Drugs for Malaria

Questions
1. What are the extra malarial uses of chloroquine?

2. What is radical cure? Which drug is used for that?

3. What test to be done before starting primaquin?

4. What is the role of primaquin in falciparum malaria?

5. Name the gametocidal drugs

6. Name the drugs for chloroquine resistant malaria

7. What is the ADR of chlroquine IV injection?

8. What are the advantages of artemisinin based treatment

 Falci
parum

Malaria Plasmo
Vivax
e dium

Ovale
 Classification

4 aminoquinolines
Chloroquine Quinoline
Chincona alkaloids
methanol
Amodiaquine Quinine
Meflo quine
Piperaquine

8 amino quinolines Diamino

Primaquine Biguanides pyrimidines
Proquanil Pyrimethamine
Tafenoquine

Artemisinin Phenanthrene
Artesunate methanol Naphthoquinone
Artemether Halofantrine Atovaquone
Arteether Lumefantrine
• Haemoglobin
Aminoacid CHLOROQUINE

Haem
Haem polymerase

Polymerization

Haemozoin
Pharmacokinetics Spectrum

Well
Trophozoite
absorbed,
of all species
distributed

No effect
Oral, IM, IV
other stages
 Uses

Malarial Extramalarial

Clinical
Amoebiasis
cure,prophylaxis
Rh.arthritis
All P.Ovale
Discoid lupus
Malariae

Lepra reaction
Most Vivax
IMN
Some falciparum
Photogenic reactions
 Toxicity

Oral IV
Visual
Hypotension
Phototoxicity

Grey Hair Cardiac

Loss of hearing Arrythmias
 Quinine
Uses Toxicity
Choloroquine resistant
Severe, Cerebral Black Water Fever
malaria
G 6PD defieciency
1st trimester
pregnancy

Cinchonism
Nocturnal Leg Cramps
Hypoglycemia
Babesiosis
Cardiac Arrythmias
Myotonia Congenita
 Mefloquine
• MOA: Like Quinine
PK • PK: Enterohepatic circulation; t1/2 2-3 weeks
&
PD
• Treatment and Prophylaxis of Chloroquine resistant
Malaria
Us • With artesunate
es

• Neuropsychiatric Manifestations
AD • Cardiac Arrythmias; visual disturbances
R
 Primaquine
Inhibit Coenzyme Q

Causal
Prophylaxis Gametocyte
Radical cure
Pnemocystis Hypnozoite
Carinii

G6PD deficiency
Meth Hbemia
Dihydro Folate Reductase Inhibitors
Pyrimethamine Proguanil

Preerythroctic
Toxoplasmosis Erythrocytic
Pneumo.carinii

With
sulphonamide With atovaquone
/Dapsone

Rashes Treatment &

Megaloblastic Prophylaxis of
anaemia Malaria
Atovaquone Halofantrine

Inhibit mitochondrial MDR malaria

RS chain MOA Not clearly
known

Resistant Malaria
Pneumocystis Cardiac Toxicity
pneumonia
Not with mefloquine
Toxoplasmosis
• Like chloroquine
Lumifantrine • Like chloroquine
• Not for • Less cardiotoxic • MDR malaria
prophylaxis • With artemisinin
• Agrnulocytosis • MDR malaria

Amodiaquine Piperaquine
 Artemisinin Compounds
Artemether
Arteether

Semisynthetic Artesunate

Newer
Classification Arterolane
compounds

Natural Artemisinin
Clevage of endo
peroxide bridge

Parasite
Death
Inhibit Ca
ATPase
 Bio POOR
ava
i
Cro labilit
ssBB B y

pro QT Ora
l
Leu
lon
gati Par , Recta
ent
cop
eni
on
ral l
a

Sev
Er y
Falc ere M thr
i p a DR
m a r um pha ocytic
lari se
a
 Artemether-
Lumifantrine

Artesunate-
Combined with
mefloquine(AS/
long acting drug
mq)

Artesunate-
Artemisinin Amodiaquine
Based AS/AQ
Combinations
Dihydro
artimisnin +
Less resistance piperaquine
3 day therapy
Artesunate
Less ADR
Sulfadoxine
Pyrimethamine
 Artesunate-
• In India mefloquine • With fatty meal
• National • Not with CYP2D6
• For resistant cases
programme metabolisers
• Not in vivax • Less in India
• Arthralgia, Myalgia
• Toxic
Artesunate
Artemether-
Sulfa/
Pyrimethamine Lumifantrine
 Dihydro artimisnin
• In CQ resistant + piperaquine • Equal to
areas • In 8:1 artemether
combination lumifantrine

Artesunate- Arterolane –
Amodiaquine piperaquine
 u
p
p • Primaquine; proquanil
r
e
Causal
s
prophylaxis
s
i
v • Chloroquine,mefloquine, doxycycline
e
p
r
o
Cli p • Artemisinin, chloroquine
ni h
cal y
cu l
Ra a
re
di x
ca i
l
cu
s • Primaquine
re
G
a
m
et
oc
id
 Chloroquine
resistant
malaria

Artesunate
Artesunate
Sulfadoxine
Mefloquine
Pyrimethamine

Quinidine
Artemether
Doxycyclie
Lumifantrine
Clindamycin
 Quinidine
clindamycin
I trimester
Artesunate
Pregnancy clindamycin

II &III Quinidine
Trimester clindamycin
 Questions
1. What are the extra malarial uses of chloroquine?
2. What is radical cure? Which drug is used for that?
3. What test to be done before starting primaquin?
4. What is the role of primaquin in falciparum malaria?
5. Name the gametocidal drugs
6. Name the drugs for chloroquine resistant malaria
7. What is the ADR of chlroquine IV injection?
8. What are the advantages of artemisinin based treatment