Felodip extended-release film-coated tablets 10 mg N30

Compound

Description of the dosage form

Extended-release film-coated tablet, 2.5 mg: round, biconvex, yellow film-coated, odorless, with “2.5” engraved on one side.

Extended-release film-coated tablet, 5 mg: round, biconvex, light pink, odorless, film-coated, with “5” engraved on one side.

Extended-release film-coated tablet, 10 mg: round, biconvex, red-brown, odorless, film-coated, with “10” engraved on one side.

On the break of the tablet you can see a white or almost white core (for all dosages).

Pharmacokinetics

Absorption and distribution. The slow release of felodipine from film-coated tablets leads to an extension of the absorption phase of the drug and ensures a uniform concentration of felodipine in the blood plasma over 24 hours. Felodipine is almost completely absorbed from the gastrointestinal tract. The bioavailability of the drug does not depend on the dose within the therapeutic interval and is approximately 15%. 99% of felodipine binds to plasma proteins, primarily albumin.

Metabolism and excretion. Felodipine is completely metabolized in the liver, and all its metabolites are inactive. T1/2 of felodipine is 25 hours. With long-term use, felodipine does not accumulate.

Pharmacokinetics in special groups of patients

Elderly patients. In elderly patients and in cases of impaired liver function, the concentration of felodipine in the blood plasma is higher than in young patients.

Renal dysfunction. The pharmacokinetic parameters of felodipine do not change in patients with impaired renal function, including those undergoing hemodialysis. About 70% of the dose taken is excreted by the kidneys, and the rest by the intestines in the form of metabolites. Less than 0.5% of the dose taken is excreted unchanged by the kidneys. Felodipine penetrates the BBB into the placenta and is excreted in breast milk.

Pharmacological properties of the drug Felodip

Pharmacodynamics. Felodip is a dihydropyridine derivative, a selective blocker of L-type calcium channels. It has a high affinity for smooth muscle cells of peripheral arterioles and coronary arteries. Felodip dilates arterioles, reduces peripheral vascular resistance and blood pressure. In therapeutic doses it has virtually no effect on myocardial contractility. Felodip has an antianginal effect by reducing vascular resistance of the coronary vessels, improving coronary circulation and oxygen supply to the myocardium, and also reduces afterload on the heart, which leads to a decrease in myocardial oxygen demand. Felodip improves exercise tolerance and reduces the frequency of attacks in patients with stable angina, and has an anti-ischemic effect in vasospastic angina. The primary hemodynamic effect of Felodip is a decrease in general peripheral vascular resistance, thereby reducing blood pressure. This effect is dose dependent. As a rule, a decrease in blood pressure is observed 2 hours after a single dose and lasts for at least 24 hours, the T/P ratio (plateau/peak) reaches a value well above 50%. There is a positive relationship between the concentration of the drug in the blood plasma, the level of decrease in OPSS and the decrease in blood pressure. Felodip has a slight natriuretic and diuretic effect, since it reduces tubular reabsorption of sodium. Felodip does not affect the daily excretion of potassium. In patients with reduced renal function, glomerular filtration rate may increase during treatment with Felodip. Felodip is well tolerated by patients after kidney transplantation. The drug does not affect the concentration of glucose in the blood and the lipid profile. Pharmacokinetics. Felodip is completely absorbed into the gastrointestinal tract. Bioavailability is about 15% and does not depend on the dose taken (first pass effect through the liver). 99% of Felodipa binds to blood plasma proteins, mainly albumin. Due to the peculiarities of the dosage form, the prolonged release of felodipine extends the absorption phase and ensures its uniform concentration in the blood plasma over 24 hours. The drug penetrates the BBB and the placental barrier, and into breast milk. Felodipine is completely metabolized in the liver, all of its metabolites are inactive. The half-life of felodipine is 25 hours. With prolonged use, accumulation of the active substance does not occur. In elderly patients and with impaired liver function, plasma concentrations of felodipine are higher than in young patients. The pharmacokinetics of Felodip does not change in patients with impaired renal function, including those undergoing hemodialysis. About 70% of the dose taken is excreted in the urine, and 30% is excreted in the feces in the form of metabolites. 0.5% of the dose taken is excreted unchanged in the urine.

Side effects

As with other CCBs, Felodip may cause facial flushing, headache, palpitations, dizziness and fatigue. These reactions are reversible and most often occur at the beginning of treatment or when the dose of the drug is increased. Also, depending on the dose, peripheral edema may appear, which is a consequence of precapillary vasodilation. Patients with gum disease or periodontitis may experience mild swelling of the gums. This can be prevented by practicing good oral hygiene.

The incidence of side effects is classified according to WHO recommendations: very often - at least 10%; often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely (including isolated cases) - less than 0.01%.

From the immune system: very rarely - hypersensitivity reaction, angioedema.

From the central and peripheral nervous system: often - headache; infrequently - dizziness, paresthesia; rarely - fainting.

From the cardiovascular system: very often - peripheral edema; often - hot flashes; rarely - tachycardia, palpitations.

From the gastrointestinal tract: infrequently - nausea, abdominal pain; rarely - vomiting; very rarely - gum hyperplasia, gingivitis.

From the liver and biliary tract: very rarely - increased activity of hepatic transaminases.

From the skin and subcutaneous tissues: infrequently - rash, itching of the skin; rarely - urticaria; very rarely - photosensitivity reaction, leukocytoclastic vasculitis.

From the musculoskeletal system and connective tissue: rarely - arthralgia, myalgia.

From the kidneys and urinary tract: very rarely - pollakiuria.

Other: infrequently - fatigue; rarely - sexual dysfunction.

Side effects of the drug Felodip

Like other calcium antagonists, felodipine can cause facial flushing, headache, palpitations, dizziness, and fatigue. These reactions are temporary and occur more often at the beginning of treatment or when the dose is increased. Depending on the dose, edema in the ankle area may occur as a result of precapillary vasodilation. Patients with gum disease or periodontitis may experience mild swelling of the gums; this can be prevented by maintaining good oral hygiene. As with the use of other dihydropyridines, in some cases an increase in the manifestations of angina was noted, mainly at the beginning of treatment. Cardiovascular system: tachycardia, palpitations, rarely - syncope, peripheral edema, facial flushing. Central and peripheral nervous system: headache, dizziness, rarely - paresthesia. Gastrointestinal tract: nausea, abdominal pain, in isolated cases - hyperplasia, inflammation of the gums. Liver: in isolated cases, an increase in the level of liver transaminases is noted. Musculoskeletal system: rarely - pain in joints and muscles. Allergic reactions: facial flushing, skin rash, itching; rarely - urticaria; in isolated cases - photosensitivity, vasculitis. Urinary system: in isolated cases - pollakiuria. Other: rarely - fatigue, sexual dysfunction, impotence; in isolated cases - hypersensitivity reactions, for example angioedema, increased body temperature.

Interaction

Felodipine increases the concentration of digoxin in the blood plasma, but no dose adjustment of felodipine is required.

Cytochrome P450 inhibitors (for example, cimetidine, erythromycin, itraconazole, ketoconazole) slow down the metabolism of felodipine in the liver, increasing the concentration of the drug in the blood plasma.

Inducers of microsomal enzymes (phenytoin, carbamazepine, rifampicin, barbiturates) reduce the concentration of felodipine in the blood plasma.

NSAIDs do not reduce the hypotensive effect of felodipine.

The high degree of protein binding of felodipine does not affect the binding of the free fraction of other drugs (for example, warfarin).

Felodipine should not be used concomitantly with grapefruit juice due to the flavonoid it contains, which increases the bioavailability of felodipine.

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

With simultaneous use, it is possible to increase the concentration of tacrolimus in the blood plasma, which may require adjustment of the tacrolimus dose.

Drug interactions Felodip

The hypotensive effect of Felodip is enhanced by other antihypertensive drugs (beta-adrenergic receptor blockers, ACE inhibitors, diuretics), tricyclic antidepressants, and alcohol. When using Felodip, β-adrenergic receptor blockers and organic nitrates, the antianginal effect of these drugs is summed up. When used simultaneously with NSAIDs Felodip, the antihypertensive effect of Felodip is not reduced. Inhibitors of microsomal enzymes (cimetidine, erythromycin, ranitidine, ketoconazole, itraconazole, ritonavir, saquinavir, quinidine) increase the concentration of felodipine in the blood plasma, therefore the prescribed dose of Felodipine should be reduced when used simultaneously with this group of drugs. Inducers of microsomal enzymes (for example, phenytoin, carbamazepine, rifampicin and barbiturates) can reduce the concentration of felodipine in the blood plasma, so the dose of Felodipine should be adjusted when these drugs are used in combination. When Felodip is used simultaneously with digoxin, the concentration of the latter increases, but no change in the dose of Felodip is required. Significant binding of felodipine to plasma proteins does not affect the particle free fractions of another drug, which is also characterized by significant binding to plasma proteins (for example, warfarin). Grapefruit juice, due to the presence of a flavonoid in it, increases the plasma level and bioavailability of felodipine, so it cannot be used together with Felodipine.

Directions for use and doses

Inside. The drug is best taken in the morning, before meals or after a light breakfast. Film-coated tablets should not be cracked, divided or crushed.

Arterial hypertension

Adults (including the elderly). The dose is always determined individually. Therapy begins with a dose of 5 mg once a day. If necessary, the dose can be increased; The usual maintenance dose is 5–10 mg once a day. To determine your individual dose, it is best to use tablets containing felodipine 2.5 mg. In elderly patients or patients with impaired liver function, the recommended starting dose is 2.5 mg once daily.

Stable angina

Adults. The dose is always determined individually. Treatment begins with a dose of 5 mg 1 time per day; if necessary, the dose can be increased to 10 mg 1 time per day. The maximum daily dose is 20 mg 1 time per day.

The drug Felodip can be used in combination with β-blockers, ACE inhibitors or diuretics. Combination therapy usually enhances the hypotensive effect of the drug. It is necessary to beware of the development of arterial hypotension. In patients with severe liver dysfunction, the therapeutic dose should be reduced. In patients with impaired renal function, the pharmacokinetics of the drug does not change significantly.

Overdose

Symptoms: marked decrease in blood pressure, bradycardia.

Treatment: carry out symptomatic therapy. If there is a pronounced decrease in blood pressure, the patient should be placed in a horizontal position with his legs elevated. If bradycardia develops, intravenous administration of atropine at a dose of 0.5–1 mg is indicated. If this is not enough, it is necessary to increase the volume of blood plasma by infusion of a solution of dextrose (glucose), sodium chloride or dextran. Symptomatic drugs with a predominant effect on alpha-adrenergic receptors are used when the above measures are ineffective.

Felodip overdose, symptoms and treatment

Symptoms: arterial hypotension and bradycardia. Treatment: the stomach is washed, activated carbon is used, and the patient is subsequently placed in an intensive observation room to monitor the function of the cardiovascular and respiratory systems. In case of severe arterial hypotension, it is necessary to place the patient in a horizontal position with the lower limbs raised upward, increase the volume of blood plasma by administering a physiological solution of sodium chloride, glucose, dextran; introduce sympathomimetics: norepinephrine, mesaton, dopamine, dobutamine, as well as calcium chloride. In case of bradycardia, AV block of II–III degree, or the appearance of asystole, atropine sulfate, norepinephrine or calcium chloride is administered intravenously. If necessary and if indicated, an artificial pacemaker is used.

special instructions

The drug Felodip, as well as other vasodilators, can in rare cases cause significant arterial hypotension, which in some predisposed patients can lead to the development of myocardial ischemia. Currently, there is no data on the advisability of using the drug as secondary prevention of myocardial infarction.

The drug Felodip is effective and well tolerated by patients regardless of gender and age, as well as by patients with concomitant diseases such as bronchial asthma and other lung diseases; impaired renal function; diabetes; gout; hyperlipidemia; Raynaud's syndrome, as well as after lung transplantation.

The drug Felodip does not affect the concentration of glucose in the blood and the lipid profile.

Impact on the ability to drive vehicles and work with equipment. Patients who experience weakness or dizziness during treatment with Felodip should avoid performing activities that require increased concentration and speed of psychomotor reactions.

Special instructions for the use of the drug Felodip

During treatment with Felodip, you should refrain from engaging in potentially dangerous activities that require concentration and speed of psychomotor reactions. Patients with angina pectoris should take into account that the drug can cause arterial hypotension, which can cause the appearance or intensification of myocardial ischemia. If liver function is impaired, it is necessary to adjust the dose of the drug. Felodip does not affect the concentration of glucose in the blood plasma and the lipid profile. Felodipine should not be taken in combination with grapefruit juice due to the fact that the latter contains a flavonoid that increases the concentration of felodipine in the blood serum. Felodip is effective and well tolerated by patients regardless of gender and age, persons with asthma, other obstructive pulmonary diseases, impaired renal function, patients with diabetes mellitus, gout, hyperlipidemia, Raynaud's syndrome, and after lung transplantation. Felodip is prescribed with caution, especially in combination with β-adrenergic receptor blockers, to patients with severe heart failure.