Disease relevance of Flukanide

• The oral toxicity of the veterinary anthelmintic Rafoxanide was evaluated in newborn rats exposed in utero and during lactation [1].
• Rafoxanide induced, in some pups (35%), the formation of cataracts [1].
• The use of injectable rafoxanide against natural ovine nasal myiasis [2].
• In a farm-scale veterinary preventive programme run from 1973 to 1976 the use of rafoxanide (Flukanide; Merck Sharp & Dohme) in the prophylaxis of ovine fascioliasis resulted in a marked reduction in the percentage of ewes passing fluke eggs in the faeces and an absence of clinical cases of fascioliasis throughout these years [3].
• Amaurosis in sheep resulting from treatment with rafoxanide [4].

High impact information on Flukanide

• Haemonchus contortus: the in vitro effects of DL-tetramisole and rafoxanide on glycolytic enzymes [5].
• The marked decrease in ATP and glycogen, and the increase in total [NAD+]/[NADH] and [oxaloacetate]/[malate], together with the changed content of other metabolites, led to the conclusion that the mode of action of rafoxanide against F. hepatica in vivo is by uncoupling oxidative phosphorylation [6].
• The in vivo effects of rafoxanide on the energy metabolism of Fasciola hepatica [7].
• A controlled trial was conducted to evaluate the current efficacy of albendazole (ABZ), rafoxanide (RFX), triclabendazole (TRC) or clorsulon (CLS) against Fasciola hepatica in naturally infected cattle [8].
• The results of this study indicated simultaneous resistance of Haemonchus contortus against benzimidazoles, levamisole and rafoxanide and Trichostrongylus columbriformis and Oesophagostomum sp. against levamisole on the same farm [9].

Chemical compound and disease context of Flukanide

• Several cases of toxicity and mortality have been reported for closantel and rafoxanide in sheep and goats [10].

Biological context of Flukanide

• This method was applied to the characterization of rafoxanide plasma kinetics following oral administration of therapeutic doses to sheep [11].
• The effects of DL-tetramisole and rafoxanide on tricarboxylic acid cycle enzymes of Haemonchus contortus, in vitro [12].
• Relative bioavailability of rafoxanide following intraruminal and intra-abomasal administration in sheep [13].
• The pharmacokinetics of rafoxanide administered orally at 15 mg kg-1 were compared in suckling lambs (n = 8), aged 5-8 weeks and weaned lambs (n = 8), aged 21-22 weeks [14].
• The area under the rafoxanide plasma concentration versus time curve (AUC), AUC extrapolated to infinity, and maximum plasma rafoxanide concentrations (Cmax), were used to compare the extent of absorption of the formulations [15].

Anatomical context of Flukanide

• Part of this putative efficacy against immature flukes may be due to rafoxanide persisting in the plasma and affecting the mature flukes when they reach the bile ducts [16].

Associations of Flukanide with other chemical compounds

• Rafoxanide and nitroxynil were used at a dose rate of 10 mg/kg, rafoxanide being given orally and nitroxynil by subcutaneous injection [17].
• 1. The effect of the salicylanilide compound rafoxanide against immature stages of Fasciola hepatica was investigated in sheep using a series of antipyrine clearance tests and measuring glutamate dehydrogenase and gamma-glutamyl transferase activities in plasma [18].
• Resistance in South Africa to rafoxanide and other anthelmintics, namely, closantel, ivermectin and the benzimidazoles is reviewed [19].
• The comparative efficacy of diamphenethide and rafoxanide against fasciola gigantica in sheep [20].
• Rapid death of Fasicola gigantica and P. explanatum resulted in vitro when 10(-3) M oxyclozanide, hexachlorophene, nitroxynil or rafoxanide, were added to the incubation medium [21].

Gene context of Flukanide

• 5. Glutamate dehydrogenase activity fell dramatically 2 weeks after treatment but increased again at 12 weeks post-infection in the infected rafoxanide-treated group [18].
• Rafoxanide had no mutagenic activity in the Ames and CHO/HGPRT tests [1].

Analytical, diagnostic and therapeutic context of Flukanide

• Rafoxanide concentrations in plasma were measured by means of HPLC analysis [13].
• Possible differential diagnoses and predisposing factors for rafoxanide toxicity are discussed [22].

References