Anti-Helminths Flashcards
Typical targets for drugs
Metabolic energy production
Cytoskeletal filament proteins
Motor/motility activity
Which two drugs cause flaccid paralysis
Ivermectin
DEC
Which two drugs cause spastic paralysis
PP
Praziquantel
Difference between mebendazole and albendazole
Mebendazole: NOT GI absorbed (lumen infections)
Albendazole: GI absorbed, for systemic infections
Benzimidazoles
Mebendazole, albendazole Use: nematodes and lymphatic filariasis MOA: binds B tubular to inhib MT polymerization AE: GI, BM suppression Contra: pregnant and kids <2
Resistance against benzimidazoles
Switch B tubular isotope from 1 -> 2 at position 200
Ivermectin
Use: nematodes, river blindness, elephant
MOA: activates glutamate-gated Cl channels -> flaccid paralysis
AE: Mazzotti
Contra: loiasis, impaired BBB
What is a Mazzotti like reaction
Caused by dying microfilarie
Itching, swollen LN, HA, dizziness, fever, tachycardia
Tx: aspirin, antihistamines, steroids
What is loiasis
Eye worm dz via deer flies
Leads to life threatening encephalopathy
How does resistance develop against Ivermectin
upreg p-glycoprotein transport for efflux
Mutation in Cl channel
Doxycycline
Kills Wolbachia and causes sterility in female adult worms
DEC
Use: loiasis, elephant
Only available from CDC
MOA: stim host immune response, platelet aggregation
AE: rare, Mazzotti, alkaline urine prolongs t1/2
Contra: onchocerciasis
Pyrantel Pamoate
MOA: depolarizing NM blocker -> spastic paralysis
AE: GI, HA, NM blockade at high dose
Praziquantel
Use: schistomiasis, ineffective against nematodes
MOA: inc membrane perm to Ca -> spastic paralysis
AE: GI disturbance, HA, CYP
Contra: intraocular cysticercosis (pork tapeworm in eye)
