Lerkamen 10 tablets p/o 10mg №15×4

Name:
Lerkamen 10 tablets p / o 10 mg in a blister in pack No. 15×4
Description:
Film-coated tablets from pale yellow to light yellow, round, biconvex, with a risk on one side; on a break – light yellow color. The main active ingredient Lercanidipine Release form Pale yellow to light yellow film-coated tablets, round, biconvex, scored on one side; on a break – light yellow color. 1 tab. lercanidipine hydrochloride 10 mg Excipients: 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. Shell composition: Opadry OY-SR-6497 – 3 mg (hypromellose – 1.913 mg, macrogol 6000 – 0.3 mg, talc – 0.15 mg, titanium dioxide – 0.6 mg, iron dye yellow oxide – 0.037 mg). 15 pcs. – blisters (4) – packs of cardboard. Influence on the ability to drive vehicles and control mechanisms Since dizziness, asthenia, fatigue and, in rare cases, drowsiness may occur during Lerkamen® therapy, during the period of drug use, patients should drive vehicles with extreme caution and engage in other potentially hazardous activities that require high speed of psychomotor reactions. Pharmacological action Selective blocker of slow calcium channels with a predominant effect on the vessels, a derivative of dihydropyridine. Inhibits the transmembrane current of calcium ions into vascular smooth muscle cells. The mechanism of the antihypertensive action of lercanidipine is due to a direct relaxing effect on vascular smooth muscle cells, resulting in a decrease in peripheral vascular resistance. Despite a relatively short plasma half-life, lercanidipine has a prolonged antihypertensive effect due to its high membrane distribution coefficient. Due to the high vascular selectivity, it does not have a negative inotropic effect. Acute arterial hypotension with reflex tachycardia rarely occurs due to the gradual development of vasodilation when 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 duration of the therapeutic effect is 24 hours. Pharmacokinetics Absorption Lercanidipine is completely absorbed after oral administration. Cmax in plasma is reached after 1.5-3 hours and is 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 a similar pharmacokinetic profile: they have the same time to reach Cmax, the same T1 / 2; Cmax and AUC values are 1.2 times higher for the (-)S-enantiomer. Interconversions of enantiomers were not observed in experiments in vivo. Due to the “first pass” effect through the liver, the absolute bioavailability of lercanidipine when taken orally after a meal is approximately 10%, when taken on an empty stomach, the bioavailability value decreases by 1/3. When taking lercanidipine no later than 2 hours after a fatty meal, its bioavailability increases by 4 times, so Lerkamen® should not be taken after meals. With oral administration of lercanidipine, its plasma concentration is not directly proportional to the dose taken (nonlinear kinetics). Saturation of presystemic metabolism occurs gradually. Thus, bioavailability increases with increasing dose. Distribution Distribution from plasma to tissues and organs is rapid and extensive. Plasma protein binding exceeds 98%. Metabolism and excretion Lercanidipine is metabolized with the participation of the 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 intestines). Elimination occurs mainly by biotransformation. The average T1 / 2 is 8-10 hours. Cumulation of lercanidipine with repeated oral administration is not observed. Pharmacokinetics in special clinical situations The pharmacokinetics of lercanidipine in elderly patients, in patients with renal insufficiency (CC more than 30 ml / min) and in patients with mild to moderate hepatic insufficiency have been shown to be similar to the pharmacokinetics observed in the general patient population. In patients with renal insufficiency (CC less than 30 ml / min) and in patients on hemodialysis, plasma concentrations of lercanidipine were higher (approximately 70%). In patients with severe renal and / or hepatic insufficiency due to a decrease in plasma protein concentration, the free fraction of lercanidipine may increase. In patients with moderate to severe hepatic insufficiency, the systemic bioavailability of lercanidipine is likely to be increased, since lercanidipine is metabolized primarily in the liver. Indications for use – essential hypertension I-II severity. Dosing and Administration The drug is taken orally, at least 15 minutes before meals, preferably in the morning, without chewing, drinking plenty of water. Assign 10 mg 1 time / day. Depending on the individual tolerability of the drug by the patient, the dose may be increased to 20 mg. The therapeutic dose is selected gradually, because. The 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, the risk of side effects increases. The pharmacokinetic profile and data from clinical studies show that in elderly patients dose adjustment of Lerkamen® is not required. However, caution should be exercised at the initial stage of treatment with Lerkamen® in this group of patients. When using the drug Lerkamen® in patients with mild to moderate renal and hepatic insufficiency, caution should be exercised. In case of renal insufficiency (CC more than 30 ml / min) or mild or moderate hepatic insufficiency, the initial dose is 10 mg, then the dose is increased with caution to 20 mg / day. The antihypertensive effect may be enhanced in patients with mild or moderate hepatic insufficiency and dose adjustment (reduction) may be required. With renal failure (CC less than 30 ml / min) and severe liver failure, the use of the drug Lerkamen® Use during pregnancy and lactation The use of the drug Lerkamen® during pregnancy and during breastfeeding, as well as in women of childbearing age in the absence of reliable contraception is contraindicated . In preclinical studies, no teratogenic effect of lercanidipine was detected in rats and rabbits, the reproductive function of rats was unchanged. In view of the lack of clinical experience with the use of lercanidipine during pregnancy and lactation, and since other dihydropyridine derivatives are known to have a teratogenic effect in animals, lercanidipine is not recommended for use during pregnancy and in women of childbearing age who do not use reliable methods of contraception. Due to the high lipophilicity of lercanidipine, it can be assumed that it passes into breast milk, so the drug is not recommended for use during breastfeeding elderly, with SSSU (without a pacemaker), coronary artery disease, left ventricular dysfunction. Interaction with other drugs Lercanidipine can be used simultaneously with beta-blockers, diuretics, ACE inhibitors. With simultaneous use with metoprolol, the bioavailability of lercanidipine is reduced by 50%. This effect may also occur when used simultaneously with other beta-blockers, so dose adjustment of lercanidipine may be required to achieve a therapeutic effect with this combination. Lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme, therefore, inhibitors and inducers of this isoenzyme, when used simultaneously, can affect the metabolism and excretion of lercanidipine. Co-administration of lercanidipine with CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) is not recommended. The simultaneous use of cyclosporine and lercanidipine is not recommended, because. there is an increase in the concentration of both substances in the blood plasma. Caution should be exercised when lercanidipine is co-administered with other CYP3A4 substrates (terfenadine, astemizole, class III antiarrhythmics, eg amiodarone, quinidine). With the simultaneous use of lercanidipine at a dose of 20 mg with midazolam, the bioavailability of lercanidipine in elderly patients can increase by approximately 40%. Lercanidipine should be administered with caution concomitantly with CYP3A4 inducers, such as anticonvulsants (phenytoin, carbamazepine) and rifampicin, since the antihypertensive effect of the drug may be reduced. Regular blood pressure monitoring is required. With the simultaneous use of lercanidipine at a dose of 20 mg in patients constantly taking beta-methyldigoxin, no pharmacokinetic interaction was observed, while in healthy volunteers who were treated with digoxin, there was an increase in Cmax for digoxin by an average of 33% after taking 20 mg lercanidipine on an empty stomach, while AUC and renal clearance did not change significantly. Patients taking digoxin and lercanidipine concomitantly should be monitored for signs of digoxin intoxication. The simultaneous use of lercanidipine with cimetidine (up to 800 mg) does not cause significant changes in the concentration of lercanidipine in blood plasma. At high doses of cimetidine, the bioavailability and antihypertensive effect of lercanidipine may increase. With the 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 – α-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. No changes in the pharmacokinetics of warfarin were observed when lercanidipine 20 mg was co-administered with warfarin in healthy volunteers. Simultaneous use with fluoxetine (an inhibitor of CYP2D6 and CYP3A4) in elderly patients did not have a clinically significant change in the pharmacokinetics of lercanidipine. It is possible to increase the antihypertensive effect while taking grapefruit juice and lercanidipine. Ethanol may potentiate the antihypertensive effect of lercanidipine. Contraindications – untreated heart failure; – unstable angina; – obstruction of blood vessels emanating from the left ventricle of the heart; – a period within 1 month after myocardial infarction; – severe liver 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 reception with grapefruit juice; – lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome; – pregnancy; – lactation period (breastfeeding); – use in women of childbearing age who do not use reliable methods of contraception; – children and adolescents under 18 years of age (efficacy and safety have not been studied); – hypersensitivity to the components of the drug; – Hypersensitivity to other derivatives of the dihydropyridine series. Composition 1 tab. lercanidipine hydrochloride 10 mg Excipients: 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. Shell composition: Opadry OY-SR-6497 – 3 mg (hypromellose – 1.913 mg, macrogol 6000 – 0.3 mg, talc – 0.15 mg, titanium dioxide – 0.6 mg, iron dye yellow oxide – 0.037 mg). Overdose Presumably, in case of an overdose of lercanidipine, symptoms similar to those with an overdose of other dihydropyridine derivatives will be observed: peripheral vasodilation with a marked decrease in blood pressure and reflex tachycardia. Treatment: symptomatic therapy; in the case of a pronounced decrease in blood pressure, loss of consciousness, cardiovascular therapy is indicated, in case of bradycardia – in / in the introduction of atropine. There are data on 3 cases of overdose when taking lercanidipine at doses of 150 mg, 280 mg and 800 mg with the aim of suicide. Drowsiness has been observed in the case of lercanidipine 150 mg + alcohol (unspecified amount). Treatment: gastric lavage, activated charcoal. In the case of taking 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 of catecholamines, plasma substitutes. In the case of taking 800 mg of lercanidipine, nausea and a pronounced decrease in blood pressure were observed. Treatment: taking activated charcoal and a laxative, IV – dopamine. In all cases of overdose, all patients survived. There is no information available on dialysis efficacy for lercanidipine. It is most likely that due to the high binding of lercanidipine to plasma proteins, dialysis may not be effective. Side effects Possible side effects are listed below in descending frequency of occurrence: often (<1/10, ?1/100), infrequently (<1/100, ?1/1000), rarely (<1/1000, ?1/10000), very rarely (<1/10000), including individual messages. From the nervous system: infrequently - headache, dizziness; rarely - drowsiness. From the side of the cardiovascular system: infrequently - palpitations, tachycardia, flushing of blood to the skin of the face; rarely - angina pectoris, chest pain; very rarely - fainting, in patients with angina pectoris, an increase in the frequency, duration and severity of attacks is possible. From the digestive system: rarely - nausea, dyspepsia, diarrhea, epigastric pain, vomiting. From the skin and subcutaneous tissues: rarely - skin rash. From the musculoskeletal system: rarely - myalgia. From the urinary system: rarely - polyuria. From the immune system: very rarely - hypersensitivity reactions. On the part of the body as a whole: infrequently - peripheral edema; rarely - asthenia, fatigue. There are reports of the following very rare (<1/10,000) side effects: myocardial infarction, gingival hyperplasia, a reversible increase in the activity of "liver" transaminases, a pronounced decrease in blood pressure, pollakiuria (increased frequency of urination), chest pain. Storage conditions The drug should be stored in a place inaccessible to children at a temperature not exceeding 30 ° C. Buy Lerkamen 10 tablets p/o 10mg №15x4 Price for Lerkamen 10 tablets p/o 10mg №15x4