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DRUG MOA PK CI ADR

4- Schizontocidal all Chloroquine


aminoquinolin species of malaria 50% bound to resistant Parenteral
es: Accumulates in plasma Liver damage administration
CHLOROQUI the acidic vesicle Slowly Neuro and can cause
NE of the parasite excreted in hemato disease hypotension
raises vesicular urine *not to be Cardiac
PH interfere with administer with depression
degradation of mefloquine arrhythmias
hemoglobin by ,amiodarone*
parasite lysozyme
Quinoline- Highly Dizziness
methanol: in chloroquine plasma Nausea
MEFLOQUIN resistance protein bound Mefloquine Vomiting
E Mefloquine and resistant SERIOUS
complex damages concentrated Interacts with Ataxia
the membrane of in different quinidine causes Anxiety
parasite organ. cardiac arrest Hallucinations
Erythrocytic primarily
schizontocide secreted in
bile
Cinchona Kills vivax Completely Pregnancy Cinchonism
alkaloid: gametes absorbed in causes Diarrhea
QUININE oral hemorrhage Flushing
Same as Metabolizes In patient with Fever
chloroquine certain Falciparum Tachypnea
fraction in malaria results
liver by hemoglobinuria
CYP3A4 and liver damage

Biguanides: Schizontocidal Partly Rapid resistance Mild abdominal


Proguanil Cycled in body to metabolized *SAFE IN upset
triazine derivative and excreted PREGNANCY* Vomiting
inhibits plasmodial in urine Occasional
DHFRase stomatitis
hematuria
Pyrimethami Inhibits Good but Epileptic Rashes
ne plasmoidal slow seizures Nausea
DHFRase ,doesnt absorption Liver problems occasional
need conversion from G.I.T Kidney diseases
to cyclic triazine Inadequate folic
Schizogony stops acid
Decreased bone
marrow function

Sulfonamide Schizontocidal Readily In pregnancy Abdominal pain


pyrimethamin Have effect In absorbed In G6-PD GI upset
e primary as well as after oral deficiency Weakness
secondary tissue ingestion condition TOXIC
Combination: phase of malarial POTENTIAL:
PRIMAQUIN parasite Dose related
E Highly active hemolysis
against Methaemoglobi
gametocyte and naemia
hypnozoites
Artemisinin Endoperoxide Prodrugs Antiarrhythmic Nausea
derivatives: bridge interacts drugs, Vomiting
ARTESUNAT with haeme and antidepressants, Abdominal pain
E iron mediated phenothizine Itching
cleavage of bridge causes cardiac Drug fever
releases a highly conduction
reactive species defect
of free radical
leading to
damage to
endoplasmic
reticulum