Rate-Limiting Step: Difference between revisions

Line 7:

Codeine (3-methylmorphine) is a [[prodrug]] for morphine. While codeine has some activity of its own, the vast majority of its pharmacological activity comes from its conversion to morphine. Codeine is metabolized into morphine in the liver by the enzyme P450 CYP2D6. Too much codeine will saturate these enzymes, leading to a "ceiling effect" around 400mg, where further dosage will not increase blood morphine concentrations. For this reason, codeine is ''relatively'' safe in overdose compared to other opiates, which is not to say that caution isn't warranted.

The same holds for codeine (3-methylmorphine)'s closely related chemical cousin, 3-[[ethylmorphine]]. Ethylmorphine is also metabolized by ~~P450(CYP)2D6~~.<ref>Zhurong Liu et al. (1995) ''Evidence for a role of cytochrome P450 2D6 and 3A4 in ethylmorphine metabolism'', retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364985/pdf/brjclinpharm00013-0077.pdf </ref>

The same holds for codeine (3-methylmorphine)'s closely related chemical cousin, 3-[[ethylmorphine]]. Ethylmorphine is also metabolized by CYP2D6.<ref>Zhurong Liu et al. (1995) ''Evidence for a role of cytochrome P450 2D6 and 3A4 in ethylmorphine metabolism'', retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364985/pdf/brjclinpharm00013-0077.pdf </ref>

===[[Lisdexamfetamine]]===

@@ Line 7: / Line 7: @@
 Codeine (3-methylmorphine) is a [[prodrug]] for morphine. While codeine has some activity of its own, the vast majority of its pharmacological activity comes from its conversion to morphine. Codeine is metabolized into morphine in the liver by the enzyme P450 CYP2D6. Too much codeine will saturate these enzymes, leading to a "ceiling effect" around 400mg, where further dosage will not increase blood morphine concentrations. For this reason, codeine is ''relatively'' safe in overdose compared to other opiates, which is not to say that caution isn't warranted.
-The same holds for codeine (3-methylmorphine)'s closely related chemical cousin, 3-[[ethylmorphine]]. Ethylmorphine is also metabolized by P450(CYP)2D6.<ref>Zhurong Liu et al. (1995) ''Evidence for a role of cytochrome P450 2D6 and 3A4 in ethylmorphine metabolism'', retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364985/pdf/brjclinpharm00013-0077.pdf </ref>
+The same holds for codeine (3-methylmorphine)'s closely related chemical cousin, 3-[[ethylmorphine]]. Ethylmorphine is also metabolized by CYP2D6.<ref>Zhurong Liu et al. (1995) ''Evidence for a role of cytochrome P450 2D6 and 3A4 in ethylmorphine metabolism'', retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364985/pdf/brjclinpharm00013-0077.pdf </ref>
 ===[[Lisdexamfetamine]]===