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Codeine: Difference between revisions
>8Brainzap8 codeine legality |
>Acetyl Redose note and continuation of cite. |
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Codeine is not itself centrally active, and must first be converted via first pass metabolism into [[morphine]] by the cytochrome P450 enzyme CYP2D6 (as such, it is a [[prodrug]] for morphine). Codeine is also metabolised into the inactive norcodeine via the CYP3A4 enzyme system. Both resultant forms are conjugated by UGT2B7 into their corresponding 3-glucuronide.{{citation needed}} | Codeine is not itself centrally active, and must first be converted via first pass metabolism into [[morphine]] by the cytochrome P450 enzyme CYP2D6 (as such, it is a [[prodrug]] for morphine). Codeine is also metabolised into the inactive norcodeine via the CYP3A4 enzyme system. Both resultant forms are conjugated by UGT2B7 into their corresponding 3-glucuronide.{{citation needed}} | ||
Some percentage of the population produce less CYP2D6 enzymes and so experience a significant reduction of effects from codeine in comparison to that of the average person. However, others produce CYP2D6 enzymes in higher quantities which can result in a hypersensitivity to the drug. Some methods of potentiating [[opioids]], such as using grapefruit juice throughout the day before consumption, inhibits the CYP3A4 enzyme.<ref>https://www.ncbi.nlm.nih.gov/pubmed/17995595</ref> This results in less codeine being converted into norcodeine which leaves more to be metabolised into morphine. | Some percentage of the population produce less CYP2D6 enzymes and so experience a significant reduction of effects from codeine in comparison to that of the average person. However, others produce CYP2D6 enzymes in higher quantities which can result in a hypersensitivity to the drug. Some methods of potentiating [[opioids]], such as using grapefruit juice throughout the day before consumption, inhibits the CYP3A4 enzyme.<ref>https://www.ncbi.nlm.nih.gov/pubmed/17995595</ref> This results in less codeine being converted into norcodeine which leaves more to be metabolised into morphine. This also indicates a lacking capability in metabolism of codeine into morphine when a user consumes antihistamines such as [[diphenhydramine]] prior to ingestion of codeine. <ref>https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2148980/</ref> | ||
There is an upper limit to the amount of codeine which can be converted by enzymatic metabolism into morphine throughout an individual session. This limit is commonly referred to as the "ceiling dose", which is commonly believed to be around 400mg. Consuming higher doses will lead to greater side effects such as [[itchiness]] and [[nausea]], but will not increase [[euphoria]]. | There is an upper limit to the amount of codeine which can be converted by enzymatic metabolism into morphine throughout an individual session. This limit is commonly referred to as the "ceiling dose", which is commonly believed to be around 400mg. Consuming higher doses will lead to greater side effects such as [[itchiness]] and [[nausea]], but will not increase [[euphoria]]. | ||
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*'''[[Effect::Cognitive euphoria]]''' - This particular substance can be considered as less intense in its cognitive euphoria when compared with that of [[morphine]] or [[diacetylmorphine]] (heroin) due to the upper limit of how much can be converted into its active form through metabolism. It is still, however, capable of extreme intensity and overwhelming bliss at heavier dosages with a low tolerance. The sensation itself can be described as powerful and overwhelming feeling of emotional bliss, contentment, and happiness. | *'''[[Effect::Cognitive euphoria]]''' - This particular substance can be considered as less intense in its cognitive euphoria when compared with that of [[morphine]] or [[diacetylmorphine]] (heroin) due to the upper limit of how much can be converted into its active form through metabolism. It is still, however, capable of extreme intensity and overwhelming bliss at heavier dosages with a low tolerance. The sensation itself can be described as powerful and overwhelming feeling of emotional bliss, contentment, and happiness. | ||
*'''[[Effect::Anxiety suppression]]''' | *'''[[Effect::Anxiety suppression]]''' | ||
*'''[[Effect::Compulsive redosing]]''' | *'''[[Effect::Compulsive redosing]]''' - It is worth noting that redosing codeine will not amplify the intensity of its effects. | ||
*'''[[Effect::Dream potentiation]]''' | *'''[[Effect::Dream potentiation]]''' | ||
*'''[[Effect::Sleepiness]]''' | *'''[[Effect::Sleepiness]]''' | ||