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72 Cards in this Set
- Front
- Back
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If someone has a gastric reflux what could you not give them if they were taking chloroquine?
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antacids decrease the absorption
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What is the MOA of chloroquine?
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accumulates in food vacuole of plasmodia and prevents polymerization of heme into hemozoin. Heme is thus toxic and kills cells
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What are the mechanisms of resistance to chloroquine?
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decreased intracellular accumulation of heme via pumps and pfcrt transporter gene
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When is chloroquine the drug of choice?
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acute attacks of nonfalciparum and sensitive falciparum malaria and for chemoprophylaxis
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What other condition is chloroquine used for?
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rheumatoid arthritis
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What are the toxicities of chloroquine?
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severe skin lesions, peripheral neuropathies, myocardial depression, retinal damage, auditory impairment and toxic psychosis. Can cause porphyria attacks
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What is the MOA of quinine?
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binds dsDNA to prevent separation
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When is quinine given? What is it given with?
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chloroquine resistant p falciparum.
doxycycline or clindamycin to shorten the duration of use |
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When is quinidine given and how?
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IV for severe complicated p falciparum infection
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What are the toxicities of quinine use?
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1) cinchonism
2) cardiac conduction problems 3) hemolysis in G6PD deficient people 4) Blackwater fever |
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Can quinine be given during pregnancy?
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no
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What is cinchonism? What causes it?
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It is cuased by quinine. person develops GI distress, headache, vertigo, blurred vision, and tinnitus
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What is blackwater fever? What causes it?
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It is caused by quinine and is a rare possibly fatal intravascular hemolysis that can lead to kidney failure
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When is mefloquine given?
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1st line drug for prophylaxis in chloroquine resistant areas and is an alternative to quinine in acute attacks
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What are the side effects of mefloquine?
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cardiac conduction defects, pyschiatric disorders, neurologic symptoms and seizures
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What is the MOA of primaquine?
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inhibits electron-transferring redox compounds that act as cellular oxidants
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What drug is a tissue schizonticide and also a gametocide?
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primaquine
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What organisms is primaquine used against?
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P vivax and ovale... note needs to be used with a blood schizonticide
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What are the toxicities of primaquine?
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well tolerated but can cause pruritus, headaches, methmeglobinemia, hemolysis in G6PD deficient people
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Can primaquine be given during pregnancy?
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no
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What are examples of the antifolate drugs used for malaria?
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pyrimethamine, proguanil, sulfadoxine and dapsone
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What is the MOA of sulfonamides?
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antimetabolites of PABA that block folic acid synthesis by inhibiting dihydropteroate synthase
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What is the MOA of pyrimethamine and proguanil?
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inhibit protozoan dihydrofolate reductase
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Are the antifols blood or tissue schizonticides?
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blood
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What is Fandisar? When is it used?
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combo of pyrimethamine and sulfadoxine. Used during chloroquine resistance
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What is malarone? When is it used?
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combo of proguanil and atovaquone. Used for both prophylaxis of mefloquine and chloroquine resistance
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What are the toxic effects of sulfonamides?
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skin rashes (steven johnsons), GI distress, hemolysis, kidney damage and drug displacement from plama proteins
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What is the concern when giving pyrimethamine?
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development of folic acid deficiency
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What is doxycycline and when is it used?
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a tetracycline used in chloroquine and mefloquine resistant areas
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When is amodiaquine used? What are its toxicities?
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1) chloroquine resistant p falciparum
2) hematologic toxicity, agranulocytosis, aplastic anemia |
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What is the MOA of atovaquone?
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mitochondrial ETC disruption
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When is atovaquone used for malaria?
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prophylaxis and treatment of p falciparum
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What is halofantrine effective against?
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erythrocytic stages of all 4 malaria species
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What are the toxicities of halofantrine?
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QT prolongation and embroytoxicity
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What is the MOA of artesunate and artemether?
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metabolized in food vacuole to become free radicals
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What are artemisins active against?
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blood schizonticides active against multi-drug resistant p falciparum
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What is the only drug reliably effective against quinine resistant p falciparum?
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artemesins
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Prevention in multidrug resistant areas of p falciparum is acheived with what?
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doxycycline or malarone (proguanil and atovaquone)
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What are tissue amebicides?
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chloroquine, emetines, metronidazole... act in bowel wall and liver
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What are luminal ambecides?
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diloxanide furoate, iodoquinol, paromomycin
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What is the first line treatment for asymptomatic amebiasis? What about mild to severe?
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1) diloxanide furoate
2) metronidazole plus luminal agent |
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What is the MOA of emetine and dehydroemetine?
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inhibit protein synthesis by blocking ribosomal movement
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What are the side effects of emetines?
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muscle weakness, arrythmias and CHF
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When is iodoquinol used?
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mild to severe intestinal amebiasis
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What are the toxic effects of iodoquinol?
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if absorbed thyroid enlargement, peripheral neuropathy and visual dysfunction
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What is the MOA of metronidazole and tinidazole?
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reductive activation of nitro group by ferredoxin to form cytotoxic products
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What infections is metronidazole the drug of choice?
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trichomoniasis and amebiasis, G vaginalis, B fragilis, C difficile, H pylori
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What are the adverse effects of metronidazole?
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GI irritation, headache, DARK urine, LEUKOPENIA, dizziness and ATAXIA. Disulfuram like effect and potentiation of coumarin
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What is paromomycin used for?
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cyrptosporidiosis in AIDS and symptomatic amebiasis
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What are the side effects of parmomycin if it gets absorbed?
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if absorbed get headache, dizziness, rashes and arthralgia
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What is the MOA of nitazoxanide?
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interfers with the pyruvate:ferredoxin oxidoreductase (PFOR) enzyme dependent electron transfer reaction which is essential to anaerobic energy metabolism.
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What is nitazoxanide used to treat?
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G. lamblia, C parvum, metronidazole resistant protozoa
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What is pentamide used for?
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p jeroveci prophylaxis... note that it is inhaled... also used for Trypanosoma gambiense and T rhodesiense
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What are the toxicities of pentamide?
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1) respiratory stim followed by depression
2) hypotension 3) hypoglycemia 4) anemia, neutropenia 5) hepatopancreatitis Note toxicities are limited when used as an inhalant |
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What is the first drug of choice in p jeroveci prophylaxis?
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TMP-SMX
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What is used as prophylaxis against toxoplasmosis and isospora belli?
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TMP-SMX
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What are the toxicities of TMP-SMX?
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rash (steven-johnsons), fever, neutropenia, thrombocytopenia
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What is used to treat toxoplasmosis? What should be given to reduce side effects?
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pyrimethamine and sulfadiazine given with folinic acid
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What are the toxic effects pryamethamine and sulfadiazine?
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glossitis, headache, insomnia, seizures, megaloblastic anemia, thrombocytopenia and steven-johnson
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Atovaquone is approved for mild to moderate treatment of p jeroveci. Who should this drug not be given to?
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people with a history of siezures, psychiatric disorders, and cardiac conduction defects
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What is pentamidine used for?
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the hemolymphatic stages of Trypanosoma gambiense and rhodesiense. also used for p jeroveci, kala azar leishmaniasis
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Is pentamide used in early or late stages of trypanosomissis
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Used in early infection because it cannot cross blood brain barrier
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When is melarsoprol used? What is its MOA? What are its toxicities?
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organic arsenical that inhibits enzyme sulfhydryl groups. It enters CNS and can be used against African sleeping sickness. It may cause reactive encephalopathy and be fatal
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What is nifurtimox used for? What is its MOA?
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inhibits trypanothione reductase unique to parasites. It is drug of choice for American trypanosomiasis (chagas) and can be used against leishmaniasis
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What is suramin used for?
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it is a polyionic compound used in early hemolymphatic stages of African trypanosomiasis
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What is the MOA of eflornithine? When is it used? What are SE?
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inhibits ornithine decarboxylase. Used in African trypanosomiasis and penetrates CNS. Causes hematotoxicity and seizures
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What are drugs used to treat leishmaniasis?
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sodium stibogluconate ihibits glycolysis and nucleic acid metabolism
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What are the toxic effects of sodium stibogluconate?
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long QT
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What is miltefosine used for?
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visceral leishmaniasis. also use pentamindine
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What can be used to treat cutaneous leishmaniasis?
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fluconazole or metronidazole
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mucocutaneous leishmaniasis is treated with?
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amphotericin B
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What drug should be used in with an acute attack of P vivax?
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chloroquine for acute attacks
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