Clinical pharmacokinetics of lorazepam

  title={Clinical pharmacokinetics of lorazepam},
  author={David J Greenblatt and R. T. Schillings and Adrian A. Kyriakopoulos and RichardI. Shader and Samuel F. Sisenwine and John A. Knowles and Hans W. Ruelius},
  journal={Clinical Pharmacology \& Therapeutics},
Eight healthy male subjects received single 2‐mg oral doses of lorazepam containing 24 uLCi Img of 2‐14C‐lorazepam. Multiple venous blood samples were drawn during the .first 96 hr after the dose, and all urine and stool were collected for 120 hr after dosing. Concentrations of lorazepam and its metabolites in body fluids were determined by appropriate analytic techniques. Following a lag time, lorazepam was absorbed with an apparent first‐order half‐life of 15 min. The peak plasma… 

Clinical Pharmacokinetics of Lorazepam. III. Intravenous Injection. Preliminary Results

Four healthy male volunteers received 5 mg lorazepam as a single intravenous injection. Concentrations of lorazepam and its glucuronide metabolite were determined in multiple venous blood samples

Clinical Pharmacokinetics of Lorazepam. IV. Long‐Term Oral Administration

Mean steady-state lorazepam levels were highly correlated with daily dose in mg/kg, but were not related to age, and Lorzepam was not detected in any plasma samples drawn one week after discontinuation of treatment.

Single- and multiple-dose kinetics of oral lorazepam in humans: The predictability of accumulation

Overall, the rate and extent of lorazepam accumulation during multiple dosage were reasonably well predicted by the single-dose kinetic study, however, accurate prediction for any specific individual was not always achieved.

Pharmacokinetics and bioavailability of intravenous and intramuscular lorazepam with an adjunct test of the inattention effect in humans.

The inattention effect of lorazepam was assessed by exposing the subjects during the intravenous pharmacokinetic experiments to a binaural stimulation test, which revealed various degrees of acute reduced attention in only three of the subjects.

The pharmacokinetics and biotransformation of the new benzodiazepine lormetazepam in humans I. Absorption, distribution, elimination and metabolism of lormetazepam-5-14C

The pharmacokinetics and metabolism of the new benzodiazepine lormetazepam were investigated in five male volunteers using thel4C-abelled drug, finding that the drug was absorbed completely and eliminated almost exclusively by the renal route.

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

The pharmacokinetic profiles of a sublingual and a conventional oral lorazepam tablet formulation were established following chronic administration to twelve healthy male volunteers, and the observed time to steady-state for both formulations was approximately 3 days, which agrees well with that predicted from previous single dosing studies.

Disposition pharmacokinetics of lorazepam in the rabbit.

The disposition pharmacokinetics of the sedative and anxiolytic drug lorazepam were investigated in 8 rabbits in relation to intravenous bolus injection of 0.3 or 0.6 mg of the compound. Lorazepam

Antipyrine Plasma and Urine Metabolite Disposition with Lorazepam Coadministration

Although antipyrine and lorazepam have been individually used in the separate assessment of phase I and phase II liver function, their simultaneous use after a single injection has also been suggested and the plasma total-body clearances of the two agents were not different when they were administered alone or in combination.

Placebo‐controlled comparative study of the anxiolytic activity and of the pharmacokinetics of oral and sublingual lorazepam in generalized anxiety

Both the oral and sublingual lorazepam produced a significant anxiolytic effect; there was no statistically significant difference between the therapeutic effectiveness of the two forms of lorzepam.

Analysis of lorazepam and its 30-glucuronide in human urine by capillary electrophoresis: evidence for the formation of two distinct diastereoisomeric glucuronides.

Analysis of the extracts prepared from enzymatically hydrolyzed urines by MEKC in the presence of 2-hydroxypropyl-beta-CD revealed the enantiomerization process of LOR (observation of two peaks of equal magnitude connected with a plateau zone).



Lorazepam: glucuronide formation in the cat.

The findings indicate that the cat is capable of using glucuronidation as a major route of conjugation, contrary to the many reports that cats conjugate exogenous materials poorly with glucuronic acid.


Radioassay of blood, various tissues, and excreta indicated that the drug was well absorbed and the fate of oxazepam in humans was similar to that in dogs and pigs.

Central nervous system and cardiovascular effects of lorazepam in man

The sedative‐hypnotic activity of single oral doses of lorazepam, a new member of the benzodiazepine series, acted indirectly on vasomotor reflexes by way of the central nervous system and about two thirds of the doses were recovered in urine as glucuronide within 96 hours.

Lorazepam (WY 4036) as a pre‐operative medication

A pilot study in sixty gynaecological patients suggested that lorazepam in 2 mg doses was a suitable pre-operative medication with few side-effects and without overt effects on the respiratory or

Some considerations as to the determination and significance of biologic half-life.

The biologic half-life of a drug as determined from the terminal exponential phase of appropriate semilogarithmic plots is shown to dictate the steady-state levels of drug upon repetitive dosing,

Lorazepam versus Glutethimide as a Sleep‐Inducing Agent for the Geriatric Patient

ABSTRACT: The safety of lorazepam was compared with that of a standard drug, glutethimide, in 50 chronically ill geriatric patients. Repeated physical examinations, laboratory determinations and

Bioavailability of Drugs: The Digoxin Dilemma

Determination of absolute bioavailability of a given digoxin preparation requires a comparative study using intravenous digoxin as a standard, and is unlikely to account for unexpected clinical results during digoxin therapy.

Oral premedication with lorazepam (Ativan): a comparison with heptabarbitone (Medomin) and diazepam (Valium).

The results of the trial suggest that in these doses the three drugs were almost equipotent in sedative effect whilst lorazepam showed appreciably better anterograde amnesia for the day of operation.

Hypnotic efficacy of lorazepam and flurazepam

In a double‐blind crossover study involving 15 insomniac subjects, the hypnotic efficacy of lorazepam, 2 and 4 mg, was compared with flurazepam, 15 and 30 mg, and placebo. Five subjective measures