Each extended release film-coated tablet contains: Felodipine 10 mg.
Pharmacology: Felodipine is a dihydropyridine calcium-channel blocker with actions similar to those of nifedipine. It is used in the treatment of hypertension and angina pectoris. Felodipine is a highly vascular selective calcium antagonist which lowers arterial blood pressure by decreasing systemic vascular resistance. Due to 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 is effective in all grades of hypertension. It can be used as monotherapy or in combination with other antihypertensive drugs eg, β-adrenoceptor blockers, diuretics or ACE inhibitors, in order to achieve an increased antihypertensive effect. Felodipine reduces both systolic and diastolic blood pressure and can be used in isolated systolic hypertension. Felodipine maintains its antihypertensive effect during concomitant therapy with nonsteroidal anti-inflammatory drugs. Felodipine has anti-anginal and anti-ischaemic effects due to improved myocardial oxygen supply/demand balance. Felodipine improves exercise tolerance and reduces anginal attacks in patients with stable effort-induced angina pectoris. Felodipine is effective and well tolerated in adult patients irrespective of age and race and is also well tolerated in the presence of concomitant disease such as congestive heart failure, asthma and other obstructive pulmonary disease, impaired renal function, diabetes, gout, hyperlipidaemia, Raynaud's disease and in renal transplant recipients. Felodipine has no effect on blood glucose levels or lipid profile.
Pharmacokinetics: Felodipine is administered as extended-release tablets from which it is completely absorbed in the gastrointestinal tract. The extended-release film-coated tablets produce a prolonged absorption phase of felodipine. This results in even felodipine plasma concentrations within the therapeutic range for 24 hours. Plasma concentrations are directly proportional to dose within the therapeutic dose range 2.5-10 mg. It is extensively metabolized in the liver and is excreted almost entirely as metabolites about 70% of a dose being excreted in urine and the remainder in faeces. There is no significant accumulation during long-term treatment.
Used in the treatment of hypertension and angina pectoris.
Felodipine is given oral, generally in extended release formulation for administration once daily in the morning. In hypertension, the usual initial dose is 5 mg daily by oral, adjusted as required to a maximum of 20 mg daily, the usual maintenance dose is 5 mg to 10 mg daily. In angina pectoris, the usual dose is 5 mg daily increase if necessary to 10 mg daily. Lower doses may be required in the elderly and in patients with impaired liver function.
Pregnancy; unstable angina; significant aortic stenosis; within 1 month of myocardial infarction; hypersensitivity to felodipine.
Felodipine should not be given during pregnancy.
Felodipine, like other effective arteriolar dilators may in rare cases precipitate significant hypotension, which in susceptible individuals, may result in myocardial ischaemia.
Dosage of felodipine should be adjusted carefully in geriatric patients and in patients with impaired hepatic function; the usual initial dose is 2.5 mg daily in such patients.
Withdraw if ischaemic pain occurs or existing pain worsens shortly after initiating treatment or if cardiogenic shock develops.
Concomitant oral administration of felodipine with grapefruit juice usually should be avoided since it may cause an increase in felodipine plasma concentrations.
Like other arteriolar dilators, felodipine can cause flushing, headache, palpitations, dizziness and fatigue.
Rarely tachycardia, palpitations, syncope.
Vascular (extracardiac): peripheral oedema,
In isolated cases nausea, vomiting.
Rarely rash, pruritus.
Metabolism of felodipine is mediated by the cytochrome P450 (CYP) isoenzyme 3A4 and the possibility exists that drugs that inhibit this isoenzyme (e.g. ketoconazole, itraconazole, erythromycin, grapefruit juice, cimetidine) may increase plasma felodipine concentrations several fold which result in increased cardiac effects (e.g. decreases in blood pressure and increases in heart rate).
The possibility that felodipine may share the drug interaction potential of nifedipine, another 1,4-dihydropyridine derivative, also should be considered and the usual precautions observed.
Store at temperatures not exceeding 30°C.
C08CA02 - felodipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.