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Ivermectin

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From Pharmacopedia
Ivermectin
Stromectol (oral, generic), Sklice (lice, topical), Soolantra (rosacea, topical 1%)

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Summary
Common uses
Strongyloidiasis0, Onchocerciasis (river blindness)0, Scabies (including crusted/Norwegian scabies)0, Head lice (topical Sklice)0, Inflammatory rosacea (topical Soolantra)0, Lymphatic filariasis (combination)0
Pharmacy
Starting dose
Strongyloides 200 mcg/kg PO single dose; scabies 200 mcg/kg PO repeated at 7-14 days; onchocerciasis 150 mcg/kg q6-12 months
Preparations
3 mg tablets (Stromectol); 0.5% topical lotion (Sklice); 1% topical cream (Soolantra)
US FDA Max
Single 200-400 mcg/kg per dose for systemic indications
Pharmacology
Routes
Oral, topical
Onset
Hours to days
Duration
Variable
Half-life
~16-18 hours[1]
Bioavailability
~60% (oral; substantially increased with high-fat meal)[1]
Pregnancy
Limited data; risk-benefit case by case; pregnancy is not a strict contraindication in WHO mass drug administration programs.[citation needed]
Legal status
Rx-only in US (the veterinary preparations are not for human use)
Purported mechanism
Ivermectin binds invertebrate glutamate-gated chloride channels (and to a lesser extent GABA-gated channels) in nerve and muscle cells of parasites, opening the channels and producing hyperpolarization and paralysis; mammalian neurons lack the equivalent channel, and P-glycoprotein at the mammalian blood-brain barrier excludes the drug from the CNS, accounting for the wide safety margin in humans.0 Substantially more concentrated topical formulations (Soolantra 1%) exploit local anti-inflammatory and antiparasitic effects against Demodex in rosacea. P-glycoprotein loss-of-function (rare in humans, common in some collie dog breeds) produces severe CNS toxicity[1].

References

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  1. 1.0 1.1 1.2 FDA Prescribing Information, Stromectol (ivermectin), Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/050742s026lbl.pdf