use after the expiration date printed on the packaging.

Dispensing Status

The drug is dispensed by prescription.

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.