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. 2014 Dec 8;15(1):85. doi: 10.1186/1129-2377-15-85

Table 1.

The various parameters for Triptans marketed in Japan[11-20]

Drugs Administration route (dosage form) Standard dose in Japan (mg) MW (g/mol) Plasma unbound fraction; fu Ki 1B * (nM) Ki 1D * (nM)
Sumatriptan [11-13]
SC
3
295.41
0.66
12.6
12.6
 
PO
50
       
 
NS
20
       
Zolmitriptan [14-16]
PO
2.5
[unchanged drug]
[unchanged drug]
[unchanged drug]
[unchanged drug]
 
ODT
 
287.30
0.8
6.31
2.51
 
 
 
[active metabolite]
[active metabolite]
[active metabolite]
[active metabolite]
 
 
 
273.36
0.75
1.58
0.5
Eletriptan [17]
PO
20
382.52
0.13
10.0
1.2
Rizatriptan [18,19]
PO
10
269.35
0.86
138
13.1
 
ODT
         
Naratriptan [20] PO 2.5 335.47 0.71 2.2 2.3

*calculated from pKi or pIC50.

SC: subcutaneous injection.

PO: oral tablet.

NS: nasal spray.

ODT: orally disintegrating tablet.

Ki1B: 5-HT1B receptor dissociation constant.

Ki1D: 5-HT1D receptor dissociation constant.