Milbemycin oxime

Milbemycin oxime
Milbemycin oxime
Clinical data
Pregnancy cat.  ?
Legal status  ?
Routes Oral
Pharmacokinetic data
Bioavailability 5–10%
Metabolism Liver
Excretion Biliary
Identifiers
CAS number 129496-10-2
ATC code  ?
Chemical data
Formula C31H43NO7 (30%)
C32H45NO7 (70%)
Mol. mass 541.68 g/mol (30%)
555.702 g/mol (70%)
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Milbemycin oxime (trade name Interceptor, marketed by Novartis) is a veterinary drug from the group of milbemycins, used as a broad spectrum antiparasitic. It is active against worms (anthelmintic), insects (insecticide)[citation needed] and mites (miticide).

Contents

Mechanism of action

Like avermectins, milbemycins are products of fermentation by Streptomyces species. They have a similar mechanism of action, but a longer half-life than the avermectins. Milbemycin oxime is produced by Streptomyces hygroscopicus aureolacrimosus. It opens glutamate sensitive chloride channels in neurons and myocytes of invertebrates, leading to hyperpolarisation of these cells and blocking of signal transfer.

Uses

Milbemycin oxime is active against a broad spectrum of nematodes, although it is less potent against heartworms than ivermectin. Its miticide spectrum includes Sarcoptes and Demodex. The USA FDA approval for milbemycin oxime as formulated alone does not indicate insecticidal activity.[1]

The substance is often combined with other parasiticides to achieve a broader spectrum of action. Such products include:

Recently the drug has been used in marine reef aquaria to control parasitic harptacoid copepod (Tegastidae) infestations on captive hard coral colonies. It is an effective full tank treatment for these parasites because it is not toxic to corals in the dosage required to kill the parasites. Shrimps, crabs and other crustaceans should be removed prior to treatment, as they will be killed by the treatment.

Side effects

The drug is tolerated well, even by dogs with multiple drug resistance. In high doses, it can cause side effects like stupor, tremor and ataxia.

References

  1. ^ NADA number 140-915