Cocaínaaspectos farmacológicos

  1. I. Lizasoain 1
  2. M.A. Moro 1
  3. P. Lorenzo 1
  1. 1 Departamento de Farmacología. Facultad de Medicina. Universidad Complutense de Madrid
Journal:
Adicciones: Revista de socidrogalcohol

ISSN: 0214-4840

Year of publication: 2002

Volume: 14

Issue: 1

Pages: 57-64

Type: Article

DOI: 10.20882/ADICCIONES.513 DIALNET GOOGLE SCHOLAR lock_openOpen access editor

More publications in: Adicciones: Revista de socidrogalcohol

Abstract

The routes of administration of cocaine are different depending on the cocaine source (leaves, sulphate, hydrochloride and crack), and this affects not only its pharmacokinetics but also its pharmacological effects, as well as other aspects such as toxicity, tolerance, dependence and withdrawal effects of this drug. In our country, cocaine is mainly smoked or inhaled, and intravenous administration can be also used. Cocaine is rapidly absorbed by many routes. Cocaine produces central effects in 30 seconds after nasal or intravenous administration and in only 5 seconds when cocaine is smoked. The major route for cocaine metabolism involves hydrolysis of its ester groups producing benzoylecgonine, ecgonine methyl ester and ecgonine as metabolites. An important metabolic interaction occurs when cocaine and alcohol are taken concurrently; cocaine is then transesterified to cocaethylene, which is toxic. Cocaine is a potent inhibitor of catecholamine uptake by noradrenergic, dopaminergic and serotoninergic nerve terminals and strongly enhances the effects of these neurotransmitters Pharmacological and toxic effects are derived from its actions on the catecholaminergic system.

Bibliographic References

  • Cami J, Farre M, Gonzalez ML, Segura J, de la Torre R. Cocaine metabolism in human after use of alcohol. Clinical and research implications. Recent Dev Alcohol. 1998. 14: 437-55.
  • Dean RA, Bosron WF, Zachman FM, Zhang J, Brzezinski MR. Effects of ethanol on cocaine metabolism and disposition in the rat. NIDA Res Monogr. 1997. 173: 35-47.
  • Dean RA, Christian CD, Sample RHB, Bosron WF. Human liver cocaine esterases: ethanol-mediated formation of ethylcocaine. FASEB. J. 1991. 5: 2735-9.
  • Diagnostic and statistical manual of mental disorders. 4th ed.: DSM-IV. Washington, D.C.: American Psychiatric association, 1994.
  • Gawin FH, Ellinwood EHJr. Cocaine and other stimulants: actions, abuse and treatment. N. Engl. J. Med. 1988. 318: 1173-82.
  • Gawin FH, Kleber HD. Abstinence symptomatology and psychiatric diagnosis of cocaine abusers. Arch. Gen. Psychiatry. 1986. 443: 107-13.
  • Hatsukami DK, Fischman MW. Crack cocaine and cocaine hydrochloride. Are the differences myth or reality?. JAMA. 1996. 276: 1580-8.
  • Jones RT. Pharmacokinetics of cocaine: considerations when assessing cocaine use by urinalysis. NIDA Res Monogr. 1998. 175: 221-34.
  • Keller RW Jr, Snyder-Keller A. Prenatal cocaine exposure. Ann N Y Acad Sci. 2000. 909: 217-32.
  • Leshner AI. Molecular mechanisms of cocaine addiction. N. Engl. J. Med. 1996. 335: 128-9.
  • Lorenzo P, Ladero JM, Leza JC, Lizasoain I. Drogodependencias. Farmacología. Patología. Psicología. Legislación. Panamericana SA. MADRID. 1998.
  • Lorenzo P, Leza JC, Lizasoain I. Drogodependencias. En: Velázquez. Farmacología. (Eds. Velasco, Lorenzo, Serrano, Andrés-Trelles). Ed. Mc Graw-Hill-Interamericana. Madrid. pp. 498-519. 1993.
  • Mendelson JH, Mello NK. Management of cocaine abuse and dependence. N. Engl. J. Med. 1996. 334: 965-72.
  • National Institute on Drug Abuse. http://www.nida.nih.gov
  • National Institute on Drug Abuse. NIDA Infofax, Crack and cocaine, 1998.
  • National Institute on Drug Abuse. Research report series. Cocaine. Abuse and addiction. 1999.
  • Plan Nacional sobre Drogas. Ministerio del Interior. http://www.mir.es/pnd/index.htm
  • Plan Nacional sobre Drogas. Memoria 1998. Ministerio del Interior. Delegación del Gobierno para el Plan Nacional sobre Drogas. 1999.
  • Wolf JH, Huang L, Ishifuro Y, Morgan JP. Negative inotropic effect of methylecgonidine, a major product of cocaine base pyrolysis, on ferret and human myocardium. J Cardiovasc Pharmacol. 1997. 30: 352-9.