Imidazoles

Publication Title: 
Zoology (Jena, Germany)

Currently, there is concern about declining bee populations and the sustainability of pollination services. One potential threat to bees is the unintended impact of systemic insecticides, which are ingested by bees in the nectar and pollen from flowers of treated crops. To establish whether imidacloprid, a systemic neonicotinoid and insect neurotoxin, harms individual bees when ingested at environmentally realistic levels, we exposed adult worker bumble bees, Bombus terrestris L. (Hymenoptera: Apidae), and honey bees, Apis mellifera L.

Author(s): 
Cresswell, James E.
Page, Christopher J.
Uygun, Mehmet B.
Holmbergh, Marie
Li, Yueru
Wheeler, Jonathan G.
Laycock, Ian
Pook, Christopher J.
de Ibarra, Natalie Hempel
Smirnoff, Nick
Tyler, Charles R.
Publication Title: 
Biochemical Pharmacology
Author(s): 
Morita, K.
Yamamoto, I.
Iwata, H.
Publication Title: 
Archives Internationales De Pharmacodynamie Et De Thérapie

Etomidate, R-(+)-ethyl-1-(1-phenylethyl)-1H-imidazole-5-carboxylate was found to be a potent, short-acting and safe hypnotic; when given intravenously in single doses to mice, rats, guinea-pigs, rabbits and dogs. In rats of different body weight (50, 100, 200 and 300 g) two injection rates were used (2 sec and 2 min). By rapid iv injection in rats of 200 g etomidate (ED50 equal to 0.57 mg/kg) is about 6 times more potent than methohexital (ED50 equal to 3.51 mg/kg) and 25 times more potent than propanidid and thiopental (ED50's equal to 13.4 mg/kg).

Author(s): 
Janssen, P. A.
Niemegeers, C. J.
Marsboom, R. P.
Publication Title: 
European Journal of Pharmacology

Beagles, implanted with cortical and subcortical electrodes, were given etomidate i.v. (1 mg/kg) over a period of 10 sec. The effects on the EEG were compared with those obtained with 7 mg/kg of methohexital. Both compounds induced hypnosis for a duration of approximately 8 min. The EEGs showed a remarkable similarity. Visual inspection of the records as well as power spectrum analysis revealed a sustained theta-activity with underlying fast activity. The configuration of the waves was rather sharp.

Author(s): 
Wauquier, A.
van den Broeck, W. A.
Verheyen, J. L.
Janssen, P. A.
Publication Title: 
Archives Internationales De Pharmacodynamie Et De Thérapie

RU 31158, 6-(orthochlorophenyl)-1, 2-dihydro-2 (N-methylpiperazine-1-yl) methylene-8-nitro-IH, 4H-imidazo [1,2-a] [1,4] benzodiazepin-1-one methanesulphonate, demonstrated potent hypnotic activity compared to diazepam when examined in the mouse and rat. RU 31158 potentiated minimal hypnosis in mice induced by both hexobarbital and chlorprothixene with ED50 values of 2.15 (1.53-3.01) and 0.69 (0.46-1.02) mg/kg p.o. respectively; these compared to values for diazepam of 17.00 (11.25-25.67) and 3.60 (2.25-5.76) mg/kg p.o.

Author(s): 
Johns, T. G.
Piper, D. C.
James, G. W.
Publication Title: 
South African Medical Journal = Suid-Afrikaanse Tydskrif Vir Geneeskunde

Etomidate (Hypnomidate; Ethnor) in an alcoholic solution was used as the hypnotic component of a technique of total intravenous anaesthesia in an open pilot evaluation in 50 patients undergoing surgery. No anaesthetic gases were used. Despite cardiovascular stability, lack of respiratory depression and a short awakening time, unwanted movements by the patients made total intravenous anaesthesia with this technique unsatisfactory.

Author(s): 
Van Eeden, A. F.
Leiman, B. C.
Publication Title: 
Archives Internationales De Pharmacodynamie Et De Thérapie

The interaction of four imidazole antimycotics clotrimazole, econazole, ketoconazole and miconazole with other drugs was studied in in vivo models known to reveal inhibition and induction of microsomal enzymes. In rats the duration of methohexital hypnosis and the prothrombin time prolongation induced by acenocoumarol were changed after oral administration of all four antimycotics. The oral ED50-values of miconazole, econazole and clotrimazole for prolongation of methohexital hypnosis in female rats (acute inhibiton of microsomal enzymes) were 3.55, 3.56 and 10.7 mg/kg.

Author(s): 
Niemegeers, C. J.
Levron, J. C.
Awouters, F.
Janssen, P. A.
Publication Title: 
British Journal of Anaesthesia

Etomidate was injected i.v. within 10 or 60 s at various doses. After etomidate 0.3 mg kg-1 the plasma concentration was 1.6 micrograms ml-1 at 1 min after the end of injection. For about 7 min a good hypnotic effect (stages C0-D2) was observed on the e.e.g. recording. For surgical procedures, however, a combination with analgesic drugs appeared to be necessary. When the dose of etomidate was increased (0.1-0.4 mg kg-1) a linear increase in plasma concentration and slow e.e.g. activity was observed concomitantly.

Author(s): 
Doenicke, A.
Löffler, B.
Kugler, J.
Suttmann, H.
Grote, B.
Publication Title: 
Anaesthesia

A review of the hypnotic, anticonvulsant and brain protective action of etomidate in animals shows that when given as a single injection in different animal species recovery from hypnosis is quick and that the safety margin is large. In dogs a bolus or infusion produces high amplitude theta activity on the electroencephalogram (EEG). During infusion burst suppression is seen. After high doses, behaviour and EEG changes returned to normal within 3 hours. The wide spectrum of anticonvulsant activity suggests that etomidate may be useful in the treatment of status epilepticus.

Author(s): 
Wauquier, A.
Publication Title: 
Anesthesia and Analgesia

An etomidate infusion regimen for hypnosis as part of balanced, totally intravenous anesthesia was designed to maintain plasma etomidate concentrations above the awakening concentration of 300 ng/ml while avoiding dose-related side effects. The etomidate infusion regimen of 0.1 mg/kg/min for 3 min, 0.02 mg/kg/min for 27 min, and 0.01 mg/kg/min for the remainder of the anesthesia was used together with intravenous bolus doses of fentanyl, droperidol, and pancuronium. This was evaluated in 11 patients and the kinetics of etomidate were reexamined.

Author(s): 
Fragen, R. J.
Avram, M. J.
Henthorn, T. K.
Caldwell, N. J.

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