Lercanidipine tabs 10mg #30

Lercanidipine user manual

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Lercanidipine is an antihypertensive agent.

Release form and composition

Dosage form - film-coated tablets: round, biconvex, from beige-yellow to beige (dosage 10 mg) and pinkish-orange (dosage 20 mg); the cross section shows a light yellow core (10 or 30 pcs. in blister contour packs, in a cardboard box 3 or 6 packs of 10 tablets, or 1 or 2 packs of 30 tablets; 30 pcs. in polymer cans or vials , in a cardboard box 1 can or 1 bottle; each box also contains instructions for the use of Lercanidipine).
Composition of 1 tablet:
    active substance: lercanidipine hydrochloride - 10 or 20 mg;
    auxiliary components: magnesium stearate, hypromellose (hydroxypropyl methylcellulose), sodium starch glycolate, microcrystalline cellulose, lactose monohydrate (milk sugar);
    film shell: Opadray II, including polyvinyl alcohol (partially hydrolyzed), macrogol (polyethylene glycol) 3350, talc, titanium dioxide (E171), as well as dyes: dosage 10 mg - iron oxide red (E172), iron oxide yellow (E172) and iron oxide black (E172); dosage of 20 mg - iron oxide red (E172) and iron oxide yellow (E172).

Pharmacodynamics

The active ingredient of the drug is lercanidipine hydrochloride, a slow calcium channel blocker, a 1,4-dihydropyridine derivative, a racemic mixture of right- (R) and levorotatory (S) stereoisomers. Lercanidipine selectively blocks the flow of calcium ions into the cells of the vascular wall, into the heart cells and smooth muscle cells.
The hypotensive effect is due to the ability of lercanidipine to have a direct relaxing effect on vascular smooth muscle cells.
The drug is characterized by high selectivity for vascular smooth muscle cells, due to which it does not have a negative inotropic effect.
Lercanidipine is a metabolically neutral drug, therefore it has no significant effect on the level of lipoproteins and apolipoproteins in the blood serum, as well as on the lipid profile in patients with arterial hypertension.
The antihypertensive effect develops within 5-7 hours after taking the drug inside and lasts for 24 hours.

Pharmacokinetics

After oral administration, lercanidipine is completely absorbed from the gastrointestinal tract. The maximum plasma concentration (Cmax) is observed after 1.5-3 hours and is 3.3 ± 2.09 ng / ml after taking a dose of 10 mg, 7.66 ± 5.9 ng / ml - a dose of 20 mg.
The (+) R-enantiomer and (-) S-enantiomer of the drug have a similar pharmacokinetic profile: the same time to reach Cmax and an equivalent half-life (T½).
The AUC (area under the concentration-time curve) and Cmax of the (-) S-enantiomer of lercanidipine are approximately 1.2 times higher than the (+) R-enantiomer. In in vivo studies, interconversions of enantiomers were not observed.
The drug undergoes the effect of the first pass through the liver. Its absolute bioavailability when taken on an empty stomach is ~ 3%. In the case of taking the drug after a meal, this figure increases by about 3 times. If the drug is taken orally within 2 hours after a meal with a high fat content, its bioavailability increases by 4 times. For this reason, the tablets are not recommended for use after meals.
The pharmacokinetics of lercanidipine is non-linear. When using doses of 10, 20 and 40 mg, the Cmax ratio is 1: 3: 8, respectively, and the AUC ratio is 1: 4: 18, which suggests a progressive saturation during the first passage through the liver. Thus, bioavailability increases with increasing dose.
The drug quickly penetrates into tissues and organs. The connection with plasma proteins is more than 98%. In severe violations of liver and kidney function, due to a decrease in the content of proteins in the plasma, an increase in the free fraction of lercanidipine is possible.
It is metabolized with the participation of the CYP3A4 isoenzyme, as a result of which pharmacologically inactive metabolites are formed.
It is excreted by the kidneys and through the intestines in approximately equal amounts. T½ is on average 8-10 hours. With multiple doses in the body does not accumulate.
In the elderly, patients with moderate to moderate renal impairment [creatinine clearance (CC)> 30 ml / min] and patients with mild hepatic impairment, the pharmacokinetic parameters of lercanidipine are similar to those in healthy volunteers.
In patients with severe renal insufficiency (CC <30 ml / min) and patients on hemodialysis, the plasma concentration of the drug increases by about 70%.
In moderate and severe hepatic insufficiency, the systemic bioavailability of the drug is likely to increase, since lercanidipine is metabolized mainly in the liver.

Indications for use

Lercanidipine is intended for the treatment of grade I – II arterial hypertension.

Contraindications

Absolute:
    lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
    severe renal failure (CC less than 30 ml / min);
    severe liver failure;
    obstruction of the outflow tract of the left ventricle;
    unstable angina;
    untreated heart failure;
    myocardial infarction transferred less than a month ago;
    age under 18;
    period of pregnancy and lactation;
    childbearing age in women who do not use reliable methods of contraception;
    simultaneous use of inhibitors of the isoenzyme CYP3A4 (for example, erythromycin, ketoconazole, ritonavir, itraconazole, troleandomycin), cyclosporine, grapefruit juice;
    hypersensitivity to any component of the drug or other derivatives of the dihydropyridine series.
Relative (Lercanidipine tablets are used with caution, after a careful assessment of the benefits and risks):
    chronic heart failure;
    dysfunction of the left ventricle of the heart;
    coronary heart disease;
    sick sinus syndrome (without a pacemaker);
    dysfunction of the liver of mild to moderate severity;
    renal failure (CC more than 30 ml / min);
    elderly age;
    concomitant use of beta-blockers, digoxin, inducers of the CYP3A4 isoenzyme (for example, rifampicin or anticonvulsants such as phenytoin and carbamazepine), substrates of the CYP3A4 isoenzyme (for example, asmethol, terfenadine, class III antiarrhythmics such as quinidine and amiodarone).

Instructions for use: method and dosage

Lercanidipine tablets should be taken orally, once a day, in the morning, at least 15 minutes before breakfast, swallowing whole and drinking the required amount of water.
The starting dose is 10 mg. If the expected effect is not achieved, after 2 weeks the dose is increased to 20 mg. A further increase in dosage is impractical, since the likelihood of an increase in the effect is low, but the risk of side effects is high.
In patients with moderate and severe renal / hepatic insufficiency, an increase in the daily dose to 20 mg should be carried out with caution.

Side effects

Possible side effects (according to the frequency of development are distributed as follows: often - from> 1/100 to <1/10, infrequently - from> 1/1000 to <1/100, rarely - from> 1/10 000 to <1/1000 , very rarely - <1/10 000, including individual messages):
    from the immune system: very rarely - hypersensitivity reactions;
    on the part of the cardiovascular system: infrequently - rush of blood to the skin of the face, tachycardia, palpitations; rarely - angina pectoris; very rarely - chest pain, marked decrease in blood pressure (BP), fainting, myocardial infarction; in patients with angina pectoris, an increase in the frequency, severity and duration of attacks;
    from the musculoskeletal system: rarely - myalgia;
    from the digestive system: rarely - abdominal pain, diarrhea, nausea, vomiting, dyspepsia; very rarely - a reversible increase in the activity of liver enzymes;
    from the kidneys and urinary tract: rarely - pollakiuria (increased frequency of urination);
    from the nervous system: infrequently - headache, vertigo; rarely - drowsiness;
    on the part of the skin and subcutaneous tissues: rarely - skin rashes;
    others: infrequently - peripheral edema; rarely - increased fatigue, general weakness; very rarely - gingival hyperplasia.

Overdose

Symptoms: nausea, peripheral vasodilation with a marked decrease in blood pressure and reflex tachycardia. Three cases of overdose have been reported after taking the drug at a dose of 150, 280 and 800 mg. All patients survived.
Overdose treatment is symptomatic. With a pronounced decrease in blood pressure and fainting, cardiovascular therapy is performed, with bradycardia, atropine is administered intravenously. The effectiveness of hemodialysis has not been established, however, due to the high degree of binding of lercanidipine to plasma proteins, dialysis is probably ineffective. In case of taking too high a dose of Lercanidipine (800 mg), it is recommended to take activated charcoal and laxatives, intravenous dopamine.
There is evidence of taking 150 mg of lercanidipine simultaneously with ethanol (the amount is unknown). The patient was drowsy. In such cases, gastric lavage and intake of activated charcoal are necessary.
With the combined use of 280 mg of lercanidipine with moxonidine at a dose of 5.6 mg, mild renal failure, severe myocardial ischemia, and cardiogenic shock occurred. In this case, high doses of catecholamines, furosemide (diuretic), cardiac glycosides, plasma substitutes are indicated.

Special instructions

Patients with coronary heart disease are at risk of increased angina attacks, therefore, drug treatment should be carried out with caution.
In chronic heart failure, it is possible to start taking Lercanidipine only after compensating for the disease.

Influence on the ability to drive vehicles and complex mechanisms

When using the drug (especially at the initial stage of treatment and during the period of increasing the dose), caution should be exercised by vehicle drivers and persons employed in potentially hazardous industries that require concentration of attention, speed of reactions and accuracy of movements.

Application during pregnancy and lactation

In animal studies, no teratogenic effect of lercanidipine was found, however, teratogenic effects were noted with the use of other dihydropyridine derivatives. For this reason, the drug is contraindicated in pregnant and breastfeeding patients, as well as in women of reproductive age who do not use reliable methods of contraception.
Due to the high lipophilicity of the drug, it is assumed that lercanidipine can penetrate into breast milk, therefore, its use is contraindicated during lactation.

Childhood use

The efficacy and safety of the drug for pediatric patients has not been established, therefore the drug is contraindicated in children and adolescents under 18 years of age.

With impaired renal function

In severe renal failure (CC <30 ml / min), Lercanidipine is prohibited for use.
In mild and moderate disorders (CC> 30 ml / min), correction of the dosage regimen is usually not required, but treatment should be carried out under close medical supervision.

For violations of liver function

In severe hepatic impairment, the drug is prohibited for use.
In mild to moderate disorders, dosage adjustment is usually not required, but therapy should be carried out with caution.

Use in the elderly

There is no need to adjust the dosage regimen of the drug for elderly patients, however, constant monitoring of their condition is required.

Drug interactions

Lercanidipine has no effect on the pharmacokinetics of warfarin.
Elderly patients treated with fluoxetine (an inhibitor of CYP2D6 and CYP3A4 isoenzymes) did not show significant changes in the pharmacokinetics of lercanidipine.
If necessary, the drug can be used simultaneously with ACE inhibitors (angiotensin-converting enzyme), beta-blockers, diuretics.
Contraindicated combinations:
    inhibitors of the isoenzyme CYP3A4 of cytochrome P450 (for example, erythromycin, ketoconazole, itraconazole): the plasma concentration of lercanidipine increases and, as a result, the hypotensive effect increases;
    cyclosporine: there is a mutual increase in plasma concentrations of drugs;
    grapefruit juice: the metabolism of lercanidipine is inhibited, as a result of which the antihypertensive effect is enhanced.
Drug interactions to take into account:
    midazolam: in the elderly, the bioavailability of lercanidipine increases by about 40%;
    ethanol: the hypotensive effect of lercanidipine is enhanced;
    rifampicin, anticonvulsants (for example, carbamazepine, phenytoin): a decrease in the plasma concentration of lercanidipine and, as a result, its effect is possible;
    simvastatin: its AUC increases by 56%, the AUC of its active metabolite beta-hydroxy acid - by 28% (this effect can be avoided by taking drugs at different times of the day);
    cimetidine (in high doses): it is possible to increase the bioavailability of lercanidipine and, as a result, its hypotensive action;
    metoprolol: the bioavailability of the drug is significantly reduced (by about 50%);
    digoxin: it is possible to increase its plasma concentration by approximately 33% (it is necessary to monitor the patient's condition for the development of signs of intoxication).
With caution, lercanidipine should be used in combination with class III antiarrhythmic drugs (for example, amiodarone), as well as with quinidine, astemizole, terfenadine.

Terms and conditions of storage

Store at a temperature not exceeding 25 ° C out of the reach of children, protected from light.
Shelf life is 3 years.

Reviews

According to reviews, Lercanidipine is an effective antihypertensive drug that reduces high blood pressure well, does not cause side effects even with prolonged use, and is affordable.

Terms of sell

You can buy Lercanidipine without a doctor's prescription.