Amlodipine Prana tablets 10mg, No. 30

• 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).

For adults, when taken orally, the initial dose is 5 mg 1 time / day. The dose can be increased if necessary.

Maximum dose: for oral administration - 10 mg / day.

Active ingredient: amlodipine - 10 mg

• 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.

pharmachologic effect

Class II selective 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 the systemic vascular resistance, reflex tachycardia does not occur in this case. 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 dilatation of large-caliber coronary arteries and coronary arterioles of both intact and ischemic myocardium. This ensures the supply of oxygen to the myocardium during spasms of the coronary arteries.

Pharmacokinetics

When ingested, it is absorbed from the gastrointestinal tract slowly and almost completely, Cmax in blood plasma is reached within 6-9 hours. Protein binding is 95-98%. Undergoes minimal metabolism during the first passage through the liver and a slow but significant hepatic metabolism with the formation of metabolites with little pharmacological activity.

T1 / 2 on average is 35 hours and with arterial hypertension can increase on average up to 48 hours, in elderly patients - up to 65 hours and with impaired liver function - up to 60 hours. It is excreted mainly in the form of metabolites: 59-62% - by the kidneys , 20-25% - through the intestines.

Indications of the active substances of the drug Amlodipine

• 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).

Side effect

From the side of 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 side of the central nervous system and peripheral nervous system: headache, fatigue, drowsiness, dizziness; with prolonged use - paresthesia.

Allergic reactions: skin rash, itching.

Others: with prolonged use - pain in the limbs.

Contraindications for use

• 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.

Application during pregnancy and lactation

The safety of using amlodipine during pregnancy has not been established, therefore, use is possible only when the intended 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 slow 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 question of stopping breastfeeding should be resolved.

Application for violations of liver function

Use with caution for violations of liver function.

Application for impaired renal function

Use with caution in case of impaired renal function.

Application in children

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

Use in elderly patients

Elderly patients do not need dose reduction.

special instructions

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

Against the background of the use of amlodipine in patients with chronic heart failure (class III and IV according to the NYHA classification) of non-ischemic genesis, there was an increase in the incidence of pulmonary edema, despite the absence of signs of worsening heart failure.

In elderly patients, T1 / 2 may increase and amlodipine clearance may decrease. Dose changes are not required, but more careful monitoring of patients in this category is necessary.

The efficacy and safety of the use of amlodipine in hypertensive crisis has not been established.

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

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

Drug interactions

It is possible to enhance the antianginal and antihypertensive action 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 action when used together with alpha1-blockers, neuroleptics.

Although in the study of amlodipine, a negative inotropic effect was usually not observed, nevertheless, some slow calcium channel blockers can increase the severity of the negative inotropic effect of antiarrhythmic drugs that cause prolongation of the QT interval (for example, 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 (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.

Antipsychotics and isoflurane enhance the antihypertensive effect of dihydropyridine derivatives. With the simultaneous use of drugs for inhalation anesthesia, an increase in the hypotensive effect is possible.

With the simultaneous use of amiodarone, an increase in the antihypertensive effect is possible.

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

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 a 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 the antihypertensive effect is possible.

Calcium supplements can reduce the effect of slow calcium channel blockers.

With the simultaneous use of diltiazem (an inhibitor of the isoenzyme CYP3A4) 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, 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 (increase in AUC by 22%). Although the clinical significance of these effects is not fully understood, they may be more pronounced in older patients. Potent inhibitors of the CYP3A4 isoenzyme (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 are no data on the effect of inducers of the CYP3A4 isoenzyme on the pharmacokinetics of amlodipine. Blood pressure should be carefully monitored while the use of amlodipine and inducers of the isoenzyme CYP3A4.

Storage conditions

In a dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Shelf life

4 years. Do not use after the expiration date.

Vacation conditions

Dispensed by prescription.