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felodipine (Plendil)
Tradename: Plendil.
Indications:
- hypertension
- angina pectoris
- Prinzmetal angina
- left ventricular diastolic dysfunction
- Raynaud's phenomenon
Contraindications:
-> NOT for use in controlling ventricular response to atrial fibrillation
a) does NOT block AV nodal conduction
b) increases AV nodal conduction
Dosage: start: 2.5-5 mg PO QD, max 10 mg QD.
Tabs: 2.5, 5, 10 mg. Do NOT crush, split or chew tablets!
Pharmacokinetics:
1) oral bioavailability is about 20%
2) significant 1st pass metabolism
3) > 99% of drug bound to plasma proteins
4) metabolized in the liver by cyt P450 3A4
-> 6 inactive metabolites are excreted in the urine
5) elimination 1/2life is 11-16 hours
Adverse effects:
1) headache
2) flushing
3) dizziness
4) nausea
5) heartburn
6) muscle cramps
7) peripheral edema
8) hypotension
Drug interactions:
1) barbiturates decrease felodipine bioavailability
2) erythromycin increases pharmacologic effect of felodipine
3) beta-blockers increase adverse effects of felodipine
4) carbamazepine in combination increases carbamazepine levels & decreases felodipine levels
5) grapefruit increases absorption of felodipine (40%)
6) digoxin levels may be increased by felodipine
7) any drug that inhibits cyt P450 3A4 may increase levels of felodipine
8) any drug that induces cyt P450 3A4 may diminish levels of felodipine
Mechanism of action:
1) dihydropyridine Ca+2 channel blocker
2) decreases peripheral vascular resistance
3) slightly increases heart rate, contractility & AV nodal conduction
Interactions
drug interactions
drug adverse effects (more general classes)
Related
cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
General
calcium channel blocker (CCB)
dihydropyridine
Properties
MISC-INFO: elimination route LIVER
1/2life 11-16 HOURS
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Deprecated Reference
Component-of
enalapril/felodipine (Lexxel)