anti malarial agents

2. • Malaria is an Arthropod borne infection (Infection transmitted
from one host to another by an arthropod vector-The mosquito)
• The infection with a specific sporozoan parasites of the genus
Plasmodium and transmitted to man by certain species of infe-
cted female ANOPHELES mosquito

3. CAUSATIVE AGENT
Malaria is caused by 4 distinct species of malaria parasite
o PLASMODIUM VIVAX
o PLASMODIUM FALCIPARUM
o PLASMODIUM MALARIAE
o PLASMODIUM OVALE
malaria is an infection of the red blood cells, causing recurring fever of
sudden onset

4. SITE OF ACTION OF ANTIMALARIAL AGENTS
 Kills the sporozoites injected by the mosquito or prevailing the
entering of sporozoites entering the liver- Prophylactic agent
 Drug active against erythrocytic phase – eg: Amodiaqunine,
Chloroqunine, Quinine
 Kills the merozoites in the blood and/or prevent their multiplication
known as a suppressive agent – Chloroquine, Amodiaquine
 Kills the gametocytes before they enter the mosquito and reproduce
in to zygotes eg: primaquine

6. • 9 – Amino acridine - Mepacrine
• Pyrimidine analogue - Pyrimethamine
• Polycyclics - Doxycycline, Halofantrine
• Sesquiterpene Lactones - Arteether, Arteemether, Artesunate
• Miscellanous - Metaloamine sulphadoxine,mefloquine
• Newer antimalarial agents - Artemisinin, fosmidomycin

7. oQuinine was the first known antimalarial ,obtained from
Cinchona Officinalis
oIt is a 4 –Quinoline Methanol derivative bearing a substituted
Quinuclidine ring
o Four stereo isomeric chiral centers exist in the molecule at C- 3,
C-4,C-8,C-9
o The dextro isomer of Quinine is Quinidine which is used as
Anti Arrythmic drug
CINCHONA ALKALOIDS

8. QUININNE (QUINEX,QUINER)
It is a di –acid tertiary base
Bitter in taste
It contains two major fused ring systems
namely aromatic Quinoline and Bicyclic
quinuclidine
ADR
Tinnitus, impaired hearing, disturbed
vision, nausea and vomiting

9.  DOSE
650 MG GIVEN EVERY EIGHT HOUR FOR 7 DAYS
 USE
Used to treat Chloroquine resistant strains of PLASMODIUM
FALCIPARUM
4-AMINOQUINOLINES
Act against PLASMODIUM in the ERYTHROCYTIC stage.
They act by intercalating in to the DNA of the parasite

10. CHLOROQUINE ( Cadiquin, Melubrin )
 It prevent the development of malarial parasites in the blood
 It does not destroy the plasmodium vivax, p.ovale parasites
that remain in the liver
 The phosphate salt is used in oral dosage form and
hydrochloride salt is used in the paraentral formulation
 ADR
 Retinopathy
 Hair loss
 Photo sensitivity
 Sleep disturbances

11. Concentrating in parasite food vacuoles, preventing the
biocrystallization of the hemoglobin breakdown product,
heme, into hemozoin, and thus eliciting parasite toxicity
due to the buildup of free heme.
DOSE: 300mg once weekly & continued for at least 4 weeks
USE: Blood Schinoticide
MECHANISM OF ACTION

12. HYDROXY CHLOROQUINE ( Hqtor, winflam)
4,7 dichloro quinoline
4-amino-1-{(N-hydroxyl
ethyl)ethylamino pentane}
Hydroxy chloroquine
SYNTHESIS

13. ADR
• Retinopathy
• Hair loss
• Photo sensitivity
• Tinnitus
DOSE: Intially 800mg followed by 400mg
USE: Both Prophylaxis and treatment
8- AMINO QUINOLINES
PRIMAQUINE (pmq, Malquine)
ADR: NAUSEA,VOMITING,EPIGASTRIC DISTRESS

14. • DOSE:15 mg daily for 14 days
• USE: It is active against Exoerythrocytic Plasmodium Vivax
malaria and also inhibits gametocyte stage
BULAQUINE(Aablaquin)
DOSE: 25 mg daily for 7 days
USE : Treatment and prevention
of p.vivax

15. PYRIMIDINE ANALOGUES
PYRIMETHAMINE(pyralfin,malasulf)
MOA: It act by interferes with TETRRAHYDROFOLIC acid synthesis from
FOLIC acid by inhibiting the enzyme DIHYDROFOLATE REDUCTASE
ADR: Urticaria,photosensitization,arthralgia
DOSE:25mg as a single dose
•Used in combination regimens, in the treatment and
prevention of malaria.

16. • FANSIDAR It is the fixed combination of PYRIMETHAMINE AND
SULFADOXINE
SESQUITERPENE LACTONE
ARTEETHER(acter)
DOSE:150 mg once daily
USE: Treatment of CHOLROQUINE resistant p.falciparum

17. • ADR: Headache, Nausea, Cough, Dizziness
ARTEMETHER( lartither, paluther)
ADR: Dizziness,Tinnitus,Nausea,Vomiting
DOSE:80 mg daily
USE: It is used in the Suppressive prophylactic for the prevention of severe
attack due to malaria parasite

18. SULPHADOXINE
It is an Anti-Bacterial group
It interferes with parasitic ability to synthesis FOLIC ACID
ADR:Urticaria,photosensitization,& Arthralgia
DOSE:500mg As a single dose
USE: It has Antibacterial activity,in combination with
TRIMETHOPRIM
It act as Anti Malarial agent in combination with
PYRIMETHAMINE&MEFLOQUINE

19. MISCELLANOUS
MEFLOQUINE(mqf,mefque)
ADR:Nausea,Vomiting,Abdominal
pain,and Diarrhoea
DOSE:20 TO 25 mg as a single dose
USE:It is effective against the Erythrocytic
form of malaria

20. SULPHADOXINE MEFLOQUINE