Felodipine

Brand Canonpharma

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Available since: 2019-09-19

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Clinical Pharmacology

Pharmacotherapeutic group: “slow” calcium channel blocker

ATC code: C08CA02

Pharmacological properties

Pharmacodynamics

Felodipine is a blocker of the “slow” calcium channels of the dihydropyridine series. It has antihypertensive, antianginal effect. Decreases blood pressure (BP) by reducing general peripheral vascular resistance, especially in arterioles. It has a dose-dependent anti-ischemic effect. Reduces the size of myocardial infarction, protects against reperfusion complications. Conductivity and contractility of vascular smooth muscle is suppressed by affecting the calcium channels of the cell membrane. Due to the high selectivity for arteriole smooth muscles, 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, also has a slight effect on the motility of the gastrointestinal tract. With long-term use, felodipine does not have a clinically significant effect on the concentration of blood lipids. In patients with type 2 diabetes mellitus with felodipine administered for 6 months, no clinically significant effect on metabolic processes was observed. Felodipine can also be given to patients with reduced left ventricular function who are receiving standard therapy, patients with asthma, diabetes, gout, or hyperglycemia.

The antihypertensive effect of felodipine is due to a decrease in total peripheral vascular resistance. Felodipine effectively lowers blood pressure in patients with arterial hypertension, both in the “lying” and “sitting” and “standing” positions, at rest and during exercise. Since felodipine has no effect on smooth muscle of the veins or adrenergic vasomotor control, the development of orthostatic hypotension does not occur. At the beginning of treatment, as a result of a decrease in blood pressure in patients receiving felodipine, a temporary reflex increase in heart rate (HR) and cardiac output can be observed. Increase in heart rate prevents the use of beta-blockers simultaneously with felodipine. The effect of felodipine on blood pressure and total peripheral vascular resistance correlates with the plasma concentration of felodipine. In equilibrium, the clinical effect persists between taking doses and decreasing blood pressure for 24 hours.

Felodipine treatment leads to regression of left ventricular hypertrophy. Felodipine has natriuretic and diuretic effects and does not have a potassium uretic effect. When felodipine is taken, tubular reabsorption of sodium and water is reduced, 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 glomerular filtration rate and albumin excretion. 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 angiotensin-converting enzyme (ACE) inhibitors.

Felodipine's anti-ischemic effect is due to an improvement in myocardial blood supply due to dilatation of the coronary vessels. Reducing the load on the heart is provided by reducing the total peripheral vascular resistance (reducing the load overcome by the cardiac muscle), which leads to a decrease in myocardial oxygen demand. Felodipine relieves spasm of the coronary vessels.

Pharmacokinetics

Suction and distribution

Slow release of felodipine from coated pills leads to an elongation of the drug's absorption phase and ensures a uniform concentration of felodipine in the blood plasma for 24 hours. Felodipine is almost completely absorbed in the gastrointestinal tract.Felodipine systemic bioavailability is approximately 15% and does not depend on the meal. However, the rate of absorption, but not its degree, can vary depending on the meal, and the maximum concentration in the blood plasma, therefore, increases by about 65%. Maximum plasma concentration (C_max) is achieved in 3-5 hours. The drug binds to plasma proteins by 99%, especially albumin. 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. Felodipine's half-life is 25 hours, the plateau phase is reached in about 5 days. Does not accumulate even with long-term use. The total plasma clearance on average is 1200 ml / min. Reduced clearance in elderly patients and in patients with reduced liver function leads to an increase in plasma felodipine concentration.

Pharmacokinetics in Special Patient Groups

In elderly patients and in cases of abnormal liver function, the concentration of felodipine in the blood plasma is higher than in young patients. Felodipine pharmacokinetic parameters do not change in patients with impaired renal function, including during hemodialysis. About 70% of the dose taken is excreted by the kidneys, and the rest is excreted through the intestine in the form of metabolites. Unchanged by the kidneys excreted less than 0.5% of the accepted dose. Felodipine penetrates the hemato-placental barrier and is excreted in breast milk.

Indications

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

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

Composition

1 tablet of the prolonged action, film coated, contains:

active ingredient: felodipine 2.5 mg;

excipients: hypromellose (hydroxypropyl methylcellulose) 52 mg, calcium hydrogen phosphate dihydrate 19 mg, silicon colloid dioxide 1 mg, lactose monohydrate 34.8 mg, magnesium stearate 0.7 mg, sodium alginate 5 mg, povidone K-30 5 mg;

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

Felodipine is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Felotenz	Canonpharma	Russia	pills
Felodip	Teva	Israel	pills
Plandil	AstraZeneca	UK	pills

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Dosage and Administration

Orally, preferably, drinking water, on an empty stomach or with a small amount of food low in fat and carbohydrates.

The tablet does not divide, 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 is best to use pills with a felodipine 2.5 mg.

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

Stable angina pectoris

The dose is always determined individually. Treatment begins with a dose of 5 mg 1 time a day, if necessary, you can increase the dose to 10 mg 1 time a day.

Preparation °° Felotenz^® Retard can be used in combination with beta-blockers, ACE inhibitors or diuretics. Combination therapy usually enhances the antihypertensive effect of the drug. Must beware of the development of arterial hypotension. In patients with impaired renal function, the pharmacokinetics of the drug does not significantly change. Care must be taken in patients with impaired renal function (CC less than 30 ml / min).

Adverse reactions

As with the use of other “slow” calcium channel blockers, the drug can cause facial flushing, headache, palpitations, dizziness, and increased fatigue. These reactions are reversible and most often occur at the beginning of treatment or with an increase in the dose of the drug. Also, depending on the dose, peripheral edema may occur, which are the result of precapillary vasodilation. Patients with gum disease or periodontitis may experience mild swelling of the gums. This can be prevented by careful oral hygiene.

WHO (World Health Organization) classification of the incidence of side effects:

often from ≥1 / 100 to <1/10 of appointments (> 1% and <10%);

infrequently - from ≥1 / 1000 to <1/100 of appointments (> 0.1% and <1%);

rarely from ≥1 / 10000 to <1/1000 of appointments (> 0.01% and <0.1%);

very rarely - <1/10000 appointments (<0.01%).

Since the cardiovascular system

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

infrequently - tachycardia, palpitations, pronounced decrease in blood pressure, accompanied by reflex tachycardia and worsening of angina;

very rarely - extrasystole, leukocytoclastic vasculitis.

The nervous system

often - headache;

infrequently - paresthesia, dizziness;

rarely - fainting.

From the digestive system

infrequently - nausea, abdominal pain;

rarely vomiting;

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

From the musculoskeletal system

rarely - arthralgia, myalgia.

Allergic reactions

infrequently - skin rash, itching;

rarely - urticaria;

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

On the part of the urinary system

very rarely - frequent urination.

Other:

infrequently - increased fatigue;

rarely, impotence / sexual dysfunction;

very rarely - fever, hyperglycemia.

A causal relationship has not been established: chest pain, swelling of the face, flu-like syndrome, marked reduction in blood pressure, myocardial infarction, syncope, angina pectoris, arrhythmia, extrasystole, diarrhea, dryness of the oral mucosa, flatulence, gynecomastia, anemia, arthralgia, pain in the mouth back, myalgia, pain in the upper and lower extremities, depression, insomnia, anxiety, nervousness, drowsiness, irritability, pharyngitis, shortness of breath, bronchitis, flu, sinusitis, nasal bleeding, erythema, bruising, leukocytoclastic vasculitis, impaired vision Niya, polyuria, dysuria.

Contraindications

- hypersensitivity to felodipine and other derivatives of the dihydropyridine series;

- unstable angina;

- acute myocardial infarction and the period within one month after suffering a 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;

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

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

Carefully

Liver dysfunction, severe renal failure (creatinine clearance (CC) less than 30 ml / min), aortic and mitral stenosis, blood pressure lability and heart failure after myocardial infarction, old age.

Drug interactions

Digoxin: Felodipine increases the concentration of digoxin in the blood plasma, but a dose change 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 plasma.

Inductors of the CYP3A4 isoenzyme (phenytoin, carbamazepine, rifampicin, barbiturates, phenobarbital, Hypericum perforatum drugs) reduce AUC (area under the pharmacokinetic concentration-time curve) of felodipine by 93% and C_max on
82%. Avoid joint appointment.

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

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

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

Antimicrobial drugs of the azole series (ketoconazole, itraconazole) with a joint appointment of AUC felodipine increases 8 times, C_max - 6 times.

Macrolide antibiotics (erythromycin): with co-administration of AUC and C_maxfelodipine is increased 2.5 times.

HIV protease inhibitors also increase felodipine concentration in the blood.

Grapefruit juice increases AUC and C_maxfelodipine 2 times, so felodipine should not be used simultaneously with grapefruit juice.

Tacrolimus: felodipine increases plasma plasma tacrolimus when used together (monitoring plasma plasma tacrolimus and a possible dose adjustment is recommended).

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

Cimetidine increases C_max and felodipine AUC by 55%.

Pregnancy and Lactation

Drug felotens^®retard is contraindicated during pregnancy and during breastfeeding.

Currently there are no data on the use of felodipine in pregnant women. Based on animal data on fetal developmental impairment, felodipine should not be administered during pregnancy. Slow calcium channel blockers can inhibit uterine contraction in preterm labor, but there is insufficient evidence to support an increase in the duration of physiological labor. The risk of fetal hypoxia is possible if the mother has arterial hypotension and a decrease in perfusion in the uterus due to redistribution of blood flow and peripheral vasodilation.

Felodipine gets into breast milk. When felodipine is taken by nursing mother in therapeutic doses, only a small amount of felodipine passes into breast milk. The lack of experience with felodipine in women during breastfeeding does not exclude the risk of the drug being exposed to breastfed babies. If necessary, continue therapy with the drug Felotenz^® retard to achieve the clinical effect of breastfeeding should be discontinued.

Special instructions

The drug Felotenz® retard should be prescribed with caution in patients with a tendency to tachycardia and severe dysfunction of the left ventricle. 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. Currently, there is no data on the feasibility of using the drug as a secondary prevention of myocardial infarction.

Felodipine is effective and well tolerated by patients regardless of gender and age, as well as patients with comorbidities such as bronchial asthma and other lung diseases, renal dysfunction, diabetes, gout, hyperlipidemia, Raynaud's syndrome, and after lung transplantation.

Preparation °° Felotenz^® retard has no effect on blood glucose concentration and lipid profile. Hyperglycemia is observed only in some cases.

Impaired renal function does not affect the concentration of the drug in the blood plasma, therefore, dose adjustment in patients with impaired renal function is not required. However, in the appointment of the drug in patients with renal insufficiency, care must be taken.

Careful oral hygiene must be observed, due to the possible development of gingival hyperplasia and gingivitis.

Impact on the ability to drive vehicles and mechanisms for patients who have felotenz during treatment^®retard there is weakness, dizziness, should abandon the control of motor vehicles and work that requires increased concentration of attention and speed of psychomotor reactions.

Overdosage

Symptoms: In case of overdose, symptoms of intoxication appear 12-16 hours after taking the drug, sometimes symptoms may occur several days after taking the drug. The following symptoms may be noted: marked reduction in blood pressure, bradycardia, AV (atrioventricular) block I-III degree, ventricular premature beats, atrial-ventricular dissociation, asystolia, ventricular fibrillation; headache, dizziness, disturbance of consciousness (or coma), seizures; shortness of breath, pulmonary edema (non-cardiac) and apnea; adults may develop respiratory distress syndrome; acidosis, hypokalemia, hyperglycemia, hypocalcemia; facial flushing, hypothermia; nausea, vomiting.

Treatment: Gastric lavage, the appointment of activated carbon, in some cases effective even at the late stage of intoxication. Specific antidote - calcium supplements. With a pronounced decrease in blood pressure, the patient should be given a horizontal position, legs raised. With the development of bradycardia shown in / in the introduction of atropine at a dose of 0.25-0.5 mg, which should be prescribed before gastric lavage, due to the risk of stimulation of the vagus nerve. ECG monitoring. If necessary, ensure airway and adequate ventilation of the lungs. Correction of acid-base status and serum electrolytes is shown. In the case of bradycardia and AV blockade, atropine 0.5-1.0 mg IV is prescribed, if necessary, repeat the introduction, or isoprenaline 0.05-0.1 µg / kg / min is initially administered. In acute intoxication at an early stage, an artificial pacemaker may be needed. Reduction of blood pressure is corrected by intravenous injection of fluid (dextrose solution, 0.9% solution of sodium chloride, dextran), adults of intravenous injection of calcium gluconate solution of 20-30 ml for
5 minutes, if necessary, repeat the introduction in the same dose. If necessary, norepinephrine (adrenaline) or dopamine is administered by infusion. In acute intoxication, glucagon may be administered. When convulsions prescribed diazepam.