Lerkamen 20 coated pills 20mg N28
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Active ingredients
Lercanidipine
Release form
Pills
Composition
1 tab.: Lercanidipine hydrochloride 20 mg. Adjuvants: lactose monohydrate - 30 mg, microcrystalline cellulose - 39 mg, sodium carboxymethyl starch (type A) - 15.5 mg, povidone K30 - 4.5 mg, magnesium stearate - 1 mg. Coat composition: sedate OY-SR-6497 - 3 mg (hypromellose - 1.913 mg, macrogol 6000 - 0.3 mg, talc - 0.15 mg, titanium dioxide - 0.6 mg, iron yellow dye - 0.037 mg).
Pharmacological effect
Selective blocker of slow calcium channels with a predominant effect on the vessels, a derivative of dihydropyridine. Inhibits transmembrane current of calcium ions in vascular smooth muscle cells. The mechanism of the antihypertensive effect of lercanidipine is due to a direct relaxing effect on vascular smooth muscle cells, resulting in a reduced OSS. Despite the relatively short half-life from plasma, lercanidipine has a prolonged antihypertensive effect due to the high coefficient of membrane distribution. Due to the high vascular selectivity does not have a negative inotropic effect. Acute hypotension with reflex tachycardia is rarely due to the gradual development of vasodilation while taking lercanidipine. Lercanidipine is a racemic mixture of (+) R- and (-) S-enantiomers. The antihypertensive effect of lercanidipine is primarily due to the S-enantiomer. The therapeutic effect is 24 hours.
Pharmacokinetics
Lercanidipine absorption is completely absorbed after oral administration. Plasma Cmax is reached in 1.5-3 hours and amounts to 3.3 ± 2.09 ng / ml and 7.66 ± 5.90 ng / ml after taking 10 and 20 mg of lercanidipine, respectively. (+) R- and (-) S-enantiomers of lercanidipine demonstrate similar pharmacokinetic profile: have the same time to achieve Cmax, the same T1 / 2; Cmax and AUC values are 1.2 times higher for the (-) S-enantiomer. Interconversions of enantiomers in in vivo experiments were not observed. Due to the effect of the first passage through the liver, the absolute bioavailability of lercanidipine when taken orally after a meal is approximately 10%, when taken on an empty stomach, the value of bioavailability decreases by 1/3. When taking lercanidipine no later than 2 hours after ingestion of fatty foods, its bioavailability increases 4 times, so Lerkamen should not be taken after meals.With oral administration of lercanidipine, its concentration in the blood plasma is not directly proportional to the dose taken (nonlinear kinetics). Saturation of the systemic metabolism occurs gradually. Thus, bioavailability increases with increasing doses. Distribution Distribution from blood plasma to tissues and organs occurs rapidly and extensively. Plasma protein binding exceeds 98%. Metabolism and elimination of Lercanidipine is metabolized with the participation of CYP3A4 isoenzyme with the formation of inactive metabolites. About 50% of the dose taken is excreted by the kidneys (about 50% is excreted by the intestine). Elimination occurs mainly by biotransformation. The average T1 / 2 is 8–10 hours. There is no observed accumulation of lercanidipine on repeated ingestion. Pharmacokinetics in special clinical situations It has been shown that the pharmacokinetics of lercanidipine in elderly patients, patients with renal insufficiency (CC more than 30 ml / min) and mild and moderate hepatic insufficiency is similar to the pharmacokinetics observed in the general population of patients. In patients with renal insufficiency (CC less than 30 ml / min) and in patients on hemodialysis, the concentrates and lercanidipine plasma levels were higher (approximately 70%). In patients with severe renal and / or liver failure, due to a decrease in plasma protein concentration, the free fraction of lercanidipine may increase. In patients with moderate and severe hepatic insufficiency, systemic The bioavailability of lercanidipine is likely to increase as lercanidipine is metabolized mainly in the liver.
Indications
- Essential hypertension I-II severity
Contraindications
- Untreated heart failure; - Unstable angina; - Obstruction of vessels emanating from the left ventricle of the heart; - Period for 1 month after suffering a myocardial infarction; - Severe hepatic failure; - Severe renal failure (CC less than 30 ml / min); - simultaneous use with CYP3A4 inhibitors (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin); - simultaneous use with cyclosporine; - simultaneous use with grapefruit juice; - lactose intolerance, lactase deficiency,glucose-galactose malabsorption syndrome - pregnancy; - lactation period (breastfeeding); - use in women of childbearing age not using reliable methods of contraception; - children and adolescents under 18 years of age (efficacy and safety have not been studied); components of the drug; - hypersensitivity to other derivatives of the dihydropyridine series. It should be used with caution in renal (CC more than 30 ml / min) and / or mild and moderate hepatic insufficiency, elderly patients, with SSSU (without pacemaker), ischemic heart disease, left ventricular dysfunction.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
The use of Lerkamen during pregnancy and during breastfeeding, as well as in women of childbearing age in the absence of reliable contraception is contraindicated. During preclinical studies, no teratogenic effect of lercanidipine in rats and rabbits was detected, the reproductive function of rats was unchanged. Due to the lack of clinical experience lercanidipine during pregnancy and during breastfeeding, and since it is known that other dihydropyridine derivatives had a teratogenic effect on the stomach lercanidipine is not recommended for use in pregnancy and in women of childbearing age who do not use reliable contraceptive methods. Due to the high lipophilicity of lercanidipine, its penetration into breast milk can be assumed; therefore, the drug is not recommended for use during breastfeeding.
Dosage and administration
The drug is taken orally, at least 15 minutes before a meal, preferably in the morning, without chewing, drinking plenty of water. Assign 10 mg 1 time / day. Depending on the individual tolerance of the drug by the patient, the dose may be increased to 20 mg. The therapeutic dose is selected gradually, since maximum antihypertensive effect develops approximately 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 / day, at the same time increasing the risk of side effects. The pharmacokinetic profile and data from clinical studies show that elderly patients do not require dose adjustment of Lerkamen.However, caution should be exercised at the initial stage of treatment with Lerkamen in this group of patients. When using Lerkamen in patients with mild to moderate renal and hepatic insufficiency, caution should be exercised. When renal insufficiency (CC more than 30 ml / min) or mild hepatic insufficiency or moderate severity, the initial dose is 10 mg, then carefully increase the dose to 20 mg / day. The antihypertensive effect may be enhanced in patients with mild to moderate hepatic insufficiency and dose adjustment may be required (reduced). In case of renal insufficiency (CC less than 30 ml / min) and severe hepatic insufficiency, the use of Lerkamen is contraindicated.
Side effects
Possible side effects are listed below in descending frequency of occurrence: often (less than 1/10, ≥1/100), infrequently (less than 1/100, ≥1 / 1000), rarely (less than 1/100, ≥1 / 10000), very rarely (less than 1 / 10,000), including separate messages. For the nervous system: infrequently - headache, dizziness; rarely - drowsiness. From the side of the cardiovascular system: infrequently - feeling of heartbeat, tachycardia, flushing of blood to the skin of the face; rarely - angina, chest pain; very rarely - fainting; in patients with angina pectoris, an increase in the frequency, duration and severity of attacks is possible. On the digestive system: rarely - nausea, dyspepsia, diarrhea, epigastric pain, vomiting. On the side of the skin and subcutaneous tissues: rarely - skin rash. musculoskeletal system: rarely - myalgia. From the urinary system: rarely polyuria. From the immune system: very rarely - hypersensitivity reactions. From the whole body: rarely - peripheral edema; rarely - asthenia, fatigue. There are reports of the following very rare (less than 1 / 10,000) events: myocardial infarction, gingival hyperplasia, a reversible increase in liver transaminase activity, marked reduction in blood pressure, pollakiuria (increased frequency of urination), pain in the chest.
Overdose
Presumably, in the case of an overdose of lercanidipine, symptoms similar to those with an overdose of other dihydropyridine derivatives will be observed: peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia. Treatment: symptomatic therapy; in case of a pronounced decrease in blood pressure, loss of consciousness, cardiovascular therapy is indicated,with bradycardia - in / in the introduction of atropine. There are data on 3 cases of overdose when taking lercanidipine in doses of 150 mg, 280 mg and 800 mg for suicide. In the case of receiving 150 mg of lercanidipine + alcohol (an unspecified amount), drowsiness was observed. Treatment : gastric lavage, taking activated carbon. In the case of receiving 280 mg of lercanidipine + 5.6 mg of moxonidine, the following symptoms were observed: cardiogenic shock, severe myocardial ischemia, mild renal failure. Treatment: cardiac glycosides, diuretics (furosemide), high doses teholaminov, plazmozameniteli.V case of receiving 800 mg lercanidipine and nausea were observed marked reduction AD.Lechenie: administration of activated charcoal and a laxative, in / - dopamin.Vo all cases of overdose, all patients were alive. Information on the effectiveness of dialysis for lercanidipine is missing. Most likely, due to the high association of lercanidipine with plasma proteins, dialysis may be ineffective.
Interaction with other drugs
Lercanidipine can be used simultaneously with beta-blockers, diuretics, ACE inhibitors. When used simultaneously with metoprolol, the bioavailability of lercanidipine is reduced by 50%. This effect can occur with simultaneous use with other beta-blockers, so you may need to adjust the dose of lercanidipine to achieve a therapeutic effect with this combination. Lercanidipine is metabolized with the participation of CYP3A4 isoenzyme, therefore inhibitors and inductors of this isoenzyme, when used simultaneously, can affect the metabolism and elimination of lercanidipine. The simultaneous use of lercanidipine with CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) is not recommended. The simultaneous use of cyclosporine and lercanidipine is not recommended. an increase in the concentration of both substances in the blood plasma is observed. Caution should be exercised when simultaneously using lercanidipine with other CYP3A4 substrates (terfenadine, astemizole, class III antiarrhythmic drugs, for example, amiodarone, quinidine). Elderly patients may increase by approximately 40%. Lercanidipine should be administered with caution simultaneously with inducers of CYP3A4, for example, anticonvulsants (hair dryer itoin, carbamazepine) and rifampicin, since a decrease in the antihypertensive effect of the drug is possible.Regular blood pressure monitoring is necessary. With simultaneous use of lercanidipine at a dose of 20 mg in patients constantly taking beta-methyldigoxin, no pharmacokinetic interaction was observed, while healthy volunteers who were treated with digoxin showed an increase in Cmax for digoxin by an average of 33 % after taking 20 mg of Lercanidipine on an empty stomach, while the AUC and renal clearance changed slightly. It is necessary to control the presence of signs of digoxin intoxication in patients taking both digoxin and lercanidipine. Simultaneous use of lercanidipine with cimetidine (up to 800 mg) does not cause significant changes in plasma concentration of lercanidipine. At high doses of cimetidine, the bioavailability and antihypertensive effect of lercanidipine may increase. With simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg), the AUC value for simvastatin increased by 56%, and the same value for its active metabolite - β-hydroxy acid - by 28%. When taking medications at different times of day (lercanidipine in the morning, simvastatin in the evening), undesirable interactions can be avoided. With simultaneous use of lercanidipine at a dose of 20 mg and warfarin in healthy volunteers, no changes in the pharmacokinetics of warfarin were observed. Simultaneous use with fluoxetine (CYP2D6 inhibitor and CYP3P3 inhibitor). in elderly patients, there was no clinically significant change in the pharmacokinetics of lercanidipine. It is possible to enhance the antihypertensive effect while taking grapefruit juice and lehrka nidipina.Etanol may potentiate the antihypertensive effect of lercanidipine.
special instructions
Influence on the ability to drive motor vehicles and control mechanisms. Since therapy with Lerkamen may cause dizziness, asthenia, fatigue and in rare cases of drowsiness, during the period of use of the drug, patients should be especially careful to drive vehicles and engage in other potentially dangerous activities that require high speed psychomotor reactions.