Milbemycin oxime

  • ( 10E, 14E, 16E ) - ( 1R, 4S, 5 'S, 6R, 6'R, 8R, 13R, 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 - tetraenes )-6 -spiro -2'- (tetrahydropyran ) -2,21 -dione 21 - (SR) -oxime (70 %)
  • ( 10E, 14E, 16E ) - ( 1R, 4S, 5 'S, 6R, 6'R, 8R, 13R, 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 - tetraene )-6 -spiro- 2'- (tetrahydropyran ) - 2,21 -dione 21 - ( EZ ) -oxime (30%)
  • C31H43NO7 (30%)
  • C32H45NO7 (70%)

QP54AB01

Antiparasitic

  • 541.68 g.mol -1 ( 30%)
  • 555.70 g.mol -1 ( 70%)

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Milbemycin oxime is inserted in veterinary medicine drug from the milbemycin, which is used as a broadband anti-parasitic application. It is against worms ( anthelmintic ), insects ( insecticides ) and mites ( acaricide ) effective.

Mechanism of action

Milbemycins are as avermectins fermentation products of Actinomyces ( Streptomyces spp.) And have a similar mechanism of action, but a significantly longer effective. Milbemycin oxime is obtained from Streptomyces hygroscopicus aureolacrimosus. It increases in invertebrates, the membrane permeability of the nerve or muscle cells for chloride ions by binding to glutamate -activated chloride channels. This leads to hyperpolarization of the cell membrane and to a blocking of the excitation transition.

Application

The drug is administered orally and absorbed only about 5 to 10%, the major portion is excreted unchanged in the feces. The elimination of the absorbed fraction in the liver via the bile. Milbemycin oxime is well tolerated and can also be used in dogs with the MDR1 defect. In high doses it may be temporary side effects such as rigidity, tremor and ataxia.

Milbemycin oxime is effective against a wide range of nematodes, it may also be used against heartworm, wherein the efficacy is, however, lower than that of ivermectin. In addition, it is effective against various mites ( Sarcoptes, Demodex ).

In the preparations currently available on the market milbemycin oxime is combined with other active ingredients, so that the activity spectrum is widened.

Trade names

  • With praziquantel: Milbemax
  • With lufenuron: Program Plus
  • With praziquantel and lufenuron: Sentinel Spectrum
CAS registry number PubChem Anatomical Therapeutic Chemical Classification System Chlorine Dirofilaria immitis
572506
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