Term
Chloroquine (Aralen) and hydroxychloroquine (Plaquenil)
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Definition
Blood Schizonticides (Mirozoits)
DOC (for sensitive organisms)
Use: Prophylaxis, active against asexual erythrocytic forms
P. Falciparum is RESISTANT; Transport pump removed drug from parasite
Mechanism: maybe interferes with degradation of hemoglobin
PHK: Oral or IV; once weekly for prophylaxis
Tox: increased risk of QT prolongation and Torsade de pointes; Contraindicated in pts with psoriasis and porphyria; retinal and corneal toxicity (monitior vision)
NOT EFFECTIVE AGAINST P VIVAX AND P OVALE SECONDARY TISSUE FORMS! |
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Term
Quinine sulfate and quinidine gluconate
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Definition
Blood Schizonticides: steroisomers
Use: Erythrocytic forms, gametocidal vs. P. vivax and P. ovale
DOC for complicated, chloroquine-resistant plasmodia (combo with doxycyclin/(clindamycin if pregnant)) i.e. unconscious pt
Tox: Cinchonism - tinnitus, headache, dizzines, flushing, visual disturbance (not a reason to stop!);
Quinidine = antiarrhythmic agent - class 1A QT elongation, GI, Hemolysis in G6PD pts
DO NOT use in pregnant pts or children
PHK: Oral (quinine) or IV (quinidine)
NOT EFFECTIVE AGAINST P VIVAX AND P OVALE SECONDARY TISSUE FORMS!
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Term
Doxycycline (Vibramycin)
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Definition
Blood Schizonticides: Tetracycline abx
Use: combined with quinidine or quinine for tx of complicated, chloroquine-resistant malaria (clindamycin in children/pregnant women); Monotherapy for prevention
NOT EFFECTIVE AGAINST P VIVAX AND P OVALE SECONDARY TISSUE FORMS! |
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Term
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Definition
Blood Schizonticides
First line drug for chloroquine-resistant strains
DOC for prophylaxis against all chloroquine-resistant plasmodia
PHK: oral, well absorbed/distribution; very slow elimination = single megadose possible
Tox: Can cause seizures and may aggravate latent psychoses; should NOT be used in pts with hx of mental illness or epilepsy; potential cardiac tox (do NOT combine with quinine, synergistic cardiac toxicity)
Not recommended for pregnancy
NOT EFFECTIVE AGAINST P VIVAX AND P OVALE SECONDARY TISSUE FORMS! |
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Term
| Pyrimethamine + sulfadoxine (Fansidar) NOT BOLDED |
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Definition
Blood Schizonticides
Use: Main effect on erythrocytic forms, som effect on sporozoites and pre-erythrocytic stages, some effect on cryptomerozoites (secondary tissue forms, Proguanil)
Mechanism: Folate metabolims Inhibitor; sulfadoxine (inhibits incorporation of PABA into folic acid_
NOT EFFECTIVE AGAINST P VIVAX AND P OVALE SECONDARY TISSUE FORMS!
Other Drugs: Pyrimethamine (Daraprim) - inhibit dihydrofolate reductase
Trimethoprim (Proloprim)
Proguanil/chloroguanide (Paludrine) - inhibit dihydrofolate reductase
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Term
| Atovaquone + proguanil (Malarone) |
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Definition
Blood Schizonticide
Use: Active against tissue and erythrocytic forms; Also pneumocystis jirovecii; Tx for uncomplicated chloroquine resistant malaria as well as prophylaxis against choloquine-resistant P. falciparum
Mechanism: Atovaquone messes with the energy production in the cell, and Proguanil inhibits protein synthesis; widely used and well tolerated
Synergistic combo - effective in regions where chloroquine and mefloquine resistance is high
Side effects: Rash, fever, vomiting, diarrhea
Caution when use in pregnant women, mutagen in mice
NOT EFFECTIVE AGAINST P VIVAX AND P OVALE SECONDARY TISSUE FORMS!
Other Drugs: Halofantrine (Halfan)
Lumefantrine
Artemisinin and derivatives - chinese herbal preparation; P. falciparum
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Term
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Definition
TISSUE SCHIZONTICIDE!!!
Use: hepatic stages, P vivax and P ovale, prevents relapses; need to use for radical cure; Terminal prophylaxis (presumptive antirelapse therapy): ALWAYS combo with blood schizonticide
Toxicity: Hemolytic anemia - G6PD deficiency is contraindicated - treat relapse; contraindicated for SLE or RA or pregnancy
Generally too toxic for prophylaxis, but can be used for it
DO NOT SUPPRESS SYMPTOMS/DISEASE ONCE ERYTHROCYTIC STAGES HAVE BEEN ESTABLISHED (Falciparum) |
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