Felodipine
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| Systematic (IUPAC) name | |
|---|---|
|
(RS)-3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate | |
| Clinical data | |
| Trade names | Plendil |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a692016 |
| Pregnancy category |
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| Routes of administration | Oral |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 15%[1] |
| Metabolism | Hepatic |
| Onset of action | 2.5–5 hours |
| Biological half-life | 25 hours[2] |
| Excretion | Renal |
| Identifiers | |
| CAS Number |
72509-76-3  |
| ATC code | C08CA02 (WHO) |
| PubChem | CID 3333 |
| IUPHAR/BPS | 4190 |
| DrugBank |
DB01023 |
| ChemSpider |
3216 |
| UNII |
OL961R6O2C |
| KEGG |
D00319 |
| ChEBI |
CHEBI:585948 |
| ChEMBL |
CHEMBL1480 |
| Chemical data | |
| Formula | C18H19Cl2NO4 |
| Molar mass | 384.259 g/mol |
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Felodipine is a calcium channel blocker (calcium antagonist), a drug used to control hypertension (high blood pressure). It is marketed under the brand name Plendil by AstraZeneca and Renedil by Sanofi-Aventis. The formulation patent for the substance expired in 2007.
AstraZeneca dropped Plendil from its support and AZ&Me free Rx access program in October 2008.
Interactions
Studies dating back to 1989 have suggested that felodipine in combination with grapefruit juice can cause toxic effects. Oral administration of felodipine is first metabolized in the gastrointestinal tract and liver by the enzyme CYP3A4. Grapefruit juice contains bergamottin which is found to have an inhibiting effect over this enzyme and as a result the bioavailability of the drug increases, raising the risk for abnormal side effects.[3]
Contraindications and cautions
Contraindicated with allergy to felodipine or other calcium channel blockers, sick sinus syndrome, AV heart block (second and third degree), lactation. Use cautiously with pregnancy, impaired hepatic function.
Mechanism
Felodipine is a calcium channel blocker.
Felodipine has additionally been found to act as an antagonist of the mineralocorticoid receptor, or as an antimineralocorticoid.[4]
References
- ↑ AstraZeneca MI Department, 16 April 2010.
- ↑ https://www.medicines.org.uk/emc/medicine/191/SPC/Plendil+2.5mg,+Plendil+5mg+and+Plendil+10mg/
- ↑ 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:10.1186/1475-2891-6-33. PMC 2147024. PMID 17971226. Retrieved 2008-04-09..
- ↑ Luther, James M. (2014). "Is there a new dawn for selective mineralocorticoid receptor antagonism?". Current Opinion in Nephrology and Hypertension 23 (5): 456–461. doi:10.1097/MNH.0000000000000051. ISSN 1062-4821.
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