Proflosin (Tamsulosin) 0.4 mg

Active substances:

tamsulosin hydrochloride 400 mcg.

Excipients:

microcrystalline cellulose - 276.9 mg,

a copolymer of methacrylic acid and ethyl acrylate (1: 1) - 16.5 mg,

triethyl citrate - 1.65 mg, talc - 16.5 mg.

The composition of the pellet shell:

a copolymer of methacrylic acid and ethyl acrylate (1: 1) - 21.63 mg,

talcum powder - 8.65 mg,

triethyl citrate - 2.16 mg.

The composition of the capsule body:

iron oxide red oxide - 0.0239 mg,

titanium dioxide - 0.53 mg,

yellow iron oxide dye - 0.258 mg,

gelatin - 38.938 mg.

The composition of the capsule cap:

indigo carmine - 0.00152 mg,

iron oxide black oxide - 0.0107 mg,

titanium dioxide - 0.356 mg,

yellow iron oxide dye - 0.114 mg,

gelatin - 23.889 mg.

Pharmacodynamics

Tamsulosin selectively and competitively blocks postsynaptic α1A-adrenergic receptors located in the smooth muscles of the prostate gland, bladder neck and prostatic urethra. This leads to a decrease in the tone of smooth muscles of the prostate gland, bladder neck, prostatic urethra and an improvement in the outflow of urine.

Α-adrenoreceptor blockers can lower blood pressure (BP) by reducing peripheral vascular resistance. However, in clinical trials of tamsulosin, in patients with a normal level of blood pressure, there was no clinically significant decrease in blood pressure.

Pharmacokinetics

Suction

After oral administration, tamsulosin is rapidly and almost completely absorbed from the digestive tract. The absorption of tamsulosin is somewhat slowed after a meal. After a single oral administration of the drug in a dose of 0.4 mg, the maximum concentration (Cmax) of tamsulosin in the blood plasma is reached after about 6 hours.

Distribution

Communication with blood plasma proteins is about 99%, the distribution volume is small - 0.2 l / kg.

Metabolism

Tamsulosin does not undergo the “first pass” effect and is slowly metabolized in the liver to form less active metabolites. Most tamsulosin is present in the blood in an unchanged form. The experiment revealed the ability of tamsulosin to slightly induce the activity of microsomal liver enzymes.

Breeding

Tamsulosin and its metabolites are excreted mainly in the urine, 9% of the drug is excreted unchanged. The half-life (T1 / 2) of tamsulosin is approximately 10 hours (with a single dose after meals), with a regular intake of -13 hours.

Benign prostatic hyperplasia (treatment of dysuric disorders).

The drug is prescribed only to men.

• Hypersensitivity to tamsulosin or other components of the drug;
• orthostatic hypotension (including history);
• severe liver failure.

Precautions: chronic renal failure (CC less than 10 ml / min); arterial hypotension.

Possible side effects when using the drug are listed below in descending incidence:

• often (<1/10,> 1/100);
• infrequently (<1/100,> 1/1000);
• rarely (<1/1000,> 1/10000);
• very rarely (<1/10000), including individual messages.

Violations of the nervous system: often - dizziness; infrequently - a headache; rarely - fainting conditions.

Disorders from the CCC: infrequently - tachycardia, orthostatic hypotension.

Disorders from the gastrointestinal tract: infrequently - constipation, diarrhea, nausea, vomiting.

Violations of the reproductive system: infrequently - violation of ejaculation; very rarely - priapism.

Disturbances from the skin and subcutaneous tissues: infrequently - rash, skin itching, urticaria; rarely - angioedema.

Other: in some cases, the development of atonic iris syndrome (narrow pupil syndrome) during cataract surgery, asthenia, rhinitis.

Tamsulosin does not interact with atenolol, enalapril, nifedipine and theophylline.

With simultaneous use with cimetidine, a slight increase in the concentration of tamsulosin in plasma was noted; with furosemide - a decrease in concentration, but this does not require dose adjustment of the drug Proflosin®, since the concentration of the drug remains within the normal range.

Diclofenac and warfarin may increase the rate of tamsulosin excretion.

The simultaneous administration of tamsulosin with other a1-adrenergic blockers can lead to a decrease in blood pressure.

Inside, 1 capsule 1 time per day after breakfast or the first meal.

The capsule should be swallowed whole, without chewing, with a sufficient amount of water.

The capsule cannot be divided into parts or broken, as this can affect the rate of release of the active substance.

Duration of use is not limited.

Cases of overdose when taking the drug to date have not been observed. However, theoretically there is a likelihood of a sharp decrease in blood pressure and tachycardia, which may require appropriate measures.

To restore blood pressure (including with orthostatic hypotension) and heart rate to normal values, the patient must be laid down. Hemodialysis is impractical because tamsulosin has a high affinity for blood plasma proteins.

To prevent further absorption of tamsulosin, it is advisable to rinse the stomach, take activated charcoal or an osmotic laxative (for example, sodium sulfate).

At the first signs of orthostatic hypotension (dizziness, weakness), the patient should be seated or laid down.

Before starting therapy with Proflosin®, the patient should be excluded from the presence of diseases and conditions that can cause symptoms similar to those for benign prostatic hyperplasia.

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

In case of development of angioedema, therapy with Proflosin should be discontinued immediately. Repeated administration of the drug is contraindicated. With surgery for cataracts while taking the drug, the development of atonic iris syndrome is possible, which must be taken into account by the surgeon for the preoperative preparation of the patient and during the operation.

Influence on the ability to drive vehicles and other mechanisms requiring increased concentration of attention

Caution must be exercised when driving vehicles and engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions, due to the fact that dizziness is possible.

Sustained-Release Capsules