Nitop tablets p/o 30mg №10×3

Name:
Nitop. Forms of release Tablets. INNNimodipine. FTGBmkk.
Description:
White or almost white coated tablets. Composition 1 tablet contains: Active substance: 30 mg of nimodipine. Fillers: microcrystalline cellulose – 142.5 mg, polyvidone – 75.0 mg, crospovidone – 44.4 mg, corn starch – 37.5 mg, magnesium stearate – 0.6 mg, hypromellose – 5.4 mg, macrogol 4000 – 1.8 mg, titanium dioxide E171 – 1.8 mg. Pharmacotherapeutic group Selective calcium channel blockers, dihydropyridine derivatives. ATS code – С08СА06. Pharmacological properties Pharmacodynamics Selective blocker of calcium channels of the II class, derivative of dihydropyridine. Selectively interacts with type L calcium channels and blocks the transmembrane entry of calcium ions. It has a vasodilating effect mainly on the vessels of the brain. Prevents or eliminates vasospasm caused by various vasoconstrictor biologically active substances. Causes a more pronounced increase in perfusion in areas of the brain with insufficient blood supply (compared to areas with normal blood supply). Improves cerebral circulation in subarachnoid hemorrhage. Stabilizes the functional state of brain neurons. Improves memory and ability to concentrate. It has no significant effect on systemic blood pressure. Pharmacokinetics Absorption After oral administration, nimodipine is almost completely absorbed. Nimodipine and primary metabolites are found in the blood plasma within 10-15 minutes after taking the pill. After repeated oral administration (30 mg 3 times / day), the maximum concentration in elderly patients was reached after 0.6-1.6 hours and was 7.3-43.2 ng / ml in young patients after taking single doses of 30 mg and 60 mg, the maximum concentration is 16 ± 8 ng / ml and 31 ± 12 ng / ml, respectively. The increase in maximum concentration and area under the concentration-time curve is dose-dependent. Due to the intensive metabolism during the “first pass” through the liver (85-95%), the absolute bioavailability of nimodipine is 5-15%. Distribution Nimodipine is intensely bound to plasma proteins (97-99%) and crosses the placental barrier. The concentration of nimodipine and its metabolites in breast milk significantly exceeds the concentration in blood plasma. After oral administration, the concentration of nimodipine in the cerebrospinal fluid is about 0.5% of the plasma concentration. Metabolism and excretion Nimodipine is metabolized mainly by dehydrogenation of the dihydropyridine ring and oxidative ester cleavage. The three main metabolites found in plasma do not have clinically significant activity. The effect of nimodipine on liver enzyme activity has not been studied. Metabolites are 50% excreted by the kidneys and 30% with bile. When taken orally, the half-life of nimodipine (T1 / 2 initial phase) is 1.1-1.7 hours, the final phase T1 / 2 is 5-10 hours. Indications for use Prevention and treatment of ischemic neurological disorders caused by spasm of cerebral vessels against the background of subarachnoid hemorrhage caused by aneurysm rupture (used after previous intravenous therapy with nimodipine infusion solution). Severe brain dysfunction in elderly patients (decreased memory and concentration, emotional instability). Contraindications Hypersensitivity to any of the components of the drug, severe liver dysfunction (for example, cirrhosis of the liver), simultaneous administration with rifampicin or antiepileptic drugs (phenobarbital, phenytoin, carbamazepine), pregnancy, lactation, age up to 18 years. Nitop should not be administered to patients during or within one month after a myocardial infarction or an episode of unstable angina. With caution in arterial hypotension (systolic blood pressure less than 100 mm Hg. Art.); in patients with unstable angina or within the first 4 weeks after acute myocardial infarction, an assessment of the ratio of potential risk (decrease in coronary artery perfusion and myocardial ischemia) and benefits (improvement of cerebral perfusion) is necessary; in elderly patients with comorbidities with severe renal impairment (glomerular filtration less than 20 ml / min). Elderly patients with severe heart failure receiving a drug for the treatment of brain dysfunction need regular examination. Precautions Special instructions: The appointment of nimodipine to elderly patients with a large number of concomitant diseases, severe renal insufficiency (glomerular filtration rate less than 20 ml / min) and severe cardiovascular diseases should be especially carefully justified. During therapy and after its completion, such patients need regular medical supervision. In patients with impaired liver function, due to a decrease in the intensity of primary metabolism and a slowdown in metabolic inactivation, the bioavailability of nimodipine may increase. As a result, the main and side effects, in particular, its hypotensive effect, may be enhanced. In such cases, the dose of the drug should be reduced depending on the degree of reduction in blood pressure, and if necessary, nimodipine should be discontinued. Nimodipine should not be used in patients with traumatic subarachnoid hemorrhage, since the benefit / risk ratio of this intervention for this category of patients has not been established and the specific groups of patients for whom this drug is indicated have not been determined. Nimodipine should be used with caution in cases of cerebral edema or intracranial hypertension. Although nimodipine does not increase intracranial pressure, careful monitoring is recommended in cases of intracranial hypertension or fluid in the brain (generalized cerebral edema). Caution is necessary in patients with arterial hypotension. Influence on the ability to drive vehicles and control mechanisms The use of nimodipine may impair the ability to drive vehicles and mechanisms due to a possible decrease in blood pressure and the occurrence of dizziness. Pregnancy There are no adequate controlled studies in pregnant women. Reproductive toxicity studies in animals following oral administration have not shown a teratogenic effect, although reproductive toxicity has been identified in the course of the study. lactation period. Nimodipine and its metabolites have been shown to be present in human milk. Nursing mothers are advised not to breastfeed while taking this medicine. Fertility in vitro. The ability of calcium antagonists to cause reversible biochemical changes in the head of the spermatozoon has been demonstrated in vitro, which can lead to impaired sperm function. Children Pediatric dosage has not been established. Method of administration and doses Prevention and treatment of ischemic neurological disorders caused by spasm of cerebral vessels against the background of subarachnoid hemorrhage caused by aneurysm rupture: Tablets should be taken after 5-14 days of intravenous therapy with an infusion solution of nimodipine. The recommended dose is 2 tablets 6 times a day (60 mg nimodipine 6 times a day) for 7 days, the tablets should be swallowed whole with a small amount of liquid. Therapy of brain disorders in elderly patients: the recommended dose is 1 tablet 3 times a day, unless another dose is prescribed by the attending physician. In patients with significantly reduced renal function (glomerular filtration rate less than 20 ml / min), the need for drug treatment should be carefully considered and the patient should be systematically examined. In case of development of adverse reactions, the dose should be reduced, and if necessary, stop using the drug. Serious violations of liver function, especially cirrhosis of the liver, can lead to an increase in the bioavailability of nimodipine due to a decrease in primary metabolism and a decrease in metabolic clearance. In this case, adverse reactions (for example, lowering blood pressure) may be more pronounced. In such cases, the dose should be reduced and, if necessary, stop treatment. With the simultaneous use of the drug with inhibitors or indicators of CYP 3A4, dose adjustment may be required. (See section “Interaction with other medicinal products and other forms of interaction”). Tablets should be swallowed whole, without chewing, with a small amount of liquid, regardless of food intake, at intervals of at least 4 hours. Grapefruit juice should be avoided. Elderly patients: there are no special requirements for changing the dosage in this category of patients. Children: Pediatric dosage has not been established. Interaction with other medicinal products and other forms of interaction Nitop is metabolized with the participation of the enzyme of the cytochrome P450 3A4 system, therefore drugs that induce or inhibit the activity of liver enzymes may affect the plasma concentration of nimodipine. Based on the experience of using other slow calcium channel blockers, it can be expected that rifampicin, which is a reducer of the activity of “liver” enzymes, is able to accelerate the metabolism of nimodipine. With the simultaneous use of rifampicin and nimodipine, the effectiveness of the latter may be reduced. Antiepileptic drugs that induce the cytochrome P450 3A4 enzyme system (phenobarbital, phenytoin and carbamazepine) significantly reduce the bioavailability of nimodipine, so their combined use is contraindicated. Drugs that inhibit the activity of enzymes of the P450 3A4 system may increase the plasma concentration of nimodipine: Macrolides (eg, erythromycin). Structurally related azithromycin does not have these properties HIV protease inhibitors (eg, ritonavir) Azole antimycotics (eg, ketoconazole) Antidepressants nefazodone and fluoxetine (up to 50% increase in plasma concentrations of nimodipine when administered together) Quinopristin/dalfopristin Cimetidine Valproic acid drugs, dose reduction of nimodipine and blood pressure monitoring should be considered. Long-term use of nimodipine with the antidepressant nortriptyline leads to a slight decrease in plasma concentrations of nimodipine; nortriptyline concentration remains unchanged. Nimodipine can lower blood pressure when co-administered with: diuretics beta-blockers ACE inhibitors AT-1 receptor blockers other calcium antagonists alpha-blockers methyldopa phosphodiesterase inhibitors. With the combined use of nimodipine with drugs from these groups, careful monitoring of blood pressure is required. In patients on long-term therapy with haloperidol, no drug interactions of nimodipine with haloperidol were found. Simultaneous intravenous administration of zidovudine and nimodipine leads to a significant increase in AUC for zidovudine and a decrease in its volume of distribution and clearance. Calcium preparations reduce the effectiveness of nimodipine. Grapefruit juice inhibits the metabolism of dihydropyridine oxidation. The combination of grapefruit juice and nimodipine should be avoided as it may lead to increased plasma concentrations of nimodipine. Side effects Adverse reactions reported in connection with the use of nimodipine are summarized in the tables below. In each group, adverse effects are presented in order of decreasing severity. The frequency is defined as: very often (≥ 1/10), often (≥ 1/100, < 1/10), infrequently (≥ 1/1000, < 1/100), rarely (≥ 1/10 000, < 1/10 1000), very rare (<1/10,000). Table 1: Adverse reactions reported in connection with the use of nimodipine in ischemic neurological disorders. Organ system class (MedDRA) Uncommon Rare Blood and lymphatic system disorders Thrombocytopenia Immune system disorders Allergic reactions, rashes Nervous system disorders Headaches Cardiac disorders Tachycardia Bradycardia Vascular disorders Hypotension, vasodilation Gastrointestinal tract disorders Nausea Ileus Hepatobiliary system disorders Transient elevation of liver enzymes Table 2: Adverse reactions to nimodipine reported in connection with the use of impaired brain function in elderly patients. Organ system class (MedDRA) Common Uncommon Immune system disorders Allergic reactions, rash Nervous system disorders Headaches, vertigo, dizziness, hyperkinesia, tremor Cardiac disorders Palpitations, tachycardia Vascular disorders Hypotension, vasodilation Syncope, edema Gastrointestinal disorders Constipation, diarrhea , Flatulence OverdoseSymptoms: a pronounced decrease in blood pressure, tachycardia or bradycardia, vomiting, pain in the epigastric region, symptoms of impaired activity of the central nervous system. In case of an overdose, the drug should be stopped immediately. Treatment is symptomatic. First aid includes gastric lavage and activated charcoal. If there is a significant decrease in blood pressure, intravenous dopamine or norepinephrine should be administered. Specific antidotes for nimodipine are unknown. Release form: 30 mg film-coated tablets. In a package of 30 tablets. Shelf life 3 years. Storage conditions Store at a temperature not exceeding 25 ° C, protected from light. Keep out of the reach of children. Conditions for dispensing from pharmacies It is dispensed by doctor's prescription. Buy Nitop tablets p/o 30mg No. 10x3