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Pharmacokinetics of theophylline in relation to increased pain sensitivity in the rat

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Abstract

In the rat, theophylline increases, in proportion to dose, the sensitivity to painful stimulation. A study of the pharmacological registration of this property combined with the determination of drug levels in plasma indicated that theophylline behaves according to a two-compartment open model. By relating the pharmacological activities to the drug level data using different pharmacokinetic types of calculation, it was concluded that the site of action of theophylline in the central nervous system lies closer to the central (plasma) compartment than to the peripheral one. The registered pharmacological effects of theophylline are thus directly reflected by the plasma concentration of this drug.

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References

  1. Physiology and pharmacology of cyclic AMP. In P. Greengard and G. A. Robinson (eds.).Advances in Cyclic Nucleotide Research, Vol. 1, Raven Press, New York, 1972.

    Google Scholar 

  2. G. Paalzow and L. Paalzow. The effects of caffeine and theophylline on nociceptive stimulation in the rat.Acta Pharmacol. Toxicol. 32: 22–32 (1973).

    Article  CAS  Google Scholar 

  3. G. Paalzow and L. Paalzow. Theophylline increased sensitivity to nociceptive stimulation and regional turnover of rat brain 5-HT, noradrenaline and dopamine.Acta Pharmacol. Toxicol. 34: 157–173 (1974).

    Article  CAS  Google Scholar 

  4. G. Paalzow, L. Paalzow, and B. Stalby. Pentazocine analgesia and regional rat brain catecholamines.Europ. J. Pharmacol. 27: 78–88 (1974).

    Article  CAS  Google Scholar 

  5. M. N. Carroll and R. K. S. Lim. Observations on the neuropharmacology of morphine and morphinelike analgesia.Arch. Int. Pharmacodyn. 125: 383–403 (1960).

    CAS  PubMed  Google Scholar 

  6. F. Hoffmeister and G. Kroneberg. Experimental studies in animals on differentiation of analgesic activity. In P. Mantegazza and F. Piccinini (eds.).Methods in Drug Evaluation. North-Holland Publishing Co., Amsterdam, 1966, p. 270.

    Google Scholar 

  7. A. Arbin and P.-O. Edlund. Determination of theophylline in biological material.Acta Pharm. Suec. 11: 249–256 (1974).

    CAS  PubMed  Google Scholar 

  8. A. Arbin and P.-O. Edlund. Determination of theophylline in biological material by means of electron capture gas chromatography.Ada Pharm. Suec. 12 (1975), in press.

  9. S. Riegelman, J. C. K. Loo, and M. Rowland. Shortcomings in pharmacokinetic analysis by conceiving the body to exhibit properties of a single compartment.J. Pharm. Sci. 57: 117–123 (1968).

    Article  CAS  PubMed  Google Scholar 

  10. S. Riegelman, J. Loo, and M. Rowland. Concept of a volume of distribution and possible errors in evaluation of this parameter.J. Pharm. Sci. 57: 128–133 (1968).

    Article  CAS  PubMed  Google Scholar 

  11. J. G. Wagner.Biopharmaceutics and Relevant Pharmacokinetics. Drug Intelligence Publications, Hamilton, Ill., 1971.

    Google Scholar 

  12. J. G. Wagner, E. Novak, L. G. Leslie, and C. M. Metzler. Absorption, distribution, and elimination of spectinomycin dihydrochloride in man.Int. J. Clin. Pharmacol. 1: 261–285 (1968).

    CAS  Google Scholar 

  13. M. Gibaldi, G. Levy, and H. Weintraub. Drug distribution and pharmacological effects.Clin. Pharmacol. Ther. 12: 734–742 (1971).

    CAS  PubMed  Google Scholar 

  14. V. F. Smolen. Quantitative determination of drug bioavailability and biokinetic behavior from pharmacological data for ophthalmic and oral administrations of a mydriatic drug.J. Pharm. Sci. 60: 354–365 (1971).

    Article  CAS  PubMed  Google Scholar 

  15. R. R. Sokal and F. J. Rohlf.Biometry: The Principles and Practice of Statistics in Biological Research, Freeman, San Francisco, 1969.

    Google Scholar 

  16. G. Levy, M. Gibaldi, and W. J. Jusko. Multicompartment pharmacokinetic models and pharmacological effects.J. Pharm. Sci. 58: 422–424 (1969).

    Article  CAS  PubMed  Google Scholar 

  17. G. Levy and M. Gibaldi. Pharmacokinetics of drug action.,Ann. Rev. Pharmacol. 12: 85–98 (1972).

    Article  CAS  PubMed  Google Scholar 

  18. D. D. Perrin.Dissociation Constants of Organic Bases in Aqueous Solution, Butterworths, London, 1965.

    Google Scholar 

  19. Pharmacopea Nordica, V. Pettersson, Stockholm, 1961.

  20. P. A. Mitenko and R. I. Ogilvie. Rapidly achieved plasma plateaus, with observations on theophylline kinetics.Clin. Pharmacol. Ther. 13: 329–335 (1972).

    CAS  PubMed  Google Scholar 

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Authors and Affiliations

  1. Department of Pharmaceutical Pharmacology, University of Uppsala, Box 573, S-751 23, Uppsala

    Lennart K. Paalzow

  2. Centrallaboratoriet, Apoteksbolaget AB, Box 3045, S-171 03, Solna 3, Sweden

    Lennart K. Paalzow

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  1. Lennart K. Paalzow
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Paalzow, L.K. Pharmacokinetics of theophylline in relation to increased pain sensitivity in the rat. Journal of Pharmacokinetics and Biopharmaceutics 3, 25–38 (1975). https://doi.org/10.1007/BF01066593

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  • DOI: https://doi.org/10.1007/BF01066593

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