Mictosin (Capsules) Instructions for Use

Marketing Authorization Holder

Sandoz, d.d. (Slovenia)

Manufactured By

Lek d.d. (Slovenia)

ATC Code

G04CA02 (Tamsulosin)

Active Substance

Tamsulosin (Rec.INN registered by WHO)

Dosage Form

Mictosin

Extended-release capsules 400 mcg: 10, 20, 30, 40, or 50 pcs.

Dosage Form, Packaging, and Composition

Extended-release capsules hard gelatin, opaque, size No. 2, with a yellow body marked “TML 0.4” and a light green cap; capsule contents – pellets from white to light yellow.

Excipients: pellet core: polysorbate 80 – 300 mcg, sodium lauryl sulfate – 300 mcg, microcrystalline cellulose – 171 mg, polyacrylate 30% dispersion – 93.333 mg¹ (28 mg²).

Pellet coating composition polyacrylate 30% dispersion (methacrylic acid and ethyl acrylate copolymer (1:2)¹) – 23.554 mg (7.066 mg²), methacrylic acid copolymer (methacrylic acid copolymer dispersion (methacrylic acid and ethyl acrylate copolymer (1:1)¹) – 7.852 mg (2.356 mg²), talc – 4.711 mg.

¹ is a 30% aqueous dispersion. The water included in this dispersion is removed during the manufacturing process.
² mass of anhydrous substance.

Capsule shell composition iron oxide red dye – 0.003 mg (0.0049%), titanium dioxide – 1.281 mg (2.1%), iron oxide yellow dye – 0.124 mg (0.2033%), indigo carmine (FD&C Blue 2) – 0.005 mg (0.0082%), gelatin – 59.587 mg (up to 100%).
Marking ink composition shellac (E904) – 24-27%, anhydrous ethanol – 23-26%, isopropyl alcohol – 1-3%, propylene glycol – 3-7%, concentrated ammonia solution – 1-2%, iron oxide black (E172) – 24-28%, potassium hydroxide – 0.5-1%, purified water – 15-18%.

10 pcs. – blisters (1) – cardboard packs.
10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (4) – cardboard packs.
10 pcs. – blisters (5) – 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, 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 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 capsuleonce daily.

Swallow the capsule whole. Do not chew, crush, or open the capsule.

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

Do not exceed the recommended daily dose.

The therapeutic effect typically appears after 2 to 4 weeks of continuous treatment.

Continue treatment as long as prescribed by your physician.

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.

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

Seek immediate medical attention if an erection persists for more than 4 hours.

Adverse Reactions

From the cardiovascular system palpitations, atrial fibrillation, arrhythmia, tachycardia, dyspnea, orthostatic hypotension.

From the CNS headache, dizziness, syncope.

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 (IFIS) during cataract and glaucoma surgery in patients taking Tamsulosin have been reported.

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 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 α₁-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 surgical interventions for cataract or glaucoma, 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 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 possible development of intraoperative floppy iris syndrome during surgery.

Effect on ability to drive vehicles and mechanisms

During the use of tamsulosin, patients should exercise caution when driving vehicles and mechanisms, 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 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-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.