Lerkanydypyn | Lercanidipine-SZ tablets coated. captivity. about. 10 mg 30 pcs.

Latin name

LERCANIDIPINE-SZ

Release form

Film-coated tablets from beige yellow to beige, round, biconvex. In a cross section, the core of the tablet is light yellow in color (dosage of 10 mg).

Pharmacological action of

Slow calcium channel blocker

Contraindications

- Hypersensitivity to lercanidipine, other derivatives of the dihydropyridine series or any component of the

preparation - untreated heart failure

- unstable stenocardia of the left ventricular spermaturia, severe myocardial infarction - severe renal failure (CC less than 30 ml / min)

- pregnancy and the period of breastfeeding

- use in women of childbearing age and not using reliable contraception

- up to age 18 years (effectiveness and safety have not been established)

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome

- simultaneous administration with inhibitors of the CYP3A4 isoenzyme (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin)

- simultaneous administration with cyclosporine

- simultaneous administration with grape juice.

Precautions:

- Renal failure (creatinine clearance greater than 30 ml / min)

- impaired liver function of mild to moderate severity

- advanced age

- sinus node weakness syndrome (without pacemaker)

- left ventricular heart disease and

heart disease - chronic heart failure

- simultaneous use with CYP3A4 isoenzyme substrates (terfenadine, asmetol, class III antiarrhythmic drugs, for example, amiodarone, quinidine)

- simultaneous use with inducers of the CYP3A4 isoenzyme, for example, anticonvulsants (phenytoin, carbamazepine) and rifampicin

- simultaneous use with beta-blockers, digoxin.

Use during pregnancy and lactation

Pregnancy

In animal studies, lercanidipine did not have teratogenic effects, but teratogenic effects were noted with other dihydropyridine derivatives. Therefore, the use of the drug Lercanidipine-SZ during pregnancy and in women of childbearing age who do not use reliable contraception is contraindicated.

Breastfeeding period

Due to the high lipophilicity of lercanidipine, it can be assumed that it passes into breast milk, therefore, the use of the drug Lercanidipine-SZ during breastfeeding is contraindicated.

Special instructions

Caution should be exercised when prescribing to patients with impaired renal function, coronary heart disease (there is a risk of frequent attacks of angina pectoris), in relation to chronic heart failure: must be compensated before using the drug.

With extreme caution, the drug should be used in patients with sinus node syndrome (without a pacemaker).

even though Since controlled hemodynamic studies did not reveal disturbances in the function of the left ventricle, treatment with calcium channel blockers of patients with signs of left ventricular dysfunction should be carried out with extreme caution. There is also an opinion that patients with coronary heart disease receiving short-acting dihydropyridines represent a high-risk group for diseases of the cardiovascular system.

Special care should be taken in the initial stages of treatment of patients with mild to moderate severity of liver failure.

Impact on the ability to drive transp. Wed and fur .:

During treatment, care should be taken when performing work requiring increased attention when driving vehicles, especially at the beginning of treatment and with an increase in the dose of the drug (risk of drowsiness, headache and dizziness).

Composition

1 film-coated tablet contains:

dosage 10 mg

active ingredient: lercanidipine hydrochloride - 10 mg

excipients (core): lactose monohydrate (milk sugar) - 31.5 mg cellulose 38 microcrystals mg sodium starch glycolate - 15, 5 mg hypromellose (hydroxypropyl methylcellulose) - 3.5 mg magnesium stearate - 1.0 mg

excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed - 1.2 mg titanium dioxide E 171 - 0.67998 mg talc - 0.444 mg macrogol (polyethylene glycol) 3350 - 0.606 mg dye iron oxide yellow E 172 - 0.06825 mg dye iron oxide red E 172 - 0.00096 mg dye iron oxide black E 172 - 0.00081 mg).

Dosage and Administration

Inside. The drug Lercanidipine-SZ is prescribed 10 mg once a day in the morning, at least 15 minutes before a meal, without chewing, drinking plenty of water.

Dose may be increased to 20 mg (if the expected effect is not achieved with 10 mg). The therapeutic dose is selected gradually, increasing the dose to 20 mg is carried out 2 weeks after the start of the drug.

It is unlikely that the effectiveness of the drug will increase with increasing doses of more than 20 mg per day, at the same time, the risk of side effects increases.

Use in elderly patients

Dose adjustment is not required, however, when taking the drug, constant monitoring of the patient's condition is necessary.

Use in patients with impaired renal or hepatic function

In the presence of mild or moderate renal or hepatic insufficiency, as a rule, dose adjustment is not required, the initial dose is 10 mg, a dose increase to 20 mg per day should be carried out with caution. If the antihypertensive effect is too pronounced, the dose should be reduced.

Side effects of

The following is a list of adverse reactions distributed by organ systems and frequency of occurrence (World Health Organization classification):

often - from more than 1/100 to less than 1/10,

infrequently - from more than 1/1000 to less than 1/100,

rarely - from more than 1/10000 to less than 1/1000,

very rarely - less than 1/10000, including individual messages.

Disorders of the nervous system

Infrequently: headache, dizziness

Rarely: drowsiness.

Cardiovascular disorders

Infrequently: palpitations, tachycardia, flushing of the skin

Rarely: angina pectoris

Very rarely: fainting, marked decrease in blood pressure, chest pain, myocardial infarction, in patients with angina pectoris , duration and severity of seizures.

Gastrointestinal disorders

Rarely: nausea, vomiting, diarrhea, abdominal pain, dyspepsia

Very rarely: increased activity of liver enzymes (reversible).

Disorders of the skin and subcutaneous tissue

Rarely: skin rash.

Disorders of the musculoskeletal and connective tissue

Rarely: myalgia.

Disorders of the kidneys and urinary tract

Rarely: pollakiuria (increased frequency of urination).

General disorders

Infrequently: peripheral edema

Rarely: asthenia, increased fatigue

Very rarely: gingival hyperplasia.

Immune system disorders:

Very rare: hypersensitivity reactions.

Drug interaction

The drug cannot be used simultaneously with CYP3A4 inhibitors (isoenzyme of cytochrome P450 of the liver), such as ketoconazole, itraconazole, erythromycin (increase the concentration of lercanidipine in the blood and lead to a potentiation of the antihypertensive effect). The simultaneous administration of lercanidipine with cyclosporine is contraindicated since this leads to an increase in the content of both substances in the blood plasma.

Lercanidipine should not be taken with grapefruit juice, as this leads to inhibition of the metabolism of lercanidipine and potentiation of the antihypertensive effect.

Caution should be exercised while taking with drugs such as terfenadine, astemizole, quinidine and class III antiarrhythmic drugs (eg, amiodarone).

Concomitant use with anticonvulsants (e.g. phenytoin, carbamazepine) and rifampicin can lead to a decrease in the concentration of lercanidipine in the blood plasma and, therefore, to reduce the antihypertensive effect of lercanidipine.

In patients continuously taking digoxin, pharmacokinetic interaction was not observed with the simultaneous use of lercanidipine at a dose of 20 mg. However, healthy volunteers who took

digoxin

showed an increase in Cmax of digoxin in plasma by an average of 33% after fasting 20 mg of lercanidipine by mouth on an empty stomach, while the AUC and renal digoxin clearance did not change significantly. It is necessary to control the presence of signs of digoxin intoxication in patients taking digoxin and lercanidipine at the same time.

With the simultaneous use of lercanidipine at a dose of 20 mg with midazolam, the bioavailability of lercanidipine in elderly patients may increase by approximately 40%.

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, therefore, it can also occur when used with other drugs in this group.

Cimetidine at a dose of 800 mg per day does not lead to significant changes in the concentration of lercanidipine in blood plasma, however, special care is required, since at higher doses of cimetidine the bioavailability of lercanidipine, and therefore its antihypertensive effect, may increase.

With the simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg), the AUC value for simvastatin increased by 56%, and for its active metabolite of beta-hydroxy acid - by 28%. When taking drugs at different times of the day (lercanidipine in the morning,

simvastatin

in the evening), unwanted interactions can be avoided.

With simultaneous use with fluoxetine (an inhibitor of the isoenzymes CYP2D6 and CYP3A4) in elderly patients, clinically significant changes in the pharmacokinetics of lercanidipine were not detected.

Taking lercanidipine concomitantly with warfarin does not affect the pharmacokinetics of the latter.

Lercanidipine can be used simultaneously with beta-blockers, diuretics, angiotensin-converting enzyme (ACE) inhibitors. Ethanol may enhance the antihypertensive effect of lercanidipine.

Overdose

Symptoms

Presumably, in the event of an overdose of lercanidipine, symptoms similar to those of overdosage of other dihydropyridine derivatives (peripheral vasodilation with marked decrease in BP and renal dysfunction) will be observed.

Treatment

Symptomatic. In the case of marked decrease in blood pressure, loss of consciousness is shown cardiovascular therapy, with bradycardia - intravenous injection of atropine. There is no information on the effectiveness of hemodialysis. Given the high degree of association with blood plasma proteins, dialysis may be ineffective.

There are three cases of overdose with lercanidipine 150 mg, 280 mg and 800 mg. In all cases of overdose, patients remained alive.

In the case of concomitant administration of 150 mg of lercanidipine with ethanol (unspecified amount), drowsiness was observed. Treatment: gastric lavage, intake of activated charcoal.

Following concomitant administration of 280 mg lercanidipine with 5.6 mg moxonidine, the following symptoms were observed: cardiogenic shock, severe myocardial ischemia, mild renal failure. Treatment: cardiac glycosides, diuretics (furosemide), high doses of catecholamines, plasma substitutes.

In the case of 800 mg of lercanidipine observed: nausea, marked decrease in blood pressure. Treatment: intake of activated charcoal and laxatives, intravenously - dopamine.

Storage Conditions

In a dark place at a temperature not exceeding 25 РC.

Keep out of the reach and sight of children.

Shelf life

3 years.

Do not use after the expiration date printed on the package.

Active ingredient

lercanidipine

drugstore terms

drugstore prescription

dosage form

tablets

Possible product names

Lercanidipine-SZ tablets are coated. captivity. about. 10 mg 30 pcs.