Lerkamen 10 - a derivative of dihydropyridine; Selective calcium channel blocker, affecting mainly vessels.
Release form and composition
Dosage form - tablets: round, biconvex, film-coated from pale to light yellow color, with a risk on one side (7 pieces in blisters, in a cardboard bundle 1 blister; 14 pieces in blisters, in a cardboard bundle 1 or 2 blisters; 15 pieces in blisters, in a cardboard box 4 or 6 blisters).
The composition of the drug (1 tablet):
- Active ingredient: lercanidipine hydrochloride - 10 mg;
- Auxiliary components: microcrystalline cellulose, Povidone K30, lactose monohydrate, sodium carboxymethyl starch (type A), magnesium stearate;
- The composition of the shell: opadry OY-SR-6497 (macrogol 6000, hypromellose, titanium dioxide, talc, dye iron oxide yellow).
Indications for use
Lerkamen 10 is intended for the treatment of essential hypertension of grades I-II.
- Severe renal failure (creatinine clearance less than 30 ml / min);
- Severe liver failure;
- Unstable Angina;
- Obstruction of vessels emanating from the left ventricle of the heart;
- Untreated heart failure;
- Period 1 month after myocardial infarction;
- Lactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
- Simultaneous use of cyclosporine or inhibitors of CYP3A4 (itraconazole, ketoconazole, ritonavir, erythromycin, troleandomycin);
- Simultaneous intake with grapefruit juice;
- Lack of reliable contraceptive methods;
- Lactation period;
- Age up to 18 years;
- Hypersensitivity to the components of the drug or other derivatives of the dihydropyridine series.
- Renal failure (creatinine clearance more than 30 ml / minute);
- Hepatic failure mild to moderate severity;
- Sick sinus syndrome;
- Coronary heart disease;
- Left ventricular dysfunction;
- Elderly age.
Dosing and Administration
Lerkamen 10 should be taken orally, preferably in the morning, at least 15 minutes before a meal, swallowing the pill whole and drinking plenty of water.
Adult patients are prescribed 10 mg (1 tablet) 1 time per day, if necessary, the dose can be increased to 20 mg.
The maximum hypotensive effect develops after about 2 weeks, so the optimal therapeutic dose is selected gradually. It is unlikely that the effect will increase with an increase in the daily dose of more than 20 mg, but the likelihood of side effects will increase.
- Nervous system: - dizziness and / or headache; rarely - drowsiness;
- Cardiovascular system: infrequently - flushing of the skin of the face, tachycardia, sensation of heartbeat; rarely - pain behind the sternum, angina; very rarely - fainting, in patients with angina pectoris - an increase in the frequency, severity and duration of the attacks;
- Digestive system: rarely - epigastric pain, nausea, diarrhea, vomiting, dyspepsia;
- Urinary system: rarely - polyuria;
- Musculoskeletal system: rarely - myalgia;
- Immune system: very rarely - hypersensitivity reactions;
- Skin and Subcutaneous Tissues: Rarely, skin rashes;
- Other: infrequent - peripheral edema; rarely - increased fatigue, asthenia.
There are reports of very rare cases (less than in 1 patient out of 10,000) of the following side effects: pollakiuria, reversible increase in liver transaminase activity, gum hyperplasia, chest pain, marked reduction in blood pressure, myocardial infarction.
Lerkamen 10 can cause fatigue, dizziness, asthenia and, in rare cases, drowsiness, therefore, during treatment, special care should be taken when driving and engaging in potentially hazardous activities that require high-speed psychophysical reactions.
If necessary, Lerkamen 10 can be prescribed in combination with diuretics, beta-blockers, angiotensin-converting enzyme inhibitors.
With the simultaneous use of metoprolol, the bioavailability of lercanidipine hydrochloride is reduced by 50%. This phenomenon is also possible when taking other beta-blockers, therefore, in order to achieve a therapeutic effect with such a combination, a dose adjustment of Lerkamen may be required.
Lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme, so the inducers and inhibitors of this isoenzyme can affect its metabolism and excretion. It is not recommended to use inhibitors of CYP3A4 (ritonavir, itraconazole, erythromycin, ketoconazole, troleandomycin) at the same time. When prescribing CYP3A4 inducers (for example, anticonvulsants, rifampicin), caution should be exercised and blood pressure should be monitored regularly. There is a possibility of reducing the hypotensive effect of the drug.
With caution during treatment with Lerkamen, other CYP3A4 substrates are prescribed, such as class III antiarrhythmic drugs, astemizole, terfenadine.
When taking Lerkamena at a dose of 20 mg in combination with midazolam, the bioavailability of lercanidipine in the elderly can increase by about 40%.
If necessary, the concomitant use of digoxin is necessary to monitor the patient's condition in time to identify possible signs of intoxication.
Lercanidipine is not recommended to be prescribed in combination with cyclosporine, since with such a combination an increase in plasma concentration of both substances is noted.
Cimetidine, used in high doses, can increase the bioavailability and antihypertensive effect of lercanidipine.
While taking lercanidipine at a dose of 20 mg and simvastatin at a dose of 40 mg, the AUC value (total plasma concentration during the entire observation period) of simvastatin increased by 56%, and its active metabolite - β-hydroxy acid - by 28%. It is possible to avoid this undesirable interaction if you take drugs at different times of the day: in the morning - lercanidipine, in the evening - simvastatin.
Ethanol and grapefruit juice potentiate the antihypertensive effect of Lerkamen.
Terms and conditions of storage
Store at temperatures up to 30 ºС out of the reach of children.
Shelf life - 3 years.