Antimalarial drugs

1. ANTIMALARIAL DRUGS
Prepared by,
Mr. Namdeo Shinde
M. Pharm
SATARA COLLEG OF PHARMACY, SATARA (Maharashtra) India-415004.

2. Malaria parasites:
Plasmodium vivax
Plasmodium falciparum
Plasmodium malarae
Plasmodium ovale
Half lifecycle of Plasmodia is completed in body
of mosquito and remaining half in human liver
and RBCs.

3. Malaria lifecycle
Sporozoites
(in mosquito
saliva)
Primary
schizonts
Reinjected back
into mosquito
(Human liver)
Merozoites
In RBCs produces
toxines
Gametocytes
Secondary
schizonts
(in RBCs)
(Human liver)

4. Life cycle of
Plasmodium

5. Symptoms of malaria
Chill
Fever
Pain in joints
Vomiting
If malaria not treated early complicates into anaemia
and jaundice.

6. Antimalarial drugs
Drugs which kills P. Vivax and P. falciparum and used
for prophylaxis and treatment of malaria are called
antimalarial drugs.
CLASSIFICATION
PRIMARY SCHIZONTICIDES
Primaquine
SECONDARY SCHIZONTICIDES
Chloroquine-Primaquine
Blood SCHIZONTICIDES
Chloroquine, Quinine
GAMETOCITES
Primaquine
SPORONTICIDES
Chlorguanil, Pyremethamine

7. Mechanism of antimalarials
Chloroquine concentrates in RBCs and kills secondary
schizontes by increasing basicity of plasmodial cell
Artemisinin derivatives release highly reactive peroxide
radicals which destroy plasmodial cell.
Sporonticides inhibit plasmodial dihydrofolate
reductase

8. QUININE
CVS- Hypotension, Cardiac depression
GIT- Bitter stomachic
CNS- Anaesthetic
Weak analgesic and antipyretic
Uterus- Causes abortion
Endocrine- Releases insulin and lower blood sugars

9. CHLOROQUINE
THERAPEUTIC USES
Acute malaria
Prophylaxis of malaria
Rheumatoid arthritis
ADVERSE EFFECTS
Epigastric distress, Nausea, vomiting, headache
Loss of vision due to retinal damage, Skin rash
Loss of hearing
CONTRAINDICATIONS
Eye dysfunction
Heart diseases
Cautiously used in liver diseases
With antiarrythmic drugs

10. PREPARATIONS
Tab. Primaquine 15mg daily/2weeks
Tab. Quinine sulphate 600mg TDS oral for 5 days
tab. Sulfadoxime 500mg+ Pyremethamine 25mg oral
Inj. Artemether 80 mg BD i.m. 1st day then 80 mg OD
oral