Some aspects of the pharmacodynamics of flukicidal and related drugs

Mohammed Ali, Nidhal Abdul Kader (1985) Some aspects of the pharmacodynamics of flukicidal and related drugs. PhD thesis, University of Glasgow.

Abstract

The pharmacokinetics of four trimethoprim/sulphonamide formulations (Trivetrin, Tribrissen, Duphatrim and Leotrox) available for treatment of bacterial infections in sheep were compared in five sheep after intramuscular administration at a total dose rate of 15 mg.kg-1 of active ingredients (12.5 mg. kg -1 sulphonamide plus 2.5 mg. kg-1 trimethoprim). The maximum concentrations of trimethoprim in plasma occurred at one hour after intramuscular administration of Trivetrin and Leotrox. After administration of Tribrissen and Duphatrim intramuscularly, trimethoprim was not detected in plasma (< 0.1 mug.ml-1). The mean plasma elimination half-life of trimethoprim was 1.3 and 1 hour after administration of Trivetrin and Leotrox respectively. The maximum concentrations of sulphadoxine, sulphadiazine, sulphadiazine and sulphatroxazole occurred at 2, 1, 1 and 1 hours after administration of Trivetrin, Tribrissen, Duphatrim and Leotrox respectively. The mean elimination half-lives of sulphadoxine, sulphadiazine, sulphadiazine and sulpha troxazole were 4.8, 2.9, 2.6 and 9.30 hours after intramuscular administration of Trivetrin, Tribrissen, Duphatrim and Leotrox respectively. No significant differences were found between the plasma concentrations of trimethoprim and sulphadoxine administered at 1 and 3 intramuscular sites. Bioavailability of sulphadoxine and sulphatroxazole were 81 and 88% respectively. The study revealed that administration of trimethoprim/sulphonamide combinations in solution type products (Trivetrin and Leotrox) produced better pharmacokinetic profile than those of suspension type products (Tribrissen and Duphatrim). The degree of plasma-protein binding of sulphadoxine, sulphadiazine and sulphatroxazole was found to be 50, 14 and 70% respectively which appeared to be well correlated to their rates of elimination from plasma. A detailed study was made of the pharmacokinetics of the commonly used flukicidal drugs, a new sulphonamide product, clorsulon, the salicylanilides rafoxanide, closantel and oxyclozanide, and a unique benzimidazole triclabendazole which has flukicidal activity with no nematodicidal activity. All the flukicidal drugs studied showed markedly long plasma elimination half-lives and a high degree of binding to plasma-proteins.

• Item Type: Thesis (PhD)
• Qualification Level: Doctoral
• Keywords: Pharmacology
• Date of Award: 1985
• Depositing User: Enlighten Team
• Unique ID: glathesis:1985-76550
• Copyright: Copyright of this thesis is held by the author.
• Date Deposited: 19 Nov 2019 14:10
• Last Modified: 19 Nov 2019 14:10
• URI: https://theses.gla.ac.uk/id/eprint/76550