Amlodipine (in the form of besylate) 10 mg
Selective calcium channel blocker class II. Antihypertensive effect due to a direct relaxing effect on vascular smooth muscle. It is assumed that the antianginal effect of amlodipine is associated with its ability to expand peripheral arterioles; this leads to a decrease in OPSS, reflex tachycardia does not occur. As a result, there is a decrease in myocardial oxygen demand and energy consumption by the heart muscle. On the other hand, amlodipine, apparently, causes the expansion of large-caliber coronary arteries and coronary arterioles in both intact and ischemic myocardial regions. This provides oxygen to the myocardium during spasms of the coronary arteries.
When ingestion is absorbed from the gastrointestinal tract slowly and almost completely, Cmax in the blood plasma is achieved within 6-9 hours. Protein binding is 95-98%. It undergoes minimal metabolism during the first passage through the liver and a slow but significant hepatic metabolism with the formation of metabolites with negligible pharmacological activity. T1 / 2 averages 35 hours and in arterial hypertension can increase on average to 48 hours, in elderly patients - up to 65 hours and in case of abnormal liver function, up to 60 hours. It is eliminated mainly as metabolites: 59-62% by the kidneys, 20-25% through the intestines.
Arterial hypertension (as monotherapy or as part of combination therapy). Stable angina pectoris, unstable angina pectoris, Prinzmetal angina pectoris (as monotherapy or as part of combination therapy).
Severe arterial hypotension (systolic blood pressure less than 90 mm Hg); obstruction of the outflow tract of the left ventricle (including severe aortic stenosis); hemodynamically unstable heart failure after myocardial infarction; children and adolescents under 18 years of age (efficacy and safety have not been established); Hypersensitivity to amlodipine and other dihydropyridine derivatives.
In the course of treatment, exacerbation of psoriasis is possible. During pheochromocytoma, propranolol can be used only after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually,under the supervision of a doctor. Against the background of treatment with propranolol, it is necessary to avoid intravenous injection of verapamil, diltiazem. For several days before undergoing anesthesia, it is necessary to stop taking propranolol or to choose a remedy for anesthesia with minimal negative inotropic effect. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
The safety of using amlodipine during pregnancy has not been established; therefore, it is possible to use it only if the intended benefit to the mother outweighs the potential risk to the fetus. There is no data indicating the elimination of amlodipine in breast milk. However, it is known that other blockers of slow calcium channels (dihydropyridine derivatives) are excreted in breast milk. In this regard, if necessary, the use of amlodipine during lactation should decide on the termination of breastfeeding.
Dosage and administration
For adults, by ingestion, the initial dose is 5 mg 1 time / day. If necessary, the dose may be increased. The maximum dose: when administered orally - 10 mg / day.
Since the cardiovascular system: peripheral edema, tachycardia, skin hyperemia; when used in high doses - arterial hypotension, arrhythmias, shortness of breath. On the part of the digestive system: nausea, abdominal pain; rarely - gingival hyperplasia. From the side of the central nervous system and peripheral nervous system: headache, fatigue, drowsiness, dizziness; with long-term use - paresthesia. Allergic reactions: skin rash, itching. Others: with prolonged use - pain in the limbs.
Interaction with other drugs
It is possible to enhance the antianginal and antihypertensive action of blockers of slow calcium channels when used together with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as enhance their anti-hypertensive action when combined with alpha1-blockers,neuroleptic drugs. While in the study of amlodipine, negative inotropic effects were not usually observed, however, some blockers of slow calcium channels may increase the severity of the negative inotropic effects of antiarrhythmic drugs that cause prolongation of the QT interval (eg, amiodarone and quinidine). Simultaneous multiple use of amlodipine at a dose of 10 mg and simvastatin at a dose of 80 mg leads to an increase in the bioavailability of simvastatin by 77%. In such cases, the dose of simvastatin should be limited to 20 mg. Antiviral drugs (for example, ritonavir) increase plasma concentrations of blockers of slow calcium channels, including. amlodipine. With simultaneous use of sympathomimetics, estrogens, a decrease in the antihypertensive effect due to sodium retention in the body is possible. Neuroleptics and isoflurane increase the antihypertensive effect of dihydropyridine derivatives. With simultaneous use of drugs for inhalation anesthesia, hypotensive effect may be enhanced. With simultaneous use of amiodarone, increased antihypertensive effect is possible. With simultaneous use of lithium carbonate, manifestations of neurotoxicity are possible (including nausea, vomiting, diarrhea, ataxia, tremors, and / or tinnitus ). With the simultaneous use of orlistat reduces the antihypertensive effect of amlodipine, which can lead to a significant increase in blood pressure, the development of hypertensive crisis. At the same time Indomethacin and other NSAIDs may reduce the antihypertensive effect of amlodipine due to inhibition of prostaglandin synthesis in the kidneys and fluid retention under the influence of NPVS. Simultaneous use of quinidine may increase the antihypertensive effect. Calcium preparations can reduce the effect of slow calcium channel blockers. ) at a dose of 180 mg and amlodipine at a dose of 5 mg in elderly patients (from 69 to 87 years old) with arterial hypertension, tsya increase the bioavailability of amlodipine by 57%. The simultaneous use of amlodipine and erythromycin in healthy volunteers (from 18 to 43 years old) does not lead to significant changes in the exposure to amlodipine (an increase in AUC by 22%).Although the clinical significance of these effects is not completely clear, they may be more pronounced in older patients. Potent inhibitors of the isoenzyme CYP3A4 (for example, ketoconazole, itraconazole) can lead to an increase in the concentration of amlodipine in the blood plasma to a greater extent than diltiazem. Amlodipine and CYP3A4 isoenzyme inhibitors should be used with caution. There is no data on the effect of CYP3A4 isoenzyme inducers on the pharmacokinetics of amlodipine. Blood pressure should be carefully monitored with simultaneous use of amlodipine and CYP3A4 isoenzyme inducers.
Caution should be used in patients with hepatic insufficiency, chronic heart failure of non-ischemic etiology of III-IV functional class according to NYHA classification, unstable angina, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 month after), SSS (severe tachycardia, bradycardia), arterial hypotension, with simultaneous use with inhibitors or inducers of CYP3A4 isoenzyme. Against the background of the use of amlodipine and in patients with chronic heart failure (NYHA class III and IV) of non-ischemic genesis, there was an increase in the incidence of pulmonary edema, despite no signs of worsening heart failure. In elderly patients, T1 / 2 may increase and clearance of amlodipine may decrease. Changes in doses are not required, but more careful monitoring of patients in this category is needed. The efficacy and safety of using amlodipine in hypertensive crisis has not been established. Despite the fact that blockers of slow calcium channels have no withdrawal syndrome, discontinuation of treatment with amlodipine is desirable gradually. Clinical data on the use of amlodipine in pediatrics are absent.