Felodipine
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Felodipine
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| Systematic (IUPAC) name | |
| ethyl methyl 4-(2,3-dichlorophenyl)-1,4-dihydro -2,6-dimethyl-3,5- pyridinedicarboxylate |
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| Identifiers | |
| CAS number | |
| ATC code | C08 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C18H19Cl2NO4 |
| 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. The formulation patent for the substance expired in 2007.
[edit] 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.[2]
[edit] References
- ^ Blychert E. (1992). "Felodipine pharmacokinetics and plasma concentration vs effect relationships". Blood Press Suppl. 2: 1-30.
- ^ Jawad Kiani, Sardar Z Imam (October 30 2007). "Medicinal importance of grapefruit juice and its interaction with various drugs". Nutr J. 6 (33): 33. doi:. PMID 17971226.
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