Avermectins
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Avermectins
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. Half of the 2015 Nobel Prize in Physiology or Medicine was awarded to William C. Campbell and Satoshi Ōmura for discovering avermectin, "the derivatives of which have radically lowered the incidence of river blindness and lymphatic filariasis, as well as showing efficacy against an expanding number of other parasitic diseases." History I ...
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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 infestations including head lice, scabies, river blindness (onchocerciasis), strongyloidiasis, trichuriasis, ascariasis and lymphatic filariasis. It works through many mechanisms to kill the targeted parasites, and can be taken orally, or applied to the skin for external infestations. It belongs to the avermectin family of medications. William Campbell and Satoshi Ōmura won the 2015 Nobel Prize in Physiology or Medicine for its discovery and applications. It is on the World Health Organization's List of Essential Medicines, and is approved by the U.S. Food and Drug Administration as an antiparasitic agent. In 2018, it was the 420th most commonly prescribed medication in the United States, with more than 100,000 prescriptions. It is availab ...
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Abamectin
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 (also called Avermectin B1), 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 (a and b) forms the bulk of the fermentation. The non proprietary name, abamectin, is a combination of Bla (~ 80%) and B1b (~ 20%). Out of all the Avermectins, abamectin is the only one that is used both in agriculture and pharmaceuticals. Mode of Action Avermectins bind to the glutamate-gated chloride channels that are found in invertebrate nerve and muscle cells. They cause hyperpolarization of these cells resulting in paralysis and death. Mammals only possess glutamate-gated chloride channels in the brain and spinal cord and as the Avermec ...
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Avermectin Skeletal
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. Half of the 2015 Nobel Prize in Physiology or Medicine was awarded to William C. Campbell and Satoshi Ōmura for discovering avermectin, "the derivatives of which have radically lowered the incidence of river blindness and lymphatic filariasis, as well as showing efficacy against an expanding number of other parasitic diseases." History I ...
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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 also be called vermifuges (those that stun) or vermicides (those that kill). Anthelmintics are used to treat people who are infected by helminths, a condition called helminthiasis. These drugs are also used to treat infected animals. Pills containing anthelmintics are used in mass deworming campaigns of school-aged children in many developing countries. The drugs of choice for soil-transmitted helminths are mebendazole and albendazole; for schistosomiasis and tapeworms it is praziquantel. Types Antiparasitics that specifically target worms of the genus ''Ascaris'' are called ascaricides. * Benzimidazoles: ** Albendazole – effective against threadworms, roundworms, whipworms, tapeworms, hookworms ** Mebendazole – effective against v ...
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Streptomyces Avermitilis
''Streptomyces avermitilis'' is a species of bacteria in the genus ''Streptomyces''. This bacterium was discovered by Satoshi Ōmura in Shizuoka Prefecture, Japan. The first complete genome sequence of ''S. avermitilis'' was completed in 2003. The genome consists of a single chromosome with a linear structure, unlike most bacterial genomes, which exist in the form of circular chromosomes. Avermectins are industrially produced from ''S. avermitilis''. Avermectin itself was discovered by the Satoshi Ōmura group and first disclosed in Burg ''et al.'' 1979. One of the most widely employed drugs against nematode and arthropod infestations is the avermectin derivative ivermectin, as well as abamectin, a widely used insecticide and antihelmintic. See also * List of Streptomyces species, List of ''Streptomyces'' species References External links *Type strain of ''Streptomyces avermitilis'' at Bac''Dive'' - the Bacterial Diversity Metadatabase
Streptomyces, avermitilis ...
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Merck Sharp And Dohme
Merck & Co., Inc. is an American multinational pharmaceutical company headquartered in Rahway, New Jersey, and is named for Merck Group, founded in Germany in 1668, of whom it was once the American arm. The company does business as Merck Sharp & Dohme or MSD outside the United States and Canada. Merck & Co. was originally established as the American affiliate of Merck Group in 1891. Merck develops and produces medicines, vaccines, biologic therapies and animal health products. It has multiple blockbuster drugs or products each with 2020 revenues including cancer immunotherapy, anti-diabetic medication and vaccines against HPV and chickenpox. The company is ranked 71st on the 2022 ''Fortune'' 500 and 87th on the 2022 ''Forbes'' Global 2000, both based on 2021 revenues. Products The company develops medicines, vaccines, biologic therapies and animal health products. In 2020, the company had 6 blockbuster drugs or products, each with over $1 billion in revenue: ''Keytruda'' (p ...
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Nematospiroides Dubius
''Heligmosomoides polygyrus'', previously named ''Nematospiroides dubius'', is a naturally occurring intestinal roundworm of rodents. It belongs to the family Trychostrongylidae, and male and female worms are morphologically distinguishable. The parasite has a direct lifecycle, with its larval form being the infective stage. ''H. polygyrus'' has the ability to establish chronic infections in rodents and alter host immune responses. This nematode is widely used as a gastrointestinal parasitic model in immunological, pharmacological, and toxicological studies. Lifecycle and morphology This parasite has a direct lifecycle with no intermediate hosts. The lifecycle takes about 13–15 days to complete. Infected mice pass faeces containing eggs, and egg sizes vary between 70 and 84 micrometres (µm) in length and 37 and 53 µm in width. Eggs are shed from the host at the 8– to 16-cell stage and hatch in the environment, roughly 24 hours after passing through the host. L1 larv ...
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Parenteral
A route of administration in pharmacology and toxicology is the way by which a drug, fluid, poison, or other substance is taken into the body. Routes of administration are generally classified by the location at which the substance is applied. Common examples include oral and intravenous administration. Routes can also be classified based on where the target of action is. Action may be topical (local), enteral (system-wide effect, but delivered through the gastrointestinal tract), or parenteral (systemic action, but delivered by routes other than the GI tract). Route of administration and dosage form are aspects of drug delivery. Classification Routes of administration are usually classified by application location (or exposition). The route or course the active substance takes from application location to the location where it has its target effect is usually rather a matter of pharmacokinetics (concerning the processes of uptake, distribution, and elimination of drugs). Exc ...
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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 inhabiting a broad range of environments. Less formally, they are categorized as Helminths, but are taxonomically classified along with Arthropod, arthropods, Tardigrade, tardigrades and other moulting animalia, animals in the clade Ecdysozoa, and unlike platyhelminthe, flatworms, have tubular digestion, digestive systems with openings at both ends. Like tardigrades, they have a reduced number of Hox genes, but their sister phylum Nematomorpha has kept the ancestral protostome Hox genotype, which shows that the reduction has occurred within the nematode phylum. Nematode species can be difficult to distinguish from one another. Consequently, estimates of the number of nematode species described to date vary by author and may change rapidly over ...
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Macrolide
The Macrolides are a class of natural products that consist of a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. The lactone rings are usually 14-, 15-, or 16-membered. Macrolides belong to the polyketide class of natural products. Some macrolides have antibiotic or antifungal activity and are used as pharmaceutical drugs. Rapamycin is also a macrolide and was originally developed as an antifungal, but is now used as an immunosuppressant drug and is being investigated as a potential longevity therapeutic. Macrolides are bacteriostatic in that they suppress or inhibit bacterial growth rather than killing bacteria completely. Definition In general, any macrocyclic lactone having greater than 8-membered rings are candidates for this class. The macrocycle may contain amino nitrogen, amide nitrogen (but should be differentiated from cyclopeptides), an oxazole ring, or a thiazole ring. Benzene rings are exclude ...
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Arthropod
Arthropods (, (gen. ποδός)) are invertebrate animals with an exoskeleton, a Segmentation (biology), segmented body, and paired jointed appendages. Arthropods form the phylum Arthropoda. They are distinguished by their jointed limbs and Arthropod cuticle, cuticle made of chitin, often Mineralization (biology), mineralised with calcium carbonate. The arthropod body plan consists of segments, each with a pair of appendages. Arthropods are bilaterally symmetrical and their body possesses an exoskeleton, external skeleton. In order to keep growing, they must go through stages of moulting, a process by which they shed their exoskeleton to reveal a new one. Some species have wings. They are an extremely diverse group, with up to 10 million species. The haemocoel, an arthropod's internal cavity, through which its haemolymph – analogue of blood – circulates, accommodates its interior Organ (anatomy), organs; it has an open circulatory system. Like their exteriors, the internal or ...
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Kitasato Institute
is a private medical university headquartered in Shirokane, Minato, Tokyo, Japan. The head of the university is on the Shirokane campus, neighboring the original Kitasato Institute, the first private medical research facility in Japan which was the starting point for the university in its present form. Kitasato University is ranked by Times Higher Education among the 350 best universities in Asia. History The school was named after Kitasato Shibasaburō. He was nominated for the Nobel Prize in Physiology or Medicine in 1901. The 2015 Nobel Prize in Physiology or Medicine was awarded to Satoshi Ōmura, a professor at Kitasato University. Organization Undergraduate schools * School of Pharmacy * School of Veterinary Medicine * School of Medicine * School of Marine Biosciences * School of Nursing * School of Science ** Department of Physics ** Department of Chemistry ** Department of Biological Sciences * School of Allied Health Sciences ** Department of Health Science ** Dep ...
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