pharmacy

1. Pharmacology IV
Topic : Anti Malarial Drug Chloroquine
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2. Contents
Classification
Pharmacokinetics
Biochemistry of plasmodium
Mechanism of action of chloroquine
Pharmacological actions
Adverse effects
Uses and contraindications
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3. Chloroquine
Synthesized at Bayer laboratories,
and named as "Resochin“
Classification:
Chemically 4-aminoquinoline
Therapeutically
As Supressive prophylactic
and in Clinical cure (erythrocytic schizonticide)
Gametocidal for p.vivax (prevent transmission)
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Sporozoites
injected by
mosquitoe
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Tissue
schizonts
in liver
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Blood
schizonts in
RBCs
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Gametocyte
s taken up
by mosquito
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Sporozoite
production
in
mosquito
Life cycle of Plasmodium
(Cause of Malaria)

4. Pharmacokinetics :
Synthetically
available as
chloroquine
phosphate
Rapidly and
completely
absorbed from
GIT.
Metabolised in
liver.
Peak conc.
Achieved in 2-3 hrs
after oral dose.
High tissue
distribution
esp in liver,
spleen ,lung,
kidney.
t½ 3-4days but
terminal t½1-
2months
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5. Biochemistry of Plasmodium:
Human blood has hemoglobin
Parasite utilize it to get Aminoacids
Heme is released toxic to parasite
Parasite do biocrystallization of heme into Hemozoin
(insoluble crystals)
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6. Mechanism of action
Chloroquine (basic) concentrates in parasite food
vacuole (acidic).
Prevent heme polymerization into hemozoin
causing heme accumulation (toxic to parasite).
Drug complex with heme disrupt cell
membrane function.
Other mechanism include intercalating of parasite
DNA, DNA synthesis inhibition.

7. Pharmacological activity
Antimalarial action:
 Active against erythrocytic vivax ,malariae, ovale ,sensitive falciparum and
gametocytes of vivax .
Infections:
 Amoebic liver abcesses ,Giardiasis, taeniasis
Organ system effect:
 Depress myocardium
 Anti inflammatory
 Vascular smooth muscle relaxant

8. Adverse Effects:
CVS
• Cardiomyopathy,abrupt
fall in BP
CNS
• Insomnia
• Neuromyopathy
• Ototoxicity
Ocular toxicity
• Retinopathy
Blue black
pigmentation,edema
Long term use
• Myopathy
• Pheripheral
neuropathy
Intolerance
• Nausea , vomiting
• Skinrashes,photosnsitivity
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9. Uses
Malaria
Giardiasis
Infectious mononeucleosis
Amoebic liver abcess
Rheumatoid arthritis
Contraindications and cautions
Myopathy
Visual abnormalities
Phorphyria
Hematologic disorders
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10. References
Goodman and Gillman’s Manual of Pharmacology and therapeutics
Basic and Clinical Pharmacology Katzung by Betram G.Katzung, Susan
B.Masters,Anthony J.Trevor
Lippincott
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11. Thankyou
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