Dosing & Uses
Dosage Forms & Strengths
powder for injectable solution
- 1g (reconstitute to100mg/mL)
Trypanosomiasis
100-200 mg (test dose) IV, then 1 g IV on days 1, 3, 7, 14, 21
TB Gambiense
10 mg/kg IV q5day to total of 12 injections
May repeat after 1 month; use concomitantly with tryparsamide
Refractory Prostate Cancer (Orphan)
Treatment of hormone-refractory prostate cancer
Orphan indication sponsor
- Warner-Lambert Company
- Parke-Davis Pharmaceutical Research Division; 2800 Plymouth Rd; Ann Arbor, MI 48105-2430
Adverse Effects
Frequency Not Defined
Vomiting
Urticaria
Paresthesia
Peripheral neuropathy
Kidney damage
Blood dyscrasias
Polyuria
Polydipsia
Pancytopenia
Shock
Optic atrophy
Warnings
Contraindications
Hypersensitivity
Caution
Proteinuria and renal toxicity reported with use
Avoid use in renal or hepatic impairment
Pregnancy & Lactation
Pregnancy Category: no human studies conducted
Lactation: not known if excreted in breast milk
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Trypanocidal activity; inhibits enzymes involved with the oxidation of reduced NADH
Pharmacokinetics
Protein binding: 99.7%
Absorption: Poor
Vd: 90 ± 21 L (terminal phase); 38 ± 8 L (Steady state)
Half-life: 36-60 days (terminal phase)
Peak plasma concentration: >100 mcg/mL
Metabolism: None
Excretion: Urine
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Formulary
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