Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
Selective calcium channel blocker II class. Antihypertensive action is caused by a direct relaxing effect on the smooth muscle of the vessels. It is suggested 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 appears to induce the expansion of large-scale coronary arteries and coronary arterioles in both intact and ischemic myocardial regions. This ensures the supply of oxygen to the myocardium with spasms of the coronary arteries.
When ingested absorbed from the gastrointestinal tract slowly and almost completely, C max in the blood plasma is reached within 6-9 hours. Binding with proteins is 95-98%. It is subject to minimal metabolism during the first passage through the liver and slow but significant hepatic metabolism with the formation of metabolites with little pharmacological activity.
T 1/2 on the average is 35 hours and with arterial hypertension can increase on average to 48 hours, in elderly patients - up to 65 hours and with violations of liver function - up to 60 hours. It is excreted mainly in the form of metabolites: 59-62% kidneys, 20-25% - through the intestines.
Arterial hypertension (as a monotherapy or as part of a combination therapy).
Stable angina, unstable angina, Prinzmetal angina (as a monotherapy or as part of a combination therapy).
For adults with oral administration, the initial dose is 5 mg 1 time / day. If necessary, the dose may be increased.
The maximum dose: with oral administration - 10 mg / day.
From the cardiovascular system: peripheral edema, tachycardia, hyperemia of the skin; when used in high doses - arterial hypotension, arrhythmias, dyspnea.
On the part of the digestive system: nausea, abdominal pain; rarely - gingival hyperplasia.
From the central nervous system and peripheral nervous system: headache, fatigue, drowsiness, dizziness; with prolonged use - paresthesia.
Allergic reactions: skin rash, itching.
Other: with prolonged use - pain in the limbs.
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 not established); hypersensitivity to amlodipine and other dihydropyridine derivatives.
PREGNANCY AND LACTATION
The safety of the use of amlodipine in pregnancy is not established, so the application is only possible if the intended benefit to the mother exceeds the potential risk to the fetus.
There is no evidence that amlodipine is excreted 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 you need to use amlodipine during lactation, you should decide whether to stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution for violations of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution for violations of liver function.
APPLICATION FOR CHILDREN
Clinical data on the use of amlodipine in pediatrics are not available.
APPLICATION IN ELDERLY PATIENTS
Older patients do not need a dose reduction.
It should be used with caution in patients with hepatic insufficiency, chronic heart failure of III-IV non-ischemic etiology of NYHA classification, unstable angina, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after it); SSSU (pronounced tachycardia, bradycardia), arterial hypotension, while simultaneous application with inhibitors or inducers of the isoenzyme CYP3A4.
The use of amlodipine in patients with chronic cardiac insufficiency (class III and IV in the NYHA classification) of non-ischemic origin was associated with an increased incidence of pulmonary edema, despite the absence of signs of worsening heart failure.
In elderly patients, T 1/2 can increase and decrease the clearance of amlodipine. Dose changes are not required, but more careful monitoring of patients of this category is necessary.
The efficacy and safety of the use of amlodipine in hypertensive crisis is not established.
Despite the lack of slow calcium channel blockers of withdrawal syndrome, discontinuation of amlodipine treatment is desirable to be carried out gradually.
Clinical data on the use of amlodipine in pediatrics are not available.
It is possible to intensify the antianginal and antihypertensive effect of slow calcium channel blockers when combined with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as enhance their antihypertensive action when combined with alpha 1 adrenoceptor blockers and antipsychotics.
Although no negative inotropic effects were usually observed in the study of amlodipine, nevertheless some slow calcium channel blockers may increase the negative inotropic effect of antiarrhythmic agents that cause prolongation of the QT interval (eg, amiodarone and quinidine).
Simultaneous repeated use of amlodipine in 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 dosage of simvastatin should be limited to 20 mg.
Antiviral drugs (eg, ritonavir) increase plasma concentrations of slow calcium channel blockers, incl. amlodipine.
With the simultaneous use of sympathomimetics, estrogens, it is possible to reduce the antihypertensive effect due to sodium retention in the body.
Neuroleptics and isoflurane increase the antihypertensive effect of dihydropyridine derivatives. With the simultaneous use of funds for inhalation anesthesia, an increase in the hypotensive effect is possible.
With the simultaneous use of amiodarone, an increase in antihypertensive action is possible.
With the simultaneous use of lithium carbonate, manifestations of neurotoxicity are possible (including nausea, vomiting, diarrhea, ataxia, tremor and / or tinnitus).
With simultaneous use orlistat reduces the antihypertensive effect of amlodipine, which can lead to a significant increase in blood pressure, the development of hypertensive crisis.
With the simultaneous use of indomethacin and other NSAIDs, it is possible to reduce the antihypertensive effect of amlodipine due to inhibition of prostaglandin synthesis in the kidneys and fluid retention under the influence of NSAIDs.
With the simultaneous use of quinidine, an increase in antihypertensive action is possible.
Calcium preparations can reduce the effect of blockers of slow calcium channels.
With the simultaneous use of diltiazem (inhibitor isoenzyme CYP3A4) at a dose of 180 mg and amlodipine at a dose of 5 mg in elderly patients (from 69 to 87 years) with arterial hypertension, there is an increase in the bioavailability of amlodipine by 57%. The simultaneous use of amlodipine and erythromycin in healthy volunteers (18 to 43 years old) does not lead to significant changes in the exposure of amlodipine (an AUC increase of 22%). Despite the fact that the clinical significance of these effects is not completely clear, they can be more pronounced in elderly patients. Powerful inhibitors of the isoenzyme CYP3A4 (eg, ketoconazole, itraconazole) can lead to an increased concentration of amlodipine in the blood plasma to a greater extent than diltiazem. Caution is advisable to use amlodipine and inhibitors of the isoenzyme CYP3A4.
Data on the effect of inducers of the isoenzyme CYP3A4 on the pharmacokinetics of amlodipine are not available. It is necessary to carefully monitor blood pressure while using amlodipine and inducers of the isoenzyme CYP3A4.