Zanidip-Recordati, 10 mg 56 pcs

A “slow” calcium channel blocker. Lercanidipine is a racemic mixture of right- (R) and left-rotating (S) stereoisomers, a 1,4-dihydropyridine derivative capable of selectively blocking the flow of calcium ions inside vascular wall cells, cardiac cells and smooth muscle cells.

Indications

Active ingredient

How to take, the dosage

The drug is prescribed 10 mg 1 time per day (in the morning) at least 15 minutes before meals. Depending on the individual effect, the drug dose may be increased up to 20 mg. The therapeutic dose is adjusted gradually, if necessary, the dose is increased in 2 weeks after the start of the drug.

The tablets are taken orally, without chewing, with plenty of water.

There is no need to adjust the dose in elderly patients, but continuous monitoring of the patient’s condition is necessary when taking the drug.

In mild to moderate renal or hepatic impairment, no dose adjustment is usually required; the initial dose is 10 mg, and then the dose should be cautiously increased to 20 mg/day. If the antihypertensive effect is too pronounced, the dose should be reduced.

Interaction

The drug should not be taken concomitantly with CYP3A4 inhibitors (hepatic cytochrome P450 isoenzyme) such as ketoconazole, itraconazole, erythromycin (they increase the blood concentration of lercanidipine and lead to potentiation of the antihypertensive effect).

The concomitant administration of lercanidipine with cyclosporine is contraindicated since it leads to increased plasma levels of both substances.

Lercanidipine should not be taken together with grapefruit juice, because this inhibits the metabolism of lercanidipine and potentiates the antihypertensive effect.

Caution should be exercised when taking concomitantly with drugs such as terfenadine, astemizole, quinidine and class III antiarrhythmic drugs (e.g., amiodarone).

Concomitant use with anticonvulsants (e.g., phenytoin, carbamazepine) and rifamycin may decrease plasma levels of lercanidipine and, therefore, decrease the antihypertensive effect of lercanidipine.

In concomitant administration of digoxin, regular monitoring for signs of digoxin intoxication should be performed.

The administration of the drug with midazolam in the elderly leads to increased absorption of lercanidipine and decreased absorption rate.

Metoprolol decreases the bioavailability of lercanidipine by 50%; the bioavailability of metoprolol remains unchanged. This effect may occur due to decreased hepatic blood flow caused by beta-adrenoblockers; therefore, it may also occur when used with other drugs of this group.

Cimetidine at a dose of 800 mg/day does not lead to significant changes in plasma concentrations of lercanidipine, however, special caution is required because the bioavailability of lercanidipine and, therefore, its antihypertensive effect, may increase at higher doses of cimetidine.

When used concomitantly 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 concomitantly with warfarin has no effect on the pharmacokinetics of the latter.

Lercanidipine may be used concomitantly with beta-adrenoblockers, diuretics, ACE inhibitors.

Ethanol may increase the antihypertensive effect of lernidipine.

Special Instructions

Caution should be exercised when prescribing to patients with impaired renal function, CHD (there is a risk of increased angina attacks).

Chronic heart failure should be compensated before starting the drug.

Particular caution should be exercised in the initial stages of treatment in patients with mild to moderate hepatic impairment.

Impact on driving and operating machinery

At the time of treatment, caution should be exercised when performing activities requiring increased attention, driving vehicles, especially at the beginning of treatment and when increasing the dose of the drug (risk of drowsiness, headache, and dizziness).

Contraindications

– decompensated chronic heart failure;

– unstable angina pectoris;

– Left ventricular vascular obstruction;

– recent myocardial infarction (within 1 month);

– severe hepatic impairment;

– renal impairment (glomerular filtration rate less than 39 ml/min);

– simultaneous use with potent CYP3A4 isoenzyme inhibitors (ketoconazole, itraconazole, erythromycin), as well as with grapefruit juice, cyclosporine;

– lactase deficiency, lactose intolerance, glucose/galactose malabsorption syndrome;

– Children and adolescents under 18 years of age (efficacy and safety not established);

– pregnancy;

– period of lactation;

– women of childbearing age who are not using reliable contraception;

– hypersensitivity to lercanidipine, other dihydropyridine-type derivatives or any component of the drug.

With caution: mild to moderate hepatic impairment; sinus node weakness syndrome (without pacemaker); left ventricular insufficiency and CHD; chronic heart failure; concomitant use of beta-adrenoblockers, digoxin.

Side effects

The incidence of adverse events was classified as follows: very frequently (1/10), frequently (1/100), infrequently (1/1000), rarely (1/10 000), very rarely (< 1/10 000).

Nervous system disorders: rare – drowsiness; infrequent – headache, dizziness.

The immune system: very rare – hypersensitivity.

The cardiovascular system: infrequent – tachycardia, palpitations, skin rush; rare – angina; very rare – fainting, marked BP decrease, chest pain, myocardial infarction.

The digestive system: rarely – nausea, vomiting, diarrhea, abdominal pain, dyspepsia; very rare – reversible increase in liver enzymes activity.

Skin: rare – skin rash.

Muscular system: rarely – myalgia.

Urinary system: rarely – polyuria.

Others: infrequent – peripheral edema; rare – asthenia, increased fatigue; very rare – gum hyperplasia.

Overdose

Symptoms: peripheral vasodilation with marked BP reduction and reflex tachycardia, increased frequency and duration of angina attacks, myocardial infarction.

Treatment: symptomatic therapy is carried out.

Pregnancy use

Similarities