Antiparasitics Flashcards
For nematode (roundworm) infections; selective damage to cytoplasmic microtubles, immobilizes and kills parasite; active for many intestinal roundworms, kills some ova; low systemic bioavailability
Mebendazole
For nematode (roundworm) infections; same mechanism as Mebendazole except liver quickly converts it to albendazole sulfoxide which is an active metabolite with good systemic distribution; used for neurocysticercosis due to taenia solum and cutaneous larval migrans
Albendazole
What are some side effects of Albendazole?
elevated hepatic enzymes
abdominal pain, nausea, vomiting, headache
For nematode (roundworm) infections; in hookworms it affects energy metabolism via inhibition of mitochondrial fumarate reductase; in Strongyloides it inhibits assembly of parasitic microtubles; used for Strongyloides, cutaneous larval migrans, alternate agent for other roundworm infections; administration topical
Thiabendazole
For nematode (roundworm) infections; depolarizing neuromuscular blocker, causing spastic paralysis of worm; used for hookworm, pinworm and roundworm; NOT effective against Trichuris
Pyrantel pamoate
What is a side effect of Thibendazole? Of Pyrantel Pamoate?
Thibendazole: N/V, dizziness
Pyrantel Pamoate: GI symptoms
Drug for Fluke infection; increases cell membrane permeability to calcium, resulting in marked muscle contraction; drug of choice for all Schistosoma, good activity against many cestodes; SE: abdominal discomfort, nausea
Praziquantel
Drug for cestode infection; for Taenia solium will prevent neurocysticercosi; good activity against many cestodes
Praziquantel
Drug for cestode infection; treats neurocysticercosis
Albendazole
Drug for cestode infection; good activity against many cestodes
Paromomycin Sulfate
Blood schizonticide; selectively toxic to parasite because parasitized erythrocytes concentrate the drug
Chloroquine
What is the mechanism of Chloroquine?
inhibits heme polymerization
Uses of Chloroquine
Prevent attacks of all 4 species of malaria
Eradicate P. malariae and chloroquine-sensitive P. falciparum
Main SE of Chloroquine
Visual impairment
Blood schizonticide, used for chloroquine-resistant and multidrug-resistant P. falciparum;
Used as prophylaxis in areas where organisms are resistant to chloroquine
Mefloquine
What are some side effects of Mefloquine?
Psychiatric effects: paranoia, depression, anxiety
Vestibular effects: dizziness, vertigo
In which individuals is Mefloquine contraindicated?
those with epilepsy or psychiatric disorder
Two drugs that block pyrimidine synthesis, blood schizonticides; Used to treat chloroquine-resistant P. falciparum
Atovaquone + Proguanil
Selectively inhibits malarial mitochondrial electron transport; ultimate effect is disruption of pyrimidine synthesis
Atovaquone
Prodrug; inhibits malarial dihydrofolate reductase; ultimately pyrimidine synthesis
Proguanil
Blood schizonticide against all four malarial parasites; agents of choose for severe acute attacks; treatment of chloroquine-resistant P. falciparum
Quinine
Decreases malarial protein synthesis and depress dihydroorotate dehydrogenase activity, thereby interfering with pyrimidine synthesis; for multi drug-resistant P. falciparum
Doxycycline
Radical cure or terminal prophylaxis of P. vivax and P. ovale because it will kill dormant liver schizonts; should be use in conjunction with blood schizonticide; used in combo with clindamycine to treat Pneumocystis jiroveci (carnii) pneumonia in AIDS patients
Primaquine
Main SE of Primaquine
hemolytic reactions in those with G6PD deficiency
Tissue amebicide for mild to severe symptomatic infections of E. histolytica
Metronidazole
Aminoglycoside-like, inhibiting protein synthesis; luminal amebicide; SE: diarrhea, nausea, vomiting, epigastric pain
Paramomycin Sulfate
Luminal amebicide; in combination with metronidazole for mild to sever infections of E. histolytica; SE: diarrhea and other GI symptoms; Contraindicated in those with hypersensitivity to iodine-containing preparations
Iodoquinol
Drug of choice for Giardia lamblia, Trichomonas vaginalis
Metronidazole
Selective inhibitor of protozoal mitochondrial electron transport; ultimate effect is disruption of protozoal pyrimidine synthesis; alternate prophylaxis or treatment for mild/moderate Pneumocystic jiroveci (carnii) in AIDS patients intolerant of TMP/SMX; active against Toxoplasma gondii
Atovaquone
Inhibits pyruvate:ferredoxin oxidoreductase; used for Giardia lamblia, Cryptosporidium parvum
Nitazoxanide