You can watch this lecture video on youtube https://www.youtube.com/watch?v=51OgNKXhbYc Complete Chapter of Anti-malarial Drugs Part -2 -Synthesis of Important drugs -Mechanism Of action -Uses & Adverse effects -Brand Name

1. Complete Chapter of
Anti-malarial Drugs Part -2
-Synthesis of Important drugs
-Mechanism Of action
-Uses & Adverse effects
-Brand Name
B. Pharm 6th
Semester &
Pharm.D 3rd Year

2. Chloroquine-Anti-Malarial Drug
Step-1
O
Ethylene oxide
+
N
H
H2
C
H3C
H2
C
CH3
Diethylamine
C H 3 O H
2 -D ie th y l am in o eth a n o l
C H 2 O H
H 2 C N
C 2 H 5
C 2 H 5
SOCl2
CH2Cl
H2C N
C2H5
C2H5
CH3COCH2COOC2H5
-HCl
CH3COCHCOOC2H5
C
H2
H2
C N C2H5
C2H5
KOH,Hydrolysis
-C2H5OH
-CO2
CH3CO(CH2)3N
C2H5
C2H5
LiAlH4
[H]
CH3CH
OH
(CH2)3N
C2H5
C2H5
-H2O
NH3
CH3C-(CH2)3N
C2H5
C2H5
NH2
Step-2
CH3C-(CH2)3N
C2H5
C2H5
NH2
N
Cl
Cl
4,7-Dichloro-quinoline
+ -HCl
Condensation
N
Cl
HNC
H
(CH2)3N
CH3
C2H5
C2H5
(7-Chloro-quinolin-4-yl)-(1,1-diethyl-2-methyl-pyrrolidin-2-yl)-amine
Or Chloroquine
4-Amino-1-diethylamino
pentane

3. Uses
-Chloroquine is used to treat or prevent malaria
-Chloroquine is also used to treat amebiasis
(infection caused by amoebae).
Adverse Effects
-signs of an allergic reaction (hives, difficult breathing,
swelling in your face or throat)
-severe skin reaction (fever, sore throat, burning eyes,
skin pain, red or purple skin rash with blistering and
peeling).
Brand Name:-Aralen, Aralen Phosphate, Aralen
Hydrochloride

4. N
N H 2
H 3 C O
6 - M e t h o x y - q u i n o l i n - 8 - y l a m i n e
N
C2H5
C2H5
H2
C
C
H2
H2
C
CH
CH3
Cl
(4-Chloro-pentyl)-diethyl-amine
+ N
H N
H 3 C O
N
C H 3
C 2 H 5
C 2 H 5
Pamaquine
Synthesis of Pamaquine
Use
Pamaquine is an 8-aminoquinoline drug formerly used for the treatment of malaria.
Adverse Effects
Gastrointestinal reactions, methemoglobinemia, and in persons with G6PD deficiency, mild
to severe intravascular hemolysis.
Brand Name:-Gamefar

5. Mechanism of action of Pamaquine
ROS=Reactive
oxygen species

6. Synthesis of Hydroxy chloroquine

7. Mechanism of Action of Hydroxychloroquine
It has been shown that
hydroxychloroquine accumulates in the
lysosomes of the malaria parasite, raising
the pH of the vacuole.
This activity interferes with the parasite's
ability to proteolyse hemoglobin,
preventing the normal growth and
replication of the parasite.
Hydroxychloroquine can also interfere
with the action of parasitic heme
polymerase, allowing for the
accumulation of the toxic product beta-
hematin.

8. Uses:
• Hydroxychloroquine is used to treat malaria
• It is also used to treat symptoms of rheumatoid arthritis
• Used in the treatment of discoid or systemic lupus erythematosus.
• Used in the treatment of juvenile idiopathic arthritis
Brand Name: Plaquenil
Adverse Effects:
• Skin rashes, especially those made worse by sunlight
• Feeling sick (nausea) or indigestion
• Diarrhoea
• Headaches
• Bleaching of the hair or mild hair loss
• Tinnitus (ringing in the ears)
• Visual problems.

9. Synthesis of Primaquine

12. Uses:Primaquine is a medication used to treat and prevent malaria and to treat
Pneumocystis pneumonia. Specifically it is used for malaria due to Plasmodium
vivax and Plasmodium ovale along with other medications
Brand Name: Jasoprim, Malirid, Neo-Quipenyl, Pimaquin, Pmq, Primachina,
Primacin, Primaquina, Primaquine, Primaquine diphosphate, Primaquine
Phosphate, and Remaquin
Adverse Effects:
• Nausea
• Stomach pain or upset
• Vomiting
• Loss of appetite
• Heartburn
• Abdominal cramps

13. Synthesis of Pyrimethamine

15. Uses: It is used with leucovorin to treat the parasite diseases toxoplasmosis
and cysto-isosporiasis.
This medication is used with other medication (such as a sulfonamide) to
treat of the body, brain, or eye or to prevent toxoplasmosis infection in people
with HIV infection.
Brand Name: Daraprim
Adverse Effects: Common side effects include gastrointestinal upset, severe
allergic reactions, and bone marrow suppression.
It should not be used by people with folate deficiency that has resulted in
anemia

18. Uses: ART and its active derivatives have been widely used as antimalarial
drugs for more than 30 years, and they have also been shown recently to be
effective in killing cancer cells
Brand Name: Arteannuin, Alaxin, Armiqin
Adverse Effects:
• Skin rash
• nausea
• vomiting
• tremors
• liver issues