P - Contraindicated in pregnancy
L - Caution when used during lactation
FI - Food *
Felodipine is a calcium channel blocker (calcium antagonist), a drug used to control hypertension (high blood pressure). It is marketed with the brand name Plendil by AstraZeneca. The formulation patent for the substance expired in 2007. AstraZeneca dropped Plendil from its support and AZ&Me free Rx access program in October 2008.
Felodipine relaxes coronary vascular smooth muscles by inhibiting calcium ions from entering the 'slow channels' or voltage-sensitive areas of vascular smooth muscles and myocardium during depolarisation. It also increases myocardial O2 delivery in patients with vasospastic angina.
Absorption Almost completely absorbed from the GI tract (oral).
Distribution Protein-binding: 99%.
Metabolism Gut and liver (extensive 1st pass effect).
Excretion Via urine (70% as metabolites), via faeces (remaining dose); 11-16 hr (elimination half-life).
Information Not Available
Flushing, headache, peripheral oedema, tachycardia, palpitation, dizziness, fatigue. Ankle swelling may occur. Hyperplasia, rash, pruritus. Gingival enlargement, angina, angioedema, decreased libido, insomnia, irritability in patients with pronounced gingivitis or periodontitis.
Monitor Monitor BP during dosage adjustments, especially in the elderly and those with hepatic function impairment. Hepatic Function May have elevated felodipine plasma concentrations and may respond to lower doses. Heart Failure Use with caution, especially in combination with a beta-blocker. Hypotension May occasionally precipitate significant hypotension and, rarely, syncope. Reflex tachycardia may occur, which may precipitate angina pectoris in susceptible patients. Overdosage Symptoms Excessive peripheral vasodilation with marked hypotension, bradycardia.
Impaired renal or hepatic function, CHF, sick-sinus syndrome, severe left ventricular dysfunction, hypertrophic cardiomyopathy. May cause hypotension with reflex tachycardia resulting in MI in susceptible patients; severe liver disease. Elderly, children. Lactation.
Increased absorption with ethanol. Plasma levels increased by enzyme inhibitors e.g. cimetidine. Plasma levels reduced by enzyme inducers e.g. phenytoin, carbamazepine and barbiturates. Potentially Fatal: Additive hypotensive effect with sildenafil and vardenafil. Increased conc with ciclosporin. Increases plasma digoxin concentrations by approximately 40%.
Food Interaction Grapefruit juice significantly increase bioavailability. High fat and carbohydrate meals.
Oral Hypertension Adult: As modified-release preparation: Initially, 5 mg once daily in the morning, adjust dose according to patient's response. Maintenance: 2.5-10 mg daily. Up to 20 mg daily may be used if needed. Renal impairment: Dose reduction may be required. Oral Angina pectoris Adult: Initially, 5 mg daily, increased to 10 mg daily if necessary. Renal impairment: Dose reduction may be required.
May be taken with or without food. (Take without food or w/ a light meal.)
Contraindicated in pregnancy Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Caution when used during lactation
Safety and efficacy not established
Consider starting at low end of dosing range, reflecting the higher frequency of decreased hepatic, renal, or cardiac function, and comorbidity.
Oral Store below 30℃
Oral Store below 30℃