Lerkamen 20, pills 20mg, 28pcs

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 K 30-9 mg,

magnesium stearate-2 mg

Shell composition:

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).

Pharmacological action

Selective blocker of slow calcium channels with a predominant effect on blood vessels, dihydropyridine derivative. Inhibits the transmembrane flow of calcium ions into vascular smooth muscle cells.

The mechanism of antihypertensive action of lercanidipine is due to a direct relaxing effect on vascular smooth muscle cells, resulting in a decrease in OPSS. Despite the relatively short plasma half-life, lercanidipine has a prolonged antihypertensive effect due to its high membrane distribution coefficient.

Due to its high vascular selectivity, it does not have a negative inotropic effect.

Acute arterial hypotension with reflex tachycardia is rare 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 action – 24 hours

Indications

Essential hypertension of I-II degrees of severity.

Use during pregnancy and lactation

The use of Lerkamen® during pregnancy and lactation, as well as in women of childbearing age in the absence of reliable contraception is contraindicated.

Preclinical studies did not reveal the teratogenic effect of lercanidipine in rats and rabbits, and the reproductive function of rats was unchanged.

Due to the lack of clinical experience with the use of lercanidipine during pregnancy and lactation, and since it is known that other dihydropyridine derivatives have had a teratogenic effect in animals, lercanidipine is not recommended for use during 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 for use during breastfeeding.

Contraindications

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

Pregnancy and lactation; women of childbearing age who do not use reliable contraception; Age up to 18 years (efficacy and safety have not been 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:

effects related to the vasodilating properties of the drug – peripheral edema, feeling the tides of blood to the face, palpitations, tachycardia, chest pain, lowering blood pressure, angina, myocardial infarction, asthenia, fatigue, headache, dizziness: very rare: gastrointestinal disturbances (dyspepsia, nausea, vomiting, epigastric pain, diarrhea), increased activity of “liver” enzymes (reversible), polyuria, rash, somnolence, myalgia, gingival hyperplasia.

Interaction

During complex therapy, it is well compatible with beta-blockers. diuretics, angiotensin converting enzyme (ACE) inhibitors. When using Lerkamen 20 simultaneously with cardiac glycosides, it is necessary to conduct frequent monitoring for signs of digoxin intoxication.

Concomitant use with cimetidine does not cause significant changes in the concentration of lercanidipine in plasma, with high doses of cimetidine, the bioavailability and hypotensive effect of lercanidipine may increase. Caution should be exercised when using CYP-4 inhibitors: ketoconazole, intraconazole, erythromycin, etc. When prescribing Lerkamen 20 together with CYP inducers FOR 4: anti-depressants, rifampicin, it is possible to reduce the hypotensive effect of the drug.

When using grapefruit juice, it is possible to increase the hypotensive effect. The use of ethanol can potentiate the effect of the drug. Effects on the ability to drive motor vehicles and manage mechanisms Since dizziness, asthenia, fatigue and in rare cases drowsiness may occur during therapy with Lerkamen 20, patients should drive with extreme caution during the use of the drug and engage in other potentially dangerous activities that require a high rate of psychomotor reactions.

How to take, course of use and dosage

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

Assign 10 mg 1 time / day. Depending on the individual tolerance of the drug to the patient, the dose can be increased to 20 mg.

The therapeutic dose is selected gradually, since the maximum antihypertensive effect develops approximately 2 weeks after the start of taking the drug. It is unlikely that the effectiveness of the drug will increase with an increase in the dose of more than 20 mg / day, at the same time, the risk of side effects increases.

The pharmacokinetic profile and data from clinical studies indicate that no dose adjustment of Lerkamen is required in elderly patients. However, caution should be exercised at the initial stage of treatment with Lerkamen® in this group of patients.

Caution should be exercised when using Lerkamen in patients with mild to moderate renal and hepatic insufficiency.

In case of renal insufficiency (creatinine clearance more than 30 ml / min) or mild or moderate hepatic insufficiency, the initial dose is 10 mg, then the dose is increased with caution to 20 mg / day.

The antihypertensive effect may be increased in patients with mild or moderate hepatic insufficiency and dose adjustment (reduction) may be required.

In patients with renal insufficiency (creatinine clearance less than 30 ml / min) and severe hepatic insufficiency, the use of Lerkamen® is contraindicated.

Overdose

Presumably, in the case of an overdose of lercanidipine, symptoms similar to those of an overdose of other dihydropyridine derivatives will be observed: peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia.

Treatment: symptomatic therapy; in the case of a marked decrease in blood pressure, loss of consciousness, cardiovascular therapy is indicated, with bradycardia – intravenous use of atropine.

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

In the case of taking 150 mg of lercanidipine + alcohol (unknown amount), drowsiness was observed.

Treatment: gastric lavage, taking activated charcoal.

When taking 280 mg of lercanidipine + 5.6 mg of moxonidine, the following symptoms were observed: cardiogenic shock, severe myocardial ischemia, mild renal failure.

Treatment: cardiac glycosides, diuretics (furosemide), high-dose catecholamines, plasma substitutes. In the case of taking 800 mg of lercanidipine, nausea and a marked decrease in blood pressure were observed.

Treatment: taking activated charcoal and laxatives, IV-dopamine.

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

Special instructions

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

Since dizziness, asthenia, fatigue and, in rare cases, drowsiness may occur during therapy with Lerkamen®, patients should drive vehicles with extreme caution and engage in other potentially dangerous activities that require a high rate of psychomotor reactions.

Form of production

Film-coated tablets.

Storage conditions

Keep out of 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