Fokusin capsules with modif. release 0.4mg N30
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Active ingredients
Tamsulosin
Release form
Capsules
Composition
1 capsule contains tamsulosin hydrochloride 400 mcg. Excipients: copolymer of methacrylic acid and ethyl acrylate (1: 1) 30% dispersion - 74.9 mg (in the form of a solid) *, microcrystalline cellulose - 257.1 mg, dibutyl sebacate - 8.4 mg, polysorbate 80 - 500 μg, colloidal silicon dioxide - 3.7 mg , talc - 300 mkg. * for one capsule 30% dispersion of copolymer of methacrylic acid and ethyl acrylate (1: 1) in an amount of 249.67 mg, which corresponds to 74.9 mg in the form of a solid, is used. The composition of the capsule shell: azorubine dye - 0.2%, dye blue patented - 0.12%, gelatin - up to 100%.
Pharmacological effect
Tamsulosin selectively and competitively blocks postsynaptic α1A-adrenergic receptors of smooth muscles of the prostate, bladder neck and prostatic urethra and α1D-adrenergic receptors of the bladder, which leads to a reduction in smooth muscle tone of the prostate, bladder neck and prostatic urethra, improve detrusor function and reduce symptoms of obstruction and irritation associated with benign prostatic hyperplasia. As a rule, the therapeutic effect develops Xia 2 weeks. after starting the drug, although in a number of patients, a reduction in the severity of symptoms is noted after taking the first dose. The ability of tamsulosin to affect α1A-adrenoreceptors is 20 times greater than its ability to affect α1D-adrenergic receptors of vascular smooth muscles. Due to such high selectivity, the drug does not cause any clinically significant reduction in systemic blood pressure in patients with arterial hypertension, and in patients with normal baseline blood pressure.
Pharmacokinetics
Suction. After oral administration, tamsulosin is rapidly and almost completely absorbed from the gastrointestinal tract, its bioavailability is almost 100%. After a single dose of the drug Fokusin orally at a dose of 400 mcg Cmax of the active substance in plasma is achieved after 6 hours. Distribution. After 5 days of the course taking, the Cmax value of the active substance in the blood plasma is 60–70% higher than the Cmax after a single dose. Plasma protein binding - 99%. Tamsulosin Vd is negligible (approximately 0.2 l / kg). Metabolism.Tamsulosin does not undergo the first-pass effect and is slowly biotransformed in the liver with the formation of pharmacologically active metabolites that retain a high selectivity for α-adrenergic receptors. Most of the active substance is present in the blood unchanged. Inference. Tamsulosin is excreted by the kidneys, 9% of the dose is excreted unchanged. T1 / 2 tamsulosin in a single dose - 10 hours, after repeated administration - 13 hours, the final - 22 hours.
Indications
Treatment of functional disorders in benign prostatic hyperplasia
Contraindications
Orthostatic hypotension (including history); severe hepatic impairment; age up to 18 years (efficacy and safety not established); hypersensitivity to the drug components. The drug should be used with caution in chronic renal failure (CC less than 10 ml / min), arterial hypotension (including orthostatic), a planned cataract operation, with simultaneous use of powerful and moderately active inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole, voriconazole). Zano-use of the drug in patients with severe liver failure. Use for violations of renal functionWith caution, you should use the drug for chronic renal failure (CC less than 10 ml / min).
Precautionary measures
Caution should be used tamsulosin in patients with a predisposition to orthostatic hypotension. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should be seated or placed. Before beginning the use of the drug, the diagnosis must be verified. Use with caution in chronic renal failure (Creatinine clearance less than 10 ml / min). Use with caution in severe hepatic insufficiency. Effect on the ability to drive motor vehicles and control mechanisms During the period of treatment, the patient must be careful when driving and other potential otherwise dangerous activities that require increased concentration of attention and quickness of psychomotor reactions
Use during pregnancy and lactation
Fokusin not intended for use in women
Dosage and administration
The drug is taken orally at a dose of 400 micrograms (1 capsule) / day. Capsules should be taken after the first meal, without chewing, drinking a sufficient amount of water. Focus can be used both as monotherapy and in combination with 5α-reductase inhibitors (finasteride dutasteride)
Side effects
The frequency of adverse reactions is presented according to the MedDRA classification: very often (> 10%), often (≥1%, <10%), infrequently (≥0.1%, <1%), rarely (≥0.01%, <0.1%) , very rarely (<0.01%), the frequency is unknown (it is not possible to determine the frequency of occurrence from the available data). For the immune system: very rarely for hypersensitivity reactions. For the nervous system: often for dizziness; infrequently - headache; rarely - syncopal states; frequency is unknown - sleep disturbance (drowsiness or insomnia). On the part of the organ of vision: frequency is unknown - blurred vision, blurred vision. On the part of the cardiovascular system: infrequently - feeling of heartbeat, orthostatic hypotension; frequency is unknown - tachycardia. On the respiratory system: infrequently - rhinitis; frequency is unknown - nasal bleeding. On the part of the digestive system: rarely - nausea, vomiting, constipation or diarrhea. On the side of the skin and subcutaneous tissues: rarely - skin rash, itching, urticaria; rarely, angioedema; very rarely - Stevens-Johnson syndrome; frequency is unknown - erythema multiforme, exfoliative dermatitis. On the part of the genital organs and the mammary gland: very rarely - priapism; frequency is unknown - ejaculatory disorders (including retrograde ejaculation), decreased libido. Common disorders: infrequently - asthenic syndrome; frequency unknown - back pain, chest pain.
Overdose
Symptoms: pronounced decrease in blood pressure. Treatment: cardiotropic therapy, general maintenance therapy, control of renal function, administration of volume-substituting solutions or vasoconstrictor drugs. To prevent further absorption of tamsulosin, gastric lavage, taking activated carbon or osmotic laxative is possible.
Interaction with other drugs
Simultaneous use of tamsulosin with other alpha1-adrenergic blockers may lead to a decrease in blood pressure. Diclofenac and indirect anticoagulants (warfarin) slightly increase the clearance rate of tamsulosin. Cimetidine increases the concentration of tamsulosin in the plasma, while reducing furosemide (it does not have a natural meaning, it does not have a real value, it has no value, a factor has no value to it). with atenolol,There were no signs of drug interaction with enalapril or theophylline. In vitro, the administration of diazepam, propranolol, trichloromethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin did not alter the free fraction of tamsulosin in the blood plasma. Tamsulosin also had no effect on the free fractions of diazepam, propranolol, trichloromethiazide and chlormadinone. Simultaneous use of tamsulosin and potent inhibitors of CYP3A4 may cause an increase in systemic exposure of tamsulosin. Simultaneous use of tamsulosin with ketoconazole (a potent inhibitor of CYP3A4 isoenzyme) resulted in an increase in AUC and Cmax of tamsulosin by 2.8 times and 2.2 times, respectively. Tamsulosin should not be used in combination with potent inhibitors of the CYP3A4 isoenzyme in a patient with a slow-metabolism, in the case of ip; use caution while applying tamsulosin with potent and moderately active inhibitors of the CYP3A4 isoenzyme
special instructions
Before starting therapy with Fokusin, it is necessary to exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before treatment, and regularly during therapy, an examination of the prostate gland should be carried out (digital rectal examination, PSA determination). As with other alpha1-adrenergic blockers, when using Fokusin, in some cases a decrease in blood pressure may occur, which can lead to fainting. Fokusin drug should be used with caution in patients with a predisposition to orthostatic hypotension. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should be seated or folded. When developing angioedema, as well as other immunological reactions, such as Stevens-Johnson syndrome, the use of the drug should stop immediately. The patient must be under the supervision of a physician until the elimination of this pathological condition; Re-appointment of tamsulosin is not allowed. During surgery for cataracts in some patients who received Tasmulozin Hydrochloride at the time of surgery and in the past, the development of the intraoperative iris instability syndrome (narrow pupil syndrome) took place.Intraoperative instability of the iris can lead to an increased risk of organ complications during and after surgery. Tamsulosin hydrochloride should not be used in combination with potent inhibitors of the CYP3A4 isoenzyme in patients with a slow metabolism phenotype of the CYP2D6 isoenzyme. Effect on ability to drive of motor transport and control mechanisms. Care should be taken when driving and occupations that require an increased concentration of mania and psychomotor speed reactions. In the event of dizziness, it is necessary to refrain from driving and performing other potentially hazardous activities.