Melarsoprol

Definition
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Antiprotozoal agent, organic arsenic compound.

Pharmacodynamics (Effect)
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Binding to essential SH groups of enzymes.

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Spectrum of action
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Trypanosoma brucei gambiense and rhodiense.

Indication
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Cerebral stage of sleeping sickness.

Dosage and method of use
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3 times 0.6-1.2 mg/kg bw/day for 3 days, repeated after 10-21 days Because of the danger of the Herxheimer reaction, treatment is often carried out according to the scheme (see Table 1) in combination with suramin or pentamidine diisethionate.

Undesirable effects
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At first administration in 60% fever. Albuminuria, vomitus, myocardial damage, hypertension, colic, Herxheimer reaction, encephalopathy (occurs in 10%, fatal in up to 40%), peripheral neuropathy.

Notice. Because of possible life-threatening complications, the preparation should only be used in the clinic!

Contraindication
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None, because of the lethality of the disease.

Preparations
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Arsobal, Mel B (available through the international pharmacy)

Tables
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Dosage of melarsoprol in combination therapies

Day	Preparation	Dose [mg/kg bw]	Preparation	Dose [mg/kg bw]	Preparation	Dose [mg/kg bw]
	Kenya/Sambia (Tr. b. rhod.)		Uganda/Tanzania (Tr. b. rhod.)		Ivory Coast (Tr. b. gamb.)
1.	Suramin	5	Suramin	5	Pentamidine i.m.	4
2.	-	-	-	-	-	-
3.	Suramin	10	Suramin	10	Pentamidine i.m.	4
4.	-	-	-	-	Melarsoprol	1,2
5.	Suramin	20	Melarsoprol	1,8	Melarsoprol	2,4
6.	-	-	Melarsoprol	2,2	Melarsoprol	3,6
7.	Melarsoprol	0,36	Melarsoprol	2,56	-	-
8.	Melarsoprol	0,72	-	-	-	-
9.	Melarsoprol	1,1	-	-	-	-
10.	-	-	-	-	-	-
11.	-	-	-	-	-	-
12.	-	-	-	-	-	-
13.	-	-		-	-	-
14.	-	-	Melarsoprol	2,56	-	-
15.	-	-	Melarsoprol	2,9	-	-
16.	Melarsoprol	1,4	Melarsoprol	3,26	-	-
17.	Melarsoprol	1,8	-	-	Melarsoprol	1,2
18.	Melarsoprol	1,8	-	-	Melarsoprol	2,4
19.	-	-	-	-	Melarsoprol	3,6
20.	-	-	-	-	Melarsoprol	3,6
21.	-	-	-	-	-	-
22.	-	-	-	-	-	-
23.	-	-	Melarsoprol	3,6	-	-
24.	-	-	Melarsoprol	3,6	-	-
25.	Melarsoprol	2,2	Melarsoprol	3,6	-	-
26.	Melarsoprol	2,9	End		-	-
27.	Melarsoprol	3,6			-	-
28.	-	-			-	-
29.	-	-			-	-
30.	-	-			Melarsoprol	1,2
31.	-	-			Melarsoprol	2,4
32.	-	-			Melarsoprol	3,6
33.	-	-			Melarsoprol	3,6
34.	Melarsoprol	3,6			End
35.	Melarsoprol	3,6
36.	Melarsoprol	3,6
	End