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Felodipine


Felodipine
Systematic (IUPAC) name
ethyl methyl 4-(2,3-dichlorophenyl)-1,4-dihydro -2,6-dimethyl-3,5- pyridinedicarboxylate
Identifiers
CAS number	72509-76-3
ATC code	C08CA02
PubChem	3333
DrugBank	APRD00374
Chemical data
Formula	C₁₈H₁₉Cl₂N O₄
Mol. mass	383.069 g/mol
Pharmacokinetic data
Bioavailability	>95% ^[1]
Metabolism	Hepatic
Half life	??
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status	℞ Prescription only
Routes	Oral

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.

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Interactions

Recent findings have suggested that felodipine in combination with grapefruit juice can cause abnormal (toxic) effects. Oral administration of Felodipine is first metabolized in the gastrointestinal tract (GI) and liver by CYP3A4. Grapefruit juice is found to have an inhibiting effect over cytochrome P450 3A4. As a result the bioavailability of the drug and area under the curve (AUC) increase, increasing the risk for abnormal side effects. Therefore, special caution must be taken when mixing grapefruit juice with Felodipine.

References

^ Blychert E. (1992). "Felodipine pharmacokinetics and plasma concentration vs effect relationships". Blood Press Suppl. 2: 1-30.

v • d • e Calcium channel blockers (C08)
Dihydropyridines	Amlodipine • Felodipine • Isradipine • Lacidipine • Lercanidipine • Nicardipine • Nifedipine • Nimodipine • Nisoldipine • Nitrendipine
Phenylalkylamines	Verapamil
Benzothiazepines	Diltiazem