Overdose : מינון יתר

11    OVERDOSAGE
No specific antidote is available for overdosage with Trikafta. Treatment of overdosage consists of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient.

12     DESCRIPTION
Trikafta is a co-package of elexacaftor, tezacaftor and ivacaftor fixed-dose combination tablets and ivacaftor tablets. Both tablets are for oral administration.

The elexacaftor, tezacaftor and ivacaftor fixed-dose combination tablets are available as an orange, film-coated tablet containing 100 mg of elexacaftor, 50 mg of tezacaftor, 75 mg of ivacaftor, or light orange, film-coated tablet containing 50 mg elexacaftor, 25 mg of tezacaftor, 37.5 mg of ivacaftor. The fixed-dose combination tablet contains the following inactive ingredients: microcrystalline cellulose, croscarmellose sodium, hypromellose acetate succinate (HPMCAS), hypromellose (HPMC), magnesium stearate, and sodium lauryl sulfate (SLS). The film coat of the 100 mg elexacaftor/50 mg tezacaftor/75 mg ivacaftor tablet contains opadry orange 20A130036. The film coat of the 50 mg elexacaftor/25 mg tezacaftor/37.5 mg ivacaftor tablet contains opadry orange 20A130039.

The ivacaftor tablet is available as a light blue, film-coated tablet containing 150 mg or 75 mg of ivacaftor and the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, hypromellose acetate succinate (HPMCAS), croscarmellose sodium, magnesium stearate, sodium lauryl sulfate (SLS), and colloidal silicon dioxide. The tablet film coat contains polyvinyl alcohol, titanium dioxide, PEG 3350, talc, FD&C Blue #2/indigo carmine aluminum lake, and carnauba wax.
The printing ink contains shellac, iron oxide black, propylene glycol, and ammonium hydroxide.

The active ingredients of Trikafta are described below.

Elexacaftor
Elexacaftor is a white solid that is practically insoluble in water (<1 mg/mL). Its chemical name is N-(1,3-dimethyl-1H-pyrazole-4-sulfonyl)-6-[3-(3,3,3-trifluoro-2,2- dimethylpropoxy)-1H-pyrazol-1-yl]-2-[(4S)-2,2,4-trimethylpyrrolidin-1-yl]pyridine-3-carboxamide. Its molecular formula is C26H34N7O4SF3 and its molecular weight is 597.66. Elexacaftor has the following structural formula:



Tezacaftor
Tezacaftor is a white to off-white solid that is practically insoluble in water (<5 microgram/mL). Its chemical name is 1-(2,2-difluoro-2H-1,3-benzodioxol-5-yl)-N-{1- [(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl}cyclopropane-1-carboxamide. Its molecular formula is C26H27N2F3O6 and its molecular weight is 520.50. Tezacaftor has the following structural formula: 


Ivacaftor
Ivacaftor is a white to off-white crystalline solid that is practically insoluble in water (<0.05 microgram/mL). Pharmacologically it is a CFTR potentiator. Its chemical name is N-(2,4-di-tert-butyl-5-hydroxyphenyl)-1,4-dihydro-4-oxoquinoline-3-carboxamide. Its molecular formula is C24H28N2O3 and its molecular weight is 392.49.
Ivacaftor has the following structural formula:


TRIK-SPC-0324-V1                                             Page 8 of 16 O    HN            OH

O

N
H