Omnik okas tablets coated with ob. with counter.highlight. 0.4 mg No. 30

Pharmacological properties of the drug Omnic ocas

Pharmacodynamics. Tamsulosin selectively and competitively blocks postsynaptic α1-adrenergic receptors, especially α1A and α1D subtypes located in the smooth muscles of the prostate gland, bladder neck, prostatic urethra and detrusor. This causes a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and prostatic urethra and an improvement in urine outflow. At the same time, the severity of symptoms of obstruction (emptying) and irritation (filling) of the bladder associated with benign prostatic hyperplasia decreases. The described effect of the drug on symptoms of obstruction and irritation persists with prolonged use. The ability of α1A-adrenergic receptor blockers to reduce blood pressure is associated with a decrease in peripheral vascular resistance. Omnic Okas in a daily dose of 0.4 mg does not cause a clinically significant decrease in systemic blood pressure both in patients with hypertension (arterial hypertension) and with normal initial blood pressure. Pharmacokinetics. Absorption. Omnic Okas is a prolonged-release tablet with a controlled release of the active substance based on a matrix using a non-ionic gel. This dosage form provides a prolonged and slow release of tamsulosin, which ensures exposure of the active substance with minor fluctuations over 24 hours. After oral administration, 57% of tamsulosin is absorbed in the intestine. The rate and extent of absorption do not depend on food intake. Tamsulosin has linear pharmacokinetics. After a single dose of Omnic Okas on an empty stomach, the maximum concentration of the active substance in the blood plasma is achieved after 6 hours. In the equilibrium state, which is achieved on the 4th day of taking the drug, the maximum concentration is observed after 4-6 hours, regardless of food intake. The maximum plasma concentration increases from 6 ng/ml after the first dose to 11 ng/ml at steady state. As a result of prolonged release, the minimum plasma concentration of tamsulosin is 40% of the maximum concentration, regardless of food intake. Distribution . Plasma protein binding - 99%. The volume of distribution is insignificant - up to 0.2 l/kg body weight. Metabolism. Tamsulosin hydrochloride is not subject to the first pass effect through the liver and is slowly metabolized in the liver to form pharmacologically active metabolites that retain high selectivity for α1A-adrenergic receptors. Most of the active substance is found in the blood unchanged. Excretion. Tamsulosin hydrochloride is excreted in the urine, 4–6% unchanged. The half-life of tamsulosin with a single dose and at steady state is 19 and 15 hours, respectively.

Omnik Okas tab with controlled release 0.4 mg No. 30

Compound

Active substance: tamsulosin hydrochloride 400 mcg.
Excipients: macrogol 8000 - 40 mg, macrogol 7 000 000 - 200 mg, magnesium stearate - 1.2 mg. Shell composition: yellow opadry 03F22733 - 7.25 mg (hypromellose - 69.536%, macrogol 8000 - 13.024%, yellow iron oxide dye - 17.44%).

Pharmacokinetics

After oral administration, tamsulosin is quickly and almost completely absorbed from the gastrointestinal tract. After a single oral dose of 400 mcg, the Cmax of the active substance in plasma is achieved after 6 hours.

Plasma protein binding - 99%. Vd 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 α1A-adrenergic receptors. Most of the active substance is present in the blood unchanged.

T1/2 of tamsulosin with a single dose is 10 hours, terminal T1/2 is 22 hours. It is excreted by the kidneys, 9% unchanged.

Indications for use

Benign prostatic hyperplasia.

Contraindications

• Hypersensitivity to tamsulosin.
• Orthostatic hypotension.
• Severe liver failure.

With caution: Chronic renal failure (creatinine clearance below 10 ml/min), severe liver dysfunction, arterial hypotension.

Directions for use and doses

Orally, 1 tablet 1 time per day, regardless of meals. The duration of use is not limited; the drug is prescribed as continuous therapy.

The tablet must be taken whole and should not be chewed as this may affect the prolonged release of the active substance.

Storage conditions

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

Best before date

3 years. Do not use after the expiration date stated on the package.

special instructions

During surgical interventions for cataracts while taking the drug, the development of intraoperative instability syndrome of the iris (narrow pupil syndrome) is possible, which must be taken into account by the surgeon for preoperative preparation of the patient and during the operation.

Before starting therapy with Omnic Ocas, the patient should be examined to exclude 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 and, if required, determination of prostate specific antigen (PSA) should be performed.

In case of renal failure, no dose change is required.

Description

Alpha1-adrenergic blocker.

Pharmacodynamics

α1-adrenergic receptor blocker; a drug for the symptomatic treatment of benign prostatic hyperplasia.

Selectively blocks postsynaptic α1A-adrenergic receptors of smooth muscles of the prostate gland, bladder neck, prostatic urethra. As a result, the tone of the smooth muscles of these formations decreases, and the outflow of urine is facilitated. At the same time, the symptoms of obstruction and irritation associated with benign prostatic hyperplasia are reduced. The therapeutic effect appears approximately 2 weeks from the start of treatment.

Tamsulosin's ability to block α1B-adrenergic receptors of vascular smooth muscles is much less pronounced, so the effect on systemic blood pressure is insignificant.

Side effects

From the cardiovascular system: rarely - dizziness, orthostatic hypotension, palpitations.

From the side of the central nervous system: headache, asthenia are possible.

From the reproductive system: rarely - retrograde ejaculation.

Use during pregnancy and breastfeeding

Not intended for women.

Interaction

With simultaneous use of tamsulosin with cimetidine, a slight increase in the concentration of tamsulosin in the blood plasma was noted, and with furosemide - a decrease in concentration; with other α1-blockers - a pronounced increase in the hypotensive effect is possible.

Diclofenac and indirect anticoagulants slightly increase the rate of elimination 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 showed no interaction at the level of hepatic metabolism with amitriptyline, salbutamol, glibenclamide and finasteride.

Other α1-blockers, acetylcholinesterase inhibitors, alprostadil, anesthetics, diuretics, levodopa, antidepressants, beta-blockers, slow calcium channel blockers, muscle relaxants, nitrates and ethanol may increase the severity of the hypotensive effect.

Overdose

Symptoms: decreased blood pressure, compensatory tachycardia.
Treatment is symptomatic. Blood pressure and heart rate can be restored when the patient takes a horizontal position. If there is no effect, you can use drugs that increase the volume of circulating blood and, if necessary, vasoconstrictors. It is necessary to monitor kidney function. It is unlikely that dialysis will be effective since tamsulosin is intensely bound to plasma proteins. To prevent further absorption of the drug, it is advisable to lavage the stomach, take activated charcoal and osmotic laxatives.

Impact on the ability to drive vehicles and operate machinery

There is no data on the negative impact on the ability to drive vehicles and engage in potentially hazardous activities. However, due to the possibility of dizziness, until the patient’s individual reaction is clarified, you should refrain from activities that require increased concentration and speed of psychomotor reactions, including driving.

Side effects of the drug Omnic ocas

Common side effects (1% but ≤10%) are dizziness (1.3%). Uncommon side effects (0.1%, but ≤1%) are headache, tachycardia, postural hypotension, rhinitis, constipation, diarrhea, nausea, vomiting, rash, urticaria, itching, retrograde ejaculation, asthenia. Rare side effects (0.01%, but ≤0.1%) are fainting, angioedema. Very rare (≤0.01%) - priapism. Cases of intraoperative instability of the iris (narrow pupil syndrome) during cataract surgery in patients taking tamsulosin for a long time have been described.

Special instructions for the use of the drug Omnic ocas

Like other α1-adrenergic receptor blockers, Omnic Ocas should be used with caution in patients with a tendency to orthostatic hypotension. At the first symptoms of orthostatic hypotension (dizziness, weakness), the patient should be seated or laid down. During surgery for cataracts while taking the drug, intraoperative instability of the iris (narrow pupil syndrome) may develop, which should be taken into account by the surgeon during the preoperative preparation of the patient and the operation. Before starting treatment and regularly during therapy, a digital rectal examination should be performed and, if necessary, a specific prostate antigen (PSA) should be determined in the blood. Patients with impaired renal function do not reduce the dose of the drug; the drug is prescribed with caution to patients with creatinine clearance below 10 ml/min. There are no data on use in children. There is no evidence of adverse effects on the ability to drive vehicles or operate potentially dangerous machinery.

Pharmacodynamics

Tamsulosin is a specific competitive blocker of postsynaptic α1-adrenergic receptors, especially the α1A and α1D subtypes, which are responsible for relaxing the smooth muscles of the prostate gland, bladder neck and prostatic urethra. Omnic Okas at a dosage of 0.4 mg increases the maximum speed of urination, and also reduces the tone of the smooth muscles of the prostate gland and urethra, improving the outflow of urine, etc. reducing the severity of bowel movements. Omnic Okas also reduces the severity of filling symptoms, in the development of which detrusor overactivity plays an important role.

With long-term therapy, the effect on the severity of filling and emptying symptoms is maintained, reducing the risk of developing acute urinary retention and the need for surgical intervention.

α1A-adrenergic blockers may lower blood pressure by reducing peripheral resistance. When using the drug Omnic Okas in a daily dose of 0.4 mg, no cases of clinically significant decrease in blood pressure were observed.

Interactions of the drug Omnic ocas

No interactions were observed with the simultaneous use of tamsulosin hydrochloride with atenolol, enalapril, nifedipine and theophylline. When the drug was used in combination with cimetidine, a slight increase in the concentration of tamsulosin in the blood plasma was observed, and with furosemide - a decrease in concentration, but this does not require a change in the dose of Omnica Ocas. Diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not change the free fraction of tamsulosin in human plasma. Tamsulosin also does not change the free fractions of diazepam, propranolol, trichlormethiazide and chlormadinone. In vitro, there was no effect of tamsulosin on the level of metabolism of amitriptyline, salbutamol, glibenclamide and finasteride by microsomal liver enzymes. Diclofenac and warfarin may increase the rate of elimination of tamsulosin. Concomitant treatment with other α1-adrenergic receptor antagonists can lead to a pronounced increase in the hypotensive effect.

Composition and release form

10 pcs in a blister made of PVC foil and aluminum foil laminated; in a cardboard pack 1 or 3 blisters.

Overdose of the drug Omnic ocas, symptoms and treatment

Cases of acute overdose of the drug have not been described. Theoretically, after an overdose of the drug, there is the possibility of developing acute hypotension, which requires the administration of cardiotropic therapy, monitoring of the function of the cardiovascular system and renal function. To prevent further absorption of the drug, gastric lavage, the use of activated charcoal or an osmotic laxative are indicated. Dialysis is not advisable due to the significant binding of tamsulosin to plasma proteins.

Overdose

Symptoms: decreased blood pressure, compensatory tachycardia.

Treatment: symptomatic. Blood pressure and heart rate can be restored when the patient assumes a horizontal position. If there is no effect, you can use drugs that increase blood volume and, if necessary, vasoconstrictors. It is necessary to monitor kidney function. It is unlikely that dialysis will be effective because... Tamsulosin binds intensively to plasma proteins.

To prevent further absorption of the drug, it is advisable to lavage the stomach, take activated charcoal and osmotic laxatives.