1 prolonged-release film-coated tablet contains:
active substance :
felodipine 2.5 mg.
colloidal anhydrous silicon,
iron oxide yellow,
iron oxide red,
Felodip belongs to the blockers of "slow" calcium channels of the dihydropyridine series. It has a hypotensive, antianginal effect.
Reduces blood pressure (BP) by reducing peripheral vascular resistance. It has a dose-dependent anti-ischemic effect. Reduces the size of myocardial infarction, protects against complications of reperfusion. Has practically no negative inotropic effect, has a minimal effect on the cardiac conduction system.
Absorption and distribution
Delayed 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 within 24 hours. Felodipine is almost completely absorbed in the gastrointestinal tract. Bioavailability does not depend on the dose within the therapeutic interval and is approximately 15%. 99% of felodipine binds to blood proteins, primarily albumin.
Metabolism and excretion
Felodipine is completely metabolized in the liver, and all of its metabolites are inactive.
The half-life of felodipine is 25 hours. With prolonged use, cumulation of felodipine does not occur.
Pharmacokinetics in special groups of patents
In elderly patients and in cases of liver dysfunction, the concentration of felodipine in blood plasma is higher than in young patients. Pharmacokinetic parameters of felodipine do not change in patients with impaired renal function, including during hemodialysis. About 70% of the dose taken is excreted in the urine, and the rest in the feces in the form of metabolites. Less than 0.5% of the dose is excreted unchanged in the urine. Felodipine crosses the blood-placental barrier into the placenta and is excreted in breast milk.
Arterial hypertension, stable angina (including Prinzmetal's angina)
- Hypersensitivity to felodipine and other dihydropyridine derivatives
- Unstable angina
- Acute myocardial infarction and within one month after myocardial infarction
- Cardiogenic shock
- Clinically significant aortic stenosis
- Pregnancy and lactation
- Chronic heart failure in the stage of decompensation
- Severe arterial hypotension
- Age under 18 years of age (efficacy and safety have not been established)
Hepatic and / or renal failure, aortic stenosis, BP lability, and heart failure after myocardial infarction
As with other slow calcium channel blockers, the drug can cause facial flushing, 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 is a consequence of precapillary vasodilation. Patients with gum disease or periodontitis may experience mild gum swelling. This can be prevented by maintaining good oral hygiene.
The frequency of side effects is determined according to the following definitions: often (1/100 or more), less often (1 / 1000-1 / 100) rarely (1 / 10000-1 / 1000), very rarely (less than 1/10000).
From the side of the cardiovascular system: often - "hot flashes" of blood to the skin of the face, accompanied by facial flushing, swelling of the ankles; less often - tachycardia, palpitations; rarely - fainting; very rarely - extrasystole, a marked decrease in blood pressure, accompanied by reflex tachycardia and worsening angina pectoris, leukocytoclastic vasculitis.
From the nervous system: often - headache; less often - paresthesia, dizziness.
From the digestive system: less often - nausea, abdominal pain; rarely - vomiting; very rarely - increased activity of "hepatic" transaminases; rarely - hyperplasia of the gums, mucous membrane of the tongue, gingivitis.
On the part of the musculoskeletal system: rarely - arthralgia, myalgia.
Allergic reactions: less often - skin rash, itching; rarely - urticaria; very rarely - angioedema of the lips or tongue, photosensitivity reaction.
From the urinary system: very rarely - often urination.
Others: less often - fatigue; rarely, impotence / sexual dysfunction; very rarely - fever, hyperglycemia.
From the side of the skin: rarely - urticaria and itching. In rare cases, photosensitization reactions;
A causal relationship has not been established: chest pain, facial edema, flu-like syndrome, decreased blood pressure, myocardial infarction, syncope, angina pectoris, arrhythmia, extrasystole, diarrhea, dry mouth, flatulence, gynecomastia, anemia, arthralgia, back pain, myalgia , pain in the upper and lower extremities, depression, insomnia, anxiety, nervousness, drowsiness, irritability, pharyngitis, shortness of breath, bronchitis, influenza, sinusitis, nosebleeds, erythema, bruising, leukocytoclastic vasculitis, visual impairment, polyuria, dysuria.
Felodipine increases the concentration of digoxin in the blood plasma, however, no change in the dosage of felodipine is required.
Inhibitors of cytochrome P450 (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.
Microsomal enzyme inducers (phenytoin, carbamazepine, rifampicin, barbiturates) lower the concentration of felodipine in blood plasma. Non-steroidal anti-inflammatory drugs do not weaken the hypotensive effect of felodipine.
The high degree of binding of felodipine to proteins does not affect the binding of the free fraction of other drugs (for example, warfarin). Do not use felodipine at the same time as grapefruit juice. Beta-blockers, verapamil, tricyclic antidepressants and diuretics increase the hypotensive effect of felodipine.
Inhibitors of cytochrome P450 (cimetidine, erythromycin, ketoconazole, itraconazole, HIV protease inhibitors, grapefruit juice), slowing down the metabolism of the drug in the liver, increase its plasma concentration: with itraconazole - AUC of felodipine increases 8 times, Cmax - 6 times erythromycin - AUC and Cmax 2.5 times, with grapefruit juice - 2 times, respectively.
Microsomal oxidation inducers - phenytoin, carbamazepine, phenobarbital, rifampicin, tincture of St. John's wort - reduce the AUC of felodipine by 93% and Cmax by 82%.
Increases the concentration of tacrolimus in the blood plasma when used together (it is recommended to control the concentration of tacrolimus in the blood plasma and a possible dose adjustment).
Cyclosporine increases Cmax of felodipine by 150%, AUC by 60% (the effect of felodipine on the pharmacokinetic parameters of cyclosporine is minimal). Cimetidine increases the Cmax and AUC of felodipine by 55%.
How to take, course of administration and dosage
The drug is best taken orally in the morning, before meals or after a light breakfast.
Film-coated tablets must not be bitten, divided or crushed.
Adults (including the elderly): The
dosage is always determined individually. Therapy begins with a dose of 5 mg once a day. If necessary, the dosage can be increased; the usual maintenance dose is 5-10 mg once a day. To determine the individual dose, it is best to use tablets containing 2.5 mg of felodipine. In the elderly or patients with impaired liver function, the recommended starting dosage is 2.5 mg once a day.
dosage is always determined individually. Treatment begins with a dose of 5 mg once a day, if necessary, you can increase the dose to 10 mg once a day. The maximum daily dose is 20 mg once a day.
Felodip can be used in combination with beta-blockers, angiotensin-converting enzyme (ACE) inhibitors or diuretics.
Combination therapy usually enhances the antihypertensive effect of the drug.
It is necessary to beware of the development of arterial hypotension. In patients with severely impaired liver function, the therapeutic dose should be reduced.
In patients with impaired renal function, the pharmacokinetics of the drug does not significantly change.
Symptoms: marked decrease in blood pressure, bradycardia.
Treatment: symptomatic therapy is performed. With a pronounced decrease in blood pressure, the patient should be given a horizontal position, his legs should be raised. With the development of bradycardia, intravenous administration of atropine in a dose of 0.5-1.0 mg is indicated.
If this is not enough, it is necessary to increase the blood plasma volume by infusion of dextrose (glucose) solution, sodium chloride or dextran. If the above measures are ineffective, symptomatic drugs with a predominant effect on alpha-adrenergic receptors are prescribed.
The drug felodip, as well as other vasodilators, in rare cases 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 advisability 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 by patients with concomitant diseases such as bronchial asthma and other lung diseases; impaired renal function; diabetes; gout; hyperlipidemia; Raynaud's syndrome, and also after lung transplantation.
Felodipine has no effect on blood glucose concentration and lipid profile.
Influence on the ability to drive vehicles and control mechanisms:
patients who experience weakness, dizziness during treatment with felodipine should refuse to drive vehicles and work that requires increased attention and concentration.
Sustained-release film-coated tablets