Aminorex and rexamino as metabolites of levamisole in the horse

Ho, Emmie N.M.; Leung, David K.K.; Leung, Gary N. W.; Wan, Terence S.M.; Wong, April S. Y.; Wong, Colton H.F.; Soma, Lawrence R.; Rudy, Jeffrey A.; Uboh, Cornelius E.; Samś, R. A.

doi:10.1016/j.aca.2009.02.033

Cited by 40 publications

(51 citation statements)

References 7 publications

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“…Although unlikely due to species-specific action of levamisole, it is theoretically possible that cocaine and levamisole may have a synergistic action at nicotinic acetylcholine receptors resulting in increased nicotinic and dopaminergic effects [26]. Also, studies in horses have suggested that levamisole may get metabolized to aminorex, an amphetamine derivative with stimulant effects similar to cocaine and amphetamine [34]. Other possible explanation for using levamisole as a cocaine adulterant may be its use as a “marker” or “signature” compound by manufacturers to trace its market distribution [26].…”

Section: Discussionmentioning

confidence: 99%

Levamisole-induced leukocytoclastic vasculitis and neutropenia in a patient with cocaine use: An extensive case with necrosis of skin, soft tissue, and cartilage

Arora

Jain

Bhanot

et al. 2012

Addict Sci Clin Pract

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Levamisole-induced vasculitis is a relatively new entity in people who use cocaine. We describe a 44-year-old woman with a history of cocaine use who presented with a complaint of a painful rash of 2-3 month’s duration on her extremities, cheeks, nose, and earlobes. She had not experienced fever, weight loss, alopecia, dry eyes, oral ulcers, photosensitivity, or arthralgia. Examination revealed tender purpuric eruptions with central necrosis on her nose, cheeks, earlobes, and extremities. Laboratory investigations revealed neutropenia, an elevated erythrocyte sedimentation rate (ESR), presence of lupus anticoagulant, low complement component 3 (C3), and presence of perinuclear anti-neutrophil cytoplasmic antibody (p-ANCA). A urine toxicology screen was positive for cocaine, and gas chromatography–mass spectrometry was positive for levamisole. Skin biopsy showed leukocytoclastic vasculitis and small vessel thrombosis. Necrotic lesions of the nose led to its self-amputation. Large bullae on the lower extremities ruptured, leading to wound infection and extensive necrosis that required multiple surgical debridements. When necrosis progressed despite debridement, bilateral above-knee amputation of the legs was performed. Once new lesions stopped appearing, the patient was discharged home. Two months later, she had a recurrence related to cocaine use. To the best of our knowledge, this is only the second reported case of levamisole-induced vasculitis that required above-knee amputation.

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Section: Discussionmentioning

confidence: 99%

Levamisole-induced leukocytoclastic vasculitis and neutropenia in a patient with cocaine use: An extensive case with necrosis of skin, soft tissue, and cartilage

Arora

Jain

Bhanot

et al. 2012

Addict Sci Clin Pract

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“…They suggested that the adverse effects might have been due to some unrecognized adulterant [3]. These speculations were followed five years later by controlled studies demonstrating the equine conversion of levamisole to aminorex [4]. Our laboratory demonstrated that the same conversion of levamisole to aminorex occurs in humans [5].…”

Section: Introductionmentioning

confidence: 80%

Aminorex poisoning in cocaine abusers

Karch¹,

Mari

Bartolini

et al. 2012

International Journal of Cardiology

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“…Levamisole (L-[-]-2,3,5,6-Tetrahydro-6-phenylimidazo[2,1b]-thiazole hydrochloride) is a drug that is routinely used in veterinary medicine to treat parasitic worm infections [29]. Additionally, levamisole acts as an allosteric modulator of human neuronal α3β2 and α3β4 nAChRs [27].…”

Section: Discussionmentioning

confidence: 99%

Levamisole: A Positive Allosteric Modulator for the α3β4 Nicotinic Acetylcholine Receptors Prevents Weight Gain in the CD-1 Mice on a High Fat Diet

Lewis

Yakel

Pandya

2017

CPD

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Neuronal nicotinic acetylcholine receptors (nAChRs) regulate the function of multiple neurotransmitter pathways throughout the central nervous system. This includes nAChRs found on the proopiomelanocortin neurons in the hypothalamus. Activation of these nAChRs by nicotine causes a decrease in the consumption of food in rodents. This study tested the effect of subtype selective allosteric modulators for nAChRs on the body weight of CD-1 mice. Levamisole, an allosteric modulator for the α3β4 subtype of nAChRs, prevented weight gain in mice that were fed a high fat diet. PNU-120596 and desformylflustrabromine were observed to be selective PAMs for the α7 and α4β2 nAChR, respectively. Both of these compounds failed to prevent weight gain in the CD-1 mice. These results suggest that the modulation of hypothalamic α3β4 nAChRs is an important factor in regulating food intake, and the PAMs for these receptors need further investigation as potential therapeutic agents for controlling weight gain.

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Aminorex and rexamino as metabolites of levamisole in the horse

Cited by 40 publications

References 7 publications

Levamisole-induced leukocytoclastic vasculitis and neutropenia in a patient with cocaine use: An extensive case with necrosis of skin, soft tissue, and cartilage

Levamisole-induced leukocytoclastic vasculitis and neutropenia in a patient with cocaine use: An extensive case with necrosis of skin, soft tissue, and cartilage

Aminorex poisoning in cocaine abusers

Levamisole: A Positive Allosteric Modulator for the α3β4 Nicotinic Acetylcholine Receptors Prevents Weight Gain in the CD-1 Mice on a High Fat Diet

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