Glansin capsules with modified release 0.2mg, 30pcs

Composition

Each modified-release capsule contains:

Active ingredient: tamsulosin hydrochloride pellets 0.2% * – 100 mg,

containing tamsulosin hydrochloride-0.2 mg

Auxiliary substances of pellets: granulated sugar [sucrose, starch molasses] 91.33 mg, ethylcellulose 0.8 mg, methylacrylic acid and ethyl acrylate copolymer [1: 1] 7.05 mg, macrogol-6000 0.62 mg

Auxiliary substances: granulated sugar [sucrose, starch molasses] 160.0 mg

Capsule cap: gelatin 20.1157 mg, water 3.4800 mg, iron oxide dye red 0.1440 mg, iron oxide dye yellow 0.0799 mg, titanium dioxide 0.1612 mg, sodium lauryl sulfate 0.0190 mg

Capsule body: 32,6880 mg gelatin, water 5,6550 mg, dye iron oxide red 0,2340 mg, dye iron oxide yellow 0,1299 mg, titanium dioxide 0,2619 mg, sodium lauryl 0,0312 mg

Ink for the inscription on the shell of the capsules: ethanol 30-34%,2-propanol 3-6%, butanol 3-6%, propylene glycol 0,5-2%, Polysorbate 80 0-1%, shellac 20-25%, titanium dioxide 30-34%.

Pharmacological properties

pharmacotherapeutic group: α₁-blocker.

ATX code: G04CA02.

Pharmacological properties

Pharmacodynamics :

Tamsulosin is a specific blocker of postsynaptic α1-adrenergic receptors located in the smooth muscles of the prostate, bladder neck and prostatic part of the urethra. Blockade_{of α1}-adrenergic receptors with tamsulosin leads to a decrease in the smooth muscle tone of the prostate, bladder neck and prostatic part of the urethra and an improvement in the outflow of urine. At the same time, both the symptoms of emptying and the symptoms of filling the bladder due to increased smooth muscle tone and detrusor hyperactivity in benign prostatic hyperplasia are reduced.

The ability of tamsulosin to act on_{the α1 A} subtype of adrenoreceptors is 20 times greater than its ability to interact with_{the α1 b} subtype of adrenoreceptors, which are located in vascular smooth muscle. Due to its high selectivity, the drug does not cause a clinically significant decrease in systemic blood pressure (BP) both in patients with arterial hypertension and in patients with normal baseline blood pressure. The drug has a prolonged action (with a modified release).

Pharmacokinetics:

Tamsulosin is well absorbed in the intestine and has almost 100% bioavailability. Tamsulosin absorption slows down somewhat after a meal. The same level of absorption can be achieved if the patient takes the drug every time after a regular breakfast. Tamsulosin is characterized by linear kinetics. After a single oral intake on an empty stomach of a 0.4 mg capsule, the maximum concentration (cmax) of tamsulosin in blood plasma is reached after 6 hours. When taking an oral capsule of 0.4 mg per day for several days, the equilibrium concentration is reached by day 5, while its value is approximately 2/3 higher than the value of this parameter after taking a single dose. Binding to plasma proteins is 99%. The volume of distribution is insignificant and amounts to about 0.2 l / kg. Tamsulosin is slowly metabolized in the liver to form less active metabolites. Most of tamsulosin is present in the blood plasma in unchanged form.

In patients with mild to moderate hepatic insufficiency, no dosage adjustment is required.

Tamsulosin and its metabolites are mainly excreted in the urine, with about 9% of the drug excreted unchanged. The half-life of the drug with a single dose of tamsulosin capsule at a dose of 0.4 mg after meals is 10 hours, when taken for several days-13 hours.

In patients with renal insufficiency, no dose reduction is required, and if the patient has severe renal insufficiency (creatinine clearance less than 10 ml/min), tamsulosin should be administered with caution.

Indications

Treatment of dysuric disorders in benign prostatic hyperplasia (including treatment of urinary disorders).

Use during pregnancy and lactation

The drug Glansin is intended for use only in males.

Contraindications

Hypersensitivity to tamsulosin or any other component of the drug; sucrose/isomaltase deficiency; fructose intolerance; glucose-galactose malabsorption; orthostatic hypotension (including in the anamnesis); severe liver failure, children under 18 years of age.

With caution-severe renal insufficiency (creatinine clearance less than 10 ml / min); arterial hypotension, when used simultaneously with alpha_-1-blockers.

Side effects

Gradation of the frequency of side effects:

very common >1/10>

common > 1/100 to >< 1/10

uncommon > 1/1000 to >< 1/100

rare >1/10 000 to >< 1/1000

very rare

From the cardiovascular system: infrequently-palpitation, postural hypotension, very rarely-atrial fibrillation, shortness of breath, arrhythmia. From the gastrointestinal tract: infrequently-constipation, diarrhea, nausea, vomiting, very rarely – dry mouth. From the nervous system: often – dizziness; infrequently-headache, rarely-fainting, drowsiness. From the reproductive system: often-ejaculation disorders, very rarely-priapism. Respiratory, thoracic and mediastinaldisorders: infrequently-rhinitis, very rarely – nosebleeds. Skin and subcutaneous tissue disorders: infrequently-rash, pruritus, urticaria; rarely-angioedema (including angioedema); very rarely-Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis. General condition disorders: infrequently-asthenia. Other: intraoperative instability of the iris (narrow pupil syndrome) during cataract surgery in patients treated with tamsulosin.

Interaction

When used concomitantly with cimetidine, there was a slight increase in the concentration of tamsulosin in blood plasma, with furosemide-a decrease in the concentration of tamsulosin, but this does not require a change in the dose of tamsulosin, since the concentration of the drug remains within the normal range. Diclofenac and warfarin may slightly increase the rate of tamsulosin elimination. Concomitant use of tamsulosin with other α1-adrenergic antagonists may lead to a decrease in blood pressure. No drug interactions were observed when co-administered with atenolol, enalapril, or nifedipine. Diazepam, propranolol, trichloromethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin, and warfarin do not alter the free fraction of tamsulosin in human plasma in vitro. Tamsulosin does not alter the free fractions of diazepam, propranolol, trichloromethiazide, and chlormadinone. In vitro studies showed no interaction at the level of hepatic metabolism with amitriptyline, salbutamol, glibenclamide and finasteride.

Concomitant use of tamsulosin with potent inhibitors of the CYP3A4 isoenzyme may lead to an increase in the effect of tamsulosin. When co-administered with ketoconazole (a known potent CYP3A4 inhibitor), the area under the concentration-time curve (AUC) Cmax of tamsulosin increases by a factor of 2.8 and 2.2, respectively. Tamsulosin should not be used concomitantly with potent CYP3A4 inhibitors in patients with a slow metabolism phenotype of the CYP2D6 isoenzyme. When tamsulosin was co-administered with paroxetine (a potent inhibitor of the CYP2D6 isoenzyme), the AUC and Cmax of tamsulosin increased 1.3 and 1.6 times, respectively, but this increase was not clinically significant.

How to take, course of use and dosage

Inside 0.4 mg (1 capsule) 1 time a day after the first meal (the time interval between taking the drug should be 24 hours). The capsule should be swallowed whole (it should not be chewed or crushed, as this may affect the rate of release of tamsulosin). No dose adjustment is required for mild to moderate hepatic or renal impairment. If the dose of 0.4 mg is intolerant, a dose of 0.2 mg per day is prescribed. If the dose of 0.2 mg or 0.4 mg was interrupted for two weeks (for any reason), then treatment should be started again with the same dosage. The duration of use is not limited, the drug is prescribed in the form of continuous therapy.

Overdose

There were no cases of acute overdose of the drug.

Symptoms. Acute arterial hypotension and compensatory tachycardia may occur.

Treatment. Symptomatic therapy is performed: giving the patient a horizontal position, if necessary – the introduction of plasma-substituting solutions or vasoconstrictor drugs. Kidney function should be monitored. Dialysis is unlikely to be effective, as tamsulosin is 99% bound to plasma proteins.

To prevent further absorption of tamsulosin, gastric lavage, taking activated charcoal or an osmotic laxative are possible.

Description

Dosage 0.2 mg: solid gelatin capsule No. 2, brown body and cap, with the inscription “HiGlance” in white on the cap.

Special instructions

Caution should be exercised in patients with severe renal insufficiency (creatinine clearance less than 10 ml / min), as with other alpha_-1-blockers. The drug should be used with caution in patients with a predisposition to orthostatic hypotension. At the first sign of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down and remain in this position until the above signs disappear. Before starting to use the drug, it is necessary to verify the diagnosis and exclude the presence of other diseases that may cause similar symptoms.

Before starting and regularly during therapy, a digital rectal examination should be performed and, if necessary, the determination of prostate specific antigen (PSA).

It is advisable to stop taking the drug 1-2 weeks before surgery for cataracts and glaucoma (while taking the drug, intraoperative instability of the iris may develop (narrow pupil syndrome), which should be taken into account by the surgeon for preoperative preparation of the patient and during surgery). Long-term erections and priapism have been reported with alpha-1-adrenoblockers. If the erection persists for 4 hours, you should immediately seek medical help. If priapism therapy is not carried out immediately, it can lead to penile tissue damage and permanent loss of potency.

1 capsule (0.2 mg or 0.4 mg) contains 0.26 g of carbohydrates, which corresponds to 0.026 XE (1 XE (bread unit) – 10 g of carbohydrates). The content of a minimum amount of carbohydrates allows you to prescribe the drug to patients with diabetes mellitus.

Influence on the ability to drive vehicles and mechanisms

During treatment, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, since the drug can cause dizziness and other side effects that may affect these abilities.

Form of production

For pharmacies: Modified release capsules 0.2 mg,04 mg. 10 capsules per Al / Al blister and / or PVDC/PVC / Al blister. 1,3,6 or 9 blisters each 10 (№10, №30, №60 or No. 90) capsules with instructions for medical use in a cardboard pack.

For hospitals: Modified release capsules 0.2 mg,04 mg. 100,500 or 1000 capsules in a PVC bag, a package with instructions for use in a high-density polyethylene jar.

Storage conditions

Store at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 4 years. Do not use after the expiration date.

Active ingredient

Tamsulosin

Conditions of release from pharmacies

By prescription

Dosage form

long-acting capsule