Anti Malarials Flashcards
What are the primary antimalarial drugs developed historically?
Cinchona alkaloids chloroquine
What is the significance of artemisinin-based combination therapies (ACTs)?
ACTs have significantly reduced malaria-related deaths especially in endemic regions.
How is malaria transmitted and what are the main Plasmodium species involved?
Transmitted via Anopheles mosquitoes; major species include P. falciparum P. vivax
What are tissue schizonticides?
Drugs acting on primary tissue forms in the liver to prevent malaria’s erythrocytic stage; examples include pyrimethamine and primaquine.
What is the role of blood schizonticides in malaria treatment?
Blood schizonticides target blood forms of the parasite to end clinical attacks; examples include chloroquine quinine
What are gametocytocides?
Drugs that destroy sexual forms of malaria parasites in the blood reducing transmission to mosquitoes; examples include chloroquine
What are the aryl amino alcohols used as antimalarials?
Quinine quinidine
Name two 4-aminoquinolines used as antimalarials.
Chloroquine and amodiaquine.
What are the two types of folate synthesis inhibitors in antimalarial therapy?
Type 1: Inhibitors of dihydropteroate synthase (sulphones sulphonamides); Type 2: Inhibitors of dihydrofolate reductase (proguanil
What are the artemisinin derivatives used as antimalarials?
Artemether artesunate
What is the primary action of chloroquine in treating malaria?
It prevents heme polymerization within the parasite leading to toxic heme accumulation and parasite death.
Why is chloroquine often ineffective against P. falciparum?
Chloroquine resistance is common in P. falciparum due to genetic mutations.
What is the mechanism of action for artemisinin and its derivatives?
They generate free radicals within the parasite rapidly killing it
What is a key advantage of artemisinin-based therapies in treating P. falciparum?
Fast-acting and effective against chloroquine-resistant strains.
How is primaquine primarily used in malaria treatment?
Primaquine targets liver hypnozoites of P. vivax and P. ovale preventing relapse.
Why must patients be screened for G6PD deficiency before taking primaquine?
Primaquine can cause hemolysis in individuals with G6PD deficiency.
What are common side effects of chloroquine?
Nausea vomiting
What are the major side effects of quinine?
Tinnitus headache
What is mefloquine primarily used for?
Chemoprophylaxis and treatment of chloroquine-resistant malaria.
What are potential side effects of mefloquine?
Gastrointestinal symptoms and neuropsychiatric effects such as anxiety depression
How does atovaquone act as an antimalarial?
It disrupts mitochondrial electron transport in the parasite especially when combined with proguanil.
Why is atovaquone often combined with proguanil (as in Malarone)?
Combination enhances efficacy against P. falciparum and reduces resistance risk.
What are the major uses of pyrimethamine and sulfadoxine in malaria treatment?
Uncomplicated malaria particularly for chloroquine-resistant strains; also used in intermittent preventive therapy during pregnancy.
What are serious side effects of pyrimethamine and sulfadoxine?
Gastrointestinal upset and risk of severe skin reactions like Stevens-Johnson syndrome.
What is the primary use of artesunate?
Intravenous treatment for severe malaria particularly P. falciparum.
What is the role of prophylactic antimalarial drugs?
Prevent malaria in travelers to endemic regions; examples include chloroquine mefloquine