Antiparasitic drugs (Most important) Flashcards
Metronidazole - Classification
Nitromidazole compound, tissue amebicide
Metronidazole - MoA
It inhibits nucleic acid synthesis by disrupting the DNA of microbial cells.
Inhibit pyruvate-ferredoxin oxidoreductase (PFOR)
Metronidazole - Clinical use
Entamoeba histolytica
Giardia intestinalis (Giardia lamblia)
Trichonomas vaginalis
Anaerobic bacteria:
Bacteroides fragilis
Helicobacter pylori
Clostridium difficle
Amebiasis
Giardiasis
Trichonomiasis
Dracunculiasis by Dracunulus medinensis (Guinea worm infection)
Enterocolitis
Rosacea (acne rosacea)
Metronidazole - Contraindications
Contraindicated during first trimester of pregnancy
Metronidazole - Adverse effects
Metallic taste
Transient leukopenia
Thrombocytopenia
Metronidazole - Interactions
Increased effect of warfarin.
Ethanol: disulfiram-like reaction
Serum levels affected by drugs inhibiting/inducing CYP3A4.
Drugs for malaria
Quinine Chloroquine Mefloquinine Primaquine Artesunate Artemether Atovaquone Proguanil Pyrimethamine Sulfadoxine
Quinine, Chloroquine, Mefloquinine - MoA
Inhibits nucleic acid synthesis/function during erythrocytic schizogony
Quinine - Clinical use
Alternative to artesunate for severe malaria
Chloroquine - Clinical use
P. falciparum, prevention and treatment
Combination with primaquine to eradicate P. vivax
Chloroquine - Contraindications
Should be used cautiously in pregnant women because fetal damage has been reported
Chloroquine - Adverse effects
Toxic overdose: Retinal damage and blindness
Exacerbation of psoriasis and pruritus
Mefloquinine - Clinical use
Prophylaxis and treatment of falciparum malaria, where it is known to be effective
Combination with artesunate is a first-line therapy in parts of Southeast Asia and South America
Mefloquinine - Adverse effects
Severe neuropsychiatric syndrome characterized by hallucinations, anxiety, confusion, seizures and coma
Leukopenia
Thrombocytopenia
Bradycardia and arrythmias
Primaquine - Classification
Aminoquinoline derivative
Primaquine - MoA
Form quinones that oxidize and destroy schizont membranes
Primaquine - Clinical use
P. vivax and P. ovale in combination with chloroquine or other drugs
Primaquine - Contraindications
G6PD deficiency
Primaquine - Adverse effects
Hemolytic anemia in G6PD deficiency
Artesunate, Artemether - MoA
Form free radicals that attack heme and proteins in malarial parasites and inhibit erythocytic schizogony
Artesunate - Clinical use
IV is 1st line for severe falciparum malaria (children + adults)
P. vivax
Artemether - Clinical use
P. falciparum malaria
P. vivax
Atovaquone - MoA
Inh synthesis of pyrimidines and nucleic acid synthesis by selective inhibition of mitochondria electron transport in plasmodia
Atovaquone - Clinical use
Prophylaxis and treatment of Chloroquine-resistant falciparum malaria in combination with proguanil or doxycycline
Alone: pneumocystitis jiroveci infections
Proguanil - MoA
Inh synthesis of pyrimidines and nucleic acid synthesis by inhibiting folate reductase
Proguanil - Clinical use
Prophylaxis and treatment of Chloroquine-resistant falciparum malaria in combination with atovaquone
Pyrimethamine, Sulfadoxine - MoA
Inhibit folic acid synthesis
Pyrimethamine, Sulfadoxine - Clinical use
Malaria
Toxoplasmosis (with sulfadiazine)
Pyrimethamine, Sulfadoxine - Adverse effects
Skin rashes
Megaloblastic anemia and other hematologic reactions
Drugs for toxoplasmosis
Pyrimethamine + sulfadiazine
Spiramycin
Pyrimethamine + sulfadiazine - Clinical use
Toxoplasmosis in AIDS
Spiramycin - Classification
Macrolide
Spiramycin - Clinical use
Fetal toxoplasmosis
Pyrimethamine + sulfadiazine - Adverse effects
Folate deficiency and hematologic abnormalities
Pyrimethamine + sulfadiazine - Interactions
Leucovorin (folic acid) can be added to reduce the hematologic effects of these drugs
Albendazole - Classification
Benzimidazole compound
Albendazole - MoA
Binds β-tubulin and inhibit its polymerization to form microtubules in the parasites. Makes it impossible for them to obtain glucose.
Albendazole - Clinical use
Intestinal nematode infections (ascariasis, capillariasis, hookworm inf, pinworm inf, whiphworm inf)
Trichinosis (combo with corticosteroid to relieve inflamation)
Cysticercosis, echinococcosis, microsporidiosis
Albendazole - Contraindications
Contraindicated during pregnancy because of potential to inhibit mitosis and impair fetal development
Albendazole - Adverse effects
Well tolerated
High doses: Hepatitis, hemtologic toxicity
Albendazole - Interactions
Increased absorption with high fat meal
Pyrimethamine - Contraindications
Folate deficiency anemia (Vitamin B9)