Clinical pharmacokinetics of oxazepam and lorazepam

Clinical Pharmacokinetics
D J Greenblatt

Abstract

Oxazepam and lorazepam are 3-hydroxy benzodiazepine derivatives used as sedatives and anxiolytics. The major metabolic pathway for both compounds involves conjugation to glucuronic acid at the 3-position, followed by urinary excretion of the inactive glucuronide metabolite. Oxazepam has been administered to humans by the oral route only. Usual ranges for kinetic parameters are: elimination half-life, 5 to 15 hours; volume of distribution, 0.6 to 2.0 L/kg; clearance, 0.9 to 2.0 ml/min/kg. Age and liver disease have a minimal influence on oxazepam kinetics, but renal disease is associated with a prolonged half-life and increased volume of distribution. Typical kinetic values for lorazepam are: elimination half-life, 8 to 25 hours; volume of distribution, 1.0 to 1.3 L/kg; clearance, 0.7 to 1.2 ml/min/kg. Lorazepam clearance is somewhat reduced in old age, but liver disease has a minimal effect on clearance. Oral and intramuscular lorazepam are rapidly absorbed, with systemic availability averaging 90% or more. Both oxazepam and lorazepam are extensively bound to plasma protein, but the free fraction for lorazepam (8 to 12%) is greater than that for oxazepam (2 to 4%).

Citations

Jul 1, 1991·Journal of Clinical Pharmacology·J L SegalM Vulpe
Jan 1, 1988·European Journal of Clinical Pharmacology·J SonneP B Andreasen
Jan 1, 1987·European Journal of Clinical Pharmacology·P S WisselC E Inturrisi
Aug 16, 1984·Klinische Wochenschrift·H R OchsU Klehr
Sep 1, 1996·Psychopharmacology·P VidailhetD Grangé
Feb 1, 1990·Pharmacology, Biochemistry, and Behavior·E P WalaT A Pruitt
Jan 1, 1985·Neuroscience and Biobehavioral Reviews·R R GriffithsJ V Brady
Sep 1, 1987·Journal of Affective Disorders·J Ananth
Sep 1, 1987·Journal of Affective Disorders·D V Sheehan
Jan 17, 2004·International Journal of Pharmaceutics·Joseph V TurnerDavid J Cutler
Feb 20, 2002·Forensic Science International : Synergy·Svetlana SkurtveitAsbjørg S Christophersen
Dec 1, 1994·The Journal of Adolescent Health : Official Publication of the Society for Adolescent Medicine·E V Capparelli
Dec 22, 2005·Experimental and Clinical Psychopharmacology·Miriam Z Mintzer, Roland R Griffiths
Aug 11, 1983·The New England Journal of Medicine·D J GreenblattD R Abernethy
May 29, 2004·American Journal of Physical Medicine & Rehabilitation·Rodney S Li Pi Shan, Nigel L Ashworth
Dec 1, 1995·Critical Care Medicine·M A MirskiD F Hanley
Feb 18, 2010·Current Opinion in Critical Care·Marek A Mirski, John J Lewin
Dec 1, 1991·British Journal of Addiction·M Farré, J Camí
Aug 1, 1994·British Journal of Clinical Pharmacology·G StormJ H Jonkman
Sep 1, 1992·British Journal of Pharmacology·A M StijnenM Danhof
Jan 1, 1993·Pharmacology & Toxicology·J Sonne
Jun 18, 1983·British Medical Journal·N Hockings, B R Ballinger
Jul 29, 2003·Clinical Pharmacokinetics·Mikko NiemiKari T Kivistö
Mar 21, 2012·Anesthesia Progress·Daniel E Becker
Oct 15, 2013·Clinical Pharmacokinetics·Gail D Anderson, Shahin Hakimian
Jul 1, 1994·Psychopharmacology·P VidailhetJ L Imbs
Jun 3, 2014·Brain Research·Glenn F GuerinNicholas E Goeders
Sep 1, 1990·Electroencephalography and Clinical Neurophysiology·P BartelP Becker
May 1, 1995·Disease-a-month : DM·R C BoneM Guerrero
Jan 22, 2013·Expert Opinion on Drug Metabolism & Toxicology·Alfredo Carlo AltamuraSilvio Bareggi
Jan 1, 1983·Drug Metabolism Reviews·D J GreenblattR I Shader
Mar 10, 2010·Journal of Pharmaceutical Sciences·Mohamed A KamalDaniele Ouellet
Apr 9, 2008·Acta Anaesthesiologica Taiwanica : Official Journal of the Taiwan Society of Anesthesiologists·Wei-Hung ChanTzuu-Huei Ueng
Nov 1, 1983·American Journal of Kidney Diseases : the Official Journal of the National Kidney Foundation·W M BennettI Singer
Nov 29, 2011·Forensic Science International : Synergy·Vigdis VindenesJørg Mørland
Nov 5, 2011·The Journal of Pediatrics·James M ChamberlainUNKNOWN Pediatric Emergency Care Applied Research Network (PECARN)
Jan 20, 2010·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·P Van RuitenbeekW J Riedel

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.