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Table 1 Pharmacokinetic and pharmacodynamic parameters of triptans [12, 15, 1924]

From: Theoretical analysis of headache recurrence in patients administered triptans for migraine based on receptor occupancy

Drug (formulation)

t1/2 (hr)

MW

fu

Ki (nM)

5-HT1B

5-HT1D

Sumatriptan (subcutaneous injection) [19]

1.46

295.40

0.66

12.59

12.59

Zolmitriptan (oral tablet)

Unchanged drug [12, 20]

2.40

287.30

0.75

a6.31

a2.51

Active metabolite [12, 20, 21]

2.35

273.36

0.75

a1.58

a0.50

Eletriptan (oral tablet) [22]

3.20

382.52

0.13

10.0

1.15

Rizatriptan (oral tablet) [23, 24]

1.60

269.35

0.86

7.24

2.34

Naratriptan (oral tablet) [15]

5.05

335.47

0.71

2.24

2.30

  1. aCalculated from radioligand test