milbemycin oxime
{{Short description|Chemical compound}}
{{Drugbox
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| verifiedrevid = 450771830
| image = Milbemycinoxime.png
| pronounce =
| tradename = Interceptor, others
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| DailyMedID = Milbemycin oxime
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| routes_of_administration = By mouth
| class =
| ATCvet = yes
| ATC_prefix = P54
| ATC_suffix = AB01
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| legal_US = Rx-only
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| bioavailability = 5–10%
| protein_bound =
| metabolism = Liver
| elimination_half-life =
| excretion = Bile duct
| CAS_number_Ref = {{cascite|correct|CAS}}
| CAS_number = 129496-10-2
| UNII_Ref = {{fdacite|changed|FDA}}
| UNII = 0502PUN0GT
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| chemical_formula = C31H43NO7 (30%)
C32H45NO7 (70%)
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| molecular_weight = 541.68 g/mol (30%)
555.702 g/mol (70%)
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Milbemycin oxime, sold under the brand name Interceptor among others, is a veterinary medication from the group of milbemycins, used as a broad spectrum antiparasitic. It is active against worms (anthelmintic) and mites (miticide).{{cite journal|pmid=22488596|year=2012|last1=Mueller|first1=R. S.|title=An update on the therapy of canine demodicosis|journal=Compendium (Yardley, Pa)|volume=34|issue=4|pages=E1-4}}
Mechanism of action
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.{{cite book| vauthors = Mehlhorn H |title=Encyclopedia of Parasitology: A-M|url=https://books.google.com/books?id=Jpg1ysgVn-AC&pg=PA646|year=2008|publisher=Springer Science & Business Media|isbn=978-3-540-48994-8|page=646}}
Uses
Milbemycin oxime is active against a broad spectrum of nematodes. Its miticide spectrum includes Sarcoptes and Demodex. The drug is FDA-approved for prevention of heartworm in dogs and cats,{{cite web|title=NADA 140-915 Interceptor – supplemental approval (September 9, 1996)|website=Food and Drug Administration|url=https://www.fda.gov/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/ucm054860.htm|archive-url=https://web.archive.org/web/20090710082912/http://www.fda.gov/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/ucm054860.htm|url-status=dead|archive-date=July 10, 2009}} although it is less potent against heartworms than ivermectin.{{Citation needed|date=May 2017}}
The substance is often combined with other parasiticides to achieve a broader spectrum of action. Such products include:{{cn|date=February 2023}}
- Milbemax and Interceptor Plus (with praziquantel)
- Sentinel Flavor Tabs (with lufenuron)
- Trifexis (with spinosad)
- Nexgard Spectra (with afoxolaner)
The drug has been used in marine reef aquaria to eliminate parasitic Tegastidae arthropod infestations on captive hard coral colonies. This treatment is not selective and will also kill desired arthropods such as shrimps and crabs.{{cite book| vauthors = Roberts HE |title=Fundamentals of Ornamental Fish Health|url=https://books.google.com/books?id=ZwydxKMbzz8C&pg=PT93|year=2011|publisher=John Wiley & Sons|isbn=978-1-119-94948-0|pages=93–94}}{{cite book| vauthors = Lewbart GA |title=Invertebrate Medicine|url=https://books.google.com/books?id=NaAMh8sEU4oC&pg=PA71|year=2011|publisher=John Wiley & Sons|isbn=978-0-470-96078-3|page=71}}
Side effects
The drug is usually tolerated well, but such side effects may occur such as vomiting, phlegming, and glassy eyes.{{citation needed|date=May 2016}}