364 Section 9/ ChemotherapyIt is rapidly absorbed from intestine,
undergoes high hepatic first pass
metabolism. It readily crosses the blood
brain barrier.
Adverse effects are nausea, abdominal
pain, headache, dizziness.
Suramin (1 gm. each wk for 5 wk. IV or 1
gm. on day 1, 3, 7, 14, 21)
Melarsoprol 3.6 mg/kg/day IV for 3-4 days
Eflornithine 100 mg/kg IV every 6 hrs. for 14
days
Nifurtimox 8-10 mg/kg orally 3-4 months.
SURAMIN
It is a sulfated napthylamine and used in
first line therapy for early hemolymphatic
African trypanosomiasis. (caused by T. brucei
gambiense). It is very tight protein binding and
having short initial half life but terminal half
life is about 50 days and is excreted by kidney.
It is also used for chemoprophylaxis against
African trypanosomiasis. Adverse effects
include nausea, vomiting, fatigue, dermatitis,
fever, photophobia, haemolytic anaemia,
albuminuria and hematuria.
MELARSOPROL
Chemically it is trivalent arsenical used
for advanced CNS African trypanosomia-
sis. It is administered intravenously in pro-
pylene glycol and after administration it
rapidly excreted. It is highly toxic and used
only in advanced trypanosomiasis when
no alternative is there, these effects include
vomiting, fever, abdominal pain, renal and
cardiac disease and encephalopathy char-
acterized by cerebral edema, seizures, coma
(even death).EFLORNITHINE
It is an inhibitor of ornithine
decarboxylase and is used as second
therapy for advanced CNS African
trypanosomiasis. After oral or intravenous
administration, peak plasma level reached
rapidly and elimination half life is
approximately 3 hours.
It is effective against advanced T. brucei
gambiense infection. Adverse effect includes
vomiting, diarrhoea, leukopenia, thrombocy-
topenia, anemia and seizures.