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Milbemycin oxime
Systematic (IUPAC) name
(10E,14E,16E)-(1 R,4S,5′S,6R,6′R,8R,13 R,20R,24S)- 24-hydroxy-5′,6′,11,13,22-pentamethyl- (3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa- 10,14,16,22-tetraen)-6-spiro-2′-(tetrahydropyran)- 2,21-dion 21-(EZ)-oxim (30%)

(10E,14E,16E)-(1 R,4S,5′S,6R,6′R,8R,13 R,20R,24S)- 6′-ethyl-24-hydroxy-5′,11,13,22-tetramethyl- (3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]- pentacosa-10,14,16,22-tetraene)-6-spiro- 2′-(tetrahydropyran)-2,21-dion 21-(EZ)-oxim (70%)

Identifiers
CAS number 129496-10-2
ATC code  ?
PubChem  ?
Chemical data
Formula C31H43NO7 (30%)
C32H45NO7 (70%)
Mol. mass 541.68 g/mol (30%)
555.702 g/mol (70%)
Pharmacokinetic data
Bioavailability 5–10%
Metabolism Liver
Half life  ?
Excretion Biliary
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

Milbemyine 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) and mites (miticide).

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

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

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.

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