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| + | ==Introduction== |
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| − | |sublink1 = Anthelmintic Drugs
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| − | |subtext1 = Anthelmintic Drugs
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| − | |pagetype = Drugs
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| | This group of drugs are derived from ''Streptomyces'' species and are coded as '''3-AV''' products. They are commonly known as '''avermectins''' and '''milbemycins'''. Drugs in use include; '''ivermectin, abamectin, doramectin, moxidectin, eprinomectin''' and '''selamectin'''. | | This group of drugs are derived from ''Streptomyces'' species and are coded as '''3-AV''' products. They are commonly known as '''avermectins''' and '''milbemycins'''. Drugs in use include; '''ivermectin, abamectin, doramectin, moxidectin, eprinomectin''' and '''selamectin'''. |
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| | ==Activity== | | ==Activity== |
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| | * They are inactive against trematodes, cestodes and adult filarial worms. Though are active against migrating heart worm larvae and are used as heartworm prophylactics in cats and dogs. | | * They are inactive against trematodes, cestodes and adult filarial worms. Though are active against migrating heart worm larvae and are used as heartworm prophylactics in cats and dogs. |
| | * Their mode of action is by opening invertebrate specific glutamate-gated chloride channels on the post-synaptic membranes. This results in '''flaccid paralysis''' of the parasite. | | * Their mode of action is by opening invertebrate specific glutamate-gated chloride channels on the post-synaptic membranes. This results in '''flaccid paralysis''' of the parasite. |
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| | ==Pharmacokinetics== | | ==Pharmacokinetics== |
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| | * These drugs are excreted very slowly and so the plasma concentration curve has a very long tail. | | * These drugs are excreted very slowly and so the plasma concentration curve has a very long tail. |
| | * The initial peak will kill all adult worms and the residual "tail" is able to have a high enough concentration to ensure that infective larvae ingested, for a time after treatment, are incapable of establishing. This provides a '''period of protection against reinfection'''. | | * The initial peak will kill all adult worms and the residual "tail" is able to have a high enough concentration to ensure that infective larvae ingested, for a time after treatment, are incapable of establishing. This provides a '''period of protection against reinfection'''. |
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| | ==Safety== | | ==Safety== |
| | + | * These are on the whole safe drugs to use. |
| | + | * But '''Collie type breeds''' of dogs, especially '''Rough Coated Collies''' can be fatal. This is because they can lack a efflux transporter protein that removes these drugs from the CNS. This means toxic concentrations are capable of accumulating. |
| | + | * This can also occur when Ivermectin is used at the higher doses needed for some heartworm therapies. |
| | + | * They are often in high concentrations in faeces, this means that bettles and other insects that use dung-pats for their development can be killed. This is currently a heated topic, especially in areas of a delicate ecosystem. |