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Chapter: Modern Medical Toxicology: Miscellaneous Drugs and Poisons: Anti-Infectives

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Chloroguanide (Proguanil) - Antifungal

Chloroguanide is a biguanide derivative and is usually used in combination with chloroquine or atovaquone, for the prophy-laxis and treatment of acute, uncomplicated falciparum malaria, particularly in areas where chloroquine resistance has been reported.

Chloroguanide (Proguanil)

Chloroguanide is a biguanide derivative and is usually used in combination with chloroquine or atovaquone, for the prophy-laxis and treatment of acute, uncomplicated falciparum malaria, particularly in areas where chloroquine resistance has been reported. It is a prodrug that metabolises to cycloguanil, the active dihydrofolate reductase inhibitor antimalarial agent, and is administered orally.

Adverse effects are uncommon and manifest as occasional nausea and diarrhoea. Mouth ulceration, headaches, dizzi-ness, and skin rash have also been reported. Total alopecia was reported in several patients following chronic proguanil therapy. The severity of alopecia was directly proportional to the duration of proguanil use and appeared to be reversible upon discontinuation of the medication.

Overdose (more than 1 gm) may cause vomiting, abdominal pain, diarrhoea and haematuria. Large doses of proguanil may result in the transient appearance of epithelial cells and casts in the urine. Megaloblastic anaemia and pancytopenia have been reported in patients with severe renal impairment. Fatalities have not been reported.

Treatment is symptomatic and supportive. Monitor CBC as indicated in symptomatic patients. Monitor fluid and electrolyte status in patients with significant vomiting and/or diarrhoea.


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