Felodipine, 10 mg 30 pcs

A class II selective calcium channel blocker from the group of dihydropyridine derivatives. Like other dihydropyridine derivatives, felodipine has significantly higher affinity for calcium channels of smooth muscle cells of arterial vessels than for calcium channels of cardiomyocytes.

Blocking calcium channels and disrupting the flow of calcium ions into the smooth muscle cells of arterial vessels, causes their dilation, reduces PPS and lowers BP. It reduces the afterload on the heart.

It has practically no inhibitory effect on myocardial contractility and conduction, causes moderately pronounced reflex tachycardia. It increases coronary blood flow.

Decreases intake of extracellular calcium into cardiomyocytes and smooth muscle cells of coronary and peripheral arteries; in high doses it reduces the release of calcium ions from intracellular depots. Reduces the number of functioning channels without affecting the time of their activation, inactivation and recovery.

Disassociates the processes of excitation and contraction in the myocardium mediated by tropomyosin and troponin and in vascular smooth muscle mediated by calmodulin.

In therapeutic doses it normalizes the transmembrane calcium flow disturbed in a number of pathological conditions, especially in arterial hypertension. It reduces BP due to vasodilatation and decreases RPS. It does not affect venous tone and adrenergic vasomotor innervation, therefore it does not cause orthostatic hypotension.

It has a dose-dependent anti-ischemic effect. It increases coronary blood flow, improves blood supply of ischemic zones of myocardium without development of “bypass” phenomenon, activates functioning of collaterals, protects from reperfusion complications, slightly increases HR. By dilating the peripheral arteries, it reduces the afterload.

It has almost no effect on the sinoatrial and AV nodes. Virtually no negative inotropic effect (the reflex increase in heart rate in response to vasodilation masks the negative inotropic effect).

It increases renal blood flow, has a moderate natriuretic and diuretic effect.

The action begins after 2-5 hours and lasts for 24 hours. The severity of the effect correlates with the dose and plasma concentration.

Pharmacokinetics

Indications

Active ingredient

Composition

How to take, the dosage

The oral administration is primarily in dosage forms providing a continuous release of the active substance – 5-10 mg once daily, if necessary – 20 mg once daily.

The maximum daily dose is 20 mg.

Interaction

Concomitant use with inhibitors of microsomal liver enzymes may increase the plasma concentration of felodipine.

Possible decrease in plasma concentration of felodipine due to increased intensity of its metabolism in the liver under the influence of carbamazepine, phenytoin and phenobarbital (which are inducers of liver microsomal enzymes) and accelerated excretion.

Concomitant use with digoxin may increase plasma concentrations of digoxin.

Concomitant use with itraconazole, ketoconazole slows down the metabolism of felodipine in the liver, which leads to increased plasma concentration of felodipine and increased risk of side effects.

Concomitant use with erythromycin increases the bioavailability of felodipine. Increased therapeutic and adverse effects of felodipine have been reported in patients receiving erythromycin.

Induces bioavailability of propranololol. Concomitant use with beta-adrenoblockers increases the risk of chronic heart failure.

Decreased antihypertensive effect is observed with concomitant use of felodipine with NSAIDs, GCS (sodium retention and blockade of prostaglandin synthesis by the kidneys) and estrogens (sodium retention), calcium preparations; antihypertensive effect is enhanced with concomitant use with inhaled anesthetics, beta-adrenoblockers, alpha-adrenoblockers, sympathomimetics and other hypotensive drugs.

Drugs that cause prolongation of the QT interval increase the negative inotropic effect and may increase the risk of significant QT interval prolongation.

Special Instructions

With caution, use in patients with heart failure, BP labile, renal failure, heart failure after myocardial infarction.

When used in patients with angina pectoris, it should be noted that in rare cases felodipine may cause significant arterial hypotension, which leads to myocardial ischemia.

Contraindications

Side effects

Cardiovascular system disorders: skin flushing accompanied by facial hyperemia, tachycardia, swelling of the ankle joint (as a consequence of precapillary vasodilation), syncope, extrasystole, marked arterial hypotension accompanied by reflex tachycardia and worsening of angina pectoris, leukocytoclastic vasculitis.

CNS disorders: headache, dizziness, fatigue, paresthesia.

Digestive system disorders: nausea, abdominal pain, vomiting, increased liver transaminase activity, gum hyperplasia, tongue mucosa, gingivitis.

Muscular system disorders: rare – arthralgia, myalgia.

Allergic reactions: skin rash, itching, urticaria, angioedema of the lips or tongue, photosensitization reaction.

Others: impotence/sexual dysfunction, frequent urination, fever, hyperglycemia.

Pregnancy use

It is contraindicated in pregnancy (including possible).

Persons with children

It is contraindicated under 18 years of age.

Similarities