13.0 Anti-Malarials Flashcards
What is the DOC for treatment and prophylaxis of vivax and ovale?
Chloroquine
Which form of species of plasmodium causes the most severe form of disease?
P. falciparum
Choloquine is highly effective against what? (antimalarial action)
Blood shizonts but not against liver parasites
What is the MOA of Chloroquine?
• Concentrates in parasite food vacuoles
• Prevents biocrystallization of hemoglobin breakdown
product heme to non-toxic hemozoin
How does chloroquine gain resistance?
• P. falciparum: mutations in putative transporter, PfCRT are
common
What is the most important AE to know for Chloroquine?
Hemolysis (G6PD-deficiency)
What are the contraindications for Chloraquine?
- psoriasis or porphyria (may precipitate attacks)
* retinal or visual field abnormalities
What are the clinical applications of quinine and quinidine?
• Parenteral treatment of severe falciparum malaria
(Quinidine)
• Oral treatment of falciparum malaria (alternative in
chloroquine-resistant areas) (Quinine)
What is the MOA of quinine and quinidine?
• Depresses O2 uptake and carbohydrate metabolism
• Intercalates into DNA, disrupting parasite’s replication and
transcription
What are the AE of quinine and quinidine?
• Cinchonism: tinnitus, headache, nausea, dizziness,
flushing & visual disturbances
• Hypersensitivity: skin rashes, urticaria, angioedema,
bronchospasm
• Hematologic abnormalities: hemolysis (G6PD
deficiency), leukopenia, agranulocytosis,
thrombocytopenia
• Hypoglycemia: stimulation of insulin release
• Uterine contractions: still used in treatment of severe
falciparum malaria in pregnancy
- Severe hypotension: too rapid IV infusion
- ECG abnormalities: QT prolongation
• Blackwater fever: hemolysis & hemoglobinuria (likely
hypersensitivity reaction)
What are the clinical applicaitons of Mefloquine?
• Chemoprophylaxis: effective against most strains of P.
falciparum and P.vivax
• Currently only medication recommended for chemoprophylaxis in pregnant women in
chloroquine-resistant areas
Which antimalarial is associated with Neuropsychiatric toxicity?
Mefloquine
Do not administer coadminister Mefloquine with what other drugs?
quinine, quinidine or
halofantrine
Primaquine is the DOC for what?
eradication of dormant liver forms of P. vivax and P. ovale
What is an important AE with primaquine?
Hemolysis or methemoglobinemia (especially in
G6PD deficient patients)
