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Ivermectin
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| Systematic (IUPAC) name | |
| Ivermectin (22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b) | |
| Identifiers | |
| CAS number | 71827-03-7 |
| ATC code | P02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C48H74O14 (22,23-dihydroavermectin B=1a) C47H72O14 (22,23-dihydroavermectin B=1b) |
| Mol. mass | 875.10 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 93% |
| Metabolism | liver; CYP450 |
| Half life | 18 hours |
| Excretion | feces; <1% urine |
| Therapeutic considerations | |
| Pregnancy cat. |
C |
| Legal status | |
| Routes | Oral |
Ivermectin (22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b) is a broad-spectrum antiparasitic medication, traditionally used against worms (except tapeworms), but more recently found to be effective against most mites and some lice too. It is sold under brand names Stromectol in the United States, Mectizan in Canada by Merck and Ivexterm in Mexico by Valeant Pharmaceuticals International. Mectizan is currently being used to help eliminate river blindness (onchocerciasis) in the Americas and stop transmission of lymphatic filariasis around the world.[1] [2]
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Ivermectin and the related molecule avermectin (an insecticide most frequently used in home-use ant baits) are macrocyclic lactones derived from the bacterium Streptomyces avermitilis. Ivermectin kills by interfering with nervous system and muscle function, in particular by enhancing inhibitory neurotransmission. The drug binds and activates glutamate-gated chloride channels (GluCls) present in neurons and myocytes (Cully et al., 1994; Cully et al., 1997, Dent et al., 1997), resulting in neuro-muscular paralysis and death.
Ivermectin can be given either per os or parenterally. It does not readily cross the blood-brain barrier of mammals (Schinkle et al., 1994), although crossing may still become significant if ivermectin is given at high doses (in which case, brain levels peak 2-5 hours after administration).
The main concern is neurotoxicity, which in most mammalian species may manifest as CNS depression, and consequent ataxia, as might be expected from potentiation of inhibitory GABA-ergic synapses
Ivermectin is a broad-spectrum antiparasitic agent. It is mainly used in humans in the treatment of onchocerciasis, but is also effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis and enterobiasis). More recent evidence supports its off-label use in the treatment of mites such as scabies, usually limited to cases that prove resistant to topical treatments and/or who present in advanced state (such as Norwegian scabies).
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