Felodipine

When ATH:
C08CA02

Characteristic.

Calcium channel blocker from the group of 1,4-dihydropyridine. Slightly yellow crystalline powder, insoluble in water, readily soluble in dichloromethane and ethanol. Molecular weight 384,26.

Pharmacological action.
Gipotenzivnoe, antianginalnoe, diuretic, natriuretic.

Application.

Arterial hypertension, angina (stable angina, incl. Prinzmetal angina, in unstable form in case of intolerance or ineffectiveness of beta-blockers or nitrates), Raynaud's syndrome.

Contraindications.

Hypersensitivity (incl. to other dihydropyridine derivative), severe hypotension, acute myocardial infarction and during 1 months after myocardial infarction, cardiogenic shock, clinically significant aortic stenosis, decompensated heart failure, pregnancy, lactation.

Restrictions apply.

Unstable angina, strongly marked bradycardia or heart failure, severe liver, Children up to age 18 years (Safety and efficacy have not been determined).

Pregnancy and breast-feeding.

Contraindicated in pregnancy.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

At the time of treatment should stop breastfeeding.

Side effects.

Cardio-vascular system and blood (hematopoiesis, hemostasis): ≥ 1% — tides; 0,1-1% of tachycardia; 0,01-0.1%-swoon.

From the nervous system and sensory organs): ≥ 1% — headache; 0,1-1% of fatigue, weakness, dizziness, paraesthesia; <0,01% - Myalgia.

With the genitourinary system: ≥ 1% of peripheral edema (ankles, stop, goleneй); <0,01% — an increase in the frequency of urination; 0,01-0.1% of sexual disorders, impotence.

From the digestive tract: 0,1-1% of nausea; 0,01-0.1% of vomiting; <0,01% — giperplazia gums, elevated liver enzymes.

On the part of the musculoskeletal system: 0,01-0.1%, arthralgia.

For the skin: 0,1-1% skin rashes, itch; <0,01% - Photosensitivity.

Allergic reactions: 0,01-0.1% of urticaria; <0,01% -fever, angioedema.

Other: 0,01-0.1% of gynecomastia (after long-term therapy in elderly patients).

Cooperation.

Antihypertensive effect of felodipine strengthen other antihypertensives, incl. beta-blockers, verapamil, diuretics and alcohol. Cmax felodipine in the blood increase the inhibitors of cytochrome P450: cimetidine (on 50%), Erythromycin, some flavonoids, present in grapefruit juice; lower-inductors mikrosomaionah enzymes (phenytoin, Carbamazepine, rifampicin, barbiturates). Release ad.felodipin increases the concentration of Digoxin in plasma.

Overdose.

Symptoms: severe hypotension, bradycardia.

Treatment: simptomaticheskaya therapy. When expressed arterial hypotension patient attach horizontal position with pripodnatami feet, If you want to increase the volume of plasma (a glucose solution, sodium chloride or dextran), appoint adrenomimetiki favouring effect on Alpha1-adrenoreceptory; When bradycardia with atropine used (0,5-1 mg in/in).

Dosing and Administration.

Inside, without chewing, drinking water, 1 once a day (morning). Dosage is strictly individually. When hypertension: the initial dose - 5 mg (for elderly patients and in violation of the liver 2,5 mg), If necessary, adjust the dose, usually supporting dose is 5-10 mg. Angina: the initial dose - 5 mg, if necessary - up 10 mg. The maximum daily dose - 20 mg.

Precautions.

Be wary appointed in congestive heart failure, especially in combination with beta-adrenoblokatorami. In patients with angina pectoris in rare cases may develop arterial expressed hypotension, resulting in deterioration of the blood supply to the myocardium. There are currently no data on the appropriateness of drug for secondary prevention of myocardial infarction. If any of the liver needed correction doses. Patients, who during treatment felodipinom there is weakness and dizziness, should abandon driving and work, which requires high concentration of attention.

Cooperation

Active substanceDescription of interaction
AkarʙozaFMR: antagonizm. Amid felodipina weakened the effect; with a joint appointment is necessary to monitor the concentration of glucose in the blood.
VerapamilFMR: synergism. Strengthens (mutually) hypotensive effect.
GlipizideFMR: antagonizm. Amid felodipina weakened the effect; joint application requires monitoring of blood glucose levels.
DigoxinFKV. Against the backdrop of increased felodipina (at 20-40%) The plasma concentration.
DoxorubicinFMR. Against the background of an increased risk of breaches felodipina of cardiac activity.
CarbamazepineFKV. FMR. Accelerates biotransformation, lowers concentration in the blood and reduces the effect of.
PrymydonFKV. FMR. Accelerates biotransformation, reduces the effect of.
PropranololFKV. FMR. Strengthens (mutually) hypotensive effect. Against the backdrop of increased bioavailability felodipina.
PhenytoinFKV. FMR. Accelerates biotransformation, lowers concentration in the blood and reduces the effect of.
PhenobarbitalFKV. FMR. Accelerates biotransformation, lowers concentration in the blood and reduces the effect of.
ErythromycinFKV. Oppressing biotransformatia and increases plasma concentration.
EthanolFMR: synergism. Strengthens (mutually) effect; at the time of treatment should abandon admission alcohol.

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