Antimalarial and Anti Parasitic Flashcards
4-aminoquinolone derivative that prevents polymerizarion of the hemoglobin breakdown product heme into hemozoin
Drug of choice for P falciparum (chloroquine sensitive)
Heme accumulation is toxic to parasite
Blood schizonticide
Chloroquine
GI upset
Rash
Headache
Chloroquine resistance is brought about by
Decreased intracellular accumulation via increased activity of membrane transporters
Decreased accumulation of chloroquine via a transporter encoded by the pfcrt gene (chloroquine-resistance transporter gene)
Complexes with double stranded DNA to prevent strand separation resulting in blockade of DNA replication and transcription to RNA
Drug of choice for chloroquine resistant malaria
Solely a schizonticide
Quinine
Rare and fatal complication in quinine-sensitized persons
Blood lysis -> hemoglobinuria -> fatal
Contraindicated in pregnancy
Blackwater fever
Forms quinoline-quinone metabolites which are electron-transferring redox compounds that act as cellular oxidants
Tissue schizonticide and limits transmission by acting as a gametocide
Active against liver forms of P vivax and ovale
Primaquine
Also PCP
Metabolism to toxic free radicals in protozoa
Blood schizonticide
Artemisinins
GI upset
Disrupts mitochondrial metabolism
For falciparum
Atovaquone
Alternative for PCP
Fever
Rash
GI upset
Can cause blood cytopenias
Hemolysis in G6PD deficiency
Primaquine
Inhibits folate synthesis
Mostly blood schizonticides
Antifolates
Pyrimethamine
Proguanil
Fansidar (Pyrimethamine + Sulfadoxine)
GI upset
Rashes (sometime severe severe)
Cytopenias
Undergoes a reductive bioactivation of its nitro group by ferredoxin (present in anaerobic parasites) to form reactive cytotoxic products
E hystolitica Giardiasis Trichomonas vaginalis Gardnerella vaginalis Bacteroides fragilis C difficile
Metronidazole
Drug of choice for trichomonas
Giardiasis, Gardnerella vaginalis, Anaerobic bacteria (B fragilis, C difficle)
H. pylori
Metronidazole
Amebiasis
trophozoites
cyst
Metronidazole
Diloxanide - luminal
Giardiasis
Metronidazole
Trichomoniasis
Metronidazole
treat both partners
Pneumocystis
TMP-SMX
Toxoplasmosis
Pyrimethamine-Sulfadiazine
If with HIV TMP-SMX
Leishmania
Stibogluconate
Trypanosome
Nifurtimox - Chagas
Suramin - African
Crosses CNS and placenta
For acute attacks of malaria
Because of antiinflammatory effect, it is sometimes used in autoimmune disease
Chloroquine
Chloroquine SE
Low dose: GI, headache, rash
High dose: Retinal damage, neuropathies, myocardial depression, psychosis, hearing loss
Long term: discoloration of mucous membrane, hemolytic anemia in G6PD
Quinine SE
Cinchonism
Hemolytic anemia G6PD
Blackwater fever
MOA unknown
Excreted in feces
Used in prophylaxis and treatment of chloroquine-resistant P falciparum
May cause seizures, hallucinations, depression at high doses
Mefloquine
(Pyrimethamine) Dihydrofolate reductase inhibitor
For chloroquine-resistant species
Drug of choice for toxoplasmosis
Pyrimethamine-Sulfadoxine (Fansidar)
Forms redox compounds acting as cellular oxidants
Used for relapsing malaria -> eradicates liver stages of P vivax and ovale
Primaquine
Primaquine SE
Hemolytic anemia G6PD
Granulocytopenia
Headache
Methemoglobinemia
Drug of choice for toxoplasmosis
Pyrimethamine with sulfadiazine with folinic acid
From infected sandflies
Leishmaniasis
Kala azar
Sodium stibogluconate
Inhibits PFK reaction of glycolysis
Monitor renal and hepatic function
Adverse effect: Arrythmia
Sodium stibogluconate
Prophlaxis and treatment of African sleeping sickness without CNS involvement
Kerandel’s sign
Suramin
Drug of choice for African sleeping sickness with CNS involvement
Melarsoprol
Drug of choice for hemolymphatic stages of African Sleeping Sickness
Kerandel’s sign
Pentamidine
Drug of choice for American sleeping sickness Chagas
Chagoma
Romana’s sign
Nifurtimox
Metronidazole SE
Disulfiram-like reactions with alcohol Metallic taste Potentiation of Warfarin’s effect Nausea and vomiting Urine discoloration Oral candidias CNS disturbance - dizziness, vertigo, numbness, paresthesia Contraindicated in pregnancy
H pylori triple treatment
Clarithromycin + Metronidazole/Amoxicillin + PPI
Drug of choice for asymptomatic cyst shedders ameba
Contrandicated in pregnant women and those <2
Diloxanide furoate
Iodoquinol tetracycline emetine dehydroemetine chloroquine
Drug of choice for pinworm (enterobius) and whipworm (trichiuris), hookworm (necator)
Effective against round worm (ascaris)
Teratogenic
Mild SE: nausea and vomiting
Mebendazole
Drug of choice for ascaris and hookworm (necator)
Depolarizing neuromuscular blockade -> paralyzes the worm
Pyrantel pamoate
For threadworm (Strongyloides stercoralis)
May cause tingling, numbness, diarrhea, nausea and SJS
Thiabendazole
For cysticercosis, hydatid cyst, cutaneous larva migrans
Inhibits uptake of glucose
Albendazole
Inhibits microtubule synthesis and glucose uptake in nematodes
Mebendazole
Drug of choice for filariasis caused by Wuchereria bancrofti
Unknown MOA
Diethylcarbamazine
Dying microfilariae Pruritus Lymphadenopathy Hypotension Tachycardia
In treatment of Wuchereria and onchocerca
Mazzotti reaction
Drug of choice for onchocerca volvulus, threadworm (strongyloides)
Intensifies GABA transmission -> paralysis of worm
Ivermectin
For schistosomiasis
Increases permeability to calcium -> tetanic contraction of nematode
Praziquantel
Drug of choice for tapeworm (cestode) infection
Inhibits mitochondrial anaerobic phosphorylation of adenosine diphosphate within cestodes
Niclosamide
Treats river blindness
Oncocerca volvulus
Ivermectin
