Felodipine - instructions for use, dose, side effects, contraindications

Selective L-type calcium channel blocker. Has antianginal and hypotensive effect. Prevents the entry of extracellular calcium into cardiomyocytes and muscle cells of the coronary and peripheral arteries. In high doses, it inhibits the release of calcium ions from intracellular stores. Does not affect the tone of the veins.

Strengthens the coronary blood flow, improving the blood supply of ischemic zones of the myocardium, does not cause a "robbery syndrome". Expands peripheral arteries, reduces overall peripheral resistance, postnagruzku and the need for myocardium in oxygen. Does not affect the drivers of rhythm: sinoatrial and atrioventricular nodes. Has a weak antiarrhythmic effect.

It enhances kidney blood flow, causes a moderate natriuresis.

Reflex activation of the sympathoadrenal system overlaps the negative chrono-,dromo- and inotropic action due to an increase in heart rate in response to peripheral vasodilation.

Pharmacokinetics:

After oral administration, an empty stomach is absorbed in the gastrointestinal tract up to 15-20%. The maximum concentration in the blood plasma is achieved after 2.5-5 hours. The connection with plasma proteins is up to 99%. Penetrates through blood-brain and placental barriers, it is found in breast milk. Metabolized in the liver to inactive metabolites.

Therapeutic effect develops 2 hours after taking and continues for 24 hours.

The half-life is 25 hours. Elimination by the kidneys in 70%, in 30% - with feces in the form of inactive metabolites.

Indications:It is used for the treatment of angina pectoris, arterial hypertension. Used as a symptomatic therapy for Raynaud's syndrome.

ICD-10

IX.I70-I79.I73.0 Raynaud's syndrome

IX.I10-I15.I10 Essential [primary] hypertension

IX.I20-I25.I20 Angina pectoris [angina pectoris]

Contraindications:Acute myocardial infarction, unstable angina, aortic stenosis, aortic hypotension, individual intolerance, children under 18 years.

Carefully:Stenosis of the mitral valve, acute disorders of cerebral circulation, renal and hepatic insufficiency.

Pregnancy and lactation:

Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

Dosing and Administration:Inside the morning at the same time, regardless of food intake, 5-10 mg once a day. If necessary, the dose is doubled - up to 20 mg per day.

The highest daily dose: 20 mg.

The highest single dose: 20 mg.

Side effects:

Central and peripheral nervous system: dizziness, headache, with prolonged use - paresthesia of the extremities, depression.

The cardiovascular system: possible exacerbation of angina in the first days of taking the drug, flushing of the blood to the skin of the face, tachycardia.

Musculoskeletal system: arthralgia, myalgia, convulsions of the upper and lower extremities.

Dermatological reactions: rashes, itching, photosensitivity reactions.

Digestive system: nausea, gingival hyperplasia.

urinary system: rarely - polyuria.

Reproductive system: sexual dysfunction, impotence.

Allergic reactions.

Overdose:

Headache, arrhythmia.In severe cases - loss of consciousness, coma.

Treatment is symptomatic. Antidotes are calcium preparations. Hemodialysis is ineffective, plasmapheresis is recommended.

Interaction:

Incompatible with alcohol. The intake of grapefruit juice slows the absorption of the drug.

With the simultaneous use of the drug with antihypertensive drugs, as well as with inhalational anesthetics, tricyclic antidepressants, nitrates, cimetidine, diuretics, the hypotensive effect intensifies.

Incompatible with rifampicin, it accelerates the metabolism of slow calcium channel blockers.

Increases the concentration of indirect anticoagulants in blood plasma.

Special instructions:Stop taking the drug should be gradual.

Before an operative intervention it is necessary to inform the anesthesiologist about taking the drug by the patient.

Instructions

Felodipine (Felodipinum)