Table 1.
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.