antimalarial drugs
Post on 31-May-2015
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ANTIMALARIAL DRUGS
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ANTIMALARIAL DRUGS :
MALARIA
Malaria is a protozoan infection .It is caused by 4 species:
Species causing malaria
Plasmodium vivax benign Plasmodium ovale Plasmodium falciparum
malignant Plasmodium malaria. Benign
tertian.
TRANSMISSION OF MALARIA
BITE OF FEMALE ANOPHELES MOSQUITO
SHARING NEEDLES
BLOOD TRANSFUSION
LIFE CYCLE AND SITES OF DRUG ACTIONS:
CHLOROQUINE
It is a 4- aminoquinoline
It is a rapidly acting erythrocytic schzonticide against all species of plasmodium.
Controls most clinical attacks in 1-2 days with disappearance of parasites from peripheral blood in 1-3 days.
Mechanism of action
It is a basic drug, which is taken by acidic food vacuoles of susceptible plasmodia and inhibits conversion of haeme to haemozoin.
Mechanism of action
chloroquine
concentrated in acidic vacuole of parasite
binds to haeme drug
haeme complex damages
plasmodia membrane
pharmacokinetics
Oral absorption is excellent .absorption after i.m inj is also good
About 50% is bound to plasma
High affinity for melanin and nuclear chromatin : gets tightly bound to these tissue constituents and is concentrated in liver ,spleen,kidney,lungs,skin,leucocytes and some other tissues.
Its selective accumulation in retina is responsible for ocular toxicity seen with prolonged usage. +
Partly metabolised in liver and excreted in urine.
Early plasma half life is 3-10 days.because of tight tissue binding, small amounts persist in body with a terminal half life of 1-2 months.
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