Safety, tolerability, and pharmacokinetics of an extended-release formulation of fluvastatin administered once daily to patients with primary hypercholesterolemia

Journal of Cardiovascular Pharmacology
H SabiaP Rothenberg

Abstract

Fluvastatin sodium (Lescol, Novartis Pharmaceutical Corp., East Hanover, NJ, U.S.A.), a potent 3-hydroxy-3-methylglutaryl coenzyme A (HMG Co-A) reductase inhibitor that limits cholesterol biosynthesis, is available as a 40-mg immediate-release formulation capsule. An extended-release formulation for once-daily administration has been developed for patients with primary hypercholesterolemia who may benefit from doses higher than 40 mg/day. This phase I study evaluated the safety, tolerability, and pharmacokinetics of a new fluvastatin extended-release formulation at doses ranging from 80-640 mg/day in 40 hypercholesterolemic patients. After a 2-week dietary stabilization phase, patients (Fredrickson type IIa/IIb), 18-55 years of age, were randomly assigned to four groups to receive oral fluvastatin extended-release (80, 160, 320, or 640 mg) or matching placebo once daily for 13 days. Fluvastatin extended-release was generally safe and well tolerated at doses of 80-320 mg/day. Within this dose range, linear pharmacokinetics was observed after single and multiple dosing. At 640 mg, fluvastatin extended-release was not well tolerated. Six of the seven actively treated patients at this dose experienced adverse events, including diar...Continue Reading

References

Jul 1, 1992·Journal of Clinical Pharmacology·F L TseA Troendle
May 26, 1994·The American Journal of Cardiology·L A Jokubaitis
Nov 1, 1993·American Journal of Hypertension·H T SmithW T Robinson
Dec 5, 1998·The New England Journal of Medicine·UNKNOWN Long-Term Intervention with Pravastatin in Ischaemic Disease (LIPID) Study Group
May 11, 1999·Drugs·H D Langtry, A Markham

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Citations

Jan 25, 2013·Clinical Pharmacokinetics·Anne-Charlotte CastellanUNKNOWN Genophar Working Group
Feb 22, 2002·Current Opinion in Nephrology and Hypertension·Domenic A Sica, Todd W B Gehr
Jan 5, 2002·The American Journal of Geriatric Cardiology·Domenic A Sica, Todd W B Gehr
Feb 28, 2002·Journal of Clinical Pharmacology·S Appel-DingemanseM Merz
Jun 18, 2004·Drugs·Alberto CorsiniChristie M Ballantyne
Jun 19, 2010·Expert Opinion on Drug Safety·Michiel T VoûteDon Poldermans
May 24, 2007·Current Medical Research and Opinion·B IlerigelenUNKNOWN TULIPS Investigators
Dec 14, 2004·International Journal of Clinical Practice·G De Angelis
Sep 9, 2008·Journal of Cardiovascular Electrophysiology·Yu-Feng HuShih-Ann Chen
Apr 2, 2005·Current Medical Research and Opinion·Evagelos N LiberopoulosMoses S Elisaf
Sep 8, 2005·Expert Opinion on Pharmacotherapy·Mark Y Chan, Chi Hang Lee
Nov 20, 2002·Expert Opinion on Pharmacotherapy·J M Lawrence, J P D Reckless
Nov 2, 2013·Neuromuscular Disorders : NMD·M Needham, F L Mastaglia
Sep 8, 2004·Expert Review of Cardiovascular Therapy·Anders Asberg, Hallvard Holdaas
Apr 1, 2005·Expert Review of Pharmacoeconomics & Outcomes Research·Paul Scuffham
Feb 7, 2002·Pharmacoepidemiology and Drug Safety
Apr 16, 2008·The American Journal of Gastroenterology·Ted BaderMuhammad Hasan
Nov 21, 2002·Current Opinion in Lipidology·Chiara BolegoRodolfo Paoletti
Aug 3, 2004·American Journal of Cardiovascular Drugs : Drugs, Devices, and Other Interventions·Andras Vermes, Istvan Vermes
Apr 3, 2008·The Canadian Journal of Neurological Sciences. Le Journal Canadien Des Sciences Neurologiques·Steven K Baker, Imtiaz A Samjoo

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