Ivermectin
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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 QP54 QS02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C48H74O14 (22,23-dihydroavermectin B1a) C47H72O14 (22,23-dihydroavermectin B1b) |
| 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. | |
| Legal status | |
| Routes | Oral |
Ivermectin (22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b) is a broad-spectrum antiparasitic medication.
It is sold under brand names Stromectol in the United States, Mectizan in Canada by Merck and Ivexterm in Mexico by Valeant Pharmaceuticals International.
Contents |
[edit] Uses
It is traditionally used against worms, but more recently found to be effective against mites[1][2][3] and some lice too.[4][5]
Mectizan is currently being used to help eliminate river blindness (onchocerciasis) in the Americas and stop transmission of lymphatic filariasis around the world.[6] [7] Currently, large amounts of Mectizan are donated by Merck to fight river blindness in countries that are unable to afford the drug [8].
[edit] Veterinary use
Ivermectin is also used in veterinary medicine, particularly for horses and dogs. It is sometimes mixed with other medications to reach a wide spectrum of animal parasites.
[edit] Pharmacodynamics
Ivermectin and the related 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)[9]. GluCls are invertebrate-specific members of the Cys-loop family of ligand-gated ion channels present in neurons and myocytes.
[edit] Pharmacokinetics
Ivermectin can be given either per os or parenterally. It does not readily cross the blood-brain barrier of mammals,[citation needed] although crossing may still become significant if ivermectin is given at high doses (in which case, brain levels peak 2-5 hours after administration).
[edit] Toxicity
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
[edit] Ecotoxicity
Field studies have demonstrated that the dung of animals treated with ivermectin supports a significantly reduced diversity of invertebrates, and that the dung persists for longer.[10]
[edit] Indications for use
[edit] Humans
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,[3] usually limited to cases that prove resistant to topical treatments and/or who present in advanced state (such as Norwegian scabies).
[edit] References
- ^ Brooks PA, Grace RF (August 2002). "Ivermectin is better than benzyl benzoate for childhood scabies in developing countries". J Paediatr Child Health 38 (4): 401–4. doi:. PMID 12174005. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=1034-4810&date=2002&volume=38&issue=4&spage=401.
- ^ Victoria J, Trujillo R (2001). "Topical ivermectin: a new successful treatment for scabies". Pediatr Dermatol 18 (1): 63–5. doi:. PMID 11207977. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0736-8046&date=2001&volume=18&issue=1&spage=63.
- ^ a b Strong M, Johnstone PW (2007). "Interventions for treating scabies". Cochrane Database of Systematic Reviews (Online) (3): CD000320. doi:. PMID 17636630.
- ^ Dourmishev AL, Dourmishev LA, Schwartz RA (December 2005). "Ivermectin: pharmacology and application in dermatology". International Journal of Dermatology 44 (12): 981–8. doi:. PMID 16409259.
- ^ Strycharz JP, Yoon KS, Clark JM (January 2008). "A new ivermectin formulation topically kills permethrin-resistant human head lice (Anoplura: Pediculidae)". Journal of Medical Entomology 45 (1): 75–81. doi:. PMID 18283945.
- ^ The Carter Center, "River Blindness (Onchocerciasis) Program", http://www.cartercenter.org/health/river_blindness/index.html, retrieved on 2008-07-17
- ^ The Carter Center, "Lymphatic Filariasis Elimination Program", http://www.cartercenter.org/health/lf/index.html, retrieved on 2008-07-17
- ^ http://www.mectizan.org/about.asp
- ^ Yates DM, Wolstenholme AJ (August 2004). "An ivermectin-sensitive glutamate-gated chloride channel subunit from Dirofilaria immitis". Int. J. Parasitol. 34 (9): 1075–81. doi:. PMID 15313134. http://linkinghub.elsevier.com/retrieve/pii/S0020751904000979.
- ^ Iglesias LE, Saumell CA, Fernández AS, et al. (December 2006). "Environmental impact of ivermectin excreted by cattle treated in autumn on dung fauna and degradation of faeces on pasture". Parasitology Research 100 (1): 93–102. doi:. PMID 16821034.
[edit] See also
[edit] External links
- Stromectol
- The Carter Center River Blindness (Onchocerciasis) Control Program
- Mectizan Donation Program
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