Drug Metabolism (Biotransformation)

  • Ronald J. Tallarida
  • Robert B. Raffa
  • Paul McGonigle
Part of the Springer Series in Pharmacologic Science book series (SSPHARMACOL)


When a drug molecule is introduced into a living organism or tissue, it is immersed in a highly reactive biological mixture in which thousands of chemical reactions are simultaneously proceeding in complex, but organized, patterns. These reactions operate in a coordinated manner within cells to conserve certain endogenous compounds and nutrients and to eliminate potentially harmful foreign material. A drug molecule will very likely be affected by one or more of the many chemical reactions occurring in a cell.


Cocaine NADH Diazepam Ketamine Halogen 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Adriani J: The Pharmacology of Anesthetic Drugs. Springfield, Ill, Charles C. Thomas, 1970, p 1–16.Google Scholar
  2. 2.
    Baden JM, Rice SA: Metabolism and toxicity of inhaled anesthetics, in Miller RD (ed): Anesthesia, New York, Churchill Livingstone, 1981, p 383–424.Google Scholar
  3. 3.
    Bentley JB: Deuterated volatile anesthetics, in Brown BR Jr (ed): New Pharmacologic Vistas in Anesthesia, Philadelphia, FA Davis Co, 1983, p 19–26.Google Scholar
  4. 4.
    Brenner RR: Metabolism of endogenous substrates by microsomes. Drug Metab Rev 1977;6:155–212.PubMedCrossRefGoogle Scholar
  5. 5.
    Brown BR: Hepatic microsomal enzyme induction. Anesthesiology 1973; 39:178–187.PubMedCrossRefGoogle Scholar
  6. 6.
    Caldwell J: Conjugation reactions in foreign compound metabolism: definition, consequences, and species variations. Drug Metab Rev 1982; 13:745–777.PubMedCrossRefGoogle Scholar
  7. 7.
    Cascorbi HF: Biotransformation of drugs used in anesthesia. Anesthesiology 1973; 39:115–125.PubMedCrossRefGoogle Scholar
  8. 8.
    Ciaccio EI: Intimate study of drug action II: fate of drugs in the body, in Di Palma JR (ed): Drill’s Pharmacology in Medicine, New York, McGraw-Hill, 1971, pp 36–66.Google Scholar
  9. 9.
    Conti A, Bickel MH: History of drug metabolism: discoveries of the major pathways in the 19th century. Drug Metab Rev 1977; 6:1–50.CrossRefGoogle Scholar
  10. 10.
    Coon MJ: Drug metabolism by cytochrome P-450: progress and perspectives. Metab Disposit 1981; 9:1–4.Google Scholar
  11. 11.
    Csaky TZ: Introduction to General Pharmacology. New York, Appleton-Century-Crofts, 1969, pp 55–80.Google Scholar
  12. 12.
    Feinman L, Rubin E, Lieber CS: Adaptation of the liver to drugs, in Orlandi F, Jezequel AM (eds): Liver and Drugs. New York, Academic Press, 1972, pp 41–83.Google Scholar
  13. 13.
    Gibaldi M, Perrier D: Route of administration and drug disposition. Drug Metab Rev 1974;3:185–199.PubMedCrossRefGoogle Scholar
  14. 14.
    Goth A: Medical Pharmacology. St Louis, CV Mosby Co, 1984, pp 29–39.Google Scholar
  15. 15.
    Guenthner TM: Monoclonal antibodies to cytochrome P-450 isozymes. Trends in Pharmacological Sciences 1983; 4:5.CrossRefGoogle Scholar
  16. 16.
    Hansch C: Quantitative relationships between lipophilic character and drug metabolism. Drug Metab Rev 1972; 1:1–14.CrossRefGoogle Scholar
  17. 17.
    Hucker HB: Intermediates in drug metabolism reactions. Drug Metab Rev 1973; 2:33–56.PubMedCrossRefGoogle Scholar
  18. 18.
    Jenner P, Testa B: The influence of stereochemical factors on drug disposition. Drug Metab Rev 1973; 2:117–184.PubMedCrossRefGoogle Scholar
  19. 19.
    Kato R: Sex-related differences in drug metabolism. Drug Metab Rev 1914; 3:1–32.CrossRefGoogle Scholar
  20. 20.
    LaDu BN: Genetic factors modifying drug metabolism and drug response, in LaDu BN, Mandel HG, Way EL (eds): Fundamentals of Drug Metabolism and Drug Disposition. Baltimore, Williams & Wilkins Co, 1971, pp 308–327.Google Scholar
  21. 21.
    Lawrence DR, Bennett PN: Clinical Pharmacology, ed 5, New York, Churchill Livingstone, 1980, pp 124–128.Google Scholar
  22. 22.
    Mandel HG: Pathways of drug biotransformation: biochemical conjugations, in LaDu BN, Mandel HG, Way EL (eds): Fundamentals of Drug Metabolism and Drug Disposition. Baltimore, Williams & Wilkins Co, 1971, pp 149–205.Google Scholar
  23. 23.
    Mannering GJ: Microsomal enzyme systems which catalyze drug metabolism, in LaDu BN, Mandel HG, Way EL (eds): Fundamentals of Drug Metabolism and Drug Disposition. Baltimore, Williams & Wilkins Co, 1971, pp 206–252.Google Scholar
  24. 24.
    Mayer SE, Melmon KL, Gilman AG: Introduction; the dynamics of drug absorption, distribution, and elimination, in Gilman AG, Goodman LS, Gilman A (eds): The Pharmacological Basis of Therapeutics, ed 6, New York, Macmillan Publishing, 1980, pp 12–20.Google Scholar
  25. 25.
    Preisig R, Bircher J (eds): The Liver: Quantitative Aspects of Structure and Function. Proc 3rd Intl Gstaad Symposium, September, 1978. Editio Cantor Aulendorf, pp 269–350.Google Scholar
  26. 26.
    Prescott LF, Critchley JAJH: The treatment of acetaminophen poisoning. Ann Rev Pharmacol Toxicol 1983; 23:87–101.CrossRefGoogle Scholar
  27. 27.
    Short CR, Kinden DA, Stith R: Fetal and neonatal development of the microsomal monooxygenase system. Drug Metab Rev 1976; 5:1–42.CrossRefGoogle Scholar
  28. 28.
    Stanski DR, Watkins WD: Drug Disposition in Anesthesia. New York, Grune & Strat-ton, 1982, pp 47–71.Google Scholar
  29. 29.
    Vesell ES: Individual variations in drug response, in Orlandi F, Jezequal AM (eds): Liver and Drugs. New York, Academic Press, 1972, pp 1–40.Google Scholar
  30. 30.
    Way EL, Adler TK: The pharmacologic implications of the fate of morphine and its surrogates. Pharmacol Revs 1960; 12:383–446.Google Scholar
  31. 31.
    White RE, Coon MJ: Oxygen activation by cytochrome P450. Ann Rev Biochem 1980; 49:315–356.PubMedCrossRefGoogle Scholar

Copyright information

© Springer-Verlag New York Inc. 1988

Authors and Affiliations

  • Ronald J. Tallarida
    • 1
  • Robert B. Raffa
    • 1
    • 2
    • 3
  • Paul McGonigle
    • 4
  1. 1.Department of PharmacologyTemple University School of MedicinePhiladelphiaUSA
  2. 2.Janssen Research FoundationUSA
  3. 3.Jefferson Medical CollegePhiladelphiaUSA
  4. 4.Department of PharmacologyUniversity of Pennsylvania School of MedicinePhiladelphiaUSA

Personalised recommendations