Paradoxical Role of Cytochrome P450 3A in the Bioactivation and Clinical Effects of Levo-α-Acetylmethadol: Importance of Clinical Investigations to Validate In Vitro …

ED Kharasch, D Whittington, C Hoffer, K Krudys… - Clinical …, 2005 - Springer
Abstract Objective: Levo-α-acetylmethadol (LAAM, levacetylmethadol) is a long-acting
opioid agonist used for the prevention of opioid withdrawal. LAAM undergoes sequential N …
被引用次数：20 相关文章 所有 6 个版本

Ketoconazole, a cytochrome P450 3A4 inhibitor, markedly increases concentrations of Levo‐acetyl‐α‐methadol in ppioid‐naive individuals

DE Moody, SL Walsh, DE Rollins… - Clinical …, 2004 - Wiley Online Library
Background Levo‐acetyl‐α‐methadol (LAAM) exerts most of it μ‐agonist activity through the
action of its 2 N‐demethylation metabolites, norLAAM and dinorLAAM. The N‐demethylation …
被引用次数：35 相关文章 所有 7 个版本
[PDF] psu.edu

Metabolism of levo-α-acetylmethadol (LAAM) by human liver cytochrome P450: involvement of CYP3A4 characterized by atypical kinetics with two binding sites

Y Oda, ED Kharasch - Journal of Pharmacology and Experimental …, 2001 - ASPET
levo-α-Acetylmethadol (LAAM) is a long-acting opioid agonist prodrug used for preventing
opiate withdrawal. LAAM undergoes bioactivation via sequential N-demethylation to nor …
被引用次数：44 相关文章 所有 5 个版本

Determination of l-α-acetylmethadol (LAAM), norLAAM, and dinorLAAM in clinical and in vitro samples using liquid chromatography with electrospray ionization and …

W Huang, PA Bemis, MH Slawson… - Journal of pharmaceutical …, 2003 - Elsevier
ABSTRACT l-α-Acetylmethadol (LAAM) is an alternative to methadone for the maintenance
treatment of opioid dependence. LAAM has a longer therapeutic half-life than methadone …
被引用次数：11 相关文章 所有 7 个版本

Metabolism of methadone andlevo-α-acetylmethadol (LAAM) by human intestinal cytochrome P450 3A4 (CYP3A4): potential contribution of intestinal metabolism to …

Y Oda, ED Kharasch - Journal of Pharmacology and Experimental …, 2001 - ASPET
Methadone and levo-α-acetylmethadol (LAAM) are opioid agonists used for analgesia and
preventing opiate withdrawal. Methadone is sequentially N-demethylated to the inactive …
被引用次数：107 相关文章 所有 3 个版本

The Involvement of Cytochrome P450 3A4 in theN-Demethylation ofl-α-Acetylmethadol (LAAM), norLAAM, and Methadone

DE Moody, ME Alburges, RJ Parker, JM Collins… - Drug Metabolism and …, 1997 - ASPET
The N-demethylation of LAAM, norLAAM, and methadone has been investigated in human
liver microsomes and microsomes containing cDNA-expressed human P450s. Gas …
被引用次数：180 相关文章 所有 5 个版本
[PDF] psu.edu

Intravenous and oral l-α-acetylmethadol: pharmacodynamics and pharmacokinetics in humans

SL Walsh, RE Johnson, EJ Cone, GE Bigelow - Journal of Pharmacology …, 1998 - ASPET
Levo-α-acetylmethadol (LAAM) is a long-acting opioid agonist approved for use as a
maintenance treatment for opioid dependence. Previous clinical studies report that the onset …
被引用次数：44 相关文章 所有 8 个版本

Paroxetine, a Cytochrome P450 2D6 Inhibitor, Diminishes the Stereoselective O‐demethylation and Reduces the Hypoalgesic Effect of Tramadol

S Laugesen, TP Enggaard… - Clinical …, 2005 - Wiley Online Library
Objective Tramadol hydrochloride (INN, tramadol) exerts its antinociceptive action through a
monoaminergic effect mediated by the parent compound and an opioid effect mediated …
被引用次数：136 相关文章 所有 7 个版本

Pharmacokinetic interactions of almorexant with midazolam and simvastatin, two CYP3A4 model substrates, in healthy male subjects

M Hoch, P Hoever, F Alessi, R Theodor… - European journal of …, 2013 - Springer
Purpose Pre-clinical experiments have shown that almorexant, a dual orexin receptor
antagonist, is able to inhibit cytochrome P450 3A4 (CYP3A4). Therefore, a study was …
被引用次数：30 相关文章 所有 9 个版本
[PDF] psu.edu

Relative potency of levo-α-Acetylmethadol and methadone in humans under acute dosing conditions

T Eissenberg, ML Stitzer, GE Bigelow… - … of Pharmacology and …, 1999 - ASPET
levo-α-Acetylmethadol (LAAM) and methadone are full μ-opioid agonists used to treat opioid
dependence. Current labeling indicates that LAAM is less potent than methadone. Clinical …
被引用次数：26 相关文章 所有 8 个版本