Section 30
Chapter 29,854

Accumulation and release of Cl4-prilocaine by isolated guinea pig atria

Lahrtz, H.G.; Lullmann, H.; Van Zwieten, P.A.

Eur J Pharmacol 1(3): 177-187


Accession: 029853683

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The uptake of C14-prilocaine by isolated, electrically stimulated guinea pig atria was studied. The prilocaine concentrations used did not impair the contractile force of the atria. A rapid uptake of the local anesthetic was observed in all experiments. Depending on the prilocaine concentration in the medium the uptake reached equilibrium in 10-60 min. The uptake capacity of the atria decreased when the concentration of the drug in the medium was raised. For a given concentration the uptake increased when the medium was made alkaline, whereas at an acid pH the uptake was reduced. At a lower frequency of beating prilocaine was taken up more slowly. The release of prilocaine bound to atria took place very rapidly. The release proved independent of the concentration used. Acidification of the medium (pH 6.0-6.2) did not affect the release of prilocaine. The results are discussed and compared with other uptake processes of drugs by isolated organs, described in the literature.

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