FELODIP (FELODIP)

FELODIPINUM C08C A02

Teva

IVAX Pharmaceuticals

STRUCTURE AND PACKAGING:

tab. pro-longum. deyst., p/o of 2.5 mg, No. 30, No. 100

Felodipin

2.5 mg

Other ingredients: lactose, cellulose microcrystalline, propylene glycol.

No. UA/4378/01/01 from 13.04.2006 to 13.04.2011

tab. pro-longum. deyst., p/o of 5 mg, No. 30, No. 100

Felodipin

5 mg

Other ingredients: lactose, cellulose microcrystalline, propylene glycol.

No. UA/4378/01/02 from 13.04.2006 to 13.04.2011

tab. pro-longum. deyst., p/o of 10 mg, No. 30, No. 100

Felodipin

10 mg

Other ingredients: lactose, cellulose microcrystalline, propylene glycol.

No. UA/4378/01/03 from 13.04.2006 to 13.04.2011

PHARMACOLOGICAL PROPERTIES:

Pharmacodynamics. Felodip — derivative dihydropyridine, a selection blocker of calcium channels of L-type. Has high affinity to cells of unstriated muscles of peripheral arterioles, coronary arteries. Felodip expands arterioles, reduces OPSS and the ABP. In therapeutic doses practically does not affect contractility of a myocardium. Felodip has anti-anginal effect thanks to decrease in vascular resistance of coronary vessels, improvement of coronary circulation and supply of a myocardium with oxygen and also reduces an afterload on heart that leads to decrease in need of a myocardium for oxygen.
Felodip improves shipping of physical activities and reduces the frequency of emergence of attacks at patients with stable stenocardia, has anti-ischemic effect in vasospastic stenocardia.
Primary hemodynamic action of Felodip — decrease in the general peripheral vascular resistance thanks to what the ABP decreases. This action depends on a dose. As a rule, decrease in the ABP is noted in 2 h after single dose and not less than 24 Parts proceed, the ratio of T/R (plateau/peak) reaches size much over 50%. There is a positive ratio between concentration of medicament in blood plasma, the level of decrease in OPSS and decrease in the ABP.
Felodip has insignificant natriuretic and diuretic effect as reduces a tubular reabsorption of sodium. Felodip does not influence daily discharge of potassium. At patients with reduced function of kidneys in the course of treatment by Felodip the speed of glomerular filtration can increase. Felodip patients after transplantation of kidneys well transfer.
Drug does not affect concentration of glucose in blood and a lipidic profile.
Pharmacokinetics. Felodip is completely soaked up in a GIT. The bioavailability is about 15% and does not depend on the accepted dose (effect of primary passing through a liver). 99% of Felodip contacts blood plasma proteins, mainly albumine. Thanks to features of a dosage form the prolonged release of a felodipin extends a phase of absorption and provides its uniform concentration in blood plasma for 24 h. Drug gets through GEB and a placental barrier, into breast milk. Felodipin is completely metabolized in a liver, all his metabolites are inactive. Elimination half-life of a felodipin makes 25 h. At long use of cumulation of active ingredient does not occur.
At patients of advanced age and in an abnormal liver function plasmatic concentration of a felodipin is higher, than at patients of young age. Felodip's pharmacokinetics does not change at patients with a renal failure including when carrying out a hemodialysis. About 70% of the accepted dose of medicament are removed with urine, and 30% — with a stake in the form of metabolites. In not changed view with urine 0.5% of the accepted dose are removed.

INDICATION:

AG, an ischemic heart disease — stenocardia (stable, vasospastic).

USE:

AG by
Dose is determined individually (including at elderly people). The initial dose usually makes 5 mg of 1 times a day. If necessary the dose can be raised or added other antihypertensive drug. The maintenance dose usually makes 5–10 mg of 1 times a day. For definition of an individual dose it is the best of all to use tablets on 2.5 mg. For use for elderly people the initial dose makes 2.5 mg/days
Stable stenocardia. Treatment begin with
with a dose 5 mg of 1 times a day, if necessary the dose can be raised to 10 mg of 1 times a day. The maximum daily dose — 20 mg in 1 reception.
to Patients with heavy abnormal liver functions a therapeutic dose needs to be lowered (the recommended initial dose — 2.5 mg/days). At persons with a renal failure of change of pharmacokinetics are insignificant therefore dose adjustment of medicament is not required. it is better for
to take the Drug in the morning to food or after a light breakfast. The tablets Felodipa cannot be chewed, divided or crushed.
Experience of use of Felodip in pediatrics is absent.

CONTRAINDICATION:

period of pregnancy and feeding by a breast, age up to 18 years. Allergic reaction on felodipin or other dihydropyridines (probability of emergence of cross-reaction).
Clinically apparent aortal stenosis; dekompensirovanny heart failure, an acute myocardial infarction or the period lasting 1 month after a myocardial infarction; profound arterial hypotension, cardiogenic shock, unstable stenocardia.

SIDE EFFECTS:

to

it is similar to other antagonists of calcium, felodipin can cause hyperaemia of the person, a headache, heartbeat, dizziness, increased fatigue. These reactions temporary and more often arise in an initiation of treatment or at increase in a dose. Emergence depending on a dose of hypostases in the anklebones which are a consequence of a precapillary vazodilatation is possible.
At patients with inflammation of gums or periodontitis is possible slight hypostasis of gums; it can be prevented at respect for hygiene of an oral cavity. As well as at use of other dihydropyridines, strengthening of manifestations of stenocardia, generally in an initiation of treatment is in some cases noted.
Cardiovascular system: tachycardia, heart consciousness, it is rare — a syncope, peripheral hypostases, hyperaemia of the person.
Central and peripheral nervous system: a headache, dizziness, it is rare — paresthesias.
a GIT: nausea, an abdominal pain, in isolated cases — a hyperplasia, inflammation of gums.
Liver: in isolated cases note increase in level of hepatic transaminases.
Musculoskeletal system: it is rare — joint and muscles pain.
Allergic reactions: hyperaemia of the person, skin rash, itching; seldom — a small tortoiseshell; in isolated cases — a photosensitization, a vasculitis.
Urinary system: in isolated cases — a pollakiuria. Other
: it is rare — fatigue, sexual disturbances, impotence; in isolated cases — reactions of hypersensitivity, for example angioneurotic shock, fervescence.

SPECIAL INSTRUCTIONS:

during treatment by Felodip should abstain from occupations potentially dangerous activity demanding concentration of attention and speed of psychomotor reactions. Patients with stenocardia need to take into account that medicament can cause arterial hypotension that can cause emergence or strengthening of ischemia of a myocardium.
In an abnormal liver function is necessary carrying out dose adjustment of drug.
Felodip does not affect concentration of glucose in blood plasma and on a lipidic profile.
Felodip should not be accepted combined with grapefruit juice because the last contains the flavonoid increasing concentration of a felodipin in blood serum.
Felodip is effective and is well transferred by patients irrespective of gender and age, persons with OH, other obstructive pulmonary diseases, with a renal failure, sick with diabetes, gout, a lipidemia, with Reynaud's syndrome, after transplantation of lungs.
With care appoint Felodip, especially in combination with blockers of β-adrenoceptors, the patient with the profound heart failure.

INTERACTION:

hypotensive action of Felodip are strengthened by other antihypertensive medicaments (blockers of β-adrenoceptors, APF inhibitors, diuretics), tricyclic antidepressants, alcohol. At Felodip's use, blockers of β-adrenoceptors and organic nitrates the anti-anginal effect of these medicaments is summarized.
At simultaneous use with Felodip of NPVP antihypertensive action of Felodip does not decrease.
Inhibitors of microsomal enzymes (Cimetidinum, erythromycin, ranitidine, ketokonazol, itrakonazol, ritonavir, sakvinavir, quinidine) increase concentration of a felodipin in blood plasma therefore the appointed Felodip's dose has to be reduced at simultaneous use with this group of drugs.
Inductors of microsomal enzymes (for example Phenytoinum, carbamazepine, rifampicin and barbiturates) can reduce concentration of a felodipin in blood plasma therefore Felodip's dose should be korrigirovat at the combined use of these drugs. At simultaneous use of Felodip with digoxin the concentration of the last increases, but change of a dose of Felodip is not required. Considerable linking of a felodipin with proteins of blood plasma does not influence a particle of free fractions of other medicinal substance of which considerable linking with proteins of blood plasma is also characteristic (for example warfarin). Grapefruit juice in connection with existence of a flavonoid in it increases level in blood plasma and bioavailability of a felodipin therefore it cannot be applied together with Felodip.

OVERDOSE:

symptoms: arterial hypotension and bradycardia. Treatment: wash out a stomach, apply activated carbon with further accommodation of the patient in chamber of intensive observation to monitoring of function of cardiovascular and respiratory systems. In heavy arterial hypotension it is necessary to place the patient in horizontal position with the lower extremities raised up, to increase blood plasma volume by administration of physiological solution of sodium of chloride, glucose, a dextran; to enter sympathomimetics: Norepinephrinum, phenylephine hydrochloride, dopamine, Dobutaminum and also Calcii chloridum. In bradycardia, AV blockade of the II-III degree, appearance of an asystolia in/in enter Atropini sulfas, Norepinephrinum or Calcii chloridum. If necessary and availability of indications apply an artificial pacemaker.

STORAGE CONDITIONS:

in the dry, protected from light place at a temperature not above 30 °C.

Description of goods is certified by the producer Merkle .

Editorial group Date of creation: 04.01.2023 Date of updating: 06.04.2023 Novgorodsk Yul_ya Boris_vn Author Turumkulov of a _rin of Mikhayl_vn Reviewer

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Description of the medicament Felodip of the tab. of 5 mg No. 30 on this page — the simplified author's version of website apteka911 created on the basis of the instruction(s) for use. Before acquisition or use of medicament you have to consult with the doctor and study the original instruction of the producer (it is applied to each packing of drug).

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Frequently asked questions

How much is Felodip of the tab. of 5 mg No. 30?

Prices on Felodip the tab. of 5 mg No. 30 begin from 263.21 UAH - whether a plate / 10 pieces

Can be given this medicine to children?

It is impossible. It is necessary to consult with your attending physician more in details.

What storage conditions at the tablets Felodip (Merkle)?

It agrees with the instruction storage temperature Felodip (Merkle) makes from 5 °C to 30 °C. To store out of children's reach.

What analogs at the tablets Felodip No. 10?

Analogues with similar therapeutic effect are:

• Felodip of the tab. of 10 mg No. 30
• Felodip of the tab. of 2.5 mg No. 30

What country of origin at Felodip (Merkle)?

Country the producer at Felodip (Merkle) - Germany.

Structure

Active ingredient: felodipin;

1 tablet contains 2.5 mg or 5 mg or 10 mg of a felodipin;

Excipients: lactoses monohydrate, cellulose microcrystalline, gipromelloza, povidone, propyl gallate, silicon dioxide colloidal anhydrous, magnesium stearate;

a tablet Cover on 2.5 mg: gipromelloza, ferrous oxide yellow (E 172), titan dioxide (E 171), talc, propylene glycol;

a tablet Cover on 5 mg and 10 mg: gipromelloza, ferrous oxide red (E 172), ferrous oxide yellow (E 172), titan dioxide (E 171), talc, propylene glycol.

Dosage form

Tablet with the modified release.

Main physical and chemical properties:

• a tablet on 2.5 mg: tablets, coated, yellow color, round, biconvex, with a diameter of 9 mm, with reflection "2.5" on the one hand;
• a tablet on 5 mg: tablets, coated, light pink color, round, biconvex, with a diameter of 9 mm, with reflection "5" on the one hand;
• a tablet on 10 mg: tablets, coated, red-brown color, round, biconvex, with a diameter of 9 mm, with reflection "10" on the one hand.

Pharmacological group

Selection blockers of calcium channels with primary action on vessels. Dihydropyridine derivatives. ATX C08C A02 code.

Pharmacological properties

Pharmacodynamics

Felodipin - a vazoselektivny blocker of calcium channels which reduces arterial blood pressure by reduction of peripheric vascular resistance. In therapeutic doses felodipin selectively influences unstriated muscles of arterioles, has no direct impact on contractility and conductivity of heart. Drug does not influence unstriated muscles of veins both adrenergic vasomotorial mechanisms, and, therefore, reception of a felodipin is not connected with symptoms of orthostatic hypotension. Felodipin has own moderate natriuretic and diuretic effect and, thus, does not cause a liquid delay in an organism.

Felodipin is effective

at various degrees of arterial hypertension. It can be applied as monotherapy or in a combination with other antihypertensive medicaments (for example β-blockers, diuretics or inhibitors of angiotensin-converting enzyme (APF)) to strengthening of antihypertensive action. Felodipin reduces systolic and diastolic arterial blood pressure, and it is possible to appoint it in case of the isolated systolic hypertensia. Felodipin keeps the antihypertensive efficiency also in a combination with non-steroidal anti-inflammatory drugs.

Felodipin shows anti-anginal and antiischemic action thanks to influence on balance between consumption and delivery of a myocardium oxygen. Felodipin reduces resistance of coronary vessels. A blood stream through coronary vessels and saturation of a myocardium oxygen also raise thanks to dilatation of epicardial arteries and arterioles. Felodipin effectively prevents education and development of a spasm of coronary vessels. The decrease in system arterial blood pressure caused felodipiny weakens afterloads on a left ventricle and reduces the need of a myocardium for oxygen.

Felodipin improves shipping of loadings and reduces the frequency of emergence of attacks at patients with a stable angina of exertion. Patients with stable stenocardia felodipin can appoint as monotherapy or in a combination with ß adrenoceptors blockers.

Felodipin is an effective remedy, is well had by adult patients, despite age, race, at patients with associated diseases, such as stagnant heart failure, bronchial asthma and other obstructive diseases of lungs, renal failure, diabetes, gout, lipidemia, Reynaud's phenomenon and also to patients after transplantation of kidneys. Felodipin does not influence glucose level in blood and a lipidic profile.

Place and mechanism of action. Main pharmakodinamichesky line of a felodipin consists highly vascular selectivity. Myogenetic active unstriated muscles of resistive 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 the general peripheric vascular resistance that causes a lowering of arterial pressure. This effect depends on a dose. Generally the lowering of arterial pressure is observed in 2 hours after single dose and at least 24 hours last, and T/R ratio (trough/peak - a ratio of final and peak effect) reaches sizes higher, than 50%. There is a positive ratio between concentration of a felodipin in blood plasma, decrease in peripheric vascular resistance and arterial blood pressure.

Warm effects. In therapeutic doses felodipin does not affect contractility of heart, AV conductivity and the refractory period of an AV node. Hypotensive therapy felodipiny is connected with considerable regression of the existing hypertrophy of a left ventricle.

Renal effects. Felodipin has insignificant natriuretic and diuretic effect as reduces a canalicular reabsorption of sodium. 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 impaired renal function in the course of treatment felodipiny SKF can raise.

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

Effective decrease in high arterial blood pressure is especially useful for

for patients with diabetes.

Clinical performance. In the research HOT (Hypertension Optimal Treatment - "Optimum Treatment of Arterial Hypertension") studied dependence of big cardiovascular events (such as acute myocardial infarction, stroke and lethal outcome because of a cardiovascular disease) from target diastolic arterial blood pressure ≤ 90 mm Hg., ≤ 85 mm Hg. and ≤ 80 mm Hg. and the reached indicator of arterial blood pressure, at the same time felodipin it was applied as basic therapy.

generally 18790 patients with arterial hypertension (diastolic arterial blood pressure of 100-115 mm Hg.) at the age of 50-80 years were under observation within on average 3.8 years (from 3.3 to 4.9). Felodipin was applied as monotherapy or in a combination with β-blockers and/or APF inhibitor and/or diuretics. Decrease in systolic and diastolic arterial blood pressure to 139 and 83 mm Hg was positive takes of a research. in compliance.

In the research STOP-2 (Swedish Trial in Old Patients with Hypertension-2 - "The Swedish Research with Participation of Patients of Advanced Age with Arterial Hypertension-2") in which 6614 patients aged from 70 up to 84 years, blockers of calcium channels participated that are dihydropyridine derivatives (felodipin and isradipin), showed the same effect concerning mortality and incidence owing to cardiovascular pathologies, as well as other widely applied classes of antihypertensive medicines - APF inhibitors, β-blockers and diuretics.

Pharmacokinetics

Absorption. Felodipin is completely soaked up in digestive tract after oral administration of tablets with the modified release. The bioavailability at the person is about 15% and does not depend on the accepted dose in the range of a therapeutic interval. Thanks to features of a dosage form the modified release of a felodipin extends a phase of absorption and provides its uniform concentration in blood plasma within 24 hours. At use of a dosage form with the prolonged action the maximum level of a felodipin in blood plasma (t _max ) is reached in 3-5 hours. In case of simultaneous use of a felodipin with greasy food the absorption speed without change of extent of absorption increases.

Distribution. 99% of a felodipin contact blood plasma proteins, mainly albumine. Distribution volume in an equilibrium state is 10 l/kg.

Metabolism. Felodipin is metabolized in a liver by means of P450 3A4 cytochrome (CYP3A4), all its metabolites are inactive. Felodipin treats medicines with high clearance which averages 1200 ml/min. At prolonged use the significant cumulation of medicine is noted.

concentration of a felodipin in blood plasma is higher than

At patients of advanced age and patients with an abnormal liver function, than at younger patients. The pharmacokinetics of a felodipin does not change at patients with a renal failure, including the patients who are on a hemodialysis.

Conclusion. Elimination half-life of a felodipin makes about 25 hours, and equilibrium concentration is reached in 5 days. At prolonged use of cumulation of active ingredient does not occur. About 70% of a dose of medicament are removed with urine, and the others - with a stake in the form of metabolites. In not changed view with urine less than 0.5% of a dose are removed.

Linearity/nonlinearity. Concentration in blood plasma are directly proportional to a dose within therapeutic range that makes 2.5-10 mg.

Indication

Arterial hypertension.

Preventive treatment of chronic stable stenocardia.

Contraindication

Hypersensitivity to a felodipin and to other dihydropyridines (theoretical risk of cross-responsiveness) or to other components of drug.

Dekompensirovannaya heart failure.

Unstable stenocardia.

Acute myocardial infarction.

Dynamic obstruction of the taking-out path of a left ventricle.

Profound aortal/mitral stenosis.

Interaction with other medicines and other types of interactions

Felodipin is metabolized by

in a liver by means of P450 3A4 cytochrome (CYP3A4). Simultaneous use of substances which interact with the fermental system of P450 3A4 cytochrome can affect at the level of a felodipin in blood plasma.

Fermental interactions.

Drugs which are inhibitors or inductors of an isoenzyme 3A4 of P450 cytochrome can show influence on the level of a felodipin in blood plasma.

Interaction, leading to increase in concentration of a felodipin in blood plasma.

Inhibitors of enzymes, such as Cimetidinum, ranitidine, erythromycin, itrakonazol, ketokonazol, anti-VICH-preparaty / protease inhibitors (for example ritonavir), the quinidine and some flavonoids which are contained in grapefruit juice increase concentration of a felodipin in blood plasma. At use together with powerful CYP3A4 inhibitor itrakonazoly C _max and AUC of a felodipin grew in 8 and 6 times respectively. At simultaneous use with max _{erythromycin C} and AUC of a felodipin increased by 2.5 times, and Cimetidinum raised the C _max and AUC of a felodipin approximately for 55%. It is necessary to avoid combinations of a felodipin with powerful CYP3A4 inhibitors. In case of development of clinically significant by-effects owing to excessive influence of a felodipin that arose at a medicament combination with powerful CYP3A4 inhibitors, it is recommended to modify a dose of a felodipin and/or to stop CYP3A4 inhibitor use.

Interaction, leading to decrease in concentration of a felodipin in blood plasma.

Inductors of enzymes, such as Phenytoinum, carbamazepine, rifampicin, barbiturates, efavirenz, not Virapinum and a St. John's wort (Hypericum perforatum) , can reduce concentration of a felodipin in blood plasma therefore higher doses can be required by the patients taking this medicine. At use of a felodipin together with carbamazepine, Phenytoinum or _{phenobarbital C of max} a felodipina AUC decreased by 82%, and - for 96%. It is necessary to avoid combinations of a felodipin with the powerful inductors CYP3A4.

in case of insufficient clinical performance owing to decrease in concentration of a felodipin at its use in a combination with the powerful inductors CYP3A4 is recommended to modify a dose of a felodipin and/or to stop use of the inductor CYP3A4.

Additional interactions.

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 modify a dose.

Felodipin does not affect plasma concentration of cyclosporine.

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

Antihypertensive medicaments prolong hypotensive action of a felodipin.

Sympathomimetics reduce effect of a felodipin.

Correction of a dose is not required to

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.

Efficiency and safety of use of a felodipin at treatment of hypertensive crisis did not investigate

Feature of use

.