Anti-malarials as per PCI syllabus for Diploma in Pharmacy

1. ANTIMALARIALS
(STRICTLY AS PER PCI SYLLABUS FOR
DIPLOMA IN PHARMACY)
Mrunalini Kulkarni
Assistant Professor,
VU School of Pharmacy.

2. CONTENTS
 Introduction
 Life cycle of Malaria
 Antimalarials
 Classification
 Individual class of drugs
Mrunalini H Kulkarni
Note- structures have not been asterisk marked in syllabus therefore not included in
presentation.

3. WHAT IS MALARIA?
Malaria is a life-threatening disease. It’s typically transmitted through the bite of an infected Anopheles
mosquito. Infected mosquitoes carry the Plasmodium parasite. When this mosquito bites you, the
parasite is released into your bloodstream.
Once the parasites are inside your body, they travel to the liver, where they mature. After several days,
the mature parasites enter the bloodstream and begin to infect red blood cells.
Within 48 to 72 hours, the parasites inside the red blood cells multiply, causing the infected cells to
burst open.
The parasites continue to infect red blood cells, resulting in symptoms that occur in cycles that last two
to three days at a time.
Mrunalini H Kulkarni

4. LIFE CYCLE OF MALARIA
Mrunalini H Kulkarni

5.  Drugs which are used in the treatment of Malaria are known as anti-malarials.
 There are four kinds of malaria parasites that can infect humans: Plasmodium vivax, P. ovale, P.
malariae, and P. falciparum.
ANTIMALARIALS
Mrunalini H Kulkarni

6. CLASSIFICATION
 Chemical Classification-
 1. Arylaminoalcohols- Quinine, Cinchonine,Mefloquine
 2. 4-amino quinolines- Amodiaquine, Chloroquine.
 3. 8-amino quinolines- Primaquine.
 4. Acridine derivatives- Quinacrine Hyrochloride.
 5. Biguanides- Proguanil, Chloroproguanil,Cycloguanil.
 6. Diaminopyrimidine- Pyrimethamine.
 7. Miscellaneous- Trimethoprim.
Mrunalini H Kulkarni
Note- Drugs marked with purple colour are included in syllabus.

7. SITE OF ACTION OF ANTIMALARIAL DRUGS
Mrunalini H Kulkarni

8. QUININE SULPHATE
 Properties- It is alkaloid, obtained from Cinchona bark. It is white or faintly yellow crystalline
powder, It is very slightly soluble in water, soluble in alcohol, Dilute acids and dilute ammonia
solution.
 Storage- It turns brown when exposed to light therefore stored in well-closed light resistant
container.
 Uses- To treat severe and complicated malaria, cerebral malaria , to relieve nocturnal leg cramp,
mild analgesic and antipyretic property.
 Formulations- Tablets ,injection,Suspension
 Brandnames- Malaria mixture, Flue-foe, Vigitab,Nine, Rez-Q,Kwinil,Queenolar.
Mrunalini H Kulkarni

9. MEFLOQUINE
 Properties- It is White or slightly yellow crystalline powder; odorless; m p 259-260 °C
(decomposes). Exhibits polymorphism. Freely soluble in methanol; soluble in ethanol, ethyl
acetate; very slightly soluble in water.
 Storage- It is stored in well closed and light resistant container .
 Uses- For the treatment of mild to moderate acute malaria caused by Mefloquine-susceptible
strains of Plasmodium falciparum (both chloroquine-susceptible and resistant strains) or by
Plasmodium vivax. Also for the prophylaxis of Plasmodium falciparum and Plasmodium vivax
malaria infections, including prophylaxis of chloroquine-resistant strains of Plasmodium
falciparum.
 Formulations- Tablets
 Brandnames- confal,Facital,MQF, Mefax, Larimef,Mefloc.
Mrunalini H Kulkarni

10. CHLOROQUINE
 Properties- It is Available as Hydrochloride and Phosphate salt. It is an odorless white powder
with a bitter taste. It is freely soluble in water, practically insoluble in alcohol, chloroform and
ether.
 Storage- It discolors on exposure to light. It should be stored in well closed containers
protected from light.
 Uses- It kills Schizonts at all stages of erythrocytic cycle. Also effective against extra intestinal
amoebiasis especially amoebic hepatitis.
 Formulations- Injection, Tablets, Syrups, Suspension
 Brandnames- Arquin, Bitaqiune, C-Quin, Cadiquin, Clokit,Emquin, E-Mal, Falciquin.
Mrunalini H Kulkarni

11. PRIMAQUINE
 Properties- It is available as Phosphate salt, it is odorless orange red crystalline powder, bitter
in taste. It is slightly soluble in water ,Practically insoluble in alcohol, ether, chloroform.
 Storage- It should be stored in well closed containers protected from light.
 Uses- It kills Plasmodium at exo erythrocytic stage and also gametocytes.
 Formulations- Injection, Tablets.
 Brandnames- PMQ, Primalex, Primacip, Malquin, Pqine,Primacip,Primalex.
Mrunalini H Kulkarni

12. QUINACRINE
 Properties- It is available as Hydrochloride salt, it is White crystalline powder also available as
bright yellow solid. It is slightly soluble in water, Soluble in organic solvents like ethanol,
DMSO. Insoluble in benzene chloroform .
 Storage- It should be stored in well closed containers protected from light.
 Uses- Quinacrine has been used as an antimalarial drug and as an antibiotic. It is used to treat
giardiasis, a protozoal infection of the intestinal tract, and certain types of lupus
erythematosus, an inflammatory disease that affects the joints, tendons, and other connective
tissues and organs.
 Formulations- Tablets.
 Brandnames- Maladin, Mepalex, Atabrine.
Mrunalini H Kulkarni

13. PROGUANIL
 Properties-Proguanil is a Biguanide derivative available as hydrochloride salt. It is odorless,
White crystalline powder with bitter taste. It is Slightly soluble in alcohol, Water very slightly
soluble in ether ,chloroform.
 Storage- It is Hygroscopic therefore stored in well –closed containers.
 Uses-Action depends upon the formation of active metabolite cycloguanil. It kills parasites
undergoing schizony in RBC and tissue, it doesn’t kill gametocytes.
 Formulations –Tablets
 Brandnames- Progunal, Laveran, Malarone, Paludrine.
Mrunalini H Kulkarni

14. CYCLOGUANIL
 Properties-Cycloguanil is a triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-
1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl
groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug
proguanil.
 metabolite of the antimalarial drug proguanil.
 Storage- stored in well –closed containers.
 Uses- same as that of Proguanil.
 Formulations- Tablets
 Brandnames- Malarone .
Mrunalini H Kulkarni

15. PYRIMETHAMINE
 Properties- it is odorless and white crystalline powder. It is soluble in warm, dilute mineral acids,
slightly soluble in alcohol, chloroform, insoluble in water.
 Storage- stored in well –closed light resistant containers.
 Uses- same as that of proguanil hydrochloride.
 Formulations-tablets, injection.
 Brandnames- Laridox, Amalar, lari, Calfin, Domine, Falcipar, Kemar, Kelfin.
Mrunalini H Kulkarni

16. Thank you
Thank you
Mrunalini H Kulkarni