Please enable JavaScript.
Coggle requires JavaScript to display documents.
MELARSOPROL (ADVERSE REACTION/SIDE EFFECT :warning: (Hypertension,…
MELARSOPROL
-
INDICATION
Treatment of African trypanosomiasis caused by Trypanosoma brucei gambiense or T. b. rhodesiense in patients with late or chronic disease with central nervous system (CNS) involvement.
-
ADME
Distribution:
Crosses the blood-brain barrier; cerebrospinal fluid (CSF) concentration is about 50-fold lower than that in the serum.
Mean CSF concentration is about 30 ng/mL.
Metabolism:
One such metabolite, Mel Ox, reaches maximum plasma levels about 15 minutes after melarsoprol injection.
Absorption:
Fairly well absorbed after oral administration but is not normally given by this route; usually given parenterally.
Elimination:
Renal—Rapidly excreted in the urine within days of administration; total clearance is about 50 mL per minute.
PRECAUTION
-
Intercurrent infections, such as pneumonia and malaria, should be treated before melarsoprol is administered.
-
Cannot be given to patient deficient in glucose-6-phosphate dehydrogenase as in can cause severe haemolytic reactions have occurred in patients .
This medication should be given in the supine position and in a fasting state to minimize gastrointestinal disturbances
After melarsoprol treatment, patients should be followed up every 6 months for 2 to 3 years and the CSF examined on each occasion.
DOSE
-
PEDIATRIC
-
-
0.36 mg per kg per day,gradually increasing to 3.6 mg per kg per day at intervals of one to five days
MOA
- It work by disruption of energy generation in the trypanosome parasite due to the high affinity of melarsoprol for sulfhydryl groups.
- These groups form the active sites of many enzymes (especially the kinases), and are involved in the maintenance of the secondary and tertiary structures of proteins.
3.Once inside the trypanosome, melarsoprol inactivates the enzyme, pyruvate kinase, which is present in the cytoplasm. 4. This causes inhibition of the synthesis of adenosine triphosphate (ATP), which is the energy required for the survival of the parasite.
- The trypanosome eventually dies as a result of diminished energy production.
-
-
-
-
-
-
