Active substanceFelodipineFelodipine
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  • Dosage form: & nbsptablets of prolonged action, film-coated
    Composition:

    1 tablet contains:

    active substance: felodipine 2,500 mg / 5,000 mg / 10,000 mg;

    Excipients: lactose monohydrate 25,200 mg / 23,950 mg / 21,450 mg; microcrystalline cellulose (type Avicel PH 101) 51.750 mg / 50.500 mg / 48,000 mg; hypromellose (Methocel E50LV) 110,000 mg / 110,000 mg / 110,000 mg; povidone (type K-25) 7.350 mg / 7.350 mg / 7.350 mg; propyl gallate 0.067 mg / 0.067 mg / 0.067 mg; microcrystalline cellulose (type Emcocel 90 M) 8,000 mg / 8,000 mg / 8,000 mg; silicon colloidal dioxide 1,300 mg / 1,300 mg / 1,300 mg; magnesium stearate 0.833

    mg / 0.833 mg / 0.833 mg;

    film sheath: hypromellose (type Pharmacoat 606) 6.149 mg / 6.666 mg / 6.572 mg; ferric oxide red oxide (E 172) 0.019 mg / 0.081 mg; ferric iron oxide yellow (E 172) 0.192 mg / 0.007 mg / 0.044 mg; titanium dioxide (E 171) 0.954 mg / 0.435 mg / 0.467 mg; talc 0.930 mg / 1.008 mg / 0.992 mg; propylene glycol 1.074 mg / 1.165 mg / 1.144 mg.

    Description:

    Dosage of 2.5 mg. Round biconvex tablets, covered with a film shell of yellow color, engraved "2.5" on one side, odorless.

    Dosage of 5 mg. Round biconvex tablets, covered with a film shell of light pink color, engraved "5" on one side, odorless.

    Dosage of 10 mg. Round biconvex tablets, covered with a film shell of red-brown color, engraved "10" on one side, odorless.

    At the break of the tablet, the nucleus is visible white or almost white (for all dosages).

    Pharmacotherapeutic group:blocker of "slow" calcium channels
    ATX: & nbsp

    C.08.C.A.02   Felodipine

    Pharmacodynamics:

    Felodipine refers to blockers of "slow" calcium channels dihydropyridine series. Has hypotensive, antianginal action. Reduces blood pressure (BP) by decreasing peripheral vascular resistance. Has a dose-dependent anti-ischemic effect. Reduces the size of myocardial infarction, protects against complications of reperfusion. Virtually does not have a negative inotropic effect, renders minimal action on the conduction system of the heart.

    Pharmacokinetics:

    Suction and distribution

    The delayed release of felodipine from film-coated tablets leads to an elongation of the absorption phase of the preparation and provides a uniform concentrationfelodipine in the blood plasma for 24 hours. Felodipine 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 binds to blood plasma proteins, primarily with albumins.

    Metabolism and excretion

    Felodipine is completely metabolized in the liver, and all its metabolites are inactive. The half-life of felodipine is 25 hours. With prolonged use of cumulation, felodipine does not occur.

    Pharmacokinetics in specific patient groups

    In elderly patients and in cases of impaired liver function, the concentration of felodipine in the blood plasma is higher than in young patients.

    Pharmacokinetic parameters of felodipine do not change in patients with impaired renal function, including hemodialysis. About 70% of the dose taken is excreted by the kidneys, and the rest by the intestine in the form of metabolites. In unchanged form, the kidneys produce less than 0.5% of the dose taken.

    Felodipine penetrates the blood-brain barrier into the placenta and is excreted in breast milk.

    Indications:- Arterial hypertension;

    - fromtamil angina (including angina of Prinzmetal).

    Contraindications:

    - Hypersensitivity to felodipine and other dihydropyridine derivatives;

    - unstable angina;

    acute infarction myocardium and within one month after the transferred myocardial infarction;

    - cardiogenic shock;

    - clinically significant aortic stenosis;

    - Pregnancy;

    - the period of breastfeeding;

    - heart failure in the stage of decompensation;

    - severe arterial hypotension;

    - age under 18 years (effectiveness and safety not established);

    - lactose intolerance, lactase deficiency; glucose-galactose malabsorption.

    Carefully:

    Hepatic and / or renal failure, age over 65 years.

    Dosing and Administration:

    The drug is best taken in the morning inside, before meals or after a light breakfast.

    Tablets, covered with a film shell, can not be bitten, divided or crushed.

    Arterial hypertension

    Adults (including elderly patients):

    The dose is always determined individually.

    Therapy begins with a dose of 5 mg 1 time per day. If necessary, the dose can be increased; usually supporting cases is 5-10 mg once a day.To determine the individual dose, it is best to use tablets with a content of felodipine 2.5 mg.

    Have elderly patients or patients with impaired liver function the recommended initial dose is 2.5 mg once a day.

    Stable angina

    Adults:

    The dose is always determined individually.

    Treatment begins with a dose of 5 mg 1 time per day, if necessary, you can increase the dose to 10 mg once a day. The maximum daily dose is 20 mg once a day. The drug Felodip can be used in combination with beta-blockers, angiotensin-converting enzyme (ACE) inhibitors or diuretics. Combination therapy usually increases the hypotensive effect of the drug. It is necessary to beware of the development of arterial hypotension.

    In patients with severe impairment of liver function, the therapeutic dose should be reduced.

    Have a patients with impaired renal function, the pharmacokinetics of the drug does not change significantly.

    Side effects:

    Just as with the use of other "slow" calcium channel blockers, Felodip can cause reddening of the face, headache, palpitations, dizziness and increased fatigue.These reactions are reversible and most often appear at the beginning of treatment or with an increase in the dose of the drug. Also, depending on the dose, peripheral edema may appear, which are a consequence of precapillary vasodilation. Patients with gingival inflammation or periodontitis may experience mild swelling of the gums. This can be prevented by careful hygiene of the oral cavity

    The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0,01%, but less than 0,1%; very rarely (including isolated cases) - less than 0.01%.

    From the immune system: very rarely - a hypersensitivity reaction, angioedema.

    From the central and peripheral nervous system: often - headache; infrequently - dizziness, paresthesia; rarely - faint.

    From the side of the cardiovascular system: very often peripheral edema; often - "tides"; rarely tachycardia, palpitations.

    From the gastrointestinal tract: infrequently - nausea, pain in the abdomen; rarely vomiting; very rarely - gingival hyperplasia, gingivitis.

    From the liver and biliary tract: very rarely - increased activity of "liver" transaminases.

    From the skin and subcutaneous tissues: infrequent - a rash, itching of the skin; rarely - hives; very rarely - the reaction of photosensitization, leukocytoclasic vasculitis.

    From the musculoskeletal system and connective tissue: rarely - arthralgia, myalgia.

    From the side of the kidneys and urinary tract: very rarely - pollakiuria.

    Other: infrequently - fatigue; rarely - a violation of sexual function.

    Overdose:

    Symptoms: marked decrease in blood pressure, bradycardia.

    Treatment: conduct symptomatic therapy. In the case of a marked decrease in blood pressure, the patient should be given a horizontal position, and the legs should be raised. With the development of bradycardia, intravenous atropine at a dose of 0.5-1 mg is indicated. If this is not enough, it is necessary to increase the volume of blood plasma by infusing a solution of dextrose (glucose), sodium chloride or dextran. Symptomatic drugs with a predominant effect on alpha-adrenoreceptors are used when the above measures are ineffective.

    Interaction:

    Felodipine increases the concentration of digoxin in the blood plasma, however, correction of the dose of felodipine is not required.

    Inhibitors of cytochrome P450 (eg, cimetidine, erythromycin, itraconazole, ketoconazole) slow down the metabolism of felodipine in the liver, increasing the concentration of the drug in the blood plasma.

    Inductors of microsomal enzymes (phenytoin, carbamazepine, rifampicin, barbiturates) reduce the concentration of felodipine in the blood plasma.

    Nonsteroidal anti-inflammatory drugs do not weaken the hypotensive effect of felodipine.

    The high degree of binding of felodipine to proteins does not affect the binding of the free fraction of other drugs (eg, warfarin).

    Felodipine should not be used concomitantly with grapefruit juice due to the flavanoid present in it, which increases the bioavailability of felodipine. Beta- adrenoblockers, verapamil, tricyclic antidepressants and diuretics increase the hypotensive effect of felodipine

    With simultaneous use, an increase in tacrolimus concentration in the blood plasma is possible, which may require correction of the dose of tacrolimus.

    Special instructions:

    The drug Felodip, as well as other vasodilators, can rarely cause significant arterial hypotension, which in a number of predisposed patients can lead to the development of myocardial ischemia.At present, there is no evidence of the advisability of using the drug as a secondary prevention of myocardial infarction.

    The drug Felodip is effective and well tolerated by patients regardless of sex and age, as well as patients with concomitant diseases such as bronchial asthma and other lung diseases; impaired renal function; diabetes; gout; hyperlipidemia; Raynaud's syndrome, and also after lung transplantation.

    The drug Felodip has no effect on the concentration of glucose in the blood and the lipid profile.

    Effect on the ability to drive transp. cf. and fur:

    Patients who have weakness, dizziness during treatment with Felodip, should refrain from performing actions that require a high concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets of prolonged action, film-coated, 2.5 mg, 5 mg and 10 mg.

    Packaging:

    10 tablets in a blister of Al-PVC / PVDC / PE.

    3 or 10 blisters together with instructions for use in a cardboard bundle.

    Storage conditions:

    At a temperature of 10 ° C to 25 ° C in a dark place.

    Keep out of the reach of children.

    Shelf life:

    4 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013365 / 01
    Date of registration:26.08.2010
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp19.09.2015
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