Felodipine
Felodipine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Felodipine
ATX code: C08CA02
Active ingredient: Felodipine (felodipine)
Manufacturer: Zhejiang Supor Pharmaceuticals Co. Ltd. PR China (China), Everlight Chemical Industrial Corporation (Taiwan), Nivedita Chemicals Pvt. Ltd (India), Kanonpharma production CJSC (Russia)
Description and photo update: 2018-25-10
Prices in pharmacies: from 217 rubles.
Buy
Felodipine is a dihydropyridine drug, a selective blocker of slow calcium channels, antihypertensive and antianginal action.
Release form and composition
Dosage form of the drug Felodipine - tablets of prolonged action, film-coated: round, biconvex, a white core and a shell from light yellow to yellow stand out on the cross section (10, 15 or 30 pcs. In cellular contour packages made of polyvinyl chloride film (PVC) and printed lacquered aluminum foil; in a cardboard box 1, 2, 3, 6 packs of 10 pcs., or 1, 2, 4 packs of 15 pcs., or 1, 2 packs of 30 pcs.).
Composition for 1 tablet of prolonged action, film-coated:
- active substance: Felodipine - 2.5; 5 or 10 mg;
- additional components: hydroxypropyl methylcellulose Benecel MP 824 (hypromellose), calcium hydrogen phosphate dihydrate, aerosil (colloidal silicon dioxide), milk sugar (lactose), sodium alginate (Kelton HVCR), magnesium stearate, povidone (Kollidon 30);
- film casing: Selecoat AQ-01812 [hydroxypropyl methylcellulose (hypromellose), macrogol (polyethylene glycol 400 and polyethylene glycol 6000), quinoline yellow dye, iron oxide yellow dye, titanium dioxide].
Pharmacological properties
Pharmacodynamics
The active component of the drug - felodipine, is a slow calcium channel blocker (BMCC), has hypotensive and antianginal efficacy. By reducing peripheral vascular resistance, it helps to reduce blood pressure (BP); has a dose-dependent anti-ischemic effect; reduces the size of the necrotic area of the heart muscle formed as a result of myocardial infarction and protects against complications during the resumption of blood flow (reperfusion). Felodipine practically does not have a negative inotropic effect, minimally affecting the PSS (cardiac conduction system).
Pharmacokinetics
Pharmacokinetic parameters of the drug:
- absorption and distribution: a special film coating slows down the release of felodipine from the tablets, which helps to lengthen the phase of its absorption and ensures an even distribution of the drug in the blood plasma for 24 hours. Felodipine is almost completely absorbed in the gastrointestinal tract (gastrointestinal tract), its bioavailability within the therapeutic interval does not depend on the dose and is ~ 15%; up to 99% of the substance binds to blood proteins, primarily albumin;
- metabolism and excretion: felodipine is almost completely metabolized in the liver to form inactive metabolites. T 1/2 (half-life) - 25 hours. Up to 70% of the dose taken in the form of metabolites is eliminated in the urine, the rest with feces. Unchanged, less than 0.5% of the dose taken is excreted in the urine. Long-term use of the drug does not lead to its cumulation.
In elderly patients and with impaired liver function, the plasma concentration of felodipine is higher than in healthy young patients.
With impaired renal function, including in patients on hemodialysis, there was no change in the pharmacokinetic parameters of felodipine.
Felodipine enters the placenta through the hematoplacental barrier, and is also excreted during lactation in breast milk.
Indications for use
According to the instructions, Felodipine is recommended for use in arterial hypertension and stable angina pectoris (including Prinzmetal's angina).
Contraindications
Absolute:
- severe arterial hypotension;
- unstable angina;
- cardiogenic shock;
- acute myocardial infarction and the period within 1 month after myocardial infarction;
- clinically significant aortic stenosis;
- chronic heart failure (CHF) in the stage of decompensation;
- period of pregnancy and lactation;
- children and adolescents under 18 years of age;
- hypersensitivity to derivatives of the dihydropyridine series, including felodipine, as well as to other components of the drug.
Relative contraindications in which the drug must be used with caution: renal / hepatic failure, blood pressure lability, aortic stenosis, heart failure due to myocardial infarction.
Instructions for the use of Felodipine: method and dosage
Felodipine extended-release tablets are intended for oral administration, they cannot be bitten, crushed or divided. It is preferable to take the drug in the morning, before meals or after a light breakfast.
Recommended dosage according to indications (taking once a day):
- arterial hypertension (adult patients, including the elderly): start treatment with a dose of 5 mg, if necessary, it can be increased; the standard maintenance dose is 5-10 mg. In order to titrate an individual dose, it is recommended that elderly patients and patients with impaired liver function begin treatment with tablets at a dosage of 2.5 mg;
- stable angina pectoris (adult patients): start treatment with a dose of 5 mg, if necessary, it can be increased to 10 mg; the maximum daily dose should not exceed 20 mg.
The dosage in each case is determined individually.
The drug can be used in combination with angiotensin-converting enzyme (ACE) inhibitors, β-blockers and diuretics. It should be borne in mind that when using Felodipine as part of a combination treatment, its hypotensive effect is usually enhanced, and therefore one should beware of the development of arterial hypotension.
In case of severe violations of liver function, a decrease in the therapeutic dose of the drug is required.
In patients with impaired renal function, the pharmacokinetics of the drug does not change significantly.
Side effects
Like the use of other BMCCs, Felodipine can cause dizziness, headache, facial flushing, palpitations, and increased fatigue. These side effects are most often manifested at the beginning of therapy or when the dose is increased, and are reversible. Peripheral edema resulting from precapillary vasodilation is also dose-dependent. With gum disease or periodontitis, mild gum swelling may occur, which can be prevented by careful oral hygiene.
The frequency of side effects by systemic organ classes, depending on the number of recorded episodes (scale used: ≥ 0.01 - often; 0.001-0.01 - less often; 0.0001-0.00001 - rarely; 0.00001 - extremely seldom):
- cardiovascular system: often - flushing of the face, accompanied by hyperemia, swelling of the ankles; less often - palpitations, tachycardia; rarely - fainting; extremely rarely - accompanied by a worsening of the course of angina pectoris and reflex tachycardia, a pronounced decrease in blood pressure, extrasystole, leukocytoclastic vasculitis;
- nervous system: often - headache; less often - dizziness, paresthesia;
- digestive system: less often - nausea, pain in the abdominal region; rarely - vomiting, hyperplasia of the gums and mucous membrane of the tongue, gingivitis; extremely rarely - increased activity of hepatic transaminases;
- musculoskeletal system: rarely - myalgia, arthralgia;
- hypersensitivity reactions: less often - skin rash, itching; rarely - urticaria; extremely rarely - angioedema of the lips or tongue, photosensitivity reaction;
- urinary system: extremely rare - frequent urination;
- other reactions: less often - fatigue; rarely, impotence and / or sexual dysfunction; extremely rare - hyperglycemia, fever;
- skin: rarely - urticaria, itchy skin; isolated episodes - photosensitivity reactions.
Side effects manifested during treatment, the causal relationship of which with Felodipine intake has not been established: facial edema, chest pain, decreased blood pressure, flu-like syndrome, flu, syncope, myocardial infarction, arrhythmia, angina pectoris, extrasystole, dry mouth, diarrhea, flatulence, anemia, gynecomastia, arthralgia, back pain, pain in the upper and lower extremities, myalgia, insomnia, nervousness, depression, anxiety, drowsiness, irritability, shortness of breath, pharyngitis, bronchitis, sinusitis, nosebleeds, bruising, erythema, leukocytoclastic, visual impairment, dysuria, polyuria.
Overdose
Overdose symptoms are marked decrease in blood pressure and bradycardia.
In the case of a pronounced decrease in blood pressure, the patient should be laid in a horizontal position, and the legs should be raised.
With the development of bradycardia, 0.5–1.0 mg of atropine is administered intravenously. If the condition does not stabilize, an infusion of a dextrose (glucose) solution, dextran, or sodium chloride is required to increase plasma volume. When the above measures do not have the desired effect, therapy is carried out with symptomatic drugs with a predominant effect on α-adrenergic receptors.
special instructions
Like other vasodilators, Felodipine, in rare cases, can cause clinically significant arterial hypotension with further development of myocardial ischemia in predisposed patients. To date, there is no data on the advisability of using Felodipine in the secondary prevention of myocardial infarction.
Felodipine does not affect the lipid profile and blood glucose concentration.
The drug is well tolerated and highly effective in treating patients regardless of gender and age, as well as in the following concomitant diseases: bronchial asthma and other pulmonary pathologies, Raynaud's syndrome, renal dysfunction, gout, diabetes mellitus, hyperlipidemia, the period after lung transplantation.
Influence on the ability to drive vehicles and complex mechanisms
With the manifestation of such side effects as dizziness and weakness, patients should temporarily refuse to perform types of work that require increased concentration of attention and increased reaction speed, including from driving.
Application during pregnancy and lactation
Felodipine is contraindicated for pregnant and lactating women.
Pediatric use
In pediatric practice, the use of the drug for the treatment of children and adolescents under 18 years of age is contraindicated due to the lack of reliable data on the effectiveness and safety of therapy in patients of this age category.
With impaired renal function
When therapy with Felodipine, patients with impaired renal function should be careful.
For violations of liver function
When therapy with Felodipine, patients with impaired liver function should be careful.
Drug interactions
- digoxin: felodipine increases its plasma concentration, dose adjustment is not required;
- erythromycin, cimetidine, ketoconazole, itraconazole, and other inhibitors of cytochrome P450: inhibit hepatic metabolism of felodipine, thereby increasing its concentration in blood plasma;
- phenytoin, carbamazepine, rifampicin, barbiturates, etc. inducers of microsomal enzymes: reduce the plasma concentration of felodipine;
- NSAIDs (non-steroidal anti-inflammatory drugs): do not reduce the hypotensive effect of felodipine;
- warfarin and other drugs, the free fraction of which binds to proteins: felodipine does not affect their binding to proteins;
- grapefruit juice: should not be taken simultaneously with felodipine;
- verapamil, β-blockers, tricyclic antidepressants, diuretics: increase the hypotensive effect of felodipine;
- cimetidine, erythromycin, ketoconazole, itraconazole, HIV protease inhibitors, grapefruit juice and other inhibitors of cytochrome P450: slow down the hepatic metabolism of the drug, increasing its plasma concentration (itraconazole: increases the AUC of felodipine by 8 times, Cmaxrom - by 6 times; AUC and Cmax - 2.5 times; grapefruit juice - 2 times, respectively);
- carbamazepine, phenytoin, phenobarbital, tincture of St. John's wort, rifampicin, and other inducers of microsomal oxidation: reduce the performance of felodipine, AUC - by 93% and Cmax - by 82%;
- tacrolimus: its concentration in blood plasma increases, it is recommended to monitor the indicator and adjust the dose if necessary;
- cyclosporine: increases Cmax of felodipine by 150% and AUC by 60%, felodipine minimally affects the pharmacokinetic parameters of cyclosporine;
- cimetidine: increases the Cmax and AUC of felodipine by 55%.
Analogs
The analogues of Felodipine are Plendil, Felotenz retard, Amlong, Amlodipine, Agen, Amlo, Corinfar, Kordafen, Kordipin, Lerkamen, Nimopin, Normodipin, Nifedipin, Norvask, Tenox, Stamlo, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a dry and dark place. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Felodipine
In cases where the drug is suitable for the main therapeutic effect and does not cause strong side reactions, the reviews about Felodipine are extremely favorable. Patients for whom the drug is not suitable for any indicators avoid its use.
Doctors recommend approaching the selection of antihypertensive drugs very carefully and purely individually, taking into account the anamnestic data, the severity of the disease and the personal characteristics of the body.
Felodipine price in pharmacies
Estimated price for Felodipine tablets 10 mg for 30 pcs. in the package - 237 rubles.
Felodipine: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Felodipine 2.5 mg film-coated tablets of prolonged action 30 pcs. 217 r Buy |
|
Felodipine 5 mg film-coated tablets of prolonged action 30 pcs. 267 r Buy |
|
Felodipine 10 mg film-coated tablets with prolonged release 30 pcs. 448 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
