Disease relevance of Diamfenetide

• The systematic use of diamphenethide at this dose level at intervals of up to six weeks during the period of metacercarial challenge should prevent ovine fascioliasis [1].
• When given at a dosage of 10 mg/kg of body weight, diamfenetide was 87% effective in preventing establishment of F hepatica infections in sheep that were given the drug daily for 14 days, and was 96% effective in sheep that were given the drug for 21 days [2].

High impact information on Diamfenetide

• The inclusion of rabbit liver microsomes in the basal culture medium resulted in diamphenethide exhibiting cidal activity equivalent to that seen when its free-amine active metabolite was assayed [3].
• Studies of the effect of diamphenethide and oxyclozanide on the metabolism of Fasciola hepatica [4].
• Short-term (1-3 hr) incubations in vitro of immature and adult Fasciola hepatica with 10(-4) to 10(-5) M free amine of diamfenetide (DPT-FA) demonstrated a time/dose-dependent, irreversible paralysis that involved an increase in muscular tension and decrease in contraction amplitude [5].
• The activity of diamfenetide (N,N'-[oxybis(2,1-ethan diyloxy-4,1-phenylene)] bis acetamide) was studied in lambs experimentally inoculated with Fasciola hepatica [6].
• When exposed to certain known fasciolicides, newly excysted flukes were susceptible only to diamphenethide, the free amine of diamphenethide, emetine hydrochloride and albendazole [7].

Analytical, diagnostic and therapeutic context of Diamfenetide

• Ultrastructural changes to the tegument of 5-week-old, 3-week-old and freshly-excysted Fasciola hepatica following in vitro incubation with the deacetylated (amine) metabolite of diamphenethide (DAMD, 10 microgramsml-1) were examined by transmission electron microscopy [8].
• The effect of the deacetylated (amine) metabolite of diamphenethide (DAMD, 10 micrograms ml-1) on the uptake and incorporation by adult Fasciola hepatica of radioactively labelled precursors of DNA, RNA and protein synthesis ([3H]thymidine, [3H]uridine and [3H]leucine, respectively) was measured by liquid scintillation counting [9].
• Chemoprophylaxis with diamfenetide against experimental infections of Fasciola hepatica in ruminants [2].
• The effect of the deacetylated (amine) metabolite of diamphenethide (10 micrograms/ml) on the tegumental surface of Fasciola hepatica over a 24 h period in vitro has been determined by scanning electron microscopy [10].

References