物质信息

ID:203

名称和标识
IUPAC传统名
codeine
别名
Codeine anhydrousL-CodeineMorphine monomethyl etherMethylmorphineNorcodeine, N-MethylCodeineNorcodine, N-Methyl
商标名
CodiceptCoducept
IUPAC标准名
(1S,5R,13R,14S,17R)-10-methoxy-4-methyl-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10,15-tetraen-14-ol
数据登录号
PubChem CID
CAS号
PubChem SID
化合物性质
理化性质
疏水性(logP)
1.19 [AVDEEF,A ET AL. (1996)]
溶解度
9 mg/mL at 20 oC [YALKOWSKY,SH & DANNENFELSER,RM (1992)]
描述信息
Drug Groups
illicit; approved
Description
An opioid analgesic related to morphine but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough. [PubChem]
Indication
For treatment and management of pain (Systemic), also used as an Antidiarrheal and as a cough suppressant.
Pharmacology
Codeine, an opiate agonist in the CNS, is similar to other phenanthrene derivatives such as morphine. Codeine, in combination with guaifenesin or iodinated glycerol, is used as a cough suppressant and, as a single agent or in combination with acetaminophen or other products, is used for pain control and as an antidiarrheal agent.
Toxicity
Respiratory depression, sedation and miosis and common symptoms of overdose. Other symptoms include nausea, vomiting, skeletal muscle flaccidity, bradycardia, hypotension, and cool, clammy skin. Apnea and death may ensue.
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic. Codeine is a prodrug, itself inactive, but demethylated to the active morphine by the liver enzyme CYP2D6.
Absorption
Well absorbed following oral administration with a bioavailability of approximately 90%.
Half Life
2-4 hours
Protein Binding
7-25%
References
• Schroeder K, Fahey T: Over-the-counter medications for acute cough in children and adults in ambulatory settings. Cochrane Database Syst Rev. 2004 Oct 18;(4):CD001831. [Pubmed]
• Vree TB, van Dongen RT, Koopman-Kimenai PM: Codeine analgesia is due to codeine-6-glucuronide, not morphine. Int J Clin Pract. 2000 Jul-Aug;54(6):395-8. [Pubmed]
• Srinivasan V, Wielbo D, Tebbett IR: Analgesic effects of codeine-6-glucuronide after intravenous administration. Eur J Pain. 1997;1(3):185-90. [Pubmed]
External Links
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参考文献
• Schroeder K, Fahey T: Over-the-counter medications for acute cough in children and adults in ambulatory settings. Cochrane Database Syst Rev. 2004 Oct 18;(4):CD001831. Pubmed
• Srinivasan V, Wielbo D, Tebbett IR: Analgesic effects of codeine-6-glucuronide after intravenous administration. Eur J Pain. 1997;1(3):185-90. Pubmed
• Vree TB, van Dongen RT, Koopman-Kimenai PM: Codeine analgesia is due to codeine-6-glucuronide, not morphine. Int J Clin Pract. 2000 Jul-Aug;54(6):395-8. Pubmed