Milbemycin oxime
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Milbemycin oxime, sold under the brand name Interceptor among others, is a veterinary medication from the group of
milbemycin The milbemycins are a group of macrolides chemically related to the avermectins and were first isolated in 1972 from '' Streptomyces hygroscopicus''. They are used in veterinary medicine as antiparasitic agents against worms, ticks and fleas.
s, used as a broad spectrum
antiparasitic Antiparasitics are a class of medications which are indicated for the treatment of parasitic diseases, such as those caused by helminths, amoeba, ectoparasites, parasitic fungi, and protozoa, among others. Antiparasitics target the parasitic agent ...
. It is active against worms (
anthelmintic Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. They may a ...
) and mites (
miticide Acaricides are pesticides that kill members of the arachnid subclass ''Acari'', which includes ticks and mites. Acaricides are used both in medicine and agriculture, although the desired selective toxicity differs between the two fields. Termino ...
).


Mechanism of action

Milbemycins are products of
fermentation Fermentation is a metabolic process that produces chemical changes in organic substrates through the action of enzymes. In biochemistry, it is narrowly defined as the extraction of energy from carbohydrates in the absence of oxygen. In food ...
by ''
Streptomyces ''Streptomyces'' is the largest genus of Actinomycetota and the type genus of the family Streptomycetaceae. Over 500 species of ''Streptomyces'' bacteria have been described. As with the other Actinomycetota, streptomycetes are gram-positive, ...
'' species. They have a similar mechanism of action, but a longer half-life than the avermectins. Milbemycin oxime is produced by ''
Streptomyces hygroscopicus ''Streptomyces hygroscopicus'' is a bacterial species in the genus '' Streptomyces''. It was first described by Hans Laurits Jensen in 1931. Biochemistry Cultures of different strains of ''S. hygroscopicus'' can be used to produce a number of ...
aureolacrimosus''. It opens
glutamate Glutamic acid (symbol Glu or E; the ionic form is known as glutamate) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a non-essential nutrient for humans, meaning that the human body can syn ...
sensitive
chloride channel Chloride channels are a superfamily of poorly understood ion channels specific for chloride. These channels may conduct many different ions, but are named for chloride because its concentration ''in vivo'' is much higher than other anions. Severa ...
s in
neuron A neuron, neurone, or nerve cell is an electrically excitable cell that communicates with other cells via specialized connections called synapses. The neuron is the main component of nervous tissue in all animals except sponges and placozoa. N ...
s and
myocyte A muscle cell is also known as a myocyte when referring to either a cardiac muscle cell (cardiomyocyte), or a smooth muscle cell as these are both small cells. A skeletal muscle cell is long and threadlike with many nuclei and is called a muscl ...
s of
invertebrate Invertebrates are a paraphyletic group of animals that neither possess nor develop a vertebral column (commonly known as a ''backbone'' or ''spine''), derived from the notochord. This is a grouping including all animals apart from the chordate ...
s, leading to hyperpolarisation of these cells and blocking of signal transfer.


Uses

Milbemycin oxime is active against a broad spectrum of
nematode The nematodes ( or grc-gre, Νηματώδη; la, Nematoda) or roundworms constitute the phylum Nematoda (also called Nemathelminthes), with plant-Parasitism, parasitic nematodes also known as eelworms. They are a diverse animal phylum inhab ...
s. Its miticide spectrum includes ''
Sarcoptes ''Sarcoptes'' is a genus of mites. In some contexts, the types are all considered subordinate to ''Sarcoptes scabiei ''Sarcoptes scabiei'' or the itch mite is a parasitic mite that burrows into skin and causes scabies. The mite is found ...
'' and ''
Demodex ''Demodex'' is a genus of tiny mites that live in or near hair follicles of mammals. Around 65 species of ''Demodex'' are known. Two species live on humans: ''Demodex folliculorum'' and ''Demodex brevis'', both frequently referred to as eyelash ...
''. The drug is FDA-approved for prevention of
heartworm ''Dirofilaria immitis'', also known as heartworm or dog heartworm, is a parasitic roundworm that is a type of filarial worm, a small thread-like worm, that causes dirofilariasis. It is spread from host to host through the bites of mosquitoe ...
in dogs and cats, although it is less potent against heartworms than
ivermectin Ivermectin (, '' EYE-vər-MEK-tin'') is an antiparasitic drug. After its discovery in 1975, its first uses were in veterinary medicine to prevent and treat heartworm and acariasis. Approved for human use in 1987, today it is used to treat inf ...
. The substance is often combined with other parasiticides to achieve a broader spectrum of action. Such products include: * Milbemax and Interceptor Plus (with
praziquantel Praziquantel (PZQ), sold under the brandname Biltricide among others, is a medication used to treat a number of types of helminthiasis, parasitic worm infections in mammals, birds, amphibians, reptiles, and fish. In humans specifically, it is us ...
) * Sentinel Flavor Tabs (with
lufenuron Lufenuron is the active ingredient in the Veterinary medicine, veterinary flea control medication Program, and one of the two active ingredients in the flea, heartworm, ringworm and anthelmintic medicine milbemycin oxime/lufenuron (Sentinel). Luf ...
) * Trifexis (with
spinosad Spinosad is an insecticide based on chemical compounds found in the bacterial species ''Saccharopolyspora spinosa''. The genus ''Saccharopolyspora'' was discovered in 1985 in isolates from crushed sugarcane. The bacteria produce yellowish-pink ae ...
) * NexGard Spectra (with
afoxolaner Afoxolaner (INN) is an insecticide and acaricide that belongs to the isoxazoline chemical compound group. It acts as an antagonist at ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid ...
) The drug has been used in marine
reef aquaria A reef aquarium or reef tank is a marine aquarium that prominently displays live corals and other marine invertebrates as well as fish that play a role in maintaining the tropical coral reef environment. A reef aquarium requires appropriately ...
to control parasitic
Tegastidae Tegastidae is a family of copepods, which are characterised by having laterally compressed bodies (resembling that of an amphipod), a claw-like mandible in the nauplius stage, and by a modified male genital complex. 85 species have been describ ...
copepod infestations on captive hard coral colonies. Other arthropod invertebrates will be killed by the treatment.


Side effects

The drug is usually tolerated well, but such side effects may occur such as vomiting, phlegming, and glassy eyes.


References

{{Endectocides Anthelmintics Insecticides Veterinary drugs Spiro compounds