Aminorex poisoning in cocaine abusers

Karch, Steven B.; Mari, Francesco; Bartolini, Viola; Bertol, Elisabetta

doi:10.1016/j.ijcard.2011.06.105

Cited by 44 publications

(31 citation statements)

References 28 publications

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“…It was also used as an immunomodulator for minimalchange glomerulopathy and rheumatoid arthritis and was even approved by the Food and Drug Administration in 1991 as adjuvant therapy for colorectal cancer. In 1999, however, it was withdrawn from the market in the United States because of adverse effects, most notably agranulocytosis (86,87). Of note, it is still under investigation as a possible therapy for aplastic anemia (88).…”

Section: Recent Emergence Of Levamisole-adulterated Cocainementioning

confidence: 99%

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Nephrotoxic Effects of Common and Emerging Drugs of Abuse

Pendergraft

Herlitz

Thornley‐Brown

et al. 2014

Clinical Journal of the American Society of Nephrology

112

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The kidneys can be injured in diverse ways by many drugs, both legal and illegal. Novel associations and descriptions of nephrotoxic effects of common and emerging drugs of abuse have appeared over the past several years. Anabolic androgenic steroids, illicitly used by athletes and others for decades to increase muscle mass and decrease body fat, are emerging as podocyte toxins given recent descriptions of severe forms of FSGS in long-term abusers. Synthetic cannabinoids, a new group of compounds with marijuana-like effects, recently became popular as recreational drugs and have been associated with an atypical form of AKI. 3,4-Methylenedioxymethamphetamine, commonly known as ecstasy, is a widely used synthetic recreational drug with mood-enhancing properties and a constellation of toxicities that can result in death. These toxic effects include hyperthermia, hypotonic hyponatremia due to its arginine vasopressin secretagogue-like effects, rhabdomyolysis, and cardiovascular collapse. Cocaine, a serotonin-norepinephrine-dopamine reuptake inhibitor that serves as an illegal stimulant, appetite suppressant, and anesthetic, also causes vasoconstriction and rhabdomyolysis. Recent adulteration of much of the world's supply of cocaine with levamisole, an antihelminthic agent with attributes similar to but distinct from those of cocaine, appears to have spawned a new type of ANCAassociated systemic vasculitis. This review discusses the nephrotoxic effects of these common and emerging drugs of abuse, of which both community and health care providers should become aware given their widespread abuse. Future investigation into pathogenetic mechanisms associated with these drugs is critical and may provide a window into ways to lessen and even prevent the nephrotoxic effects of these drugs of abuse and perhaps allow a deeper understanding of the nephrotoxicities themselves.

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Section: Recent Emergence Of Levamisole-adulterated Cocainementioning

confidence: 99%

“…It is thought that cocaine is cut with levamisole because levamisole is a white, odorless powder that may potentiate euphoria. Furthermore, levamisole is metabolized to aminorex, an anorectic and amphetamine-like stimulant (87).…”

Section: Recent Emergence Of Levamisole-adulterated Cocainementioning

confidence: 99%

Nephrotoxic Effects of Common and Emerging Drugs of Abuse

Pendergraft

Herlitz

Thornley‐Brown

et al. 2014

Clinical Journal of the American Society of Nephrology

112

View full text Add to dashboard Cite

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“…[17] Reports about the detection and characterization of 4-MAR, on the other hand, began to appear following a case report about a fatality in the late 1980s. [18] The presence of two chiral carbons in 4-MAR gives rise to two diastereomeric cis - and trans racemates that have been previously studied.…”

Section: Introductionmentioning

confidence: 99%

Characterization of a novel and potentially lethal designer drug (±)‐cis‐para‐methyl‐4‐methylaminorex (4,4'‐DMAR, or ‘Serotoni’)

Brandt

Baumann

Partilla

et al. 2014

Drug Testing and Analysis

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During the second half of 2013, a total of 26 deaths involving para-methyl-4-methylaminorex (4,4’-DMAR) were reported to the European Monitoring Centre for Drugs and Drug Addiction. While aminorex and 4-methylaminorex (4-MAR) are known psychostimulants, nothing is known about the comparatively new para-methyl analogue. Analytical characterization of two independent samples obtained from online vendors confirmed the presence of the (±)-cis isomer that also appeared to be involved in at least 18 of the 26 deaths. Extensive characterizations included crystal structure analysis, single, tandem and high-resolution mass spectrometry, liquid and gas chromatography and nuclear magnetic resonance spectroscopy. For the work described here, both the (±)-cis and (±)-trans racemates were also synthesized, confirming that the differentiation between these two forms was straight-forward. Monoamine transporter activity was studied using rat brain synaptosomes. (±)-cis-4,4'-DMAR was a potent, efficacious substrate-type releaser at transporters for dopamine, norepinephrine and serotonin with EC50 values of 8.6 ± 1.1 nM (DAT), 26.9 ± 5.9 nM (NET) and 18.5 ± 2.8 nM (SERT), respectively. A comparison with d-amphetamine, aminorex and (±)-cis-4-MAR revealed that activity at SERT varied more than 100-fold across the four drugs, with (±)-cis-4,4’-DMAR exhibiting the highest potency for releasing 5-HT. The potent releasing activity of (±)-cis-4,4’-DMAR at all three monoamine transporters predicts a potential for serious side-effects such as psychotic symptoms, agitation, hyperthermia and cardiovascular stimulation, especially after high-dose exposure or following combination with other psychostimulants.

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“…The application route is usually nasal or oral and a typical dose amounts to 10-60 mg, single cases reported of the intake of up to 200 mg [5].…”

Section: 4´-dmarmentioning

confidence: 99%