Ivermectin

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Ivermectin

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Catalog Number	PR70288867
CAS	70288-86-7
Description	Ivermectin is an antiinfective agent with activity against several parasitic nematodes and scabies and is the treatment of choice for onchocerciasis (river blindness). It is typically given as one or two oral doses. Ivermectin therapy has been associated with minor, self-limiting serum aminotransferase elevations and very rare instances of clinically apparent liver injury.
Synonyms	Ivermectin B1a
Molecular Weight	875.1
Molecular Formula	C48H74O14
InChI	AZSNMRSAGSSBNP-XPNPUAGNSA-N
InChI Key	InChI=1S/C48H74O14/c1-11-25(2)43-28(5)17-18-47(62-43)23-34-20-33(61-47)16-15-27(4)42(26(3)13-12-14-32-24-55-45-40(49)29(6)19-35(46(51)58-34)48(32,45)52)59-39-22-37(54-10)44(31(8)57-39)60-38-21-36(53-9)41(50)30(7)56-38/h12-15,19,25-26,28,30-31,33-45,49-50,52H,11,16-18,20-24H2,1-10H3/b13-12+,27-15+,32-14+/t25-,26-,28-,30-,31-,33+,34-,35-,36-,37-,38-,39-,40+,41-,42-,43+,44-,45+,47+,48+/m0/s1
Drug Categories	Agents Causing Muscle Toxicity; Agrochemicals; Anthelmintics; Anti-Infective Agents; Antinematodal Agents; Antiparasitic Agents; Antiparasitic Products, Insecticides and Repellents; Avermectines; BCRP/ABCG2 Substrates; Compounds used in a research, industrial, or household setting; Cytochrome P-450 CYP2D6 Substrates; Cytochrome P-450 CYP2E1 Substrates; Cytochrome P-450 CYP3A Substrates; Cytochrome P-450 CYP3A4 Substrates; Cytochrome P-450 Substrates; Dermatologicals; Insecticides; Lactones; OATP1B1/SLCO1B1 Inhibitors; OATP1B3 inhibitors; P-glycoprotein inducers; P-glycoprotein inhibitors; P-glycoprotein substrates; Pediculicides; Pesticides; Polyketides; Scabicides and Pediculicides; Toxic Actions
Drug Interactions	Abametapir-The serum concentration of Ivermectin can be increased when it is combined with Abametapir. Abemaciclib-Abemaciclib may decrease the excretion rate of Ivermectin which could result in a higher serum level. Acenocoumarol-Ivermectin may increase the anticoagulant activities of Acenocoumarol. Acipimox-The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Acipimox. Afatinib-Afatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Half-Life	Following oral administration, the half-life of ivermectin is approximately 18 hours.
Isomeric SMILES	CC[C@H](C)[C@@H]1[C@H](CC[C@@]2(O1)C[C@@H]3C[C@H](O2)C/C=C(/[C@H]([C@H](/C=C/C=C/4\CO[C@H]5[C@@]4([C@@H](C=C([C@H]5O)C)C(=O)O3)O)C)O[C@H]6C[C@@H]([C@H]([C@@H](O6)C)O[C@H]7C[C@@H]([C@H]([C@@H](O7)C)O)OC)OC)\C)C
Type	Small Molecule
Therapeutic Category	Antihelmintics

Pharmacology

Indications

Ivermectin is available in various formulations and serves multiple therapeutic purposes. Topically applied ivermectin cream is approved for managing·h rosacea. Additionally, an over-the-counter ivermectin lotion is available for topical use in treating·head lice infestations in patients aged six months and older. Orally administered ivermectin serves as a broad-spectrum antiparasitic agent and is used to treat intestinal strong·hocerciasis caused by Onchocerca volvulus. Internationally, systemic ivermectin is utilized in addressing·hers.

Pharmacodynamics

Ivermectin is a semisynthetic anthelmintic compound that belong·he avermectin class. Avermectins are a group of pentacyclic sixteen-membered lactones, specifically macrocyclic lactone disaccharides, derived from the soil bacterium Streptomyces avermitilis. These compounds are renowned for their potent and broad-spectrum antiparasitic efficacy.

Absorption

Ivermectin demonstrates moderate absorption when administered. Its absorption profile improves notably with the intake of a high-fat meal, indicating·hat dietary factors can influence its pharmacokinetic properties.

Metabolism

Ivermectin undergoes primary metabolism in the liver. The drug, along·h its metabolites, is predominantly excreted in the feces over approximately 12 days, with less than 1% of the administered dose being·hrough urine. This elimination pattern underscores the compound's hepatic metabolic processing·hway.

Mechanism of Action

Ivermectin operates by selectively binding to glutamate-gated chloride ion channels found in the muscle and nerve cells of invertebrates, specifically targeting the microfilaria. This interaction significantly increases the permeability of the cell membrane to chloride ions, resulting in hyperpolarization. As a consequence, the parasite experiences paralysis and ultimately dies. Furthermore, Ivermectin acts as an agonist for gamma-aminobutyric acid (GABA), interfering with GABA-mediated neurosynaptic transmission within the central nervous system. Additionally, Ivermectin may hinder the normal intrauterine development of Onchocerca volvulus microfilariae and inhibit their release from the uteri of gravid female worms.

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