Overdose : מינון יתר

12      OVERDOSAGE
Dialysis is not helpful as KOSELUGO is highly protein bound and is extensively metabolized.



13      DESCRIPTION
Selumetinib is a kinase inhibitor. The chemical name is 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-6- [(2-hydroxyethoxy)carbamoyl]-1-methyl-1H-benzimidazol-3-ium hydrogen sulfate. The molecular formula for selumetinib sulfate is C17H17BrClFN4O7S and the relative molecular mass is 555.76 g/mol.
Selumetinib sulfate has the following structural formula:

H
HO                   N
Cl
H
N
.H2SO4

Br

Selumetinib sulfate is a white to yellow monomorphic crystalline powder that exhibits a pH dependent solubility. Selumetinib sulfate is freely soluble at pH < 1.5, sparingly soluble in the pH range at 1.5 to 3 and slightly soluble at pH > 3. Selumetinib sulfate has two ionizable functions with pKa values of 2.8 and 8.4.
KOSELUGO (selumetinib) 10 mg capsules for oral use, contain 10 mg selumetinib (equivalent to 12.1 mg selumetinib hyd-sulfate) and the excipient, vitamin E polyethylene glycol succinate. The capsule shell contains hypromellose, purified water, titanium dioxide, potassium chloride, and carrageenan. The capsule is imprinted with black ink that contains shellac, iron oxide black, propylene glycol and ammonium hydroxide.
KOSELUGO (selumetinib) 25 mg capsules for oral use, contain 25 mg selumetinib (equivalent to 30.25 mg selumetinib hyd-sulfate) and the excipient, vitamin E polyethylene glycol succinate. The capsule shell, body and cap contain hypromellose, purified water, titanium dioxide, potassium chloride, carrageenan, FD&C blue 2 and ferric oxide yellow. The capsule is imprinted with black ink that contains White shellac, FD&C Blue Aluminium lake, Ferric oxide yellow, Ferric oxide red, Carnauba wax and Glyceryl monooleate.