Difference between revisions of "Ivermectin"

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It is mainly used in humans in the treatment of [[onchocerciasis]], but is also effective against other worm infestations (such as [[strongyloidiasis]], [[ascariasis]], [[trichuriasis]], [[filariasis]] and [[enterobiasis]]).  
 
It is mainly used in humans in the treatment of [[onchocerciasis]], but is also effective against other worm infestations (such as [[strongyloidiasis]], [[ascariasis]], [[trichuriasis]], [[filariasis]] and [[enterobiasis]]).  
  
−
Ivermectin, under the brand name Mectizan, is currently being used to help eliminate [[river blindness]] (onchocerciasis) in the [[Americas]] and stop [[transmission (medicine)|transmission]] of [[lymphatic filariasis]] and onchocerciasis around the world.<ref name="RBP">{{Citation | author= The Carter Center| title="River Blindness (Onchocerciasis) Program"|url=http://www.cartercenter.org/health/river_blindness/index.html|accessdate=2008-07-17}}</ref><ref name="LFEP">{{Citation | author= The Carter Center| title="Lymphatic Filariasis Elimination Program"|url=http://www.cartercenter.org/health/lf/index.html|accessdate=2008-07-17}}</ref><ref name="APOC">{{Citation | author= WHO|title="African Programme for Onchocerciasis Control" |http://www.who.int/blindness/partnerships/APOC/en/ accessdate=2009-11-12}}</ref> Currently, large amounts of Ivermectin are donated by [[Merck & Co.|Merck]] to fight river blindness in countries that are unable to afford the drug <ref>http://www.mectizan.org/about.asp</ref>. The disease is endemic in 30 African countries, 6 Latin American countries and Yemen, according to studies conducted by the World Health Organization.<ref name="UFAR">{{Citation | author= United Front Against Riverblindness| title="Riverblindness"|url=http://www.riverblindness.org/index.php?menu=tn2&page=aboutRiverblindness}}</ref> The drug rapidly kills microfilariae but not the adult worms. A single oral dose of ivermectin, taken annually for the 10-15 year life span of the adult worms, is all that is needed to protect the individual from onchocerciasis.<ref name="UFAR Treatment">{{Citation|author= United Front Against Riverblindness| title="Riverblindness"|url=http://www.riverblindness.org/index.php?menu=tn3&page=Treatment}}</ref>
+
Ivermectin, under the brand name Mectizan, is currently being used to help eliminate [[river blindness]] (onchocerciasis) in the [[Americas]] and stop [[transmission (medicine)|transmission]] of [[lymphatic filariasis]] and onchocerciasis around the world.<ref name="RBP">{{Cite web | author= The Carter Center| title="River Blindness (Onchocerciasis) Program"|url=http://www.cartercenter.org/health/river_blindness/index.html|accessdate=2008-07-17 | postscript= <!--None-->}}</ref><ref name="LFEP">{{Cite web | author= The Carter Center| title="Lymphatic Filariasis Elimination Program"|url=http://www.cartercenter.org/health/lf/index.html|accessdate=2008-07-17 | postscript= <!--None-->}}</ref><ref name="APOC">{{Cite web | author= WHO|title="African Programme for Onchocerciasis Control" | url= http://www.who.int/blindness/partnerships/APOC/en/ accessdate=2009-11-12 | postscript= <!--None-->}}</ref> Currently, large amounts of ivermectin are donated by [[Merck & Co.|Merck]] to fight river blindness in countries that are unable to afford the drug <ref>http://www.mectizan.org/about.asp</ref>. The disease is endemic in 30 African countries, 6 Latin American countries and Yemen, according to studies conducted by the World Health Organization.<ref name="UFAR">{{Cite web | author= United Front Against Riverblindness| title="Riverblindness"|url=http://www.riverblindness.org/index.php?menu=tn2&page=aboutRiverblindness | postscript= <!--None-->}}</ref> The drug rapidly kills microfilariae, but not the adult worms. A single oral dose of ivermectin, taken annually for the 10-15 year life span of the adult worms, is all that is needed to protect the individual from onchocerciasis.<ref name="UFAR Treatment">{{Cite web|author= United Front Against Riverblindness| title="Riverblindness"|url=http://www.riverblindness.org/index.php?menu=tn3&page=Treatment|postscript= <!--None-->}}</ref>
  
 
===Arthropod===
 
===Arthropod===
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===Veterinary use===
 
===Veterinary use===
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Ivermectin is also used in veterinary medicine, particularly for [[horse]]s, [[dog]]s and [[cat]]s. It is sometimes mixed with other medications to reach a wide spectrum of animal parasites. Some breeds (especially the [[Rough Collie]], the [[Smooth Collie]] and the [[Australian Shepherd]]) are affected by a genetic defect, a mutation within the MDR1 gene. Affected dogs are very sensitive to some drugs, such as Ivermectin, as well as to some antibiotics, opioids and steroids – over 100 drugs in total. Kittens are also very sensitive and ivermectin should never be used on kittens less than 10-12 weeks of age. Nor should it be used on any weak, dehydrated or debilitated animal except in dire situations. {{Citation needed|date=February 2010}}
+
Ivermectin is also used in veterinary medicine, particularly for [[horse]]s, [[dog]]s and [[cat]]s. It is sometimes mixed with other medications to reach a wide spectrum of animal parasites. Some breeds (especially the [[Rough Collie]], the [[Smooth Collie]] and the [[Australian Shepherd]]) are affected by a genetic defect, a mutation within the MDR1 gene. Affected dogs are very sensitive to some drugs, such as ivermectin, as well as to some antibiotics, opioids and steroids – over 100 drugs in total. Kittens are also very sensitive and ivermectin should never be used on kittens less than 10-12 weeks of age, nor should it be used on any weak, dehydrated or debilitated animal except in dire situations. {{Citation needed|date=February 2010}}
 +
Ivermectin is sometimes used as an acaricide in reptiles, both by injection and as a diluted spray. While this works really well in some cases, care must be taken as several species of reptile are very sensitive to ivermectin. Use in Chelonians is particularly contra-indicated, because it is nearly often fatal.
  
 
==Pharmacodynamics==
 
==Pharmacodynamics==
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Ivermectin can be given either by mouth or injection. It does not readily cross the [[blood-brain barrier]] of [[mammal]]s,{{Citation needed|date=March 2009}} although crossing may still become significant if ivermectin is given at high doses (in which case, brain levels peak 2–5 hours after administration).
 
Ivermectin can be given either by mouth or injection. It does not readily cross the [[blood-brain barrier]] of [[mammal]]s,{{Citation needed|date=March 2009}} although crossing may still become significant if ivermectin is given at high doses (in which case, brain levels peak 2–5 hours after administration).
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In contrast to mammals Ivermectin can cross the blood-brain barrier in tortoises, with often fatal consequences.
  
 
==Toxicity==
 
==Toxicity==

Latest revision as of 15:41, 27 September 2010

Ivermectin
File:Ivermectin skeletal.svg
Systematic (IUPAC) name
Ivermectin (22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b)
Clinical data
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
administration		 Oral
Pharmacokinetic data
Protein binding 93%
Metabolism liver; CYP450
Biological half-life 18 hours
Excretion feces; <1% urine
Identifiers
CAS Number 70288-86-7 71827-03-7
ATC code P02CF01 (WHO) QP54AA01 QS02QA03
PubChem CID 6474909
DrugBank APRD01058
Chemical data
Formula C48H74O14 (22,23-dihydroavermectin B1a)
C47H72O14 (22,23-dihydroavermectin B1b)
Molar mass 875.10 g/mol
Script error: No such module "TemplatePar".Expression error: Unexpected < operator.

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.

Uses

Ivermectin is a broad-spectrum antiparasitic agent.

Helminth

It is traditionally used against worms.

It is mainly used in humans in the treatment of onchocerciasis, but is also effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis, filariasis and enterobiasis).

Ivermectin, under the brand name Mectizan, is currently being used to help eliminate river blindness (onchocerciasis) in the Americas and stop transmission of lymphatic filariasis and onchocerciasis around the world.[1][2][3] Currently, large amounts of ivermectin are donated by Merck to fight river blindness in countries that are unable to afford the drug [4]. The disease is endemic in 30 African countries, 6 Latin American countries and Yemen, according to studies conducted by the World Health Organization.[5] The drug rapidly kills microfilariae, but not the adult worms. A single oral dose of ivermectin, taken annually for the 10-15 year life span of the adult worms, is all that is needed to protect the individual from onchocerciasis.[6]

Arthropod

More recent evidence supports its off-label use against arthropods:

Veterinary use

Ivermectin is also used in veterinary medicine, particularly for horses, dogs and cats. It is sometimes mixed with other medications to reach a wide spectrum of animal parasites. Some breeds (especially the Rough Collie, the Smooth Collie and the Australian Shepherd) are affected by a genetic defect, a mutation within the MDR1 gene. Affected dogs are very sensitive to some drugs, such as ivermectin, as well as to some antibiotics, opioids and steroids – over 100 drugs in total. Kittens are also very sensitive and ivermectin should never be used on kittens less than 10-12 weeks of age, nor should it be used on any weak, dehydrated or debilitated animal except in dire situations.[citation needed] Ivermectin is sometimes used as an acaricide in reptiles, both by injection and as a diluted spray. While this works really well in some cases, care must be taken as several species of reptile are very sensitive to ivermectin. Use in Chelonians is particularly contra-indicated, because it is nearly often fatal.

Pharmacodynamics

Ivermectin and other avermectins (insecticides 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)[12]. GluCls are invertebrate-specific members of the Cys-loop family of ligand-gated ion channels present in neurons and myocytes.

Pharmacokinetics

Ivermectin can be given either by mouth or injection. 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). In contrast to mammals Ivermectin can cross the blood-brain barrier in tortoises, with often fatal consequences.

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. Dogs with defects in the P-glycoprotein gene can be severely poisoned by ivermectin.

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.[13]

See also

References

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Use <references />, or <references group="..." />

External links

Antiplatyhelmintic agents
Binds tubulin
Other/unknown
Binds tubulin
Other/unknown
Antinematodal agents
(including
macrofilaricides)
Binds tubulin
macrolide (Ivermectin#)
Other/unknown
Insecticide/pediculicide
Chlorine-containing products
Ivermectin
Acaricide/miticide/scabicide
Ivermectin
Sulfur-containing products
Chlorine-containing products
Other/ungrouped
cs:Ivermektin

de:Ivermectin es:Ivermectina fr:Ivermectine nl:Ivermectine ja:イベルメクチン pt:Ivermectina zh:伊維菌素

it:Ivermectina
  1. ↑ The Carter Center. ""River Blindness (Onchocerciasis) Program"". Retrieved 2008-07-17. 
  2. ↑ The Carter Center. ""Lymphatic Filariasis Elimination Program"". Retrieved 2008-07-17. 
  3. ↑ WHO. accessdate=2009-11-12 ""African Programme for Onchocerciasis Control"" Check |url= value (help). 
  4. ↑ http://www.mectizan.org/about.asp
  5. ↑ United Front Against Riverblindness. ""Riverblindness"". 
  6. ↑ United Front Against Riverblindness. ""Riverblindness"". 
  7. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  8. ↑ Victoria J, Trujillo R (2001). "Topical ivermectin: a new successful treatment for scabies". Pediatr Dermatol. 18 (1): 63–5. doi:10.1046/j.1525-1470.2001.018001063.x. PMID 11207977. 
  9. ↑ 9.0 9.1 Strong M, Johnstone PW (2007). "Interventions for treating scabies". Cochrane Database of Systematic Reviews (Online) (3): CD000320. doi:10.1002/14651858.CD000320.pub2. PMID 17636630. 
  10. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  11. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  12. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  13. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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