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antifungal and antiprotozoal agents
(better to refer to caleb's…
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drugs against roundworm, strongyloidiasis and scabies
albendazole
MOA: inhibits microtubule functions of parasites through inhibition of polymerization of β-tubulin into microtubules followed by disruption of glucose uptake and transport which can lead to the eventual death of the helminths.
clinical indication:
- broad range of activity against helminthic infections
- neurocysticercosis (caused by tapeworm), ascariasis, hookworm, pinworm, and
whipworm infections and an alternative drug for treatment of threadworm infections
Pharmacokinetics
- Oral administration
- Absorption is improved when given with a fatty
meal when used against tissue parasites.
Adverse Effects
- GI symptoms
- Elevated liver enzymes
ivermectin
MOA: probably binds to glutamate-activated Cl− channels found in nematode nerve or muscle cells and causes hyperpolarization by increasing intracellular chloride concentration, resulting in paralysis.
- resistance might be due to lack of high-affinity avermectin receptors in cestodes and trematodes
may explain why these helminths are not sensitive to ivermectin
Clinical indication:
- Strongyloides stercoralis, which causes strongyloidiasis
- Onchocerca volvulus, which causes Onchocerciasis (river blindness) (tissue nematode)
- Scabies
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adverse effects
- generally well tolerated
- pregnancy --> not safe for use
permethrin
MOA: It impairs the function of voltage-gated sodium channels in the mites, leading to
disruption of neurotransmission and paralysis
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Administration
For scabies - treatment with permethrin consists of a single application from the neck down for 8–12 hours then washed off, repeated in 1 week. Patients often continue to itch for several weeks after treatment
Pharmacokinetics
- < than 2% is absorbed via the skin
- Well absorbed and extensively metabolized by
hepatic CYP3A4 enzymes
adverse effects
- Pruritus
- Safe for use in infants as young as two months of age, children, adults, and pregnant
or lactating individuals