Proflosin, 0.4 mg 30 pcs

Pharmacodynamics

Tamsulosin selectively and competitively blocks postsynaptic α1A-adrenoreceptors located in the smooth muscles of the prostate, bladder neck and prostatic urethra. This results in reduction of the tone of the smooth muscles of the prostate, bladder neck and prostatic part of the urethra and improvement of the outflow of urine.

The α-adrenoreceptor blockers can lower blood pressure (BP) by reducing peripheral vascular resistance. However, in clinical trials of tamsulosin, no clinically significant BP reduction has been observed in patients with normal BP levels.

Pharmacokinetics

Intake

After oral administration, tamsulosin is rapidly and almost completely absorbed from the GI tract. Absorption of tamsulosin slows down slightly after meals. After a single oral dose of 0.4 mg, maximum plasma concentration (Cmax) of tamsulosin is reached after about 6 hours.

Distribution

The binding to plasma proteins is about 99%, the volume of distribution is small – 0.2 l/kg.

Metabolism

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

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 (when taken once after a meal), with regular use – 13 hours.

Indications

Benign prostatic hyperplasia (treatment of dysuric disorders).

Active ingredient

Composition

Active ingredients:

Tamsulosin hydrochloride 400 mcg.

Auxiliary substances:

Microcrystalline cellulose – 276.9 mg,

Methacrylic acid and ethyl acrylate copolymer (1:1) – 16.5 mg,

triethylcitrate – 1.65 mg, talc – 16.5 mg.

Pellet shell composition:

Methacrylic acid and ethyl acrylate copolymer (1:1) – 21.63 mg,

talc – 8.65 mg,

triethylcitrate – 2.16 mg.

Capsule body composition:

iron oxide red dye – 0.0239 mg,

titanium dioxide – 0.53 mg,

iron oxide yellow dye – 0.258 mg,

gelatin – 38.938 mg.

Capsule cap composition:

indigo carmine – 0.00152 mg,

iron oxide black dye – 0.0107 mg,

titanium dioxide – 0.356 mg,

iron oxide yellow dye – 0.114 mg,

gelatin – 23.889 mg.

How to take, the dosage

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

The capsule should be swallowed whole, without chewing, with plenty of water.

The capsule must not be broken into pieces or crushed as this may affect the rate of release of the active ingredient.

The duration of use is not limited.

Interaction

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

In concomitant use with cimetidine some increase in plasma concentration of tamsulosin was noted; with furosemide some decrease in concentration, but this does not require adjusting the dose of Proflosin® , because the drug concentration remains within the normal range.

Diclofenac and warfarin may increase the excretion rate of tamsulosin.

The concomitant administration of tamsulosin with other a1-adrenoreceptor blockers may lead to a decrease in blood pressure.

Special Instructions

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

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

Perioperative rectal examination and, if necessary, specific prostatic antigen (PSA) testing should be performed before initiating treatment and routinely during therapy.

If angioedema develops, therapy with Proflosin should be discontinued immediately. Reapplication of the drug is contraindicated. In surgical intervention for cataract taking the drug may cause atonic iris syndrome, which must be taken into account by the surgeon for pre-operative preparation of the patient and during the operation.

Impact on ability to drive vehicles and other mechanisms requiring high concentration

We should use caution when driving motor transport and engaging in potentially dangerous activities requiring increased concentration and speed of psychomotor reactions due to the possible development of dizziness.

Contraindications

With caution: chronic renal insufficiency (CKR less than 10 ml/min); arterial hypotension.

Side effects

Possible side effects when using the drug are listed below in descending order of frequency of occurrence:

Nervous system disorders: frequent – dizziness; infrequent – headache; rare – fainting.

System disorders: infrequent – tachycardia, orthostatic hypotension.

Gastrointestinal disorders: infrequent – constipation, diarrhea, nausea, vomiting.

Reproductive system disorders: infrequent – disruption of ejaculation; very rare – priapism.

Skin and subcutaneous tissue disorders: infrequent – rash, pruritus, urticaria; rarely – angioedema.

Others: in single cases – development of atonic iris syndrome (narrow pupil syndrome) during cataract surgery, asthenia, rhinitis.

Overdose

There have been no cases of overdose when taking the drug so far. However, there is theoretically a possibility of a sharp decrease in blood pressure and tachycardia, which may require appropriate measures.

The patient must be laid down to restore BP (including in orthostatic hypotension) and heart rate to normal values. Hemodialysis is not advisable because tamsulosin has a high affinity for plasma proteins.

In order to prevent further absorption of tamsulosin, gastric lavage, administration of activated charcoal or osmotic laxatives (e.g., sodium sulfate) are advisable.

Pregnancy use

The drug is prescribed only to men.

Similarities