Lerkamen 20 is a selective calcium channel blocker that primarily affects vessels.
Release form and composition
Dosage form - tablets: round, biconvex, film-coated reddish-pink color, with a risk on one side (7 pieces in blisters, in a cardboard bundle 1 or 5 blisters; 10 pieces in blisters, in a cardboard bundle 5, 6, 9 or 10 blisters; 14 pieces in blisters, in a cardboard bundle 1, 2, 3, 4 or 7 blisters).
The composition of the drug (1 tablet):
- Active ingredient: lercanidipine hydrochloride - 20 mg;
- Auxiliary components: microcrystalline cellulose, lactose monohydrate, povidone K30, sodium carboxymethyl starch (type A), magnesium stearate;
- The composition of the shell: opadry 02F25077 9 (titanium dioxide, macrogol 6000, talc, hypromellose, iron oxide (III)).
Indications for use
Lerkamen 20 is used for essential hypertension of grades I-II.
- Age up to 18 years;
- Period 1 month after myocardial infarction;
- Obstruction of vessels emanating from the left ventricle of the heart;
- Unstable Angina;
- Untreated heart failure;
- Severe liver failure;
- Severe renal failure (creatinine clearance less than 30 ml / min);
- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome;
- Simultaneous intake with grapefruit juice;
- Simultaneous use of cyclosporine or CYP3A4 inhibitors (erythromycin, ritonavir, troleandomycin, itraconazole, ketoconazole);
- Lack of reliable contraceptive methods;
- Hypersensitivity to the components of the drug or other dihydropyridine derivatives.
- Elderly age;
- Mild and moderate liver failure;
- Renal failure (or creatinine clearance more than 30 ml / minute);
- Coronary heart disease;
- Sick sinus syndrome;
- Dysfunction of the left ventricle.
Dosing and Administration
The drug is taken orally, preferably in the morning, at least a quarter of an hour before meals. Tablets are swallowed whole with water.
The initial recommended dose is 10 mg 1 time per day. If the effect is insufficient, the dose is increased to 20 mg.
It is necessary to select an effective therapeutic dose gradually, since The maximum hypotensive effect of the drug appears after about 2 weeks of treatment. With increasing doses of more than 20 mg / day is unlikely to increase the effect, but it is well established that the risk of side effects will increase.
Classification of side effects: often - less than 1/10, but more or equal to 1/100, infrequently - less than 1/100, but more and equal to 1/1000, rarely - less than 1/1000, but more or equal to 1/10000, extremely rarely less than 1/10000, including isolated cases.
Possible side effects:
- Digestive system: rarely - pain in the area of epigastria, nausea and / or vomiting, diarrhea, dyspepsia;
- Immune system: extremely rare - hypersensitivity reactions;
- Cardiovascular system: infrequently - tachycardia, flushing of the skin of the face, feeling of heartbeat; rarely - pain behind the sternum and angina; extremely rarely - fainting, in patients with angina pectoris, an increase in severity, duration and frequency of seizures is possible;
- Musculoskeletal system: rarely - myalgia;
- Urinary system: rarely - polyuria;
- Skin and subcutaneous tissue: rarely - skin rash;
- Nervous system: infrequently - dizziness, headache; rarely - drowsiness;
- Other: infrequent - peripheral edema; rarely - asthenia and fatigue.
There were separate reports that in very rare cases (<1/10000) the following side effects developed: chest pain, gingival hyperplasia, marked reduction in blood pressure, pollakiuria, reversible increase in liver transaminase activity, myocardial infarction.
While taking Lerkamena 20, fatigue, asthenia, dizziness and drowsiness are possible, therefore during the initial stages of treatment, while the patient is able to assess the degree of adverse effects of the drug, it is recommended to use caution when driving vehicles and performing work with potentially dangerous consequences that require high mental and physical speed reactions.
Lerkamen 20 can be used in combination with angiotensin-converting enzyme inhibitors, beta-blockers and diuretics.
Ethanol and grapefruit juice may enhance the antihypertensive effect of Lerkamena.
Metoprolol, taken simultaneously, reduces the bioavailability of lercanidipine hydrochloride by 50%. The same reaction is possible with the use of other beta-blockers, therefore, to achieve a therapeutic effect in the case of the appointment of this combination, it is necessary to adjust the dose of lercanidipine.
Since lercanidipine is metabolized by a CYP3A4 isoenzyme, inhibitors and inductors of this enzyme can affect the metabolism and excretion of the active substance Lerkamena. Inductors (for example, rifampicin and anticonvulsants) can reduce the hypotensive effect of the drug, so they should be used with caution, under constant control of blood pressure. Inhibitors (including ketoconazole, erythromycin, troleandomycin, itraconazole, ritonavir) are not recommended at the same time. Other CYP3A4 isoenzyme substrates should be used with caution, for example, astemizole, terfenadine and class III antiarrhythmic drugs.
When receiving Lerkamena 20 mg by the elderly, simultaneously with midazolam, the bioavailability of lercanidipine increases by approximately 40%.
When using cimetidine in high doses, it is possible to increase the bioavailability and hypotensive action of lercanidipine.
In clinical studies on volunteers who received digoxin treatment, it was found that after taking Lerkamena 20, the concentration of digoxin increases on an empty stomach by an average of 33%. Renal clearance and the total concentration varies slightly. If necessary, the appointment of such a combination should be monitored the appearance of signs of digoxin intoxication.
With simultaneous use of lercanidipine and cyclosporine, a mutual increase in plasma concentration is possible, therefore this combination is contraindicated.
At the same time taking Lerkamena 20 and simvastatin in a dose of 40 mg, the total concentration of simvastatin increases by about 56%, and the concentration of its active metabolite - β-hydroxy acid - by 28%. To avoid undesirable interaction of these drugs can be when they are taken at different times of day: lercanidipine in the morning, simvastatin in the evening.
Terms and conditions of storage
Store at a temperature not exceeding 30 ° C. Keep out of the reach of children.
Shelf life - 3 years.