MALARIA It is an infectious disease of humans caused by parasitis protozoans belonging to the genus plasmodium. It is endemic in most parts of India and other tropical countries. As per WHO, malaria causes one death every minute globally and about 40,000 annual deaths in India. The disease is transmitted by the bite of an infected female Anopheles mosquito. Four species of protozoa plasmodium can cause malaria which are P. falciparum, P. vivax, P. ovale and P. malariae. INTRODUCTION These are the drugs which are used for the treatment, prophylaxis and prevention of relapses of malaria. The treatment of malaria is available since 17 century. During those times, the bark of Cinchona tree was used in the crude form. Later in 1820, quinine was isolated from the bark. Since 1920, quinine and other drugs are commercially available in the market OBJECTIVES IN USE OF ANTIMALARIAL DRUGS The various objectives are: To prevent clinical attack of malaria. To treat clinical attack of malaria. To completely eradicate the parasite from the patient’s body. To cut down human to mosquito transmission. THERAPEUTIC CLASSIFICATION 1. CAUSAL PROPHYLACTICS: (Destroy parasite in liver cells and prevent invasion of erythrocytes) e.g. primaquine, pyrimethamine 2.BLOOD SCHIZONTOCIDES SUPPRESIVES (destroy parasites in the RBC and terminate clinical attacks of malaria): e.g. chloroquine, quinine, mefloquine, halofantrine, pyrimethamine 3. TISSUE SCHIZONTOCIDES used to prevent relapse: act vivax and P. ovale that produce replapses. E.g. primaquine 4. GAMETOCIDAL DRUGS: primaquine, chloroquine, quinine. 1. CHLOROQUINE It acts as erythrocytic schizontocide against all species of plasmodia. The parasite disappears from peripheral blood in 1-3 days. It control the clinical attacks of malaria within 1-2 days. It doesn’t have any gametocidal activity. It is bitter in taste, so patient should be advised ‘not to chew the tablet’ it is used for the treatment of malaria during pregnancy: no teratogenic effects have been reported. MECHANISM OF ACTION Its gets concentrated in the infected RBCs and then is actively taken up by the susceptible plasmodia. The chloroquine binds to the heme and forms chloroquine heme complex. Complex inhibits the formation of hemozoin and also damages the Plasmodium memberane PHARMACOKINETICS It is well absorbed orally. 50% of the drug is plasma protein bound, gets concentrated in liver, spleen, kidneys, lungs, skin and leukocytes. The plasma half life is 3-10 days, whereas the terminal half life is 1-2 months. On prolonged use, it gets accumulated selectively in the retina and causes ocular toxicity. It is partially metabolized in liver and slowly excreted in urine. INDICATIONS ADVERSE EFFECTS Clinical drug of choice for malaria. Extraintestinal amoebiasis. Rheumatoid arthritis Infectious mononucleosis. Mil

1. ANTI-
MALARIAL
DRUGS
NEHA BHARTI
M.Sc. N(MEDICAL SURGICAL NURSING)
NURSING TUTOR, SMVDCoN

2. MALARIA
• It is an infectious disease of humans caused by parasitis
protozoans belonging to the genus plasmodium.
• It is endemic in most parts of India and other tropical
countries.
• As per WHO, malaria causes one death every minute
globally and about 40,000 annual deaths in India.

3. • The disease is transmitted by the bite of an infected
female Anopheles mosquito.
• Four species of protozoa plasmodium can cause
malaria which are P. falciparum, P. vivax, P. ovale
and P. malariae.

4. INTRODUCTION
• These are the drugs which are used for the treatment,
prophylaxis and prevention of relapses of malaria.
• The treatment of malaria is available since 17 century.
During those times, the bark of Cinchona tree was used in
the crude form.
• Later in 1820, quinine was isolated from the bark.
• Since 1920, quinine and other drugs are commercially
available in the market

5. OBJECTIVES IN USE OF
ANTIMALARIAL DRUGS
• The various objectives are:
To prevent clinical attack of malaria.
To treat clinical attack of malaria.
To completely eradicate the parasite from the
patient’s body.
To cut down human to mosquito transmission.

7. THERAPEUTIC CLASSIFICATION
1. CAUSAL PROPHYLACTICS: (Destroy parasite in
liver cells and prevent invasion of erythrocytes)
e.g. primaquine, pyrimethamine
2.BLOOD SCHIZONTOCIDES SUPPRESIVES
(destroy parasites in the RBC and terminate clinical
attacks of malaria): e.g. chloroquine, quinine,
mefloquine, halofantrine, pyrimethamine
3. TISSUE SCHIZONTOCIDES used to prevent
relapse: act vivax and P. ovale that produce replapses.
E.g. primaquine
4. GAMETOCIDAL DRUGS: primaquine,
chloroquine, quinine.

8. CLASSIFICATION OF
ANTIMALARIAL DRUGS
1.
CHLOROQUINE
2 PRIMAQUIN 3. MEFLOQUIN
6. ARTEMETHER
4.
PYRIMETHAMINE
5. PROGUANOIL

9. 1. CHLOROQUINE
• It acts as erythrocytic schizontocide against all species of
plasmodia.
• The parasite disappears from peripheral blood in 1-3 days.
It control the clinical attacks of malaria within 1-2 days.

10. • It doesn’t have any gametocidal activity.
• It is bitter in taste, so patient should be advised ‘not
to chew the tablet’ it is used for the treatment of
malaria during pregnancy: no teratogenic effects have
been reported.

11. MECHANISM OF ACTION
Its gets concentrated in the infected RBCs and then is actively
taken up by the susceptible plasmodia.
The chloroquine binds to the heme and forms chloroquine
heme complex.
Complex inhibits the formation of hemozoin and also
damages the Plasmodium memberane

12. PHARMACOKINETICS
• It is well absorbed orally.
• 50% of the drug is plasma protein bound, gets
concentrated in liver, spleen, kidneys, lungs, skin and
leukocytes.
• The plasma half life is 3-10 days, whereas the terminal
half life is 1-2 months. On prolonged use, it gets
accumulated selectively in the retina and causes ocular
toxicity.
• It is partially metabolized in liver and slowly excreted in
urine.

13. INDICATIONS ADVERSE EFFECTS
• Clinical drug of choice for
malaria.
• Extraintestinal amoebiasis.
• Rheumatoid arthritis
• Infectious mononucleosis.
• Mild side effects like
nausea, vomiting, anorexia,
uncontrollable itching,
epigastric pain, uneasiness
are quite frequent.
• On prolonged use, it may
lead to loss of vision.

14. 1.i. AMODIAQUINE
Amodiaquine is having similar properties to chloroquin,
except:
• It is fast acting and less bitter in taste.
• It is useful in uncomplicated falciparum malaria.
• In combination with artesunate, it is the first line treatment
of falciparum malaria.

15. • Itching is less common with it, other side effects are
same as that of chloroquine.
• It is given in a dose of 25-30mg/kg over 3 days for
the treatment of acute attack of malaria.

16. 2. PRIMAQUINE
• It is a poor erythrocytic schizontocide but more active
against P. falciparum.
• It differs from all other available antimalarial in having an
additional effect on primary as well as secondary hepatic
phases on the malarial parasite.
• It also highly active against gametocytes.

17. • Mechanism Of Action is not clearly known.
• Pharmacokinetics: it is given orally and has rapid and
complete absorption.
• Metabolized in liver and excreted slowly in urine. Its
half life is 6-8 hours and excreted in urine within 24
hrs.

18. INDICATIONS ADVERSE EFFECTS
• Indicated for radical cure of
relapsing malaria caused by P.
Ovale and P. Vivax. In India
15mg/day for 2 weeks is given
along with full curative dose of
Chloroquine .
• Falciparum malaria: a single 45
mg dose of primaquine is given
with the curative dose of
chloroquine to kill the gametes
and cut down transmission to
mosquito.
• Mild side eefcts are Nausea,
Vomiting, Anorexia and
epigastric pain.
• It should not be given in
pregnancy, because the fetus is
deficient in G6PD.

19. 3. MEFLOQUINE
• Mefloquine is a fast acting erythrocytic schizontocide, but
slower than chloroquine.
• It is effective against choloquine sensitive as well as
resistant Plasmodium.
• It has good activity against Chloroquine resistant P.
falciparum.

20. • It is bitter in taste, so patient should be advised ‘not
to chew the tablet’
MECHANISM OF ACTION: Similar to chloroquine,
it accumulates in the infected RBC’s binds to hence and
this complex damages the cell memberanes of parasite.

21. PHARMACOKINETICS
• It is given orally and is absorbed very slowly.
• It is highly plasma protein bound and gets
concentrated in various organs such as liver, lungs
and intestine.
• It is metabolized in liver and excreted in bile.
• It’s half life is long i.e. 2-3 weeks

22. INDICATIONS ADVERSE EFFECTS
• Multi drug resistance P. Falciparum
malaria.
• In conbination of artesunate based
combination therapy for
uncomplicated falciparum including
chloroquine resistant and
chloroquine+sulfa pyrimethamine
resistant cases.
• For the prophylaxis of malaria among
travellers to areas with multidrug
resistance;5mg/kg(adults 250mg) per
week is started preferably 1-2 weeks
before travel.
• Mild side effects are Nausea,
Vomiting, anorexia, epigastric pain.
• Some patients may experience
neuropsychiatric reactions i.e.
disturbed sense of balance, ataxia,
errors in operating machinery, These
reactions subside after 2-3 weeks of
discontinuation of treatment.

23. 4. PYRIMETHAMINE
• It is a slow acting erythrocytic schizontocide for P.
Falciparum..
• It has good but slow oral absorption.
• It is more potent and relatively safer than Proguanil.
• It is excreted slowly in nature.
• It is used in combination with sulfonamide for
chloroquine resistant P.Falciparum.

24. 5. PROGUANIL
• It is pre erythrocytic schizontocide for P. Falciparum and
erythrocytic schizontocide for both P. Falciparum and P.
Vivax.
• It is a prodrug and the active metabolite is cycloguanil.
• MECHANISM OF ACTION: It inhibits the plasmodial
dihydrofolate reductase thymidylate synthase in parasite,
thereby exerting the cidal effect.

25. • PHARMACOKINETICS: It is given orally and
having slow but complete absorption. It is
metabolized in liver and excreted in urine. Its half life
is 16-20 hours.

26. • ADVERSE EFFECTS: It is well tolerated with mild
abdominal discomfort. Rarely vomiting, stomatitis,
hematuria, rashes and transient loss of hair may be
seen.
• INDICATIONS: It is used in prophylaxis and
treatment of Chloroquine resistant P. Falciparum
malaria.

27. 6. ARTEMISININ DERIVATIVES
• It is the active ingredient of the chinese traditional medicine
‘Quinghaosu’ which is obtained from the planet Artemisia
Annua.
• Ms Tu YOUYOU was awarded half nobel prize in 2015 for
the discovery of Artemisinin.

28. • These derivatives are better tolerated, safer and
highly efficacious.
• They are very potent and rapidly acting anti-malarial
drugs.
• They also have good gametocidal activity but do not
affect hepatic forms.
• They are effective in erythrocytic stage of all malarial
parasites.

29. • MECHANISM OF ACTION: Exact mechanism is
unknown.
• INDICATIONS:
Uncomplicated falciparum malaria.
Severe and complicated falciparum malaria.

30. ADVERSE EFFECTS:
• Mild side effects are nausea, vomiting,
• Abdominal pain, itching

31. PHARMACOKINETICS
• Artemether is lipid soluble and is administered by oral or
IM administration only.

32. QUININE
• It is an erythrocyte schizontocide for all species of
plasmodia.
• It is effective against Chloroquine and multidrug resistance
strains of P. falciparum.
• It is less effective and more toxic than chloroquine.
• Mechanism of action is same that of chloroquine.
• PHARMACOKINETICS: It is given orally and is absorbed
rapidly and completely.
It is 70% plasma protein bound.
It is metabolized in liver and excreted in bile.
Its half life is 10-12 hrs.

33. INDICATIONS
• Uncomplicated Chloroquine resistant P. Fa,ciparum
malaria.
• Complicated malaria

34. ADVERSE EFFECTS
• The adverse effects are generally dose related.
• Mild side effects are Nausea, vomiting, anorexia, epigastric
pain.
• At higher doses, Patient experiences nausea vomiting,
headache, tinnitus, vertigo, visual defects and mental
confusions.

35. PROPHYLACTIC THERAPY IN
INDIA
• DOXYCYCLINE 100mg daily starting ‘day before
travelling to endemic areas and taken ‘till 4 weeks after
return from endemic area’ for chloroquine resistant P.
Falciparum.
• MEFLOQUINE 250mg started 1-2 weeks before and taken
weekly till 4 weeks return from endemic area has been used
for areas where Chloroquine resistant P. Falciparum is
prevelant.
• In India, use of mafloquine for prophylaxis is not allowed
among indians residen, but may be used by forein travellers.

36. NURSING IMPLICATIONS
• Nurse should enquire the patient about unusual visual and
auditory sensations.
• Drug should be given with food to decrease the GI
irritation.
• Monitoring of urine output is mandatory during antimalarial
therapy because it leads to renal damage.
• Closely monitor the vital signs.
• Closely monitor the blood glucose levels in patients
receiving quinine therapy, as rapid iv injection can cause
hypoglycemia.
• Nurse should check that antimalarial regimen is followed
properly.