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Felodipine

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Title: Felodipine  
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Subject: AstraZeneca, Nicardipine, Grapefruit–drug interactions, Calcium channel blocker, ATC code C08
Collection: Calcium Channel Blockers, Carboxylate Esters, Chloroarenes, Dihydropyridines, Organochlorides
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Felodipine

Felodipine
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
MedlinePlus
Pregnancy
category
  • US: C (Risk not ruled out)
Legal status
  • (Prescription only)
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability 15%[1]
Metabolism Hepatic
Onset of action 2.5–5 hours
Biological half-life 25 hours[2]
Excretion Renal
Identifiers
CAS Registry Number  Y
ATC code C08
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  Y
Chemical data
Formula C18H19Cl2NO4
Molecular mass 384.259 g/mol
 Y   

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.

References

  1. ^ AstraZeneca MI Department, 16 April 2010.
  2. ^ https://www.medicines.org.uk/emc/medicine/191/SPC/Plendil+2.5mg,+Plendil+5mg+and+Plendil+10mg/
  3. ^ Jawad Kiani, Sardar Z Imam (October 30, 2007). "Medicinal importance of grapefruit juice and its interaction with various drugs". Nutr J. 6 (33): 33.  .
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