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31 Cards in this Set
- Front
- Back
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What is radical cure
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elimination of all erythrocytic and hepatic stages of malaria
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Primaquine is a Tissue _________cide -
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Primaquine is a Tissue Schizonticide -
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Synthetic 8-aminoquinoline is active against hepatic stages of all human malaria parasites. (Only available agent active against the dormant hypnozoite stages of P. ______ & P. ______.).
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Synthetic 8-aminoquinoline is active against hepatic stages of all human malaria parasites. (Only available agent active against the dormant hypnozoite stages of P. vivax & P. ovale.).
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Primaquine
Low incidence of adverse effects. Standard doses may cause hemolysis or methemoglobinemia (manifested by cyanosis), in patients with genetically low levels of __________________ dehydrogenase. Patients should be tested for ____ deficiency before Primaquine is prescribed. Infrequently causes N, epigastric pain, abdominal cramps and headache. Contraindicated in _________ |
Primaquine
Low incidence of adverse effects. Standard doses may cause hemolysis or methemoglobinemia (manifested by cyanosis), in patients with genetically low levels of glucose-6-phosphate dehydrogenase. Patients should be tested for G6PD deficiency before Primaquine is prescribed. Infrequently causes N, epigastric pain, abdominal cramps and headache. Contraindicated in pregnancy |
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Clinical cure – blood schizonticides (ery. cycle) used to kill all erthrocytic forms
With P. __________/P. ________ clinical cure is a radical cure |
Clinical cure – blood schizonticides (ery. cycle) used to kill all erthrocytic forms
With P. falciparum/P. malariae clinical cure is a radical cure |
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Primaquine
Often used in conjunction with a _____ schizonticide (chloroquine, quinine, mefloquine, or pyrimethamine) because it is not effective against the ____________ stage of malaria. |
Primaquine
Often used in conjunction with a blood schizonticide (chloroquine, quinine, mefloquine, or pyrimethamine) because it is not effective against the erythrocytic stage of malaria. |
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Blood Schizonticide: Chloroquine (ARALEN)
DOC in the treatment of erythrocytic P. __________ malaria, except in resistant strains. Drug conc. in infected RBCs Plasmodia eat globin for amino acids, heme is toxic but they possess heme polymerase to detoxify heme to hemozoin. Drug inhibits heme polymerase leading to accumulation of toxic ferric heme that damages plasmodial membranes, inhibits synthesis of nucleic acids. Good PO absorption Raises pH from plasmoidal vacuoles |
Blood Schizonticide: Chloroquine (ARALEN)
DOC in the treatment of erythrocytic P. falciparum malaria, except in resistant strains. Drug conc. in infected RBCs Plasmodia eat globin for amino acids, heme is toxic but they possess heme polymerase to detoxify heme to hemozoin. Drug inhibits heme polymerase leading to accumulation of toxic ferric heme that damages plasmodial membranes, inhibits synthesis of nucleic acids. Good PO absorption Raises pH from plasmoidal vacuoles |
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Chloroquine
Weekly dose for prophylaxis T1/2 – 6-7 days Initial daily doses for active disease, IV or PO Adverse Effects: Usu. Well tolerated, even with prolonged use. ________ common (primarily in Africans) Uncommon – N, V, abdominal pain, headache, anorexia, malaise, blurring of vision, & urticaria. Rare – hemolysis in ____-deficient persons, impaired hearing, confusion, psychosis, seizures, agranulocytosis, exfoliative dermatitis, alopecia, bleaching of hair, hypotension and electrocardiographic changes (QRS widening, T wave abnormalities). |
Chloroquine
Weekly dose for prophylaxis T1/2 – 6-7 days Initial daily doses for active disease, IV or PO Adverse Effects: Usu. Well tolerated, even with prolonged use. Pruritus common (primarily in Africans) Uncommon – N, V, abdominal pain, headache, anorexia, malaise, blurring of vision, & urticaria. Rare – hemolysis in G6PD-deficient persons, impaired hearing, confusion, psychosis, seizures, agranulocytosis, exfoliative dermatitis, alopecia, bleaching of hair, hypotension and electrocardiographic changes (QRS widening, T wave abnormalities). |
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Chloroquine
High doses used as antiinflamatory/immunosuppressant in RA and l____ e____________; ADRs – retinopathy, cardiac depression, peripheral neuropathies, ototoxicity. |
Chloroquine
High doses used as antiinflamatory/immunosuppressant in RA and lupus erythematosis; ADRs – retinopathy, cardiac depression, peripheral neuropathies, ototoxicity. |
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Hemozoin?
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parasite usually converts heme to hemozoin to protect itself.
Chloroquine keeps the conversion from happening |
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Does chloroquin cross the BBB?
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yes
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Patients with _________ or _________ should not be treated with chloroquine, because an acute attack may be provoked.
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Patients with psoriasis or porphyria should not be treated with chloroquine, because an acute attack may be provoked.
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Blood Schizonticide: Mefloquine
Effective against chloroquine-and multidrug resistant P. falciparum; drug also used for prophylaxis in areas where there is chloroquine- resistance. T1/2 17 days, allows once weekly admin for prophylaxis, admin PO, no IV prep – not used for severe/complicated cases. MA: thought to damage the parasite’s membrane (like q_______) |
Blood Schizonticide: Mefloquine
Effective against chloroquine-and multidrug resistant P. falciparum; drug also used for prophylaxis in areas where there is chloroquine- resistance. T1/2 17 days, allows once weekly admin for prophylaxis, admin PO, no IV prep – not used for severe/complicated cases. MA: thought to damage the parasite’s membrane (like quinine) |
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Chloroquine (ARALEN
Primarily an antimalarial drug Used hepatic amebiasis / abscesses Highly concentrated in _____ Primarily an alternative to _____________ when there are contraindications to the use of _____________ or with _____________ when severe liver abscesses are present |
Chloroquine (ARALEN
Primarily an antimalarial drug Used hepatic amebiasis / abscesses Highly concentrated in liver Primarily an alternative to metronidazole when there are contraindications to the use of metronidazole or with metronidazole when severe liver abscesses are present |
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Blood Schizonticide: Quinine
Alkaloid from cinchona bark Action on erythrocytic forms all species: MA similar to chloroquine DOC severe/complicated malaria, slow IV Used in chloroquine – and multidrug resistant P. falciparum infections, adm TID PO daily; t1/2 – 10 hr. Quinidine, dextrorotatory stereoisomer of quinine, also IV in severe infections, but >more cardiac toxicity |
Blood Schizonticide: Quinine
Alkaloid from cinchona bark Action on erythrocytic forms all species: MA similar to chloroquine DOC severe/complicated malaria, slow IV Used in chloroquine – and multidrug resistant P. falciparum infections, adm TID PO daily; t1/2 – 10 hr. Quinidine, dextrorotatory stereoisomer of quinine, also IV in severe infections, but >more cardiac toxicity |
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Quinine
_________ ( syndrome causing N, V, tinnitus and vertigo), myocardial depression, oxytocic @ high doses Contraindicated in pregnancy, fetotoxic Treatment should be suspended if a positive ______ test for hemolytic anemia occurs. |
Quinine
Cinchonism ( syndrome causing N, V, tinnitus and vertigo), myocardial depression, oxytocic @ high doses Contraindicated in pregnancy, fetotoxic Treatment should be suspended if a positive Coombs test for hemolytic anemia occurs. |
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Blood Schizonticide: Artemisinin
Artemisinin (insoluble) (derived from ginghaosu plant) (no IV use) and analogs: arte______ and artesunate; rapidly-acting blood schizonticides; endoperoxide/free radical formation action in parasite food vacuole: PO/IV for resistant P. falciparum and quinine-resistant strains, used SE Asia, Africa, (not in USA) |
Blood Schizonticide: Artemisinin
Artemisinin (insoluble) (derived from ginghaosu plant) (no IV use) and analogs: artemether and artesunate; rapidly-acting blood schizonticides; endoperoxide/free radical formation action in parasite food vacuole: PO/IV for resistant P. falciparum and quinine-resistant strains, used SE Asia, Africa, (not in USA) |
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Pyrimethamine + s_________ (FANSIDAR), f_____ antagonists used in combination in resistant P. falciparum
Limited use due to serious potential toxicities: Stevens-Johnson syndrome, agranulocytosis, pneumonitis, hepatitis |
Pyrimethamine + sulfadoxine (FANSIDAR), folate antagonists used in combination in resistant P. falciparum
Limited use due to serious potential toxicities: Stevens-Johnson syndrome, agranulocytosis, pneumonitis, hepatitis |
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Treatement of Chagas disease
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nifurtimox
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Treatment of african sleeping sickness
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Early: Suramin and pentamidine
CNS: Metarsoprol |
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Pentamidine (PENTAM)
Main indication (USA) - P. ________ (formerly carinii) Active uptake by organism, inhibits mitochondrial ____isomerases (DNA) which interfer with glucose metabolism IV for infection (21 days), aerosol for prevention/maintance AIDS (monthly) Used as alternative to DOC: trimethoprim – sulfamethoxazole ADRs: breathlessness/bronchospasm (aerosol), hypotension/fainting, v. tachycardia, liver\renal dysfunction, pancreatitis, rash/S-J syndrome |
Pentamidine (PENTAM)
Main indication (USA) - P. jiroveci (formerly carinii) Active uptake by organism, inhibits mitochondrial topoisomerases (DNA) which interfer with glucose metabolism IV for infection (21 days), aerosol for prevention/maintance AIDS (monthly) Used as alternative to DOC: trimethoprim – sulfamethoxazole ADRs: breathlessness/bronchospasm (aerosol), hypotension/fainting, v. tachycardia, liver\renal dysfunction, pancreatitis, rash/S-J syndrome |
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What protects humans from nifurtimox
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superoxide dismutase
catalase glutathione peroxidase |
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Chemotherapy for Leishmaniasis
Three types of Leishmaniasis: C________ M____________ V______ (liver and spleen) – the parasite is in bloodstream & can cause very serious problems. Leishmaniasis transmitted from animals to humans (and between humans) by the bite of infected sandflies. |
Chemotherapy for Leishmaniasis
Three types of Leishmaniasis: Cutaneous Mucocutaneous Viseral (liver and spleen) – the parasite is in bloodstream & can cause very serious problems. Leishmaniasis transmitted from animals to humans (and between humans) by the bite of infected sandflies. |
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Treatment for cutaneous Leishmaniasis
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metronidazole
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Life cycle of the causitive organism: Leishmania
Sandfly transfers the flagellated ____________ form of the protozoa, which is rapidly phagocytized by macrophages. In the macrophage, the _____________ rapidly change to nonflagellated ___________ and multiply, killing the cell. The newly released ___________ are again phagocytized, and the cycle continues. |
Life cycle of the causitive organism: Leishmania
Sandfly transfers the flagellated promastigote form of the protozoa, which is rapidly phagocytized by macrophages. In the macrophage, the promastigotes rapidly change to nonflagellated amastigotes and multiply, killing the cell. The newly released amastigotes are again phagocytized, and the cycle continues. |
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Chemotherapy for Leishmaniasis
Diagnosis – Established by demonstrating the parasite in biopsy material and skin lesions. Pentavalent antimonials, such as sodium ______________, are the conventional therapy used. Exact MA undetermined. Evidence for inhibition of glycolysis in the parasite at the phosphofructokinase reaction has been found. Adverse Effects: pain at injection site, GI upsets, and cardiac arrhythmias. Renal and hepatic function should be monitored periodically. |
Diagnosis – Established by demonstrating the parasite in biopsy material and skin lesions.
Pentavalent antimonials, such as sodium stibogluconate, are the conventional therapy used. Exact MA undetermined. Evidence for inhibition of glycolysis in the parasite at the phosphofructokinase reaction has been found. Adverse Effects: pain at injection site, GI upsets, and cardiac arrhythmias. Renal and hepatic function should be monitored periodically. |
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Chemotherapy for _____________
One of the most common infections in humans is caused by the protozoan __________ ______, which is transmitted to humans when they consume raw or inadequately cooked, infected meat. An infected pregnant woman can transmit the organism to her fetus. Cats are the only animals that shed oocysts, which can infect other animals as well as humans. |
Chemotherapy for Toxoplasmosis
One of the most common infections in humans is caused by the protozoan Toxoplasma gondii, which is transmitted to humans when they consume raw or inadequately cooked, infected meat. An infected pregnant woman can transmit the organism to her fetus. Cats are the only animals that shed oocysts, which can infect other animals as well as humans. |
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Chemotherapy for Toxoplasmosis
DOC is the antifolate drug _____________. A combination of ____________ and pyrimethamine is also efficacious. __________ is often administered to protect against folate deficiency. NOTE: At the first appearance of a rash, pyrimethamine should be discontinued, because hypersensitivity to this drug can be severe. |
Chemotherapy for Toxoplasmosis
DOC is the antifolate drug pyrimethamine. A combination of sulfadiazine and pyrimethamine is also efficacious. Leucovorin is often administered to protect against folate deficiency. NOTE: At the first appearance of a rash, pyrimethamine should be discontinued, because hypersensitivity to this drug can be severe. |
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Drugs for Toxoplasmosis
Pryrimethamine + sulfadiazine, inhibits 2 steps in folic acid synthesis, DOC, 3-4 weeks Pryrimethamine + clindamycin (CLEOCIN) Trimethoprim / sulfamethoxazole (SEPTRA) Alternate drugs: Pryrimethamine + atovaquone, or + dapsone, or + one of newer macrolides Note: dihydrofolate reductase inhibitors usually requires leucovorin co-adm. to prevent myelosuppression Maintenance therapy usu required with AIDS |
Drugs for Toxoplasmosis
Pryrimethamine + sulfadiazine, inhibits 2 steps in folic acid synthesis, DOC, 3-4 weeks Pryrimethamine + clindamycin (CLEOCIN) Trimethoprim / sulfamethoxazole (SEPTRA) Alternate drugs: Pryrimethamine + atovaquone, or + dapsone, or + one of newer macrolides Note: dihydrofolate reductase inhibitors usually requires leucovorin co-adm. to prevent myelosuppression Maintenance therapy usu required with AIDS |
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Chemotherapy for Giardiasis
_______ _______ is the most commonly diagnosed intestinal parasite in the U.S. Has only 2 life-cycle stages: the binucleate trophozoite with _ flagellae, and the drug-resistant, _-nucleate cyst. |
Giardia lamblia is the most commonly diagnosed intestinal parasite in the U.S.
Has only 2 life-cycle stages: the binucleate trophozoite with 4 flagellae, and the drug-resistant, 4-nucleate cyst. |
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Chemotherapy for Giardiasis
Although some infections are asymptomatic, severe diarrhea can occur, which can be very serious in immune suppressed patients. DOC is _____________ |
Chemotherapy for Giardiasis
Although some infections are asymptomatic, severe diarrhea can occur, which can be very serious in immune suppressed patients. DOC is metronidazole |
