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. Author manuscript; available in PMC: 2011 Nov 1.
Published in final edited form as: Curr Top Med Chem. 2011;11(10):1255–1274. doi: 10.2174/156802611795429167

Table 1.

Current Drugs for the treatment of HAT

Drug Use Limitations Mechanism of
action
Dosing
Suramin T. b. rhodesiense
early stage only
Does not cross
the blood brain
barrier; toxicity
unknown IV injection 100- 200
mg test dose then 1 g
given on days 1, 3, 7,
14 and 21
Pentamidine T. b. gambiense, early
stage only
Does not cross
the blood brain
barrier
unknown IM injection in single
doses of 4.0 mg/kg per
day for 7 days
Melarsoprol Late Stage T. b
rhodesiense; Late
stage T. b. gambiense
if eflornithine is
unavailable
Severe toxicity
– causes
reactive
enceplapthy
resulting in
death in up to
6% of patients
unknown T.b. rhodesiense, 3
series of 3 daily doses
IV with a 7 day rest
period in between: 1.8,
2.7 and 3.6 mg/kg on
days 1, 2, and 3
respectively with
subsequent series at 3.6
mg/kg daily; T. b.
gambiense, 2.2
mg/kg/day IV for 10
days
Eflornithine Late state T. b
gambiense
Not effective
against T. b
rhodesiense;
difficult dosing
regime
requiring
prolong i.v.
administration
Mechanism
based inhibitor
of ornithine
decarboxylase
400 mg/kg/day in
divided doses IV every
6 h for 14 days
Nifurtimox/
Eflornithine
(NECT)
Late stage T. b
gambiense
Not effective
against T. b
rhodesiense
MOA of
nifurtimox –
activated by a
NADH-
dependent
mitochondrial
nitroreductase
leading to the
generation of
intracellular
free
radicals[169]
eflornithine 400 mg/kg/
day IV in divided doses
every 12 h for 7 days
and nifurtimox 15
mg/kg/day orally every
8 h for 10 days