C/3. Antiprotoozal And Antihelminthic Drugs Flashcards
Drugs for malaria (7)
Chloroquine Mefloquine Quinine Artemether Lumefantrine Atovaquone Primaquine
Drugs for Other protozoal disease (1)
Metronidazole
Drugs for helminthic infections (3)
Mebendazole
Ivermectin
Niclosamide
Chloroquine
Blood schizonticide
Inhibit heme polymerisation into hemozoin->heme accumulation is toxic
Oral
Tx+prophylaxis for P. Falciparum, P. Vivax and P. Ovale
GI distress, rash, headache
In high dose: Retinal, Auditory damage, QT prolongation
Mefloquine
Blood schizonticide
Unknown mechanism
Oral
Tx+prophylaxis for P. Falciparum (1st line agent)
GI distress
Skin rash
Conduction abnormalities
Neurotoxicity (seizures)
Quinine
Blood schizonticide
Inhibit protozoa DNA replication
Oral
IV in severe infections
Oral
Tx of multidrug resistant malaria
Cinchonism (GI distress, headasche, vertigo, blurred vision, tinnitus)
Acute hemolysis in G6PD deficient pts
Conduction abnormailities
Teratogenic
Artemether
Blood schizonticide
Production of free radical within vacuoles
Oral
IV in severe infections
Use as prophylaxis
Tx of multidrug resistant malaria
Effective against quinine resistant trains
Generally well-tolerated
Nausea, vomiting, diarrhea
Lumefantrine
Blood schizonticide
Mechanism unknown
Oral
In combination with artemether against P. Falciparum
QT prolongation
Atovaquone/Proguanil
Atovaquone : disrupts mitochondrial metabolism
Proguanil : antimetabolite (inhibits folate synthesis)
Oral
Tx+prophylaxis of multidrug-resistant P.falciparum
Generally well-tolerated
GI distress, fever, rash
Primaquine
Tissue schizonticide (kill schizonts in the liver) Metabolites act as oxidants
Oral
Eradication of liver stages of P. Vivax and P. Ovale
Used in combination with chlroquine
GI distress
Rash, headaches
Acute hemolysis in G6PD deficient pts
Teratogenic
Metronidazole
Form free radicals->interfere with nucleic acid synthesis
Oral, parenteral
Hepatic metabolism
Inhibitor of CYP450 enzymes
Antibacterial
Antiprotozoal againt Giardia lamblia, T. Vaginalis, Entamoeba histolytica
GI distress
Leukopenia
CNS effects
Mebendazole
Inhibits microtubule synthesis
Inhibits glucose uptake
Oral
90% of the given dose is not absorbed- luminal active agent
Uses
- Ascaris lumbricoides
- Enterobius vermicularis (pinworm)
- Trichuris trichuria (whipworm)
- Vsceral larva migrans
GI distress
Granulocytopenia, alopecia(at high dose)
Teratogenic
Ivermectin
Facilitates GABA-mediated transmission in nematodes
Causes immobilization of parasites
Oral
Doesnt cross BBB
Intestinal nematodes : Strongyloides steroralis
Tissue/blood nematodes : Cutaneous larva migrans, Oncocerca volvulus
Reaction to the dying worms
Fever, headach
Rash, pruitus
Joint and muscle pain
Niclosamide
Uncoupling oxidative phosphorylation
Oral
Tapeworms Taenia saginate (beef tapeworm) Taenia solium (pork tapeworm) Diphyllobathriumn latum (fish tapeworm)
Generally well-tolerated
GI distree, fever, rash
