Naloxone Does Not Antagonize Diazepam-induced Sedation

Christensen, K N; Hüttel, M.; Marshall, Bryan E.

doi:10.1097/00000542-197908000-00035

Cited by 19 publications

(6 citation statements)

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“…The discovery of such a benzodiazepine antagonist is analogous to that of the opiate antagonists and should have considerable scientific and therapeutic significance. Previous attempts to antagonize the central effects of diazepam using cholinesterase inhibitors (Di Liberti, O'Brien and Turner, 1975;Rupreht, 1980) or naloxone (Bell, 1975;Christensen and Huttel, 1979) have yielded inconclusive results, but have highlighted the potential usefulness of such an antidote in benzodiazepine overdose, or for abolishing the central effects of the benzodiazepine administered for surgical or diagnostic reasons, when rapid reversal of sedation may be required.…”

Section: Discussionmentioning

confidence: 99%

Ro 15–1788 Antagonizes the Effects of Diazepam in Man Without Affecting Its Bioavailability

O'Boyle

Lambe

Darragh

et al. 1983

British Journal of Anaesthesia

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In a double-blind, placebo-controlled three-way cross over study, the efficacy of Ro 15-1788 200 mg, a new benzodiazepine antagonist, in blocking the amnesic, cognitive, psychomotor and subjective effects of diazepam 20 mg, was investigated in a group of six healthy male volunteers. The amnesic effects of diazepam were markedly attenuated by the combined administration of Ro 15-1788. The psychomotor and subjective effects of diazepam by mouth were most pronounced 2.5 h after administration. Concurrent oral administration of Ro 15-1788 completely prevented these effects at 2.5 h. Plasma diazepam concentrations observed after administration of the combination of diazepam and the antagonist did not differ from those observed following diazepam alone.

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Section: Discussionmentioning

confidence: 99%

Ro 15–1788 Antagonizes the Effects of Diazepam in Man Without Affecting Its Bioavailability

O'Boyle

Lambe

Darragh

et al. 1983

British Journal of Anaesthesia

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“…Previously, it had been thought that naloxone might have a partial antagonist effect at the benzodiazepine receptor, although this is refuted by some authors (Christensen & Huettel, 1979). Naloxone is thought to act primarily at the |i,-opiate receptor (responsible for analgesia and respiratory depression).…”

Section: Discussionmentioning

confidence: 99%

Reversal of unconsciousness by use of naloxone in a profoundly mentally handicapped epileptic

Turner

Stewart

1991

J intellect Disabil Res

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The reversal of a state of impaired consciousness in a known epileptic following a period of prolonged post-ictal unconsciousness (with flexor response to nociceptive stimuli) was achieved by use of 0-4 mg naloxone intravenously. This decision was based on the similarity of the individuals clinical presentation to that seen in cases of opiate overdose. The implications of this dnimatic clinical intervention are discussed. I CASE REPORTThe patient is a 20-year-old male with profound mental handicap, grand mal epilepsy and ataxic cerebral palsy. He was born following a prolonged second stage of labour, in a delivery requiring the use of forceps, and was the second of non-identical twins. At the birth, it was felt that neonatal hypoxia might have occurred, resulting in diffuse brain damage. The twin sister suffers no mental handicap, nor do his four siblings. There is no history of handicap in the family. The patient developed his first fit at age 4 months, 2 weeks after receiving a pertussis vaccination.On the occasion prompting this report, the patient was found unrousable; neurological examination revealed him to be unconscious, with pin-point pupils and responding to nociceptive stimuli by flexion (Glasgow Coma Scale 3/14). He had brisk symmetrical reflexes with bilateral extensor plantars. Additionally, the patient revealed marked hypotension of 80/40, a bradycardia of 45 beats per min and shallow respiration of 15 breaths per min. He was judged to have sustained a grand mal seizure. The patient had previously been extensively investigated including repeated electroencephalograms showing 'considerable global dysrhythmia suggestive of Lennox-Gastaut syndrome' (a diagnosis based on a characteristic EEG trace, similar to petit mal epilepsy, Laidlaw & Richens, 1982). There had also been repeated CAT scanning which had demonstrated no evidence of intracranial trauma, normal ventricular systems with no cortical abnormahty. He had had three CAT scans performed as a result of previous episodes similar to that described when a head injury was feared responsible for the sustained loss of consciousness.

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Section: Discussionmentioning

confidence: 99%

“…Previous attempts to antagonise the central effects of the benzodiazepines by cholinesterase inhibitors (Di Liberti et al, 1975;Rupreht, 1980) or naloxone (Bell, 1975: Christensen & Huttel, 1979 have been inconclusive, but have demonstrated the potential value of an effective benzodiazepine antagonist. Clinically, a drug such as Ro 15-1788 would be of benefit in the management of benzodiazepine overdose, and in the rapid reversal of benzodiazepine anaesthesia.…”

Section: Discussionmentioning

confidence: 99%

RO 15‐1788 antagonises the central effects of diazepam in man without altering diazepam bioavailability.

Darragh¹,

Lambe²,

Kenny³

et al. 1982

Brit J Clinical Pharma

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1 In a double‐blind, placebo controlled study, the efficacy of Ro 15‐ 1788, a new benzodiazepine antagonist, in blocking the cognitive, psychomotor and subjective effects of diazepam, was investigated in a group of six healthy male volunteers. 2 The central effects of orally administered diazepam (40 mg) were most pronounced 1 h after dosing and persisted for 9 h with decreasing severity. 3 Concurrent oral administration of Ro 15‐1788 (200 mg) completely prevented the impairment in cognitive and psychomotor function observed after diazepam alone. 4 The duration of action of Ro 15‐1788 was shorter than that of diazepam. 5 Plasma diazepam levels after administration of the diazepam/antagonist combination were very similar to those observed following diazepam alone.

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Naloxone Does Not Antagonize Diazepam-induced Sedation

Cited by 19 publications

References 0 publications

Ro 15–1788 Antagonizes the Effects of Diazepam in Man Without Affecting Its Bioavailability

Ro 15–1788 Antagonizes the Effects of Diazepam in Man Without Affecting Its Bioavailability

Reversal of unconsciousness by use of naloxone in a profoundly mentally handicapped epileptic

RO 15‐1788 antagonises the central effects of diazepam in man without altering diazepam bioavailability.

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