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Drugs that work at the schizont stage (in the liver)/ used for prophylaxis:
- Primaquine
- Tafenoquine
- Atovaquone
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Artemisinin MOA:
Production of free radicals
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Artemisinin combination therapy agents:
- Artesunate-amodiaquine
- Artemether-lumefantrine
- Artesunate-mefloquine
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T/F: artemisinin is used in combination with a longer acting agent and together they are the standard therapy in endemic areas for ovale/vivax malaria
False; Artemisinin is standard therapy for falciparum malaria
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Adverse effects of artemisinin:
n/v/d and dizziness
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For severe falciparum malaria, what is the preferred route of administration for artemisinin?
IV
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MOA of Chloroquine?
Prevent the detoxification of heme into hemozoin
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Chloroquine therapeutic indications?
- Uncomplicated nonflaciparum and sensitive falciparum malaria
- Drug of choice for treatment and prophylaxis
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Adverse effects of chloroquine?
- High fever!
- Not so much GI complaints
- At high enough dose can lead to suicide
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Contraindications for chloroquine?
Psoriasis or porphyria
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MOA of quinine and quinidine?
Unknown
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Therapeutic indications for quinine and quinidine?
- Severe uncomplicated falciparum malaria
- Babesiosis
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Which drug can be used to treat babesiosis as well as falciparum malaria?
Quinine and quinidine
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Which drug, if given too fast intravenously, could lead to arrhythmia and have cardiotoxic effet?
Quinine and quinidine
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What are adverse effects of quinine and quinidine?
- Cinchonism- tinnitus, headache, nausea, dizziness, flushing
- Visual disturbances
- GI upset
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Contraindications for quinine/ quinidine?
Underlying visual and auditory problems (do not want to exacerbate these sxs since these are potential side effects of quinine/ quinidine
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MOA of mefloquine?
Unknown
-
Therapeutic indication for mefloquine?
- For chloroquine resistance falciparum malaria, and vivax malaria
- Also used as chemoprophylaxis
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Adverse effects of mefloquine?
- n/v. dizziness.
- Neuropsychiatric toxicity: seizure, depression (black box warning)
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Contraindications or precautions for mefloquine?
- Epilepsy
- Psych disorders
- Arrhythmia (like quinine, so not to be used with quinine/ quinidine)
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Which of the malarial drug comes with a black box warning for adverse neuropsychiatric reaction?
Mefloquine
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Which malarial drugs could lead to arrhythmia?
- Quinine and mefloquine.
- These two so never be taken at the same time
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MOA of primaquine?
Unknown
-
Indication for primaquine use?
- Vivax and ovale malaria (in addition with chloroquine use, primaquine kills the hypnozoite)
- Terminal prohpylaxis of vivax and ovale malaria
- Gametocidal action
-
Adverse effect of primaquine?
Hemolysis due to G6PD deficiency. Because primaquine uses oxidative stress to kill the parasite
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Contraindications for primaquine?
- G6PD deficient individuals
- Pregnancy
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Atovaquone-Proguanil MOA:
- Atovaquone: Disrupts electron transport chain which in turn affects nucleotide synthesis
- Proguanil: inhibiting dihydrofolate reductase
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Trade name for atovaquone-proguanil?
Malarone
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Therapeutic indications for atovaquone-proguanil (malarone):
Chemoprophylaxis and treatment of falciparum malaria
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Adverse effects of atovaquone-proguanil:
- n/v/d
- headache and insomnia
-
precautions for atovaquone-proguanil:
pregnancy
-
which malarial drugs should be avoided when pregnant?
- Atovaquone-proguanil
- Primaquine
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Atovaquone-doxycycline MOA:
- Atovaquone- disrupts ETC
- Doxycycline- blocks 30S ribosomal subunit (a tetracycline antibiotic); prevent tRNA from binding to mRNA
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Doxycycline is used in combination with _____, ____ and _____
- Quinine
- Artesunate
- Atovaquone
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