Tamsulosin Canon - instructions for use, dose, side effects, contraindications

Excipients: hypromellose E5 (hydroxypropilmetiltsellyuloza) 1.9132 mg, 0.2088 mg of dibutyl phthalate, 55 mg of starch, macrogol 6000 (polyethylene glycol 6000) 6.2058 mg, methacrylic acid-ethyl acrylate copolymer (1: 1) 62.0585 mg, 0.2 mg sodium lauryl sulfate, sucrose 165 mg talc 7.5358 mg, 1.7748 mg ethylcellulose, magnesium stearate 1.5 mg talc 1.5 mg.

hard gelatin capsule №2:

housing - gelatin 37,3478 mg, iron oxide yellow 0.381 1 mg, titanium dioxide 0.3811 mg;

cap - gelatin 22.4322 mg, iron oxide yellow 0.2289 mg, titanium dioxide 0.2289 mg.

Description:Hard gelatin capsules number 2, body and lid yellow.

The contents of capsules are white or almost white spherical granules.

Pharmacotherapeutic group:alpha1-blocker

ATX: & nbsp

G.04.C.A.02 Tamsulosin

Pharmacodynamics:

Tamsulosin is a specific blocker of postsynaptic alpha-1 adrenergic receptors located in the smooth muscle of the prostate, bladder neck and prostatic urethra.Blockade of alpha-1-adrenergic receptors with tamsulosin leads to a decrease in the tone of the smooth muscles of the prostate gland, the neck of the bladder and the prostatic part of the urethra, and an improvement in the outflow of urine. At the same time, both the symptoms of emptying and the filling symptoms caused by an increased tone of smooth muscle and de-hyperactive hypertension in benign prostatic hyperplasia (BPH) decrease both.

The ability of tamsulosin to affect the alpha-1-A subtype of adrenoreceptors is 20 times greater than its ability to interact with the alpha-1-B subtype of adrenoreceptors that are located in the smooth muscle of the vessels. Due to its high selectivity, tamsulosin does not cause a clinically significant decrease in systemic arterial pressure (BP) in both patients with arterial hypertension and in patients with normal initial BP.

Pharmacokinetics:

Suction: tamsulosin is well absorbed in the intestine and has almost 100% bioavailability. Absorption of tamsulosin somewhat slows down after eating. The same level of absorption can be achieved if the patient takes the drug every time after a normal breakfast. Tamsulosin characterized by linear kinetics. After a single oral intake of 0.4 mg of the drug, its maximum concentration in the plasma (C_mOh) is reached after 6 hours. After repeated intake of 0.4 mg per day, the equilibrium concentration (C_ss) is reached by the 5th day, while its value is about 2/3 higher than the value of this parameter after taking a single dose.

Distribution: the connection with plasma proteins is 99%, the volume of distribution is small (about 0.2 l / kg).

Metabolism: tamsulosin It is slowly metabolized in the liver with the formation of less active metabolites. Most of the tamsulosin is present in plasma in unchanged form.

In the experiment, the ability of tamsulosin to induce insignificantly the activity of microsomal liver enzymes was revealed.

With a slight and moderate degree of hepatic insufficiency, there is no need for correction of the dosing regimen.

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

The half-life of the drug (T_1/2) with a single intake of 0.4 mg after a meal is 10 hours, with a multiple of 13 hours.

When renal failure is not required to reduce the dose, if the patient has severe renal failure (creatinine clearance (CC) less than 10 ml / min), the appointment of tamsulosin should be done with caution.

Indications:

Treatment of dysuric disorders in benign prostatic hyperplasia.

Contraindications:

Hypersensitivity to tamsulosin or any other component of the drug; deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption; orthostatic hypotension (including in the anamnesis); severe hepatic impairment; children's age till 18 years.

Carefully:

Severe renal insufficiency (creatinine clearance less than 10 ml / min); arterial hypotension.

Pregnancy and lactation:

The drug Tamsulosin Canon 0.4 mg in capsules is intended for use only in males.

Dosing and Administration:

Adults over 18 years, as well as elderly patients

Inside, after breakfast, washing down with water, take 1 capsule (0.4 mg) 1 time per day. Capsule is not recommended to chew, as this can affect the release rate of the active substance.

In patients with impaired liver and kidney function

With renal failure, as well as with mild and moderate hepatic insufficiency, correction of the dosing regimen is not required.

Side effects:

The incidence of side effects developing with tamsulosin is classified according to the recommendations of the World Health Organization:

very often - not less than 10%;

often - not less than 1%, but less than 10%;

infrequently - not less than 0,1%, but less than 1%;

rarely - not less than 0,01%, less than 0,1%;

very rarely - less than 0.01%, including individual reports;

the frequency is unknown - there is no information on the incidence of side effects.

Disturbances from the nervous system:

often - dizziness (1.3%);

infrequently - headache;

rarely - fainting;

Heart Disease:

infrequently - a feeling of palpitations;

frequency not known - Atrial fibrillation, arrhythmia, tachycardia and dyspnea;

Vascular disorders:

infrequently - postural hypotension;

Disturbances from the respiratory system, organs of the chest and the mediastinum:

infrequently - rhinitis;

Disorders from the gastrointestinal tract:

infrequently - constipation, diarrhea, nausea, vomiting;

Disturbances from the skin and subcutaneous tissues:

infrequently - a rash, itching, hives;

rarely - angioedema;

rarely - Stevens-Johnson syndrome;

frequency unknown - erythema multiforme, exfoliative edema.

Violations of the genitals and mammary gland:

often - violation of ejaculation;

rarely - priapism;

General disorders and disorders at the site of administration:

infrequently - asthenia;

Other:

infrequently - asthenia;

frequency unknown - cases of intraoperative instability of the iris of the eye (narrow-pupil syndrome) were described in the operation concerning cataract and glaucoma in patients taking tamsulosin.

Overdose:

There are no reports of cases of acute overdose with tamsulosin. However, theoretically, with an overdose, it is possible to develop an acute decrease in blood pressure and compensatory tachycardia, in which case symptomatic therapy is necessary. Blood pressure and heart rate can be restored when a person takes a horizontal position. In the absence of effect, it is possible to use agents that increase the volume of circulating blood and, if necessary, vasoconstrictors.It is necessary to monitor kidney function. Conducting hemodialysis is inadvisable, since tamsulosin strongly associated with plasma proteins.

To prevent further absorption of the drug, it is advisable to wash the stomach, taking activated charcoal or osmotic laxative, for example magnesium sulfate.

Interaction:

When the drug was prescribed, Tamsulosin canon, together with atenolol, enalapril or nifedipine, was not detected.

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

Diazepam, propranolol, trichloromethiazide, chloromadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not change the free fraction of tamsulosin in human plasma in vitro.

In its turn, tamsulosin also does not change free fractions of diazepam, propranolol, trichloromethiazide and chloromadinone.

Diclofenac and warfarin can increase the rate of excretion of tamsulosin.

Simultaneous administration of tamsulosin with strong inhibitors of isoenzyme CYP3A4 can lead to an increase in the concentration of tamsulosin. Simultaneous administration with ketoconazole (strong inhibitor CYP3A4) led to an increase AUC and C_mOh tamsulosin in 2.8 and 2.2 times, respectively.

Tamsulosin should not be used in combination with strong inhibitors CYP3A4 in patients with a metabolic isoenzyme disorder CYP2D6.

The drug should be used with caution in combination with strong and moderate inhibitors CYP3A4.

Simultaneous administration of tamsulosin and paroxetine, a strong inhibitor CYP2D6, led to an increase in C_mOh and AUC tamsulosin in 1.3 and 1.6 times, respectively, but this increase is clinically insignificant.

Simultaneous administration of other antagonists of alpha-1-adrenergic receptors may lead to a decrease in blood pressure.

With the simultaneous use of tamsulosin with cholinesterase inhibitors, alprostadiol, anesthetics, diuretics, levodopa, muscle relaxants, nitrates, antidepressants, beta-adrenergic blockers, slow calcium channel blockers and ethanol, there is a risk of a marked decrease in blood pressure.

Special instructions:

As with the use of other alpha-1-adrenoblockers, in the treatment with Tamsulosin Canon, in some cases there may be a decrease in blood pressure, which can sometimes lead to a fainting condition. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down and remain in this position until these symptoms disappear.

Before starting therapy with tamsulosin, the patient should be examined to exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before the start of treatment and regularly during therapy, a digital rectal examination and, if necessary, the definition of a prostatic specific antigen (PSA) should be performed.

There are reports of cases of development of prolonged erection and priapism against the background of therapy with alpha1-adrenergic blockers. If the erection persists for more than 4 hours, you should immediately seek medical help. If priapism therapy has not been carried out immediately, it can lead to damage to the tissues of the penis and an irreversible loss of potency.

Treatment with Tamsulosin Canon for patients with severe renal insufficiency (creatinine clearance <10 mL / min) requires caution, studies in this category of patients have not been conducted.

In some patients who have or have previously taken tamsulosin during the surgery for cataracts or glaucoma may develop a syndrome of intraoperative irrosis of the eye (narrow pupil's syndrome), which can lead to complications during surgery or in the postoperative period. The feasibility of canceling tamsulosin therapy 1-2 weeks before surgery for cataracts or glaucoma has not been proven. Cases of intraoperative iris of the iris occurred in patients who stopped taking the drug, and at an earlier time before the operation. It is not recommended to begin therapy with tamsulosin in patients who are scheduled for surgery for cataracts or glaucoma. During the preoperative examination of the patients, the surgeon and the ophthalmologist must consider whether the patient is taking or taking the patient tamsulosin. This is necessary to prepare for the possibility of development during the operation of intraoperative iris of the eye.

If angioedema develops, the drug should be discontinued immediately. Re-administration of tamsulosin is contraindicated.

Effect on the ability to drive transp. cf. and fur:

Care must be taken when driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, due to the fact that dandruff may develop with tamsulosin.

Form release / dosage:Capsules intestine-soluble with prolonged release, 0,4 mg.

Packaging:

For 10 or 15 capsules in a contour mesh package made of a PVC film or a PVC / PCTFE film or aluminum multilayer foil and aluminum lacquered aluminum foil.

According to 1, 3, 6, 9 contour cell packs of 10 capsules or 2, 4, 6 contour cell packs of 15 capsules together with instructions for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C, in the manufacturer's packaging.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003936

Date of registration:03.11.2016

Expiration Date:03.11.2021

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp23.11.2016

Illustrated instructions

Instructions

Tamsulosin Canon (Tamsulosin Canon)