Trade Names:Plendil- Tablets, extended release 2.5 mg- Tablets, extended release 5 mg- Tablets, extended release 10 mgRenedil (Canada)
Inhibits movement of calcium ions across cell membrane in systemic and coronary vascular smooth muscle, altering contractile process.
Systemic bioavailability is about 20% and T max is 2.5 to 5 h. C max is increased about 60% and AUC is unchanged with a high fat or carbohydrate meal.
Vd is about 10 L/kg and it is more than 99% bound to plasma proteins.
Extensive first pass metabolism; 6 metabolites account for 23% of activity.
The t 1/ 2 is 11 to 16 h; 70% of the drug is eliminated in the urine and 10% in the feces.
2 to 5 h.
24 h (during chronic administration).
About 60% reduction in Cl.Elderly
Plasma concentrations of felodipine increase with age.
Treatment of hypertension.
PO The recommended starting dose is 5 mg once daily. Depending on patient response, the dose can be decreased to 2.5 mg or increased to 10 mg once daily.Elderly and hepatic function impairment
PO Recommended starting dose 2.5 mg once daily.
Store tablets below 86° F. Keep tightly closed. Protect from light.
Felodipine plasma concentrations may be reduced in epileptic patients, decreasing the therapeutic effects. Alternative therapy should be considered.Beta-blockers (eg, metoprolol)
Metoprolol plasma levels may be increased.CYP3A4 inhibitors (eg, cimetidine, erythromycin, grapefruit juice, itraconazole, ketoconazole)
Because of an increase in felodipine bioavailability or decrease in metabolism, felodipine plasma levels may be elevated several-fold, increasing the pharmacologic and adverse effects.Histamine H 2 antagonists (eg, cimetidine)
Felodipine plasma levels may be elevated, increasing the pharmacologic and adverse effects.Other antihypertensive agents
May have additive effects.Tacrolimus
Blood levels of tacrolimus may be elevated, increasing the risk of side effects.
None well documented.
Palpitation (at least 1.5%).
Asthenia, dizziness, headache, paresthesia (at least 1.5%).
Flushing, rash (at least 1.5%).
Rhinorrhea, sneezing (at least 1.5%).
Constipation, dyspepsia, nausea (at least 1.5%).
Cough, upper respiratory infection (at least 1.5%).
Peripheral edema, warm sensation (at least 1.5%).
Monitor BP during dosage adjustments, especially in the elderly and those with hepatic function impairment.
Category C .
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.
May have elevated felodipine plasma concentrations and may respond to lower doses.
Use with caution, especially in combination with a beta-blocker.
May occasionally precipitate significant hypotension and, rarely, syncope. Reflex tachycardia may occur, which may precipitate angina pectoris in susceptible patients.
Excessive peripheral vasodilation with marked hypotension, bradycardia.
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