Anti-Malarials Flashcards
Drugs for the prevention of malaria in travelers in areas without resistant P. falciparum
Chloroquine
Drugs for the prevention of malaria in travelers in areas with chloroquine resistant P. falciparum
Atovaquone + Proguanil (Malarone) Mefloquine
Drugs for the prevention of malaria in travelers in areas with multidrug resistant P. falciparum
Doxycycline
Terminal prophylaxis of P. vivid and P. ovale infections; alternative for primary prevention
Primaquine
4 species of plasmodium which cause malaria
– Plasmodium falciparum – Plasmodium vivax – Plasmodium malariae – Plasmodium ovale
Most virulent species of plasmodium; responsible for most of serious complications & deaths
Plasmodium falciparum
Drug resistance (important therapeutic problem is most notable with this virulent species)
Plasmodium falciparum
primarily pathogenic to monkeys; now known to cause illness to humans in Asia
P. knowlesi
Stage 1 of lifecycle: Transmission of (1) by Plasmodium-infected Anopheles into the bloodstream
- sporozoites
Stages 2&3 of lifecycle: (1) invade (2); divide forming (3)
- Sporozoites 2. Liver 3. multinucleated schizonts (pre-erythrocytic stage)
Active against hepatic-stage schizonts (stages 2 and 3)
Atovaquone-proguanil and primaquine
Stage 4: (1) rupture & release (2) to blood; invade RBC, forming (3) & later (4)
- Schizonts 2. merozoites 3. trophozoites 4. multinucleated schizonts (erythrocytic stage)
Blood-stage schizonticides (stage 4)
Quinoline derivatives (Chloroquine, amodiaquine, quinine, quinidine, mefloquine, primaquine, lumefantrine & halofantrine) Antifolates (sulfadoxine-pyrimethamine, atovaquone-proguanil) Antimicrobials (tetracycline, doxycycline and clindamycin) Artemisinin derivatives interrupt schizogony within red cells
Quinoline derivatives (Chloroquine, amodiaquine, quinine, quinidine, mefloquine, primaquine, lumefantrine & halofantrine)
stages 2, 3, 4, 5 Active against hepatic-stage schizonts Active against blood-stage schizonticides gametocidal drug (primaquine)
Antifolates (sulfadoxine-pyrimethamine, atovaquone-proguanil)
stages 2, 3, 4 Active against hepatic-stage schizonts Active against blood-stage schizonticides
Antimicrobials (doxycycline)
Active against Blood-stage schizonticides (stage 4)
Artemisinin derivatives interrupt schizogony within red cells
Active against Blood-stage schizonticides (stage 4) gametocidal drugs (Stage 5)
Stage 5. Some merozoites differentiate into ♂ or ♀ (1); ingested by the Anopheles mosquito & mature in the mid-gut to (2) (migrate to the salivary glands of the mosquito)
- gametocytes 2. sporozoites
gametocidal drugs
Artemisinin derivatives and Primaquine
Tissue schizonticides
drugs that eliminate developing or dormant liver forms
Blood schizonticides
drugs that act on erythrocytic forms of the parasites
Gametocidal drugs
drugs that kill sexual stages & prevent transmission to mosquitoes
Causal prophylactic drugs
prevent erythrocytic infection
Treatment & chemoprophylaxis of infection with sensitive parasites
Chloroquine