Milberoxime is a broad-spectrum anti parasitic drug of macrolide class, belonging to the category of veterinary anthelmintics, mainly used for the prevention and treatment of parasites inside and outside the body of dogs and cats.

Basic Properties

Source: Semi synthetic macrolide compounds obtained by oxidation and oximation of milbermycin A3 and A ₄ (approximately 30:70 ratio) fermented products from Streptomyces hygroscopicus aureolacrimosus.

Appearance: White to off white crystalline powder with an odor.

Melting point: 169.6 – 177.4 ° C

Solubility: Easily soluble in organic solvents such as benzene, acetone, ethanol, methanol, chloroform, DMSO, etc., insoluble in water.

Stability: It has hygroscopicity and needs to be sealed and stored at -20 ° C.

Safety: Oral LD ₅₀ for mice is 1000-1500 mg/kg; It is recommended that toxic reactions occur at a dosage of 2000 times or more; It has higher safety for mammals (better than ivermectin and avermectin).

Pharmacological action

Milbeixime works by interfering with neural conduction in invertebrates:

Binding to specific high affinity sites on parasite cells affects the permeability of the cell membrane to Cl ⁻;

Enhance the permeability of the neural membrane to Cl ⁻, causing cell membrane hyperpolarization;

Blocking neural signal transmission ultimately leads to paralysis and death of the parasite.

Due to the small amount of GABA present in the central nervous system of mammals, it is relatively safe for dogs, cats, and other mammals.

main purpose

Milberoxime is a pure veterinary drug widely used for parasitic control in companion animals (dogs, cats):

Parasites in the body

Heartworm prevention: prevention of canine heartworm infection with Dirofilaria, orally administered once a month

Intestinal nematodes: expel roundworms (such as canine roundworm and lion roundworm), hookworms (such as canine hookworm), whipworms (such as fox tail nematode), etc

External parasite

It also has a killing effect on external parasites such as mites (scabies mites, hair follicle mites/demodex mites), lice, fleas, etc

Common compound preparations

Milbemax+Praziquantel (such as Milbemax/Hylopon): simultaneously covers nematodes and tapeworms

Doxycycline+Milberoxime (such as Panam/PANORAMIS): simultaneously covers parasites and fleas in the body

Milberoxime+Chlorfenuron (such as Sentinel): Heartworm Prevention+Flea Control

pharmacokinetics

After oral administration, it is rapidly absorbed and reaches the peak blood concentration in dogs within about 4 hours

Elimination half-life of approximately 11.7 hours (A3) and longer (A3)

About 90% is excreted in its original form through feces within 48 hours

Precautions

Cannot be used in combination with cyclosporine, quinidine, and ketoconazole

For MDR-1 gene mutant dog breeds (such as Collies, Hilti, etc.), they are relatively safe at recommended doses, but high doses may cause neurotoxicity

High doses may cause adverse reactions such as ataxia, tremors, salivation, and drowsiness

Highly toxic to aquatic organisms (H410), environmental pollution should be avoided

Summary：

Dimension Description

Drug type: Macrolide broad-spectrum antiparasitic drugs

Suitable for pure animal use (dogs, cats)

Core use: prevention of heartworm worms, expulsion of intestinal nematodes, and prevention and control of ectoparasites such as mites

High safety for mammals, superior to ivermectin

Common dosage forms: Oral chewable tablets, compound tablets

Whether for human use or not, only for animal use

Milbeixime is currently a very important drug variety in the field of pet deworming, especially occupying an important position in the canine heartworm prevention market.