Felodipine sustained release pills 5mg, 30pcs

Composition

Active ingredient:  felodipine – 5.00 mg.

Auxiliary substances:  lactose monohydrate (milk sugar) – 93.00 mg; hypromellose-84.00 mg; macrogol stearate-4.00 mg; colloidal silicon dioxide-3.0 mg; magnesium stearate-1.00 mg.

Shell composition:  hypromellose-2.90 mg; macrogol-4000-0.70 mg; titanium dioxide-1.33 mg; iron oxide yellow dye-0.07 mg

Pharmacological action

Pharmacotherapy group

Slow Calcium Channel Blocker

ATX code

C08CA02

Pharmacodynamics :

Felodipine is a slow calcium channel blocker (BMCC) used for the treatment of arterial hypertension and stable angina pectoris.

Felodipine, a dihydropyridine derivative, is a racemic mixture. Felodipine reduces blood pressure (BP) by reducing total peripheral vascular resistance, especially in the arterioles.

The conduction and contractility of vascular smooth muscle is suppressed by affecting the calcium channels of cell membranes.

Due to its high selectivity for smooth muscle arterioles, felodipine in therapeutic doses does not have a negative inotropic effect on the contractility or conduction of the heart.

Felodipine relaxes the smooth muscles of the respiratory tract.

Felodipine has been shown to have little effect on gastrointestinal motility.

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

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 prescribed to patients with reduced left ventricular function receiving standard therapy and patients with bronchial asthma diabetes mellitus gout or hyperlipidemia.

Antihypertensive effect:  a decrease in blood pressure when taking felodipine is due to a decrease in 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 during exercise. Since felodipine has no effect on venous smooth muscle or adrenergic vasomotor control, orthostatic hypotension does not occur.

At the beginning of treatment, a temporary reflex increase in heart rate (HR) and cardiac output may occur as a result of a decrease in blood pressure while taking felodipine. The increase in heart rate is prevented by the simultaneous use of beta-blockers with felodipine.

The effect of felodipine on blood pressure and peripheral vascular resistance correlates with the plasma concentration of felodipine. At steady state, the clinical effect persists between doses and the reduction in blood pressure persists for 24 hours.

Treatment with felodipine leads to regression of left ventricular hypertrophy.

Felodipine has a natriuretic and diuretic effect and does not have a potash 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 increases renal perfusion. Felodipine has no effect on glomerular filtration rate and albumin excretion.

The use of felodipine in combination with angiotensin-converting enzyme (ACE) inhibitors, beta-blockers and, if necessary, diuretics reduces diastolic blood pressure below 90 mm Hg in 93% of patients.

The use of BMCC dihydropyridine derivatives as an initial course of therapy, followed by the addition of beta-blockers if necessary, does not affect the mortality rate from cardiovascular diseases compared to standard therapy with beta-blockers and/or diuretics.

For the treatment of arterial hypertension, Felodipine can be used in monotherapy or in combination with other antihypertensive drugs such as beta – blockers, diuretics or ACE inhibitors.

Anti-ischemic effect:  the use of felodipine leads to an improvement in blood supply to the myocardium due to dilation of coronary vessels. Reducing the load on the heart is provided by reducing peripheral vascular resistance (reducing the load overcome by the heart muscle) this leads to a decrease in the myocardial oxygen demand.

Felodipine relieves spasm of coronary vessels improves contractility and reduces the frequency of angina attacks in patients with stable angina pectoris. At the beginning of therapy, there may be a temporary increase in heart rate, which is stopped by the appointment of beta-blockers. The effect occurs in 2 hours and lasts for 24 hours. For the treatment of stable angina, felodipine can be used in combination with beta-blockers or as monotherapy.

Pharmacokinetics:

The systemic bioavailability of felodipine is approximately 15% and does not depend on the time of food intake. However, the rate of absorption, but not its degree, may vary depending on the time of food intake, and the maximum concentration in blood plasma is thus increased by about 65%.

The maximum concentration in blood plasma is reached in 3-5 hours. The drug binds to plasma proteins by 99%. The volume of distribution in the equilibrium state is 10 l/kg.

The elimination half-life is approximately 25 h. The plateau phase is reached within about 5 days. It does not accumulate even with prolonged use. The average total plasma clearance is 1200 ml/min.

Reduced clearance in elderly patients and in patients with reduced liver function leads to an increase in the concentration of felodipine in blood plasma. However, the age-related trait only partially explains individual changes in the plasma concentration of felodipine.

Felodipine is metabolized in the liver by the CYP3A4 isoenzyme. All identified metabolites do not have a vasodilating effect (hemodynamic activity).

About 70% of the dose taken is excreted in the form of metabolites with the kidneys, the rest-through the intestines. Less than 05% are excreted unchanged by the kidneys.

With impaired renal function, the plasma concentration of felodipine does not change, but accumulation of inactive metabolites is observed.

Felodipine is not eliminated by hemodialysis.

Indications

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

– Stable angina pectoris (in monotherapy or in combination with beta-blockers).

Use during pregnancy and lactation

Currently, there are insufficient data on the use of felodipine in pregnant women. Based on animal data on fetal malformations, felodipine should not be administered during pregnancy. Slow calcium channel blockers may inhibit uterine contractions in preterm labor, but there is insufficient evidence to support an increase in the duration of physiological labor. Fetal hypoxia may be at risk if the mother has hypotension and uterine perfusion decreases due to blood flow redistribution and peripheral vasodilation.

Felodipine passes into breast milk. When a nursing mother takes felodipine in therapeutic doses, only a small amount of the drug enters the baby’s breast milk. Insufficient experience with the use of felodipine by women during lactation does not exclude the risk of exposure to the drug in children who are breastfed, and therefore it is not recommended to prescribe felodipine to women during lactation. If it is necessary to continue therapy to achieve a clinical effect, discontinuation of breastfeeding should be considered.

Contraindications

-Hypersensitivity to felodipine or other components of the drug.

– Heart failure in the stage of decompensation.

– Acute myocardial infarction.

– Unstable angina pectoris.

– Hemodynamically significant stenosis of the heart valves.

– Hypertrophic obstructive cardiomyopathy.

– Age up to 18 years (efficacy and safety have not been established).

– Lactose intolerance lactase deficiency glucose-galactose malabsorption.

– Pregnancy and lactation (see the section “Use during pregnancy and lactation”).

With caution:

Aortic stenosis mitral stenosis blood pressure lability impaired liver function severe renal failure (creatinine clearance less than 30 ml / min) heart failure after acute myocardial infarction elderly hypotension (in predisposed patients may cause myocardial ischemia) concomitant use with inhibitors or inducers of the CYP3A4 isoenzyme.

Side effects

The most common adverse reactions when taking felodipine include a dose-dependent effect: ankle edema of mild to moderate severity due to the vasodilating properties of felodipine for this reason, approximately 2% of patients refuse to take the drug.

At the beginning of therapy or with an increase in the dose, redness of the face may occur accompanied by” hot flashes ” headache palpitation dizziness and weakness. Usually, these reactions are temporary and go away on their own.

There have been isolated reports of sleep disorders, but no association with felodipine has been established. Hyperplasia of the tongue and gum mucosa after taking felodipine has been reported in patients with severe gingivitis/periodontitis. Careful oral hygiene is recommended to avoid or reduce this side effect.

It is believed that hyperglycemia occurs against the background of taking the BMCC group, however, against the background of taking felodipine, hyperglycemia was observed only in some cases.

The adverse events presented below are listed according to the lesion of organs and organ systems and the frequency of occurrence.

The frequency of occurrence is defined as follows: common (≥1/100); uncommon (≥1/1000 and <1/100); rare (≥1/10000 <1/1000); very rare (

There is no established causal relationship between the following side effects and taking the drug::

Disorders of the blood and lymphatic system: anemia;

Mental disorders: depression insomnia anxiety disorders nervousness drowsiness irritability;

Disorders of the visual organ: visual disorders;

Cardiac disorders: myocardial infarction angina pectoris arrhythmia;

Vascular disorders: arterial hypotension syncope;

Respiratory disorders of the chest and mediastinum:pharyngitis shortness of breath bronchitis flu sinusitis nosebleeds;

Gastrointestinal disorders: diarrhea dry mouth flatulence;

Skin and subcutaneous tissue disorders: erythema bruising leukocytoclastic vasculitis;

Musculoskeletal and connective tissue disorders: arthralgia back pain muscle pain myalgia pain in the upper and lower extremities;

Kidney and urinary tract disorders: polyuria dysuria;

Genital and breast disorders: gynecomastia;

General disorders and disorders at the injection site: chest pain facial swelling flu-like syndrome.

Interaction

Felodipine is a substrate for the CYP3A4 isoenzyme. Drugs that induce or inhibit the CYP3A4 isoenzyme have a significant effect on the concentration of felodipine in blood plasma.

Drugs that induce the cytochrome P 450 isoenzyme system: phenytoin carbamazepine phenobarbital and rifampicin, as well as St. John’s wort preparations, enhance the metabolism of felodipine by inducing the cytochrome P 450 isoenzyme system.

The combined use of phenytoin, carbamazepine, phenobarbital, and rifampicin resulted in a 93% decrease in the area under the concentration-time curve (AUC) and an 82% decrease in the maximum concentration (Cmax) of felodipine. Co-use with inducers of the CYP3A4 isoenzyme should be avoided.

Drugs that inhibit the cytochrome P 450 isoenzyme system: azole antifungal drugs (itraconazole ketoconazole) Macrolide antibiotics (e. g. erythromycin) and HIV protease inhibitors are inhibitors of the CYP3A4 isoenzyme.

When itraconazole is co-administered, the cmax of felodipine increases 8-fold and the AUC increases 6-fold.

When erythromycin is co-administered, the Cmax and AUC of felodipine increases approximately 25-fold.

Co-use of felodipine and CYP3A4 inhibitors should be avoided.

Grapefruit juice inhibits the CYP3A4 isoenzyme. The use of felodipine with grapefruit juice increases the Cmax and AUC of felodipine by approximately 2 times. Simultaneous use should be avoided.

Tacrolimus: Felodipine may cause increased plasma concentrations of tacrolimus. With simultaneous use, it is recommended to monitor the concentration of tacrolimus in the blood serum. It may be necessary to adjust the dose of tacrolimus.

Cyclosporine: when cyclosporine and felodipine are co-administered, the cmax of felodipine increases by 150% and the AUC increases by 60%. However, the effect of felodipine on the pharmacokinetic parameters of cyclosporine is minimal.

Cimetidine: Co-use of cimetidine and felodipine resulted in a 55% increase in the Cmax and AUC of felodipine.

How to take, course of use and dosage

Inside, take in the morning with water. Do not divide, crush or chew the tablet. Tablets can be used on an empty stomach or with a small amount of food low in fat and carbohydrates.

Arterial hypertension

The dose should be selected individually.

The initial dose is 5 mg once a day.

The usual maintenance dose is 5 mg once daily.

If necessary, the dose may be increased or another antihypertensive agent may be added to Felodipine therapy (for example, a beta-blocker diuretic or an ACE inhibitor). Rarely prescribe the drug more than 10 mg per day.

The maximum daily dose is 10 mg / day.

Stable angina pectoris

The dose should be selected individually.

It is necessary to start treatment with a dose of 5 mg once a day, if necessary, increasing the dose to 10 mg once a day.

It can be prescribed together with beta-blockers.

Use in elderly patients

In elderly patients, the recommended starting dose is 25 mg.

Impaired renal function

Impaired renal function does not affect the concentration of the drug in the blood plasma. There is no need to adjust the treatment regimen in patients with impaired renal function, but caution should be exercised when prescribing the drug to patients with severe renal insufficiency (see the sections “With caution” and “Special instructions”).

Impaired liver function

Patients with impaired liver function may experience an increase in the concentration of felodipine in the blood plasma, so a dose of 25 mg is usually sufficient (see the section “Pharmacokinetics”).

Children

Experience with felodipine in children under 18 years of age is limited.

Overdose

Toxicity

10 mg of felodipine in a 2-year-old child caused minor intoxication. 150-200 mg of felodipine in a 17-year-old patient and 250 mg in an adult patient caused mild to moderate intoxication.

Felodipine probably has a more significant effect on peripheral blood circulation than on the heart compared to other drugs in this therapeutic group.

Symptoms

In case of overdose, symptoms of intoxication appear 12-16 hours after taking the drug, severe symptoms may occur several days after taking it. The following symptoms may occur: bradycardia (sometimes tachycardia) marked decrease in blood pressure atrioventricular (AV) block I-III degree ventricular extrasystole atrioventricular dissociation asystole ventricular fibrillation; headache dizziness impaired consciousness (or coma) convulsions; shortness of breath pulmonary edema (not cardiogenic) and apnea; adults may develop respiratory distress syndrome; acidosis hypokalemia hyperglycemia possible hypocalcemia; redness of the face accompanied by ‘hot flashes” hypothermia; nausea and vomiting. In case of overdose, the greatest risk is presented by symptoms from the cardiovascular system.

Treatment

use of activated charcoal if necessary, gastric lavage is sometimes effective even at a late stage of intoxication. A specific antidote is calcium supplements.

Important!

Atropine (025-05 mg iv for adults 10-20 mcg / kg for children) should be administered before gastric lavage (due to the risk of vagus nerve stimulation).

ECG monitoring.

If necessary, ensure airway patency and adequate ventilation of the lungs.

Correction of the acid-base state and blood serum electrolytes is shown.

In the case of bradycardia and AV blockade, atropine 05-1 mg IV is prescribed for adults (20-50 mcg / kg for children), if necessary, repeat the use or initially enter isoprenaline 005-01 mcg/kg/min.

In case of acute intoxication at an early stage, it may be necessary to install an artificial pacemaker.

A pronounced decrease in blood pressure is corrected by intravenous fluid use for adults, a solution of calcium gluconate (9 mg Ca/ml) 20-30 ml is administered intravenously for 5 minutes or as an infusion (3-5 mg Ca / kg for children), if necessary, repeat the use at the same dose. If necessary, epinephrine (epinephrine) or dopamine is infused.

In case of cardiac arrest due to an overdose, resuscitation measures may be required for several hours.

For convulsions, diazepam is prescribed.

Other symptomatic treatment is performed.

Special instructions

Special care is required for the following conditions:: aortic stenosis hepatic impairment severe renal insufficiency (creatinine clearance less than 30 ml / min) heart failure after acute myocardial infarction hypotension which can cause myocardial ischemia in predisposed patients.

The efficacy and safety of felodipine in the treatment of hypertensive crises are poorly understood.

Felodipine can cause a significant decrease in blood pressure, followed by the development of tachycardia. This can lead to myocardial ischemia in predisposed patients.

The combined use of drugs that induce the CYP3A4 isoenzyme leads to a significant decrease in the concentration of felodipine in blood plasma and insufficient therapeutic effect from taking the drug (see the section “Interaction with other drugs”). Co-use of such drugs should be avoided.

Concomitant use of drugs that inhibit the CYP3A4 isoenzyme leads to a significant increase in the concentration of felodipine in blood plasma, and therefore such combinations should be avoided. Avoid taking the drug with grapefruit juice due to a significant increase in the concentration of felodipine in the blood plasma.

Felodipine is metabolized in the liver, so patients with impaired liver function may experience an increase in the concentration of felodipine in the blood plasma. Therefore, felodipine should be used with caution in patients with hepatic impairment.

Influence on the ability to drive vehicles and mechanisms:

When driving vehicles or other mechanisms that require increased attention, you should consider the possibility of developing dizziness and weakness while taking the drug. At the beginning of therapy or during the period of increasing the dose, patients should refrain from engaging in potentially dangerous activities that require concentration of attention and speed of psychomotor reactions.

Storage conditions

Store in a dark place at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Felodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets