Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0600097 (Sedation)
 1,337 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Pharmacokinetic characteristics of the anticonvulsant phenobarbital were studied in seven pony and two Thoroughbred foals aged between four and 10 days. A single, 20 mg/kg bodyweight (bwt) dose of phenobarbital was given intravenously over 25 mins and the serum concentrations of the drug were measured using an EMIT AED assay (coefficient of variation 1.37 per cent at 30 micrograms/ml, n = 7). Phenobarbital elimination was found to follow first order kinetics. The mean (+/- sd) peak phenobarbital serum concentration was 18.6 +/- 2.1 micrograms/ml at 1 h after initiation of infusion with a mean (+/- se) half-life of 12.8 +/- 2.1 h. The mean (+/- se) volume of distribution was 0.86 +/- 0.026 litres/kg bwt and mean (+/- se) total body clearance was 0.0564 +/- 0.0065 litres/kg bwt/h. Sedation was noticed 15 to 20 mins after the beginning of infusion and lasted for up to 8 h. All foals could be aroused and could walk although they were ataxic for the first 1 to 2 h. A degree of delayed hyperexcitability occurred 3 to 8 h after infusion. In equine neonatal seizure disorders it is recommended to use a loading dose of 20 mg/kg bwt of phenobarbital, followed by maintenance doses of 9 mg/kg bwt at 8 h. With this regimen, average steady state serum phenobarbital concentrations should range between approximately 11.6 and 53 micrograms/ml. Phenobarbital serum concentrations should be monitored following the loading dose and 24 h after initiating the maintenance doses to check that levels remain within the suggested (human) therapeutic range of 15 to 40 micrograms/ml.
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PMID:Preliminary study on the pharmacokinetics of phenobarbital in the neonatal foal. 647 36

Sedation is a common side effect of anticonvulsant drug therapy. To find out whether the new antiepileptic drugs, felbamate and lamotrigine, are able to produce sedation, we carried out electroencephalographic (EEG) studies in the rat to measure drug effects on sleep-wake patterns, during both light and dark phases. For comparison, the reference drugs, carbamazepine and phenobarbital, were also studied. EEG activity was recorded for 6 h after oral (PO) administration of drugs or vehicle, and the stages of wakefulness, rapid eye movements (REM) sleep and non-REM sleep were classified thereafter. In the light phase, felbamate (30-300 mg/kg) did not produce sedative effects, while lamotrigine (3-30 mg/kg) increased wakefulness at each dose tested. Carbamazepine (10-100 mg/kg) did not produce sleep-wake alterations, and phenobarbital (100 mg/kg) markedly suppressed REM. In the dark phase, felbamate (300 mg/kg), lamotrigine (30 mg/kg), and carbamazepine (100 mg/kg) reduced REM but did not change the total amount of sleep. Phenobarbital, at 100 mg/kg, markedly increased total sleep and greatly reduced REM. This study shows that the anticonvulsant drugs examined have different effects on the states of sleep and wakefulness in the rat. The data are discussed on the basis of the mechanism of action that characterizes each individual drug.
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PMID:Effects of four antiepileptic drugs on sleep and waking in the rat under both light and dark phases. 886 55