Lerkanorm tab n / 20mg film about 30 pc

Description

Composition
Active substance:
Lercanidipine hydrochloride – 20.0 mg;
film coating: [hypromellose – 3.0000 mg; giproloza (hydroxypropyl) – 1.1640 mg; talc – 1.1556 mg; titanium dioxide – 0.6522 mg; yellow iron oxide (iron oxide) – 0.0282 mg] or [dry film coating mixture comprising hypromellose (50%), giproloza (hydroxypropylcellulose) (19.4%), talc (19.26%), titanium dioxide ( 10.87%) and yellow iron oxide (ferric oxide) (0.47%)] – 6.0 mg.
Excipients:
Microcrystalline Cellulose – 74.0 mg; lactose monohydrate – 70.0 mg; sodium carboxymethyl starch (sodium starch glycolate, type A) – 20.0 mg; Povidone K-30 – 9.0 mg; poloxamer – 5.0 mg; Magnesium stearate – 2.0 mg ;.
Description:
Round biconvex tablets, film-coated yellow. On the cross-section of the core of a light yellow color.
Product form:
Tablets, film-coated, 10 mg and 20 mg. 10, 15 or 30 tablets in blisters of PVC film and aluminum foil.
At 30 or 60 tablets in a bank of high-density polyethylene. 3 or 6, the contour of cellular packages for 10 tablets, 2 or 4 blisters 15 tablets, 1 or 2 blisters of 30 tablets or one bank together with instructions for use in a stack of cardboard.
Contraindications
– Hypersensitivity to lercanidipine, other dihydropyridine derivatives or any component of the formulation; – untreated heart failure; – unstable angina; – obstruction of blood vessels originating from the left ventricle of the heart; – the period within 1 month after myocardial infarction; – severe hepatic impairment; – severe renal impairment (creatinine clearance less than 30 mL / min); – Pregnancy and lactation; – the use in women of childbearing age who are not using reliable contraception; – the age of 18 years (effectiveness and safety have been established); – lactose intolerance, lactase deficiency, a syndrome of glucose-galactose malabsorption; – simultaneous with inhibitors isoenzyme CYP3A4 (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin) (see “Interaction with other drugs.”); – simultaneous with cyclosporin (see “Interaction with other drugs.”); – simultaneous with grapefruit juice (see “Interaction with other drugs” section.).
Precautions – renal failure (creatinine clearance of more than 30 ml / min); – liver failure, mild to moderate; – elderly age; – sick sinus syndrome (without pacemaker); – coronary artery disease; – dysfunction of the left ventricle of the heart; – Chronic heart failure; – simultaneous application isoenzyme CYP3A4 substrates (terfenadine, asmetol, class III antiarrhythmic drugs, such as amiodarone, quinidine) (see “Interaction with other drugs.”); – simultaneous application isoenzyme CYP3A4 inducers, e.g., anticonvulsants (phenytoin, carbamazepine) and rifampicin (see “Interaction with other drugs.”); – simultaneous application of digoxin (see “Interaction with other drugs.”).
Dosage
20 mg
Indications
Essential hypertension I-II severity.
Interaction with other drugs
Lercanidipine may be applied simultaneously with beta-blockers, diuretics, angiotensin prevraschayushego enzyme.
When applied simultaneously with metoprolol bioavailability of lercanidipine reduced by 50%. This effect can also occur when an application with other beta-blockers, and may require correction of lercanidipine dosage to achieve a therapeutic effect in the given combination.
Lercanidipine is metabolized by the CYP3A4 isoenzyme, with the participation, therefore, inhibitors and inducers of CYP3A4 isoenzyme, while the application may affect the metabolism and elimination of lercanidipine. Concomitant use of lercanidipine with inhibitors of CYP3A4 isoenzyme (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) (see. The section “Contra ‘).
Concomitant use of cyclosporin and lercanidipine, since an increase in concentration of both substances in the blood plasma is observed (see. The section “Contra ‘).
Caution must be exercised while the use of lercanidipine with other substrates of CYP3A4 isoenzyme (terfenadine, asmetol, class III antiarrhythmics, e.g., amiodarone, quinidine).
With simultaneous use of lercanidipine 20 mg midazolam bioavailability of lercanidipine in elderly patients can be increased by approximately 40%.
Lercanidipine should be used with caution in conjunction with inducers of CYP3A4 isoenzyme, e.g., anticonvulsants (phenytoin, carbamazepine) and rifampicin as possible to reduce the antihypertensive effect of lercanidipine. Requires regular monitoring of blood pressure.
In patients receiving digoxin continuously, while the use of lercanidipine 20mg no pharmacokinetic interaction was noted. However, in healthy volunteers who took digoxin Cmax values ​​was an increase of digoxin in plasma on average by 33% after oral administration of 20 mg lercanidipine fasting, the AUC and digoxin renal clearance changed slightly. It is necessary to control the presence of signs of digoxin toxicity in patients receiving both digoxin and lercanidipine.
The simultaneous use of lercanidipine with cimetidine (800 mg) does not cause significant changes lercanidipine plasma concentrations. When high doses of cimetidine may increase the bioavailability of lercanidipine and its antihypertensive effects.
With simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg) AUC value for simvastatin increased by 56% and its active metabolite beta-hydroxy – 28%. When receiving the drugs at different times of the day (lercanidipine – morning, simvastatin – in the evening), you can avoid unwanted interaction.
With simultaneous use of 20 mg lercanidipine and warfarin in healthy volunteers changes in the pharmacokinetics of warfarin was not observed.
While the use of fluoxetine (an inhibitor of isozyme CYP2D6 and CYP3A4) elderly patients clinically significant changes in the pharmacokinetics of lercanidipine not revealed.
May increase antihypertensive effects while taking grapefruit juice and lercanidipine (see. Section “Contraindications”).
Ethanol can potentiate the antihypertensive effect of lercanidipine.
Overdose
symptoms
Presumably, in the case of an overdose of lercanidipine be observed symptoms similar to those of overdosing of other dihydropyridine derivatives (peripheral vasodilation with marked decrease in blood pressure and reflex tachycardia), and nausea.
Treatment
Symptomatic. In case of significant decrease in blood pressure, loss of consciousness, is a cardiovascular therapy bradycardia – intravenous atropine. Information about the effectiveness of hemodialysis absent. Given the high degree of association with plasma proteins, dialysis can be inefficient.
There is evidence of three cases of overdosage by lercanidipine in doses of 150 mg, 280 mg and 800 mg. In all cases of overdose, patients survived.
In the case of simultaneously receiving 150 mg lercanidipine ethanol (unknown number) somnolence observed. Treatment: gastric lavage, administration of activated charcoal.
In the case of simultaneously receiving 280 mg lercanidipine from 5.6 mg moxonidine were observed following symptoms: cardiogenic shock, severe myocardial ischemia, renal failure mild. Treatment: cardiac glycosides, diuretics (furosemide), high doses of catecholamine plasma expanders.
In case of receiving 800 mg lercanidipine observed: nausea, marked reduction in blood pressure. Treatment: Ingestion of activated charcoal and laxatives, IV – dopamine.
pharmachologic effect
Pharmacological group:
Blocker “slow” calcium channels.
Pharmacodynamics:
Lercanidipine is a selective blocker of the “slow” calcium channels, derivatives of 1,4-dihydropyridine inhibiting transmembrane calcium ion current into vascular smooth muscle cells. The mechanism of antihypertensive action due lercanidipine direct relaxant effect on vascular smooth muscle cells, resulting in decreased total peripheral vascular resistance. Despite the relatively short half-life (T1 / 2) from the plasma, has a long lercanidipine antihypertensive action due to the high membrane coefficient distribution. The therapeutic effect is achieved within 5-7 hours after ingestion of the drug, and its duration is stored for one day (24 hours). Due to their high selectivity for vascular smooth muscle cells, lercanidipine no negative inotropic effect.
Marked decrease in blood pressure (BP) with reflex tachycardia occurs rarely because of the gradual development of vasodilation when lercanidipine.
Lercanidipine is a racemic mixture of (+) R- and (-) S-enantiomers. The antihypertensive effect of lercanidipine, as well as other asymmetric 1,4-dihydropyridine derivatives, mainly determined by S-enantiomer.
Pharmacokinetics:
Suction
Lercanidipine is completely absorbed after ingestion. The maximum concentration (Cmax) in plasma reached after 1.5-3 hours and is 3.3 ± 2.09 ng / ml and 7.66 ± 5.90 ng / ml after taking 10 mg and 20 mg lercanidipine respectively. (+) R and (-) S-enantiomers of lercanidipine demonstrate similar pharmacokinetic profile: have the same time to reach maximum concentration equal T1 / 2. Cmax in plasma and area under the curve “concentration-time» (AUC) (-) S enantiomers of lercanidipine on average 1.2 times higher than the (+) R-enantiomer. Interconversion of the enantiomers in the experiments in vivo was not observed.
By “primary pass” through the liver, the absolute bioavailability of lercanidipine when administered after a meal is about 10%. The ingestion fasting bioavailability of 1/3 of the index of bioavailability after eating. When lercanidipine inwardly within 2 hours after eating a high-fat, its bioavailability is increased 4 times, lercanidipine therefore not to be taken after meals. Pharmacokinetics of lercanidipine in the therapeutic dose range is nonlinear. When lercanidipine at doses of 10 mg, 20 mg and 40 mg Cmax in plasma was determined in a ratio of 1: 3: 8, respectively, and AUC – in a ratio of 1: 4: 18, suggesting a progressive saturation with “primary pass” through the liver. Thus, bioavailability increases with the dose.
Distribution
The distribution of lercanidipine from plasma into tissues and organs is rapid. The degree of binding to plasma proteins exceeds 98%. Patients with impaired renal function and liver, severe because of lower concentration of proteins in blood plasma of lercanidipine free fraction can be increased.
Metabolism
Lercanidipine metabolized involving CYP3A4 isozyme to inactive metabolites.
breeding
Lercanidipine excretion occurs mainly by biotransformation. About 50% of the dose is excreted by the kidneys, about 50% through the intestine. Mean T1 / 2 value is 8-10 hours. Cumulation of lercanidipine with repeated ingestion is not observed.
Pharmacokinetics in special patient groups
Pharmacokinetics of lercanidipine in elderly patients, patients with renal failure (creatinine clearance (CC) of more than 30 ml / min) and patients with liver failure mild to moderate similar to the pharmacokinetics in healthy volunteers.
In patients with renal impairment (creatinine clearance less than 30 mL / min) and in patients on hemodialysis, the concentration in plasma of lercanidipine increases by about 70%.
In patients with liver failure secondary to severe systemic bioavailability of lercanidipine is probably increased because the lercanidipine is metabolized primarily in the liver.
Pregnancy and breast-feeding
In animal studies, lercanidipine not teratogenic, but teratogenic effects were observed when other dihydropyridine derivatives. Therefore, the use of the drug Lerkanorm during pregnancy and in women of childbearing age who are not using adequate contraception, contraindicated.
Due to the high lipophilicity of lercanidipine may assume its penetration into breast milk, so Lerkanorm application of the drug during breastfeeding contraindicated.
Conditions of supply of pharmacies
Prescription.
side effects
Classification of the incidence of side effects according to the recommendations of the World Health Organization (WHO): very common> 1/10; often by> 1/100 to 1/1000 to 1/10000 to
On the part of the central nervous system: rarely – headache, dizziness; rarely – drowsiness.
Cardio-vascular system: rarely – palpitations, tachycardia, “tides” of blood to the facial skin; rarely – angina, chest pain; very rarely – a faint, marked reduction in blood pressure, heart attack, in patients with angina may increase the frequency, duration and severity of attacks.
From the digestive system: rarely – nausea, dyspepsia, diarrhea, abdominal pain, vomiting.
For the skin: rare – skin rash.
On the part of the musculoskeletal system: rarely – myalgia.
From the urinary system: rarely – polyuria; very rare – pollakiuria (increased frequency of urination).
Allergic reactions: very rarely – hypersensitivity reactions.
Laboratory findings: very rarely – reversible increase in the activity of “liver” transaminases.
Other: rarely – peripheral edema; rarely – asthenia, fatigue; very rarely – gingival hyperplasia.
special instructions
Caution should be exercised when using the drug in patients with impaired renal function, coronary heart disease (the risk of increased frequency of angina attacks). With regard to chronic heart failure: need to be compensated before starting the drug.
Particular caution should be observed in the initial stages of treatment of patients with hepatic failure or moderate due to the potential gain of antihypertensive action.
Effects on ability to drive vehicles and mechanisms
During the period of treatment must be careful when driving and mechanisms and the performance of work requiring concentration and speed of psychomotor reactions, especially at the beginning of treatment and at higher doses of the drug (the risk of drowsiness, fatigue, headache and dizziness).
Storage conditions
Store in a dark place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Dosing and Administration
Inside.
Preparation Lerkanorm take 10 mg 1 time per day in the morning, at least 15 minutes before a meal, without chewing, with a sufficient amount of water.
Depending on the therapeutic effect, and individual patient tolerance of the drug, the dose may be increased to 20 mg. The therapeutic dose is selected gradually as the maximum antihypertensive effects develop approximately 2 weeks after initiation of dosing.
It is unlikely that efficacy will increase with the dose of 20 mg per day, at the same time increases the risk of side effects.
Use in elderly patients
In applying the drug Lerkanorm elderly patients correction dose is not required, however, when receiving the drug should be careful, especially at the initial stage of treatment.
The use in patients with impaired renal or hepatic function
In applying the drug Lerkanorm in patients with renal failure (creatinine clearance of more than 30 ml / min) or hepatic insufficiency mild or moderate caution. The initial dose is 10 mg per day. Increasing the dose to 20 mg per day should be done with caution. If the antihypertensive effect is too pronounced, should reduce the dose.
Pi renal failure (creatinine clearance less than 30 mL / min) or hepatic failure, severe drug use Lerkanorm contraindicated (see. The section “Contra ‘).
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist