Felodipine sustained release pills 10mg, 30pcs

Composition

1 tablet contains the Active ingredient: felodipine 10 mg

Pharmacological action

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

Blocking calcium channels and disrupting the flow of calcium ions into the smooth muscle cells of arterial vessels, causes their expansion, reduces OPSS and lowers blood pressure. Reduces afterload on the heart.

Practically does not have a depressing effect on the contractility and conduction of the myocardium, causes moderate reflex tachycardia. Increases coronary blood flow.

Reduces the supply of extracellular calcium to cardiomyocytes and smooth muscle cells of coronary and peripheral arteries; in high doses, 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.

It separates the processes of excitation and contraction in the myocardium mediated by tropomyosin and troponin, and in vascular smooth muscles mediated by calmodulin.

In therapeutic doses, it normalizes the transmembrane calcium flow, which is disturbed in a number of pathological conditions, primarily in arterial hypertension. Reduces blood pressure by vasodilation, reducing OPSS. It does not affect vein tone and adrenergic vasomotor innervation, so it does not cause orthostatic hypotension.

It has a dose-dependent anti-ischemic effect. Increases coronary blood flow, improves blood supply to ischemic areas of the myocardium without the development of the phenomenon of “stealing”, activates the functioning of collaterals, protects against reperfusion complications, slightly increases heart rate. Dilating peripheral arteries reduces afterload.

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

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

The action starts in 2-5 hours and continues for 24 hours. The severity of the effect correlates with the dose and plasma concentration.

Pharmacokinetics

After oral use, felodipine is almost completely absorbed from the gastrointestinal tract and undergoes intensive metabolism during the” first pass ” through the liver. Binding to plasma proteins (mainly albumins) is about 99%.

In small amounts, it penetrates the BBB and placental barrier, and is excreted in breast milk. Felodipine is extensively metabolized in the liver; all its known metabolites do not have pharmacological activity. Metabolism occurs with the participation of isoenzymes CYP3A4, CYP3A5, and CYP3A7.

About 70% is excreted by the kidneys as metabolites and less than 0.5% unchanged; the remainder is excreted through the intestine. T_1/2 in the α-phase is about 4 hours, in the β-phase – about 24 hours.

In elderly patients, as well as in patients with impaired liver function, the concentration of felodipine in the blood is higher than in younger patients.

It does not accumulate even with prolonged use; in chronic renal failure, accumulation of inactive metabolites is observed.

Indications

Arterial hypertension, angina pectoris (when beta-blockers and nitrates are ineffective), Raynaud’s syndrome (as symptomatic therapy).

Use during pregnancy and lactation

It is contraindicated for use during pregnancy (including possible pregnancy).

Use in children

Contraindicated in children under 18 years of age.

Contraindications

Acute myocardial infarction, decompensated chronic heart failure, age up to 18 years, pregnancy, women of childbearing age with a high probability of pregnancy, hypersensitivity to felodipine.

Side effects

From the cardiovascular system:  flushes of blood to the skin of the face, accompanied by facial hyperemia, tachycardia, swelling in the ankle joint (as a result of precapillary vasodilation), syncope, extrasystole, severe arterial hypotension, accompanied by reflex tachycardia and worsening of angina pectoris, leukocytoclastic vasculitis.

From the central nervous system:  headache, dizziness, fatigue, paresthesia.

From the digestive system:  nausea, abdominal pain, vomiting, increased activity of hepatic transaminases, hyperplasia of the gums, tongue mucosa, gingivitis.

Musculoskeletal disorders:  rarely-arthralgia, myalgia.

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

Other services:  impotence / sexual dysfunction, frequent urination, fever, hyperglycemia.

Interaction

When used concomitantly with inhibitors of microsomal liver enzymes, it is possible to increase the concentration of felodipine in blood plasma.

It is possible to reduce the concentration of felodipine in blood plasma due to an increase in the intensity of its metabolism in the liver under the influence of carbamazepine, phenytoin and phenobarbital (which are inducers of microsomal liver enzymes) and accelerate excretion from the body.

When used concomitantly with digoxin, it is possible to increase the concentration of digoxin in blood plasma.

When used concomitantly with itraconazole, ketoconazole slows down the metabolism of felodipine in the liver, which leads to an increase in the concentration of felodipine in blood plasma and an increased risk of side effects.

When used concomitantly with erythromycin, the bioavailability of felodipine increases. There are reports of increased therapeutic and side effects of felodipine in a patient receiving erythromycin.

Increases the bioavailability of propranolol. Concomitant use with beta-blockers increases the risk of developing chronic heart failure.

A decrease in the antihypertensive effect is observed with the simultaneous use of felodipine with NSAIDs, corticosteroids (sodium retention and blockade of prostaglandin synthesis by the kidneys) and estrogens (sodium retention), calcium preparations; an increase in the antihypertensive effect occurs when used simultaneously with inhaled drugs for anesthesia, beta-blockers, alpha-blockers, sympathomimetics and other antihypertensive drugs.

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

How to take, course of use and dosage

Apply inside mainly in the form of dosage forms that provide a constant release of the Active ingredient-5-10 mg 1 time/day, if necessary-20 mg 1 time/day.

The maximum daily dose is 20 mg.

Special instructions

Use with caution in patients with heart failure, lability of blood pressure, renal failure, heart failure after myocardial infarction.

When used in patients with angina pectoris, it should be borne in mind that in rare cases felodipine can cause severe hypotension, which leads to myocardial ischemia.

Active ingredient

Felodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets