Antiparasitics Flashcards
Pentamidine
DNA minor groove binder forming tight DNA complex. It is used in early african trypanosomiasis before CNS involvement. It does not cross BBB GIVen by IM injection.
Suramin
induces oxidative stress due to inhiition of NADP H dependant dehydrogenases with subsequent impairment of mitochondrial membrane potential. Does not cross BBB, but is absorbed by the gut. very toxic. african trypanosomiasis
Melarsoprol
MOA not understood. It is the only option for trypanosomiasisthat has progressed to CNS for T. brucei rhodesiense. It is lipid soluble and crsosses the BBB, but must be disolved in propylene glycol wich is irritating. It is very toxic including encephalopathy, fever, hypertension, vomiting, and half which get the encephalopathy die of it. african trypanosomiasis
Eflornithine
Inhibits ornithine decarboxylase which turns over faster in humans. Is able to cross the BBB, stage 2 treatment. infuse over 14 days due to poor absorbtion and rapid excretion in the urine. It is trypanostatic. It is toxic but not as bad as melarsoprol. african trypanosomiasis
Best option for late stage african trypanosomia
Eflornithine and nifurtimox
Sodium stibogluconate
Interferes with glycolysis and FA beta oxidation in leishmania, and likely additional mechanisms. Toxicity builds up over time. Used to treat Leishmania.
Meglumine antimoniate
Interferes with glycolysis and FA beta oxidation in leishmania, and likely additional mechanisms. Toxicity builds up over time. Used to treat Leishmania.
Miltefosine
Unknown MOA, vomiting and diarrhea in up to 60% of patients. treates Leishmania
Treatments for Toxoplasama Gondii
Most patients recover on their own and are likekly asymptomatic. Pregnant women, newborns and infant, immunocompromised and individuals with occular toxoplasmosis get drugs. Can traet withsulfadiazine and pyrimethamine. antimalarial, folinic acid is often coadministered for specificity so T. gondii cannot utilize presynthesized folinic acid, macrolide inhibits mitochondrial fxn.
Treatments for Naegleria fowleri
Amphoteracin B, rifampicin, miconazole, dexamethazone, sulfisoxazole, pheytoin. Maybe also miltefosine too.
Naegleria fowleri
Thermophilic freshwater ameba can consume neural tissue and lead to meningitis. Enters our body via mucous layers and sx begin 5 days after infection. Initial headache, nausea fever vomiting and eventual stiff neck, confusion, balance and seizures, hallucinations.
Toxoplasma gondii
Obtain it by cysts in uncooked meat, oocysts on unwashed produce and cat shit.. Disease state is toxoplasmosis which entails fever, confusion, headache, seizures, nausea, poor coordination from cerebral abscesses.
Leischmania spp.
a type of trypanosoma which requires uptake by phagocytic cell to achieve mammalian life cycle stage. transmitted by sand fly. Cutaneous ulcerative skin lesions, viceral spleenomegaly, and mucocutaneous which affects mucous membranes around the mouth and is nasty sheet.
Trypanosoma cruzi
is a different species of trypanosome- different disease. Endemic to latin america nd mexico. transmitted via kissing bug. It has tissue intracellular and extracellular blood stages. It causes chagas disease which includs sx that are mild adnd asymptomatic , chonic leads to myocarditis, mesasophagus and megacolon.
Trypanosoma brucei gambiense
Less severe west africais the slow trpanosome for CNS involvement after 1-2 years, death in 3 if not treated. In second stage, they we see somnolence(extreme sleepiness at inappropriate times), altered gait, tremors, cranial neuropahties, urinary incontinance and personality changes. It is able to cross the blood CSF barrier (choroid plexus). demyelination occurrs in the last stages of the disease.