>10%:

Central nervous system: Fever (78%), headache; palmar and plantar hyperesthesia occur at levels >350 mcg/mL

Dermatologic: Rash (48%)

Endocrine & metabolic: Adrenal insufficiency (23%), patients usually require adrenocorticoid therapy; transaminases increased (transient 14%)

Gastrointestinal: Nausea (20%), vomiting (35%), metallic taste

Hematologic: Leukopenia, agranulocytosis, thrombocytopenia (12% to 26%), usually not dose-limiting

Hepatic: Transient increases in bilirubin levels (14%)

Neuromuscular & skeletal: Paresthesias, peripheral neuropathies (33%), may be dose-limiting; areflexia and paralysis may occur at levels >375 mcg/mL

Ocular: Keratopathy (11%), possibly related to dose and/or rate of infusion

Renal: Mild, nondose-limiting, proteinuria (33%); decrease in creatinine clearance

1% to 10%:

Gastrointestinal: Stomatitis (5%)

Neuromuscular & skeletal: Myalgia (3%)

<1%: Abdominal pain, atrial fibrillation, diarrhea; coagulopathy (dose-limiting, inhibits factors V, VIII, IX, X, XI, and XII)

Immediate hypersensitivity reactions, including nausea, vomiting, shock, and loss of consciousness (0.1% to 0.3%); a 100-200 mg (10-20 mg in children) test dose prior to the first treatment cycle is occasionally given

Absorption: Not absorbed orally

Distribution: Vd: 31-46 L; does not penetrate the CNS

Protein binding: >99%

Half-life elimination: Triphasic, terminal half-life: 50 days

Excretion: Urine (as unchanged drug); bile (small amounts)

Prostate cancer: 350 mg/m²/day continuous I.V. infusion for 7 days, then titrated to a plasma level of 250-300 mcg/mL for 7 days, repeated after an 8-week interval.

Titrate to a plasma level of 300 mcg/mL for 14 days, repeat after an 8-week interval.

Chemosensitizing agent: Doses are not yet established; anticipated to be significantly lower than cancer treatment doses.

Dosage adjustment in renal impairment: Dosage reductions have been suggested for "severe" renal dysfunction; however, specific guidelines have not been published.

Dosage adjustment in hepatic impairment: Dosage reductions of 50% to 75% have been suggested for "severe" hepatic dysfunction; however, specific guidelines have not been published.

Eisenberger MA and Reyno LM, "Suramin,"Cancer Treat Rev, 1994, 20(3):259-73.

Larsen AK, "Suramin: An Anticancer Drug With Unique Biological Effects, Cancer Chemother Pharmacol, 1993, 32(2):96-8.

Stein CA, "Suramin: A Novel Antineoplastic Agent With Multiple Potential Mechanisms of Action," Cancer Res, 1993, 53(10 Suppl):2239-48.

Voogd TE, Vansterkenburg EL, Wilting J, et al, "Recent Research on the Biological Activity of Suramin,"Pharmacol Rev, 1993, 45(2):177-203.