Zanidip-Recordati, pills 10mg 56pcs

Composition

of 1 tablet: Active ingredient: lercanidipine hydrochloride-10 mg; excipients: lactose monohydrate-30 mg, MCC-39 mg; sodium carboxymethyl starch-15.5 mg; povidone K 30-4.5 mg; magnesium stearate-1 mg. shell (dosage 10 mg): Opadry yellow (OY-SR-6497) — 3 mg (hypromellose, talc, titanium dioxide (E 171), macrogol-6000, iron oxide yellow dye (E 172.

Pharmacological action

Slow calcium channel blocker. Lercanidipine is a racemic mixture of right-(R) and left-rotating (S) stereoisomers, a 1,4-dihydropyridine derivative, and is capable of selectively blocking the flow of calcium ions into vascular wall cells, heart cells, and smooth muscle cells. The mechanism of antihypertensive action is due to the direct relaxing effect on vascular smooth muscle cells. It has a prolonged antihypertensive effect. The therapeutic effect is achieved 5-7 hours after ingestion and its duration is maintained for a day (24 hours). Due to its high selectivity to vascular smooth muscle cells, there is no negative inotropic effect. Zanidip ® – Recordati is a metabolically neutral drug and does not significantly affect the content of lipoproteins and apolipoproteins in the blood serum, and also does not change the lipid profile in patients with arterial hypertension. Pharmacokinetics of absorption After oral use, lercanidipine is almost completely absorbed from the gastrointestinal tract. _Cmax in blood plasma is reached in 1.5-3 hours and is 3.3 ng / ml and 7.66 ng/ml after taking 10 mg and 20 mg, respectively. Distributiondistribution from blood plasma to tissues and organs is rapid. Binding to plasma proteins exceeds 98%. When repeated use, it does not accumulate. Metabolismmetabolized during the” primary passage ” through the liver by biotransformation of CYP3A4 with the formation of a number of metabolites that do not have pharmacological activity. Excretion is eliminated by the kidneys and intestines after biotransformation. There are 2 phases of lercanidipine elimination: early (T_1/2 – 2-5 hours) and final (T_1/2 – 8-10 hours). The drug in unchanged form is practically not detected in the urine and feces. Pharmacokinetics in special clinical cases in patients with renal and hepatic insufficiency, the plasma protein content is reduced, so the free fraction of lercanidipine can be increased.

Indications

Zanidip-Recordati is prescribed for the treatment of essential hypertension, which occurs in mild and moderate severity.

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation.

Contraindications

chronic heart failure in the stage of decompensation;

— unstable angina;

— obstruction of blood vessels originating from the left ventricle of the heart;

— recent myocardial infarction (within 1 month);

— severe violations of liver function;

— disorders of renal function (glomerular filtration rate less than 39 ml/min);

— simultaneous use with potent inhibitors of isoenzyme CYP3A4 (ketoconazole, Itraconazole, erythromycin), as well as with grapefruit juice, cyclosporine;

— lactase deficiency, lactose intolerance, the syndrome of malabsorption of glucose/galactose;

— children’s and teenage age up to 18 years (efficacy and safety not established);

— pregnancy;

— lactation period;

— women of childbearing age not using reliable contraception;

— hypersensitivity to lercanidipine, other derivatives digidropiridinovmi series or any component of the drug.

With caution:  liver function disorders of mild and moderate severity; sinus node weakness syndrome (without pacemaker); left ventricular failure and CHD; chronic heart failure; simultaneous use of beta-blockers, digoxin.

Side effects

The frequency of adverse events was classified as follows: very common (1/10), common (1/100), infrequent (1/1000), rare (1/10 000), very rare (

Nervous system disorders:  rarely-drowsiness; infrequently-headache, dizziness.

From the immune system:  very rarely-hypersensitivity.

From the cardiovascular system:  infrequently-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-reversible increase in the activity of liver enzymes.

From the side of the skin:  rarely – skin rash.

Musculoskeletal disorders:  rarely-myalgia.

From the urinary system:  rarely-polyuria.

Other services:  infrequently-peripheral edema; rarely-asthenia, increased fatigue; very rarely-gum hyperplasia.

Interaction

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, 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 should be exercised when taking concomitant medications such as terfenadine, astemizole, quinidine, and Class III antiarrhythmic drugs (for example, amiodarone).

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

When taking digoxin at the same time, it is necessary to regularly monitor for signs of digoxin intoxication.

Taking the drug with midazolam in the elderly 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, so it can also occur when used with other drugs of this group.

Cimetidine at a dose of 800 mg / day does not cause significant changes in the concentration of lercanidipine in blood plasma, however, special caution is required, since at higher doses of cimetidine, the bioavailability of lercanidipine, and, consequently, its antihypertensive effect, may increase.

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 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 lignidipine.

How to take, course of use and dosage

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 selected gradually, if necessary, an increase in the dose is carried out 2 weeks after the start of taking the drug.

Tablets are taken orally, without chewing, with a sufficient amount of water.

In elderly patients, no dose adjustment is required, however, when taking the drug, constant monitoring of the patient’s condition is necessary.

In the presence of mild or moderate renal or hepatic insufficiency, as a rule, no dose adjustment is required; the initial dose is 10 mg, then the dose should be increased with caution to 20 mg / day. If the antihypertensive effect is too pronounced, the dose should be reduced.

Overdose

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

Treatment:  conduct symptomatic therapy.

Special instructions

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

Before starting the use of the drug, it is necessary to compensate for chronic heart failure.

Special care should be taken in the initial stages of treatment of patients with mild to moderate hepatic insufficiency.

Influence on the ability to drive motor vehicles and manage mechanisms

During treatment, care should be taken when performing work that requires increased attention, when driving vehicles, especially at the beginning of treatment and when increasing the dose of the drug (risk of drowsiness, headache and dizziness).

Form of production

Tablets covered with a film-coated light yellow color, round, biconvex, with a risk on one side; at the break – light yellow color.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 30°C.

Shelf

life is 3 years.

Active ingredient

Lercanidipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension