Plendil
Plendil: 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. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Plendil
ATX code: C08CA02
Active ingredient: felodipine (Felodipine)
Manufacturer: AstraZeneca, AB (AstraZeneca, AB) (Sweden); AstraZeneca Pharmaceutical (China)
Description and photo updated: 30.11.2018
Prices in pharmacies: from 365 rubles.
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Plendil is a slow calcium channel blocker that has antihypertensive and antianginal effects.
Release form and composition
The drug is available in the form of tablets of prolonged action, film-coated (30 pcs. In plastic bottles, 1 bottle in a cardboard box and instructions for use of Plendil):
- dosage 2.5 mg: round, Ø 8.5 mm, biconvex, yellow sheath, 2.5 engraved on one side; on the other side above the horizontal line there is the letter A, below it - FL;
- dosage 5 mg: round, Ø 9.0 mm, biconvex, pink sheath, engraved on one side 5; on the other side above the horizontal line there is the letter A, below it - Fm;
- dosage 10 mg: round, Ø 9.0 mm, biconvex, red-brown shell, engraved 10 on one side, letter A above the horizontal line on the other, FE below it.
The gradual release of the active substance is ensured by the presence in the tablet core of a hydrophilic gel matrix.
1 tablet contains:
- active substance: felodipine - 2.5; 5 or 10 mg;
- auxiliary components: anhydrous lactose, hydroxypropyl cellulose (hyprolose), hypromellose (hydroxypropyl methylcellulose), macrogol glyceryl hydroxystearate, microcrystalline cellulose, sodium stearyl fumarate, sodium aluminosilicate, propyl gallate;
- shell composition: hypromellose, carnauba wax, titanium dioxide (E171), macrogol 6000; iron dye yellow oxide (for tablets 2.5 mg); dye iron oxide reddish brown, dye iron oxide yellow (for tablets 5 and 10 mg).
Pharmacological properties
Plendil is a slow calcium channel blocker, a drug for the treatment of hypertension and stable angina pectoris.
Pharmacodynamics
The active ingredient in Plendil, felodipine, is a dihydropyridine derivative in the form of a racemic mixture. The hypotensive effect of felodipine is due to a decrease in the total peripheral vascular resistance, especially in the arterioles. By acting on the calcium channels of cell membranes, conductivity and contractility of vascular smooth muscles are suppressed. The high selectivity of felodipine in relation to the smooth muscles of the arterioles avoids the negative inotropic effect of its therapeutic doses on the contractility or conduction of the heart. The substance relaxes the smooth muscles of the respiratory tract, has a slight effect on the motility of the gastrointestinal tract. Against the background of long-term drug therapy, there is no clinically significant change in blood lipids. The biochemical blood index for glycated hemoglobin (HbA1c) in patients with type 2 diabetes mellitus after taking felodipine for 6 months does not reveal clinically significant metabolic disorders. The use of Plendil is indicated for bronchial asthma, concomitant standard therapy for reduced left ventricular function, diabetes mellitus, hyperlipidemia or gout.
In hypertensive patients, blood pressure (BP) is effectively reduced at rest and during exercise, in the supine, sitting and standing positions. Felodipine does not affect adrenergic vasomotor control or venous smooth muscle, therefore it does not contribute to the development of orthostatic hypotension. At the beginning of the use of felodipine, as a result of a decrease in blood pressure, a temporary reflex increase in heart rate (heart rate) and cardiac output is possible. Simultaneous reception of beta-blockers prevents an increase in heart rate. The effect of felodipine on peripheral vascular resistance and blood pressure correlates with its plasma concentration. The clinical effect at an equilibrium state of the plasma concentration of the drug lasts for 24 hours.
Reception of Plendil promotes regression of left ventricular hypertrophy. Felodipine has no potassium uretic effect, but has a diuretic and natriuretic effect. The lack of retention of salts and fluid in the body against the background of its intake is explained by a decrease in tubular reabsorption of sodium and water. Reduced vascular resistance in the kidneys, increased renal perfusion. Felodipine has no effect on glomerular filtration and albumin excretion.
The results of the studies showed that with mild and moderate severity of arterial hypertension, the use of Plendil in combination with angiotensin-converting enzyme (ACE) inhibitors, beta-blockers and / or diuretics caused a decrease in diastolic blood pressure below 90 mm Hg. Art. in 93% of patients.
In arterial hypertension, the use of Plendil is indicated both as monotherapy and in combination with other antihypertensive drugs, including beta-blockers, diuretics or ACE inhibitors.
The use of felodipine promotes dilatation of the coronary vessels, which leads to an improvement in the blood supply to the myocardium. Decrease in peripheral vascular resistance reduces the load on the heart and reduces myocardial oxygen demand. Plendil relieves spasm of the coronary vessels.
The use of felodipine with stable exertional angina provides an improvement in contractility, reducing the frequency of angina attacks. The therapeutic effect occurs after 2 hours and lasts for 24 hours. For the treatment of stable angina, Plendil can be taken alone or in combination with beta-blockers. At the beginning of the course, the patient may experience an increase in heart rate. this condition is temporary, but if necessary, the doctor may additionally prescribe beta-blockers.
Pharmacokinetics
After taking Plendil inside, the maximum concentration (Cmax) of felodipine in the blood plasma is reached after 3-5 hours. Its systemic bioavailability does not depend on food intake and is about 15%. The degree of absorption is also independent of the diet and remains stable. Taking the tablets with meals only changes the rate of absorption, causing an increase in Cmax by about 65%.
The binding of felodipine to plasma proteins is determined at 99%.
Vd (volume of distribution) at equilibrium is 10 l / kg.
Felodipine is metabolized in the liver, its metabolites have no hemodynamic activity.
T 1/2 (half-life) is about 25 hours, a plateau phase is reached within about 5 days. Long-term use of Plendil does not cause cumulation.
Approximately 70% of the dose taken is excreted through the kidneys in the form of metabolites, and 30% through the intestines. Less than 0.5% is excreted unchanged in the urine.
The total plasma clearance is 1200 ml / min on average. With reduced liver function or in elderly patients, a decrease in clearance causes an increase in the concentration of felodipine in the blood plasma. It should be borne in mind that the patient's age affects only partially the individual variability of the plasma concentration of felodipine.
In case of impaired renal function, accumulation of inactive metabolites is noted, the level of felodipine concentration in plasma does not change. Felodipine is not excreted during hemodialysis.
Indications for use
The use of Plendil is indicated for the treatment of arterial hypertension and stable angina pectoris.
Contraindications
Absolute:
- unstable angina;
- dynamic stenosis of the outflow tract of the heart;
- hemodynamically significant stenosis of the heart valves;
- heart failure in the stage of decompensation;
- acute myocardial infarction;
- lactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to the components of the drug.
It is recommended to prescribe Plendil tablets with caution to patients in whom arterial hypotension can cause myocardial ischemia, with aortic stenosis, blood pressure lability, heart failure after acute myocardial infarction, severe renal failure with creatinine clearance (CC) less than 30 ml / min, impaired liver function, as well as in old age.
Plendil, instructions for use: method and dosage
Plendil tablets are taken orally, swallowing whole (the integrity of the film shell must not be allowed to break) and washed down with water. The drug is taken in the morning on an empty stomach or simultaneously with a small amount of food low in carbohydrates and fats.
The dose selection is made individually.
Recommended daily dosage of Plendil:
- arterial hypertension: initial and maintenance dose - 5 mg. In the absence of the desired clinical effect, you can increase the dose or prescribe an additional intake of a beta-blocker, an ACE inhibitor or a diuretic. The maximum dose is 10 mg;
- stable angina pectoris: the initial dose is 5 mg, if necessary, it can be increased to 10 mg. Combined therapy with beta-blockers is shown.
In case of impaired liver function or in old age, a dose of 2.5 mg is considered optimal.
In case of impaired renal function, correction of the Plendil dosage regimen is not required.
Side effects
- from the nervous system: often - headache; infrequently - paresthesia, dizziness;
- from the heart: infrequently - palpitations, tachycardia;
- from the side of the vessels: often - hot flashes, redness of the face; infrequently - tachycardia as a result of a pronounced decrease in blood pressure (in some cases, more frequent attacks or the occurrence of angina pectoris); rarely - fainting; very rarely - extrasystole;
- from the endocrine system: very rarely - hyperglycemia;
- from the gastrointestinal tract: infrequently - abdominal pain, nausea; rarely - vomiting; very rarely - gingivitis, hyperplasia of the mucous membrane of the gums and tongue;
- from the hepatobiliary system: very rarely - an increase in the activity of hepatic enzymes in the blood serum;
- dermatological reactions: infrequently - itching, exanthema; rarely - urticaria; very rarely - leukocytoclastic vasculitis, increased photosensitivity;
- from the musculoskeletal and connective tissue: rarely - myalgia, arthralgia;
- from the urinary system: very rarely - frequent urination;
- from the genitals and mammary gland: rarely - sexual dysfunction, impotence;
- general disorders: very often - peripheral edema (including mild to moderate ankle edema); infrequently - fatigue; very rarely - hypersensitivity reactions (including fever, angioedema of the lips or tongue).
In the course of clinical studies and post-marketing use, the following side effects have been registered, the causal relationship of which with Plendil's reception has not been precisely established:
- from the side of the cardiovascular system: arterial hypotension, arrhythmia, syncope, angina pectoris, extrasystole, myocardial infarction;
- from the endocrine system: gynecomastia;
- from the gastrointestinal tract: dry mouth, flatulence, diarrhea;
- from the side of the blood: anemia;
- from the nervous system: insomnia, drowsiness, anxiety disorders, irritability, nervousness, depression;
- from the musculoskeletal and connective tissue: myalgia, arthralgia, back pain, pain in the upper and lower extremities, muscle pain;
- from the respiratory system: shortness of breath, bronchitis, pharyngitis, flu, epistaxis, sinusitis;
- from the kidneys and urinary tract: dysuria, polyuria;
- dermatological reactions: bruising, leukocytoclastic vasculitis, erythema;
- on the part of the organ of vision: visual disturbances;
- general disorders: chest pain, flu-like syndrome, facial swelling.
Overdose
Symptoms of an overdose of felodipine after taking a high dose of Plendil inside are: a pronounced decrease in blood pressure, bradycardia, tachycardia, ventricular extrasystole, AV block (atrioventricular block) I – III degree, atrioventricular dissociation, ventricular fibrillation, asystolation. There may be headache, impaired consciousness (including coma), dizziness, convulsions, shortness of breath, pulmonary edema, and apnea. In case of an overdose in adults, reddening of the face, accompanied by hot flashes, the appearance of nausea, vomiting, hypothermia, the development of acidosis, hypokalemia, hyperglycemia, hypocalcemia, and respiratory distress syndrome is possible.
Intoxication usually manifests itself after 12-16 hours; severe toxicity may occur after 48 hours.
Treatment: before gastric lavage, due to the increased risk of stimulating the vagus nerve, atropine is immediately administered intravenously (adults - at a dose of 0.25-0.5 mg, children - at the rate of 0.01-0.02 mg per 1 kg of body weight body). Then you should wash the stomach, even in cases of a late stage of intoxication, the appointment of activated carbon. The greatest risk in case of overdose is represented by violations of the cardiovascular system, therefore, an electrocardiogram (ECG) control, correction of the acid-base state and serum electrolytes are required. If necessary, measures are taken to ensure airway patency and adequate ventilation. With bradycardia and AV blockade, intravenous administration of atropine is indicated: for adults - 0.5–1 mg; children - 0.02-0,05 mg per 1 kg of body weight (including repeatedly according to clinical indications) or isoprenaline in appropriate doses. At an early stage of acute intoxication, it is possible to use an artificial pacemaker. To correct a pronounced decrease in blood pressure, infusion of a liquid, a solution of calcium gluconate is indicated. Calcium gluconate (9 mg / ml) is administered within five minutes for adults at a dose of 20-30 ml, for children in the form of an infusion at the rate of 3-5 mg of calcium gluconate per 1 kg of body weight. To achieve a therapeutic effect, the injections can be repeated at the same dose. In case of convulsions, the patient should be prescribed diazepam. If necessary, an infusion of epinephrine (adrenaline) or dopamine is indicated, in case of acute intoxication - glucagon. In case of cardiac arrest, resuscitation is required. After the obligatory measures, careful monitoring of the patient's condition is carried out and the appointment of symptomatic treatment.
special instructions
At the beginning of the use of Plendil or with an increase in the dose, patients may experience weakness, headache, dizziness, facial flushing, hot flashes, palpitations. In most cases, the listed reactions are transient and do not require revision of the drug dosage regimen.
Influence on the ability to drive vehicles and complex mechanisms
Due to the fact that the initiation of therapy or an increase in the dose may be accompanied by undesirable phenomena in the form of dizziness and weakness, patients are advised to temporarily refrain from those activities that require increased concentration of attention and / or high speed of psychomotor reactions.
During the period of treatment with Plendil, the risk of developing adverse events when driving or working with complex mechanisms should be taken into account.
Application during pregnancy and lactation
To date, there is not enough information about felodipine therapy during gestation. According to the results of studies of the effect of the drug on pregnancy in animals, a violation of the development of the fetus was revealed, and therefore felodipine should not be prescribed during pregnancy.
Slow calcium channel blockers are able to attenuate uterine contractions in the case of preterm labor, while there are insufficient reports to support prolongation of physiological labor.
The presence of arterial hypotension in the mother helps to reduce perfusion in the uterus due to redistribution of blood flow and peripheral vasodilation, which increases the likelihood of fetal hypoxia.
Felodipine passes into breast milk during lactation. During the intake of therapeutic doses of Plendil, a small amount of the substance is released in breast milk, which does not exclude the risk of the drug's effect on infants. Therefore, it is not recommended to prescribe felodipine to women during lactation. When continuation of therapy is necessary to achieve clinical effect, the physician should consider discontinuing breastfeeding.
Pediatric use
The appointment of Plendil for the treatment of patients under the age of 18 is contraindicated due to the limited experience of its use in pediatrics.
With impaired renal function
Plendil should be used with caution in patients with severe renal insufficiency (CC less than 30 ml / min).
In case of impaired renal function, correction of the dosage regimen is not required.
For violations of liver function
Plendil should be used with caution if liver function is impaired. The recommended daily dosage is 2.5 mg.
Use in the elderly
With caution, Plendil should be prescribed to elderly patients. The recommended daily dosage is 2.5 mg.
Drug interactions
- phenytoin, carbamazepine, rifampicin, phenobarbital, tincture of St. John's wort: being inducers of the cytochrome P 450 system, they increase the metabolism of felodipine, so it is recommended to avoid combination with drugs that induce the isoenzyme CYP3A4;
- itraconazole, ketoconazole (antifungal agents, derivatives of triazole and imidazole), erythromycin and other antibiotics of the macrolide group, inhibitors of HIV proteases, grapefruit juice: being inhibitors of the cytochrome P 450 system, they contribute to a significant increase in Cmax of felodipine in the blood plasma; therefore, such combinations should not be allowed;
- cyclosporine: it is important to take into account the possible increase in Cmax of felodipine by 1.5 times, while there is a minimal effect on the pharmacokinetic parameters of cyclosporine;
- cimetidine: concomitant therapy with cimetidine leads to an increase in Cmax of felodipine by 55%;
- tacrolimus: tacrolimus dose adjustment may be required due to an increase in its concentration in blood plasma.
Analogs
The analogues of Plendil are: Felodipine, Felodipin-SZ, Felodip, Felotenz retard and others.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Plendil
The few reviews about Plendil are positive. Patients with poor tolerance to other antihypertensive drugs report that treatment with the drug does not cause these problems.
Price for Plendil in pharmacies
The price of Plendil per pack containing 30 film-coated tablets of prolonged action is:
- dosage 2.5 mg - 412 rubles;
- dosage 5 mg - 545 rubles;
- dosage 10 mg - 797 rubles.
Plendil: prices in online pharmacies
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Drug name Price Pharmacy |
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Plendil 5 mg film-coated tablets of prolonged action 30 pcs. 365 RUB Buy |
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Plendil 10 mg film-coated tablets of prolonged action 30 pcs. 829 RUB 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!
