ANTIPROTOZOAL AGENTS Flashcards
What are the ANtimalarial agents?
Chloroquine
Quinine
Mefloquine
Primaquine
Doxycycline
Artemisinin Analogs
(Artemisinin,Artesunate Artemether)
MOA of Chloroquine?
Prevents polymerarization of heme into hemozoin
MOA of Quinine?
Complexes with DNA to prevent strand separation → blocks replication and
transcription
MOA of Mefloquine?
Unknown
MOA of Primaquine?
Forms electron-transferring redox compounds that acts as cellular oxidants
MOA of Doxycycline?
Impairs progeny of malarial apicoplast genes → abnormal cell division
MOA of Artemisin Analogs?
Forms toxic free radicals in malarial food vacuoles
Uses of Chloroquine?
● Non-falciparum chloroquine-sensitive malaria
● Chemoprophylaxis
Uses of Quinine?
● Malaria (Chloroquinone resistant areas)
● DOC for malaria in pregnant patients
Uses of Mefloquine?
● Malaria (Chloroquinone resistant areas)
Uses of Primaquine?
● Radical cure for P. vivax and P. ovale
Uses of Doxycycline?
none
Uses of Artemisin Analogs?
Malaria (uncomplicated falciparum, quinine-resistant)
Toxicity of Choholorquinine?
● GI upset
● Skin rash
● Retinal damage
● Cardiac arrhythmia
● Neuropsychiatric reaction
Toxicity of Quinine?
● Cinchonism (HA, Tinnitus,
vertigo)
Toxicity of Mefloquine?
● GI upset
● Skin rash
● Neuropsychiatric reaction
● Seizures
Toxicity of Primaquine?
● GI upset
● Pruritus
● Methemoglobenemia
● Hemolysis in G6PD deficient
patients
Toxicity of Doxycycline?
none
Toxicity of Artemisinin Analogs?
● Nausea
● Vomiting
● Diarrhea
What are the drugs used in Amebiasis(Luminal amebicide)?
Diloxanide Furoate
Iodoquinol
Poromomycin
What is the MOA of Diloxanide Fuorate?
Unknown
What is the MOA of Iodoquinol?
Unknown
What is the MOA of Poromomycin?
Inhibits Protein synthesis
Uses of Diloxanide Furoate?
DOC for symptomatic cyst carriers for E. histolytica
Uses of Iodoquinol?
Mild to severe intestinal amebiasis
Uses of Poromomycin?
● Back-up drug for asymptomatic cyst carriers
● Cryptosporidiosis
Toxicity of Diloxanide Furoate
GI upset
Toxicity of Iodoquinol?
● GI upset
● Thyroid enlargement
● Skin reaction
● Neurotoxicity
Toxicity of Poromomycin?
● HA
● Dizziness
● Rashes
● Arthralgia
What are the drugs used in Amebiasis (Tissue amebicides)
Metronidazole
Nitazoxanide
Emetine
MOA of Metronidazole?
Reactive reduction by ferrodoxin forming free radical that disrupt transport
chain
MOA of Nitazoxanide?
Reactive reduction by ferrodoxin forming free radicals that disrupt electrom
trannsport chain
MOA of Emetine?
Inhibits Protein synthesis
USES of Metronidazole?
● DOC for Severe intestinal and extraintestinal amebiasis,
Trichomoniasis, Giardiasis, Bacterial viginosis
USES of Nitazoxamide?
● Metronidazole-resistant amebiasis
● DOC for Giardiasis, Cryptosporidosis
Uses of Emetine?
● Back -up drug for severe intestinal and extraintestinal amebiasis
Toxicity of Metronidazole?
● Metallic taste
● GI upset
● Disulfiram-like effect
Toxicity of Nitazoxamide
● GI upset
Toxicity of Emetine?
● GI upset
● Muscle wealness
● CV dysfunction
What are the DRUGS FOR
PNEUMOCYSTIS AND
TAXOPLASMOSIS
Cotrimoxazole ((Trimethorprimsulfamethoxazole))
Pyrimethamine - Sulfadiazine
Uses of Cotrimoxazole
First line drug for prophylaxis and treatment for pnumocystis carinii
pneumonia
Uses of Pyremethamine?
DOC for toxoplasmosis
Toxicity of Cotrimoxazole?
● GI upset
● Rash
● Fever
● Nutropenia
● Throbocytopenia can
happen in patient with AIDS
Toxicity of Pyremethamine
● GI upset
● Hematologic toxicities
(meglobastic anemia,
thrombocytopenia)
● Neurologic symptoms (HA,
seizures, insomia, tremors)
DRUGS FOR
TRYPANOSOMIASIS
(WEST AFRICAN)
Pentamidine
Eflornithine
MOA of Pentamidine?
Unknown
MOA of Eflornithine
Suicide inhibitor of ornithine decarboxylase
Uses of pentamidine?
● DOC for hemolymphatic stage of Trypanosomiasis
● Pneumocystis jirovecii infections and Kala azar form of Leishimaniasis
Uses of Eflornithine?
DOC for West African sleeping sickness (Trypanosoma brucei
gambiense)
DRUGS FOR
TRYPANOSOMIASIS
(EAST AFRICAN)
Suramin
Melarsoprol
Sodium stibogluconate
MOA of Suramin?
unknown
MOA of Melasoprol?
Oraganic arsenical (-) enzymes with sufahydryl groups in trypanosomes
Uses of suramine?
DOC for hemolymphatic stage of trypanosomiasis
Uses of Melarsoprol?
DOC for advanced East African sleeping sickness (Trypanosoma
brucei rhodosiense)
MOA of Sodium stibogluconate
inhibits glycolysis or nucleic acid metabolism
