Opioid Metabolites Journal of Pain and Symptom Management

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Presentation transcript:

Opioid Metabolites Journal of Pain and Symptom Management Jörn Lötsch, MD, PhD Journal of Pain and Symptom Management Volume 29, Issue 5, Pages 10-24 (May 2005) DOI: 10.1016/j.jpainsymman.2005.01.004 Copyright © 2005 U.S. Cancer Pain Relief Committee Terms and Conditions

Fig. 1 Metabolism of tilidine, tramadol and meperidine into their active metabolites. The dotted frames show where the metabolic reaction takes place. Journal of Pain and Symptom Management 2005 29, 10-24DOI: (10.1016/j.jpainsymman.2005.01.004) Copyright © 2005 U.S. Cancer Pain Relief Committee Terms and Conditions

Fig. 2 Glucuronidation of opioids occurs only on free hydroxy groups. Therefore, morphine is metabolized into two glucuronides whereas hydromorphone is only metabolized into a 3-glucuronide (top). The glucuronidation of morphine is shown at the bottom. Journal of Pain and Symptom Management 2005 29, 10-24DOI: (10.1016/j.jpainsymman.2005.01.004) Copyright © 2005 U.S. Cancer Pain Relief Committee Terms and Conditions

Fig. 3 Metabolism of codeine and morphine metabolism. Journal of Pain and Symptom Management 2005 29, 10-24DOI: (10.1016/j.jpainsymman.2005.01.004) Copyright © 2005 U.S. Cancer Pain Relief Committee Terms and Conditions

Fig. 4 Metabolism of dihydrocodeine. Journal of Pain and Symptom Management 2005 29, 10-24DOI: (10.1016/j.jpainsymman.2005.01.004) Copyright © 2005 U.S. Cancer Pain Relief Committee Terms and Conditions

Fig. 5 Time course of pupil diameter and tolerance to electrical pain stimuli after administration of morphine (IV-infusion of up to 6.4 hours) to healthy volunteers.48 The contribution of M6G is given as dotted lines. This estimate bases on data obtained after administration of M6G at a separate study. These data were fitted to PK/PD model for pupil size and pain. The resulting models and parameter values were then used together with the M6G plasma concentrations after morphine administration to calculate the M6G-related time courses of pupil size and pain tolerance. Journal of Pain and Symptom Management 2005 29, 10-24DOI: (10.1016/j.jpainsymman.2005.01.004) Copyright © 2005 U.S. Cancer Pain Relief Committee Terms and Conditions