Bioavailability of diazepam after intravenous, oral and rectal administration in adult epileptic patients.

Abstract

1 The absorption of single doses of diazepam in six adult epileptic subjects following intravenous, oral and rectal administration were studied in order to evaluate the usefulness of the latter in emergency situations in the adult. 2 Diazepam tablets (Valium, Roche) and rectal solution (Valium solution for intravenous administration) produced similar peak serum concentrations after delays of 15-90 min. 3 Two suppository formulations showed statistically significant differences in absorption characteristics. 4 Serum diazepam levels above 400 ng ml-' (suggested to be necessary for a satisfactory anticonvulsant effect) were reached in only a few subjects after rectal doses of 10-20 mg of solution, and then usually after a delay of over 2 h.

A Comparison of Rectal Diazepam Gel and Placebo for Acute Repetitive Seizures

“…7 Oral diazepam and lorazepam, sublingual lorazepam, rectal solutions of lorazepam and diazepam, and diazepam suppositories have been used to treat acute repetitive seizures. [8][9][10][11][12][13] Oral or sublingual administration is frequently difficult and hazardous when the patient is actively convulsing, and absorption of diazepam and lorazepam tablets and rectal lorazepam solution is slower than that of rectal diazepam solutions. 8,14,15 Rectal diazepam solutions have many characteristics sought in the ideal drug to treat acute repetitive seizures.…”

A Single‐Blind, Crossover Comparison of the Pharmacokinetics and Cognitive Effects of a New Diazepam Rectal Gel with Intravenous Diazepam

“…Mean bioavailability for rectal solutions ranged from 81 to 102%, and t , , ranged from 17 to 65 min. With both dosage forms, there was substantial intersubject variability (8)(9)(10)22). The proprietary rectal formulation used in this study is a viscous gel with a composition different from the DZP formulations used in previous investigations.…”

“…DZP suppositories exhibit slow and variable absorption, which precludes their use as acute treatment (9,lO). In contrast, rectal DZP solutions are easily administered by nonmedical personnel and are rapidly absorbed (9)(10)(11)(12). Several commercial formulations are available in Europe, but until recently, the use of rectal DZP solution.in the United States required that the caregiver assemble a needle and syringe, withdraw the correct dose from a vial of DZP injectable solution, lubricate the syringe, and administer the dose.…”

Relative Bioavailability of Rectally Administered Carbamazepine Suspension in Humans

“…The use has been primarily for status epilepticus when rapid absorption and ease of administration is necessary. Rectally administered diazepam (Agurell et al, 1975;Knudsen, 1979;Hoppu and Santavouri, 1981;Milligan et al, 1981;Dhillon et al, 1982) and paraldehyde (Duffy and Lombroso, 1978) are frequently used. Rectal administration of clonazepam (Jensen et al, 1983) and secobarbital (Levine et al, 1982) has been proposed.…”