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QuickView for ivermectin (compound)
PubChem
| Name: | Ivermectin |
|---|---|
| PubChem Compound ID: | 11957587 |
| Description: | A mixture of mostly avermectin H2B1a (RN 71827-03-7) with some avermectin H2B1b (RN 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. It binds glutamate-gated chloride channel to cause increased permeability and hyperpolarization of nerve and muscle cells. It also interacts with other CHLORIDE CHANNELS. It is a broad spectrum antiparasitic that is active against microfilariae of ONCHOCERCA VOLVULUS but not the adult form. |
| Molecular formula: | C48H74O14 |
| Molecular weight: | 875.093 g/mol |
| Synonyms: |
EU-0100693
|
DrugBank
Identification
| Name: | Ivermectin |
|---|---|
| Name (isomeric): | DB00602 |
| Drug Type: | small molecule |
| Description: | A mixture of mostly avermectin H2B1a (RN 71827-03-7) with some avermectin H2B1b (RN 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. It binds glutamate-gated chloride channel to cause increased permeability and hyperpolarization of nerve and muscle cells. It also interacts with other CHLORIDE CHANNELS. It is a broad spectrum antiparasitic that is active against microfilariae of ONCHOCERCA VOLVULUS but not the adult form. |
| Synonyms: |
22,23-Dihyroavermectin B1; 22,23-Dihydroxy-avermectin B; 5-O-demethyl-22,23-dihydro-avermectin A1a
|
| Brand: | Ivermectin B1, Ivermectin-luminol, Sklice, Stromectol, Mectizan |
| Brand name mixture: | Heel 170 Tab(Calcium Iodide + Fucus Vesiculosus + Ivermectin B1b + Silicon Dioxide) |
| Category: | Antiprotozoal Agents, Anthelmintics, Antinematodal Agents |
| CAS number: | 70288-86-7 |
Pharmacology
| Indication: | For the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite <i>Strongyloides stercoralis</i>. Also for the treatment of onchocerciasis (river blindness) due to the nematode parasite <i>Onchocerca volvulus</i>. Can be used to treat scabies caused by <i>Sarcoptes scabiei</i>. |
|---|---|
| Pharmacology: |
Ivermectin is a semisynthetic, anthelminitic agent. It is an avermectin which a group of pentacyclic sixteen-membered lactone (i.e. a macrocyclic lactone disaccharide) derived from the soil bacterium Streptomyces avermitilis. Avermectins are potent anti-parasitic agents. Ivermectin is the most common avermectin. It is a broad spectrum antiparasitic...
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| Mechanism of Action: |
Ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria. This binding causes an increase in the permeability of the cell membrane to chloride ions and results in hyperpolarization of the cell, leading to paralysis and death of the parasite. Ivermectin al...
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| Absorption: | Moderately well absorbed. Improved absorption with high fat meal. |
| Protein binding: | 93% |
| Biotransformation: | Primarily hepatic. Ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1 % of the administered dose excreted in the urine. |
| Route of elimination: | Ivermectin is metabolized in the liver, and ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine. |
| Half Life: | 16 hours (also reported at 22-28 hours) |
| Toxicity: | LD50 = 29.5 mg/kg (Mouse, oral). LD50 = 10 mg/kg (Rat, oral). Adverse effects include muscle or joint pain, dizziness, fever, headache, skin rash, fast heartbeat. |
| Affected organisms: | Head lice||Parasitic nematodes and other roundworms |
Targets
Enzymes
Transporters
