This document presents information on the drug chloroquine, an anti-malarial agent. It discusses chloroquine's introduction, chemical and physical properties, pharmacokinetics, mechanisms of action, indications, contraindications, interactions, and administration. Key points include that chloroquine is a quinoline derivative effective against malaria parasites, it has excellent oral absorption and distributes widely in tissues, and its primary mechanisms involve preventing heme detoxification and accumulating toxic levels of heme in parasites.

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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