Amlodipine, tablets 5 mg 30 pcs

Amlodipine

Indications

Arterial hypertension (as monotherapy or as part of combination therapy).

Stable angina, unstable angina, Prinzmetal angina (as monotherapy or as part of combination therapy).

Pharmacological effect

Pharmacotherapeutic group: BMKK

Pharmacological action

Selective class II calcium channel blocker. The antihypertensive effect is 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 dilate peripheral arterioles; this leads to a decrease in peripheral vascular resistance; 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 cause dilation of large-caliber coronary arteries and coronary arterioles in both intact and ischemic areas of the myocardium. This ensures the supply of oxygen to the myocardium during spasms of the coronary arteries.

Pharmacokinetics

When taken orally, it is absorbed from the gastrointestinal tract slowly and almost completely, Cmax in blood plasma is achieved within 6-9 hours. Protein binding is 95-98%. Subjects to minimal first-pass metabolism through the liver and slow but significant hepatic metabolism to metabolites with negligible pharmacological activity.

T1/2 averages 35 hours and in case of arterial hypertension can increase to an average of 48 hours, in elderly patients – up to 65 hours and in case of liver dysfunction – up to 60 hours. Excreted mainly in the form of metabolites: 59-62% – by the kidneys, 20-25% – through the intestines.

Special instructions

Use with caution in patients with liver failure, chronic heart failure of non-ischemic etiology of functional class III-IV according to the NYHA classification, unstable angina, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after it), SSSS (severe tachycardia, bradycardia), arterial hypotension, with simultaneous use with inhibitors or inducers of the CYP3A4 isoenzyme.

When using amlodipine in patients with chronic heart failure (NYHA class III and IV) of non-ischemic origin, an increase in the incidence of pulmonary edema was observed, despite the absence of signs of worsening heart failure.

In elderly patients, T1/2 may increase and amlodipine clearance may decrease. No dose changes are required, but more careful monitoring of patients in this category is necessary.

The effectiveness and safety of amlodipine in hypertensive crisis has not been established.

Despite the absence of withdrawal syndrome with slow calcium channel blockers, it is advisable to discontinue treatment with amlodipine gradually.

There are no clinical data on the use of amlodipine in pediatrics.

Use for liver dysfunction

Use with caution in case of liver dysfunction.

Use for renal dysfunction

Use with caution in case of impaired renal function.

Use in children

There are no clinical data on the use of amlodipine in pediatrics.

Use in elderly patients

Elderly patients do not require dose reduction.

Active ingredient

Amlodipine

Composition

Active substance: amlodipine

Pregnancy

The safety of amlodipine during pregnancy has not been established, so use is only possible if the expected benefit to the mother outweighs the potential risk to the fetus.

There are no data indicating the excretion of amlodipine in breast milk. However, other calcium channel blockers (dihydropyridine derivatives) are known to be excreted in breast milk. In this regard, if it is necessary to use amlodipine during lactation, the issue of stopping breastfeeding should be decided.

Contraindications

Severe arterial hypotension (systolic blood pressure less than 90 mmHg); left ventricular outflow tract obstruction (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.

Side Effects

From the cardiovascular system: peripheral edema, tachycardia, hyperemia of the skin; when used in high doses – arterial hypotension, arrhythmias, shortness of breath.

From 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 long-term use – pain in the limbs.

Interaction

It is possible to enhance the antianginal and antihypertensive effect of slow calcium channel blockers when used together with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as enhance their antihypertensive effect when used together with alpha1-blockers, antipsychotics.

Although negative inotropic effects have not generally been observed in studies with amlodipine, some calcium channel blockers may enhance the negative inotropic effects of antiarrhythmic drugs known to prolong the QT interval (eg, amiodarone and quinidine).

Simultaneous repeated 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 slow calcium channel blockers, incl. amlodipine.

With the simultaneous use of sympathomimetics and estrogens, a decrease in the antihypertensive effect is possible due to sodium retention in the body.

Neuroleptics and isoflurane enhance the antihypertensive effect of dihydropyridine derivatives. With the simultaneous use of inhalation anesthesia, the hypotensive effect may be enhanced.

With simultaneous use of amiodarone, the antihypertensive effect may be enhanced.

With simultaneous use of lithium carbonate, manifestations of neurotoxicity (including nausea, vomiting, diarrhea, ataxia, tremors and/or tinnitus) are possible.

When used simultaneously, orlistat reduces the antihypertensive effect of amlodipine, which can lead to a significant increase in blood pressure and the development of a hypertensive crisis.

With the simultaneous use of indomethacin and other NSAIDs, the antihypertensive effect of amlodipine may be reduced due to inhibition of prostaglandin synthesis in the kidneys and fluid retention under the influence of NSAIDs.

With simultaneous use of quinidine, the antihypertensive effect may be enhanced.

Calcium supplements may reduce the effect of calcium channel blockers.

With simultaneous use of diltiazem (CYP3A4 isoenzyme inhibitor) at a dose of 180 mg and amlodipine at a dose of 5 mg in elderly patients (69 to 87 years) with arterial hypertension, an increase in the bioavailability of amlodipine by 57% was observed. Concomitant use of amlodipine and erythromycin in healthy volunteers (18 to 43 years of age) does not lead to significant changes in amlodipine exposure (22% increase in AUC). Although the clinical significance of these effects is unclear, they may be more pronounced in older patients. Potent inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole, itraconazole) may increase the plasma concentration of amlodipine to a greater extent than diltiazem. Amlodipine and inhibitors of the CYP3A4 isoenzyme should be used with caution.

There are no data on the effect of inducers of the CYP3A4 isoenzyme on the pharmacokinetics of amlodipine. Blood pressure should be carefully monitored while using amlodipine and inducers of the CYP3A4 isoenzyme.

Manufacturer

Ozon, Russia