Milbemycin oxime

Bezeichnung:Milbemycin oxime

CAS-Nr129496-10-2

Englisch Name:Milbemycin oxime

CBNumberCB11104418

Summenformel2C32H45NO7.2C31H43NO7

Molgewicht2194.78

MOL-Datei129496-10-2.mol

Milbemycin oxime physikalisch-chemischer Eigenschaften

Schmelzpunkt	169.6-177.4°
Flammpunkt	412℃
storage temp.	Store at -20°C
Löslichkeit	DMSO:100.0(Max Conc. mg/mL);91.13(Max Conc. mM)
Aggregatzustand	A crystalline solid
Farbe	White to off-white
Stabilität	Hygroscopic
InChIKey	LKMMLHTWKLEARD-MGZQXKBQSA-N

Sicherheit

RIDADR	2588
WGK Germany	3
HazardClass	6.1(b)
PackingGroup	III
HS Code	2932206000
Toxizität	LD50 orally in mice: 1000-1500 mg/kg (Ciba-Geigy)

Gefahreninformationscode (GHS)

Milbemycin oxime Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Milbemycin 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.
Verwenden
controls intestinal parasites in animals
Clinical Use
Milbemycin oxime (Milbemycin) is available as an oral chewable tablet (2.3–27 mg) for heartworm prevention in dogs and cats, as well as a 0.1% otic solution for treating ear mites. It is not available in a more concentrated dosage form, so overdoses are relatively rare[1].
Toxikologie
The therapeutic dosages of Milbemycin oxime (milbemycin) for heartworm prevention are 0.5 mg/kg in dogs and 2 mg/kg in cats. Mild clinical signs of ataxia, hypersalivation, mydriasis, and lethargy have been documented in ivermectin-sensitive dogs dosed at 5 to 10 mg/kg. In a separate report, two ABCB1-defective dogs developed mild signs (ataxia) after being dosed repeatedly with milbemycin for demodicosis; one dog received 0.8 mg/kg 2 days in a row, and the other dog received 1.5 mg/kg daily for 13 days before developing signs. Mild clinical signs have been reported to develop in normal dogs at 10 to 20 mg/kg and in cats and dogs with suspected ABCB1 gene deletions greater than 5 to 10 mg/kg. The most common clinical signs reported include ataxia, tremors, lethargy, vomiting, mydriasis, disorientation, and hypersalivation[1].
Veterinary Drugs and Treatments
Milbemycin 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.
Einzelnachweise
[1] DVM, Valentina M. Merola, Paul A. Eubig DVM MS and MS. “Toxicology of Avermectins and Milbemycins (Macrocylic Lactones) and the Role of P-Glycoprotein in Dogs and Cats.” Veterinary Clinics of North America-Small Animal Practice 42 2 (2012): Pages 313-333.

Milbemycin oxime Upstream-Materialien And Downstream Produkte

Milbemycin oxime Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

129496-10-2, Milbemycin oxime Verwandte Suche:

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