Amlodipine - instructions for use, dose, side effects, contraindications

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, apparently, causes the expansion of coronary arteries of large caliber and coronary arterioles in both intact and ischemic areas of the myocardium. This ensures the supply of oxygen to the myocardium with spasms of the coronary arteries.

Pharmacological effects

Antianginal. Antihypertensive.

The maximum effect after 7-8 days.The duration of action is 24 hours.

Pharmacokinetics:

F is 60-65%. Relationship with plasma proteins 95-98%. VD - 21 l / kg. Biotransformation in the liver (90%) to low-active metabolites (CYP3A3, 3A4). A minimal effect of the first passage through the liver is characteristic. T1 / 2 - 30-50 h. Cl - 5.9 ± 1.5 ml / min (reduced with hepatitis and in elderly patients). Elimination by the kidneys (5% - unchanged, 59-62% - in the form of metabolites) and with feces (20-25%). It is not removed during hemodialysis.

Indications:

Arterial hypertension (including as part of combination therapy), stable angina, unstable angina, Prinzmetal angina.

ICD-10

IX.I10-I15.I10 Essential [primary] hypertension

IX.I20-I25.I20 Angina pectoris [angina pectoris]

IX.I20-I25.I20.0 Unstable angina

IX.I20-I25.I20.1 Angina with documented spasm

Contraindications:

Hypersensitivity (including other dihydropyridines), severe arterial hypotension, pregnancy, breast-feeding.

Carefully:Arterial hypotension, aortic stenosis, CHF, hepatic insufficiency, AMI and 1 month after it, hypertrophic obstructive cardiomyopathy, SSSU and mitral stenosis, age under 18 years (efficacy and safety of use not established), elderly age.

Pregnancy and lactation:

Pregnancy

FDA recommendation category C.Adequate and well-controlled studies on humans have not been conducted. When used in rats at a dose of 10 mg / kg per day in the period of organogenesis caused a fivefold increase in the frequency of fetal death and a decrease in the size of the fetus by 50%. Increases the duration of labor in rats.

Lactation

There is no information on the penetration into breast milk. Do not apply!

Dosing and Administration:

Arterial hypertension: the initial dose is 2.5 mg / day; increase to 5 mg / day (in patients with diabetes - up to 10 mg / day). Stenocardia tension - 3 mg / day, vasospastic angina - 5-15 mg / day, prevention of painless myocardial ischemia: the initial dose of 5 mg / day is increased to 10 mg / day. IHD (angiographically confirmed), including those accompanied by CHF or a reduction in ejection fraction of up to 40%, to reduce the risk of hospitalization for angina pectoris or revascularization procedures.

Inside. The initial dose - 5 mg / day in 1 reception with a gradual increase to 10 mg / day.

Use in children

Arterial hypertension.

Inside. 1 month-12 years: begin with a dose of 100-200 mcg / kg once a day; if necessary, the dose is increased every 1-2 weeks to 400 mcg / kg once a day; the maximum dose is 10 mg / day.12-18 years: begin with a dose of 5 mg / day (once), if necessary, increase the dose to 10 mg / day.

The tablet can be dissolved in water.

Side effects:

Peripheral edema, dizziness, flush to the face and sensation of fever, headache, hypotension, tachycardia, unusual fatigue, weakness. Nausea, constipation. Stenocardia, arrhythmias, bradycardia, excessive hypotension (fainting). Hyperplasia of the gums, an increase in the activity of hepatic enzymes in the blood. Allergic reactions.

Overdose:

Symptoms: excessive peripheral vasodilation, pronounced and prolonged lowering of blood pressure, tachycardia. Treatment: gastric lavage, the appointment of activated charcoal, giving the patient a horizontal position with raised legs, monitoring heart and lung performance, control of bcc and diuresis; symptomatic and maintenance therapy, intravenous fluids, calcium gluconate, dopamine, phenylephrine. Hemodialysis is not effective.

Interaction:

β-Adrenoblockers - development of excessive hypotension, rarely - congestive heart failure. Antihypertensive drugs - strengthening the hypotensive effect.

Antifungal agents (azoles) - inhibition of the metabolism of amlodipine.

Rifampicin is an increase in the metabolism of amlodipine.

Special instructions:

Monitoring of blood pressure, heart rate, ECG, liver and kidney function.

The blocker of slow calcium channels dihydropyridine series of long-acting. Racemic mixture. R-amlodipine is more active. Reducing OPSS and blood pressure, reflexively activates the sympathetic nervous system.

In monotherapy, it is effective for reducing SBP in hypertension (85 studies, including 13 293 participants, 11 studies included in the final meta-analysis).

The hypotensive effect of amlodipine at a dose of 5 mg / day is equivalent to the effect of nifedipine (30 mg / day), felodipine (5 mg / day), captopril (2 times a day), irbesartan (150 mg).

The hypotensive effect of amlodipine at a dose of 2.5-10 mg / day is equivalent to the effect of atenolol (50-100 mg / day), candesartan (8-16 mg), hydrochlorothiazide (25-100 mg / day). Amlodipine in a dose of 10 mg / day is comparable in effectiveness with a combination valsartan + hydrochlorothiazide (160 mg + 12.5 mg) and nitrendipine + enalapril (20 mg + 10 mg).

According to ambulatory 24-hour blood pressure monitoring, after 8 weeks of therapy amlodipine in a dose of 5-10 mg on an antihypertensive effect surpasses felodipine in a dose of 5-10 mg (retard-form).

Amlodipine in a dose of 5 mg / day is superior nifedipine in a dose of 40 mg / day for antianginal activity and safer for the number of side effects in patients with stable angina pectoris

Instructions

Amlodipine (Amlodipinum)