Triptans, selective antagonists of 5-HT1B/1D receptor, are effective and safe drugs for acute migraine treatment. Their marketing has greatly boosted research on migraine pathogenesis, has improved the methodologies of clinical trials, and has allowed defining which characteristics should have the ideal medications for acute treatment according to patients: pain-free response within 2 hours, no recurrence or need for other drugs, consistency of response, oral administration, good tolerability, safety, and no drug-drug interactions. However, triptans do not always correspond to these parameters. In particular, the maximum response after oral administration, measured as pain-free after 2 hours, is approximately 70% in clinical trials and up to 40% of attacks fail to respond to a particular triptan. Furthermore, less than 2/3 of patients respond to a triptan in 3/3 attacks . In Italy there are available 6 triptans with similar mechanism of action, but different kinetics profiles. In alphabetical order, the first one is almotriptan. Its oral bioavailability is 70-80%, Tmax after oral administration is about 1 to 4 hours, and elimination half-life is 3 to 4 hours. Oral bioavailability of eletriptan is 50%, its elimination half-life is 4 to 5 hours, and Tmax after oral administration is about 1.3 hours. Frovatriptan presents long half-life (25 hours), but a relatively low bioavailability of 24 to 30%, and Tmax after oral administration is 2 to 4 hours. Elimination half-life of rizatriptan is 2-3 hours, bioavailability is 40-50%, and Tmax after oral administration is about 1-1.5 hours. Sumatriptan is rapidly, but incompletely absorbed following oral administration and undergoes first-pass metabolism. Bioavailability following subcutaneous administration is much higher (96%) than after oral (14 %) or intranasal (16%) administration of sumatriptan, and elimination half-life is about 2 hours. Half-life of zolmitriptan is 2.5 to 3 hours, and its oral bioavailability is approximately 40%. The clinical importance of pharmacokinetic differences after oral administration (which we have summarized above) has not been established yet, as far as both efficacy and tolerability are concerned. There are no elements to foresee which triptan works best for any given patients . However, it has been suggested that pharmacokinetics during early post-dose interval (0-2 hours) is the most important one for clinical response and that the initial rate of absorption and the height of the plasma levels reached may be closely related to headache relief . A slow and reduced early absorption after oral administration could therefore explain the poor response reported by some patients.  Dodick DW. Triptan nonresponder studies: implications for clinical practice. Headache 2005; 45(2):156-62  Maas HJ, Danhof M, Della Pasqua OE. Prediction of headache response in migraine treatment. Cephalalgia 2006; 26(4):416-22  FOX AW. Onset of effect of 5-HT1B/1D agonists: a model with pharmacokinetic validation. Headache 2004; 44(2):142-7
Triptans: what is the clinical importance of kinetic differences? / Ferrari, Anna; E., Sternieri. - In: THE JOURNAL OF HEADACHE AND PAIN. - ISSN 1129-2369. - STAMPA. - 9 (Suppl)(2008), pp. S10-S10. ((Intervento presentato al convegno XXII National Congress of The Italian Society for the Study of Headaches tenutosi a Torino nel October 2-4, 2008.
|Data di pubblicazione:||2008|
|Titolo:||Triptans: what is the clinical importance of kinetic differences?|
|Autore/i:||Ferrari, Anna; E., Sternieri|
|Rivista:||THE JOURNAL OF HEADACHE AND PAIN|
|Titolo del libro:||Proceedings of the XXII National Congress of The Italian Society for the Study of Headaches|
|Citazione:||Triptans: what is the clinical importance of kinetic differences? / Ferrari, Anna; E., Sternieri. - In: THE JOURNAL OF HEADACHE AND PAIN. - ISSN 1129-2369. - STAMPA. - 9 (Suppl)(2008), pp. S10-S10. ((Intervento presentato al convegno XXII National Congress of The Italian Society for the Study of Headaches tenutosi a Torino nel October 2-4, 2008.|
|Tipologia||Abstract in Rivista|
File in questo prodotto:
I documenti presenti in Iris Unimore sono rilasciati con licenza Creative Commons Attribuzione - Non commerciale - Non opere derivate 3.0 Italia, salvo diversa indicazione.
In caso di violazione di copyright, contattare Supporto Iris