Summary
Ro 21-3981 is a newly synthesized water soluble benzodiazepine derivative. Its pharmacological properties are similar to diazepam. This investigation was designed to establish the effective induction dosage of Ro 21-3981 and to compare it with diazepam for induction of anaesthesia. The ED50 for Ro 21-3981 induction is 0.15 mg/kg and ED100 is 0.2 mg/kg. Ro 21-3981 is one and one-half times as potent as diazepam (0.3 rng/kg) and more rapid in action. There is significantly less pain on injection with Ro 21-3981 as compared to diazepam. Cardiovascular stability and apnoea were observed with both drugs. Ro 21-3981 is a promising anaesthetic induction drug that merits further human study.
Résumé
Le RO-21-3981 est une nouvelle benzodiazépine de synthèse soluble dans ľeau. Ses propriétés pharmacologiques sont semblables àa celles du diazepam.
Cette étude avait pour but de déterminer la dose efficace ďinduction de cet agent et de comparer le RO-21-3981 au diazepam comme agent ďinduction.
Ľinduction (perte du réflexe ciliaire et absence de réponse aux commandements) se produisait chez 50 pour cent des sujets àa une dose de 0.15 mg/kilo et chez 100 pour cent des sujets avec 0.2 mg/kilo. Le RO-21-3981 est une fois et demie plus puissant que le diazepam (dose efficace : 0.3 mg/kilo) et plus rapide ďaction que ce dernier.
Il est moins irritant que lui et cause moins de douleur en injection. On a observé avec les deux médicaments une grande stabilité cardiovasculaire. Avec ľun comme avec ľautre, on peut rencontrer de ľhypoventilation et une apnée nécessitant une assistance respiratoire.
Le RO-21-3981 nous semble un agent ďinduction prometteur et mérite une étude plus poussée chez ľhumain.
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Reves, J.G., Corssen, G. & Holcomb, C. Comparison of two benzodiazepines for anaesthesia induction: midazolam and diazepam. Can. Anaesth. Soc. J. 25, 211–214 (1978). https://doi.org/10.1007/BF03004881
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DOI: https://doi.org/10.1007/BF03004881