Lernikor tab n / 20mg film about 28 pc

$8.93

Lernikor tab n / 20mg film about 28 pc

5 in stock

Quantity:

Description

Composition
Active substance:
1 tablet contains: lercanidipine hydrochloride 10 mg / 20 mg ;.
Excipients:
Cellulose microcrystalline 39 mg / 78 mg lactose monohydrate to 30 mg / 60 mg sodium carboxymethyl starch (sodium starch glycolate) 15.5 mg / 31 mg, Povidone K30 4.5 mg / 9 mg magnesium stearate 1 mg / 2 mg; Excipients for the shell: for 10 mg dosage: Opadry II 85F38107 Yellow [Polyvinyl alcohol 1.2 mg, 0.6684 mg of titanium dioxide, macrogol (polyethylene glycol) 0.606 mg Talc 0.444 mg Aluminum Lake Dye 0.0807 mg quinoline yellow, red iron oxide 0.0009 mg]; Dosing 20 mg: Opadry II 85F34555 Pink [Polyvinyl alcohol 2.4 mg, 1.4046 mg of titanium dioxide, macrogol (polyethylene glycol) 1.212 mg, 0.888 mg of talc, aluminum varnish based red dye charming 0.0348 mg Aluminum Lake Dye sunset yellow 0.0336 mg aluminum Lake dye azorubin 0.027 mg].
Description:
Dosage 10 mg: Round biconvex tablets, film-coated yellow.
Dosage 20 mg: Round biconvex tablets, film-coated pink.
On the cross-section of the core of a light yellow color.
Product form:
Tablets, film-coated, 10 mg or 20 mg.
At 7, 10, 14, 28 tablets in blisters of PVC film and aluminum foil printed patent.
1, 2, 3, 4 blisters together with instructions for use placed in a pile of cardboard.
Contraindications
Hypersensitivity to lercanidipine, other dihydropyridine derivatives or any component of the formulation.
Untreated chronic heart failure.
Unstable angina.
Obstruction of the outflow tract of the left ventricle.
Period within 1 month after myocardial infarction.
Severe hepatic insufficiency.
Severe renal impairment (creatinine clearance less than 30 mL / min).
Concomitant use with potent inhibitors of CYP3A4 (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin).
The simultaneous use of cyclosporin.
Simultaneous treatment with grapefruit juice.
Lactose intolerance, lactase deficiency, a syndrome of glucose-galactose malabsorption.
Pregnancy and breast-feeding.
Use in women of childbearing age who are not using reliable methods of contraception.
Age 18 years (effectiveness and safety have been studied).
Carefully
Renal failure (creatinine clearance of more than 30 ml / min) and / or liver failure mild to moderate severity, elderly, sick sinus syndrome (without a pacemaker), ischemic heart disease, left ventricular dysfunction.
Dosage
20 mg
Indications
Hypertension of 1-2 degrees.
Interaction with other drugs
Lercanidipine may be applied simultaneously with beta-blockers, diuretics, angiotensin converting enzyme (ACE) inhibitors.
When applied simultaneously with metoprolol, lercanidipine bioavailability is reduced by 50%. This effect can occur, and while the use of other beta-blockers. and may require correction of lercanidipine dosage to achieve a therapeutic effect in the given combination. Lercanidipine is metabolized with the participation of CYP3A4 isoenzyme, therefore, inhibitors and inducers of this isoenzyme, while the application can affect the metabolism and elimination of lercanidipine. Not recommended simultaneous application lercanidipine potent inhibitors of CYP3A4 (ketoconazole. Itraconazole, ritonavir, erythromycin, troleandomycin).
Not recommended simultaneous application of cyclosporine and lercanidipine, since an increase in concentration of both substances in the blood plasma is observed.
Caution should be exercised while the use of lercanidipine with other substrates of CYP3A4 (terfenadine, astemizole, class III antiarrhythmics, e.g., amiodarone, kvinidin).
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 together with inducers of CYP3A4, such as anticonvulsants (phenytoin, carbamazepine) and rifampicin as possible to reduce the antihypertensive effect. A regular control of blood pressure.
With simultaneous use of lercanidipine 20 mg in patients continuously receiving beta-methyldigoxin, there was no pharmacokinetic interaction, while in healthy volunteers treated with digoxin, showed an increase in Cmax values ​​for digoxin in average by 33% after receiving 20 mg lercanidipine fasting, the AUC (area under curve – “concentration-time”) and 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. At high doses of cimetidine may increase the bioavailability of lercanidipine and antihypertensive action.
With simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg), AUC value for simvastatin increased by 56%, while the same value for 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.
The simultaneous use of fluoxetine (an inhibitor of CYP2D6 and CYP3A4) in elderly patients had no clinically significant changes in the pharmacokinetics of lercanidipine.
May increase antihypertensive effects while taking grapefruit juice and lercanidipine.
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.
Treatment:
Treatment is symptomatic. In case of significant decrease in blood pressure, loss of consciousness is a cardiovascular therapy bradycardia – intravenous atropine.
There is evidence of 3 cases of overdose when lercanidipine in doses of 150 mg, 280 mg and 800 mg for the purpose of suicide.
In case of receiving 150 mg lercanidipine + alcohol (unknown number) somnolence observed. Treatment: gastric lavage, administration of activated charcoal.
In case of receiving 280 mg lercanidipine + 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 and nausea were observed marked reduction in blood pressure. Treatment: administration of activated charcoal and a laxative, intravenously – dopamine.
In all cases of overdose, all patients were alive. Information on the efficiency of dialysis for lercanidipine absent. Most likely, because of high communication lercanidipine plasma proteins, dialysis can be inefficient.
pharmachologic effect
Pharmacological group:
Blocker “slow” calcium channels.
Pharmacodynamics:
Lercanidipine is a selective blocker of the “slow” calcium channels, a derivative of 1,4-dihydropyridine inhibiting transmembrane calcium ion current into vascular smooth muscle cells.
Lercanidipine is a racemic mixture of (+) – R- and (-) S- enantiomers. The antihypertensive effect of lercanidipine primarily driven S-enantiomer. The mechanism of antihypertensive action due lercanidipine relaksiruyugtsim direct action on vascular smooth muscle cells, thereby reducing the total peripheral resistance. Despite the relatively short elimination half-life from the blood plasma, lercanidipine has prolonged antihypertensive effect due to the high membrane coefficient distribution. Due to its high vascular selectivity has no negative inotropic effects. Acute hypotension with reflex tachycardia is rare due to the gradual development of vasodilation when lercanidipine.
Lercanidipine is metabolically neutral and has no significant impact on the content of lipoproteins and apolipoproteins in the blood serum, and does not alter the lipid profile in hypertensive patients.
Pharmacokinetics:
Suction
Lercanidipine is completely absorbed after ingestion. The maximum plasma concentration (Cmax) is reached after 1.5-3 hours and is 3.3 ± 2.09 ng / ml and 7.66 ± 5.90 ng / ml after receiving the 10 and 20 mg lercanidipine, respectively. (+) – R- and (-) Z-enantiomers of lercanidipine demonstrate similar pharmacokinetic profile: have the same time to reach maximum concentration (Tstah), the same half-life (T1 / 2); value Cmax and the area under “concentration-time” curve (AUC) in 1.2-fold higher for (-) 8-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%, when receiving the value of fasting bioavailability is reduced by 1/3. When lercanidipine not later than 2 hours after a fatty meal bioavailability is increased 4 times, lercanidipine therefore not to be taken after meals. Upon oral administration of lercanidipine its plasma concentration is not directly proportional to the dose received (non-linear kinetics). Saturation of first-pass metabolism, occurs gradually. Thus, bioavailability increases with increasing dose.
Distribution
Distribution from plasma into tissues and organs is rapid and extensive. Communication with plasma proteins exceeds 98%.
Metabolism and excretion
Lercanidipine metabolized involving CYP3A4 isozyme to inactive metabolites.
About 50% of the dose is excreted by the kidneys (bowel displayed about 50%). Elimination occurs mainly through biotransformation. The average value of T | / 2 is 8-10 hours duration therapeutic effect -. 24 hours.
Cumulation of lercanidipine with repeated ingestion is not observed. Pharmacokinetics in special clinical situations
It has been shown that the pharmacokinetics of lercanidipine in elderly patients, patients with renal failure (creatinine clearance (CC) of more than 30 ml / min) and in patients with hepatic insufficiency mild to moderate severity with pharmacokinetics similar to that observed in the general population of patients.
In patients with severe renal and / or hepatic insufficiency, due to lower protein concentration in plasma free fraction of lercanidipine may be increased.
In patients with renal impairment (creatinine clearance less than 30 mL / min) and in patients on hemodialysis, lercanidipine plasma concentrations were higher (approximately 70%).
In patients with liver failure secondary to severe systemic bioavailability of lercanidipine is probably increased because lercanidipine is metabolized primarily in the liver.
Pregnancy and breast-feeding
The use of lercanidipine in pregnancy and lactation and in women of childbearing age in the absence of reliable contraception is contraindicated.
Preclinical studies revealed no teratogenic effect of lercanidipine in rats and rabbits, reproductive function of rats was unchanged.
Since there is no clinical experience with lercanidipine in pregnancy and lactation and it is known that other derivatives of dihydropyridine is teratogenic in animals, lercanidipine is not recommended during pregnancy and in women of childbearing age who are not using reliable methods of contraception. Due to the high lipophilicity of lercanidipine may assume its penetration into breast milk, however, lercanidipine is not recommended during breastfeeding.
Conditions of supply of pharmacies
Prescription.
side effects
Possible adverse reactions are listed below in descending frequency of occurrence: often (
special instructions
Particular caution should be exercised when administering lercanidipine patients with sick sinus syndrome (without a pacemaker). Despite the fact that the study hemodynamic control revealed no deterioration of the ventricular function when lercanidipine, caution should be exercised in the appointment of lercanidipine in patients with left ventricular dysfunction. It has been suggested that the intake of some dihydropyridines may be associated with the risk of increased frequency of angina attacks in patients with coronary heart disease. Therefore, in these patients lercanidipine should be carried out with extreme caution.
Effects on ability to drive and use machines Since the therapy drug may cause dizziness, asthenia, fatigue and in rare cases, sleepiness during treatment, patients should be with extreme caution to drive vehicles and to engage in other potentially hazardous activities that require high speed psychomotor reactions.
Storage conditions
At a temperature of not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Inside, at least 15 minutes before a meal, preferably in the morning, without chewing, with a sufficient amount of water.
The recommended dose – 10 mg 1 time per day. Depending on individual patient tolerance of the drug, the dose may be increased to 20 mg. If necessary, a daily dose of increasing to 20 mg performed 2 weeks after the start of treatment.
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 increasing doses of over 20 mg per day, at the same time increases the risk of side effects. Use in elderly patients
The pharmacokinetic profile and data from clinical studies suggest that elderly patients lercanidipine dosage adjustment is not required. However, caution should be exercised at the initial stage of treatment in this group of patients. The use in patients with impaired renal or hepatic function
In the presence of renal failure (creatinine clearance of more than 30 ml / min) or hepatic insufficiency mild or moderate severity, the initial dose is 10 mg, and then with caution increasing the dose to 20 mg per day. The antihypertensive effect can be enhanced in patients with hepatic insufficiency mild or moderate severity and may require adjustment (reduction) dose.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

Obolensky

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