Zanidip Recordati p / o 10mg tablets, No. 28

Essential hypertension of mild to moderate severity.

Inside.

The drug ZanidipЃ Recordati is prescribed 10 mg once a day in the morning, at least 15 minutes before meals, without chewing, drinking plenty of water.

The dose can be increased to 20 mg (in case the expected effect is not achieved when taking 10 mg). The therapeutic dose is selected gradually, an increase in the dose to 20 mg is carried out 2 weeks after the start of taking the drug.

Use in elderly patients

No dose adjustment is required, however, when taking the drug, constant monitoring of the patient's condition is necessary.

Use in patients with impaired renal or hepatic function

In the presence of renal or hepatic insufficiency of mild or moderate severity, as a rule, dose adjustment is not required, the initial dose is 10 mg, an increase in the dose to 20 mg per day should be carried out with caution. If the antihypertensive effect is too pronounced, the dose should be reduced.

One film-coated tablet contains:

active substance: lercanidipine hydrochloride - 20 mg;

excipients: lactose monohydrate - 60 mg, microcrystalline cellulose - 78 mg, sodium carboxymethyl starch - 31 mg, povidone-K30 - 9 mg, magnesium stearate - 2 mg;

shell composition: dosage 10 mg - yellow opadry (OY-SR-6497) 3 mg [hypromellose, talc, titanium dioxide (E171), macrogol-6000, iron dye yellow oxide (E172)]; dosage 20 mg - pink opadry (02F25077) 6 mg [hypromellose, talc, titanium dioxide (E171), macrogol-6000, iron dye red oxide (E172)].

Х Hypersensitivity to lercanidipine, other dihydropyridine derivatives or any component of the drug;
Х Chronic heart failure in the stage of decompensation;
Х Unstable angina pectoris, obstruction of blood vessels emanating from the left ventricle of the heart, recent myocardial infarction (within 1 month);
Х Severe liver dysfunctions, renal dysfunctions (glomerular filtration rate less than 39 ml / min);
Х Simultaneous use with powerful inhibitors of the isoenzyme CYP3A4 (ketoconazole, itraconazole, erythromycin), as well as with grapefruit juice, cyclosporine;
Х Pregnancy and lactation period; use in women of childbearing age who do not use reliable contraception;
Х Children under 18 years of age (efficacy and safety have not been established);
Х Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully

Х Dysfunction of the liver of mild to moderate severity;
Х Sick sinus syndrome (without a pacemaker);
Х Left ventricular failure and coronary heart disease;
Х Chronic heart failure;
Х Simultaneous reception of beta-blockers, digoxin.

Trade name of the drug: ZanidipЃ Recordati

INN (international non-proprietary name): lercanidipine

Dosage form:

film-coated tablets

Composition

One film-coated tablet contains:

active substance: lercanidipine hydrochloride 10 mg or 20 mg;

excipients: lactose monohydrate 30 mg / 60 mg, microcrystalline cellulose 39 mg / 78 mg, sodium carboxymethyl starch 15.5 mg / 31 mg, povidone-K30 4.5 mg / 9 mg, magnesium stearate 1 mg / 2 mg;

shell composition: dosage 10 mg - yellow opadry (OY-SR-6497) 3 mg [hypromellose, talc, titanium dioxide (E171), macrogol-6000, iron dye yellow oxide (E172)]; dosage 20 mg - pink opadry (02F25077) 6 mg [hypromellose, talc, titanium dioxide (E171), macrogol-6000, iron dye red oxide (E172)].

Description

Dosage 10 mg: Round biconvex film-coated tablets of light yellow color, with a scoring on one side, on a break of light yellow color.

Dosage 20 mg: Pink to dark pink coated round biconvex tablets with a scoring on one side, light yellow on the fracture.

Pharmacotherapeutic group

Slow calcium channel blocker.

ATC code: —08—ј13

Pharmacological properties

Pharmacodynamics.

Slow calcium channel blocker. Lercanidipine is a racemic mixture of right- (R) and levorotatory (S) stereoisomers, a 1,4-dihydropyridine derivative, capable of selectively blocking the flow of calcium ions into vascular wall cells, 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 within 5-7 hours after ingestion and its duration lasts for a day (24 hours). Due to the high selectivity for vascular smooth muscle cells, there is no negative inotropic effect.Lercanidipine is metabolically neutral and has no significant effect on serum lipoproteins and apolipoproteins, and does not alter the lipid profile in hypertensive patients.

Pharmacokinetics.

- absorption: after oral administration, lercanidipine is absorbed from the gastrointestinal tract (GIT) almost completely. The maximum concentration in blood plasma is reached after 1.5-3 hours and is 3.3 ng / ml and 7.66 ng / ml after taking 10 and 20 mg, respectively.

- distribution: distribution from blood plasma to tissues and organs is fast. The connection with blood plasma proteins exceeds 98%. In patients with renal and hepatic insufficiency, the content of plasma proteins is reduced, therefore, the free fraction of lercanidipine may be increased.

- metabolism: metabolized during the 'primary passage' through the liver by biotransformation by the isoenzyme of the CYP3A4 system with the formation of a number of metabolites that do not have pharmacological activity.

- excretion: occurs by the kidneys and intestines after biotransformation. There are 2 phases of lercanidipine release: early (half-life value (T1 / 2): 2-5 hours) and final (T1 / 2: 8-10 hours). The drug in unchanged form is practically not detected in urine and feces. Does not cumulate upon repeated use.

Indications for use

• Essential hypertension of mild to moderate severity.

Contraindications

Х Hypersensitivity to lercanidipine, other dihydropyridine derivatives or any component of the drug;
Х Chronic heart failure in the stage of decompensation;
Х Unstable angina pectoris, obstruction of blood vessels emanating from the left ventricle of the heart, recent myocardial infarction (within 1 month);
Х Severe liver dysfunctions, renal dysfunctions (glomerular filtration rate less than 39 ml / min);
Х Simultaneous use with powerful inhibitors of the isoenzyme CYP3A4 (ketoconazole, itraconazole, erythromycin), as well as with grapefruit juice, cyclosporine;
Х Pregnancy and lactation period; use in women of childbearing age who do not use reliable contraception;
Х Children under 18 years of age (efficacy and safety have not been established);
Х Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully

Х Dysfunction of the liver of mild to moderate severity;
Х Sick sinus syndrome (without a pacemaker);
Х Left ventricular failure and coronary heart disease;
Х Chronic heart failure;
Х Simultaneous reception of beta-blockers, digoxin.

Application during pregnancy and during breastfeeding

The drug is contraindicated during pregnancy and during breastfeeding.

Method of administration and dosage

Inside.

The drug ZanidipЃ-Recordati is prescribed 10 mg once a day in the morning, at least 15 minutes before meals, without chewing, drinking plenty of water.

The dose can be increased to 20 mg (in case the expected effect is not achieved when taking 10 mg). The therapeutic dose is selected gradually, an increase in the dose to 20 mg is carried out 2 weeks after the start of taking the drug.

Use in elderly patients

No dose adjustment is required, however, when taking the drug, constant monitoring of the patient's condition is necessary.

Use in patients with impaired renal or hepatic function

In the presence of renal or hepatic insufficiency of mild or moderate severity, as a rule, dose adjustment is not required, the initial dose is 10 mg, an increase in the dose to 20 mg per day should be carried out with caution. If the antihypertensive effect is too pronounced, the dose should be reduced.

Side effect

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 side of the cardiovascular system: not often - tachycardia, palpitations; 'Hot 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 side of the skin: rarely - skin rash;

From the side of 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.

Overdose

Symptoms: peripheral vasodilation with a marked decrease in blood pressure (BP) and reflex tachycardia, an increase in the frequency and duration of angina attacks, myocardial infarction. Treatment: symptomatic therapy.

Interaction with other medicinal products

The drug should not be taken simultaneously with inhibitors of CYP3A4 (isoenzyme of liver cytochrome P450), such as ketoconazole, intraconazole, erythromycin (increase the concentration of lercanidipine in the blood and lead to potentiation of the antihypertensive effect). The simultaneous administration 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 the metabolism of lercanidipine and potentiation of the antihypertensive effect.

Caution must be exercised when coadministered with drugs such as terfenadine, astemizole, quinidine, and a third class of antiarrhythmic drugs (eg, amiodarone). Simultaneous administration with anticonvulsants (for example, phenytoin, carbamazepine) and rifamycin can lead to a decrease in the level of lercanidipine in the blood plasma and, in this regard, to a decrease in the antihypertensive effect of lercanidipine.

With the simultaneous administration of digoxin, it is necessary to carry out regular monitoring for signs of intoxication with digoxin.

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 can occur due to a decrease in hepatic blood flow, which is caused by beta-blockers, therefore, it can also manifest itself when used with other drugs of 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 care 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 concurrently with warfarin does not affect the pharmacokinetics of the latter. Lercanidipine can be used simultaneously with beta-blockers, diuretics, angiotensin-converting enzyme (ACE) inhibitors. Ethanol can enhance the antihypertensive 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), in relation to chronic heart failure: it is necessary to compensate before using the drug. Particular care should be taken in the initial stages of treatment in patients with mild to moderate liver failure.

Influence on the ability to drive machinery and a car

During the period of treatment, care must be taken when performing work requiring increased attention, when driving vehicles, especially at the beginning of treatment and when the dose of the drug is increased (the risk of drowsiness, headache and dizziness).

Release form

Film-coated tablets 10 mg, 20 mg.

7, 14, 15, 25, 28, 30 tablets in a blister made of opaque PVC film / aluminum foil. 1, 2, 3, 4, 5, 6, 7 blisters with instructions for use in a cardboard box.

Storage conditions

At a temperature not higher than 30 ? C. Keep out of the reach of children.

Shelf life

3 years.

Do not use after the expiration date.

Vacation conditions

On prescription.