Pharmacokinetics of Methadone

References

• Caravati E M, Grey T, Nangle B, Rolfs R T, Peterson-Porucznik C A. Increase in poisoning deaths caused by non-illicit drugs-Utah, 1991–2003. MMWR Morb Mortal Wkly Rep 2005; 54(2)33–6
   Google Scholar
• Reisine T, Pasternak G. Opioid analgesics and antagonists. Goodman and Gilman's The Pharmacologic Basis of Therapeutics, 9th ed., L E Limbird, J G Hardman. McGraw-Hill, New York 1996; 521–55
   Google Scholar
• Ebert B, Thorkildsen C, Andersen S, Christrup L L, Hjeds H. Opioid analgesics as noncompetitive N-methyl-D-aspartate (NMDA) antagonists. Biochem Pharmacol 1998; 56(5)553–9
   PubMed Web of Science ®Google Scholar
• Liu J G, Anand K J. Protein kinases modulate the cellular adaptations associated with opioid tolerance and dependence. Brain Res Brain Res Rev 2001; 38(1–2)1–19
   Google Scholar
• Mao J. NMDA and opioid receptors: their interactions in antinociception, tolerance and neuroplasticity. Brain Res Brain Res Rev 1999; 30(3)289–304
   Google Scholar
• Eap C B, Buclin T, Baumann P. Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence. Clin Pharmacokinet 2002; 41(14)1153–93
   PubMed Web of Science ®Google Scholar
• de Castro J, Aguirre C, Rodriguez-Sasiain J M, Gomez E, Garrido M J, Calvo R. The effect of changes in gastric pH induced by omeprazole on the absorption and respiratory depression of methadone. Biopharm Drug Dispos 1996; 17(7)551–63
   Google Scholar
• Ferrari A, Coccia C P, Bertolini A, Sternieri E. Methadone-metabolism, pharmacokinetics and interactions. Pharmacol Res 2004; 50(6)551–9
   PubMed Web of Science ®Google Scholar
• Dale O, Sheffels P, Kharasch E D. Bioavailabilities of rectal and oral methadone in healthy subjects. Br J Clin Pharmacol 2004; 58(2)156–62
   PubMed Web of Science ®Google Scholar
• Ripamonti C, Zecca E, Brunelli C, et al. Rectal methadone in cancer patients with pain. A preliminary clinical and pharmacokinetic study. Ann Oncol 1995; 6(8)841–3
   Google Scholar
• Grabinski P Y, Kaiko R F, Rogers A G, Houde R W. Plasma levels and analgesia following deltoid and gluteal injections of methadone and morphine. J Clin Pharmacol 1983; 23(1)48–55
   Google Scholar
• de Vos J W, Geerlings P J, van den Brink W, Ufkes J G, van Wilgenburg H. Pharmacokinetics of methadone and its primary metabolite in 20 opiate addicts. Eur J Clin Pharmacol 1995; 48(5)361–6
   PubMed Web of Science ®Google Scholar
• Blinick G, Inturrisi C E, Jerez E, Wallach R C. Amniotic fluid methadone in women maintained on methadone. Mt Sinai J Med 1974; 41(2)254–9
   Google Scholar
• Blinick G, Inturrisi C E, Jerez E, Wallach R C. Methadone assays in pregnant women and progeny. Am J Obstet Gynecol 1975; 121(5)617–21
   PubMed Web of Science ®Google Scholar
• Eap C B, Cuendet C, Baumann P. Binding of d-methadone, l-methadone, and dl-methadone to proteins in plasma of healthy volunteers: role of the variants of alpha 1-acid glycoprotein. Clin Pharmacol Ther 1990; 47(3)338–46
   PubMed Web of Science ®Google Scholar
• Wilkins J N, Ashofteh A, Setoda D, Wheatley W S, Huigen H, Ling W. Ultrafiltration using the Amicon MPS-1 for assessing methadone plasma protein binding. Ther Drug Monit 1997; 19(1)83–7
   PubMed Web of Science ®Google Scholar
• Abramson F P. Methadone plasma protein binding: alterations in cancer and displacement from alpha 1-acid glycoprotein. Clin Pharmacol Ther 1982; 32(5)652–8
   PubMed Web of Science ®Google Scholar
• Romach M K, Piafsky K M, Abel J G, Khouw V, Sellers E M. Methadone binding to orosomucoid (alpha 1-acid glycoprotein): determinant of free fraction in plasma. Clin Pharmacol Ther 1981; 29(2)211–7
   PubMed Web of Science ®Google Scholar
• American Academy of Pediatrics committee on drugs: neonatal drug withdrawal. Pediatrics 1983; 72: 895–902
   Google Scholar
• McCarthy J J, Posey B L. Methadone levels in human milk. J Hum Lact 2000; 16(2)115–20
   PubMedGoogle Scholar
• Wojnar-Horton R E, Kristensen J H, Yapp P, Ilett K F, Dusci L J, Hackett L P. Methadone distribution and excretion into breast milk of clients in a methadone maintenance programme. Br J Clin Pharmacol 1997; 44(6)543–7
   PubMed Web of Science ®Google Scholar
• Begg E J, Malpas T J, Hackett L P, Ilett K F. Distribution of R- and S-methadone into human milk during multiple, medium to high oral dosing. Br J Clin Pharmacol 2001; 52(6)681–5
   PubMed Web of Science ®Google Scholar
• Malpas T J, Darlow B A, Lennox R, Horwood L J. Maternal methadone dosage and neonatal withdrawal. Aust N Z J Obstet Gynaecol 1995; 35(2)175–7
   PubMed Web of Science ®Google Scholar
• Malpas T J, Darlow B A. Neonatal abstinence syndrome following abrupt cessation of breastfeeding. N Z Med J 1999; 112(1080)12–3
   PubMedGoogle Scholar
• Beckett A H, Taylor J F, Casy A F, Hassan M M. The biotransformation of methadone in man: synthesis and identification of a major metabolite. J Pharm Pharmacol 1968; 20(10)754–62
   PubMedGoogle Scholar
• Verebely K, Volavka J, Mule S, Resnick R. Methadone in man: pharmacokinetic and excretion studies in acute and chronic treatment. Clin Pharmacol Ther 1975; 18(2)180–90
   PubMedGoogle Scholar
• Anggard E, Gunne L M, Homstrand J, McMahon R E, Sandberg C G, Sullivan H R. Disposition of methadone in methadone maintenance. Clin Pharmacol Ther 1975; 17(3)258–66
   PubMedGoogle Scholar
• Iribarne C, Berthou F, Baird S, et al. Involvement of cytochrome P450 3A4 enzyme in the N-demeth-ylation of methadone in human liver microsomes. Chem Res Toxicol 1996; 9(2)365–73
   PubMed Web of Science ®Google Scholar
• Moody D E, Alburges M E, Parker R J, Collins J M, Strong J M. The involvement of cytochrome P450 3A4 in the N-demethylation of L-alpha-acetylmethadol (LAAM), norLAAM, and methadone. Drug Metab Dispos 1997; 25(12)1347–53
   PubMed Web of Science ®Google Scholar
• Peng P W, Tumber P S, Gourlay D. Review article: Perioperative pain management of patients on methadone therapy: [Expose de synthese: Traitement de la douleur perioperatoire chez les patients sous therapie a la methadone]. Can J Anaesth 2005; 52(5)513–23
   Google Scholar
• Kharasch E D, Hoffer C, Whittington D, Sheffels P. Role of hepatic and intestinal cytochrome P450 3A and 2B6 in the metabolism, disposition, and miotic effects of methadone. Clin Pharmacol Ther 2004; 76(3)250–69
   PubMed Web of Science ®Google Scholar
• Foster D J, Somogyi A A, Bochner F. Methadone N-demethylation in human liver microsomes: lack of stereoselectivity and involvement of CYP3A4. Br J Clin Pharmacol 1999; 47(4)403–12
   PubMed Web of Science ®Google Scholar
• Bertschy G, Eap C B, Powell K, Baumann P. Fluoxetine addition to methadone in addicts: pharmacokinetic aspects. Ther Drug Monit 1996; 18(5)570–2
   PubMed Web of Science ®Google Scholar
• Eap C B, Bertschy G, Powell K, Baumann P. Fluvoxamine and fluoxetine do not interact in the same way with the metabolism of the enantiomers of methadone. J Clin Psychopharmacol 1997; 17(2)113–7
   PubMed Web of Science ®Google Scholar
• Wang J S, DeVane C L. Involvement ofCYP3A4, CYP2C8, and CYP2D6 in the metabolism of (R)- and (S)-methadone in vitro. Drug Metab Dispos 2003; 31(6)742–7
   PubMed Web of Science ®Google Scholar
• Gerber J G, Rhodes R J, Gal J. Stereoselective metabolism of methadone N-demethylation by cytochrome P4502B6 and 2C19. Chirality 2004; 16(1)36–44
   PubMed Web of Science ®Google Scholar
• Boulton D W, Arnaud P, DeVane C L. Pharmacokinetics and pharmacodynamics of methadone enantiomers after a single oral dose of racemate. Clin Pharmacol Ther 2001; 70(1)48–57
   PubMed Web of Science ®Google Scholar
• Eap C B, Broly F, Mino A, et al. Cytochrome P450 2D6 genotype and methadone steady-state concentrations. J Clin Psychopharmacol 2001; 21(2)229–34
   PubMed Web of Science ®Google Scholar
• Inturrisi C E, Colburn W A, Kaiko R F, Houde R W, Foley K M. Pharmacokinetics and pharmacodynamics of methadone in patients with chronic pain. Clin Pharmacol Ther 1987; 41(4)392–401
   PubMed Web of Science ®Google Scholar
• Plummer J L, Gourlay G K, Cherry D A, Cousins M J. Estimation of methadone clearance: application in the management of cancer pain. Pain 1988; 33: 313–22
   PubMed Web of Science ®Google Scholar
• Kristensen K, Blemmer T, Angelo H R, et al. Stereoselective pharmacokinetics of methadone in chronic pain patients. Ther Drug Monit 1996; 18(3)221–7
   PubMed Web of Science ®Google Scholar
• Foster D J, Somogyi A A, White J M, Bochner F. Population pharmacokinetics of (R)-, (S)- and rac-methadone in methadone maintenance patients. Br J Clin Pharmacol 2004; 57(6)742–55
   PubMed Web of Science ®Google Scholar
• Wolff K, Rostami-Hodjegan A, Hay A W, Raistrick D, Tucker G. Population-based pharmacokinetic approach for methadone monitoring of opiate addicts: potential clinical utility. Addiction 2000; 95(12)1771–83
   PubMed Web of Science ®Google Scholar
• Rostami-Hodjegan A, Wolff K, Hay A W, Raistrick D, Calvert R, Tucker G T. Population pharmacokinetics of methadone in opiate users: characterization of time-dependent changes. Br J Clin Pharmacol 1999; 48(1)43–52
   PubMed Web of Science ®Google Scholar
• Berkowitz B A. The relationship of pharmacokinetics to pharmacological activity: morphine, methadone and naloxone. Clin Pharmacokinet 1976; 1(3)219–30
   PubMedGoogle Scholar
• Baselt R C, Casarett L J. Urinary excretion of methadone in man. Clin Pharmacol Ther 1972; 13(1)64–70
   Google Scholar
• Dean M. Opioids in renal failure and dialysis patients. J Pain Symptom Manage 2004; 28(5)497–504
   PubMed Web of Science ®Google Scholar
• Mather L E. Opioid pharmacokinetics in relation to their effects. Anaesth Intensive Care 1987; 15(1)15–22
   Google Scholar
• Inturrisi C E, Verebely K. Disposition of methadone in man after a single oral dose. Clin Pharmacol Ther 1972; 13(6)923–30
   Google Scholar
• Kreek M J, Schecter A J, Gutjahr C L, Hecht M. Methadone use in patients with chronic renal disease. Drug and Alcohol Dependence 1980; 5(3)197
   PubMed Web of Science ®Google Scholar
• Anderson R J, Schrier R W. Clinical use of drugs in patients with kidney and liver disease. WB Saunders Co., Philadelphia 1981
   Google Scholar
• Izzo A A. Drug interactions with St. John's Wort (Hypericum perforatum): a review of the clinical evidence. Int J Clin Pharmacol Ther 2004; 42(3)139–48
   PubMed Web of Science ®Google Scholar
• Tong T G, Pond S M, Kreek M J, Jaffery N F, Benowitz N L. Phenytoin-induced methadone withdrawal. Ann Intern Med 1981; 94(3)349–51
   PubMed Web of Science ®Google Scholar
• Bending M R, Skacel P O. Rifampicin and methadone withdrawal. Lancet 1977; 1(8023)1211
   Google Scholar
• Kreek M J, Garfield J W, Gutjahr C L, Giusti L M. Rifampin-induced methadone withdrawal. N Engl J Med 1976; 294: 1104–6
   PubMed Web of Science ®Google Scholar
• Clarke S M, Mulcahy F M, Tjia J, et al. The pharmacokinetics of methadone in HIV-positive patients receiving the non-nucleoside reverse transcriptase inhibitor efavirenz. Br J Clin Pharmacol 2001; 51(3)213–7
   PubMed Web of Science ®Google Scholar
• Heelon M W, Meade L B. Methadone withdrawal when starting an antiretroviral regimen including nevirapine. Pharmacotherapy 1999; 19(4)471–2
   PubMed Web of Science ®Google Scholar
• Hendrix C W, Wakeford J, Wire M B, et al. Pharmacokinetics and pharmacodynamics of methadone enantiomers after co-administration with amprenavir in opioid-dependent subjects. Pharmacotherapy 2004; 24(9)1110–21
   Google Scholar
• Bart P A, Rizzardi P G, Gallant S, et al. Methadone blood concentrations are decreased by the administration of abacavir plus amprenavir. Ther Drug Monit 2001; 23(5)553–5
   PubMed Web of Science ®Google Scholar
• Smith P F, Kearney B P, Liaw S, et al. Effect of tenofovir disoproxil fumarate on the pharmacokinetics and pharmacodynamics of total, R-, and S-methadone. Pharmacotherapy 2004; 24(8)970–7
   Google Scholar
• Gourevitch M N, Friedland G H. Interactions between methadone and medications used to treat HIV infection: A review. Mt Sinai J Med 2000; 67(5–6)429–36
   PubMedGoogle Scholar
• Corkery J M, Schifano F, Ghodse A H, Oyefeso A. The effects of methadone and its role in fatalities. Hum Psychopharmacol 2004; 19(8)565–76
   Google Scholar
• Pearson E C, Woosley R L. QT prolongation and torsades de pointes among methadone users: Reports to the FDA spontaneous reporting system. Pharmacoepidemiol Drug Saf 2005
   Google Scholar
• Cobb M N, Desai J, Brown L S, Zannikos P N, Rainey P M. The effect of fluconazole on the clinical pharmacokinetics of methadone. Clin Pharmacol Ther 1998; 63: 655–62
   PubMed Web of Science ®Google Scholar
• Iribarne C, Berthou F, Carlhant D, et al. Inhibition of methadone and buprenorphine N-dealkylations by three HIV-1 protease inhibitors. Drug Metab Dispos 1998; 23: 257–60
   Google Scholar
• Shelton M J, Cloen D, DiFrancesco R, et al. The effects of once-daily saquinavir/minidose ritonavir on the pharmacokinetics of methadone. J Clin Pharmacol 2004; 44(3)293–304
   Google Scholar
• Benmebarek M, Devaud C, Gex-Fabry M, et al. Effects of grapefruit juice on the pharmacokinetics of the enantiomers of methadone. Clin Pharmacol Ther 2004; 76(1)55–63
   PubMed Web of Science ®Google Scholar
• Boulton D W, Arnaud P, DeVane C L. A single dose of methadone inhibits cytochrome P-4503A activity in healthy volunteers as assessed by the urinary cortisol ratio. Br J Clin Pharmacol 2001; 51(4)350–4
   Google Scholar
• Hamilton S P, Nunes E V, Janal M, Weber L. The effect of sertraline on methadone plasma levels in methadone-maintenance patients. Am J Addict 2000; 9(1)63–9
   PubMedGoogle Scholar
• Baumann P. Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet 1996; 31(6)444–69
   PubMed Web of Science ®Google Scholar
• Bertschy G, Baumann P, Eap C B, Baettig D. Probable metabolic interaction between methadone and fluvoxamine in addict patients. Ther Drug Monit 1994; 16(1)42–5
   PubMed Web of Science ®Google Scholar
• Begre S, von Bardeleben U, Ladewig D, et al. Paroxetine increases steady-state concentrations of (R)-methadone in CYP2D6 extensive but not poor metabolizers. J Clin Psychopharmacol 2002; 22(2)211–5
   PubMed Web of Science ®Google Scholar
• Wang J S, Ruan Y, Taylor R M, Donovan J L, Markowitz J S, DeVane C L. Brain penetration of methadone (R)- and (S)-enantiomers is greatly increased by P-glycoprotein deficiency in the blood-brain barrier of Abcb1a gene knockout mice. Psychopharmacology (Berl) 2004; 173(1–2)132–8
   Google Scholar
• Rodriguez M, Ortega I, Soengas I, Suarez E, Lukas J C, Calvo R. Effect of P-glycoprotein inhibition on methadone analgesia and brain distribution in the rat. J Pharm Pharmacol 2004; 56(3)367–74
   PubMed Web of Science ®Google Scholar
• Kharasch E D, Hoffer C, Whittington D. The effect of quinidine, used as a probe for the involvement of P-glycoprotein, on the intestinal absorption and pharmacodynamics of methadone. Br J Clin Pharmacol 2004; 57(5)600–10
   PubMed Web of Science ®Google Scholar
• Marzolini C, Troillet N, Telenti A, Baumann P, Decosterd L A, Eap C B. Efavirenz decreases methadone blood concentrations. Aids 2000; 14(9)1291–2
   Google Scholar
• Lin J H, Yamazaki M. Role of P-glycoprotein in pharmacokinetics: Clinical implications. Clin Pharmacokinet 2003; 42(1)59–98
   PubMed Web of Science ®Google Scholar
• Bruera E, Fainsinger R, Moore M, Thibault R, Spoldi E, Ventafridda V. Local toxicity with subcutaneous methadone. Experience of two centers. Pain 1991; 45(2)141–3
   Google Scholar
• Mathew P, Storey P. Subcutaneous methadone in terminally ill patients: manageable local toxicity. J Pain Symptom Manage 1999; 18(1)49–52
   PubMedGoogle Scholar
• Ettinger D S, Vitale P J, Trump D L. Important clinical pharmacologic considerations in the use of methadone in cancer patients. Cancer Treat Rep 1979; 63: 457–9
   PubMedGoogle Scholar
• Inturrisi C E. Clinical pharmacology of opioids for pain. Clin J Pain 2002; 18(4 Suppl)S3–13
   PubMed Web of Science ®Google Scholar
• AHFS Drug Information. American Society of Health-System Pharmacists, Bethesda 2001
   Google Scholar
• Weinberg D S, Inturrisi C E, Reidenberg B, et al. Sublingual absorption of selected opioid analgesics. Clin Pharmacol Ther 1988; 44(3)335–42
   PubMed Web of Science ®Google Scholar
• Dale O, Hoffer C, Sheffels P, Kharasch E D. Disposition of nasal, intravenous, and oral methadone in healthy volunteers. Clin Pharmacol Ther 2002; 72(5)536–45
   PubMed Web of Science ®Google Scholar
• Galer B S, Coyle N, Pasternak G W, Portenoy R K. Individual variability in the response to different opioids: report of five cases. Pain 1992; 49: 87–91
   PubMed Web of Science ®Google Scholar
• Mitchell T B, White J M, Somogyi A AF. B. Comparative pharmacodynamics and pharmacokinetics of methadone and slow-release oral morphine for maintenance treatment of opioid dependence. Drug Alcohol Depend 2003; 72: 85–94
   PubMed Web of Science ®Google Scholar
• Ripamonti C, Groff L, Brunelli C, Polastri D, Stavrakis A, De Conno F. Switching from morphine to oral methadone in treating cancer pain: what is the equianalgesic dose ratio?. J Clin Oncol 1998; 16(10)3216–21
   PubMed Web of Science ®Google Scholar
• Fainsinger R, Schoeller T, Bruera E. Methadone in the management of cancer pain: A review. Pain 1993; 52(2)137–47
   PubMed Web of Science ®Google Scholar
• Wolff K, Sanderson M, Hay A W, Raistrick D. Methadone concentrations in plasma and their relationship to drug dosage. Clin Chem 1991; 37(2)205–9
   PubMed Web of Science ®Google Scholar
• Methadone Drug Evaluation. Thomson MICRO-MEDEX. 2005
   Google Scholar
• Novick D M, Kreek M J, Fanizza A M, Yancovitz S R, Gelb A M, Stenger R J. Methadone disposition in patients with chronic liver disease. Clin Pharmacol Ther 1981; 30: 353–62
   PubMedGoogle Scholar
• Denson D D, Concilus R R, Warden G, Raj P P. Pharmacokinetics of continuous intravenous infusion of methadone in the early post-burn period. J Clin Pharmacol 1990; 30(1)70–5
   Google Scholar
• Pond S M, Kreek M J, Tong T G, Raghunath J, Benowitz N L. Altered methadone pharmacokinetics in methadone-maintained pregnant women. J Pharmacol Exp Ther 1985; 233(1)1–6
   PubMed Web of Science ®Google Scholar
• Jarvis M A, Wu-Pong S, Kniseley J S, Schnoll S H. Alterations in methadone metabolism during late pregnancy. J Addict Dis 1999; 18(4)51–61
   PubMed Web of Science ®Google Scholar
• Swift R M, Dudley M, DePetrillo P, Camara P, Griffiths W. Altered methadone pharmacokinetics in pregnancy: implications for dosing. J Subst Abuse 1989; 1(4)453–60
   Google Scholar
• Chana S K, Anand K J. Can we use methadone for analgesia in neonates?. Arch Dis Child Fetal Neonatal Ed 2001; 85(2)F79–81
   Google Scholar
• Lugo R A, MacLaren R, Cash J, Pribble C G, Vernon D D. Enteral methadoneto expedite fentanyl discontinuation and prevent opioid abstinence syndrome in the PICU. Pharmacotherapy 2001; 21(12)1566–73
   Google Scholar
• Tobias J D, Deshpande J K, Gregory D F. Outpatient therapy of iatrogenic drug dependency following prolonged sedation in the pediatric intensive care unit. Intensive Care Med 1994; 20(7)504–7
   Google Scholar
• Berde C B, Sethna N F, Hale R S. Pharmacokinetics of methadone in children and adolescents in the perioperative period. Anesthesiology 1987; 67: A519
   Google Scholar
• Yaster M, Deshpande J K, Maxwell L G. The pharmacologic management of pain in children. Compr Ther 1989; 15(10)14–26
   Google Scholar