Amlodipine Cardio pills 10mg, 30pcs

Composition

>of 1 tab. contains: Active ingredients: amlodipine bezylate 13.9 mg, mg, which corresponds to the content of amlodipine 10 mg. Excipients: lactose monohydrate, potato starch, hypromellose (hydroxypropylmethylcellulose), talc, magnesium stearate.

Pharmacological action

Pharmaco-therapeutic group: BMKKPHARMACOLOGICAL action is a selective calcium channel blocker of class II. The antihypertensive effect is due to a direct relaxing effect on the smooth muscles of blood vessels. It is assumed that the antianginal effect of amlodipine is associated with its ability to dilate peripheral arterioles; this leads to a decrease in OPSS, and reflex tachycardia does not occur. As a result, the myocardium’s oxygen demand and energy consumption by the heart muscle decreases. 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 oxygen supply to the myocardium during coronary artery spasms. Pharmacokinetics

When taken orally, it is absorbed from the gastrointestinal tract slowly and almost completely, _cmax in blood plasma is reached within 6-9 hours. Binding to proteins is 95-98%. It undergoes minimal metabolism during the” first pass ” through the liver and slow but significant hepatic metabolism with the formation of metabolites with insignificant pharmacological activity.

T_1/2 averages 35 hours and may increase to an average of 48 hours in patients with arterial hypertension, up to 65 hours in elderly patients, and up to 60 hours in patients with impaired liver function. It is mainly excreted in the form of metabolites: 59-62% – by the kidneys,20-25% – through the intestines.

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).

Use during pregnancy and lactation

The safety of using amlodipine during pregnancy has not been established, so it can only be used if the intended benefit to the mother outweighs the potential risk to the fetus.

There are no data indicating the elimination 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 decided.

Contraindications

Severe arterial hypotension (systolic blood pressure less than 90 mm Hg); 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 – hypotension, arrhythmias, shortness of breath.

From the digestive system:  nausea, abdominal pain; rarely gum hyperplasia.

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

Allergic reactions:  skin rash, itching.

Other services:  with prolonged use – pain in the extremities.

Interaction

It is possible to enhance the antianginal and antihypertensive effects of slow calcium channel blockers when combined with thiazide and loop diuretics, ACE inhibitors, beta-blockers and nitrates, as well as to enhance their antihypertensive effect when combined with alpha_-1-blockers, neuroleptics.

Although no negative inotropic effects have usually been observed in studies of amlodipine, however, some slow calcium channel blockers may increase the severity of the negative inotropic effects of antiarrhythmic agents 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 (e. g. ritonavir) increase plasma concentrations of slow calcium channel blockers, including 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 enhance the antihypertensive effect of dihydropyridine derivatives. With the simultaneous use of funds for inhalation anesthesia, it is possible to increase the hypotensive effect.

With simultaneous use of amiodarone, it is possible to increase the antihypertensive effect.

When lithium carbonate is used concomitantly, neurotoxicity may occur (including nausea, vomiting, diarrhea, ataxia, trembling and/or tinnitus).

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

Concomitant use of Indometacin 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 NSAIDs.

With simultaneous use of quinidine, it is possible to increase the antihypertensive effect.

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

When diltiazem (an inhibitor of the CYP3A4 isoenzyme) is co-administered at a dose of 180 mg and amlodipine at a dose of 5 mg in elderly patients (69 to 87 years) with arterial hypertension, the bioavailability of amlodipine increased by 57%. Concomitant use of amlodipine and erythromycin in healthy volunteers (18 to 43 years of age) did not result in significant changes in amlodipine exposure (a 22% increase in AUC). Although the clinical significance of these effects is not fully understood, they may be more pronounced in older patients. Powerful inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole, itraconazole) can lead to an increase in the concentration of amlodipine in blood plasma to a greater extent than diltiazem. Amlodipine and CYP3A4 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 with concomitant use of amlodipine and inducers of the CYP3A4 isoenzyme.

How to take, course of use and dosage

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

Maximum dose:  when taken orally-10 mg / day.

Special instructions

It should be used with caution in patients with hepatic insufficiency, chronic heart failure of non-ischemic etiology of NYHA functional class III-IV, unstable angina, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 month after it), SSR (pronounced tachycardia, bradycardia), arterial hypotension, when used simultaneously with inhibitors or inducers of the CYP3A4 isoenzyme.

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

In elderly patients, T_{1/2 may increase} and clearance of amlodipine may decrease. Dose changes are not required, but more careful monitoring of patients in this category is necessary.

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

Despite the absence of slow calcium channel blockers withdrawal syndrome, discontinuation of treatment with amlodipine should be carried out gradually.

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

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets