Antimalarials

The three antimalarials available at this time for the treatment of CLE are chloroquine, hydroxychloroquine, and quinacrine. Overall, these drugs are relatively safe, but there are some laboratory abnormalities to consider. Chloroquine slightly decreases creatinine levels in half of its users, most likely by raising plasma aldosterone levels (Musa-bayane 1994).Forty-five percent of hydroxychloroquine is excreted in the kidneys,and the drug is associated with up to a 10% decrease in creatinine clearance (Landewe et al. 1995). Therefore, the dosage should be adjusted for patients with renal impariment. Antimalarials also have a beneficial antihyperlipidemic effect. Hydroxychloroquine induces a 15%-20% decrease in total cholesterol, triglyceride, and LDL levels (Wallace et al. 1990). It is associated with only one case of agranulocytosis, in a patient who was given 1,200 mg daily,which is up to six times the current recommended dosage (Polano et al. 1965), and a handful of case reports of various blood dyscrasias, such as aplastic anemia, leukopenia, thrombocytopenia, and hemolysis in individuals with glucoses-phosphate dehydrogenase (G-6-PD) deficiency.

Chloroquine has been implicated in rare reports of G-6-PD deficiency hemolysis (Choudhry et al. 1978) and with agranulocytosis (Kersly and Palin 1959).Since chloro-quine is known to concentrate in the liver, it should be used with caution in patients with hepatic disease or alcoholism or in conjunction with known hepatotoxic drugs.

The prevalence of aplastic anemia among US soldiers in the Pacific during World War II rose from 0.66 to 2.84 per 100,000 after quinacrine's introduction (Custer 1946). This represented 58 patients, 48 of whom received quinacrine. Of these, 16 were associated with overdoses, and two received marrow-suppressant drugs concurrently (Wallace 1989). It is therefore recommended that patients receiving antimalarial treatment have a complete blood cell count and a serum creatinine test every few months during therapy. Patients taking chloroquine or hydroxychloroquine should undergo ophthalmologic examination at 6- or 12-month intervals, respectively.

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