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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/01/20 06:07:12」(JST)

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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.^[2]

Contraindications and cautions

Contraindicated with allergy to felodipine or other calcium channel blockers, sick sinus syndrome, heart block (second and third degree), lactation. Use cautiously with pregnancy, impaired hepatic function.

Synthesis

Berntsson, P. B.; Carlsson, A. I.; Gaarder, J. O.; Ljung, B. R.; 1981, U.S. Patent 4,264,611.

References

^ AstraZeneca MI Department, 16th April 2010.
^ 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. .

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1. 収縮機能障害による心不全におけるカルシウム拮抗剤 calcium channel blockers in heart failure due to systolic dysfunction
2. カルシウム拮抗剤の主な副作用および安全性 major side effects and safety of calcium channel blockers
3. 安定狭心症のマネージメントにおけるカルシウム拮抗剤 calcium channel blockers in the management of stable angina pectoris
4. 高血圧治療における目標血圧 what is goal blood pressure in the treatment of hypertension
5. レイノー現象に対する初期治療 initial treatment of the raynaud phenomenon

English Journal

Development and validation of TLC-densitometric method for simultaneous determination of two binary antihypertensive mixtures containing felodipine in fixed dose combinations.

Mohamed AI1, Omar MA2, Hammad MA2, Mohamed AA2.
Biomedical chromatography : BMC.Biomed Chromatogr.2015 Jun 10. doi: 10.1002/bmc.3536. [Epub ahead of print]
A new densitometric thin-layer chromatographic method has been developed for simultaneous determination of two binary mixtures containing felodipine in combination with either metoprolol (mixture I) or ramipril (mixture II). The two mixtures were quantitatively separated on 60F254 silica gel plates
PMID 26096877

Thermodynamics of Highly Supersaturated Aqueous Solutions of Poorly Water-Soluble Drugs-Impact of a Second Drug on the Solution Phase Behavior and Implications for Combination Products.

Trasi NS1, Taylor LS1.
Journal of pharmaceutical sciences.J Pharm Sci.2015 Jun 8. doi: 10.1002/jps.24528. [Epub ahead of print]
There is increasing interest in formulating combination products that contain two or more drugs. Furthermore, it is also common for different drug products to be taken simultaneously. This raises the possibility of interactions between different drugs that may impact formulation performance. For poo
PMID 26059413

LB01.06: VISIT-TO-VISIT BLOOD PRESSURE VARIABILITY AND CARDIOVASCULAR OUTCOMES IN FELODIPINE EVENT REDUCTION STUDY.

Zhang Y1, Zhang X, Liu L, Zanchetti A.
Journal of hypertension.J Hypertens.2015 Jun;33 Suppl 1:e46. doi: 10.1097/01.hjh.0000467468.46880.40.
OBJECTIVE: Many antihypertensive outcome trials have shown that visit-to-visit blood pressure variability is correlated closely with clinical outcomes in hypertensive patients. The objective of the study was to investigate the relationship between visit-to-visit blood pressure variability (BPV) and
PMID 26102827

Japanese Journal

nteractions between Grapefruit Juice and Calcium Channel Antagonists

Yonago Acta medica 52(1), 1-9, 2009-03
NAID 110007035312

Relationship between Lipophilicities of 1, 4-Dihydropyridine Derivatives and Pharmacokinetic Interaction Strengths with Grapefruit Juice

藥學雜誌 128(1), 117-122, 2008-01-01
NAID 110006533009

Incidence of gingival overgrowth caused by calcium channel blockers

歯科薬物療法 27(2), 79-85, 2008
NAID 130004040550

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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	monograph
MedlinePlus	a692016
Pregnancy; category	US: C;
Legal status	℞ Prescription only;
Routes	Oral
Pharmacokinetic data
Bioavailability	15%
Metabolism	Hepatic
Half-life	??
Excretion	Renal
Identifiers
CAS number	72509-76-3
ATC code	C08CA02
PubChem	CID 3333
IUPHAR ligand	4190
DrugBank	DB01023
ChemSpider	3216
UNII	OL961R6O2C
KEGG	D00319
ChEBI	CHEBI:585948
ChEMBL	CHEMBL1480
Chemical data
Formula	C18H19Cl2NO4
Molecular mass	384.259 g/mol
	SMILES O=C(OCC)\C1=C(\N/C(=C(/C(=O)OC)C1c2cccc(Cl)c2Cl)C)C;
	InChI InChI=1S/C18H19Cl2NO4/c1-5-25-18(23)14-10(3)21-9(2)13(17(22)24-4)15(14)11-7-6-8-12(19)16(11)20/h6-8,15,21H,5H2,1-4H3 ; Key:RZTAMFZIAATZDJ-UHFFFAOYSA-N ;
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英: felodipine
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[1] AstraZeneca MI Department, 16th April 2010.

[2] 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. .

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felodipine