Felodipine Sandoz 5 mg contains felodipine 5 mg in a slow release tablet.
Felodipine Sandoz 10 mg contains felodipine 70 mg in a slow release tablet.
Pharmacotherapeutic group: Calcium channel blockers, selective calcium channel blockers with mainly vascular effects, dihydropyridine derivatives.
Pharmacology: Pharmacodynamics: Felodipine is a vascular selective calcium antagonist, which lowers arterial blood pressure by decreasing systemic vascular resistance. Due to the high degree of selectivity for smooth muscle in the arterioles, felodipine in therapeutic doses has no direct effect on cardiac contractility or conduction. Because there is no effect on venous smooth muscle or adrenergic vasomotor control, felodipine is not associated with orthostatic hypotension.
Felodipine Sandoz is effective in all grades of hypertension. It can be used as monotherapy or in combination, e.g. with beta-receptor blockers or diuretics.
Felodipine Sandoz has antianginal and antiischemic effects due to improved myocardial oxygen supply/demand balance. Coronary vascular resistance is decreased and coronary blood flow as well as myocardial oxygen supply are increased by Felodipine Sandoz due to dilatation of both epicardial arteries and arterioles. Felodipine Sandoz effectively counteracts coronary vasospasm. The reduction in systemic blood pressure caused by Felodipine Sandoz leads to decreased left ventricular afterload.
Felodipine Sandoz improves exercise tolerance and reduces anginal attacks in patients with stable effort induced angina pectoris. Both symptomatic and silent myocardial ischemia are reduced by felodipine in patients with vasospastic angina.
Felodipine Sandoz can be used as monotherapy or in combination with β-receptor blockers in patients with stable angina pectoris.
Felodipine possesses a mild natriuretic/diuretic effect and fluid retention does not occur.
Felodipine Sandoz is generally well tolerated, also in patients with concomitant diseases such as congestive heart failure, asthma, diabetes, gout, hyperlipidemia, and Raynaud's diseases.
Paediatric population: There is limited clinical trial experience of the use of felodipine in hypertensive paediatric patients. In a randomised, double-blind, 3-week, parallel group study in children aged 6-16 years with primary hypertension, the antihypertensive effects of once daily felodipine 2.5 mg (n=33), 5 mg (n=33) and 10 mg (n=31) were compared with placebo (n=35). The study failed to demonstrate the efficacy of felodipine in lowering blood pressure in children aged 6-16 years.
The long-term effects of felodipine on growth, puberty and general development have not been studied. The long-term efficacy of antihypertensive therapy as therapy in childhood to reduce cardiovascular morbidity and mortality in adulthood has also not been established.
Pharmacokinetics: Absorption: Felodipine is administered as extended-release tablets, from which it is completely absorbed in the gastrointestinal tract. The systemic availability of felodipine is approximately 15% and is independent of dose in the therapeutic dose range. The extended-release tablets produce a prolonged absorption phase of felodipine. This results in even felodipine plasma concentrations within the therapeutic range for 24 hours. Maximum blood plasma levels (tmax) are achieved with the prolonged-release form after 3 to 5 hours. The rate but not the extent of absorption of felodipine is increased when taken simultaneously with food with a high fat content.
Distribution: The plasma protein binding of felodipine is approximately 99%. It is bound predominantly to the albumin fraction. Volume of distribution at steady state is 10 l/kg.
Biotransformation: Felodipine is extensively metabolised in the liver by cytochrome P450 3A4 (CYP3A4) and all identified metabolites are inactive. Felodipine is a high clearance medicinal product with an average blood clearance of 1200 ml/min. There is no significant accumulation during long-term treatment.
Elderly patients and patients with reduced liver function have on average higher plasma concentrations of felodipine than younger patients. The pharmacokinetics of felodipine is not changed in patients with renal impairment, including those treated with haemodialysis.
Elimination: The half-life of felodipine in the elimination phase is approximately 25 hours and steady state is reached after 5 days. There is no risk of accumulation during long-term treatment. About 70% of a given dose is excreted as metabolites in the urine; the remaining fraction is excreted in the faeces. Less than 0.5% of a dose is recovered unchanged in urine.
Linearity/non-linearity: Plasma concentrations are directly proportional to dose within the therapeutic dose range 2.5 - 10 mg.
Hypertension.
Angina Pectoris.
Hypertension: Felodipine Sandoz should be swallowed as a whole and taken together with a sufficient amount of water in the morning. The dose should be adjusted individually. The recommended dose is started with 5 mg once daily. The usual maintenance doses are 5 mg or 10 mg once daily. Depending on the patient's response, the dose can, where applicable, be decreased to 2.5 mg or increased to 10 mg daily. An increase in dosage should be carried out at intervals of at least 2 weeks. In elderly patients an initial treatment with 2.5 mg daily should be considered.
Angina pectoris: The dose should be adjusted individually. Treatment should be started with 5 mg once daily and if needed be increased to 10 mg once daily.
If severe hypotension occurs, symptomatic treatment should be instituted. The patient should be laid in horizontal position with the legs elevated. In case of accompanying bradycardia, 0.5-1.0 mg atropine should be administered intravenously. If this is not sufficient, plasma volume should be increased by infusion e.g. glucose, saline, or dextran. Sympathomimetic drugs with predominant effect on the ∞1 adrenoceptor may be given if the previously mentioned measures are insufficient.
Hypersensitivity to felodipine.
Pregnancy and lactation period.
Severe hepatic function disorders.
The efficacy and safety of felodipine in the treatment of hypertensive emergencies has not been studied.
Concomitant administration of medicinal products that strongly induce or inhibit CYP3 A4 enzymes result in extensively decreased or increased plasma levels of felodipine, respectively. Therefore such combinations should be avoided.
Mild gingival enlargement has been reported in patients with pronounced gingivitis/periodontitis. The enlargement can be avoided or reversed by careful oral hygiene.
Felodipine, like other effective arteriolar dilators, may in rare cases precipitate significant hypotension which in susceptible individuals may result in myocardial ischaemia.
Effects on ability to drive and use machines: Felodipine has minor or moderate influence on the ability to drive and use machines. If patients taking felodipine suffer from headache, nausea, dizziness or fatigue and ability to react may be impaired. Caution is recommended especially at the start of treatment.
Pregnancy: In non-clinical reproductive toxicity studies there were foetal developmental effects, which are considered to be due to the pharmacological action of felodipine.
Breastfeeding: Felodipine has been detected in breast milk, and due to insufficient data on potential effect on the infant, treatment is not recommended during breastfeeding.
Fertility: In a nonclinical reproductive study in the rat, there were effects on foetal development but no effect on fertility at doses approximating to therapeutic.
Summary of the safety profile: Felodipine can cause flushing, headache, palpitations, dizziness and fatigue. Most of these adverse reactions are dose-dependent and appear at the start of treatment or after a dose increase. Should such adverse reactions occur, they are usually transient and diminish with time.
List of adverse reactions: The adverse reactions listed as follows have been identified from clinical trials and from post-marketing surveillance.
Vascular disorders: Common: Flush.
Uncommon: Hypotension.
Rare: Syncope.
If justified: activated charcoal, gastric lavage if performed within one hour after ingestion.
Felodipine is metabolised in the liver by cytochrome P450 3A4 (CYP3A4). Concomitant administration of substances which interfere with CYP3A4 enzyme system may affect plasma concentrations of felodipine.
Interactions leading to increased plasma concentration of felodipine: CYP3A4 enzyme inhibitors have been shown to cause an increase in felodipine plasma concentrations.
Felodipine Cmax and AUC increased 8-fold and 6-fold, respectively, when felodipine was coadministered with the strong CYP3A4 inhibitor itraconazole. When felodipine and erythromycin were coadministered, the Cmax and AUC of felodipine were increased by about 2.5-fold. Cimetidine increased the felodipine Cmax and AUC by approximately 55%. The combination with strong CYP3A4 inhibitors should be avoided.
In case of clinically significant adverse events due to elevated felodipine exposure when combined with strong CYP3A4 inhibitors, adjustment of felodipine dose and/or discontinuation of the CYP3A4 inhibitor should be considered.
Felodipine tablets should not be taken together with grapefruit juice.
Interactions leading to decreased plasma concentration of felodipine: Enzyme inducers of the cytochrome P450 3A4 system have been shown to cause a decrease in plasma concentrations of felodipine.
When felodipine was coadministered with carbamazepine, phenytoin or phenobarbital, the Cmax and AUC of felodipine were decreased by 82% and 96% respectively. The combination with strong CYP3A4 inducers should be avoided.
In case of lack of efficacy due to decreased felodipine exposure when combined with potent inducers of CYP3A4, adjustment of felodipine dose and/or discontinuation of the CYP3A4 inducer should be considered.
C08CA02 - felodipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
SR tab 5 mg x 5 x 10's. 10 mg x 5 x 10's.
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