Difference between revisions of "Macrocyclic Lactones"
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+ | |sublink1 = Anthelmintic 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. | ||
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==Safety== | ==Safety== | ||
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Revision as of 12:06, 3 November 2008
This article is still under construction. |
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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.
Activity
- They have a wide spectrum of activity. They are endectocides; active against common nematodes at all developmental stages and against many arthropods.
- 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.
Pharmacokinetics
- These drugs are excreted very slowly and so the plasma concentration curve has a very long tail.