Milbemycin oxime

Milbemycin oxime Basic information
Description Uses Drug Interactions Uses Mechanism of action Side Effects
Product Name:Milbemycin oxime
Synonyms:Milbemycin oxime;Milbemycin Oxime (200 mg);Milbemycin oxime CRS;Milbemycin Oxime (Mixture of Milbemycin Oxime A3 and A4);Milbemycin OximeQ: What is Milbemycin Oxime Q: What is the CAS Number of Milbemycin Oxime Q: What is the storage condition of Milbemycin Oxime;Milbemycin Oxime (1443806);β-phenylacrylophenone;Milbemite
CAS:129496-10-2
MF:2C32H45NO7.2C31H43NO7
MW:2194.78
EINECS:206-141-6
Product Categories:APIs for Veterinary;Inhibitors;API;129496-10-2
Mol File:129496-10-2.mol
Milbemycin oxime Structure
Milbemycin oxime Chemical Properties
Melting point 169.6-177.4°
Fp 412℃
storage temp. Store at -20°C
solubility DMSO:100.0(Max Conc. mg/mL);91.13(Max Conc. mM)
form A crystalline solid
Stability:Hygroscopic
InChIKeyLKMMLHTWKLEARD-MGZQXKBQSA-N
Safety Information
RIDADR 2588
WGK Germany 3
HazardClass 6.1(b)
PackingGroup III
HS Code 2932206000
ToxicityLD50 orally in mice: 1000-1500 mg/kg (Ciba-Geigy)
MSDS Information
Milbemycin oxime Usage And Synthesis
DescriptionMilbemycin is an oral medication used as a dewormer and heartworm preventive. This medication should not be used in doses higher than the recommended heartworm prevention dose, except under veterinary supervision. Studies support the safety of milbemycin products in Collies and other breeds prone to the MDR-1 gene mutation when used at the recommended heartworm prevention dose.
UsesMilbemycin 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. The substance is often combined with other parasiticides to achieve a broader spectrum of action. Such products include: Milbemax (with praziquantel) Sentinel Flavor Tabs (with lufenuron) 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.
Drug InteractionsMilbemycin should not used in combination with cyclosporine, quinidine or ketoconazole.
UsesIntestinal parasite deworming in dogs and for heartworm prevention in dogs and cats.
Mechanism of actionLike 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.
Side EffectsThe drug is tolerated well, even by dogs with multiple drug resistance. In high doses, it can cause side effects like stupor, tremor and ataxia.
Usescontrols intestinal parasites in animals
UsesMilbemycin oxime is a semi-synthetic macrocyclic lactone prepared by the oxidation and oximation of a mixture of two natural products, milbemycin A3 and A4 (in ~30:70 ratio). Milbemycin oxime is used therapeutically for the prevention of intestinal parasites in dogs. Like the other milbemycin/avermectins, it was developed for intestinal parasite control in animals and acts by opening glutamate sensitive chloride channels in neurons of invertebrates leading to paralysis by hyperpolarisation of these cells and signal transfer blocking.
Veterinary Drugs and TreatmentsMilbemycin tablets are labeled as a once-a-month heartworm preventative (Dirofilaria immitis) and for hookworm control (Ancylostoma caninum). It has activity against a variety of other parasites, including adult hookworms (A. caninum), adult roundworms (T. canis, T. leonina) and whipworms (Trichuris vulpis). In cats, milbemycin has been used successfully to prevent larval infection of Dirofilaria immitis.
Milbemycin, like ivermectin can be used for treatment of generalized demodicosis in dogs, but treatment can be significantly more expensive. It is likely safer to use in breeds susceptible to mdr1 genetic mutation (Collies, Shelties, Australian shepherds, etc.) at the doses used for this indication, but neuro toxicity is possible. Older dogs, those that have had a long duration of disease prior to treatment, and dogs with pododemodicosis appear have a lower success rate with milbemycin treatment.
Milbemycin oxime Preparation Products And Raw materials
MilbeMycin A4 OxiMe Miconazole Impurity Milbemycin EP Impurity D 2-methyl-6-oxo-1,6-dihydro-[3,4'-bipyridine]-5-carboxylic acid Milrinone Impurity 17 Milrinone Impurity 15 Milrinone Impurity 6 1-Oxo Mirtazapine (Mirtazapine Impurity C) MilbeMycin A3 OxiMe Miconazole IMpurity H MILBEMECTIN A4 Milrinone Impurity 10 Sancycline hydrochloride SPINETORAM Milrinone Impurity 5 Milrinone Impurity 16 Milbemycin oxime FEMA 3693

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