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Cocaethylene Formation Following Ethanol and Cocaine Administration by Different Routes

Cocaethylene Formation Following Ethanol and Cocaine Administration by Different Routes

  1. NeuroChi
    Ethanol alters the hepatic biotransformation of cocaine, resulting in transesterification to a novel
    active metabolite, cocaethylene. Because of first pass metabolism, oral drug administration might
    be expected to produce relatively larger concentrations of cocaethylene than would intravenous or
    smoked administration. We, therefore, compared the effects of route of cocaine administration on
    the formation and elimination of cocaethylene. Six experienced cocaine users were tested in 6
    sessions, approximately 1 week apart. Deuterium-labeled cocaine (d5) was administered in all
    conditions. Oral cocaine-d5 2.0 mg/kg, intravenous cocaine-d5 1.0 mg/kg, and smoked cocaine-d5
    (200 mg) were administered after oral ethanol 1.0g/kg or placebo. A small, intravenous dose of
    deuterated cocaethylene (d3) also was administered with all conditions for determination of
    cocaethylene formation. Physiologic and subjective effects were recorded and plasma cocaine-d5,
    cocaethylene-d5, cocaethylene-d3, and benzoylecgonine-d5 were measured by gas chromatography-
    mass spectrometry. About 24% ( 11) of intravenous cocaine was converted to cocaethylene.
    The oral route (34%  20) was significantly greater than from the smoked route (18%  11)
    and showed a trend toward significance for greater formation of cocaethylene compared to the
    intravenous route. Within each route, the cocaine-ethanol combination produced greater increases
    in heart rate and rate-pressure product than cocaine alone. Global intoxication effects across time
    after smoking or intravenous administration were significantly greater when cocaine and ethanol
    were both given. Administration of cocaine by different routes alters the amount of cocaethylene
    formed through hepatic first-pass effects. Increased cardiovascular and subjective effects might
    explain the toxicity and popularity of the combined drugs.

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