Name | Milbemycin Oxime |
CAS number | 129496-10-2 |
EINECS number | 206-141-6 |
Synonym | CGA-179246; CGA 179246; CGA179246; Milbemycin A 5-oxime; Milbemite; Trifexis; Milbemycin oxime; trade name Interceptor. |
Description | Milbemycin oxime 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). Milbemycin oxime is a semi-synthetic macrocyclic lactone prepared by the oxidation and oximation of an 80:20 ratio of milbemycin A3 and A. 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. |
Structure | |
Molecular Formula | 2C32H45NO7.2C31H43NO7 |
Molecular Weight | 2194.78 g/mol |
Appearance | Solid powder |
Quality Standard | EP/USP/JP Standard |
Assay | ≥98% |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition | Store in cool place. Keep container tightly closed in a dry and well ventilated place. |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Milbemycin Oxime More Info
Milbemycin oxime is a broad-spectrum antiparasitic agent widely used in veterinary medicine, especially for dogs, to control internal and external parasites.
Mechanism of Action
Milbemycin oxime works by binding to specific high-affinity sites on parasite nerve and muscle cells, particularly glutamate-gated chloride channels and GABA (gamma-aminobutyric acid) receptors. This binding increases the permeability of the parasite's cell membranes to chloride ions (Cl⁻), causing hyperpolarization of nerve and muscle cells. As a result, nerve signal transmission is blocked, leading to paralysis and death of the parasites. This mechanism affects nematodes (internal parasites) and arthropods (external parasites), disrupting their neuromuscular function and also impairing reproduction in some parasites by reducing egg laying or causing abnormal oogenesis. Mammals are largely unaffected because their GABA receptors are confined to the central nervous system, which milbemycin oxime poorly penetrates.
Applications
Milbemycin oxime is used primarily for:
Prevention of heartworm disease (Dirofilaria immitis) by killing larvae before they mature into adult worms.
Treatment and control of intestinal nematodes such as roundworms, hookworms, and whipworms.
Control of certain external parasites like mites (off-label use).
It is often combined with other agents (e.g., afoxolaner, praziquantel, lufenuron, spinosad) to broaden the spectrum of activity against fleas, ticks, and tapeworms.
Safety and Side Effects
Milbemycin oxime is generally well tolerated in dogs, including young puppies from 8 weeks of age. Safety studies show no significant adverse effects even at doses up to 5 times the recommended maximum. Mild side effects may include occasional vomiting, diarrhea, lethargy, or decreased appetite, particularly in dogs already infected with heartworms. Severe reactions are rare. It is important to test for existing heartworm infection before starting treatment because killing adult worms can cause complications.
Routes of Administration
Milbemycin oxime is administered orally, commonly as chewable tablets or in combination chewable products. It is given once monthly for prevention or treatment, with dosage depending on the parasite targeted.
Pharmacokinetics
Absorption: Rapid and almost complete oral absorption with peak plasma concentrations reached within 1 to 4 hours depending on formulation.
Bioavailability: Approximately 50–80%, varying with formulation and species.
Distribution: Widely distributed throughout the body, including tissues and body fluids; volume of distribution around 2.7 L/kg.
Metabolism and Elimination: Metabolized extensively (in rats, no unchanged drug found in excreta); eliminated efficiently with a terminal half-life ranging from about 1 to 3 days in dogs.
Clearance: Efficient systemic clearance supports monthly dosing intervals.
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