Pharmacodynamics and Pharmacokinetics of Methadone during the Perioperative Period

Gourlay, Geoffrey K.; Wilson, Peter; Glynn, C. J.

doi:10.1097/00000542-198212000-00005

Cited by 168 publications

(102 citation statements)

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“…In comparison, the median minimal effective (postoperative) analgesia threshold for (racemic) methadone was 31 ng/ml. 57 Both IV and oral cyclosporine caused cutaneous sensitization to heat, similar to that reported previously for IV cyclosporine. 21 This sensitization differs from the well-described pain syndrome (bilateral bone pain in the lower extremities) caused by cyclosporine.…”

Section: Discussionsupporting

confidence: 83%

Cyclosporine-inhibitable Cerebral Drug Transport Does Not Influence Clinical Methadone Pharmacodynamics: Erratum

2015

Anesthesiology

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Background-Interindividual variability and drug interaction studies suggest that blood-brain barrier drug transporters mediate human methadone brain biodistribution. In vitro and animal studies suggest that methadone is a substrate for the efflux transporter P-glycoprotein, and that Pglycoprotein-mediated transport influences brain access and pharmacologic effect. This investigation tested whether methadone is a transporter substrate in humans.

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Section: Discussionsupporting

confidence: 83%

Cyclosporine-inhibitable Cerebral Drug Transport Does Not Influence Clinical Methadone Pharmacodynamics: Erratum

2015

Anesthesiology

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“…administration of 20 mg methadone) ranges from 20-60 ng/ml (mean value of 30 ng/ml). The terminal half-life varies from 10-78 h in these post-operative patients (Gourlay et al, 1983). Both nor-methadone and methadone are metabolised by similar routes in a range of animal species which involves N-demethylation followed by spontaneous rearrangement to produce pyrroline derivatives and N-oxide formation (Beckett etal., 1971a).…”

Section: Discussionmentioning

confidence: 99%

The role of naloxone infusions in the treatment of overdoses of long half‐life narcotic agonists: application to nor‐methadone.

Gourlay¹,

Coulthard²

1983

Brit J Clinical Pharma

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This report describes the use of a naloxone infusion at a rate of 300 ,ug/h to provide constant antagonism of the respiratory depressant effects of a near fatal nor-methadone dose in a 2 year old boy. The terminal half-life for nor-methadone was calculated to be 13.5 h. The results indicate that a single dose of a narcotic antagonist with a short half-life (e.g. naloxone) will probably be inadequate to provide long lasting reversal of the effects of overdoses of long half-life narcotic agonists, and that continuous infusion may be the preferable to repeated bolus doses.

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“…[91] Methadone is metabolised, mainly by Nmethylation, in the liver to 1,5-dimethyl-2-ethyl-3,3-diphenyl-1-pyrroline, the main metabolite. However, renal excretion of the unchanged drug is an important route of methadone elimination, accounting for approximately 20% of an administered single oral doseJ92] The majority of methadone (as the metabolite) is excreted in the faeces.…”

Section: 1 Summary Of Pharmacokineticsmentioning

confidence: 99%

Pharmacokinetics of Opioids in Renal Dysfunction

Davies

Kingswood

Street

1996

Clinical Pharmacokinetics

159

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Patients with renal insufficiency commonly require the administration of an opioid analgesic to provide adequate pain relief. The handling of morphine, pethidine (meperidine) and dextropropoxyphene in patients with renal insufficiency is complicated by the potential accumulation of metabolites. While morphine itself remains largely unaffected by renal failure, accumulation, as denoted by an increase in both mean peak concentrations and the area under the concentration-time curve, of both the active metabolite (morphine-6-glucuronide) and the principal metabolite (morphine-3-glucuronide, thought to possess opiate antagonist properties) have been reported. The increased elimination half-lives of the toxic metabolites norpethidine and norpropoxyphene in patients with poor renal function administered pethidine and dextropropoxyphene, respectively, makes their routine use ill advised. Case reports of prolonged narcosis associated with the use of both codeine and dihydrocodeine in patients with renal insufficiency call for care to be used when prescribing these agents under such conditions. Although the pharmacokinetics of buprenorphine, alfentanil, sufentanil and remifentanil change little in patients with renal failure, the continuous administration of fentanyl can lead to prolonged sedation.

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Pharmacodynamics and Pharmacokinetics of Methadone during the Perioperative Period

Cited by 168 publications

References 0 publications

Cyclosporine-inhibitable Cerebral Drug Transport Does Not Influence Clinical Methadone Pharmacodynamics: Erratum

Cyclosporine-inhibitable Cerebral Drug Transport Does Not Influence Clinical Methadone Pharmacodynamics: Erratum

The role of naloxone infusions in the treatment of overdoses of long half‐life narcotic agonists: application to nor‐methadone.

Pharmacokinetics of Opioids in Renal Dysfunction

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