Felodipine

From Wikipedia, the free encyclopedia

Felodipine chemical structure
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.


Calcium channel blockers (C08) edit
Dihydropyridines:

Amlodipine, Felodipine, Isradipine, Lacidipine, Lercanidipine, Nicardipine, Nifedipine, Nimodipine, Nisoldipine

Phenylalkylamines:

Verapamil

Benzothiazepines:

Diltiazem

[edit] References

  1. ^ http://www.chemindustry.com/, accessed 11 December, 2005.
  2. ^ Blychert E. (1992). "Felodipine pharmacokinetics and plasma concentration vs effect relationships". Blood Press Suppl. 2: 1-30.
In other languages