Comparison of heroin and cocaine concentrations in saliva with concentrations in blood and plasma.

Saliva is an alternate biological matrix for drug testing that has several advantages over more traditional fluids such as blood and urine. Collection is rapid, noninvasive, and relatively easy to obtain. Several reports have detailed the appearance of drugs of abuse in saliva, but few have compared the excretion profiles of drugs administered by different routes. In this study, subjects were administered three smoked and three intravenous doses of heroin in an ascending dose design. Blood and saliva were collected periodically after drug administration and analyzed by gas chromatography-mass spectrometry (GC-MS) for heroin, 6-acetylmorphine, and morphine. In a second study, subjects were administered a single, smoked dose of 40 mg cocaine base and an intravenous dose of 44.8 mg cocaine HO on separate occasions. Plasma and saliva were collected and analyzed by CC-MS for cocaine, anhydroecgonine methyl ester (AEME), and seven additional metabolites. Heroin and 6-acetylmorphine were detected in the first saliva sample collected (2 min) following drug administration by both routes. Peak heroin concentrations were achieved quickly, between 2 and 5 min after intravenous administration and at 2 min after smoke heroin. Peak heroin concentrations in saliva after smoking heroin base ranged from 3534 (2.6 mg) to 20,580 ng/mL (5.2 mg), and after intravenous administration, concentrations ranged from 6 (10 mg heroin HCl to 30 ng/mL (12 mg heroin HCl. Saliva concentrations of heroin declined rapidly after intravenous administration, reaching the limit of sensitivity of the assay (1 ng/mL) by 60 min. Heroin concentrations in saliva after smoking declined slowly; detection times ranged from 4 to 24 h. Cocaine was the major analyte detected in saliva and plasma after smoked and intravenous administration. Peak saliva cocaine concentrations after intravenous administration ranged from 428 to 1927 ng/mL (N = 7); after smoking, they ranged from 15,852 to 504,880 ng/mL (N = 7). Peak plasma cocaine concentrations after intravenous administration ranged from 122 to 442 ng/mL A = 7), and after smoking, concentrations ranged from 46 to 291 ng/mL A = 7). The thermal degradation product of cocaine, AEME, was detected in saliva but not in plasma after smoking. Peak saliva AEME concentrations were achieved at 2 min and ranged from 558 to 4374 ng/mL (N = 7). These are the first reported observations of heroin and metabolites in saliva following heroin smoking and of AEME in saliva after smoking cocaine base. The presence of AEME in saliva may be useful as a marker of the smoked route following cocaine administration.

[1]  G. Rosen,et al.  Cocaine-mediated hepatotoxicity. A critical review. , 1984, Biochemical pharmacology.

[2]  D. Gorelick,et al.  Cocaine and metabolite excretion in saliva under stimulated and nonstimulated conditions. , 1993, Journal of analytical toxicology.

[3]  Steven B Karch,et al.  The pathology of drug abuse , 1993 .

[4]  E. Cone,et al.  Simultaneous measurement of cocaine, cocaethylene, their metabolites, and "crack" pyrolysis products by gas chromatography-mass spectrometry. , 1994, Clinical chemistry.

[5]  C. Gorodetzky,et al.  Validity of screening methods for drugs of abuse in biological fluids; II. Heroin in plasma and saliva , 1974, Clinical pharmacology and therapeutics.

[6]  P. Craig,et al.  Cocaine and benzoylecgonine in saliva, serum, and urine. , 1993, Clinical chemistry.

[7]  W. Kalow,et al.  Metabolism of cocaine in man , 1978, Clinical pharmacology and therapeutics.

[8]  Randall C. Baselt,et al.  Disposition of toxic drugs and chemicals in man , 1982 .

[9]  I. Kopin,et al.  Norcocaine: a pharmacologically active metabolite of cocaine found in brain. , 1974, Life sciences.

[10]  J. Henningfield,et al.  Pharmacokinetics and pharmacodynamics of smoked heroin. , 1994, Journal of analytical toxicology.

[11]  B. Perrigo,et al.  Detection of drugs in saliva of impaired drivers. , 1984, Journal of forensic sciences.

[12]  D. Hatsukami,et al.  A method for delivery of precise doses of smoked cocaine-base to humans , 1990, Pharmacology Biochemistry and Behavior.

[13]  E. Cone,et al.  Correlation of saliva cocaine levels with plasma levels and with pharmacologic effects after intravenous cocaine administration in human subjects. , 1988, Journal of analytical toxicology.

[14]  E. Cone,et al.  Measurement of heroin and its metabolites by isotope-dilution electron-impact mass spectrometry. , 1993, Clinical chemistry.

[15]  E. Cone Saliva Testing for Drugs of Abuse , 1993, Annals of the New York Academy of Sciences.

[16]  M. Novak,et al.  A model experiment in the study of cocaine base smoking. Isolation of methyl 4-(3-pyridyl) butyrate from cocaine pyrolysate. , 1984, Bulletin on narcotics.

[17]  E. Cone,et al.  Testing human hair for drugs of abuse. I. Individual dose and time profiles of morphine and codeine in plasma, saliva, urine, and beard compared to drug-induced effects on pupils and behavior. , 1990, Journal of analytical toxicology.

[18]  B. Schmidt-nielsen,et al.  The pH in Parotid and Mandibular Saliva , 1946 .

[19]  E. Cone,et al.  Confirmation of cocaine in human saliva after intravenous use. , 1987, Journal of analytical toxicology.