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Ivermectin

Ivermectin is a semi-synthetic derivative of avermectins used to treat parasitic infections. It is active against many nematodes and some arthropods. Ivermectin causes muscle paralysis in invertebrates by activating ion channels. Resistance has emerged due to widespread veterinary use and reduced effectiveness has been seen in some regions.

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119 views1 page

Ivermectin

Ivermectin is a semi-synthetic derivative of avermectins used to treat parasitic infections. It is active against many nematodes and some arthropods. Ivermectin causes muscle paralysis in invertebrates by activating ion channels. Resistance has emerged due to widespread veterinary use and reduced effectiveness has been seen in some regions.

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Mano cempaka
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Ivermectin

Class:
Ivermectin is a semi-synthetic derivative of a family of macrocyclic lactones called
the avermectins
Antiparasitic Activity:
Ivermectin is active against most nematode parasites. It can also be used in the
treatment of arthropod ectoparasite infestations such as scabies. Its principal
indications are for treatment of onchocerciasis and strongyloidiasis. Additionally, it
shows useful activity against a number of other helminth parasites, particularly
Ascaris lumbricoides. A summary of the utility of ivermectin is shown in Table 1.
Mechanism of Action:
Ivermectin causes an influx of Cl- ions through the cell membrane of invertebrates by
activation of specific ivermectin-sensitive ion channels. The resultant
hyperpolarization leads to muscle paralysis.
Mechanisms of Resistance:
Widespread use of ivermectin for treatment of intestinal nematode infections of sheep
and goats has led to the development of drug resistance in veterinary practice. Reports
have emerged from West Africa pointing to a reduced effect of ivermectin in
onchocerciasis. Resistance may be associated with alterations in P-glycoprotein gene
expression.
Pharmacokinetics:
Ivermectin is rapidly absorbed with .Cmax is proportional to dose, with a value of
approximately 38-46 g/L reached after a therapeutic dose of 150-200 g/kg.
Estimates of the terminal half-life of the parent drug range from 28-56 hours.
Dosage:
Ivermectin is generally administered as a single dose of 150-200 g/kg.
Adverse Effects:
In the absence of parasitic infection, the adverse effects of ivermectin in therapeutic
doses are minimal. Adverse effects seen in filarial infections include fever, myalgia,
malaise, lightheadedness, and occasionally postural hypotension. In onchocerciasis,
skin oedema, pruritis and mild eye irritation may be seen.
Pregnancy:
While no adverse effects have been recorded in retrospective studies, administration
of the drug to pregnant women is not advised.
Drug Interactions:
None of any clinical significance has been reported.
Brand names/Manufacturer:
Mectizan, Stromectol (Merck).

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