Antimalarials

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*Quinine Sulphate*

#Formulations : 

Quinine Sulphate tablet IP

Quinine hydrochloride tablets

Quinine dihydrochloride injection IP

#Brand_Names : Vigotab, flue-foe, Qualaquin, Quinarsol - 300, Cinkona

#Pharmacological_Action : It is an erythrocytic schizontocide for all species of plasmodia. It does not makes an effect on pre erythrocytic stage. It directly kills vivax, ovale and malariae gamets. It is more effective than chloroquine.

#Side_Effects : It's toxicity is high and dose related; 8-10g taken in a single dose may be fatal. Other Side effects are-

Itching, angioedema of face and bronchoconstriction may develop.

#Therapeutic_Uses : used as antimalarial drugs.*Quinine Sulphate*

#Formulations :
Quinine Sulphate tablet IP
Quinine hydrochloride tablets
Quinine dihydrochloride injection IP


#Brand_Names : Vigotab, flue-foe, Qualaquin, Quinarsol - 300, Cinkona


#Pharmacological_Action : It is an erythrocytic schizontocide for all species of plasmodia. It does not makes an effect on pre erythrocytic stage. It directly kills vivax, ovale and malariae gamets. It is more effective than chloroquine.


#Side_Effects : It's toxicity is high and dose related; 8-10g taken in a single dose may be fatal. Other Side effects are-
Itching, angioedema of face and bronchoconstriction may develop.


#Therapeutic_Uses : used as antimalarial drugs.

*Primaquine Phosphate*

#Formulations : Primaquine tablet

#Brand_Names : Aralon, Primalex, Leoprime, Maliride

#Pharmacological_Action : It makes a big effect on pre erythrocytic stage of plasmodium falciparum. It has no effect on plasmodium vivax. The reactive intermediate metabolites of Primaquine are believed to generate inter parasitic  toxic oxidative species which disrupt the electron transport in plasmodial mitochondria.


#Side_Effects : abdominal pain, gastrointestinal upset, weakness or uneasiness in chest.


₹Take this drug with meals.


#Therapeutic_Uses : used as antimalarial drugs

*Chloroquine Phosphate*


#Formulations :
Chloroquine Phosphate tablet
Chloroquine Phosphate injection IP
Chloroquine sulphate tablet
Chloroquine sulphate Injection
Hydroxychloroquine sulphate tablet


#Pharmacological_Action : Plasmodia derive nutrition by digesting haemoglobin in their acidic vacuoles. Chloroquine is actively concentrated by sensitive intra erythrocytic plasmodia. Higher concentrations is found in infected RBCs than in non infected ones. By accumulating in the acidic vacuoles of the parasite and because of its weakly basic nature, it raises the vacuolar pH and thereby interferes with degradation of hemoglobin by parasitic lysosomes. Polymerization of toxic haeme generated from digestion of haemoglobin to non-toxic parasite pigment haemozoin is inhibited by the formation of Chloroquine heame complex. Haeme itself or its complex with chloroquine then damages the plasmodial membranes.

#Side_Effects : Nausea, vomiting, anorexia, uncontrollable itching, epigastric pain, uneasiness,

#Therapeutic_Uses : used as antimalarial drugs.

*Mefloquine*

#Formulations : Mefloquine Tablets IP

#Brand_Names : Mefque, Facital, Lariam, Confal

#Pharmacological_Action : It is intrinsically fast acting erythrocytic schizontocide but slower than chloroquine or quinone due to very slow and variable rate of absorption after oral ingestion.  It is effective against chloroquine sensitive as well as resistant plasmodia. A single dose controls fever and eliminates circulating parasites in infections caused by Plasmodium falciparum or plasmodium vivax in partially immune as well as non immune individuals.  

#Side_Effects : dizziness, nausea, vomiting, diarrhoea, abdominal pain, sinus bradycardia and Q-T prolongation. 

#Dose : 250mg per week (5mg/kg in children)

#Therapeutic_Uses : used as antimalarial

*Pyrimethamine*

#Formulations : Pyrimethamine tablet IP, BP
Pyrimethamine and sulphadoxine injection
Pyrimethamine and sulphadoxine tablet


#Brand_Names : Daraprim, Pyralfin, Onli-2


#Dose : 25- 50 mg /day

#Pharmacological_Action : It is a directly acting inhibitor of plasmodial DHFRase. Selective antimalarial action of pyrimethamine depends on high affinity for plasmodial enzyme. In contrast to trimethoprim, it has very poor action on bacterial DHFRase. Under the influence of pyrimethamine schizogony of malarial parasite in blood gradually stops. At high doses it inhibits Toxoplasma gondii.

#Side_Effects : nausea and rashes.


#Therapeutic_Uses : used as antimalarial drugs as combination with sulfonamides.

*Artemisinin*

#Formulations :
Artemisinin tablet
Artemisinin capsule
Artemisinin extract powder


#Pharmacological_Action : The endoperoxide bridge in its molecule appears to interact with heame in the parasite. Ferrous ion mediated cleavage of the bridge releases a highly reactive free radical species that binds to membrane proteins, causes lipid peroxidation, damages endoplasmic reticulum and ultimately results in the lysis of the parasite. Another line of evidence has shown that the artemisinin free radicals specifically inactivate a plasmodial SER calcium ATPase labelled Pf ATP6


#Side_Effects : nausea, vomiting, abdominal pain

#Therapeutic_Uses : used as antimalarial drugs