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Codeine metabolism





Codeine and Morphine Pathway, Pharmacokinetics - PharmGKB

7/12/2014
02:33 | Author: Sarah Gray

Codeine metabolism
Codeine and Morphine Pathway, Pharmacokinetics - PharmGKB

Representation of the candidate genes involved in metabolism of codeine and Modulation of the pharmacokinetic conversion of codeine to morphine by.

Approximay 60% of morphine is glucuronidated to morphine-3-glucuronide (M3G) while 5-10% is glucuronidated to morphine-6-glucuronide (M6G). These reactions are principally catalyzed by UGT2B7 in the liver. UGT1A1 may have a minor role in the formation of M3G, and UGT1A1 and UGT1A8 are capable of catalyzing the formation of M6G in vitro and so contribute to this pathway, although UGT1A8 is minimally expressed in liver and so is not depicted here. M6G has a higher affinity for OPRM1 than morphine and M3G and so the ratio of morphine to M6G is considered an important indicator of analgesic effect.

Codeine and morphine are pain relief drugs in the opiate family.

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Opioid Metabolism - National Center for Biotechnology Information

5/11/2014
12:26 | Author: Hannah Ramirez

Codeine metabolism
Opioid Metabolism - National Center for Biotechnology Information

The CYP2D6 enzyme is entirely responsible for the metabolism of hydrocodone,14 codeine,13 and dihydrocodeine to their active metabolites (hydromorphone.

CYP = cytochrome P450; M1 = O -desmethyltramadol; M3G = morphine-3-glucuronide; M6G = morphine-6-glucuronide; UGT = uridine diphosphate glucuronosyltransferase.

However, the enzymes responsible for glucuronidation reactions may also be subject to a variety of factors that may alter opioid metabolism. The most important UGT enzyme involved in the metabolism of opioids that undergo glucuronidation (eg, morphine, hydromorphone, oxymorphone) 12, 44 is UGT2B7. Research suggests that UGT2B7-mediated opioid metabolism may be altered by interactions with other drugs that are either substrates or inhibitors of this enzyme.

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Codeine and Morphine Metabolism (Homo sapiens) - WikiPathways

3/10/2014
02:39 | Author: Ryan Brooks

Codeine metabolism
Codeine and Morphine Metabolism (Homo sapiens) - WikiPathways

Liver cell Elimination via bile Codeine CYP3A4 UGT2B7 CYP2D6 The principal pathways for metabolism of codeine occur in the liver.

Transporters are also depicted in this pathway, as they influence clearance of codeine, morphine and their metabolites. Some of the evidence for the involvement of these transporters was derived from experiments done in mice and may or may not be translatable to human pharmacokinetics. The transporters present at the blood-brain barrier, not depicted in this pathway, as well as metabolic enzymes and transporters in the brain and GI tract, likely also play an important role in the pharmacokinetics of codeine and morphine. Saving... No Tags!

Approximay 60% of morphine is glucuronidated to morphine-3-glucuronide (M3G) while 5-10% is glucuronidated to morphine-6-glucuronide (M6G). These reactions are principally catalyzed by UGT2B7 in the liver. UGT1A1 may have a minor role in the formation of M3G, and UGT1A1 and UGT1A8 are capable of catalyzing the formation of M6G in vitro and so contribute to this pathway, although UGT1A8 is minimally expressed in liver and so is not depicted here. M6G has a higher affinity for OPRM1 than morphine and M3G and so the ratio of morphine to M6G is considered an important indicator of analgesic effect.

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Codeine Intoxication Associated with Ultrarapid CYP2D6 Metabolism

11/19/2014
06:28 | Author: Hannah Ramirez

Codeine metabolism
Codeine Intoxication Associated with Ultrarapid CYP2D6 Metabolism

CYP2D6 genotyping showed that the patient had three or more functional alleles, a finding consistent with ultrarapid metabolism of codeine.

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Codeine Sulfate (Codeine) Drug Information Clinical Pharmacology

9/18/2014
04:25 | Author: Sarah Gray

Codeine metabolism
Codeine Sulfate (Codeine) Drug Information Clinical Pharmacology

About 70-80% of the administered dose of codeine is metabolized by conjugation with glucuronic acid to codeine-6-glucuronide (C6G) and via O-demethylation.

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.

"Consumers and health care professionals will soon find updated labeling for extended-release and long-acting opioid pain relievers to help ensure their safe and appropriate use.

Here is a collection of user reviews for the medication Codeine Sulfate sorted by most helpful.

Codeine is absorbed from the gastrointestinal tract with maximum plasma concentration occurring 60 minutes post administration.

Last reviewed on RxList: 5/26/2011 This monograph has been modified to include the generic and brand name in many instances.

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