Drug profile of Chloroquine

1. A PRESENTATION ON
DRUG PROFILE
Presented by
K . Bhanu Sri Chandana
167N1R0042
Vijaya Institute of Pharmaceutical
Sciences For Women
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2. Drug name : CHLOROQUINE
( Anti – Malarial agent )
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3.  Introduction
 Physical & Chemical Properties
 Pharmacokinetics
 Pharmacodynamics
 Popular Brands
Contents :
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4. INTRODUCTION
Description :
 Chloroquine is the most commonly used drug in the treatment of malaria.
 It is a rapid erythrocytic schizonticide against all species of Plasmodium.
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5. Malaria :
 Malaria is a mosquito born
infectious disease.
 Before causing of this infection ,
it’s parasite undergoes two cycles.
 Human phase
 Mosquitoes phase
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6. Life Cycle of Malarial Parasite
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7. Chemical Structure :
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 It is a quinoline derivative.
 Consists of a chlorine atom at meta position.
 It has three Nitrogen atoms.

8. Physical and Chemical Properties of the Drug
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9. IUPAC Name :
 N-(7-Chloroquinolin-4-yl)-N, N- dimethyl
-pentane-1,4-diamine
Empirical Formula : C18 H26 ClN3
Molecular weight : 319.872 g/mol.
Melting point : 87 degrees Celsius.
Form :
 It exists in crystalline form.
 It’s colour ranges form white to slight yellow
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10. Category :
 Anti – Malarial
 Anti - inflammtory
Dose :
 The doses of drug depends on
age and body weight of the patients.
 It includes four doses.
 The total dose of chloroquine should be
41.7mg within the time period of 3 days.
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11. pKa value : Chloroquine has three pKa
values i.e., 4.0, 8.4, and 10.2.
Stability : Chloroquine is stable in heat up
to the pH 4.0 to 6.5.
Storage conditions :
 Chloroquine is stable at the room temperatures.
 It is a light sensitive drug. So, it should be protected from light.
 The powdered form of the drug is more stable. So, it can be stored for
nearly 6 months.
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12. Half – Life : 78 hours after administration.
Solubility :
 It is very slightly soluble in water.
 Soluble in dilute acids, chloroform
and ether.
 Insoluble in alcohol and benzene.
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14. Absorption :
 Oral administration of chloroquine has an
excellent rate.
 About 50% of it is bound to plasma.
 It is rapidly and completely absorbed in
the GI Tract.
 Substantial amounts are deposited in
erythrocytes, liver, spleen, kidney, lungs,
melanin, etc,.
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15. Bio-availability :
 The bioavailability of chloroquine varies.
 Along with intake of food i.e., decreases.
Biological Half-life :
One to Three days of administration.
Distribution :
 About 70-85% of drug is present in blood.
Higher concentration of drug is found in serum
Also present in thrombocytes and granulocytes
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16. Plasma elimination half-life :
 The plasma elimination half-life of
chloroquine is One - Three weeks
Metabolism :
Plasma Proteins
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Liver

17. Elimination :
 Desethylchloroquine and Bisdesethylchloroquine
declines slowly in the body.
 Then they are eliminated
within 20-60 days.
Desethylcholoroquine & Bisdesethylchloroquine
P450
Dealkylation
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18. Side effects :
Headache Confusion
Nausea Convultions
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19. Loss of Vision Renal impairment
Psychosis Rheumatoid Arthritis
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20. Indicators :
Malaria prophylaxis Rheumatoid Arthritis
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21. Contraindications :
Fabry disease Renal failure
Hypotension Dermititis
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22. Dosage :
AGE DOSAGE
Children 5 mg/kg
Adults 500 mg/kg
DOSE QUANTITY
Initial dose 16.7 mg/kg
Second dose 8.3 mg/kg - after 6 hours of first dose
Third dose 8.3 mg/kg - after 24 hours of first dose
Fourth dose 8.3 mg/kg - after 36 hours of first dose
At prophylaxis :
At treatment :
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23. Uses :
Malaria Inflammation
Extraintestinal amebiosis Rheumatoid arthritis
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24. Disciod Lupus
Erythematosis
Infectious
mononucleosis
Photogenic reaction Lepra reactions
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26. Mechanism of action :
Malarial parasite
Digest host cell’s haemoglobin
Heam (toxic)
Heamozoin (non-toxic)
Polymerization
Malaria
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27. Chloroquine
Heamozoin
Prevents polymerization
Lysis of both parasite and red blood cells
Accumulation of heam
Inhibits malaria 27

28. Drug interactions :
DRUG INTERACTIONS
Antacids Reduces absorption of chloroquine
Kaolin Reduces absorption of chloroquine
Cimetidine Increases the conc. of chloroquine
Ampicillin Reduces the conc. of chloroquine
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29. Available Dosage forms :
Oral suspension
Intravenous injections
Tablets
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30. Route of administration :
Oral administration Intravenous
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31. Strength : 50mg, 100mg, 250mg, 500mg
Brands :
Lariago
Chloroquine phosphate
Quinsh 31

32. Any Questions ???....
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