The document discusses various aspects of antimalarial drugs, including: 1) It describes the classification of antimalarials into different categories such as aminoquinolines, quinoline-methanols, cinchona alkaloids, and artemisinin derivatives. 2) It explains the uses of antimalarials for chemoprophylaxis, clinical cure of acute infections, radical cure to eliminate dormant liver stages, and as gametocides. 3) It provides recommendations for treatments of uncomplicated and severe malaria, including first-line and second-line options, and considerations for use during pregnancy.

1. ANTI -MALARIALS
MALARIA AND ITS PARASITES
LIFE CYCLE OF MALARIAL PARASITES
CLASSIFICATION OF ANTIMALARIALS
chemoprophylaxis
CLINICAL CURE [Acute Attacks]
RADICAL CURE
GAMETOCIDAL
TREATMENT OF UNCOMPLICATED MALARIA [2ND LINE ]
TREATMENT OF SEVERE AND COMPLICATED MALARIA [ACT Regimens ]
 TREATMENT OF UNCOMPLICATED MALARIA [ 1ST LINE] [ACT Regimens ]
Choice of drug in pregnancy
BY
K.MUTHUSELVAN
DOING PHARM.D

2. ANTI MALARIAL
What is malaria ?
Malaria is a life-threatening disease caused by parasites belonging
to the genus plasmodium that are transmitted to people through the bites of
infected anopholine mosquitos.
The 4 plasmodium species are plasmodium falciparum ,plasmodium
vivax ,plasmodium ovale and plasmodium malariae.
The symptoms includes fever, shivering ,pain in joints, headache, repeated
vomitting , generalised convulsions and coma.
The plasmodium species are endemic in most parts of India and tropical
countries .It is one of the major health issue.

3. LIFE CYCLE OF MALARIAL PARASITE IN MAN

4. CLASSIFICATION OF ANTI MALARIALS
 4 AMINOQUINOLINES: Chloroquine ,amodiaquine
 Quinoline-methanol : Mefloquine
 Cinchona alkaloid: Quinine ,quinidine
 Biguanide : Proguanil
 Diaminopyrimidine:Pyrimethamine
 8 amino quinoline : Primaquine
 Sulfonamides : Sulfadoxine ,sulfamethopyrazine
 Antibiotics: Tetracycline ,doxycycline,clindamycin
 Sesquiterpine lactones: Artemisinins derivatives
 Amino alcohols: Halofantrine ,lumefantrine
 Napthoquinone : Atovoquone

5. PROPERTIES OF ANTI MALARIALS

6. CHEMO - PROPHYLAXIS
 The schizontocides which suppress the erythrocytic
phase and thus attacks of malarial fever.
 Common Regimen includes
 Mefloquine 250mg started 1-2 weeks before and
taken weekly till 4 weeks after return
 Doxycycline 100mg daily day before and taken till
4 weeks after return from endemic areas
 Atavoquone 250 mg+proguanil 100 mg { Malarone}
daily and 7 days after exposure

7. CLINICAL CURE
The erythrocytic schizontocides are used to terminate an
episode of malarial fever.They act on the erythrocytic
forms of the plasmodium.
The avalilable drugs can be divided into
A) High efficacy drugs : artemisinins, CQ , AQ , Qunine,
Mefloquine, halofantrine ,lumefantrine and atovoquone
B) Low efficacy drugs : Proguanil,pyrimethamine
,sulfonamides, tetracycline and clindamycin [used as
in combination ]

8. RADICAL CURE
It is needed in relapsing malaria .in the case of vivax
and ovale malaria , drugs which attack the exo-
erythrocytic stege [hypnozoites] given together with
clinical curative to eradicate the parasites
completely.
Choice of drug here
• Primaquine 15mg daily for 14 days .
• Tafenoquine , a new long acting exo erythrocytic
schizontocide.

9. GAMETOCIDAL
Some drugs can also destroy gametocytes ,
preventing transmission by the mosquito and thus
diminishing the human reservoir of the disease .
Drug of choice here
• Primaquine 45 mg [0.75mg/kg] given after the
clinical cure .
• Proguanil or pyrimethamine may act on the
gametes .

10. TREATEMENT OF UNCOMPLICATED MALARIA
 A.vivax(also ovale ,malarie)malaria
1.chloroquine 600 mg(10mg/kg) followed by 300mg (5mg/kg) after 8 hours and then for next 2
days(total 25mg/kg over 3 days)+primaquine 15mg (0.25mg/kg)daily x 14days
In occasional case of chloroquine resistance
2.quinine 600mg (10mg/kg) 8 hrly x 7days + doxycycline 100mg daily x 7days or
+ clindamycin 600mg 12hrly x 7 days
+ primaquine 15mg (0.25mg/kg)daily x 14days
or
artemisinin-based comination therapy see below
+ primaquine 15mg (0.25mg/kg)daily x 14days
o B.chloroquine-sensitive falciparum malaria
1.chloroquine 600 mg {as above }+primaquine 45mg (0.75mg/kg)single dose (as gametocidal)
o C.chloroquine-resistant falciparum malaria
1.Artesunate 100mg bd(4mg/kg/day) x 3days + sulfadoxine 1500mg(25mg/kg) + pyrimethamine
75mg (1.25mg/kg) single dose or
2. Artesunate 100mg bd(4mg/kg/day) x 3days + mefloquine 750mg (15mg/kg) on second day and
500 mg (10mg/kg) on 3rd day or
3.Artemeter 80mg + lumifantrine 480mg twice daily x 3days (child 25-35 kg bw ¾ dose ; 15-25 kg
bw ½ dose ; 5-15 kg bw ¼ dose )
4.Quinine 600mg (10mg/kg) 8hrly x 7 days + doxycycline 100mg daily x 7 days or + clindamycin
600mg 12 hrly x 7 days

11. ACT REGIMENS FOR UNCOMPLICATED
FALCIPARUM MALARIA
 Artesunate – Sulfadoxine + Pyrimethamine
Artesunate 100mg BD [100mg /kg/day] X 3 days + sulfadoxine 1500
mg [25mg/kg] and pyrimethamine 75 mg [1.25 mg/kg ] single dose
 Artemether [80 mg BD] – lumefantrine [480mg BD] X 3 days to be
taken with fatty meal
 Artesunate 100 mg BD[4mg /kg /day] – Mefloquine 750 mg [15 mg
/kg] on 2nd day and 500 mg [10 mg / kg ] on 3rd day
 DHA 120 mg [2mg/kg] +Piperaquine 750 mg daily X 3 days
 Artesunate200 mg[4mg/kg] – Amodiaquine 600mg [10mg/kg ] per
day X 3 days
 Artesunate 25mg/50mg / 100mg + Amodiaquine 67.5/135/270mg
fixed dose combination tablets have been approved in india

12. TREATMENT OF SEVERE AND COMPLICATED
MALARIA
1. Artesunate: 2.4mg/kg i.v or i.m followed by 2.4 mg/kg after 12 hrs
and 24 hrs and then once daily for 7 days .
2. Artemether : 3.2 mg/kg i.m 1st day followed by 1.6mg/kg daily for 7
days .
3. Arteether : 3.2 mg/kg im 1st day , followed by 1.6mg/kg daily for
next 4 days.
4. Quinine dil Hcl: 20mg/kg diluted in 10mg/kg 5% dextrose /dextrose
saline and infused i.v over 4 hours followed by 10mg /kg
[maintenance dose] i.v infusion over 4hours [adults] and 2hours
[children] every 8 hours , untill patient can swallow .

13. CHOICE OF DRUG IN PREGNANCY
 Chemoprophylaxis
intermittent preventive therapy (IPTp) as
Pyrimethamine (75mg) + sulfadoxine (1500mg) single
dose in early 2nd trimester in high endemic areas
 Clinical cure
1) Quinine 600mg TDS X 7days +clindamycin 300
mg TDS/QID (20mg/kg) for 7days . In all trimester
.esp 1st
2) Artemisinin combination therapy (ACT) as 3rd
regimen in 2nd and 3rd trimester .

14. CHLOROQUINE

15. ARTEMISININS

16. Thank you