Morfinmetabolisme-farmakokinetik og-dynamik
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Morfinmetabolisme-farmakokinetik og-dynamik. / Andersen, G; Christrup, Lona Louring; Sjøgren, P.
In: Ugeskrift for Laeger, Vol. 159, No. 22, 26.05.1997, p. 3383-6.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Morfinmetabolisme-farmakokinetik og-dynamik
AU - Andersen, G
AU - Christrup, Lona Louring
AU - Sjøgren, P
PY - 1997/5/26
Y1 - 1997/5/26
N2 - With the increasing use of morphine, growing interest for the clinical implications of its metabolites, morphine-3-glucuronide (M-3-G) and morphine-6-glucuronide (M-6-G) has emerged in the literature. M-6-G binds to the opioid receptor and has analgesic properties in man. Clinical studies have not delivered strong evidence of significant correlation between the concentration of morphine and its glucuronides in plasma and cerebrospinal fluid and pharmacodynamics such as analgesia. There is no clinical evidence to indicate that M-6-G has a pronounced respiratory depressing effect in man, while the literature contains conflicting reports with regard to other side-effects. M-3-G does not bind to the m-opioid receptor and consequently has no antinociceptive effects. Studies in rodents have shown that morphine, M-6-G and especially M-3-G may induce hyperalgesia, allodynia and myoclonus. It is assumed that these side effects are caused by a spinal antiglycinergic mechanism. The role of M-3-G in morphine antagonism and development of tolerance has not yet been settled. As M-3-G and M-6-G are eliminated by the kidneys, renal insufficiency will lead to accumulation of these. Accordingly dosage should be reduced or other opioids be considered in such cases.
AB - With the increasing use of morphine, growing interest for the clinical implications of its metabolites, morphine-3-glucuronide (M-3-G) and morphine-6-glucuronide (M-6-G) has emerged in the literature. M-6-G binds to the opioid receptor and has analgesic properties in man. Clinical studies have not delivered strong evidence of significant correlation between the concentration of morphine and its glucuronides in plasma and cerebrospinal fluid and pharmacodynamics such as analgesia. There is no clinical evidence to indicate that M-6-G has a pronounced respiratory depressing effect in man, while the literature contains conflicting reports with regard to other side-effects. M-3-G does not bind to the m-opioid receptor and consequently has no antinociceptive effects. Studies in rodents have shown that morphine, M-6-G and especially M-3-G may induce hyperalgesia, allodynia and myoclonus. It is assumed that these side effects are caused by a spinal antiglycinergic mechanism. The role of M-3-G in morphine antagonism and development of tolerance has not yet been settled. As M-3-G and M-6-G are eliminated by the kidneys, renal insufficiency will lead to accumulation of these. Accordingly dosage should be reduced or other opioids be considered in such cases.
KW - Humans
KW - Morphine
KW - Receptors, Opioid, mu
M3 - Tidsskriftartikel
C2 - 9199024
VL - 159
SP - 3383
EP - 3386
JO - Ugeskrift for Laeger
JF - Ugeskrift for Laeger
SN - 0041-5782
IS - 22
ER -
ID: 46098790