Felodipine

(BAN, USAN, rINN)
Felodipine Chemical formula
Synonyms: Felodipiini; Felodipin; Felodipinas; Félodipine; Felodipino; Felodipinum; H-154/82. Ethyl methyl 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate.
Cyrillic synonym: Фелодипин.

💊 Chemical information

Chemical formula: C18H19Cl2NO4 = 384.3.
CAS — 72509-76-3; 86189-69-7.
ATC — C08CA02.
ATC Vet — QC08CA02.

Pharmacopoeias.

In Chin., Eur., and US.

Ph. Eur. 6.2

(Felodipine). A white or light yellow, crystalline powder. Practically insoluble in water; freely soluble in dehydrated alcohol, in acetone, in dichloromethane, and in methyl alcohol. Protect from light.

USP 31

(Felodipine). A light yellow to yellow, crystalline powder. Insoluble in water; freely soluble in acetone and in methyl alcohol; very slightly soluble in heptane. Store in airtight containers. Protect from light.

💊 Adverse Effects, Treatment, and Precautions

As for dihydropyridine calcium-channel blockers.

💊 Interactions

As for dihydropyridine calcium-channel blockers.

💊 Pharmacokinetics

Felodipine is almost completely absorbed from the gastrointestinal tract after oral doses but undergoes extensive first-pass metabolism, with a bioavailability of about 15% (range 10 to 25%). It is extensively metabolised in the gut and the liver and is excreted almost entirely as metabolites, about 70% of a dose being excreted in urine and the remainder in faeces. The terminal elimination half-life is reported to be about 11 to 16 hours after oral dosage with an immediate-release preparation, but longer with a modified-release formulation. Felodipine is about 99% bound to plasma proteins (mainly albumin).
1. Dunselman PHJM, Edgar B. Felodipine clinical pharmacokinetics. Clin Pharmacokinet 1991; 21: 418–30.

💊 Uses and Administration

Felodipine is a dihydropyridine calcium-channel blocker with actions similar to those of nifedipine. It is used in the management of hypertension and angina pectoris. Felodipine is given orally, generally in a modified-release formulation for use once daily in the morning. In hypertension the usual initial dose is 5 mg daily, adjusted as required; the usual maintenance dose is 2.5 to 10 mg daily and doses above 20 mg daily are not usually needed. In angina the usual initial dose is 5 mg daily increased if necessary to 10 mg daily. Lower doses may be required in patients with hepatic impairment (see below) and in the elderly.
1. Todd PA, Faulds D. Felodipine: a review of the pharmacology and therapeutic use of the extended release formulation in cardiovascular disorders. Drugs 1992; 44: 251–77
2. Walton T, Symes LR. Felodipine and isradipine: new calciumchannel-blocking agents for the treatment of hypertension. Clin Pharm 1993; 12: 261–75.

Administration in hepatic impairment.

In 9 patients with liver cirrhosis given felodipine 750 micrograms by intravenous infusion over 20 minutes and 10 mg orally as single doses on separate occasions the mean oral bioavailability was 17.1% which was not significantly different from published values in healthy subjects, but the maximum plasma concentrations were almost twice as high as normal, apparently due to reduced systemic clearance and volume of distribution.1 The fact that bioavailability was not increased suggests that much pre-systemic metabolism takes place in the gut rather than the liver. Although increased adverse effects were not associated with the raised felodipine concentrations in this study it is recommended that therapy in cirrhotic patients begin at lower doses than in patients with normal liver function. US licensed product information recommends that an initial dose of 2.5 mg once daily should be used in patients with hepatic impairment.
1. Regårdh CG, et al. Pharmacokinetics of felodipine in patients with liver disease. Eur J Clin Pharmacol 1989; 36: 473–9.

💊 Preparations

USP 31: Felodipine Extended-Release Tablets.

Proprietary Preparations

Arg.: Munobal; Plendil; Austral.: Agon†; Felodur; Plendil; Austria: Felodistad; Munobal; Plendil; Belg.: Plendil; Renedil; Braz.: Splendil; Canad.: Plendil; Renedil; Chile: Splendil; Cz.: Auronal; Felocor; Plendil; Presid; Denm.: Felodin; Hydac†; Plendil; Plendur; Fin.: Hydac; Plendil; Fr.: Flodil; Ger.: Felo-Puren; Felobeta; Felocor; Felogamma; Modip; Munobal; Gr.: Plendil; Hong Kong: Plendil; Hung.: Plendil; Presid; India: Felogard; Indon.: Nirmadil; Plendil; Irl.: Plendil; Israel: Penedil; Ital.: Feloday; Plendil; Prevex; Jpn: Splendil†; Malaysia: Plendil; Mex.: Fedin; Munobal; Plendil; Neth.: Plendil; Renedil; Norw.: Plendil; NZ: Felo; Plendil; Philipp.: Dilahex; Felim; Felop; Lodistad; Plendil; Versant; Pol.: Felohexal; Plendil; Port.: Mencor; Preslow; Rus.: Felodip (Фелодип); Plendil (Плендил); S.Afr.: Plendil; Singapore: Plendil; Spain: Fensel; Perfudal; Plendil; Swed.: Plendil; Switz.: Felodil; Munobal†; Plendil; Thai.: Felim; Felohexal; Feloten; Plendil; Tur k.: Plendil; UK: Cardioplen; Felotens; Keloc; Neofel; Plendil; Vascalpha; USA: Plendil; Venez.: Munobal†; Plendil. Multi-ingredient: Arg.: Nikion†; Triacor; Austral.: Triasyn; Austria: Tr iapin; Unimax; Belg.: Logimat; Cz.: Logimax†; Triasyn; Unimax†; Denm.: Logimax; Fin.: Logimax; Unimax; Fr.: Logimax; Ger.: Delmuno; Mobloc; Unimax; Gr.: Logimax; Triacor; Unitens; Hong Kong: Logimax; Hung.: Logimax; Triasyn; Irl.: Triapin; Israel: Logimax; Mex.: Logimax; Triacor; Neth.: Logimax; Triapin; Unimax; Philipp.: Logimax; Triapin; Port.: Unimax; Rus.: Logimax (Логимакс); S.Afr.: Tri-Plen; Spain: Logimax; Swed.: Logimax; Switz.: Logimax; Unimax; UK: Triapin; USA: Lexxel.
Published February 20, 2019.