Article: 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	C18H19Cl2NO4[1]
Mol. weight	383.0691
Pharmacokinetic data
Bioavailability	>95% [2]
Metabolism	Hepatic
Half life	??
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C: USA
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.

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 de curve (AUC) increase, increasing the risk for abnormal side effects. Therefore, special caution must me taken when mixing Grapefruit Juice with Felodipine.

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