Zanidip-Recordati, 56 pcs., 10 mg, film-coated tablets
The drug should not be taken simultaneously with inhibitors of CYP3A4 (liver cytochrome P450 isoenzyme), such as ketoconazole, itraconazole, erythromycin (increase the concentration of lercanidipine in the blood and lead to potentiation of the antihypertensive effect).
Concomitant use of lercanidipine with cyclosporine is contraindicated, because this leads to an increase in the content of both substances in the blood plasma. Lercanidipine should not be taken with grapefruit juice, as this leads to inhibition of lercanidipine metabolism and potentiation of the antihypertensive effect.
Caution must be exercised when taken concomitantly with drugs such as terfenadine, astemizole, quinidine and class III antiarrhythmic drugs (for example, amiodarone).
Concomitant use with anticonvulsants (eg phenytoin, carbamazepine) and rifamycin may lead to a decrease in the plasma level of lercanidipine and, therefore, a decrease in the antihypertensive effect of lercanidipine.
When taking digoxin concomitantly, it is necessary to regularly monitor for signs of digoxin intoxication.
Taking the drug with midazolam in old age leads to an increase in the absorption of lercanidipine and a decrease in the rate of absorption.
Metoprolol 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 may therefore also occur when used with other drugs in this group.
Cimetidine at a dose of 800 mg per day does not lead to significant changes in the concentration of lercanidipine in the blood plasma, but special caution is required because at higher doses of cimetidine, the bioavailability of lercanidipine, and therefore its antihypertensive effect, may increase.
When used concomitantly with simvastatin, Zanidip®-Recordati should be taken in the morning and simvastatin in the evening.
Fluoxetine has no effect on the pharmacokinetics of lercanidipine.
Taking lercanidipine simultaneously with warfarin does not affect the pharmacokinetics of the latter.
Lercanidipine can be used simultaneously with beta-blockers, diuretics, and ACE inhibitors.
Ethanol may enhance the antihypertensive effect of lercanidipine.
Buy Zanidip-Recordati film-coated tablets 20 mg No. 28 in pharmacies
Zanidip-Recordati Buy Zanidip-Recordati in pharmacies Zanidip-Recordati in the medicine directory DOSAGE FORMS film-coated tablets 20 mg
MANUFACTURERS Recordati Chemical and Pharmaceutical Industry S.p.A. (Italy)
GROUP Calcium channel blockers of the dihydropyridine group
INTERNATIONAL NON-PROPENTED NAME Lercanidipine
SYNONYMS Lerkamen 10, Lerkamen 20
Description
ZANIDIP-RECORDATI
Package
28 pcs.
Pharmacological action Zanidip-Recordati is a blocker of “slow” calcium channels. Lercanidipine is a racemic mixture of dextro- (R) and levorotatory (S) stereoisomers, a derivative of 1,4-dihydropyridine, capable of selectively blocking the flow of calcium ions into the cells of the vascular wall, cardiac cells and smooth muscle cells. The mechanism of hypotensive action is due to a direct relaxing effect on vascular smooth muscle cells. Has a prolonged antihypertensive effect. The therapeutic effect is achieved 5-7 hours after oral administration and its duration persists throughout the day (24 hours). Due to its high selectivity for vascular smooth muscle cells, there is no negative inotropic effect. Lercanidipine is a metabolically neutral drug and does not have a significant effect on the content of lipoproteins and apolipoproteins in the blood serum, and does not change the lipid profile in patients with arterial hypertension.
Indications Essential hypertension of mild to moderate severity.
Contraindications Hypersensitivity, decompensated CHF, unstable angina, aortic stenosis, recent myocardial infarction (within 1 month), severe liver dysfunction, renal dysfunction (creatinine clearance less than 12 ml/min), women of childbearing age who do not use reliable contraception, pregnancy , lactation period, childhood and adolescence (up to 18 years). For dosage forms containing lactose (additionally): lactose intolerance, galactosemia, glucose/galactose malabsorption syndrome. Carefully. Renal and/or liver failure, CVS (without a pacemaker), coronary artery disease, LV dysfunction, old age.
Method of administration and dosage Zanidip-Recordati is taken orally, in the morning, at least 15 minutes before meals, without chewing, with a sufficient amount of water, 10 mg 1 time per day. The dose can be increased to 20 mg (depending on the individual effect). The dose is increased to 20 mg 2 weeks after starting the drug. In case of mild or moderate renal or hepatic impairment, increasing the dose to 20 mg per day should be done with caution.
Side effects WHO statistics: very often - 1/10 appointments, often - 1/100 appointments, not often - 1/1000 appointments, rarely - 1/10000 appointments, very rarely - less than 1/10000 appointments.
From the nervous system: rarely - drowsiness; infrequently - headache, dizziness;
From the immune system: very rarely - hypersensitivity;
From the cardiovascular system: not often - tachycardia, palpitations; “flushes” of blood to the skin of the face; rarely - angina pectoris; very rarely - fainting, marked decrease in blood pressure, chest pain, myocardial infarction;
From the digestive system: rarely - nausea, vomiting, diarrhea, abdominal pain, dyspepsia, very rarely - increased activity of liver enzymes (reversible);
From the skin: rarely - skin rash;
From the musculoskeletal system: rarely - myalgia;
From the urinary system: rarely - polyuria;
General disorders and local reactions: not often - peripheral edema, rarely - asthenia, increased fatigue; very rarely - gingival hyperplasia.
Special instructions During the treatment period, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Drug interactions Compatible with beta-blockers, diuretics, ACE inhibitors. When used concomitantly with cardiac glycosides, it is necessary to monitor the symptoms and signs of digoxin intoxication. Concomitant use with cimetidine does not cause significant changes in the plasma concentration of lercanidipine; at high doses of cimetidine, the bioavailability and, accordingly, the hypotensive effect of lercanidipine increases. Use with caution with CYP3A4 inhibitors (including ketoconazole, itraconazole, erythromycin). Inducers of the CYP3A4 isoenzyme (antidepressants, rifampicin) may reduce the hypotensive effect of the drug. Grapefruit juice and ethanol may enhance the hypotensive effect of lecarnidipine.
Overdose Symptoms: peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia, increased frequency and duration of angina attacks, myocardial infarction. Treatment: symptomatic therapy.
Storage conditions : At a temperature not exceeding 30 °C. Keep out of the reach of children.
Zanidip-recordati tablet p/o film 10mg 28 pcs
The drug should not be taken simultaneously with inhibitors of CYP3A4 (liver cytochrome P450 isoenzyme), such as ketoconazole, intraconazole, erythromycin (increase the concentration of lercanidipine in the blood and lead to potentiation of the antihypertensive effect). The simultaneous use of lercanidipine with cyclosporine is contraindicated, as this leads to an increase in the content of both substances in the blood plasma. Lercanidipine should not be taken together with grapefruit juice, as this leads to inhibition of lercanidipine metabolism and potentiation of the antihypertensive effect.
Caution must be exercised when taken concomitantly with drugs such as terfenadine, astemizole, quinidine and third class antiarrhythmic drugs (for example, amiodarone).
Concomitant use with anticonvulsants (for example, phenytoin, carbamazepine) and rifamycin may lead to a decrease in the plasma level of lercanidipine and, therefore, a decrease in the antihypertensive effect of lercanidipine.
When taking digoxin concomitantly, it is necessary to regularly monitor for signs of digoxin intoxication.
Taking the drug with midazolam in old age leads to an increase in the absorption of lercanidipine and a decrease in the rate of absorption.
Metoprolol 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 may therefore also occur when used with other drugs in this group.
Cimetidine at a dose of 800 mg per day does not lead to significant changes in the concentration of lercanidipine in the blood plasma, however, special caution is required, since at 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 the pharmacokinetics of lercanidipine.
Taking lercanidipine simultaneously with warfarin does not affect the pharmacokinetics of the latter. Lercanidipine can be used simultaneously with beta-blockers, diuretics, and angiotensin-converting enzyme (ACE) inhibitors. Ethanol may enhance the antihypertensive effect of lecarnidipine.
Zanidip®-Recordati
Contraindications for simultaneous use
CYP3A4 inhibitors
Lercanidipine is known to be metabolized by the enzyme CYP3A4 and therefore CYP3A4 inhibitors used concomitantly may interact with the metabolism and elimination of lercanidipine. Concomitant use with the strong CYP3A4 inhibitor, ketoconazole, has been shown to increase plasma concentrations of lercanidipine (15-fold increase in AUC and 8-fold increase in Cmax for the S-lercanidipine enantiomer).
Avoid co-administration of lercanidipine with CYP3A4 inhibitors (for example, ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin, clarithromycin) (see section "Contraindications").
Cyclosporine
Increased plasma concentrations of both lercanidipine and cyclosporine were observed after concomitant use. A study in young healthy volunteers showed that when cyclosporine was administered 3 hours after administration of lercanidipine, plasma concentrations of lercanidipine were unchanged, while the AUC of cyclosporine increased by 27%. However, coadministration of lercanidipine with cyclosporine resulted in a 3-fold increase in lercanidipine plasma concentrations and a 21% increase in cyclosporine AUC.
Cyclosporine and lercanidipine should not be used together (see section "Contraindications").
Grapefruit or grapefruit juice
Lercanidipine should not be taken with grapefruit or grapefruit juice because simultaneous use may lead to an increase in the systemic availability of the drug and an increase in the antihypertensive effect (see section "Contraindications").
Concomitant use is not recommended
CYP3A4 inducers
Concomitant use of lercanidipine with CYP3A4 inducers such as anticonvulsants (eg, phenytoin, phenobarbital, carbamazepine) and rifampicin should be approached with caution as the antihypertensive effect may be reduced and blood pressure should be monitored more frequently than usual ( see "With Caution" section).
Ethanol (alcohol)
When taking vasodilating antihypertensive drugs, alcohol should be avoided as it may enhance their effects.
Precautions including dose adjustment
CYP3A4 substrates
Caution should be exercised when lercanidipine is co-administered with other CYP3A4 substrates such as terfenadine, astemizole, class III antiarrhythmics such as amiodarone, sotalol (See Precautions section).
Midazolam
When 20 mg of midazolam was coadministered orally in elderly volunteers, the absorption of lercanidipine was increased (by approximately 40%) and the rate of absorption was decreased (tmax was delayed from 1.75 to 3 hours) (See Precautions). Midazolam concentrations did not change.
Metoprolol
When lercanidipine was co-administered with metoprolol (a beta blocker that is primarily metabolized in the liver), the bioavailability of metoprolol was not affected, whereas the bioavailability of lercanidipine was reduced by 50%. This effect may be due to a decrease in hepatic blood flow caused by beta-blockers and may occur with other drugs in this class. Therefore, lercanidipine can be used safely with β-adrenergic blocking drugs, but dosage adjustments may be required (See Precautions section).
Digoxin
When lercanidipine (20 mg) was co-administered with digoxin, there was no evidence of pharmacokinetic interaction. However, there was a mean increase in digoxin Cmax of 33%, while AUC and renal clearance changed little. Therefore, patients receiving concomitant treatment with digoxin should be monitored for digitalis toxicity (See Precautions section).
Concomitant use with other drugs
Fluoxetine
An interaction study with fluoxetine (an inhibitor of CYP2D6 and CYP3A4) conducted in volunteers aged 65 ± 7 years (mean ± SD) did not reveal clinically significant changes in the pharmacokinetics of lercanidipine.
Cimetidine
Co-administration of cimetidine (800 mg/d) does not cause significant changes in plasma concentrations of lercanidipine, but caution should be exercised at higher doses as the bioavailability and antihypertensive effect of lercanidipine may be increased.
Simvastatin
When repeat doses of 20 mg lercanidipine were given with 40 mg simvastatin, the AUC of lercanidipine did not change significantly, while the AUC of simvastatin increased by 56% and the AUC of its active beta-hydroxykylated metabolite by 28%. It is unlikely that such changes are clinically significant. However, when lercanidipine is taken in the morning and simvastatin in the evening, no drug interactions are observed.
Warfarin
Co-administration of 20 mg lercanidipine in healthy volunteers on an empty stomach did not alter the pharmacokinetics of warfarin.
Diuretics and ACE inhibitors
Lercanidipine can be used simultaneously with diuretics and ACE inhibitors.
Other drugs that affect blood pressure
An increase in the antihypertensive effect can be observed when lercanidipine is taken simultaneously with alpha-blockers, tricyclic antidepressants, and antipsychotics. On the contrary, a decrease in the antihypertensive effect may be observed when used simultaneously with glucocorticosteroids.
