Sunday, 22 February 2015

CHLOROQUINE

One must be thorough with malarial parasite life cycle to understand about the chloroquine well . So i advice the readers to learn about the life cycle of plasmodium before reading this post.

CHLOROQUINE IS THE DRUG USED WIDELY FOR TREATING MALARIA . BEFORE WE SEE ABOUT THE DRUG IN DETAIL . LET'S REVIEW ABOUT THE DIFFERENT STAGES OF MALARIAL LIFE CYCLE AND THE SCHEMA OF TREATING MALARIA .

IN HUMANS MALARIAL PARASITE UNDERGOES 2 STAGES
1) PRE - ERYTHROCYTIC STAGE ( parasite is inside the liver ) 
2) ERYTHROCYTIC STAGE ( parasite is inside the RBC )

SCHEMA FOR TREATING MALARIA:
  1. DRUGS TO TREAT THE ACUTE ATTACK : These drugs kill the plasmodium in the RBC .eg- chloroquine , mefloquine, artemisnin derivatives . 
  2. DRUGS FOR RADICAL CURE :  For radical cure , combination of drugs that kill the erythrocytic stage + drugs that kill the exo-erythrocytic(liver) stage is used .
    eg- chloroquine + primaquine
  3. DRUGS FOR PROPHYLAXIS : These drugs kill the plasmodium in the exo-erythrocytic(liver) stage.
    eg- primaquine , proguanil 
  4. DRUGS FOR PREVENTING TRANSMISSION: These drugs kill the gametes . eg - chloroquine  

                                   CHLOROQUINE


MECHANISM :
                          Chloroquine accumulates in the food vacuole of PLASMODIUM ,  thus it is selective for erythrocytic stage of malaria ( food vacuole in the plasmodium is found only in the erythrocytic stage ). 
Then it inhibitis the conversion of heme to hemozoin .
Heme is toxic to the parasite , thus the parasite in the rbc gets killed.

OTHER ACTIONS of chloroquine:
  1. Anti-inflammatory 
  2. Anti-histamine
  3. Anti-arrythmic
  4. Local anesthetic 
  5. Active against Giardia lamblia and Entamoeba histolytica
PHARMACOKINETICS :
  1. Given orally 
  2. Partly metabolized in liver
  3. 70% excreted in urine unchanged
    30% excreted in urine as a metabolite .
USE:
  1. R - Rheumatoid arthritis
  2. E - Extra-intestinal amoebiasis
  3. D- Discoid Lupus Erythromatosis
  4. L - Lepra reaction
  5. I - Infectious mononucleosis
  6. P - Photogenic reaction
  7. M - Malaria 
  8. G - Giardiasis
   RED LIP Mahatma Gandhi is the mnemonic to remember the uses of chloroquine .

ADVERSE EFFECTS:
  1. Skin rashes ( Lichenoid eruptions )
  2. Peripheral neuropathy
  3. Auditory impairment 
  4. Blindness due to retinal damage ( bull's eye maculopathy)
  5. Porphyria
BULL'S EYE MACULOPATHY


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