Tamsulosin Retard-OBL Tablets 0.4mg N30
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Active ingredients
Tamsulosin
Release form
Pills
Composition
Tamsulosin hydrochloride 0.4 mg; Auxiliary substances: hypromellose (hydroxypropyl methylcellulose) 41.25 mg; colloidal silicon dioxide (aerosil) 0.625 mg; microcrystalline cellulose 82.1 mg; magnesium stearate 0.625 mg; Shell auxiliary materials: Paddy II (series 85 ) 3 mg [polyvinyl alcohol, partially hydrolyzed, macrogol-3350, talc, titanium dioxide, iron dye yellow oxide, iron dye red oxide, iron dye black oxide].
Pharmacological effect
Tamsulosin is a specific blocker of postsynaptic alpha1-adrenergic receptors found in the smooth muscles of the prostate gland, bladder neck, and prostatic urethra. The blockade of alpha1-adrenoreceptors with tamsulosin leads to a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and 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. 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, and in patients with normal blood pressure.
Pharmacokinetics
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 oral dose of 0.4 mg of the drug, its maximum plasma concentration (Cmax) is reached after 6 hours. After repeated ingestion of 0.4 mg per day, the equilibrium concentration (Css) is reached by the 5th day, while its value is about 2/3 higher than the value of this parameter after taking a single dose. DistributionConjunction with plasma proteins is 99%, the volume of distribution small (about 0.2 l / kg). MetabolismTamsulosin 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 dosage regimen is required. Excretion of tamsulosin and its metabolites are mainly excreted by the kidneys, 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 food is 10 hours, with repeated intake - 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
Treatment of dysuric disorders in benign prostatic hyperplasia.
Contraindications
Hypersensitivity to tamsulosin or any other component of the drug, orthostatic hypotension (including history), severe liver failure, children under 18 years of age. With cautionChronic renal insufficiency (creatinine clearance (CK) below 10 ml / min). Arterial hypotension .
Use during pregnancy and lactation
The drug Tamsulosin retard is intended for use only in males.
Dosage and administration
Inside, after breakfast, drinking water, take 1 tablet of prolonged action, film-coated (0.4 mg) 1 time per day. The tablet is not recommended to chew, as this may affect the rate of release of the drug.
Side effects
The incidence of adverse reactions is according to the WHO classification: very often (≥1 / 10 cases), often (≥1 / 100 and <1/10 cases), infrequently (≥1 / 1000 and <1/100 cases), rarely (≥ 1/10000 and <1/1000 cases) and very rarely (<1/10000 cases). On the side of the cardiovascular system: infrequently, feeling the heartbeat, orthostatic hypotension. On the part of the gastrointestinal tract: not often - constipation, diarrhea, nausea , vomiting. From the nervous system: often - dizziness; infrequently - headache; rarely - fainting. From the reproductive system: infrequently - disturbances ejaculation; very rarely - priapism. On the part of the respiratory system,thorax and mediastinal small - rhinitis. On the side of the skin and subcutaneous tissue, small - rash, pruritus, urticaria; rarely - angioedema; very rare - Stevens-Johnson syndrome; frequency unknown - exudative erythema multiforme, exfoliative dermatitis ,. unknown - nosebleeds. Cases of intraoperative instability of the iris of the eye (narrow pupil syndrome) during surgery for cataract and glaucoma in patients taking tamsulosin are described. In addition to side effects the effects described above, when using tamsulosin, atrial fibrillation, arrhythmia, tachycardia and shortness of breath were observed. Due to the fact that the data were obtained by the method of spontaneous messages in the post-registration period, determining the frequency and causal relationship of these phenomena with taking tamsulosin is difficult.
Overdose
There are no reports of cases of acute overdose with tamsulosin. However, theoretically, an overdose may develop an acute reduction in blood pressure (BP) 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. It is unlikely that dialysis will be effective, since tamsulosin is strongly associated with plasma proteins. To prevent further absorption of the drug, it is advisable to wash the stomach, take activated carbon or osmotic laxative, for example, sodium sulfate.
Interaction with other drugs
When tamsulosin was prescribed together with atenolol, enalapril or nifedipine, no interactions were detected. When tamsulosin was administered with cimetidine, there was a slight increase in plasma tamsulosin concentration and a decrease in furosemide, however, this does not require changing the dose of Tamsulosin retard because the drug concentration remains within the normal range. Diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin are not change the free fraction of tamsulosin in human plasma in vitro.In turn, tamsulosin also does not alter the free fractions of diazepam, propranolol, trichloromethiazide, and chlormadinone. In in vitro studies, no interaction at the level of hepatic metabolism with amitriptyline, salbutamol, glibenclamide and finisteride was detected. Diclofenac and warfarin can increase the rate of elimination of tamsulosin. Simultaneous use of tamsulosin with strong inhibitors of the CYP3A4 isoenzyme can lead to an increase in the concentration of tamsulosin. Simultaneous use with ketoconazole (a strong inhibitor of the CYP3A4 isoenzyme) resulted in an increase in the area under the concentration-time pharmacokinetic curve (AUC) and the maximum concentration (Cmax) of tamsulosin by 2.8 and 2.2 times, respectively. Tamsulozin should not be administered in combination with strong inhibitors of the isoenzyme CYP3A4 in patients with metabolic isozyme isoenzyme CYP2D6. The drug should be used with caution in combination with strong and moderate inhibitors of the CYP3A4 isoenzyme. Simultaneous administration of tamsulosin and paroxetine, a strong inhibitor of the isoenzyme CYP2D6, led to an increase in Cmax and AUC of tamsulosin 1.3 and 1.6 times, respectively, but this increase was considered clinically insignificant Simultaneous administration of other alpha1-adrenoreceptor antagonists can lead to a decrease in blood pressure.
special instructions
As with other alpha1-adrenergic blockers, with Tamsulosin retard treatment, in some cases, a decrease in blood pressure may occur, which can 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. With operative interventions for cataract while taking the drug, the development of the intraoperative iris instability syndrome (narrow pupil) that it is necessary to consider the surgeon for preoperative preparation of the patient and during the operation. The expediency of discontinuing therapy with tamsulosin 1-2 weeks before surgery for cataracts or glaucoma has not yet been proven. Cases of intraoperative instability of the iris occurred in patients who stopped taking the drug and earlier in the operation.It is not recommended to start therapy with tamsulosin in patients who are scheduled for cataract or glaucoma surgery. There are reports of cases of prolonged erection and priapism during therapy with alpha1-adrenergic blockers. If the erection persists for more than 4 hours, you should immediately seek medical help. If priapism therapy was not carried out immediately, it can cause damage to the tissues of the penis and irreversible loss of potency. Before starting therapy with Tamsulozin retard, the patient should be examined in order to exclude the presence of other diseases that can cause the same symptoms as and BPH. Before treatment, and regularly during therapy, a digital rectal examination should be performed and, if required, a determination of the prostate specific antigen. Effect on the ability to drive vehicles and mechanisms. Care must be taken when driving vehicles and occupying potentially dangerous activities that require increased concentration and psychomotor speed. reactions, due to the fact that the development of vertigo.