Treatment of primary hypertension in monotherapy or in combination with other antihypertensive agents, including beta-blockers, diuretics and ACE inhibitors.
Composition:
1 tabl powl. contains 4 mg or 6 mg of lacidipine; tablets contain lactose.
Action:
A potent Calcium channel blocker. It works almost exclusively on the smooth muscle of blood vessels. By expanding the peripheral arterioles, it reduces the peripheral resistance and, as a result, decreases blood pressure. Lacydizine after oral administration is rapidly but little absorbed from the gastrointestinal tract and undergoes significant metabolism during the first pass through the liver (bioavailability of about 10%). Cmax it is reached 30-150 min after administration. Strongly binds to proteins (> 95%). It is metabolised in the liver by the CYP3A4 isoenzyme. The main metabolites have very low pharmacodynamic activity. Approximately 70% of the dose is excreted in the form of metabolites in the faeces, the remaining part in the form of metabolites in the urine. T0,5 in steady state is 13-19 h.
Contraindications:
Hypersensitivity to the components of the preparation. Aortic stenosis (dihydropyridine derivatives decrease coronary blood flow). Myocardial infarction and the month of myocardial infarction. Severe failure of the left ventricle. Cardiogenic shock or unstable angina.
Precautions:
Very carefully use in patients who have previously had an allergic reaction to another dihydropyridine derivative (risk of cross-reactivity). Use with caution in patients with: hepatic impairment (increased bioavailability of lacidipine and possible aggravation of hypotensive effect); with disturbances of automatism and conduction in history (there is a theoretical possibility of influencing lacidipine activity on the sinus node and atrioventricular node); with congenital or documented acquired QT prolongation or concomitant medications that prolong QT interval, including class I and III antiarrhythmics, tricyclic antidepressants, certain antipsychotics, antibiotics (e.g. erythromycin) and some antihistamines (eg terfenadine) ; with a small functional reserve of the heart. There is no evidence of the efficacy of lacidipine in the secondary prevention of myocardial infarction. The efficacy and safety of lacidipine in the treatment of malignant hypertension has not been established. In patients who develop unstable angina or cardiogenic shock, lacidipine should be discontinued under the supervision of a physician. There is no experience regarding the use of lacidipine in children <18 years - do not use. Due to the lactose content, the drug should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
During pregnancy, use only if the expected benefits to the mother outweigh the potential risk to the fetus or newborn. Lacydizine may cause weakening of the uterine muscle contraction during delivery. Lapidipine and its metabolites are likely to pass into breast milk - avoid use during lactation (can be used during breastfeeding only if the benefits for the mother are greater than the potential risk of side effects in the baby). Some patients treated with calcium antagonists have experienced reversible biochemical changes in the sperm head that may impede fertilization.
Side effects:
Common: dizziness and headache (usually receding during continued treatment), palpitations (usually resolving during continued treatment), tachycardia, sudden redness, especially of the face (usually resolving during further treatment), abdominal discomfort, nausea, rash, erythema, pruritus, polyuria, weakness, edema (usually receding during further treatment), transient increase in alkaline phosphatase (sometimes clinically relevant). Uncommon: fainting, angina pectoris, hypotension, gingival hyperplasia.Rare: angioneurotic edema, urticaria, muscle cramps. Very rare: depression, tremor.
Dosage:
Orally. Adults: initially 2 mg once a day. The dose can be increased up to 4 mg a day and then (if necessary) to 6 mg a day, each time at least 3-4 weeks apart. No doses> 6 mg / day were found to be significantly more effective.Special groups of patients. A dose reduction may be necessary in patients with severe hepatic impairment. No dose adjustment is necessary in the elderly or in patients with impaired renal function.Way of giving. Take it at the same time every day, preferably in the morning. Table. 4 mg can be divided into equal doses.