Composition, form of production and packaging
The tablets covered with a film cover of light yellow color, round, biconcave, with risk on one side; on the bend - light yellow color.
1 tab.
lercanidipine hydrochloride 10 mg
Excipients: lactose monohydrate - 30 mg, microcrystalline cellulose - 39 mg, sodium carboxymethyl starch - 15.5 mg, povidone K30 - 4.5 mg, magnesium stearate - 1 mg.
Composition of the shell: opedraj yellow (OY-SR-6497) - 3 mg (hypromellose, talc, titanium dioxide (E171), macrogol 6000, ferric oxide yellow oxide (E172)).
7 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
14 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
15 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
25 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
28 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
30 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
The tablets covered with a film cover from pink to dark pink color, round, biconcave, with a risk on one side; on the bend - light yellow color.
1 tab.
lercanidipine hydrochloride 20 mg
Excipients: lactose monohydrate - 60 mg, microcrystalline cellulose - 78 mg, sodium carboxymethyl starch - 31 mg, povidone K30 - 9 mg, magnesium stearate - 2 mg.
Composition of the shell: opadrai pink (02F25077) - 6 mg (hypromellose, talc, titanium dioxide (E171), macrogol 6000, iron oxide red oxide (E172)).
7 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
14 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
15 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
25 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
28 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
30 pcs. - Blisters (1, 2, 3, 4, 5, 6, 7) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
The blocker of "slow" calcium channels. Lercanidipine is a racemic mixture of right (R) and levorotatory (S) stereoisomers, a 1,4-dihydropyridine derivative, capable of selectively blocking the flow of calcium ions into vascular wall cells, cardiac cells and smooth muscle cells.
The mechanism of antihypertensive action is caused by a direct relaxing action on the smooth muscle cells of the vessels. Has a prolonged antihypertensive effect. The therapeutic effect is achieved 5-7 hours after ingestion and the duration is maintained for 24 hours. Due to the high selectivity to the smooth muscle cells of the vessels, a negative inotropic effect is absent.
Zanidip В® -Recordati is a metabolically neutral preparation and does not significantly affect the content of lipoproteins and apolipoproteins in the blood serum, nor does it alter the lipid profile in patients with arterial hypertension.
PHARMACOKINETICS
Suction
After ingestion, lercanidipine is absorbed from the digestive tract almost completely. C max in blood plasma is achieved through 1.5-3 hours and is 3.3 ng / ml and 7.66 ng / ml after taking 10 mg and 20 mg respectively.
Distribution
Distribution from plasma of blood into tissues and organs occurs quickly. Binding to plasma proteins exceeds 98%.
When repeated use does not cumulate.
Metabolism
Metabolized by "primary passage" through the liver by biotransformation of CYP3A4 with the formation of a number of metabolites that do not have pharmacological activity.
Excretion
It is excreted by the kidneys and intestines after biotransformation. There are 2 phases of lercanidipine excretion: early (T 1/2 - 2-5 h) and final (T 1/2 - 8-10 h). The drug remains unchanged in 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
- Essential hypertension of mild to moderate severity.
DOSING MODE
The drug is prescribed for 10 mg 1 time / day (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, the dose is increased 2 weeks after the start of the drug.
Tablets are taken orally, without chewing, with enough water.
In elderly patients, dose adjustment is not required, however, when taking the drug, constant monitoring of the patients' condition is necessary.
In the presence of renal or hepatic insufficiency of mild or moderate severity , as a rule, dose correction is not required; the initial dose is 10 mg, then you should carefully increase the dose to 20 mg / day. If the antihypertensive effect is too severe, the dose should be lowered.
SIDE EFFECT
The incidence of adverse events was classified as follows: very often (1/10), often (1/100), infrequently (1/1000), rarely (1/10 000), very rarely (<1/10 000).
From the nervous system: rarely - drowsiness; infrequently - headache, dizziness.
From the immune system: very rarely - hypersensitivity.
From the side of the cardiovascular system: infrequently - tachycardia, a feeling of palpitations, flushes of blood to the skin of the face; rarely - angina pectoris; very rarely - a syncope, a marked decrease in blood pressure, chest pain, myocardial infarction.
From the digestive system: rarely - nausea, vomiting, diarrhea, abdominal pain, indigestion; very rarely - a reversible increase in the activity of liver enzymes.
From the skin: rarely - skin rash.
From the musculoskeletal system: rarely - myalgia.
From the urinary system: rarely - polyuria.
Other: infrequent peripheral edema; rarely - asthenia, increased fatigue; very rarely - gingival hyperplasia.
CONTRAINDICATIONS
- chronic heart failure in the stage of decompensation;
- unstable angina;
- Obstruction of vessels emanating from the left ventricle of the heart;
- recently transferred myocardial infarction (within 1 month);
severe hepatic impairment;
- impaired renal function (glomerular filtration rate less than 39 ml / min);
- simultaneous use with potent inhibitors of the isoenzyme CYP3A4 (ketoconazole, itraconazole, erythromycin), as well as with grapefruit juice, cyclosporine;
- lactase deficiency, lactose intolerance, glucose / galactose malabsorption syndrome;
- children and adolescents under 18 years of age (efficacy and safety not established);
- Pregnancy;
- lactation period;
- women of childbearing age who do not use reliable means of contraception;
- hypersensitivity to lercanidipine, other dihydropyridine derivatives or any component of the drug.
With caution: violations of liver function of mild and moderate severity; syndrome of weakness of the sinus node (without a pacemaker); left ventricular failure and coronary heart disease; chronic heart failure; simultaneous reception of beta-adrenoblockers, digoxin.
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe violations of kidney function (glomerular filtration rate less than 39 ml / min).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
With caution: violations of liver function of mild and moderate severity.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
APPLICATION IN ELDERLY PATIENTS
In elderly patients, dose adjustment is not required, however, when taking the drug, constant monitoring of the patients' condition is necessary.
SPECIAL INSTRUCTIONS
Caution should be exercised in appointing patients with impaired renal function, IHD (there is a risk of increased episodes of angina pectoris).
Before starting the use of the drug, chronic heart failure must be compensated.
Particular care should be taken in the initial stages of treatment of patients with mild to moderate degree of liver function deficiency.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when performing work requiring increased attention when driving vehicles, especially at the beginning of treatment and with increasing doses of the drug (risk of drowsiness, headache and dizziness).
OVERDOSE
Symptoms: peripheral vasodilation with marked decrease in blood pressure and reflex tachycardia, an increase in the frequency and duration of angina attacks, myocardial infarction.
Treatment: conduct symptomatic therapy.
DRUG INTERACTION
The drug should not be taken concomitantly with CYP3A4 inhibitors (the isoenzyme of cytochrome P450 of the liver), such as ketoconazole, itraconazole, erythromycin (increase the concentration of lercanidipine in the blood and lead to potentiation of the antihypertensive effect).
Contraindicated simultaneous reception of lercanidipine with cyclosporine, tk. 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 lercanidipine metabolism and potentiation of the antihypertensive effect.
Caution should be exercised when taking concomitant medication with such drugs as terfenadine, astemizole, quinidine and antiarrhythmic drugs of class III (eg, amiodarone).
Simultaneous reception with anticonvulsants (eg, phenytoin, carbamazepine) and rifamycin may lead to a decrease in the level of lercanidipine in the blood plasma and, in this connection, to reduce the antihypertensive effect of lercanidipine.
With the simultaneous administration of digoxin, regular monitoring should be carried out for signs of intoxication with digoxin.
Admission of 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%, 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 appear when used with other drugs in this group.
Cimetidine at a dose of 800 mg / day does not lead to significant changes in the concentration of lercanidipine in the blood plasma, however, special caution is required since at higher doses of cimetidine, the bioavailability of lercanidipine, and hence its antihypertensive effect, may increase.
With simultaneous application 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 simultaneously with warfarin does not affect the pharmacokinetics of the latter.
Lercanidipine can be used simultaneously with beta-blockers, diuretics, ACE inhibitors.
Ethanol can enhance the antihypertensive effect of drugadipin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 3 years.
