Felodip of the tab. of 10 mg No. 30

Pharmacological properties

Pharmacodynamics. felodip — a vazoselektivny blocker of calcium channels with primary action on vessels it is similar to dihydropyridine which lowers arterial blood pressure by decrease in peripheric vascular resistance. in therapeutic doses felodipin selectively influences unstriated muscles of arterioles, does not carry out direct influence on contractility of a myocardium and the carrying-out system of heart. medicament does not influence unstriated muscles of veins both adrenergic vasomotorial mechanisms, and, respectively, reception of a felodipin does not cause symptoms of orthostatic hypotension. felodip has insignificant natriuretic and diuretic effect, and respectively, there is no liquid delay in an organism.

at various degrees of AG. It can be used as monotherapy or in a combination with other antihypertensive drugs, for example: blockers of β-adrenoceptors, diuretics or APF inhibitors for increase in antihypertensive action. Felodip reduces systolic and diastolic arterial blood pressure and it is possible to appoint it in case of the isolated systolic hypertensia. Felodip keeps the antihypertensive efficiency also in a combination with NPVP.

Felodip has anti-anginal and antiischemic effect thanks to influence on balance between consumption and saturation of a myocardium oxygen. Felodip reduces the vascular resistance of coronary vessels. The blood stream through coronary vessels and saturation of a myocardium oxygen raises thanks to dilatation of epicardial arteries and arterioles. Felodip effectively prevents education and development of a spasm of coronary vessels. Decrease in the system ABP reduces afterloads on a left ventricle and the need of a myocardium for oxygen.

Felodip improves shipping of loading and reduces the frequency of emergence of attacks at patients with stable stenocardia of loading. Felodip reduces frequency symptomatic and the IBS latent form at patients with a vasospastic form of stenocardia.

Felodip is effective medicament which is well transferred by adult patients regardless of age, race and also persons with associated diseases, such as stagnant heart failure, OH and other obstructive diseases of lungs, a renal failure, diabetes, gout, a lipidemia, Reynaud's phenomenon and also patients after transplantation of kidneys. Felodip does not influence a glycemia and a lipidic profile.

action Mechanism. The main pharmakodinamichesky feature of a felodipin consists in high vascular selectivity. Miogenno active unstriated muscles of resistant arterioles are especially sensitive to action of a felodipin. Felodipin suppresses electric and sokratitelny activity of unstriated muscles of vessels, influencing calcium channels in a cellular membrane.

Hemodynamic effects. Primary hemodynamic effect of a felodipin consists in decrease in OPSS that leads to decrease in the ABP. This effect is dose-dependent. In general decrease in the ABP is noted in 2 h after single dose and not less than 24 Parts last, and T/R ratio (trough/peak — a ratio of final and peak effect) reaches indicators much higher than 50%. There is a positive ratio between concentration of medicament in blood plasma, the level of decrease in peripheric vascular resistance and decrease in the ABP.

Influence on function of heart. In therapeutic doses felodipin does not affect contractility of heart, AV conductivity and the refractory period of an AV node. Felodipin positively influences function of a left ventricle that is confirmed by measurements of fraction of emission and systolic volume at patients with heart failure. Reception of a felodipin is not connected with neurohumoral activation. Possibly, felodipin does not affect lifetime of patients. At patients with AG or stenocardia the use of a felodipin in case of dysfunction of a left ventricle is possible. Hypotensive therapy felodipiny is connected with considerable regression of the existing hypertrophy of a left ventricle.

Influence on function of kidneys. Felodipin has insignificant natriuretic and diuretic effect as reduces a canalicular reabsorption of sodium. The delay of sodium and liquid in an organism is noted in case of intake of other vasoconstrictive drugs. Felodipin does not influence daily removal of potassium or albumine. Vascular resistance of kidneys decreases after reception of a felodipin. The normal glomerular filtration rate (GFR) does not change. At patients with a renal failure in the course of treatment felodipiny SKF can raise.

At the patients accepting cyclosporine after transplantation of kidneys felodipin lowers the arterial blood pressure, improves a blood stream in kidneys and SKF. Felodipin can improve functioning of a transplant at early stages after transplantation.

for patients with diabetes.

Pharmacokinetics. Absorption and distribution. Felodip is completely soaked up in a GIT after oral administration of a tablet with the modified release. The bioavailability is about 15% at people and does not depend on the accepted dose during all therapeutic interval. 99% of a felodipin contact proteins of blood plasma, mainly albumine. Thanks to features of a dosage form the modified release of a felodipin prolongs a phase of absorption and provides its uniform concentration in blood plasma during 24 h

Metabolism and removal. Felodip is generally metabolized in a liver, all his metabolites are inactive. T _½ felodipina makes 24 h. At prolonged use the accumulation of active ingredient does not happen.

At elderly patients and patients with an abnormal liver function, than at patients of young age. The pharmacokinetics of a felodipin does not change at the patients with a renal failure including who are on a hemodialysis. About 70% of a dose of medicament are removed with urine, and 30% — with a stake in the form of metabolites. In not changed view with urine less than 0.5% of a dose are removed.

Indication

Essentsialnaya ag. preventive treatment of chronic stable stenocardia.

Use

Ag. adults (including patients of advanced age): the mode of dosing is defined individually.

with a dose 5 mg of 1 times a day. If necessary the dose can be lowered to 2.5 mg either to raise, or to add other antihypertensive drug. As a rule, the maintenance dose makes 5–10 mg of 1 times a day.

Stenocardia. The dosing mode is always defined individually.

with a dose of 5 mg of 1 times a day. If necessary this dose can be raised to 10 mg of 1 times a day. The maximum dose makes 20 mg/days

At patients with a renal failure of change of pharmacokinetics are insignificant therefore dose adjustment is not required.

to Patients with AG and stenocardia with heavy abnormal liver functions a therapeutic dose of a felodipin needs to be lowered (the recommended dose of 2.5 mg/days).

For elderly people the initial dose in 2.5 mg of 1 times a day can be sufficient.

Route of administration: the medicament is taken in the morning, before food or after a light breakfast. The tablet is not chewed, not divided and not crushed. It is necessary to swallow of tablets whole and to wash down with water.

Contraindication

Allergic reaction on felodipin and other dihydropyridines (theoretical risk of development of cross-responsiveness) or on other components of drug; dekompensirovanny heart failure; unstable stenocardia; sharp myocardial infarction; dynamic obstruction of the taking-out path of a left ventricle. clinically significant aortal stenosis.

Side effects

As well as other blockers of calcium channels, medicament can cause hyperaemia of the person, a headache, heartbeat, dizziness and fatigue. these reactions are temporary and are often shown in an initiation of treatment and/or at increase in a dose. also there can be, depending on a dose, hypostases in anklebones which are a consequence of a precapillary vazodilatation, but not tendency to a liquid delay in an organism. patients with inflammation of gums or with periodontitis can have an abscess of gums. it can be avoided at respect for hygiene of an oral cavity. as well as at use of other dihydropyridines, in rare instances noted deterioration in manifestations of stenocardia, generally in an initiation of treatment.

in clinical trials and during the post-registration period of monitoring of medicine.

from the immune system: hypersensitivity reactions (urticaria and Quincke's disease).

from nervous system: headache, sleep disorder, drowsiness, dizziness, paresthesias, concern, irritability, confusion of consciousness, depression.

from a respiratory system: short wind, nasal bleeding.

from a cardiovascular system: strengthening of manifestations of stenocardia (especially in an initiation of treatment), mainly at patients from a symptomatic ischemic heart disease, a syncope, feeling of the strengthened heartbeat, tachycardia, a myocardial infarction. Peripheral hypostasis (hypostasis degree in anklebones depends on a dose), arterial hypotension, a leykotsitoklastichesky vasculitis.

from a reproductive system: sexual dysfunction.

from an urinary system: frequent urination.

from digestive system: nausea, an ulitis, a hyperplasia of gums, an abdominal pain, vomiting, periodontitis, diarrhea, a constipation, dryness in a mouth.

from function of a liver and a gall bladder: increase in level of liver enzymes, cholestatic hepatitis.

from skin and hypodermic cellulose: hyperaemia, inflows (especially in an initiation of treatment when the high dose raises or entered), rash, an itching, a photosensitization, a Quincke's disease, a multiformny erythema, a knotty erythema.

from a musculoskeletal system and connective tissue: arthralgia, myalgia, tremor.

System disturbances and local reactions: increased fatigue, fervescence.

Special instructions

As well as in a case with other vazodilatator, medicament felodip can cause in rare instances severe hypotension with tachycardia which at sensitive patients can lead to myocardium ischemia.

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to patients with heavy dysfunction of a left ventricle.

Grapefruit juice increases peak plasma concentration and bioavailability of drug, perhaps, because of interaction with flavonoids in fruit juice.

Drug contains lactose therefore to patients with rare hereditary forms of intolerance of a galactose, insufficiency of lactase or at malabsorption of glucose galactose it is impossible to use this drug.

Period of pregnancy and feeding by a breast. Felodipin is contraindicated at pregnancy.

Felodipin can get into breast milk, but it is unknown whether it has negative impact on newborns. However because of limited data on safety of use of medicament for the children who are on breastfeeding, Felodipin it is impossible to use during feeding by a breast.

Children. Drug is not appointed to children.

Interaction

Simultaneous use of the substances interacting with the fermental system of p450 3a4 cytochrome can affect levels of a felodipin in blood plasma.

Inhibitors of enzymes, such as Cimetidinum, ranitidine, erythromycin, itrakonazol, ketokonazol, ritonavir, sakvinavir and quinidine, increase concentration of a felodipin in blood plasma therefore there can be a need for decrease in its dose at simultaneous use with these drugs.

Inductors of enzymes, such as Phenytoinum, carbamazepine, rifampicin, barbiturates and St. John's wort (hypericum perforatum), can reduce concentration of a felodipin in blood plasma therefore, perhaps, use of doses above recommended to the patients taking this medicament will be required.

Felodipin can increase concentration of a takrolimus. In case of simultaneous use of a felodipin and a takrolimus it is necessary to control concentration of a takrolimus in blood plasma and to respectively adjust a dose.

Grapefruit juice increases the level of a felodipin in blood plasma and also its bioavailability because of existence in it of flavonoids therefore it cannot be applied along with felodipiny.

Antihypertensive medicaments prolong hypotensive action of a felodipin.

Sympathomimetics reduce effect of a felodipin.

at simultaneous use of a felodipin with digoxin.

Felodipin does not influence a share of free fractions of other medicaments which are characterized by considerable linking with proteins of blood plasma, for example warfarin.

Overdose

Can cause an excessive peripheral vazodilatation with the profound arterial hypotension which can sometimes be followed by bradycardia.

Treatment. In heavy arterial hypotension the symptomatic treatment is shown. It is necessary to give to the patient horizontal position with raised upside down. In bradycardia enter atropine of 0.5-1 mg. If it is not enough, it is necessary to fill OCK by means of infusion, for example Dextrosums, 0.9% of solution of sodium of chloride, Polyglucinum. It is possible to appoint sympathomimetics with primary action on α ₁ - adrenoceptors.

Storage conditions

At a temperature not above 25 °C.