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18 Cards in this Set
- Front
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4 aminoquinolone prototype: Spectrum: absorption: Mechanism of action: prevention/treatment: |
prototype: chloroquine Spectrum: P. malariae, ovale, most vivax, rare falcifarum absorption: good oral, wide distribution w/ long elimination Mechanism of action: acts on process of Hemoglobin digestion in parasite food vacuole prevention/treatment: good for prevention (weekly dosing)/ treatment in non-resistant strains |
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4-aminoquinolone Adverse effects: |
headache, GI upset, pruritis, visual problems with prolonged use
may be used during pregnancy |
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Fluorinated 4-quinolone methanol prototype: Spectrum: absorption: Mechanism of action: prevention/treatment: |
prototype: Mefloquine Spectrum: chemoprophylaxis and oral treatment of uncomplicated malaria (multi- drug resistance P. falciparum) absorption: good, extensive distribution,highly plasma bound, slow elimination, cleared by hepatic biotransformation Mechanism of action: may interact with parasitic vacuole prevention/treatment: weekly dosing for prophylaxis |
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Fluorinated 4-quinolone methanol Adverse effects: Contraindications: |
Mefloquine
AEs: GI disturbances, headache, insomnia, abnormal dreams, neuropsychiatric events
Contraindications: psychiatric illness, cardiac conduction abnormalities, seizure disorders
May be used in pregnancy |
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Hydroxynapthoquinone prototype: Spectrum: absorption: Mechanism of action: prevention/treatment: |
Atovaquone Spectrum: broad antiprotazoal; erythrocytic and extraerythrocytic P. falciparum and P. vivax absorption: highly lipophilic, poor CNS Mechanism of action: inhibits electron transport prevention/treatment: both, used daily
Always in combination with proguanil |
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Folate antagonist prototype: Spectrum: absorption: Mechanism of action: prevention/treatment: |
Proguanil Spectrum: schizondicidal activity against all erythrocytic forms (vivax, ovale); sporozoites and hepatic forms of P. Falciparum absorption: poorly, short half life Mechanism of action: inhibits DHFR prevention/treatment: both in combo with atovaquone |
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Protein Synthesis inhibitor Antibacterial agent active against malaria |
doxycycline |
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Chicona alkaloids prototype: Spectrum: prevention/treatment: |
prototype: Quinine/Quinidine Spectrum: severe malaria (oral for uncomplicated malaria) prevention/treatment: treatment only
severe toxicities |
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8-aminoquinolone prototype: Spectrum: prevention/treatment: |
prototype: Primaquine Spectrum: tissue schizonticidal drug ; active against extraerythrocytic forms (p. vivax/ ovale) and gametocytes. Radical cure for vivax/ovale prevention/treatment: prophylaxis in regions where main species is P. vivax
CONTRAINDICATED IN G6PD |
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Artemesinin prototype: Spectrum: absorption: Mechanism of action: prevention/treatment: |
prototype: Artemethar-lumefantrine (artesunate for IV) Spectrum: severe malaria; acute, uncomplicated P. falciparum prevention/treatment: treament only |
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Artemethar-lumefantrine adverse effects |
many symptoms of general malaise; prolonged QT interval and should not be used with other drugs prolonging QT |
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Nitroimidazole prototype: Spectrum: absorption: Mechanism of action: contraindications: |
prototype: Metronidazole Spectrum: many protozoa; invasive amebiasis (trophozoites), giardiasis. absorption: oral or IV Mechanism of action: electron sink, damages DNA contraindications: potentiates warfarin, disulfiram like effects
Used in pregnancy after first trimester
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Second generation 5-nitroimidazole? Benefits? |
Tinidazole; longer half life than metronidazole
fewer side effects |
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Aminoglycoside? |
Paromomycin, very poor absorption in intestine, good for luminal protozoa |
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Thiazolide? |
Nitazoxanide, treats Giardia and Cryptosporidium |
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Benzimidazoles: Spectrum: absorption: Mechanism of action: |
prototype: Albendazole Spectrum: larvae, adults, eggs (GI and tissue nematodes) absorption: variable absorption improved with fatty meal Mechanism of action: microtubule polymerization by binding to beta-tubulin
DRUG OF CHOICE for helminths
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Macrocytic lactones prototype: Spectrum: absorption: Mechanism of action:
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prototype: Ivermectin Spectrum: many nematodes absorption: po well absorbed Mechanism of action: binds chloride channels hyperpolarizing and leading to slow death
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Isoquinoline-pyrazine prototype, effects? |
Praziquantal, increases membrane permeability to cations, causes spastic paralysis in worms
good oral absorption, drug of choice for Schistosoma spp, cestodes (tapeworms), most trematodes (flukes) |
