Treatment of primary hypertension. It can be used alone or in combination with other medicines that lower blood pressure, such as: β-blockers, diuretics or ACE inhibitors.
Composition:
1 tabl powl. contains 2 mg, 4 mg or 6 mg of lacidipine; tablets contain lactose.
Action:
A potent Calcium channel blocker with predominant selective activity on calcium channels of smooth muscle of blood vessels. It expands the peripheral arterioles, which results in a reduction in peripheral resistance and, as a result, a reduction in arterial pressure. In patients treated with lacidipine, there was a significant effect of the therapy on the carotid IMT (intima-media thickness), corresponding to the antiatherosclerotic effect. Lacydizine after oral administration is rapidly but minimally absorbed from the gastrointestinal tract and undergoes significant metabolism during the first pass through the liver. Bioavailability is 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. 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 first month after its passage. Cardiogenic shock or unstable angina.
Precautions:
Very carefully use in patients who have previously had an allergic reaction to another dihydropyridine derivative, because of the theoretical risk of cross-reactivity. Use with caution in patients with: hepatic impairment (possibility of aggravation of hypotensive effect); with a small heart reserve; with disturbances of the sinus-vestibular node and atrial-ventricular node function (there is a theoretical possibility of the effect of lacidipine on the function of the sinus-atrial node and atrioventricular node); with congenital or acquired QT prolongation or concomitant medications that prolong the QT interval, i.e. class I and III anti-arrhythmic drugs, tricyclic antidepressants, certain antipsychotics, antibiotics (e.g. erythromycin) and some antihistamines (eg terfenadine). 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. It is not recommended for use in children and adolescents under 18 due to lack of experience regarding safety and efficacy. 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:
In pregnancy, the drug can only be used in cases where the expected benefits outweigh the potential risk to the fetus. Lacydizine may cause weakening of the uterine contraction of the maternity. Breast-feeding should avoid lacidipine. If the preparation is necessary, breast-feeding should be discontinued. Some patients treated with calcium antagonists have experienced reversible biochemical changes in the sperm head that may interfere with fertilization.
Side effects:
Common: pain and dizziness, palpitations, tachycardia, sudden redness (especially of the face), nausea, indigestion, rash, erythema, pruritus, polyuria, weakness, edema, transient increase in alkaline phosphatase (clinically relevant - uncommon). Uncommon: exacerbation of existing angina, syncope, hypotension, gingival hyperplasia. Rare: depression, angioneurotic edema, urticaria, muscle cramps. Very rare: tremors. Not known: extrapyramidal syndrome
Dosage:
Orally. Initially 2 mg once a day.The dose can be increased to 4 mg, and if necessary to 6 mg daily. The dose should be increased after the time necessary to achieve the full pharmacological effect has elapsed; in practice, this period should not be shorter than 3-4 weeks. In patients with impaired liver function, the starting dose is 2 mg per day; patients should be carefully monitored and a dose reduction may be necessary in severe cases. No dosage adjustment is necessary for patients with kidney disease or elderly patients. The tablets should be taken at the same time every day, preferably in the morning, regardless of meals.
(C)
