恩惜膜 5 Esmya 5mg tablets - ktgh.com.tw

1 5 Esmya 5mg tablets 026312 1. Esmya 5 mg 2. ulipristal acetate 5 mg 3. 7 mm ES5 4. ulipristal acetate 5 mg 3 3 2 3 ulipristal acetate 12 : ulipristal acetate ( ) : ulipristal acetate ( ) ulipristal acetate ulipristal acetate 18 ulipristal acetate (progestagen) (progestagen) ( ) ulipristal acetate ulipristal acetate ( ) ulipristal acetate ulipristal acetate ( ) ulipristal acetate ( )

2 ulipristal acetate ( erythromycin verapamil) ( ketoconazole ritonavir nefazodone itraconazole telithromycin clarithromycin)CYP3A4 ( ) ulipristal acetate CYP3A4 ( rifampicin rifabutin carbamazepine oxcarbazepine phenytoin fosphenytoin phenobarbital primidone efavirenz nevirapine ritonavir)( ) ulipristal acetate 3 ulipristal acetate (PAEC) ( ) 2 2 3 ulipristal acetate 10 4 ulipristal acetate ulipristal acetate (progestagens) ulipristal acetate (progestagen) ( ) CYP3A4 erythromycin propionate( 500 mg 9 ) ulipristal acetate (Cmax) (AUC) ulipristal acetate AUC Cmax ( ) CYP3A4 ketoconazole( 400 mg 7 ) ulipristal acetate Cmax AUC 2 ulipristal acetate AUC Cmax ( )

3 CYP3A4 ulipristal acetate ulipristal acetate CYP3A4 ( ) CYP3A4 rifampicin( 300 mg 9 ) ulipristal acetate Cmax AUC 90% ulipristal acetate ulipristal acetate 10 ulipristal acetate CYP3A4 ( rifampicin rifabutin carbamazepine oxcarbazepine phenytoin fosphenytoin phenobarbital primidone efavirenz nevirapine ritonavir) ( ) ulipristal acetate (10 mg ) esomeprazole ( 20 mg 6 ) Cmax 65% (tmax)( ) AUC 13% pH ulipristal acetate ulipristal acetate ulipristal acetate ( ) (progestagen) (progestagen) ( ) ulipristal acetate 12 (progestagen) ulipristal acetate P-gp P-gp ulipristal acetate P-gp fexofenadine(60 mg) 10 mg ulipristal acetate fexofenadine ulipristal acetate P-gp ( dabigatran etexilate digoxin fexofenadine) ulipristal acetate ulipristal acetate ( ) ulipristal acetate ( )

4 ulipristal acetate ( ) ulipristal acetate ( ) ulipristal acetate / / ulipristal acetate ( ) ulipristal acetate ulipristal acetate ulipristal acetate ulipristal acetate 602 ulipristal acetate 5 mg 10 mg ulipristal acetate ( ) ( ) ( ) ( ) 131 2 ( 3 ) 1 3 ( 1/10) ( 1/100 <1/10) ( 1/1,000 <1/100) ( 1/10,000 <1/1,000) (<1/10,000) ( ) * ** * ** * * * * / ( [ ] )(- [ ]) ( [ ]) 1 2 ulipristal acetate 10 mg ulipristal acetate 5 mg 4 3 ( 99 )

5 2 3 ulipristal acetate 5 10 mg 1 (Cmax) ng/ml ng/ml (AUC0- ) ulipristal acetate 1 Cmax ng/ml ng/ml AUC0- ulipristal acetate (30 mg ) Cmax 45% (tmax) ( 3 ) AUC0- 25% (mono-N-demethylated) ulipristal acetate ulipristal acetate (>98%) (albumin) 1- ulipristal acetate ulipristal acetate AUCt / (mean AUCt milk/plasma ratio) / ulipristal acetate - - (di-N-demethylated metabolites) P450 3A4 (CYP3A4) 10% ulipristal acetate 5 10 mg 38 (CL/F) 100 l/h ulipristal acetate CYP1A2 2A6 2C9 2C19 2D6 2E1 3A4 CYP1A2 ulipristal acetate ulipristal acetate P-gp (ABCB1) ulipristal acetate CYP ulipristal acetate ( ) ( )

6 39 PAEC ulipristal acetate ( 1 mg/kg ) ulipristal acetate ulipristal acetate 6. Microcrystalline celluloseMannitolCroscarmellose sodiumTalcMagnesium (MFG) (EXP) Alu-PVC/PE/PVDC 28 84 7 CENEXI 17, RUE DE PONTOISE, F-95520 OSNY, FRANCE 368 7 (02) 27554881 ulipristal acetate 10-15% ( (MRI) > 16 mm) PAEC ulipristal acetate ( ) ulipristal acetate 24% ( ) leuprorelin ( )

7 ulipristal acetate 0% ulipristal acetate ulipristal acetate ulipristal acetate 2 3 / ulipristal acetate 200 mg 50 mg 10 5. ATC Code:G03XB02 ulipristal acetate ulipristal acetate 5 mg ( ) ulipristal acetate 4 PAEC ( ) ( ) ulipristal acetate 3 60% 5% 16 mm ulipristal acetate 10-15% (> 16 mm)

8 3 ulipristal acetate ulipristal acetate 5 mg ng/ml ulipristal acetate 5 mg (FSH) 3 ulipristal acetate (TSH) (ACTH) 13 ulipristal acetate 5 mg 10 mg 1 (Hb < g/dl) 80 mg(Fe++) 2 leuprorelin mg 2 (Pictorial Bleeding Assessment Chart, PBAC) 8 PBAC >100 1 ulipristal acetate ( 1) MRI ulipristal acetate 2 ulipristal acetate (leuprorelin) ulipristal acetate ( ) ( 13 ) 25 ulipristal acetate leuprorelin 1 a 1 (MRI) 2 ulipristal acetate ulipristal acetate P 1 < 2 3 < 4 < 131 2 ( 10 mg ulipristal acetate 3 )

9 ( ) CYP3A4 CYP3A4 P-gp pH 1. Esmya 5 mg 2. ulipristal acetate 5 mg 3. 7 mm ES5 4. ulipristal acetate 5 mg 3 3 2 3 ulipristal acetate 12 : ulipristal acetate ( ) : ulipristal acetate ( ) ulipristal acetate ulipristal acetate 18