Milbemycin oxime

Last updated
Milbemycin oxime
Milbemycinoxime.png
Clinical data
Trade names Interceptor
License data
Routes of
administration
By mouth
ATCvet code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 5–10%
Metabolism Liver
Excretion Bile duct
Identifiers
CAS Number
UNII
ECHA InfoCard 100.205.451 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C31H43NO7 (30%)
C32H45NO7 (70%)
Molar mass 541.68 g/mol (30%)
555.702 g/mol (70%)
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Milbemycin oxime, sold under the brand name Interceptor among others, is a veterinary medication from the group of milbemycins, used as a broad spectrum antiparasitic. [1] It is active against worms (anthelmintic) [1] and mites (miticide). [2]

Contents

Mechanism of action

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. [3]

Uses

Milbemycin oxime is active against a broad spectrum of nematodes. Its miticide spectrum includes Sarcoptes and Demodex . The drug is FDA-approved for prevention of heartworm in dogs and cats, [4] although it is less potent against heartworms than ivermectin.[ citation needed ]

The substance is often combined with other parasiticides to achieve a broader spectrum of action. Such products include:[ citation needed ]

The drug has been used in marine reef aquaria to control parasitic Tegastidae copepod infestations on captive hard coral colonies. Other arthropod invertebrates will be killed by the treatment. [5] [6]

Side effects

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

Related Research Articles

Interceptor may refer to:

<span class="mw-page-title-main">Oxytetracycline</span> Antibiotic

Oxytetracycline is a broad-spectrum tetracycline antibiotic, the second of the group to be discovered.

<span class="mw-page-title-main">Praziquantel</span> Medication

Praziquantel (PZQ), sold under the brandname Biltricide among others, is a medication used to treat a number of types of parasitic worm infections in mammals, birds, amphibians, reptiles, and fish. In humans specifically, it is used to treat schistosomiasis, clonorchiasis, opisthorchiasis, tapeworm infections, cysticercosis, echinococcosis, paragonimiasis, fasciolopsiasis, and fasciolosis. It should not be used for worm infections of the eye. It is taken by mouth.

<span class="mw-page-title-main">Abamectin</span>

Abamectin is a widely used insecticide and anthelmintic. Abamectin, is a member of the Avermectin family and is a natural fermentation product of soil dwelling actinomycete Streptomyces avermitilis. Abamectin, differs from Ivermectin, the popular member of the Avermectin family, by double bond on C-22-25. Fermentation of Streptomyces avermitilis yields 8 closely related Avermectin homologues out of which B1 forms the bulk of the fermentation. The non proprietary name, abamectin, is a combination of Bla and B1b. Out of all the Avermectins, abamectin is the only one that is used both in agriculture and pharmaceuticals.

<span class="mw-page-title-main">Natural product</span> Chemical compound or substance produced by a living organism, found in nature

A natural product is a natural compound or substance produced by a living organism—that is, found in nature. In the broadest sense, natural products include any substance produced by life. Natural products can also be prepared by chemical synthesis and have played a central role in the development of the field of organic chemistry by providing challenging synthetic targets. The term natural product has also been extended for commercial purposes to refer to cosmetics, dietary supplements, and foods produced from natural sources without added artificial ingredients.

<span class="mw-page-title-main">Cefixime</span> Ofloxacin

Cefixime, sold under the brand name Suprax among others, is an antibiotic medication used to treat a number of bacterial infections. These infections include otitis media, strep throat, pneumonia, urinary tract infections, gonorrhea, and Lyme disease. For gonorrhea typically only one dose is required. In the United States it is a second-line treatment to ceftriaxone for gonorrhea. It is taken by mouth.

<i>Dirofilaria immitis</i> Species of worm that causes parasitic disease in animals

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 mosquitoes. There are four genera of mosquitoes that transmit dirofilariasis, Aedes, Culex, Anopheles, and Mansonia. The definitive host is the dog, but it can also infect cats, wolves, coyotes, jackals, foxes, ferrets, bears, seals, sea lions and, under rare circumstances, humans.

<span class="mw-page-title-main">Selamectin</span> Topical parasiticide for dogs and cats

Selamectin is a topical parasiticide and anthelminthic used on dogs and cats. It treats and prevents infections of heartworms, fleas, ear mites, sarcoptic mange (scabies), and certain types of ticks in dogs, and prevents heartworms, fleas, ear mites, hookworms, and roundworms in cats. It is structurally related to ivermectin and milbemycin. Selamectin is not approved for human use.

<span class="mw-page-title-main">Moxidectin</span> Chemical compound

Moxidectin is an anthelmintic drug used in animals to prevent or control parasitic worms (helminths), such as heartworm and intestinal worms, in dogs, cats, horses, cattle and sheep. Moxidectin kills some of the most common internal and external parasites by selectively binding to a parasite's glutamate-gated chloride ion channels. These channels are vital to the function of invertebrate nerve and muscle cells; when moxidectin binds to the channels, it disrupts neurotransmission, resulting in paralysis and death of the parasite.

<span class="mw-page-title-main">Benazepril</span> Chemical compound

Benazepril, sold under the brand name Lotensin among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease. It is a reasonable initial treatment for high blood pressure. It is taken by mouth. Versions are available as the combinations benazepril/hydrochlorothiazide and benazepril/amlodipine.

In biology, autolysis, more commonly known as self-digestion, refers to the destruction of a cell through the action of its own enzymes. It may also refer to the digestion of an enzyme by another molecule of the same enzyme.

<span class="mw-page-title-main">Imipenem</span> Chemical compound

Imipenem is an intravenous β-lactam antibiotic discovered by Merck scientists Burton Christensen, William Leanza, and Kenneth Wildonger in the mid-1970s. Carbapenems are highly resistant to the β-lactamase enzymes produced by many multiple drug-resistant Gram-negative bacteria, thus play a key role in the treatment of infections not readily treated with other antibiotics.

<span class="mw-page-title-main">Lufenuron</span> Chemical compound

Lufenuron is the active ingredient in the veterinary flea control medication Program, and one of the two active ingredients in the flea, heartworm, ringworm and anthelmintic medicine milbemycin oxime/lufenuron (Sentinel).

<span class="mw-page-title-main">Sultamicillin</span> Chemical compound

Sultamicillin, sold under the brand name Unasyn among others, is an oral form of the penicillin antibiotic combination ampicillin/sulbactam. It is used for the treatment of bacterial infections of the upper and lower respiratory tract, the kidneys and urinary tract, skin and soft tissues, among other organs. It contains esterified ampicillin and sulbactam.

<span class="mw-page-title-main">Avermectin</span> Drugs to treat parasitic worms and insect pests

The avermectins are a series of drugs and pesticides used to treat parasitic worms and insect pests. They are a group of 16-membered macrocyclic lactone derivatives with potent anthelmintic and insecticidal properties. These naturally occurring compounds are generated as fermentation products by Streptomyces avermitilis, a soil actinomycete. Eight different avermectins were isolated in four pairs of homologue compounds, with a major (a-component) and minor (b-component) component usually in ratios of 80:20 to 90:10. Other anthelmintics derived from the avermectins include ivermectin, selamectin, doramectin, eprinomectin, and abamectin.

<span class="mw-page-title-main">Spinosad</span> Chemical compound

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 aerial hyphae, with bead-like chains of spores enclosed in a characteristic hairy sheath. This genus is defined as aerobic, Gram-positive, nonacid-fast actinomycetes with fragmenting substrate mycelium. S. spinosa was isolated from soil collected inside a nonoperational sugar mill rum still in the Virgin Islands. Spinosad is a mixture of chemical compounds in the spinosyn family that has a generalized structure consisting of a unique tetracyclic ring system attached to an amino sugar (D-forosamine) and a neutral sugar (tri-Ο-methyl-L-rhamnose). Spinosad is relatively nonpolar and not easily dissolved in water.

The combination milbemycin oxime/lufenuron is a parasite control drug in which the active ingredient, milbemycin oxime, eliminates worms, while a second active ingredient, lufenuron, arrests the development of eggs and larvae, preventing them from maturing and continuing the infestation of an animal. This combination is registered for animal use only. To achieve efficacy, the treatment is administered once monthly, together with food, in a dosage suitable for the weight of the affected animal. The usual ratio is 500 μg milbemycin oxime and 10 mg lufenuron/kg body weight. Novartis indicates the proper dosage by color-coding the packages.

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.

Streptomyces isolates have yielded the majority of human, animal, and agricultural antibiotics, as well as a number of fundamental chemotherapy medicines. Streptomyces is the largest antibiotic-producing genus of Actinomycetota, producing chemotherapy, antibacterial, antifungal, antiparasitic drugs, and immunosuppressants. Streptomyces isolates are typically initiated with the aerial hyphal formation from the mycelium.

References

  1. 1 2 3 "Interceptor Flavor Tabs- milbemycin oxime tablet". DailyMed. Retrieved 4 August 2021.
  2. Mueller, R. S. (2012). "An update on the therapy of canine demodicosis". Compendium (Yardley, Pa). 34 (4): E1-4. PMID   22488596.
  3. Mehlhorn H (2008). Encyclopedia of Parasitology: A-M. Springer Science & Business Media. p. 646. ISBN   978-3-540-48994-8.
  4. "NADA 140-915 Interceptor – supplemental approval (September 9, 1996)". Food and Drug Administration .
  5. Roberts HE (2011). Fundamentals of Ornamental Fish Health. John Wiley & Sons. pp. 93–94. ISBN   978-1-119-94948-0.
  6. Lewbart GA (2011). Invertebrate Medicine. John Wiley & Sons. p. 71. ISBN   978-0-470-96078-3.