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Antimalarial Drugs


  1. 4 aminoquinolines
    1. Chloroquine
    2. Amodiaquine
  2. 8 aminoquinolines
    1. Primaquine
    2. Bulaquine
  3. Sesquiterpine lactone
    i. Mefloquine
  4. Cinchona alkaloid
    i. Quinine sulphate
  5. Biguanides
    1. Progaunil
    2. Cycloquanil
  6. Artemisnins
    1. Artesunate
    2. Arteether
    3. Artemether
  7. Phenanthrenes
    1. Halofantrine
    2. Lumefantrine
  8. Sulfonamide (FANSIDAR)
    i. Sulfadoxine+pyrimethamine combination
  9. Chloroquine
    1. Most commonly used antimalarial
    2. Inhibits Hb utilization by parasite
    3. Basic drug, goes inside parasites, raises pH of vocules, & prevents Hb degradation
    4. Cumulative; accumulates in fats, skeletal muscles, eye & heart
    5. No action outside RBC (not an exo-Erthrocytic schizontocidal drug)
    6. Absorption reduced by antacids
    7. Long acting drug, t/1/2=50 hours to 30 days
    8. DOC
      1. Plasmodium vivax                      
      2. Plasmodium falciparum (sensitive)      
      3. Malaria in pregnancy          
      4. Tropical spleenomegaly              
      5. Prophylaxis of malaria

Extramalarial uses (RED LIP)

  1. R=Rhematoid arthritis
  2. E=Extraintestinal
  3. D=DLE
  4. L=Lepra reaction
  5. I=Infectious mononucleosis
  6. P=Photogenic reactions 

Side effects

  1. MC-GI upset
  2. Haemolysis in G-6-P-D
  3. IV injection-cardiopulmonary depression
    i. Switch to oral route as soon as possible
  4. Prolonged use-neuropathy or optic neuritis
  5. Bull’s eye maculopathy occurs
  6. Myopathy
  7. Ototoxicity
  8. Drug is safe in pregnancy, but category C


  1. Acute intermittent porphyria                
  2. Psoriasis (also avoid beta blockers)
  3. Renal failure                        
  4. Hepatic failure
  5. Hematological disorders                        
  6. Psychiatric disorders 

B. Mefloquine


Sesquiterpine lactone

Long acting; blocks DNA synthesis

Half life=30 days

AV blocker, cardiotoxic

Avoided in arrhythmias, psychiatric, & neurological disorders


Chlorquine resistant malaria in endemic areas

Chlorquine resistant malaria in pregnancy

Neuropsychiatric reactions are usual side effects


C. Quinine

  1. Alkaloid obtained from Cinchona plant
  2. Short acting; damages DNA
  3. Well absorbed
  4. Basic drug; bound to alpha-1 glycoproteins, that is why loading dose is given
  5. Rapidly acting erythrocytic schizontocidal drug
  6. Concentrates heavily in RBCs
  7. No action outside RBCs

Side effects

  1. MC-GI upset
  2. Hypoglycemia-give in 5% dextrose
  3. Black water fever-immune mediated
  4. Acute renal failure
  5. Thrombocytopenia
  6. ‘Curare like action’ 

D. Artemisnins

  1. Fastest, safest antimalarials
  2. Reduce fever with in few hours
  3. Damage DNA by liberating free radicals
  4. Well absorbed
  5. No hemolysis in G-6-P-D
  6. Rapidly acting erythrocytic schizontocidal drugs
  7. No action outside RBCs
  8. Not recommended for prophylaxis
  9. Now considered to be safe in pregnancy
  10. DOC-severe malaria 

E. Primaquine

  1. Most potent gametocidal agent; progaunil, pyrimethamine DO NOT have gametocidal property
  2. Well absorbed
  3. Reduces man to mosquito transmission of malaria
  4. Hemolysis n G6PD is MC side effect
    1. Smoky coloured urine is MC manifestation
    2. Start patient on fresh blood transfusion
  5. DOC
    1. Eradication of liver hypnozoites 7.5 to 15 mg per day x 14-21 days)
    2. Also used in pneumocystis carnii
      Bulaquine* is free from hemolysis  

F. Phenanthrenes

  1. Most toxic antimalarials
  2. Halofantrine, lumefantrine damage DNA
  3. Halofantrine absorption increased by food; avoided with food
  4. Cardiotoxicty is main problem
  5. No cardiotoxicity with lumefantrine
  6. Cardiotoxicity is less in children
  7. Used in MDR malaria

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