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 Antimalarial drugs used for
 Prophylaxis
 Treatment
 Prevention of malaria.
 Malaria is one of the major communicable
diseases affecting mankind.
 It is caused by plasmodium parasite, which is
transmitted by the bite of infective female
anopheles mosquito.
 There are four plasmodium species important to
mankind, p.vivax, p.falciparum, p.malaria, and
p.ovale.
 Chloroquine
 Amodiaquine
 Piperaquine
 Mechanism of action: it concentrates with in
parasite acid vesicles and raises internal ph
resulting in inhibition of parasite growth.
 Choloroquine is rapidly acting against all the
species of plasmodium.
 It has anti-inflammatory, and local anesthetic,
weak smooth muscle relaxant, antihistamine
and antiarrhythmic properties.
Age in years Dose Chloroquine phosphate
( No of tablets )
Day 1 day 2 day 3
>1 75mg 1/2 1/2 1/4
1-4 150mg 1 1 1/2
5-8 300mg 2 2 1
9-14 450mg 3 3 1 1/2
15 and
above
600mg 4 4 2
 Mefloquine
 Mechanism of action: it binds with heme and
forms a complex which damages the parasite’s
membrane.
 250 mg per week preferably 1-2 weeks.
 Quinine
 Quinidine
 Mechanism of action:
 it inhibits the polymerization of heme to
hemaozoin, so free heme damages parasite
membranes.
 Quinine destroys erythrocytic forms of the
parasite similar to chloroquine,
 But less effective and more toxic
 It has mild analgesic and antipyretic actions
 Also act as local anesthetic and has skeletal
muscle relaxant properties.
 It is given orally for uncomplicated chlorine
resistant malaria and I.V for complicated or
cerebral malaria.
 The 7 day quinine + doxycycline/ clindamycin is
the 2nd line treatment of chlorine resistant
malaria.
 Quinine 10mg/kg between 8 hourly in 5%
dextrose saline is preferred in case of
complicated and severe malaria.
 Proguanil
 (chloroguanide)
 Mechanism of action:
 It inhibits the pre-erythrocytic stage of
plasmodium falciparum.
 Proguanil has little role in prophylaxis or in
clinical cure of malaria.used in
 Atovaquone-proguanil is a used in travellers as a
prophylaxis for chloroquine resistant
plasmodium falciparum.
 Pyrimethamine
 Mechanism of action:
 It inhibits the enzyme dihydrofolate reductase,
there by impeding reduction of dihydrofolic acid
to tetrahydrofolic acid to tetrahydrofolic acid.
 Pyrimethamine is used in combination with
sulfonamide to treat falciparum malaria.
 It is used in dosage of sulfadoxine 1,500mg +
pyrimethamine 75mg (3tab) single dose
 Children 9-14 years 2tab, 5-8 year 1 ½ tablet,
 1-4 year 1 tablet.
 Primaquine
 Tafenoquine
 Mechanism of action: It eliminates primary
tissue exoerythrocytic forms of p.falciparum,
disrupts mitochondria and binds to DNA.
 It is active against the pre erythrocytic stage of
p.falciparum , than that of p.vivax .
Age in years Primaquine (7.5 mg
base )
No of tablets ( 1 day)
<1 Nil 0
1-4 7.5mg 1
5-8 15mg 2
9-14 30mg 4
15 and above 45mg 6
Age in years Primaquine 2.5 mg
base
Daily for 14 days
( no of tablets)
<1 Nil 0
1-4 2.5 mg 1
5-8 5.0 mg 2
9-14 10.0 mg 4
15 and above 15.0 mg 6
 Sulfadoxine (bacteriostatic)
 Sulfamethopyazine ( bacteriostatic)
 Dapsone ( anti-inflammatory)
 Mechanism of action:
 It inhibits the di-hydrofolate reductase of
plasmodia and there by blocks the DNA
synthesis and cell multiplication,
 which leads to failure of nuclear division.
 Injectable forms of artemisinin derivatives are
used for management of severe and complicated
malaria.
Drug Dosage
Artesunate 2.4 mg/kg given IM/IV followed by 1.2
mg/kg after 12 hours then 1.2 mg/kg once
daily for total duration of 5 days.
Artemether 1.6 mg/kg IM followed by 1.6mg/kg daily
for total of 6 injections
(or) 1.6 mg/kg IM injection twice daily for 3
days, a total of 6 injections.
Arteether
150 mg daily IM for 3 days in adults only
Artemisinin 10mg / kg at 0 and 4 hours followed by 7
mg/kg at 24, 36, 48 and 60 hours.
 They are used in case of uncomplicated
falciparum and for severe and complicated
falciparum malaria.
 Tetracycline
 Doxycycline
 Clindamycin
 Mechanism of action:
 They are bacteriostatic antibiotics that bind to
the 30s subunit of the ribosome and prevent the
binding of tRNA to the ribosome, thus inhibiting
bacterial protein synthesis.
 Artesunate
 Artemether
 Arteether
 Arterolane
 Mechanism of action:
 It interacts with heme resulting in the generation
of free radicals that bind to the membrane
protein and damages the parasite membrane.
 Halofantrine
 Lumefantrine
 Mechanism of action:
 Similar to that of chloroquine, quinine, and
mefloquine, by forming toxic complexes with
ferriprotoporphyrin Ix that damage the
membrane of the parasite.
 Pyronaridine
 Atovaquone
 Mechanism of action:
 It appears to interfere with electron transport in
protozoal mitochondria, inhibiting enzymes
needed for the synthesis of nucleic acids and
adenosine triphosphate.
 Use cautionly in patients with
 -renal failure
 Severe GI problems
 Neurologic
 Cardiac diseases
 History of depression
 Hemolytic anemia
 - impaired hepatic function
 -Bronchial asthma or blood disorders.
 Use cautionly in elderly patients with renal and
cardiac problems.
 Admister the drugs with food or milk.
 Monitor liver function test to prevent toxic
effect.
 Explain importance of daily drug intake.
 Educate take the medicine with food.
 Instruct the prophylaxis measures as
 -protective clothing
 -Bed nets
 -insect repellents.
 -instruct to report adverse effects if any
Antimalarial drugs converted

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Antimalarial drugs converted

  • 1.
  • 2.  Antimalarial drugs used for  Prophylaxis  Treatment  Prevention of malaria.
  • 3.  Malaria is one of the major communicable diseases affecting mankind.  It is caused by plasmodium parasite, which is transmitted by the bite of infective female anopheles mosquito.
  • 4.  There are four plasmodium species important to mankind, p.vivax, p.falciparum, p.malaria, and p.ovale.
  • 5.
  • 6.  Chloroquine  Amodiaquine  Piperaquine  Mechanism of action: it concentrates with in parasite acid vesicles and raises internal ph resulting in inhibition of parasite growth.
  • 7.  Choloroquine is rapidly acting against all the species of plasmodium.  It has anti-inflammatory, and local anesthetic, weak smooth muscle relaxant, antihistamine and antiarrhythmic properties.
  • 8. Age in years Dose Chloroquine phosphate ( No of tablets ) Day 1 day 2 day 3 >1 75mg 1/2 1/2 1/4 1-4 150mg 1 1 1/2 5-8 300mg 2 2 1 9-14 450mg 3 3 1 1/2 15 and above 600mg 4 4 2
  • 9.  Mefloquine  Mechanism of action: it binds with heme and forms a complex which damages the parasite’s membrane.
  • 10.  250 mg per week preferably 1-2 weeks.
  • 11.  Quinine  Quinidine  Mechanism of action:  it inhibits the polymerization of heme to hemaozoin, so free heme damages parasite membranes.
  • 12.  Quinine destroys erythrocytic forms of the parasite similar to chloroquine,  But less effective and more toxic  It has mild analgesic and antipyretic actions  Also act as local anesthetic and has skeletal muscle relaxant properties.
  • 13.  It is given orally for uncomplicated chlorine resistant malaria and I.V for complicated or cerebral malaria.
  • 14.  The 7 day quinine + doxycycline/ clindamycin is the 2nd line treatment of chlorine resistant malaria.  Quinine 10mg/kg between 8 hourly in 5% dextrose saline is preferred in case of complicated and severe malaria.
  • 15.  Proguanil  (chloroguanide)  Mechanism of action:  It inhibits the pre-erythrocytic stage of plasmodium falciparum.
  • 16.  Proguanil has little role in prophylaxis or in clinical cure of malaria.used in  Atovaquone-proguanil is a used in travellers as a prophylaxis for chloroquine resistant plasmodium falciparum.
  • 17.  Pyrimethamine  Mechanism of action:  It inhibits the enzyme dihydrofolate reductase, there by impeding reduction of dihydrofolic acid to tetrahydrofolic acid to tetrahydrofolic acid.
  • 18.  Pyrimethamine is used in combination with sulfonamide to treat falciparum malaria.  It is used in dosage of sulfadoxine 1,500mg + pyrimethamine 75mg (3tab) single dose  Children 9-14 years 2tab, 5-8 year 1 ½ tablet,  1-4 year 1 tablet.
  • 19.  Primaquine  Tafenoquine  Mechanism of action: It eliminates primary tissue exoerythrocytic forms of p.falciparum, disrupts mitochondria and binds to DNA.
  • 20.  It is active against the pre erythrocytic stage of p.falciparum , than that of p.vivax .
  • 21. Age in years Primaquine (7.5 mg base ) No of tablets ( 1 day) <1 Nil 0 1-4 7.5mg 1 5-8 15mg 2 9-14 30mg 4 15 and above 45mg 6
  • 22. Age in years Primaquine 2.5 mg base Daily for 14 days ( no of tablets) <1 Nil 0 1-4 2.5 mg 1 5-8 5.0 mg 2 9-14 10.0 mg 4 15 and above 15.0 mg 6
  • 23.  Sulfadoxine (bacteriostatic)  Sulfamethopyazine ( bacteriostatic)  Dapsone ( anti-inflammatory)  Mechanism of action:  It inhibits the di-hydrofolate reductase of plasmodia and there by blocks the DNA synthesis and cell multiplication,  which leads to failure of nuclear division.
  • 24.  Injectable forms of artemisinin derivatives are used for management of severe and complicated malaria.
  • 25. Drug Dosage Artesunate 2.4 mg/kg given IM/IV followed by 1.2 mg/kg after 12 hours then 1.2 mg/kg once daily for total duration of 5 days. Artemether 1.6 mg/kg IM followed by 1.6mg/kg daily for total of 6 injections (or) 1.6 mg/kg IM injection twice daily for 3 days, a total of 6 injections.
  • 26. Arteether 150 mg daily IM for 3 days in adults only Artemisinin 10mg / kg at 0 and 4 hours followed by 7 mg/kg at 24, 36, 48 and 60 hours.
  • 27.  They are used in case of uncomplicated falciparum and for severe and complicated falciparum malaria.
  • 28.  Tetracycline  Doxycycline  Clindamycin  Mechanism of action:  They are bacteriostatic antibiotics that bind to the 30s subunit of the ribosome and prevent the binding of tRNA to the ribosome, thus inhibiting bacterial protein synthesis.
  • 29.  Artesunate  Artemether  Arteether  Arterolane  Mechanism of action:  It interacts with heme resulting in the generation of free radicals that bind to the membrane protein and damages the parasite membrane.
  • 30.  Halofantrine  Lumefantrine  Mechanism of action:  Similar to that of chloroquine, quinine, and mefloquine, by forming toxic complexes with ferriprotoporphyrin Ix that damage the membrane of the parasite.
  • 32.  Atovaquone  Mechanism of action:  It appears to interfere with electron transport in protozoal mitochondria, inhibiting enzymes needed for the synthesis of nucleic acids and adenosine triphosphate.
  • 33.  Use cautionly in patients with  -renal failure  Severe GI problems  Neurologic  Cardiac diseases  History of depression  Hemolytic anemia
  • 34.  - impaired hepatic function  -Bronchial asthma or blood disorders.  Use cautionly in elderly patients with renal and cardiac problems.
  • 35.  Admister the drugs with food or milk.  Monitor liver function test to prevent toxic effect.
  • 36.  Explain importance of daily drug intake.  Educate take the medicine with food.  Instruct the prophylaxis measures as  -protective clothing  -Bed nets  -insect repellents.  -instruct to report adverse effects if any