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Pharmacological particulars
Pharmacodynamic properties
ATC Vet Code: QP52A
Pharmacotherapeutic group: Anthelmintics, Quinoline derivatives and related substances
Supaverm is a combination of the salicylanilide closantel and the benzimidazole mebendazole. Closantel is highly effective against liver flukes and haematophagous nematodes in sheep and goats and against larval stages of some arthropods in sheep. Mebendazole is highly active against gastrointestinal nematodes in sheep and goats and against lungworms and cestodes in sheep.
Closantel is an uncoupler of the mitochondrial oxidative phosphorylation resulting in inhibition of the ATP-synthesis. This induces a dramatic change in the energy metabolism which finally leads to the death of the parasite.
Mebendazole has a selective anthelmintic action through a specific interaction with the microtubular system of the absorptive cells of the parasite, leading to an irreversible lytic destruction of these cells and death of the worm.
Pharmacokinetic particulars
Closantel is rapidly absorbed into the systemic circulation after oral administration and peak plasma levels are attained at 24-48 hours after dosing. In plasma, closantel is bound more than 99 % to albumin. As a result, tissue distribution is very limited. On average, tissue levels are 15 times lower than plasma levels. The elimination half-life from plasma and tissues is 2 to 3 weeks in sheep and about 10 days in goats. Metabolism is negligible and the main excretion route is the bile. The urinary excretion is negligible.
Mebendazole is of low solubility and only slightly absorbed from the gastrointestinal tract. Consequently, mebendazole is eliminated almost unaltered via the faeces after oral administration of therapeutic doses. The slight fraction that is absorbed produces maximal plasma levels within 24 hours of administration. The absorbed fraction is metabolised by the liver. The metabolites are mainly eliminated via urine. Seven days after treatment, tissue levels of mebendazole are below the detection limit.
The kinetics of both active ingredients are not altered when given in the combination.
Environmental properties
Closantel has the potential to adversely affect non-target organisms. Following treatment, excretion of potentially toxic levels of closantel may occur over a period of several weeks. Faeces containing closantel excreted onto pasture from treated animals may reduce the abundance of dung feeding organisms which may impact dung degradation in the field.