Effects of cocaine, cocaine metabolites and cocaine pyrolysis products on the hindbrain cardiac and respiratory centers of the rabbit ag

Erzouki, Hashim K.; Allen, Andrew C.; Newman, Amy Hauck; Goldberg, Sharon; Schindler, Charles W.

doi:10.1016/0024-3205(95)02166-g

Cited by 33 publications

(20 citation statements)

References 15 publications

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“…Two other metabolites, anhydroecgonine methyl ester (AEME) and cocaethylene (CE), can be produced when the drug is consumed in the free base form (as a result of thermal degradation of smoked "crack") [15], and with simultaneous use of alcohol [16], respectively (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%

Development and validation of a gas chromatography/ion trap-mass spectrometry method for simultaneous quantification of cocaine and its metabolites benzoylecgonine and norcocaine: Application to the study of cocaine metabolism in human primary cultured renal cells

Valente¹,

Carvalho²,

Bastos³

et al. 2010

Journal of Chromatography B

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Section: Introductionmentioning

confidence: 99%

Development and validation of a gas chromatography/ion trap-mass spectrometry method for simultaneous quantification of cocaine and its metabolites benzoylecgonine and norcocaine: Application to the study of cocaine metabolism in human primary cultured renal cells

Valente¹,

Carvalho²,

Bastos³

et al. 2010

Journal of Chromatography B

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“…The concurrent use of COC and ethanol results in a biologically active molecule, cocaethylene (CE), and two non-active metabolites of CE, norcocaethylene (NCE) and ecgonine ethyl ester (EEE). COC and ethanol are frequently taken together, due to the effects of CE, which is nearly as psychoactive as COC but produces a much longer lasting high [14][15][16]. CE is even more toxic than COC, and its potency results in an increased risk of death due to overdose [17].…”

Section: Introductionmentioning

confidence: 98%

Determination of cocaine, its metabolites, pyrolysis products, and ethanol adducts in postmortem fluids and tissues using Zymark® automated solid-phase extraction and gas chromatography-mass spectrometry1

Lewis

Johnson

Angier

et al. 2004

Journal of Chromatography B

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“…Erzouki et al (1995) reported that 1.0 mg of cocaine administered intravenously to anesthetized rabbits increased mean blood pressure and peak heart rate; however, 3.0 mg of methylecgonidine also administered intravenously decreased mean blood pressure and peak heart rate (Erzouki et al, 1995). These responses to methylecgonidine mimic muscarinic agonism (Brown and Taylor, 1996).…”

mentioning

confidence: 99%

Pharmacokinetics and Pharmacodynamics of Methylecgonidine, a Crack Cocaine Pyrolyzate

Scheidweiler¹,

Plessinger²,

Shojaie³

et al. 2003

J Pharmacol Exp Ther

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Methylecgonidine is formed from cocaine base when smoked and has been identified in biological fluids of crack smokers. Ecgonidine, a metabolite of methylecgonidine formed via esterase activity, also has been identified in similar samples collected from crack smokers. Methylecgonidine and ecgonidine can be used as biomarkers to differentiate smoking from cocaine use via other routes of administration. We determined the pharmacokinetic properties of methylecgonidine and ecgonidine in sheep after intravenous administration of methylecgonidine at doses of 3.0, 5.6, and 10.0 mg/kg using gas chromatography-mass spectrometric assays. Methylecgonidine clears quickly from blood with a half-life of 18 to 21 min, whereas ecgonidine has a longer half-life of 94 to 137 min. Because ecgonidine clears more slowly, it may be a more effective biomarker of cocaine smoking. The cardiovascular stimulant effects of cocaine contrast with reported in vitro muscarinic agonist effects of methylecgonidine, decreasing contractility and stimulating nitric oxide production in cardiac cells and tissues. To test the hypothesis that methylecgonidine produces cardiovascular effects in vivo consistent with muscarinic agonism, methylecgonidine was administered to sheep intravenously (0.1-3.0 mg/kg) while monitoring heart rate and blood pressure. Significant hypotension and tachycardia occurred in all three sheep. Two of the three sheep demonstrated mild bradycardia 3 to 5 min after methylecgonidine injection. Intravenous pretreatment with atropine methyl bromide (15 g/kg) antagonized methylecgonidine-induced hypotension in all three sheep, supporting the hypothesis that methylecgonidine acts as a muscarinic agonist in vivo.Heating cocaine base (smoking crack) produces the pyrolyzate methylecgonidine (anhydroecgonine methylester). Because methylecgonidine is produced via thermal conversion from cocaine, it can be used as a marker to differentiate between smoking and cocaine use via other routes of administration. In forensic cases, methylecgonidine has been detected in urine (Jacob et al

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Effects of cocaine, cocaine metabolites and cocaine pyrolysis products on the hindbrain cardiac and respiratory centers of the rabbit ag

Cited by 33 publications

References 15 publications

Development and validation of a gas chromatography/ion trap-mass spectrometry method for simultaneous quantification of cocaine and its metabolites benzoylecgonine and norcocaine: Application to the study of cocaine metabolism in human primary cultured renal cells

Development and validation of a gas chromatography/ion trap-mass spectrometry method for simultaneous quantification of cocaine and its metabolites benzoylecgonine and norcocaine: Application to the study of cocaine metabolism in human primary cultured renal cells

Determination of cocaine, its metabolites, pyrolysis products, and ethanol adducts in postmortem fluids and tissues using Zymark® automated solid-phase extraction and gas chromatography-mass spectrometry1

Pharmacokinetics and Pharmacodynamics of Methylecgonidine, a Crack Cocaine Pyrolyzate

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