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Quinacrine
- indication:For the treatment of giardiasis and cutaneous leishmaniasis and the management of malignant effusions.
- pharmacologypharmacology:
- mechanism: The exact mechanism of antiparasitic action is unknown; however, quinacrine binds to deoxyribonucleic acid (DNA) in vitro by intercalation between adjacent base pairs, inhibiting transcription and translation to ribonucleic acid (RNA). Quinacrine does not appear to localize to the nucleus of Giaridia trophozoites, suggesting that DNA binding may not be the primary mechanism of its antimicrobial action. Fluorescence studies using Giardia suggest that the outer membranes may be involved. Quinacrine inhibits succinate oxidation and interferes with electron transport. In addition, by binding to nucleoproteins, quinacrine suppress the lupus erythematous cell factor and acts as a strong inhibitor of cholinesterase.
- toxicity: Oral, rat: LD<sub>50</sub> = 900 mg/kg; Oral, mouse: LD<sub>50</sub> = 1000 mg/kg. Symptoms of overdose include seizures, hypotension, cardiac arrhythmias, and cardiovascular collapse.
- absorprion: Absorbed rapidly from the gastrointestinal tract following oral administration.
- halflife: 5 to 14 days
- roouteelimination:
- volumedistribution:
- clearance: