Universal reference book for medicines
Product name: FELOTENZ ® RETARD (FELOTENZ RETARD)

Active substance: felodipine

Type: Calcium channel blocker

Manufacturer: КАНОНФАРМА ПРОДАКШН (Russia)
Composition, form of production and packaging
Tablets of prolonged action, 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.
1 tab.

felodipine 2.5 mg

Excipients: hypromellose (hydroxypropylmethylcellulose) - 52 mg, calcium hydrophosphate dihydrate - 19 mg, silicon colloidal dioxide - 1 mg, lactose monohydrate - 34.8 mg, magnesium stearate - 0.7 mg, sodium alginate - 5 mg, povidone K30 - 5 mg.

The composition of the film shell: opadrai II yellow - 4 mg (polyvinyl alcohol - 1.6 mg, macrogol (polyethylene glycol) - 0.8 mg, talc 0.6 mg, titanium dioxide - 0.94 mg, iron oxide, yellow oxide - 0.06 mg).

10 pieces.
- Packings contour mesh (1) - packs cardboard.
10 pieces.
- packings contour mesh (2) - packs cardboard.
10 pieces.
- Packings contour mesh (3) - packs cardboard.
10 pieces.
- packings contour mesh (6) - packs cardboard.
15 pcs.
- Packings contour mesh (1) - packs cardboard.
15 pcs.
- packings contour mesh (2) - packs cardboard.
15 pcs.
- packings contour mesh (4) - packs cardboard.
30 pcs.
- Packings contour mesh (1) - packs cardboard.
30 pcs.
- packings contour mesh (2) - packs cardboard.
Tablets of prolonged action, 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.
1 tab.

felodipine 5 mg

Excipients: hypromellose (hydroxypropylmethylcellulose) - 70 mg, calcium hydrophosphate dihydrate - 21 mg, silicon colloidal dioxide - 1.5 mg, lactose monohydrate - 72 mg, magnesium stearate - 1 mg, sodium alginate - 2 mg, povidone K30 - 7.5 mg.

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

10 pieces.
- Packings contour mesh (1) - packs cardboard.
10 pieces.
- packings contour mesh (2) - packs cardboard.
10 pieces.
- Packings contour mesh (3) - packs cardboard.
10 pieces.
- packings contour mesh (6) - packs cardboard.
15 pcs.
- Packings contour mesh (1) - packs cardboard.
15 pcs.
- packings contour mesh (2) - packs cardboard.
15 pcs.
- packings contour mesh (4) - packs cardboard.
30 pcs.
- Packings contour mesh (1) - packs cardboard.
30 pcs.
- packings contour mesh (2) - packs cardboard.
Tablets of prolonged action, 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.
1 tab.

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 K30 - 10 mg.

The composition of the film shell: opadrai II yellow - 9 mg (polyvinyl alcohol - 3.6 mg, macrogol (polyethylene glycol) - 1.818 mg, talc - 1.332 mg, titanium dioxide - 2.115 mg, iron oxide oxide yellow - 0.135 mg).

10 pieces.
- Packings contour mesh (1) - packs cardboard.
10 pieces.
- packings contour mesh (2) - packs cardboard.
10 pieces.
- Packings contour mesh (3) - packs cardboard.
10 pieces.
- packings contour mesh (6) - packs cardboard.
15 pcs.
- Packings contour mesh (1) - packs cardboard.
15 pcs.
- packings contour mesh (2) - packs cardboard.
15 pcs.
- packings contour mesh (4) - packs cardboard.
30 pcs.
- Packings contour mesh (1) - packs cardboard.
30 pcs.
- packings contour mesh (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

Blocker of slow calcium channels from the group of dihydropyridine derivatives.
Has hypotensive, antianginal action.
Reduces blood pressure by reducing the OPSS, especially in the arterioles.
Felodipine effectively reduces blood pressure in patients with arterial hypertension in both the prone position and in the sitting and standing position, at rest and under physical exertion. Since felodipine has no effect on smooth veins musculature or adrenergic vasomotor control, 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 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 OPSS is correlated with the plasma concentration of felodipine. In the equilibrium state, the clinical effect is maintained between doses and a decrease in blood pressure within 24 hours.
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 muscle arterioles, felodipine in therapeutic doses does not have a negative inotropic effect on the cardiac conduction system.
Felodipine relaxes the smooth muscles of the respiratory tract, and also has an insignificant 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 did not have a 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.
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 has no effect on GFR and albumin excretion. For the treatment of arterial hypertension, felodipine can be used as a monotherapy or in combination with other antihypertensive drugs, such as beta-blockers, diuretics or ACE inhibitors.
The anti-ischemic effect of 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 OPSS (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

Delayed release of felodipine from coated tablets leads to an extended suction phase of the drug and ensures a uniform concentration of felodipine in the blood plasma for 24 hours.

Felodipine is almost completely absorbed from the digestive tract.
Cmax in blood plasma is achieved after 3-5 hours. 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 the intake of food, C max in blood plasma, thus, increases by about 65%.
Felodipine binds to plasma proteins by 99%, especially with albumins.
V d in the equilibrium state is 10 l / kg. It penetrates through the BBB and is excreted in breast milk. Do not cumulate even with prolonged use.
Metabolism and excretion

Felodipine is completely metabolized in the liver, all metabolites are inactive.

T 1/2 of felodipine is 25 h, the plateau phase is reached approximately for 5 days.
About 70% of the dose taken is excreted by the kidneys, the rest is excreted through the intestines in the form of metabolites. In the unchanged form, the kidneys produce less than 0.5% of the dose taken. The total plasma clearance is 1200 ml / min on average.
Pharmacokinetics in specific patient groups

In elderly patients and with violations of liver function, the concentration of felodipine in the blood plasma increases.

Pharmacokinetic parameters of felodipine do not change in patients with impaired renal function, incl.
and during hemodialysis.
INDICATIONS

- arterial hypertension (as a monotherapy or combination with other antihypertensive agents, such as beta-blockers, diuretics, ACE inhibitors);

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

DOSING MODE

The drug is taken orally, preferably on an empty stomach or with a small amount of food with a low content of fats and carbohydrates.
The tablet should be swallowed whole (do not divide, crush or chew), squeezed with water.
The dose is always determined individually.

With arterial hypertension, therapy is started with a dose of 5 mg 1 time / day.
If necessary, the dose can be increased. The maintenance dose is 5-10 mg 1 time / day.To determine the individual dose, it is best to use tablets with the content of felodipine 2.5 mg.
With stable angina, treatment starts with a dose of 5 mg 1 time / day, if necessary, you can increase the dose to 10 mg 1 time / day.

In elderly patients or patients with impaired liver function, the recommended initial dose is 2.5 mg 1 time / day.
The maximum daily dose is 10 mg.
In patients with impaired renal function, the pharmacokinetics of the drug is not significantly altered, but caution should be exercised when QC is less than 30 ml / min.

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.
SIDE EFFECT

As with other slow calcium channel blockers, the drug can cause redness of the face, headache, palpitations, dizziness and 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 appointments (> 1% and <10%);
infrequently - from? 1/1000 to <1/100 of prescriptions (> 0.1% and <1%); rarely - from? 1/10000 to <1/1000 appointments (> 0.01% and <0.1%); very rarely - <1/10000 prescriptions (<0.01%).
From the nervous system: often - headache;
infrequently - paresthesia, dizziness; rarely - faint.
From the cardiovascular system: often - "hot flashes" of blood to the skin of the face, accompanied by flushing of the face, swelling of the ankles;
infrequent - tachycardia, palpitation, excessive decrease in blood pressure, accompanied by reflex tachycardia and worsening of the course of angina pectoris; very rarely - extrasystole, leukocytoclastic vasculitis.
From the digestive system: infrequently - nausea, abdominal pain;
rarely vomiting; very rarely - increased activity of hepatic transaminases, gingival hyperplasia, tongue mucosa, and gingivitis.
From the side of the urinary system: very rarely - frequent urination.

From the musculoskeletal system: rarely - arthralgia, myalgia.

Allergic reactions: infrequent - skin rash, itching;
rarely - hives; very rarely - angioedema, swelling of the lips or tongue, reaction of photosensitization.
Other: infrequently - increased fatigue;
rarely - impotence / sexual dysfunction; very rarely - fever, hyperglycemia.
Causation is not established: chest pain, facial swelling, flu-like syndrome, excessive reduction in blood pressure, myocardial infarction, fainting, angina, arrhythmia, extrasystole, diarrhea, dryness of the oral mucosa, flatulence, gynecomastia, anemia, arthralgia, pain in the back, myalgia, pain in the upper and lower extremities, depression, insomnia, anxiety, nervousness, drowsiness, irritability, pharyngitis, dyspnea, bronchitis, influenza, sinusitis, epistaxis, erythema, bruising, leukocytoclastic vasculitis, spasm
Niya, polyuria, dysuria.
CONTRAINDICATIONS

- 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;

- chronic heart failure in the stage of decompensation;

- severe arterial hypotension;

- Lactase deficiency, lactose intolerance, glucose / galactose malabsorption syndrome;

- Pregnancy;

- lactation period;

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

- hypersensitivity to felodipine and other dihydropyridine derivatives.

Caution should be given to the drug for violations of the liver, severe renal failure (QC less than 30 ml / min), aortic and mitral stenosis, lability of AD and heart failure after myocardial infarction, elderly patients.

PREGNANCY AND LACTATION

The drug Felotenz ® retard is contraindicated in pregnancy and during breastfeeding.

Currently, there is no data on the use of felodipine in pregnant women.
Based on data on the development of fetal abnormalities in animal studies, felodipine should not be given during pregnancy. Blockers of slow calcium channels can inhibit uterine contraction in premature birth, however, there is insufficient data to confirm an 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 is excreted in breast milk.
When a mother-feeding drug is used in therapeutic doses, only a small amount of felodipine is excreted in breast milk. Inadequate experience with the use of felodipine in women during lactation 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.
APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be given to patients with severe renal insufficiency (QC less than 30 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should prescribe the drug to patients with impaired liver function.

APPLICATION FOR CHILDREN

The use of the drug in children and adolescents under the age of 18 is contraindicated.

APPLICATION IN ELDERLY PATIENTS

Caution should be given to elderly patients.

SPECIAL INSTRUCTIONS

The preparation of Felotenz ® retard should be administered with caution to patients with a tendency to tachycardia and severe left ventricular dysfunction.
Like 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 drug Felotenz ® retard does not affect the concentration of glucose in the blood and the lipid profile.
Hyperglycemia is noted only in individual cases.
Impaired renal 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 hyperplasia of the gums and gingivitis.

Impact on the ability to drive vehicles and manage mechanisms

Patients who experience weakness and dizziness during treatment with the preparation Felotenz ® retard should abandon motor vehicle management and work that requires an increased concentration of attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: overdose symptoms of intoxication occur 12-16 hours after taking the drug, sometimes the symptoms can occur and a few days after taking the drug.
There may be an excessive decrease in blood pressure, bradycardia, AV blockade of I-III degree, ventricular extrasystole, 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 charcoal, in some cases is effective even at a late stage of intoxication.
Specific antidote - calcium preparations. With a marked decrease in blood pressure, the patient should be given a horizontal position with a low headboard. With the development of bradycardia, iv administration of atropine at a dose of 0.25-0.5 mg (before gastric lavage, due to the risk of vagus nerve stimulation), ECG monitoring is shown. 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 blockade, atropine is prescribed 0.5-1.0 mg IV, if necessary, repeat the administration, or initially inject 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 of a liquid (dextrose solution, 0.9% sodium chloride solution, dextran), adult iv injections of calcium gluconate solution 20-30 ml for 5 min, if necessary, repeat the administration in the same dose.If necessary, infusion is administered norepinephrine (adrenaline) or dopamine. In acute intoxication, you can assign glucagon. When cramps are prescribed diazepam.
DRUG INTERACTION

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

Inhibitors of the isoenzyme 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 the isoenzyme CYP3A4 (phenytoin, carbamazepine, rifampicin, barbiturates, phenobarbital, preparations of St. John's wort) reduce Felodipine AUC by 93% and C max by 82%.
You should avoid co-destination.
NSAIDs do not weaken the antihypertensive effect of felodipine.

A high degree of binding of felodipine to proteins does not affect the binding of the free fraction of warfarin.

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

When applied simultaneously with antimicrobial azole agents (ketoconazole, itraconazole), AUC of felodipine increases 8-fold, C max -6-fold.

When co-administered with antibiotics from the macrolide group (erythromycin), AUC and C max felodipine increases 2.5-fold.

HIV protease inhibitors also increase the concentration of felodipine in the blood.

Grapefruit juice increases AUC and Cmax felodipine by a factor of 2, so felodipine should not be used simultaneously with grapefruit juice.

Felodipine increases the concentration of tacrolimus in the blood plasma of a joint application (recommended monitoring of tacrolimus concentrations in blood plasma and a possible correction of the dose).
Cyclosporin enhances C max felodipine 150%, AUC by 60% (felodipine impact on the pharmacokinetic parameters of cyclosporine minimum).
Cimetidine increases the C max and AUC of felodipine at 55%.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Rambler's Top100
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!