anti-malarial drugs dr chetna desai professor and head department of pharmacology g.m.e.r.s. medical...
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Anti-malarial Drugs
Dr Chetna DesaiProfessor and Head
Department of PharmacologyG.M.E.R.S. Medical College,
Ahmedabad
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Antimalarial drugs Malaria is caused by four species of
protozoa:Plasmodium malariae.P. falciparum.P. vivax.P. ovale (rare)
The plasmodium transmitted to human by the
bite of an infected female anopheles mosquito.
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Malaria transmission life cycle:
Sporozoites tissue schizonts (in liver) merozoites infect RBC (blood schizonts) rupture of RBC (clinical attack) new crops of merozoites
Sexual form: some merozoites differentiate into male & female gametocytes ingested by a mosquito where they form Sporozoites human
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P. malariae & p. falciparum have one cycle of liver invasion and end by the 4th week i.e. no relapse occurs.
P.ovale & p. vivax have dormant stages (hypnozoites) in the liver. These hypnozoites may rupture months or years later causing relapse of the attacks.
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Choice of antimalarial drug Efficacy and half-life • Acceptability and adherence to treatment
formulations) • Effectiveness • Adverse effects • Drug interactions and contraindications • Use in special groups, e.g. pregnant women,
infants • Capacity of health system to implement policy • Cost-effectiveness, affordability of various
regimens • Reported resistance and/or cross-resistance
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Blood Schizonticides
Chloroquine (4- aminoquinoline derivative)
Mechanism of action: Inhibits synthesis of DNA and RNA in the
plasmodium. Increases pH of the vacuoles in the
parasite, so prevent its utilization of erythrocyte hemoglobin.
Uses: Acute attack
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Other uses:
Amebic liver abscess (as chloroquine is concentrated in the liver).
Anti-inflammatory in autoimmune diseases e.g. rheumatoid arthritis
A/E: GIAE rash, headache,
peripheral neuritis, cardiac depressant, retinal damage (X use > 5 years without regular ophthalmic examination),
toxic psychosis.
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Quinine:
Mechanism of action: Inhibits DNA strand separation,
transcription and protein synthesis.Uses: CQ resistant P. falciparum (orally). Cerebral malaria (i.v infusion until patient
can take the drug orally).A/E: Cinchonism i.e. headache, dizziness, &
tinnitus. Inhibits cardiac conductivity hemolysis in G-6-P D and black water fever
(intravascular hemolysis).
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Qinghaosu (Artemisinin)
Chinese herbal medicine used as antipyretic. Blood schizonticide against all types of
malaria including CQR PF Unknown mechanism of action.Uses: P. falciparum cerebral malaria (oral &
parenteral). Not used for prophylaxis Used in pregnancy – only in 2nd & 3rd
trimesters
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Antifolates (sulfonamides & sulfones):
Synergistic blockade of folic acid synthesis Sulfonamide inhibits dihydropteroate
synthetase, inhibits folic acid synthesis.
Pyrimethamine and proguanil inhibit dihydrofolate reductase, so inhibit tetrahydrofolate (folinic acid synthesis).
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Fansidar
Combination of sulfadoxine and pyrimethamine.
It is used in CQ R PF.A.E: Sulfonamide: rashes, renal damage, hemolysis
& GIAE, SJ syndrome. Pyrimethamine: FA deficiency, agranulocytosisDisadvantages: slow blood schizonticide
activity, drug resistance & numerous serious adverse effects.
C/I: pregnant & nursing women, G-6-PD, renal impairment & children under 2 months of age.
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Primaquine
Tissue schizonticide. It has a cellular oxidant activity and possibly
interferes with mitochondrial function. Gametocide, so inhibits transmission of
infection by mosquito.Uses: Eradication of liver stages (hypnozoites) of
P.vivax & P.ovale, after standard chloroquine therapy to prevent relapse.
A/E: GIT upset, pruritus, headache, methemoglobinemia, hemolysis especially
in G-6-PD.
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Doxycycline Tetracycline derivative Longer half life Reliable absorption Better safety profile in renal insufficiency
Use: Drug resistant P Falciparum along with
quinine Prophylaxis
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Adverse Effects: GIAE Oesophageal ulceration Take sufficient water X Pregnancy and lactation, Children
upto 8 years
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Clindamycin Lincosamide antibiotic Inhibits protein synthesis 90% is absorbed by GIT Use: CQ RPF Safe in pregnancy and children Lesser risk of resistance A/E: ANVD Pseudomembranous colitis Hypersensitivity reactions BM depression Hepatic damage
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