Felodipin-Natrapharm

Felodipin-Natrapharm

felodipine

Manufacturer:

Natrapharm

Distributor:

Natrapharm
Full Prescribing Info
Contents
Felodipine.
Action
Pharmacology: Pharmacodynamics: Felodipine is a calcium antagonist of the dihydropyridine class of calcium channel blockers. Calcium antagonist interfere with the voltage-dependent-L-type (slow) calcium channels in the plasma membranes of smooth muscle cells and reduce the inflow of calcium ions with the result of vasodilator. Felodipine is a vasoselective calcium antagonist, it has a much greater selectivity for vascular smooth muscle than for myocardial muscles. Felodipine selectively dilates arterioles with no effect on venous vessels.
Felodipine leads to a dose-related lowering blood pressure via vasodilatation and consequently a reduction of peripheral vascular resistance; it reduces both systolic and diastolic blood pressure. The hemodynamic effect of felodipine is accompanied by a reflex (baroreceptor-mediated) tachycardia. In therapeutic doses, felodipine has no direct effect on either cardiac contractility or cardiac conduction. Felodipine reduces renal vascular resistance. The glomerular filtration rate remains unchanged.
Pharmacokinetics: Felodipine is rapidly and completely absorbed following oral administration. Peak plasma levels are reached with the prolonged release formulation after 3-5 hrs. Constant levels are achieved approximately 3 days after starting treatment. Due to an extensive first-pass effect, only approximately 15% of the administered dose is systemically available.
The plasma protein-binding of felodipine is >99%. The volume of distribution is 10 L/kg, so that felodipine is rapidly distributed in extravascular tissue. Felodipine is extensively metabolized in the liver. No unchanged parent substance is detectable in the urine. The inactive hydrophilic metabolites formed by hepatic biotransformation are mainly eliminated renally (to approximately 70%) and the remainder is excreted in the feces. Felodipine is eliminated in several phases. Approximately 50% of the administered dose is excreted with a half-life (t½) of 4 hrs and the mean terminal t½ is 18 hrs. The mean plasma clearance is 1,100 mL/L and depends on the hepatic blood flow. Elevated plasma concentrations have been measured in patients with impaired hepatic functions and in elderly patients. Renal impairment does not affect the pharmacokinetics of felodipine, although accumulation of inactive metabolites occurs in renal failure. The bioavailability of felodipine is affected by the simultaneous ingestion of fatty food (increase in plasma level).
Indications/Uses
Treatment of hypertension. It may be used alone or concomitantly with other antihypertensive agents.
Dosage/Direction for Use
Unless prescribed otherwise, the following dosage regimen is recommended: Treatment should always be started with 5 mg (equivalent to two felodipine 2.5-mg tablets) once daily.
Lower strengths of this drug are available to achieve this starting dose. Dosage may be increased to 10 mg (equivalent to four felodipine 2.5-mg or two felodipine 5-mg tablets) once daily.
At least 2 weeks should have elapsed before dosage is increased. Maximum Dosage: 10 mg.
Elderly: Elderly patients in particular are recommended a starting dose of 2.5 mg once daily. Dose increase should be made with particular caution.
Hepatic Impairment: Patients with mild to moderate impairment of liver function should start treatment with 2.5 mg once daily. Dose increases should be made only after critically weighing the effects and side effects of felodipine.
Missed Dose: If a dose is missed or less than prescribed dose is taken, the dose should be taken as soon as remembered and therapy should be continued as prescribed on the following day. Never double the dose to make up for a missed dose.
Discontinuation and Duration of Therapy: Treatment should not be interrupted or stopped prematurely without consulting the doctor beforehand. Abrupt discontinuation of the drug may produce life-threatening blood pressure increase (hypertensive crisis) in isolated instances.
The duration of therapy will be decided by the treating doctor.
Administration: The tablets should be taken in the morning with a sufficient amount of liquid (eg, a glass of water, juice but not grapefruit juice). The tablets should be swallowed whole and neither chewed nor divided. The tablets should not be taken with a high-fat meal.
Overdosage
The main manifestation that might be expected is excessive peripheral vasodilation with marked hypotension and in rare cases bradycardia. The therapeutic measure should include elimination of the active ingredient and reconstitution of stable cardiovascular conditions. If hypotension occurs, symptomatic treatment should be provided; the patient should be placed supine with the legs elevated, in case of accompanying bradycardia, atropine (0.5-1 mg) should be given IV. Additional fluid administration should only be initiated if under hemodynamic control to avoid cardiac overload. Sympathomimetic drugs with predominant effect on the α-adrenoreceptor may also be given.
Felodipine is dialysable to a minimal extent (approximately 9%).
Contraindications
Hypersensitivity to felodipine or to any of the excipients of Felodipin-Natrapharm.
Felodipine must not be taken by patients with any of the following conditions: Stroke within the last 6 months, cardiovascular shock, valvular heart disease (higher-grade aortic or mitral stenosis), heart muscle disease with narrowing of the cardiac cavity (hypertrophic obstructive cardiomyopathy), unstable angina pectoris, acute myocardial infarction (within the last 8 weeks), higher-grade disturbances of impulse conduction from the atria to the ventricles of the heart (2nd and 3rd degree AV block), congestive heart failure, severe impairment of liver and kidney function [renal insufficiency: glomerular filtration rate (GFR) <30 mL/min; creatinine >1.8 mg/dL], pregnancy.
Use in pregnancy: Felodipine is contraindicated during the entire duration of pregnancy, as animal experiments have demonstrated fetal damage. Pregnancy must be excluded before starting treatment with Felodipine.
Special Precautions
Felodipine should be used with caution in patients with conduction disorders, heart failure, tachycardia and hemodynamically relevant aortic and/or mitral valve stenosis; mild to moderate hepatic impairment, as the antihypertensive effect may be enhanced; if treatment with felodipine is discontinued abruptly, a hypertensive crisis may occur in individual cases.
Effects on the Ability to Drive or Operate Machinery: Treatment of essential hypertension with felodipine requires regular medical monitoring. Individually, different reactions may alter alertness to such an extent that the ability to actively participate in road traffic, operate machines or work without a firm support is impaired. This applies especially at the start of therapy, when increasing the dose, switching medications or using alcohol at the same time.
Use in lactation: Felodipine is excreted in breast milk. If the breastfeeding mother is taking therapeutic doses of felodipine, a fully breastfed infant absorbs only a very low dose of the active substance with the breast milk. There exists no experience concerning the risk for the infant.
Use in children: Felodipine should not be used in children because safety has not been established.
Use In Pregnancy & Lactation
Use in pregnancy: Felodipine is contraindicated during the entire duration of pregnancy, as animal experiments have demonstrated fetal damage. Pregnancy must be excluded before starting treatment with Felodipine.
Use in lactation: Felodipine is excreted in breast milk. If the breastfeeding mother is taking therapeutic doses of felodipine, a fully breastfed infant absorbs only a very low dose of the active substance with the breast milk. There exists no experience concerning the risk for the infant.
Side Effects
Frequently, flushing, headache or tinnitus may occur, particularly at the beginning of treatment, when the dose is increased or when high doses are administered.
Occasionally, peripheral edema occurs; particularly at the beginning of treatment, angina pectoris attacks may occur or in patients with preexisting angina pectoris, there may be an increase in the frequency, duration and severity of the attacks. Myocardial infarction has been reported in isolated cases.
Dizziness, fatigue, hypotension, syncope, palpitation, tachycardia and dyspnea, restlessness, paresthesia, tremors, myalgia, arthralgia, gastrointestinal complaints (eg, nausea, vomiting, diarrhea, constipation), weight gain, sweating, pollakisuria, skin and hypersensitivity reactions eg, pruritus, urticaria and rash have been observed rarely. Very rarely, leukocytoclastic vasculitis and photosensitization.
Felodipine treatment may lead to gingival hyperplasia and gingivitis in rare cases.
In individual cases, hepatic function disorders (elevated transaminase levels), exfoliative dermatitis, angioedema and fever were observed.
In individual cases, erection disorders and gynecomastia have been reported.
Drug Interactions
The blood pressure-lowering effect of felodipine may be increased by other blood pressure-lowering drugs and by certain (tricyclic) antidepressants. The breakdown of felodipine involves a certain enzyme system in the liver (cytochrome P450 3A4). Concurrently, administered drugs interfere with this enzyme system may therefore, interact with felodipine to produce increased blood levels of felodipine when medicinal products that contain such drugs as cimetidine, erythromycin, itraconazole or ketoconazole are used at the same time. Grapefruit, which contains enzyme-inhibiting flavonoids, can also increase the plasma level of felodipine; reduced blood levels of felodipine when medicinal products that contain such drugs as carbamazepine, phenytoin or barbiturates are used at the same time. Please bear in mind that these precautions may also apply to recently used medicines.
Storage
Store at temperatures not exceeding 25°C.
MIMS Class
ATC Classification
C08CA02 - felodipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
Presentation/Packing
Tab 5 mg x 100's.
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