Tamsulosin Tamzelin caps with prolong release 0.4 mg x30
, INSTRUCTIONS for medical use of the drug , , Tamzelin ® , Registration number LP-000620 Trade name Tamzelin ® , International nonproprietary name Tamsulosin Dosage form Extended-release capsules Composition per capsule Active substance: , tamsulosin, hydrochloride, pellets, 0, 15,%, 267,mg, containing tamsulosin hydrochloride 0.4 mg. Pellet excipients: sucrose - 143.36 mg, starch - 95.58 mg, ethylcellulose - 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. Gelatin capsule composition: Gelatin - 62.306465 mg Cap: Dyes: Diamond black - 0.0065 mg Blue patent - 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
Description , Gelatin capsules No. 2 with a white body, light green lid. The contents of the capsules are white or almost white spherical pellets. Pharmacotherapeutic group Alpha1-adrenergic blocker. ATX code: G04CA02. Pharmacological properties Pharmacodynamics Tamsulosin is a specific blocker of postsynaptic α 1-adrenergic receptors located in the smooth muscles of the prostate gland, cervix, bladder, and prostatic part of the urethra. Blockade of α1-adrenergic receptors leads to a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and prostatic urethra and improved urine outflow. At the same time, both the symptoms of emptying and the symptoms of filling of the bladder, caused by increased tone of smooth muscles, and detrusor hyperactivity, with benign prostatic hyperplasia, are reduced. The ability of tamsulosin to act on the α 1A subtype of adrenergic receptors is 20 times greater than its ability to interact with the α 1B subtype of adrenergic receptors, which are located in vascular smooth muscle. Due to its high selectivity, tamsulosin does not cause a clinically significant decrease in systemic blood pressure (BP), both in patients with arterial hypertension and in patients with normal blood pressure. Pharmacokinetics Absorption Tamsulosin is almost completely absorbed from the gastrointestinal tract and has almost 100% bioavailability. Absorption of tamsulosin decreases slightly after meals. The same level of absorption can be achieved if the patient takes the drug after a normal breakfast each time. Tamsulosin is characterized by linear kinetics. When taking the primary dose of tamsulosin after a meal, the maximum concentration (Cmax) of the drug in the blood plasma is achieved after 6 hours. Distribution: Bonding with blood plasma proteins - 99%, volume of distribution - 0.2 l/kg . Metabolism Tamsulosin, to a minor and slow extent, undergoes primary metabolism in the liver. Most of the drug is present in the blood unchanged. The results of in vitro studies showed that CYP3A4 isoenzymes, as well as CYP2D6, are involved in the metabolism of tamsulosin hydrochloride, with possible less significant effects from other isoenzymes. Inhibition of the drug-metabolizing enzymes CYP3A4 and CYP2D6 may result in increased exposure to tamsulosin hydrochloride. With minor and moderate degrees of liver failure, no adjustment of the drug dosage regimen is required. Excretion Tamsulosin and its metabolites are excreted mainly by the kidneys, about 9% of the dose is excreted unchanged. The half-life (T 1/2) of the drug is 10-13 hours. In case of renal failure, no reduction in the dose of the drug is required, if the patient has severe renal failure (creatinine clearance (CC) less than 10 ml/min ), tamsulosin should be prescribed with caution.
Indications for use Treatment of dysuria associated with benign prostatic hyperplasia.
Contraindications Hypersensitivity to tamsulosin or any auxiliary component of the drug. Severe liver failure. Orthostatic hypotension (including history). Children under 18 years of age.
With caution: Severe renal failure (creatinine clearance less than 10 ml/min). Arterial hypotension. Use during pregnancy and breastfeeding Tamsulosin is not indicated for use in women.
Directions for use and dosage: Orally, after breakfast. It is recommended not to chew the capsule, but to wash it down with a small amount of water. Adults over 18 years of age, as well as elderly patients: 1 capsule (0.4 mg) 1 time per day. Patients with impaired liver and kidney function: For mild to moderate renal and hepatic impairment, no dose adjustment is required. , , Side effect According to , the World , Health Organization , (WHO), undesirable , reactions are classified , in , accordance , with , their , frequency , of development , in the following , way: , very , often (≥1/10), often (≥1/100, <.1/10), infrequently (≥1/1000, <.1/100), rarely (≥1/10000, <.1/1000), very rarely (<.1/10000 ), frequency unknown - based on available data, it was not possible to determine the frequency of occurrence. From the nervous system: often: dizziness, infrequently: headache, rarely: fainting, sleep disturbance (drowsiness or insomnia). On the part of the organ of vision, the frequency is unknown: blurred vision, blurred vision. From the cardiovascular system: uncommon: postural hypotension, tachycardia, palpitations, rare: chest pain, atrial fibrillation. From the respiratory system: uncommon: rhinitis, shortness of breath, frequency unknown: nosebleeds. From the gastrointestinal tract: uncommon: constipation, diarrhea, nausea, vomiting. From the skin and subcutaneous tissue: uncommon: rash, itching, urticaria, rare: angioedema, very rare: Stevens-Johnson syndrome, frequency unknown: erythema multiforme, exfoliative dermatitis. Other: often: ejaculation disorders, including retrograde ejaculation and ejaculatory insufficiency, uncommon: asthenia, back pain, small pupil syndrome during cataract surgery, very rare: priapism, decreased libido. During post-registration observations, cases of intraoperative instability syndrome of the iris (narrow pupil syndrome) were identified during surgery for cataracts and glaucoma of the eye in patients taking tamsulosin. During post-registration observations, in addition to the adverse events described above, cases of atrial fibrillation, arrhythmia, tachycardia and dyspnea associated with the use of tamsulosin were described. ,Because ,spontaneous ,reports ,have ,been ,in ,the ,framework ,of ,post-marketing ,studies ,around ,the ,world, ,it ,is ,not ,possible ,with ,sufficient ,degree ,of ,reliability ,to ,assess ,the ,frequency ,of ,the ,development ,of ,these ,phenomena, ,and ,their ,relationships. with the use of tamsulosin.
Overdose Symptoms Overdose of tamsulosin hydrochloride can potentially lead to acute hypotensive effects. Such effects have been reported under a variety of overdose conditions. Treatment In case of overdose and development of hypotension, it is recommended to transfer the patient to a horizontal position and carry out measures aimed at maintaining the activity of the cardiovascular system (restoring blood pressure and heart rate) , gastric lavage, administration of activated carbon and osmotic laxatives, agents such as sodium, sulfate. If there is no effect, it is necessary to introduce substances that increase the volume of circulating blood and, if necessary, vasoconstrictors. Kidney function should be monitored and general supportive measures should be taken. Dialysis is unlikely to be effective because tamsulosin is highly bound to plasma proteins.
Interaction with other drugs When used simultaneously with atenolol, enalapril and nifedipine, no drug interactions were identified. When used simultaneously with cimetidine, the concentration of tamsulosin in the blood serum increases; when furosemide is prescribed, it decreases. However, no dose adjustment is required since tamsulosin concentrations remain within the therapeutic range. Diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not change the level of the free fraction of tamsulosin in blood plasma in vitro. In turn, tamsulosin also does not change the content of free fractions of diazepam, propranolol, trichlormethiazide and chlormadinone. Diclofenac and warfarin may increase the elimination rate of tamsulosin. Concomitant use with strong CYP34A isoenzyme inhibitors may lead to an increase in tamsulosin concentrations. Simultaneous use with ketoconazole led to an increase in the area under the pharmacokinetic concentration-time curve (AUC) and maximum concentration (Cmax) by 2.8 and 2.2 times, respectively. Tamsulosin hydrochloride should not be used in combination with strong CYP34A inhibitors in patients with impaired metabolism of the CYP2D6 isoenzyme. The drug should be used with caution in combination with strong and moderate inhibitors of the CYP34A isoenzyme. Simultaneous administration of tamsulosin and paroxetine leads to an increase in the area under the pharmacokinetic concentration-time curve (AUC) and maximum concentration (Cmax) by 1.3 and 1.6 times, respectively. Simultaneous administration of other α1-adrenergic receptor antagonists may lead to increased hypotensive effect.
Special instructions As with the use of other α1-adrenergic blockers, during treatment with tamsulosin, in some cases, a decrease in blood pressure (BP) may be observed, which, sometimes, can lead to a fainting state. 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. During surgical interventions for cataracts while taking the drug, it is possible to develop a syndrome of intraoperative instability of the iris of the eye (narrow pupil syndrome), which must be taken into account by the surgeon during preoperative preparation of the patient and during operations. It is not recommended to initiate therapy with tamsulosin in patients scheduled for surgery for cataracts or glaucoma. ,During ,operative ,examination, ,before ,operating ,patients, ,the ,surgeon ,or ,ophthalmologist ,should ,consider ,whether ,the ,patient ,is ,taking ,tamsulosin. Before starting drug therapy, the patient should be examined to exclude the presence of other diseases that may cause the same symptoms as benign prostate hyperplasia. Digital, rectal, and, if necessary, prostate-specific antigen (PSA) examinations should be performed before treatment and at regular intervals thereafter. There are reports of cases of the development of prolonged erection and priapism during therapy with α1-blockers. If an erection persists for four hours, you should immediately seek medical help. If priapism therapy is not carried out immediately, this may lead to tissue damage to the penis, and irreversible loss of potency.
Impact on the ability to drive vehicles, machinery During the treatment period, it is necessary to observe caution when driving vehicles and performing potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Release form Extended release capsules 0.4 mg. 10 or 20 capsules per blister pack. 1, 3, 6 blister packs of 10 capsules or 3, 5 blister packs of 20 capsules with instructions for use are placed in a cardboard pack. 60, 100 capsules in polymer jars. Each jar with instructions for use is placed in a cardboard pack.
Storage conditions In a place protected from light at a temperature not exceeding 30 ℃. Keep out of the reach of children.
Shelf life: 3 years. Do not use after the expiration date.
Conditions of release Dispensed by prescription.
Tamzelin (long-acting capsule 0.4 mg No. 30)
A country
Russia
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.
Active substance
Tamsulosin
Compound
Composition per capsule Active ingredient: tamsulosin hydrochloride pellets 0.15% 267 mg containing tamsulosin hydrochloride 0.4 mg. Pellet excipients: sucrose - 143.36 mg, starch - 95.58 mg, ethylcellulose - 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. Gelatin capsule composition: Gelatin - 62.306465 mg Cap: Dyes: Diamond black - 0.0065 mg Blue patent - 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 Description Gelatin capsules No. 2 with a white body, light green lid. The contents of the capsules are white or almost white spherical pellets. Release form Extended release capsules 0.4 mg. 10 or 20 capsules per blister pack. 1, 3, 6 blister packs of 10 capsules or 3, 5 blister packs of 20 capsules with instructions for use are placed in a cardboard pack. 60, 100 capsules in polymer jars. Each jar with instructions for use is placed in a cardboard pack.
Pharmacological properties
Pharmacodynamics Tamsulosin is a specific blocker of postsynaptic α1-adrenergic receptors located in the smooth muscles of the prostate gland, bladder neck and prostatic urethra. Blockade of α1-adrenergic receptors leads to a decrease in the tone of the smooth muscles of the prostate gland, bladder neck and prostatic urethra and improves urine outflow. At the same time, both the symptoms of emptying and the symptoms of bladder filling, caused by increased smooth muscle tone and detrusor hyperactivity in benign prostatic hyperplasia, are reduced. The ability of tamsulosin to act on the α1A subtype of adrenergic receptors is 20 times greater than its ability to interact with the α1B subtype of adrenergic receptors, which are located in vascular smooth muscle. Due to its high selectivity, tamsulosin does not cause a clinically significant decrease in systemic blood pressure (BP) both in patients with arterial hypertension and in patients with normal blood pressure. Pharmacokinetics Absorption Tamsulosin is almost completely absorbed from the gastrointestinal tract and has almost 100% bioavailability. Absorption of tamsulosin decreases slightly after meals. The same level of absorption can be achieved if the patient takes the drug after a normal breakfast each time. Tamsulosin is characterized by linear kinetics. When taking the initial dose of tamsulosin after a meal, the maximum concentration (Cmax) of the drug in the blood plasma is achieved after 6 hours. Distribution: Bonding with blood plasma proteins is 99%, volume of distribution is 0.2 l/kg. Metabolism Tamsulosin undergoes primary metabolism to a small extent and slowly in the liver. Most of the drug is present in the blood unchanged. The results of an in vitro study showed that CYP3A4 isoenzymes, as well as CYP2D6, are involved in the metabolism of tamsulosin hydrochloride, with possible less significant effects from other isoenzymes. Inhibition of the drug-metabolizing enzymes CYP3A4 and CYP2D6 may result in increased exposure to tamsulosin hydrochloride. With minor and moderate degrees of liver failure, no adjustment of the drug dosage regimen is required. Excretion Tamsulosin and its metabolites are excreted mainly by the kidneys, about 9% of the dose is excreted unchanged. The half-life (T1/2) of the drug is 10-13 hours. In case of renal failure, no reduction in the dose of the drug is required; if the patient has severe renal failure (creatinine clearance (CC) less than 10 ml/min), tamsulosin should be prescribed with caution.
Indications for use
Treatment of dysuria associated with benign prostatic hyperplasia.
Contraindications
Hypersensitivity to tamsulosin or any auxiliary component of the drug. Severe liver failure. Orthostatic hypotension (including history). Children under 18 years of age. With caution: Severe renal failure (creatinine clearance less than 10 ml/min). Arterial hypotension. Use during pregnancy and breastfeeding Tamsulosin is not indicated for use in women.
Directions for use and doses
Inside, after breakfast. It is recommended not to chew the capsule and take it with a small amount of water. Adults over 18 years of age, as well as elderly patients: 1 capsule (0.4 mg) 1 time per day. Patients with impaired liver and kidney function: For mild to moderate renal and hepatic impairment, no dose adjustment is required.
Side effect
According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: very often (≥1/10), often (≥1/100, from the nervous system: often: dizziness; infrequently: headache; rarely : fainting, sleep disturbance (drowsiness or insomnia).On the visual side, frequency unknown: blurred vision, blurred vision.On the cardiovascular system: uncommon: postural hypotension, tachycardia, palpitations; rare: chest pain, atrial fibrillation. From the respiratory system: infrequently: rhinitis, shortness of breath; frequency unknown: nosebleeds. From the gastrointestinal tract: infrequently: constipation, diarrhea, nausea, vomiting. from the skin and subcutaneous tissue: infrequently: rash, itching, urticaria; rarely: angioedema ; very rare: Stevens-Johnson syndrome; frequency unknown: erythema multiforme, exfoliative dermatitis. Other: often: ejaculatory disorders, including retrograde ejaculation and ejaculatory insufficiency; uncommon: asthenia, back pain, small pupil syndrome during cataract surgery; very rare: priapism, decreased libido. During post-registration observations, cases of intraoperative iris instability syndrome (narrow pupil syndrome) were identified during cataract and glaucoma surgery in patients taking tamsulosin. During post-marketing observations, in addition to the adverse events described above, cases of atrial fibrillation, arrhythmia, tachycardia and dyspnea associated with the use of tamsulosin were described. Because these spontaneous reports were received as part of a post-marketing study worldwide, it is not possible to reliably estimate the incidence of these events and their relationship to tamsulosin use.
Overdose
Symptoms Overdose of tamsulosin hydrochloride can potentially lead to acute hypotensive effects. Such effects have been reported under a variety of overdose conditions. Treatment In case of overdose and development of hypotension, it is recommended to transfer the patient to a horizontal position and take measures aimed at maintaining the activity of the cardiovascular system (restoring blood pressure and heart rate); gastric lavage, administration of activated carbon and osmotic laxatives such as sodium sulfate. If there is no effect, substances that increase the volume of circulating blood and, if necessary, vasoconstrictors should be administered. Renal function should be monitored and general supportive measures administered. Dialysis is unlikely to be effective because tamsulosin is highly bound to plasma proteins.
Interaction with other drugs
When used simultaneously with atenolol, enalapril and nifedipine, no drug interactions were detected. When used simultaneously with cimetidine, the concentration of tamsulosin in the blood serum increases, and when furosemide is prescribed, it decreases. However, no dose adjustment is required since tamsulosin concentrations remain within the therapeutic range. Diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not change the level of the free fraction of tamsulosin in blood plasma in vitro. In turn, tamsulosin also does not change the content of free fractions of diazepam, propranolol, trichloromethiazide and chlormadinone. Diclofenac and warfarin may increase the elimination rate of tamsulosin. Concomitant use with strong CYP34A isoenzyme inhibitors may lead to an increase in tamsulosin concentrations. Co-administration with ketoconazole resulted in an increase in the area under the concentration-time pharmacokinetic curve (AUC) and maximum concentration (Cmax) by 2.8 and 2.2 times, respectively. Tamsulosin hydrochloride should not be used in combination with strong inhibitors of the CYP34A isoenzyme in patients with impaired metabolism of the CYP2D6 isoenzyme. The drug should be used with caution in combination with strong and moderate inhibitors of the CYP34A isoenzyme. Co-administration of tamsulosin and paroxetine leads to an increase in the area under the concentration-time pharmacokinetic curve (AUC) and maximum concentration (Cmax) by 1.3 and 1.6 times, respectively. Concomitant administration of other α1-adrenergic receptor antagonists may lead to increased hypotensive effect.
special instructions
As with the use of other α1-blockers, during treatment with tamsulosin, in some cases a decrease in blood pressure (BP) may be observed, 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. During surgical interventions for cataracts while taking the drug, the development of intraoperative instability syndrome of the iris (narrow pupil syndrome) is possible, which must 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 scheduled for cataract or glaucoma surgery. During the preoperative evaluation of patients, the surgeon or ophthalmologist should consider whether the patient is taking tamsulosin. Before starting drug therapy, the patient should be examined to exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. A digital rectal examination and, if necessary, prostate specific antigen testing should be performed before starting treatment and at regular intervals thereafter. There are reports of cases of the development of prolonged erection and priapism during therapy with α1-blockers. If an erection persists for four hours, you should immediately seek medical help. If priapism therapy is not carried out immediately, it can lead to damage to the tissue of the penis and irreversible loss of potency. Impact on the ability to drive vehicles and machinery During the treatment period, care must be taken when driving vehicles and performing potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
Dispensing conditions in pharmacies
On prescription
