A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)
Indication
For the short-term treatment of insomnia.
Pharmacology
Pentobarbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
Toxicity
Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.
Affected Organisms
Humans and other mammals
Biotransformation
by hepatic microsomal enzyme system
Absorption
Barbiturates are absorbed in varying degrees following oral, rectal, or parenteral administration.
Half Life
5 to 50 hours (dose dependent)
Elimination
Barbiturates are metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine, and less commonly, in the feces. Approximately 25 to 50 percent of a dose of aprobarbital or phenobarbital is eliminated unchanged in the urine, whereas the amount of other barbiturates excreted unchanged in the urine is negligible.
References
•
Knodell RG, Spector MH, Brooks DA, Keller FX, Kyner WT: Alterations in pentobarbital pharmacokinetics in response to parenteral and enteral alimentation in the rat. Gastroenterology. 1980 Dec;79(6):1211-6.
[Pubmed]
A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups.
参考文献
PubChem文献
数据源提供
• Knodell RG, Spector MH, Brooks DA, Keller FX, Kyner WT: Alterations in pentobarbital pharmacokinetics in response to parenteral and enteral alimentation in the rat. Gastroenterology. 1980 Dec;79(6):1211-6. Pubmed
USA: Schedule II (oral and parenteral); Schedule III (rectal), UK: Class B Controlled Substance
蛋白结合率
20-45%
半衰期
15-48 hours
代谢
Hepatic
安全信息
GHS警示词
Danger
联合国危险货物编号
2811
GHS危险品标识
呼吸道过敏,类别1
生殖细胞突变,类别1A,1B,2
致癌性,类别1A,1B,2
生殖毒性,类别1A,1B,2
特定目标器官毒性 – 一次接触,类别1,2
特定目标器官毒性 – 反复接触,类别1,2
吸入危险,类别1
急性毒性(口服,皮肤接触,吸入),类别1,2,3
3
CQ5775000
P281-P301+P310
H301-H361
USDEA Schedule II; Home Office Schedule 3; psychotrope; kontrollierte Droge in Deutschland; regulated under CDSA - not available from Sigma-Aldrich Canada
Eyeshields, Faceshields, full-face particle respirator type N100 (US), Gloves, respirator cartridge type N100 (US), type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges