ANTI -MALARIALSMALARIA AND ITS PARASITESLIFE CYCLE OF MALARIAL PARASITESCLASSIFICATION OF ANTIMALARIALSchemoprophylaxisCLINICAL CURE [Acute Attacks]RADICAL CURE GAMETOCIDALTREATMENT 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

BYK.MUTHUSELVAN DOING PHARM.D

ANTI MALARIALWhat 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.

LIFE CYCLE OF MALARIAL PARASITE IN MAN

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

PROPERTIES OF ANTI MALARIALS

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

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 ]

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.

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 .

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 14daysIn 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 14dayso 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 malaria1.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 or3.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

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

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 .

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 .

CHLOROQUINE

ARTEMISININS

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