Zanidip-Record pills. 20 mg N28
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Active ingredients
Lercanidipine
Release form
Pills
Composition
Lercanidipine hydrochloride 20 mg adjuvants: lactose monohydrate — 60 mg, microcrystalline cellulose — 78 mg, sodium carboxymethyl starch — 31 mg, povidone K30 — 9 mg, magnesium stearate — 2 mg. talc, titanium dioxide (e171), macrogol 6000, iron dye red oxide (e172)).
Pharmacological effect
Slow calcium channel blocker. Lercanidipine is a racemic mixture of right- (R) and left-rotating (S) stereoisomers, a derivative of 1,4-dihydropyridine, capable of selectively blocking the flow of calcium ions into the vascular wall cells, cardiac cells and smooth muscle cells. The mechanism of antihypertensive action is due to a direct relaxing effect on smooth muscle vascular cells. It has a prolonged antihypertensive effect. The therapeutic effect is achieved 5-7 hours after ingestion and its duration is maintained for 24 hours (24 hours). Due to the high selectivity to vascular smooth muscle cells, there is no negative inotropic effect. Zanidip Recordati is a metabolically neutral drug and does not have a significant effect on serum lipoproteins and apolipoproteins, and does not alter the lipid profile in patients with arterial hypertension.
Pharmacokinetics
AbsorptionAfter oral administration, lercanidipine is almost completely absorbed from the gastrointestinal tract. Cmax in plasma is reached in 1.5-3 hours and amounts to 3.3 ng / ml and 7.66 ng / ml after taking 10 mg and 20 mg, respectively. Distribution Distribution from blood plasma to tissues and organs occurs quickly. Plasma protein binding exceeds 98%. When reused, it does not cumulate. Metabolism Metabolized during the initial passage through the liver by CYP3A4 biotransformation with the formation of a number of metabolites that do not have pharmacological activity. Exit by excretion by the kidneys and intestines after biotransformation. There are 2 phases of elimination of lercanidipine: early (T1 / 2 - 2-5 h) and final (T1 / 2 - 8-10 h). The drug in an unchanged form is practically not detected in the urine and fecal masses. Pharmacokinetics in special clinical situations in patients with renal and hepatic insufficiency the plasma protein content is reduced, therefore the free fraction of lercanidipine can be increased.
Indications
- Essential hypertension mild and moderate severity.
Contraindications
- Chronic heart failure in the stage of decompensation; - Unstable angina; - Obstruction of vessels emanating from the left ventricle of the heart; - Recently suffered myocardial infarction (within 1 month); - Severe abnormal liver function; - Renal dysfunction (glomerular filtration rate less than 39 ml / min); - simultaneous use with powerful inhibitors of CYP3A4 isoenzyme (ketoconazole, itraconazole, erythromycin), as well as with grapefruit juice, cyclosporine; - lactase deficiency, lactose intolerance, malabsorption syndrome glucose / galactose; - children and adolescents under 18 years of age (efficacy and safety have not been established); - pregnancy; - lactation period; - women of childbearing age who do not use reliable contraceptives; - hypersensitivity to lercanidipine, other derivatives of the dihydropyridine series or any component drug.C caution: abnormal liver function mild and moderate severity; sick sinus syndrome (without pacemaker); left ventricular failure and ischemic heart disease; chronic heart failure; simultaneous reception of beta adrenoblockers, digoxin.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Dosage and administration
The drug is prescribed 10 mg 1 time / day (in the morning) at least 15 minutes before meals. Depending on the individual effect, the dose of the drug can be increased to 20 mg.The therapeutic dose is adjusted gradually, if necessary, the dose is increased 2 weeks after starting the drug. Tablets are taken orally without chewing, drinking a sufficient amount of water. In elderly patients, dose adjustment is not required, however, when taking the drug, constant monitoring of the patients is necessary. the presence of mild to moderate renal or hepatic failure, as a rule, dose adjustment is not required; the initial dose is 10 mg, then the dose should be carefully increased to 20 mg / day. If the antihypertensive effect is too pronounced, the dose should be reduced.
Side effects
The frequency of occurrence of adverse events was classified as follows: very often (1/10), often (1/100), infrequently (1/1000), rarely (1/10 000), very rarely (<1/10 000). nervous system: rarely - drowsiness; infrequently - headache, dizziness. From the immune system: very rarely - hypersensitivity. From the cardiovascular system: infrequently - tachycardia, feeling of heartbeat, flushing of blood to the skin of the face; rarely - angina; very rarely - fainting, marked decrease in blood pressure, chest pain, myocardial infarction. On the digestive system: rarely - nausea, vomiting, diarrhea, abdominal pain, dyspepsia; very rarely - a reversible increase in liver enzymes. From the skin: rarely - skin rash. From the musculoskeletal system: rarely - myalgia. From the urinary system: rarely - polyuria. Other: infrequent - peripheral edema; rarely - asthenia, fatigue; very rarely - gingival hyperplasia.
Overdose
Symptoms: peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia, an increase in the frequency and duration of angina attacks, myocardial infarction. Treatment: symptomatic therapy is carried out.
Interaction with other drugs
The drug should not be taken simultaneously with inhibitors of CYP3A4 (liver cytochrome P450 isoenzyme), such as ketoconazole, itraconazole, erythromycin (they increase the concentration of lercanidipine in the blood and lead to potentiation of the antihypertensive effect).this leads to an increase in the content of both substances in the blood plasma. Lercanidipine cannot be taken together with grapefruit juice, as this leads to a depression in the metabolism of lercanidipine and to a potentiation of the antihypertensive effect. III (e.g. amiodarone). Simultaneous administration with anticonvulsants (e.g. phenytoin, carbamazepine) and rifamycin may lead to a decrease in high levels of lercanidipine in the blood plasma and, therefore, reduce the antihypertensive effect of lercanidipine. When you take digoxin at the same time, you should regularly monitor signs of digoxin intoxication. Taking medication with midazolam in old age leads to an increase in absorption of lercanidipine and a decrease in the rate of absorption of lekanidipine. reduces the bioavailability of lercanidipine by 50%, while the bioavailability of metoprolol remains unchanged. This effect may occur due to a decrease in hepatic blood flow, which is caused by beta-blockers, and therefore may also manifest when used with other drugs in this group. Cimetidine at a dose of 800 mg / day does not lead to significant changes in plasma concentration of lercanidipine, however, special caution is required because with higher doses of cimetidine, the bioavailability of lercanidipine, and therefore its antihypertensive effect, may increase. When used simultaneously with simvastatin, the drug should be taken in the morning and simvastatin in the evening. Fluoxetine has no effect on lerkanidipine pharmacokinetics. warfarin has no effect on the pharmacokinetics of the latter. Lercanidipine can be used simultaneously with beta-blockers, diuretics, and ACE inhibitors. Ethanol can enhance ant Hypertensive effect of medicinidipine.
special instructions
Care should be taken when prescribing to patients with impaired renal function, ischemic heart disease (there is a risk of increased angina attacks). Before starting the drug, it is necessary to compensate for chronic heart failure. Particular caution should be taken at the initial stages of treatment.patients with mild and moderate degree of liver failure. Effect on the ability to drive vehicles and control mechanisms During the period of treatment, care must be taken when performing work that requires increased attention, while driving, especially at the beginning of treatment and when increasing the dose of the drug (risk of drowsiness, headache and dizziness).