Pharmacokinetics of two lorazepam formulations, oral and sublingual, after multiple doses. 1983

G Caillé, and J Spénard, and Y Lacasse, and J Brennan

The pharmacokinetic profiles of a sublingual and a conventional oral lorazepam tablet formulation were established following chronic administration to twelve healthy male volunteers. Fitting a multi-dose equation based on a one-compartment model to the observed data, the average elimination half-lives for the sublingual and oral doses are estimated to be 11 and 8 h, respectively, while the corresponding absorption half-lives are 15 and 55 min; this confirms earlier reports that the sublingual formulation is more rapidly absorbed. The observed time to steady-state for both formulations was approximately 3 days, which agrees well with that predicted from previous single dosing studies. Although the sublingual formulation yields a higher average steady-state minimum plasma concentration than the oral formulation (41.6 versus 38.1 ng ml-1), the maximum lorazepam concentration achieved during steady state was approximately 83 ng ml-1 for both formulations. The average steady-state plasma concentration is estimated to be 63 ng ml-1, independent of the formulation used.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008140 Lorazepam A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. Apo-Lorazepam,Ativan,Donix,Duralozam,Durazolam,Idalprem,Laubeel,Lorazep Von Ct,Lorazepam Medical,Lorazepam-Neuraxpharm,Lorazepam-Ratiopharm,Novo-Lorazem,Nu-Loraz,Orfidal Wyeth,Sedicepan,Sinestron,Somagerol,Temesta,Tolid,Témesta,WY-4036,Apo Lorazepam,Lorazepam Neuraxpharm,Lorazepam Ratiopharm,Medical, Lorazepam,Novo Lorazem,Nu Loraz,Von Ct, Lorazep,WY 4036,WY4036,Wyeth, Orfidal
D008297 Male Males
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D014059 Tongue A muscular organ in the mouth that is covered with pink tissue called mucosa, tiny bumps called papillae, and thousands of taste buds. The tongue is anchored to the mouth and is vital for chewing, swallowing, and for speech. Tongues
D014151 Anti-Anxiety Agents Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not included here. Anti-Anxiety Agent,Anti-Anxiety Drug,Anxiolytic,Anxiolytic Agent,Anxiolytic Agents,Tranquilizing Agents, Minor,Anti-Anxiety Drugs,Anti-Anxiety Effect,Anti-Anxiety Effects,Antianxiety Effect,Antianxiety Effects,Anxiolytic Effect,Anxiolytic Effects,Anxiolytics,Tranquillizing Agents, Minor,Agent, Anti-Anxiety,Agent, Anxiolytic,Agents, Anti-Anxiety,Agents, Anxiolytic,Agents, Minor Tranquilizing,Agents, Minor Tranquillizing,Anti Anxiety Agent,Anti Anxiety Agents,Anti Anxiety Drug,Anti Anxiety Drugs,Anti Anxiety Effect,Anti Anxiety Effects,Drug, Anti-Anxiety,Drugs, Anti-Anxiety,Effect, Anti-Anxiety,Effect, Antianxiety,Effect, Anxiolytic,Effects, Anti-Anxiety,Effects, Antianxiety,Effects, Anxiolytic,Minor Tranquilizing Agents,Minor Tranquillizing Agents

Related Publications

G Caillé, and J Spénard, and Y Lacasse, and J Brennan
February 1992, Antimicrobial agents and chemotherapy,
G Caillé, and J Spénard, and Y Lacasse, and J Brennan
February 1982, Journal of pharmaceutical sciences,
G Caillé, and J Spénard, and Y Lacasse, and J Brennan
May 1988, Ugeskrift for laeger,
G Caillé, and J Spénard, and Y Lacasse, and J Brennan
December 1977, European journal of clinical pharmacology,
G Caillé, and J Spénard, and Y Lacasse, and J Brennan
August 1995, Journal of clinical pharmacology,
G Caillé, and J Spénard, and Y Lacasse, and J Brennan
September 1988, International journal of clinical pharmacology, therapy, and toxicology,
G Caillé, and J Spénard, and Y Lacasse, and J Brennan
August 1995, Journal of clinical psychopharmacology,
G Caillé, and J Spénard, and Y Lacasse, and J Brennan
March 1976, European journal of clinical pharmacology,
G Caillé, and J Spénard, and Y Lacasse, and J Brennan
May 2021, Journal of veterinary pharmacology and therapeutics,
Copied contents to your clipboard!