Felotenz retard - instructions for use, dose, side effects, contraindications

Excipients: hypromellose (hydroxypropylmethylcellulose) 52 mg calcium hydrogen phosphate dihydrate, 19 mg, colloidal silica 1 mg, lactose monohydrate 34.8 mg Magnesium stearate 0.7 mg, 5 mg of sodium alginate, Povidone K-30 5 mg;

composition of film shell: Opadry II Yellow 4 mg including 1.6 mg of polyvinyl alcohol, macrogol (polyethylene glycol) 0.8 mg talc 0.6 mg titanium dioxide 0.94 mg yellow iron oxide coloring agent 0.06 mg.

Dosage 5 mg

active substance: felodipine 5 mg;

Excipients: hypromellose (hydroxypropylmethylcellulose) 70 mg Calcium hydrogen phosphate dihydrate 21 mg, colloidal silicon dioxide 1.5 mg Lactose monohydrate 72 mg Magnesium stearate 1 mg, 2 mg of sodium alginate, povidone K-30 7.5 mg;

composition of film shell: Opadrai II yellow 6 mg, including: polyvinyl alcohol 2.4 mg, macrogol (polyethylene glycol) 1.21 mg, talc 0.89 mg, titanium dioxide 1.41 mg, iron oxide dye yellow 0.09 mg.

Dosage of 10 mg

active substance: felodipine 10 mg;

Excipients: hypromellose (hydroxypropylmethylcellulose) 90 mg, calcium hydrophosphate dihydrate 27 mg, silicon dioxide colloid 2.2 mg, lactose monohydrate 126.8 mg, magnesium stearate 1.5 mg, sodium alginate 2.5 mg, povidone K-30 10 mg;

film coating: Opadrai II yellow 9 mg, including: polyvinyl alcohol 3,6 mg, macrogol (polyethylene glycol) 1,818 mg, talc 1,332 mg, titanium dioxide 2,115 mg, iron oxide dye yellow 0.135 mg.

Description:

The tablets covered with a film membrane from light yellow to yellow color, round, biconcave. On the fracture are visible two layers: the shell - from light yellow to yellow, the core - white.

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 antihypertensive, antianginal action. Reduces blood pressure (BP) by reducing the overall peripheral vascular resistance, especially in the arterioles. Has a dose-dependent anti-ischemic effect.Reduces the size of myocardial infarction, protects against complications of reperfusion.

Conductivity and contractility of the smooth muscles of blood vessels are suppressed by affecting the calcium channels of cell membranes. Due to the high selectivity for smooth arteriolar musculature, felodipine in therapeutic doses does not have a negative inotropic effect on the conduction system of the heart.

Felodipine relaxes the smooth muscles of the respiratory tract, and also has little effect on the motility of the gastrointestinal tract.

With prolonged use felodipine does not have a clinically significant effect on the concentration of blood lipids.

In patients with type 2 diabetes mellitus, the use of felodipine for 6 months had no clinically significant effect on metabolic processes.

Felodipine can also be administered to patients with reduced left ventricular function receiving standard therapy, patients with bronchial asthma, diabetes mellitus, gout or hyperglycaemia.

Antihypertensive effect Felodipine is due to a decrease in total peripheral vascular resistance. Felodipine effectively reduces blood pressure in patients with arterial hypertension both in the "lying" position, and in the "sitting" and "standing" positions, at rest and under physical exertion. Because the felodipine has no effect on smooth veins musculature or adrenergic vasomotor control, then orthostatic hypotension does not develop. At the beginning of treatment, as a result of lowering blood pressure on the background of taking felodipine, there may be a temporary reflex increase in the heart rate (heart rate) and cardiac output. An increase in heart rate is prevented by the simultaneous application of beta-blockers with felodipine. The effect of felodipine on AD and the overall peripheral vascular resistance correlates with the plasma concentration of felodipine. At an equilibrium state, the clinical effect is maintained between taking doses and lowering blood pressure within 24 hours.

Treatment with felodipine leads to regression of myocardial hypertrophy of the left ventricle. Felodipine has natriuretic and diuretic effects and does not have a potassium-uretic effect. When taking felodipine, the tubular reabsorption of sodium and water decreases, which explains the absence of salt and fluid retention in the body. Felodipine reduces vascular resistance in the kidneys and enhances renal perfusion. Felodipine does not affect the rate of glomerular filtration and albumin excretion. For the treatment of hypertension felodipine can be used in monotherapy or in combination with other antihypertensive drugs, such as beta-blockers, diuretics or angiotensin-converting enzyme (ACE) inhibitors.

Anti-ischemic effect Felodipine is due to improved blood supply to the myocardium due to dilatation of the coronary vessels. Reducing the load on the heart is provided by reducing the overall peripheral vascular resistance (reducing the load overcome by the heart muscle), which leads to a decrease in myocardial oxygen demand. Felodipine relieves spasm of the coronary vessels.

Pharmacokinetics:

Suction and distribution

The delayed release of felodipine from coated tablets leads to an elongation of the absorption phase of the drug and ensures a uniform concentration of felodipine in the blood plasma for 24 hours. Felodipine almost completely absorbed in the gastrointestinal tract.Systemic bioavailability of felodipine is approximately 15% and does not depend on food intake. However, the rate of absorption, but not its degree, can vary depending on food intake, and the maximum concentration in the blood plasma, therefore, increases by about 65%. The maximum concentration in the blood plasma (C_mOh) is achieved in 3-5 hours. The drug binds to blood plasma proteins by 99%, especially with albumins. The volume of distribution in the equilibrium state is 10 l / kg.

Metabolism and excretion

Felodipine is completely metabolized in the liver, and all its metabolites are inactive. The half-life of felodipine is 25 hours, the plateau phase is reached approximately for 5 days. Do not cumulate even with prolonged admission. The total plasma clearance is 1200 ml / min on average. Reduced clearance in elderly patients and in patients with reduced liver function leads to an increase in the concentration of felodipine in the blood plasma.

Pharmacokinetics in special patents

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 is excreted through the intestines in the form of metabolites. In unchanged form, the kidneys produce less than 0.5% of the dose taken.

Felodipine penetrates the hematoplacental barrier and is excreted in breast milk.

Indications:

- Arterial hypertension (in monotherapy or combination with other antihypertensive drugs, such as beta-blockers, diuretics and ACE inhibitors);

- Stable angina (in monotherapy and in combination with beta-blockers).

Contraindications:

- Hypersensitivity to felodipine and other dihydropyridine derivatives;

- unstable angina;

- acute myocardial infarction and a period of one month after a previous myocardial infarction;

- cardiogenic shock;

- hemodynamically significant aortic and mitral stenosis;

- hypertrophic obstructive cardiomyopathy;

- pregnancy and lactation;

- chronic heart failure in the stage of decompensation;

- severe arterial hypotension;

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

- age to 18 years (efficacy and safety not established).

Carefully:

Dysfunction of the liver, severe renal failure (creatinine clearance less than 30 ml / min), aortic and mitral stenosis, lability of blood pressure and heart failure after myocardial infarction, elderly age.

Pregnancy and lactation:

The preparation of Felotenz® retard is contraindicated in pregnancy and during the period of thoracic feeding.

Currently, there is no data on the use of felodipine in pregnant women. Based on the data obtained from animals on the development of the fetus, felodipine should not be administered during pregnancy. The blockers of "slow" calcium channels can inhibit uterine contraction in premature birth, however, there is insufficient data confirming the increase in the duration of physiological labor. There is a risk of fetal hypoxia in the presence of arterial hypotension in the mother and a decrease in perfusion in the uterus due to redistribution of blood flow and peripheral vasodilation.

Felodipine penetrates into breast milk.When taking felodipine in a nursing mother at therapeutic doses, only a small amount of felodipine penetrates into breast milk. Inadequate experience with the use of felodipine in women during breastfeeding does not exclude the risk of exposure to children who are breastfeeding. If continuation of Felotenz® retard therapy is necessary to achieve a clinical effect, breastfeeding should be discontinued.

Dosing and Administration:

Inside, preferably, with water, fasting or with a small amount of food with a low content of fats and carbohydrates.

Do not divide the tablet, do not crush or chew.

Arterial hypertension

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 the maintenance dose 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.

In elderly patients or patients with impaired liver function, the recommended initial dose is 2.5 mg 1 time per day. The maximum daily dose is 10 mg.

Stable angina

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 drug Felotenz ® retard can be used in combination with beta-blockers, ACE inhibitors or diuretics. Combination therapy usually increases the antihypertensive effect of the drug. It is necessary to beware of the development of arterial hypotension.

In patients with impaired renal function, the pharmacokinetics of the drug are not significantly altered. Caution is necessary in patients with impaired renal function (QC less than 30 ml / min).

Side effects:

As with other "slow" calcium channel blockers, the drug can cause redness 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 oral hygiene.

Classification of WHO (World Health Organization) incidence of side effects: often from ≥1 / 100 to <1/10 of prescriptions (≥1% and <10%); infrequently - from> 1/1000 to <1/100 of prescriptions (≥0.1% and <1%); rarely from ≥1 / 10,000 to <1/1000 appointments (≥0.01% and <0.1%); very rarely - <1/10000 prescriptions (<0.01%).

From the side of the cardiovascular system

often - "tides" of blood to the skin of the face, accompanied by flushing of the face, swelling of the ankles;

infrequent - tachycardia, palpitation, marked decrease in blood pressure, accompanied by reflex tachycardia and worsening of the course of angina pectoris; very rarely - extrasystole, leukocytoclastic vasculitis.

From the nervous system

often - headache;

infrequently - paresthesia, dizziness; rarely - faint.

From the digestive system

infrequently - nausea, abdominal pain;

rarely vomiting;

very rarely - increased activity of "liver" transaminases, gingival hyperplasia, tongue mucosa, and gingivitis.

From the side of the musculoskeletal system

rarely - arthralgia, myalgia.

Allergic reactions

infrequently - skin rash, itching; rarely - hives;

very rarely - angioedema, swelling of the lips or tongue, reaction of photosensitization.

From the urinary system

very rarely - frequent urination.

Proche

infrequently - increased fatigue;

rarely - impotence / sexual dysfunction;

very rarely - fever, hyperglycemia.

Causal link not establishedChest pain, swelling of the face, flu syndrome, marked reduction of blood pressure, myocardial infarction, syncope, angina pectoris, arrhythmia, arrythmia, diarrhea, dryness of the oral mucosa, flatulence, gynecomastia, anemia, arthralgia, back pain, myalgia, pain in upper and lower extremities, depression, insomnia, anxiety, nervousness, drowsiness, irritability, sore throat, shortness of breath, bronchitis, flu, sinusitis, epistaxis, erythema, bruising, leukocytoclastic vasculitis, impaired vision, polyuria, dysuria.

Overdose:

Symptoms

In overdose toxicity symptoms after 12-16 hours after administration of the drug, symptoms may sometimes occur several days after ingestion.

There may be the following symptoms: marked decrease in blood pressure, bradycardia, AV (atrioventricular) blockade I-III degree, ventricular extrasystoles, atrioventricular dissociation, asystole, ventricular fibrillation; headache, dizziness,impaired consciousness (or coma), seizures; shortness of breath, pulmonary edema (non-cardiac), and apnea; in adults, it is possible to develop respiratory distress syndrome; Acidosis, hypokalemia, hyperglycemia, hypocalcemia; redness of the face, hypothermia; nausea, vomiting.

Treatment

Gastric lavage, the appointment of activated carbon, in some cases is effective even at a late stage of intoxication. Specific antidote - calcium preparations. In the case of a marked decrease in blood pressure, the patient should be given a horizontal position, and the legs should be raised. When bradycardia develops, intravenous atropine at a dose of 0.25-0.5 mg is indicated, which should be prescribed before gastric lavage, in connection with the risk of vagal nerve stimulation. ECG monitoring. If necessary, provide airway patency and adequate ventilation of the lungs. The correction of acid-base state and electrolytes of blood serum is shown. In the case of bradycardia and AV blockades are appointed atropine 0.5-1.0 mg iv, if necessary, repeat the introduction, or initially injected isoprenaline 0.05-0.1 μg / kg / min. In acute intoxication at an early stage, it may be necessary to install an artificial pacemaker.Decrease in blood pressure is corrected by intravenous infusion (dextrose solution, 0.9% sodium chloride solution, dextran), adult iv injections of calcium gluconate solution 20-30 ml for 5 minutes, if necessary, repeat the administration in the same dose. If necessary, infusion is administered norepinephrine (epinephrine) or dopamine. In acute intoxication may be prescribed glucagon. When convulsions are prescribed diazepam.

Interaction:

Digoxin: felodipine increases the concentration of digoxin in the blood plasma, however, no change in the dose of felodipine is required.

Inhibitor inhibitors CYP3A4 (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 isoenzyme CYP3A4 (phenytoin, carbamazepine, rifampicin, barbiturates, phenobarbital, preparations of St. John's wort Perforated) reduce AUC (area under the pharmacokinetic curve "concentration-time") of felodipine by 93% and C_max on 82%. You should avoid co-destination.

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

Warfarin: a high degree of binding of felodipine with proteins does not affect the binding of the free fraction of warfarin.

Beta-blockers, verapamil, tricyclic antidepressants and diuretics increase the antihypertensive effect of felodipine.

Antimicrobial preparations of azole series (ketoconazole, itraconazole) when co-appointed AUC Felodipine increases by 8 times, C_mOh - 6 times.

Macrolide antibiotics (erythromycin): when co-appointed AUC and C_mOhFelodipine increases by 2.5 times.

HIV protease inhibitors also increase the concentration of felodipine in the blood. Grapefruit juice enhances AUC and C_mOh felodipine in 2 times, therefore felodipine Do not use simultaneously with grapefruit juice.

Tacrolimus: felodipine increases the concentration of tacrolimus in the blood plasma in a joint application (it is recommended to control the concentration of tacrolimus in the blood plasma and possible correction of the dose).

Cyclosporin increases C_mOh felodipine by 150%, AUC by 60% (the effect of felodipine on the pharmacokinetic parameters of cyclosporine is minimal).

Cimetidine increases C_mOh and AUC felodipine by 55%.

Special instructions:

The preparation of Felotenz® retard should be administered with caution in patients with a tendency to tachycardia and severe left ventricular dysfunction. As well as other vasodilators, in rare cases felodipine can 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.

Felodipine 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, renal dysfunction, diabetes mellitus, gout, hyperlipidemia, Raynaud's syndrome, and also after lung transplantation.

The preparation Felotenz® retard does not affect the concentration of glucose in the blood and the lipid profile. Hyperglycemia is noted only in individual cases.

Violation of the kidney function does not affect the concentration of the drug in the blood plasma, so dose adjustment in patients with impaired renal function is not required.However, when prescribing the drug to patients with renal insufficiency, care must be taken.

It is necessary to observe a thorough hygiene of the oral cavity, in connection with the possible development of gingivitis and gingivitis hyperplasia.

Effect on the ability to drive transp. cf. and fur:Patients who experience weakness and dizziness during treatment with the Felotenz® retard drug should abandon vehicle management and work that requires an increased 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:

For 10, 15 or 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

According to 1, 2, 3, 6 contour cell packs of 10 tablets or 1, 2, 4 contour cell packs of 15 tablets, or 1, 2 circuit packs of 30 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004594/09

Date of registration:09.06.2009

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp18.09.2015

Illustrated instructions

Instructions

Felotenz® retard (Felotenz® retard)