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Convolvulus pluricaulis (Shankhpushpi) and Erythroxylum coca (Coca plant)
Published in Azamal Husen, Herbs, Shrubs, and Trees of Potential Medicinal Benefits, 2022
Sashi Sonkar, Akhilesh Kumar Singh, Azamal Husen
The E. coca leaf contains 0.7–1.5% of total alkaloids, with (-)-cocaine (pharmacologically active ingredient), a diester of (-)-ecgonine. Ecgonine has four chiral centers and is hence optically active. Other minor components of coca leaves include tropacocaine, methylecgonine, β-truxilline, α-truxilline, and cinnamonylcocaine (Christen, 2000). Cocaine was the most abundant alkaloid, accounting for 0.56% of the total dry weight, and other alkaloids include anhydroecgonine methyl ester (0.2% dry weight), ecgonine methyl ester (0.18% dry weight), trans-cinnamoylcocaine (0.4% dry weight), and cis-cinnamoylcocaine (0.7% dry weight) (Penny et al., 2009). Additional alkaloids also found in coca leaf in coca tea bags include hygrine, nicotine, dihydrocuscohygrine, cuscohygrine, ecgonine, hydroxytropacocaine, benzoylecgonine, and methylecgonine cinnamate (Jenkins et al., 1996). The leaves also had magnesium, zinc, iron, calcium, vitamin D, vitamin E, β-carotene, and protein, with lysine being the limiting amino acid (Penny et al., 2009). So far, 18 alkaloids from pyridines, pyrrolidines, and tropanes have been identified in a cultivated variety of E. coca (Novak et al., 1984). Several alkaloids were discovered and identified in the seeds of E. coca, including trans-cinnamoylcocaine, cis-cinnamoylcocaine, cocaine, hexanoylecgonine methyl ester, benzoyltropine, N-norbenzoyltropine, cuscohygrine, ecgonine methyl ester, 3α-acetoxytropane, tropine, and methylecgonidine (Casale et al., 2005).
Inhalational Durg Abuse
Published in Jacob Loke, Pathophysiology and Treatment of Inhalation Injuries, 2020
Jacob Loke, Richard Rowley, Herbert D. Kleber, Peter Jatlow
Chemically, cocaine is methylbenzoylecgonine and is an alkaloid extracted from the South American plant Erythroxylon coca. After purification to its hydrochloride salt, cocaine is a white crystalline powder and is water soluble. Pure cocaine (base or freebase) is almost insoluble in water. It is metabolized by esterases in liver (Jones, 1984), cholinesterases in plasma, and by nonenzymatic hydrolysis. The major urinary cocaine metabolites are benzoylecgonine (Fish and Wilson, 1969) and ecgonine methyl ester (Inaba et al., 1978). In samples from patients with a pseudocholinesterase deficiency, there was a marked decrease in the in vitro rate of cocaine degradation, indicating the probable role of plasma cholinesterase in cocaine metabolism (Inaba et al., 1978; Jatlow et al., 1979). The plasma half-life of cocaine is about 1.5 hr. About 80% of the drug is excreted in the urine as ecgonine methyl ester and benzoylecgonine, both of which can be detected in the urine by drug abuse screening.
Behavioral and Convulsive Effects of Cocaine Metabolites: Mechanisms and Implications
Published in Richard J. Konkol, George D. Olsen, Prenatal Cocaine Exposure, 2020
Richard J. Konkol, Guy Schuelke
The possibility that the relatively long-lived cocaine metabolites may interact was investigated. Potential interactions between compounds producing positive effects (BE, NBE, cocaine) and those producing negative or suppressive effects (EME, EC) were tested. These studies demonstrated that EME inhibited and/or blocked the behavioral activation induced by cocaine and BE. Ecgonine possessed similar properties. In order to be effective, compounds needed to be given in molar excess within several minutes of administration of the test compound. Table 6.3 shows that preinjected EME and/or EC inhibited seizures and/or death produced by subsequently injected cocaine, BE, and pseudococaine. Moreover, we have made an additional observation that EME can inhibit cocaine analgesia when preinjected in molar excess shortly before the cocaine.33
DropWise: current role and future perspectives of dried blood spots (DBS), blood microsampling, and their analysis in sports drug testing
Published in Critical Reviews in Clinical Laboratory Sciences, 2023
M. Thevis, Katja Walpurgis, A. Thomas
Moreover, Thevis et al. comprehensively discussed the potential added value of DBS for the detection of substances whose misuse is prohibited only in competition such as stimulants, narcotics, cannabinoids, and glucocorticoids [105]. According to currently applicable regulations [106], the relevant period ranges from 11:59 pm on the day before a competition until its end or the collection of the doping control sample(s). Urine specimens obtained during this time do not necessarily reflect whether an athlete competed under the systemic influence of a drug. The collection and analysis of paired urine and DBS samples would therefore provide a more comprehensive picture of the circulating levels of prohibited drugs during competition. Based on this information, result management authorities can more accurately estimate the pharmacological relevance of the detected drug amount and decide on the athlete’s sanction accordingly. Thevis and coworkers describe two exemplary scenarios where the urinary WADA reporting levels of the respective analyte (benzoyl ecgonine/cocaine and prednisolone/prednisone) were exceeded but the paired DBS sample revealed blood concentrations that were presumed to be pharmacologically ineffective. Therefore, the definition of drug-specific parameters that trigger follow-up investigations and minimum effective blood concentrations could be of added value for routine doping controls.
Whether drug detection in urine and oral fluid is similar? A systematic review
Published in Critical Reviews in Toxicology, 2020
Milena Binhame Albini Martini, Thiago Beltrami Dias Batista, Indiara Welter Henn, Patrícia Tolentino da Rosa de Souza, Alexandre Rezende Vieira, Luciana Reis Azevedo-Alanis
Two studies evaluated cocaine and its metabolites (Jufer et al. 2006; Strano-Rossi et al. 2008). Different ways of administration such as ingested, smoked, injected, and inhaled were described. Strano-Rossi et al. (2008) evaluated only cocaine ingested (3 mg of cocaine) and its metabolites, benzoylecgonine (BZE), ecgonine methyl ester (EME) and coca. The first positive finding for metabolites was in 2 h in urine and in 1 h in oral fluid, with peak concentration for analytes after a longer time in urine (EME 34 h) than in oral fluid (BZE 9.3 h). This study did not declare cutoff values, so we used cutoff reference values from other study (Jufer et al. 2006) because both evaluated and quantified the same metabolites. The latter study evaluated cocaine and its metabolites (coca and BZE) after a single dose injected (25 mg), inhaled (32 mg) and smoked (42 mg) (Jufer et al. 2006). They reported positive results in first collection immediately after drug administration; a longer time of drug detection was observed in urine than in oral fluid, and higher concentrations of analytes were detected with inhaled drug compared to smoked drug in both urine and oral fluid. This study also evaluated chronic use of ingested cocaine (375–2000 mg) and obtained higher values of concentrations and time of positive detection than other ways of administration with lower doses besides obtaining positive value also in first collection (Table 3) (Jufer et al. 2006).
Accuracy of substance exposure history in patients attending emergency departments after substance misuse; a comparison with biological sample analysis
Published in Clinical Toxicology, 2023
Ishita Virmani, Alberto Oteo, Michael Dunn, Daniel Vidler, Clair Roper, Jane Officer, Gareth Hardy, Paul I. Dargan, Michael Eddleston, Jamie G. Cooper, Simon L. Hill, Rebecca Macfarlane, Liza Keating, Mark Haden, Simon Hudson, Simon H. L. Thomas
In our primary analysis, the presence of metabolites was considered evidence of exposure to the parent drug. These included all SCRA metabolites, major cocaine metabolites (benzoylecgonine, norcocaine and ecgonine methyl ester) and the 3,4-methylenedioxymethamphetamine (MDMA) metabolite 3,4-Methylenedioxyamphetamine (MDA). The presence of monoacetyl morphine, morphine, or morphine conjugates (henceforward referred to as selected heroin/morphine metabolites) was considered evidence of heroin (diacetylmorphine) exposure. A separate analysis was performed considering only the parent drug for cocaine, because of the possibility that metabolites, some of which have long half-lives, might persist from an earlier episode of drug use.