Glansin, 0.4 mg 30 pcs.

Pharmacological group: α₁-adrenoblocker.

ATX code: G04CA02.

Pharmacological properties

Pharmacodynamics:

Tamsulosin is a specific blocker of postsynaptic α₁-adrenoreceptors located in the smooth muscle of the prostate, bladder neck and prostatic urethra. Blockade of α₁-adrenoreceptors by tamsulosin leads to reduction of the tone of the smooth muscles of the prostate, bladder neck and prostatic part of the urethra and improves the outflow of urine. Simultaneously both symptoms of emptying and symptoms of bladder filling caused by increased tone of smooth muscles and detrusor hyperactivity in benign prostatic hyperplasia are reduced.

The ability of tamsulosin to affect α_1A subtype of adrenoreceptors is 20 times greater than its ability to interact with α_1b subtype of adrenoreceptors located in vascular smooth muscle. Due to its high selectivity, the drug does not cause clinically significant reduction of systemic arterial blood pressure (BP) both in patients with arterial hypertension and in patients with normal baseline BP. The drug has prolonged action (with modified release).

Pharmacokinetics:

Tamsulosin is well absorbed in the intestine and has almost 100% bioavailability. Absorption of tamsulosin is somewhat slower after a meal. The same level of absorption can be achieved if the patient takes the drug after the usual breakfast each time. Tamsulosin is characterized by linear kinetics. After a single oral intake of 0.4 mg capsule on an empty stomach, the maximum concentration (C_max) 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, with its value being approximately 2/3 that of this parameter after taking a single dose. Binding to plasma proteins is 99%. The volume of distribution is insignificant and is about 0.2 l/kg. Tamsulosin is slowly metabolized in the liver to form less active metabolites. Most of tamsulosin is present in plasma unchanged.

In mild to moderate hepatic impairment no dosing regimen 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 in single use of tamsulosin capsule in dose of 0.4 mg after a meal is 10 hours; in case of use over several days – 13 hours.

In case of renal failure no dose reduction is required; in patients with severe renal failure (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).

Pharmacological effect

Pharmacological group: α1-adrenergic 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 gland, bladder neck and prostatic urethra. Blockade of α1-adrenergic receptors by tamsulosin leads to a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and prostatic urethra and improves urine outflow. 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 α1A subtype of adrenergic receptors is 20 times greater than its ability to interact with the α1B subtype of adrenergic receptors, 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 initial blood pressure. The drug has a prolonged action (modified release).

Pharmacokinetics:

Tamsulosin is well absorbed from the intestine and has almost 100% bioavailability. The absorption of tamsulosin slows down somewhat after eating. The same level of absorption can be achieved if the patient takes the drug after a normal breakfast each time. Tamsulosin is characterized by linear kinetics. After a single oral administration of a 0.4 mg capsule on an empty stomach, the maximum concentration (Cmax) of tamsulosin in the blood plasma is achieved after 6 hours. When taken orally, a capsule of 0.4 mg per day for several days, the equilibrium concentration is achieved by the 5th day, while its value is approximately 2/3 higher than the value of this parameter after taking a single dose. Plasma protein binding 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 tamsulosin is present in the blood plasma unchanged.

For mild to moderate liver failure, no dosage adjustment is required.

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

In case of renal failure, no dose reduction is required; if the patient has severe renal failure (creatinine clearance less than 10 ml/min), tamsulosin should be prescribed with caution.

Special instructions

The drug should be prescribed with caution in case of severe renal failure (creatinine clearance less than 10 ml/min), as with other α1-blockers. The drug should be used with caution in patients with a predisposition to orthostatic hypotension. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down and remain in this position until the above symptoms disappear. Before starting to use the drug, it is necessary to verify the diagnosis and exclude the presence of other diseases that can cause similar symptoms.

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

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 syndrome (narrow pupil syndrome) may develop, which must be taken into account by the surgeon for preoperative preparation of the patient and during the operation). There are reports of cases of the development of prolonged erection and priapism during therapy with alpha1-adrenoblockers. If an erection persists for 4 hours, you should immediately seek medical help. If treatment for priapism is not carried out immediately, it can lead to damage to the tissue of the penis and irreversible 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 the drug to be prescribed to patients with diabetes.

Impact on the ability to drive vehicles and machinery

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, because the drug may cause dizziness and other side effects that may affect these abilities.

Active ingredient

Tamsulosin

Composition

Each modified release capsule contains:

Active ingredient:

tamsulosin hydrochloride pellets 0.2%* – 200 mg, containing tamsulosin hydrochloride – 0.4 mg

Pellet excipients: granulated sugar [sucrose, starch syrup] 182.66 mg, ethylcellulose 1.6 mg, methyl acrylic acid and ethyl acrylate copolymer [1:1] 14.1 mg, macrogol-6000 1.24 mg

Excipients: granulated sugar [sucrose, starch syrup] 60.0 mg

Capsule cap: gelatin 20.4792 mg, water 3.4800 mg, azorubine dye 0.0216 mg, sodium lauryl sulfate 0.0190 mg

Capsule body: gelatin 33.3138 mg, water 5.6550 mg, sodium lauryl sulfate 0.0312 mg

Ink for writing on the capsule shell: ethanol 30-34%, 2-propanol 3-6%, butanol 3-5%, propylene glycol 0.5-2%, shellac 20-24%, black iron oxide dye 20-24%

*in the pellet production process, 2-propanol (USP) and water (BP) are used as solvents, which are not contained in the finished product.

Pregnancy

The drug Glansin is intended for use only in males.

Contraindications

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

With caution – severe renal failure (creatinine clearance less than 10 ml/min); arterial hypotension when used simultaneously with α1-blockers.

Side Effects

Gradation of the frequency of side effects:

very often >1/10

often >1/100 to <1/10

uncommon > 1/1000 to < 1/100

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

very rare from <1/10,000, including isolated reports.

From the cardiovascular system: infrequently – palpitations, 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. From the respiratory system, chest and mediastinum: infrequently – rhinitis, very rarely – nosebleeds. Skin and subcutaneous tissue disorders: uncommon – rash, itching, urticaria; rarely – angioedema (including Quincke’s edema); very rarely – Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis. General condition disorders: infrequently – asthenia. Other: intraoperative instability of the iris (small pupil syndrome) during cataract surgery in patients taking tamsulosin.

Interaction

When used simultaneously with cimetidine, a slight increase in the concentration of tamsulosin in the blood plasma was observed, 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 elimination rate of tamsulosin. Concomitant use of tamsulosin with other α1-adrenergic receptor antagonists may lead to a decrease in blood pressure. When taken simultaneously with atenolol, enalapril, nifedipine, no drug interactions were detected. Diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not change the free fraction of tamsulosin in human plasma in vitro. Tamsulosin does not change 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 increased effects of tamsulosin. When used concomitantly with ketoconazole (a known potent inhibitor of CYP3A4), the area under the concentration-time curve (AUC) of tamsulosin Cmax increases by a factor of 2.8 and 2.2, respectively. Tamsulosin should not be used concomitantly with strong CYP3A4 inhibitors in patients with a poor CYP2D6 metabolizer phenotype. With simultaneous use of tamsulosin with paroxetine (a potent inhibitor of the CYP2D6 isoenzyme), the AUC and Cmax of tamsulosin increased by 1.3 and 1.6 times, respectively, but this increase was not clinically significant.

Overdose

There were no cases of acute overdose of the drug.

Symptoms. Acute arterial hypotension and compensatory tachycardia may occur.

Treatment. Symptomatic therapy is carried out: placing the patient in a horizontal position, and, if necessary, administering plasma-substituting solutions or vasoconstrictor drugs. It is necessary to monitor kidney function. It is unlikely that dialysis will be effective since tamsulosin is 99% bound to plasma proteins.

To prevent further absorption of tamsulosin, gastric lavage, activated charcoal or an osmotic laxative may be taken.

Storage conditions

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

Shelf life

4 years. Do not use after expiration date.

Manufacturer

Highglans Laboratories Pvt. Ltd, India