Lercamen 20,20 mg 28 pcs.

Selective slow calcium channel blocker with predominant effect on blood vessels, dihydropyridine derivative. Inhibits transmembrane flow of calcium ions into vascular smooth muscle cells. < br>

The mechanism of antihypertensive action of lercanidipine is due to a direct relaxant effect on vascular smooth muscle cells, resulting in a decrease of RPS. Despite relatively short plasma elimination half-life, lercanidipine has prolonged antihypertensive effect due to high membrane distribution coefficient. < br>

Lack of negative inotropic effect due to high vascular selectivity. < br>

Acute arterial hypotension with reflex tachycardia occurs rarely due to the gradual development of vasodilation when taking lercanidipine. Lercanidipine is a racemic mixture of (+)R- and (-)S-enantiomers. The antihypertensive effect of lercanidipine is primarily due to the S-enantiomer. Duration of therapeutic effect – 24 h

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Indications

Essential hypertension of degree I-II severity.

Active ingredient

Composition

Active ingredients:

Lercanidipine hydrochloride 20 mg.

Auxiliary substances:

Lactose monohydrate – 60 mg,

Microcrystalline cellulose – 78 mg,

Sodium carboxymethyl starch (type A) – 31 mg,

Povidone K30 – 9 mg,

Magnesium stearate – 2 mg

Shell contents:

Opadray 02F25077 – 6 mg (hypromellose – 3.825 mg, talc – 0.3 mg, titanium dioxide – 1.2 mg, macrogol 6000 – 0.6 mg, iron oxide (III) – 0.075 mg).

How to take, the dosage

The drug is taken orally at least 15 minutes before a meal, preferably in the morning, without chewing, with plenty of water.

The drug is prescribed at 10 mg 1 time per day. Depending on individual tolerance of the patient, the dose can be increased up to 20 mg.

The therapeutic dose is adjusted gradually, because the maximum antihypertensive effect develops approximately 2 weeks after starting the drug. It is unlikely that the efficacy of the drug will increase with increasing doses over 20 mg/day, at the same time increasing the risk of side effects.

The pharmacokinetic profile and data from clinical studies show that no dose adjustment of Lercamen® is required in elderly patients. However, caution should be exercised during initial treatment with Lercamen® in this group of patients.

When using Lercamen® in patients with mild to moderate renal and hepatic impairment, caution should be exercised.

In patients with renal failure (CKD greater than 30 ml/min) or mild to moderate hepatic failure, the initial dose is 10 mg and then the dose is increased with caution to 20 mg/day.

The antihypertensive effect may be enhanced in patients with mild to moderate hepatic impairment and dose adjustment (reduction) may be required.

In patients with renal failure (CKD less than 30 ml/min) and in patients with severe hepatic failure the use of Lercamen® is contraindicated.

Interaction

In complex therapy, it is well compatible with β-adrenoblockers. diuretics, angiotensin-converting enzyme inhibitors (ACEIs). If Lercamen 20 is used concomitantly with cardiac glycosides, frequent monitoring for signs of digoxin intoxication is necessary.

Concomitant use with cimetidine does not cause significant changes in plasma concentrations of lercanidipine, the bioavailability and hypotensive effect of lercanidipine may be increased at high doses of cimetidine. Caution should be used with CYP ZL4 inhibitors: ketoconazole, intraconazole, erythromycin, etc. When prescribing Lercamen 20 together with inducers of CYP ZA4: antidensants, rifampicin may reduce the hypotensive effect of the drug.

The use of grapefruit juice may increase the hypotensive effect. The use of ethanol may potentiate the effect of the drug. Influence on driving and operating machinery During the period of the drug use patients should be especially careful when driving vehicles and performing other potentially dangerous activities requiring high speed of psychomotor reactions during the treatment with Lercamenom 20.

Special Instructions

Impact on ability to drive vehicles and other mechanisms requiring high concentration

As dizziness, asthenia, fatigue and in rare cases drowsiness may occur during the therapy with Lercamen® , patients should be especially careful while using the drug to drive vehicles and engage in other potentially dangerous activities requiring high speed psychomotor reactions.

Contraindications

Chronic heart failure (decompensation stage); Unstable angina pectoris; aortic stenosis; within 1 month after myocardial infarction; expressed liver dysfunction; impaired renal function (creatinine clearance less than 12 ml/min); lactose intolerance, galactosemia. glucose/galactose malabsorption syndrome.

Pregnancy and lactation; women of childbearing age not using reliable contraception; Age less than 18 years (efficacy and safety not established); Hypersensitivity to lercanidipine, other dihydropyridine derivatives or any component of the drug.

With caution: renal and/or hepatic insufficiency, advanced age, sinus node weakness syndrome (without pacemaker), coronary heart disease, left ventricular dysfunction.

Side effects

The drug is well tolerated.

Rarely:

The effects associated with the vasodilator properties of the drug – peripheral edema, feeling of blood rush to the face, palpitations, tachycardia, chest pain, decreased blood pressure, angina pectoris, myocardial infarction, asthenia, fatigue, headache, dizziness: very rare: gastrointestinal disorders (dyspepsia, nausea, vomiting, epigastric pain, diarrhea), increased activity of “liver” enzymes (reversible), polyuria, skin rash, drowsiness, myalgia, gum hyperplasia.

Overdose

In case of lercanidipine overdose, symptoms similar to those of other dihydropyridine derivatives will presumably be observed: peripheral vasodilation with marked BP decrease and reflex tachycardia.

The treatment: conducting symptomatic therapy; in case of marked BP decrease, loss of consciousness cardiovascular therapy is indicated, in bradycardia – intravenous injection of atropine.

There have been data on 3 cases of overdose when taking lercanidipine in doses of 150 mg, 280 mg and 800 mg for the purpose of suicide.

Drowsiness has been observed in cases in which 150 mg of lercanidipine + alcohol (unspecified amount) was taken.

Treatment: gastric lavage, administration of activated charcoal.

In case of administration of 280 mg of lercanidipine + 5.6 mg of moxonidine the following symptoms were observed: cardiogenic shock, pronounced myocardial ischemia, mild renal failure.

Treatment: cardiac glycosides, diuretics (furosemide), high doses of catecholamines, plasma substitutes. If 800 mg of lercanidipine was administered, nausea and marked BP decrease were observed.

Treatment: administration of activated charcoal and laxative, IV dopamine.

In all cases of overdose all patients survived. There is no information on dialysis efficacy for lercanidipine. It is most likely that due to the high binding of lercanidipine to plasma proteins, dialysis may not be effective.

Pregnancy use

The use of the drug Lercamen® is contraindicated in pregnancy and during breastfeeding as well as in women of childbearing age in the absence of reliable contraception.

In preclinical studies no teratogenic effect of lercanidipine was found in rats and rabbits, reproductive function of rats was unchanged.

In the absence of clinical experience with lercanidipine in pregnancy and during breastfeeding, and because other dihydropyridine derivatives are known to have teratogenic effects in animals, lercanidipine is not recommended for use in pregnancy and in women of childbearing age who do not use reliable methods of contraception.

Due to the high lipophilicity of lercanidipine, its penetration into breast milk can be assumed, so the drug is not recommended during breastfeeding.

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