Felodip, 5 mg 30 pcs

Felodipine refers to BCCs of the dihydropyridine series. It has hypotensive and antianginal action. Reduces BP by reducing peripheral vascular resistance. It has a dose-dependent anti-ischemic effect. Reduces the size of myocardial infarction, protects against reperfusion complications. It has practically no negative inotropic effect and has minimal effect on the cardiac conduction system.

Pharmacokinetics

Intake and distribution. Delayed release of felodipine from film-coated tablets leads to prolongation of the phase of drug absorption and ensures uniform concentration of felodipine in blood plasma within 24 hours. Felodipine is almost completely absorbed in the gastrointestinal tract. Bioavailability of the drug does not depend on the dose within the therapeutic interval and is approximately 15%. 99% of felodipine is bound to blood plasma proteins, especially to albumin.

Metabolism and excretion. Felodipine is completely metabolized in the liver, and all its metabolites are inactive.T1/2 of felodipine is 25 h. There is no cumulation of felodipine with prolonged use.

Pharmacokinetics in special groups of patients

Elderly patients. In elderly patients and in cases of impaired liver function, plasma concentrations of felodipine are higher than in younger patients.

Kidney function impairment. Pharmacokinetic parameters of felodipine do not change in patients with impaired renal function, including those under hemodialysis. About 70% of the administered dose is excreted by the kidneys and the rest by the intestine in the form of metabolites. Less than 0.5% of the administered dose is excreted unchanged by the kidneys. Felodipine penetrates through the placenta and is excreted with breast milk.

Indications

Stenocardia, Cardialgia (heart pain), Hypertension (high blood pressure)

Arterial hypertension; stable angina pectoris (including Prinzmetal angina).

Active ingredient

Felodipine

Composition

Active ingredient:

felodipine 5 mg.

Auxiliary substances:

Lactose monohydrate,

Microcrystalline cellulose,

Hypromellose,

povidone,

propyl gallate,

magnesium stearate,

colloidal anhydrous silicon,

iron oxide yellow,

iron oxide red,

titanium dioxide,

talc,

propylene glycol.

How to take, the dosage

The drug is recommended to be taken in the morning before meals or after a light breakfast. Coated tablets must not be crushed, split or crushed.

Application in arterial hypertension: the dosage regimen for adults (including elderly persons) is determined individually. The initial dose is 5 mg 1 time per day (during dose selection it is recommended to use 2.5 mg tablets). If necessary, the dose can be increased, the average dose for maintenance therapy is 5-10 mg/day. Felodip may be used in combination with beta-adrenoblockers, ACE inhibitors or diuretics, which increase the hypotensive effect (caution should be exercised because of increased risk of arterial hypotension).

Perhaps in elderly patients or patients with hepatic impairment: the initial dose is 2.5 mg/day.

Perhaps in patients with severe hepatic impairment: The dose should be reduced.

Application in stable angina pectoris: The dose is determined individually. The initial dose for adults is 5 mg once daily; if necessary, the dose is increased to 10 mg once daily. The maximum daily dose is 20 mg once daily.

Interaction

In concomitant use with Felodip, plasma concentrations of digoxin are increased, but there is no need to change the dosing regimen of Felodip.

Concomitant use with cytochrome P450 inhibitors (including cimetidine, erythromycin, itraconazole, ketoconazole) slows down the metabolism of felodipine in the liver, which leads to increased plasma concentrations.

Concomitant use with inducers of microsomal liver enzymes (including phenytoin, carbamazepine, rifampicin, barbiturates) decreases the plasma concentration of felodipine. NSAIDs do not weaken the hypotensive effect of Felodip.

The high degree of binding of felodipine to plasma proteins does not affect the binding of free fractions of other drugs (including warfarin).

Beta-adrenoblockers, verapamil, tricyclic antidepressants and diuretics increase the hypotensive effect of FELODIP.

Felodip should not be used concomitantly with grapefruit juice because of the flavonoid in it, which increases the bioavailability of felodipine.

Special Instructions

Felodip (like other vasodilators) may in rare cases cause significant arterial hypotension, which in predisposed patients may lead to the development of myocardial ischemia.

There are currently no data on the appropriateness of using the drug as a secondary prevention of myocardial infarction.

Felodip is effective and well tolerated by patients regardless of gender and age, as well as patients with bronchial asthma and other obstructive pulmonary diseases, with impaired renal function, diabetes, with gout, hyperlipidemia, Raynaud’s syndrome, and after lung transplantation.

Felodip has no effect on plasma glucose concentration and lipid profile.

Impact on the ability to drive and operate machinery:

Patients who experience weakness, dizziness during treatment with Felodip should refrain from driving and work requiring increased attention and concentration.

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Contraindications

• high sensitivity to felodipine and other dihydropyridine derivatives;
• unstable angina pectoris;
• acute myocardial infarction within 1 month after myocardial infarction;
• cardiogenic shockacute myocardial infarction and within 1 month of myocardial infarction;
• cardiogenic shock;
• clinically significant aortic stenosis;
• cardiac failure in the decompensated stage.decompensated heart failure;
• severe arterial hypotension;
• lactose intolerance, lactase deficiency;
• glucose-galactose malabsorption;
• pregnancy;
• breastfeeding period;
• age below 18 years (effectiveness and safety not established).

With caution: hepatic and/or renal failure, age over 65 years.

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Side effects

The drug (as with other slow calcium channel blockers) may cause redness of the face, headache, palpitations, dizziness, increased fatigue.

These reactions are reversible and most often occur at the beginning of treatment and when the drug dose is increased. Also, depending on the dose, peripheral edema may occur, which is a consequence of precapillary vasodilation. Patients with gum inflammation or periodontitis may experience mild swelling of the gums. This can be counteracted by good oral hygiene.

In individual cases:

Dermatological reactions: rarely, urticaria, itching; in isolated cases, photosensitization.

Muscular system disorders: in single cases – arthralgia, myalgia.

CNS and peripheral nervous system: headache, dizziness; in single cases – paraesthesia.

Digestive system disorders: rarely – nausea, gum hyperplasia, increased liver enzymes activity.

Cardiovascular system: rare – palpitations, tachycardia, peripheral edema.

Others: rarely – fatigue; in single cases – hypersensitivity reactions (including angioedema).

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Overdose

Symptoms: severe arterial hypotension, bradycardia.

Treatment: conduct symptomatic therapy. In severe arterial hypotension the patient should be given a horizontal position with elevated legs. In bradycardia – intravenous injection of atropine in a dose of 0.5-1 mg. If necessary, to increase plasma volume, infusion of glucose solution, sodium chloride or dextran should be carried out. Drugs with a predominant effect on α-adrenoreceptors shall be prescribed if the above measures are ineffective.

Similarities

Felodipine, Plendil, Felodip