Tamselin, 0.4 mg capsules 30 pcs

Pharmacotherapeutic group: alpha 1-adrenoblocker

ATC code: G04CA02

Pharmacodynamics:

Selectively and competitively blocks postsynaptic alpha 1a-adrenoreceptors located in the smooth muscle of the prostate bladder neck and the prostatic part of the urethra. Decreases the tone of the smooth muscle of the prostate bladder neck and the prostatic part of the urethra, improving the outflow of urine. Simultaneously the symptoms of obstruction and irritation of the urinary tract associated with benign prostatic hyperplasia are reduced.

Therapeutic effect occurs within 2 weeks after the start of treatment. Its tropism to alpha1a-adrenoreceptors in the urinary bladder is 20 times higher than its ability to interact with alpha 1b-adrenoreceptors in the vascular smooth muscle. Due to this high selectivity, it does not cause any clinically significant reduction in systemic blood pressure in patients with arterial hypertension as well as in patients with normal baseline blood pressure.

Pharmacokinetics:

The absorption is high (more than 90%). Maximum plasma concentration after a single oral administration of 04 mg is reached after 6 hours. Binding with plasma proteins is 94-99 %. The volume of distribution is insignificant – 02 l/kg.

It is slowly metabolized in the liver to form pharmacologically active metabolites. Most of it is present in blood unchanged. It is excreted by kidneys (4-9% unchanged). Half-life period is 10-12 hours.

Indications

Benign prostatic hyperplasia (treatment of dysuric disorders).

Active ingredient

Composition

Composition per capsule:

The active ingredient:

Tamsulosin hydrochloride pellet 0.15% 267 mg containing 0.4 mg tamsulosin hydrochloride.

Pellet excipients: sucrose 143.36 mg, starch 95.58 mg, ethyl cellulose 3.74 mg, hypromellose 2.56 mg, povidone K-30 1.5 mg, copovidone (plasdon S-630) 2.54 mg, hypromellose phthalate 10.4 mg, cetyl alcohol 1.0 mg, diethyl phthalate 0.35 mg, talc 5.47 mg.

Composition of the gelatin capsule: Gelatin – 62.306465 mg

Caps:

Dyes: Brilliant black – 0.0065 mg, Patent blue – 0.00715 mg, Quinoline yellow – 0.00871 mg, Iron oxide yellow – 0.071175 mg, Titanium dioxide – 1.3 mg

Base: Dyes: Titanium dioxide -1.3 mg.

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How to take, the dosage

Ingestion, after breakfast. It is recommended not to chew the capsule and to drink a small amount of water.

Adults over 18 years of age and elderly patients: 1 capsule (0.4 mg) once daily. Patients with impaired hepatic and renal function:

In mild to moderate renal and hepatic impairment, no dose adjustment is required.

Interaction

No drug interactions have been found with atenolol, enalapril and nifedipine when concomitant use.

Concomitant use with cimetidine increases tamsulosin serum concentration, when administered with furosemide it decreases. However, correction of the drug dose is not required, since the concentration of tamsulosin remains in the therapeutic range.

Diazepam, propranololol, trichloromethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not change plasma levels of free tamsulosin fraction in vitro.

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

Diclofenac and warfarin may increase the excretion rate of tamsulosin. Concomitant use with strong inhibitors of CYP34A isoenzyme may lead to increased concentration of tamsulosin.

Concomitant use with ketoconazole led to an increase in the area under the pharmacokinetic curve “concentration-time” (AUC) and maximum concentration (Cmax) by 2.8 and 2.2 times, respectively.

Tamsulosin hydrochloride should not be used in combination with strong CYP34A isoenzyme inhibitors in patients with impaired CYP2D6 isoenzyme metabolism. The drug should be used with caution in combination with strong, moderate inhibitors of CYP34A isoenzyme.

Concomitant administration of tamsulosin and paroxetine results in a 1.3-fold and 1.6-fold increase in the area under the pharmacokinetic concentration-time curve (AUC) and maximum concentration (Cmax), respectively.

The concomitant administration of other α1-adrenoreceptor antagonists may increase the hypotensive effect.

Special Instructions

As with other α1-adrenoblockers, treatment with tamsulosin may occasionally produce a decrease in blood pressure (BP), which may sometimes lead to fainting. At the first signs of orthostatic hypotension (dizziness, weakness) the patient should sit or lie down and remain in this position until the signs disappear.

In surgical interventions for cataract with the drug administration, development of intraoperative iris instability syndrome (narrow pupil syndrome) may occur, which should be taken into account by the surgeon during the preoperative preparation of the patient and during the operation.

It is not recommended to initiate tamsulosin therapy in patients who are scheduled for cataract or glaucoma surgery. The surgeon or ophthalmologist should consider whether the patient is taking tamsulosin during the surgical evaluation prior to surgery.

Before starting therapy with the drug, the patient should be examined to rule out the presence of other conditions that may cause the same symptoms as benign prostatic hyperplasia. A rectal palpate examination and, if necessary, prostate-specific antigen testing should be performed before starting treatment and at regular intervals thereafter.

There have been reports of cases of prolonged erections and priapism on therapy with α1-adrenoblockers. If an erection persists for four hours, immediate medical attention should be sought. If therapy of priapism is not carried out immediately, it may lead to penile tissue damage and irreversible loss of potency.

Influence on driving, operating machinery

At the time of treatment, caution should be exercised when driving vehicles and performing potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Hypersensitivity to tamsulosin or any excipient of the drug.

Serious hepatic insufficiency. Orthostatic hypotension (including history). Childhood under 18 years of age.

With caution

Severe renal insufficiency (CKR less than 10 ml/min).

Arterial hypotension.

Side effects

According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: Very common (≥1/10), common (≥1/100, < 1/10), infrequent (≥1/1000, < 1/100), rare (≥1/10000, < 1/1000), very rare (< 1/10000); frequency unknown – the incidence could not be determined from available data.

Nervous system disorders frequently: dizziness; infrequently: headache; rarely: fainting, sleep disturbance (drowsiness or insomnia).

An organ of vision: frequency unknown: blurred vision, visual impairment.

Cardiovascular system side:

infrequent: postural hypotension, tachycardia, palpitations;

rare: chest pain, atrial fibrillation.

Respiratory system infrequent: rhinitis, shortness of breath;

frequency unknown: nasal bleeding. Gastrointestinal tract infrequent: constipation, diarrhea, nausea, vomiting.

Skin and subcutaneous tissue infrequent: rash, itching, urticaria;

rare: angioedema;

very rare: Stevens-Johnson syndrome;

frequency unknown: polymorphic erythema, exfoliative dermatitis.

Other:

often: ejaculation disorders, including retrograde ejaculation and ejaculatory failure;

infrequent: asthenia, back pain, narrow pupil syndrome during cataract surgery;

very rare: priapism, decreased libido.

In post-registration observations, cases of intraoperative iris instability syndrome (narrow pupil syndrome) during cataract and glaucoma surgery were identified in patients taking tamsulosin. During post-registration observations, in addition to the adverse events described above, cases of atrial fibrillation, arrhythmias, tachycardia, and dyspnea associated with tamsulosin use have been described. Because these spontaneous reports were reported in the study after the drug was placed on the market worldwide, it is not possible to reliably estimate the frequency of these events and their association with tamsulosin use.

Overdose

Symptoms

Tamsulosin hydrochloride overdose has the potential to cause acute hypotensive effects. Such effects have been reported in a variety of overdose conditions.

Treatment

In case of overdose and development of hypotension, it is recommended that the patient be transferred to a horizontal position and measures be taken to support cardiovascular activity (restoration of blood pressure and heart rate); gastric lavage, administration of activated charcoal and osmotic laxatives such as sodium sulfate. If there is no effect, substances that increase circulating blood volume and, if necessary, vasoconstrictors should be administered. Renal function should be monitored and general supportive measures should be taken. Dialysis is unlikely to be effective since tamsulosin is largely bound to plasma proteins.

Pregnancy use

Similarities