TAMSULOSIN MODIFIED RELEASE CAPSULES 0,4MG

Trade name:

Tamsulosin Canon

International non-proprietary or grouping name tamsulosin

Dosage Form

Enteric capsules with prolonged release.

Composition

1 capsule contains:

active substance: Tamsulosin substance-pellets 0.133% - 300 mg:

active substance: tamsulosin hydrochloride 0.4 mg,

Excipients: Hypromellose E5 (hydroxy-propylmethylcellulose) 1.9132 mg, dibutyl phthalate 0.2088 mg, starch 55 mg, macrogol 6000 (polyethylene glycol 6000) 6.2058 mg, methacrylic acid and ethyl acrylate copolymer (1: 1) 62.0585 mg, sodium lauryl sulfate 0.2 mg, sucrose 165 mg, talc 7.5358 mg, ethyl cellulose 1.7748 mg, Magnesium stearate 1.5 mg, talc 1.5 mg.

hard gelatin capsule number 2:

case - gelatin 37.3478 mg, iron oxide yellow 0.3811 mg, titanium dioxide 0.3811 mg;

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

Pharmacotherapeutic group:

alpha-1 blocker.

Pharmacological properties

Pharmacodynamics

Tamsulosin is a specific postsynaptic blocker.
alpha-l-adrenoreceptors, located in the smooth muscles of the prostate gland, bladder neck and prostatic urethra. The blockade of alpha-1-adrenergic receptors with tamsulosin leads to a decrease in the tone of the smooth muscles of the prostate gland, the bladder neck and the prostatic part of the urethra and the improvement of urine flow.At the same time, both emptying symptoms and filling symptoms due to increased smooth muscle tone and detrusor hyperactivity in benign prostatic hyperplasia (BPH) are reduced.

The ability of tamsulosin to affect the alpha-l-A subtype of adrenergic receptors is 20 times greater than its ability to interact with the alpha-l-B subtype of adrenergic receptors, which are located in vascular smooth muscle. Due to its high selectivity, tamsulosin does not cause a clinically significant reduction in systemic arterial pressure (BP) in patients with arterial hypertension, or in patients with normal baseline blood pressure.

Pharmacokinetics

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

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

Metabolism: Tamsulosin is slowly metabolized in the liver to form less active metabolites. Most tamsulosin is present in plasma in unchanged form.

The experiment revealed the ability of tamsulosin to slightly induce the activity of microsomal liver enzymes.

With an insignificant and moderate degree of liver failure, no correction of the dosing regimen is required.

Excretion: Tamsulosin and its metabolites are mainly excreted in the urine, with about 9% of the drug being excreted unchanged.

The half-life of the drug (T1/2,) with a single dose of 0.4 mg after a meal is 10 hours, with multiple - 13 hours.

In case of renal insufficiency, a dose reduction is not required, if the patient has severe renal insufficiency (creatinine clearance (QC) less than 10 ml / min), the administration of tamsulosin should be carried out with caution.

Indications for use

Treatment of dysuric disorders in benign prostatic hyperplasia.

Contraindications

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

Carefully

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

Use during pregnancy and during breastfeeding

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

Dosage and administration

Adults over 18 and older patients

Inside, after breakfast, drinking water, take 1 capsule (0.4 mg) 1 time per day. The capsule is not recommended to chew, as this may affect the rate of release of the active substance.

In patients with impaired liver and kidney function

In renal failure, as well as in mild and moderate liver failure, no dosage regimen is required.

Side effect

The frequency of side effects that develop when taking tamsulosin is classified according to the recommendations of the World Health Organization:

very often - at least 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%, but less than 0.1%;

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

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

Nervous system disorders:

often - dizziness (1.3%);

infrequently - headache;

seldom - fainting;

Heart disorders:

infrequently - feeling of heartbeat;

frequency not known - Atrial fibrillation, arrhythmia, tachycardia and shortness of breath;

Vascular disorders:

infrequently -postural hypotension;

Disorders of the respiratory system, organs of the chest and mediastinum:

infrequently - rhinitis;

Violations of the gastrointestinal tract:

infrequently - constipation, diarrhea, nausea, vomiting;

Violations of the skin and subcutaneous tissues:

infrequently - rash, pruritus, urticaria;

seldom - angioedema;

very rarely - Stevens-Johnson syndrome;

frequency is unknown - erythema multiforme, exfoliative edema.

Violations of the genital and breast organs:

often - impaired ejaculation;

very rarely - priapism;

Other:

infrequently - asthenia;

Other:

Infrequently - asthenia;

frequency unknown - described cases of intraoperative instability of the iris (narrow pupil syndrome) during surgery for cataracts and glaucoma in patients taking tamsulosin.

Overdose

There are no reports of cases of acute overdose with tamsulosin. However, theoretically, an overdose may develop a sharp decrease in blood pressure and compensatory tachycardia, in which case symptomatic therapy is necessary. Blood pressure and heart rate can recover when a person assumes a horizontal position. In the absence of effect, it is possible to apply agents that increase the volume of circulating blood and, if necessary, vasoconstrictor agents. It is necessary to monitor the function of the kidneys. Conducting hemodialysis is impractical because tamsulosin is strongly associated with plasma proteins.

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

Interaction with other drugs

When prescribing the drug Tamsulosin, Canon along with Atenolol, Enalapril or Nifedipine interactions were found.

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

Diazepam, propranolol, trichloromethiazide, 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, trichloromethiazide and chlormadinone.

Diclofenac and warfarin may increase the rate of elimination of tamsulosin.

The simultaneous administration of tamsulosin with strong inhibitors of the CYP3A4 isoenzyme may lead to an increase in the concentration of tamsulosin. Co-administration with Ketoconazole (a strong CYP3A4 inhibitor) has resulted in an increase in AUC and Cmax tamsulosin 2.8 and 2.2 times, respectively.

Tamsulosin should not be used in combination with strong inhibitors of CYP3A4 in patients with impaired metabolism of the isoenzyme CYP2D6. The drug should be used with caution in combination with strong and moderate inhibitors of CYP3A4.

Simultaneous administration of tamsulosin and paroxetine, a strong inhibitor of CYP2D6, led to an increase in Cmax and Ams of tamsulosin 1.3 and 1.6 times, respectively, but this increase was considered clinically insignificant.

The simultaneous appointment of other antagonists of alpha-l-adrenergic receptors can lead to a decrease in blood pressure.

When tamsulosin is used together with cholinesterase inhibitors, alprostadiol, anesthetics, diuretics, levodopa, muscle relaxants, nitrates, antidepressants, beta-blockers, slow Calcium channel blockers and ethanol, there may be a risk of marked reduction in blood pressure.

special instructions

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

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

There are reports of cases of prolonged erection and priapism during therapy with alpha1-blockers.If an erection persists for more than 4 hours, you should immediately seek medical attention. If priapism therapy was not carried out immediately, it can cause damage to the tissues of the penis and irreversible loss of potency.

Treatment with Tamsulosin Canon in patients with severe renal insufficiency (creatinine clearance <10 ml / min) requires caution, since studies in this category of patients was not conducted.

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