Sumatriptan is a selective agonist at serotonin 5-HT1-like receptors,
including 5-HT1B/1D subtypes. It is an effective treatment for acute m
igraine attacks and the injectable form has also shown efficacy in the
treatment of cluster headaches. In placebo-controlled clinical trials
, sumatriptan, administered subcutaneously, orally, intranasally or re
ctally was significantly more effective than placebo in relieving migr
aine headache and in producing resolution or reduction of other sympto
ms associated with migraine, including nausea, photophobia and phonoph
obia. Improvements in clinical disability were also significantly grea
ter after sumatriptan than after placebo. Headache recurred in 21 to 5
7% of patients who received oral or subcutaneous sumatriptan, but most
patients responded to a second dose of the drug. Results of comparati
ve trials showed that subcutaneous sumatriptan 6mg was significantly m
ore effective than either patients' usual antimigraine treatments or i
ntranasal dihydroergotamine mesylate 1mg in relieving migraine headach
e. Subcutaneous sumatriptan 6mg and subcutaneous dihydroergotamine mes
ylate 1mg provided similarly effective migraine relief, but the headac
he recurrence rate was significantly higher after sumatriptan than aft
er this formulation of dihydroergotamine mesylate. Response rates achi
eved after oral sumatriptan were similar to those reported after treat
ment with oral naratriptan, rizatriptan or lysine acetylsalicylate plu
s metoclopramide. Treatment of acute migraine attacks with oral or sub
cutaneous sumatriptan leads to less loss of workplace productivity tha
n other antimigraine therapies. Several pharmacoeconomic analyses show
ed that gains in workplace productivity in sumatriptan recipients rang
ed from 12.1 to 89.8 hours per patient per year. Significant improveme
nts from baseline in overall health-related quality-of-life scores wer
e also experienced by sumatriptan recipients. Sumatriptan is generally
well tolerated. Nausea, vomiting, malaise and fatigue are the most co
mmon adverse events with oral sumatriptan. Injection site reactions oc
cur in 10 to 40% of patients receiving the drug subcutaneously. A bitt
er taste at the back of the mouth occurs frequently after intranasal a
dministration. Serious adverse events occur in about 0.14% of patients
with migraine treated with sumatriptan. As the drug is associated wit
h the rare development of cardiovascular effects, it is contraindicate
d in patients with a history of cardiovascular disease. Conclusions. D
espite its relatively high acquisition cost, reductions in lost workpl
ace productivity experienced by patients treated with sumatriptan may
result in savings in the overall cost of migraine to society. Thus, su
matriptan is a useful first- or second-line treatment option for patie
nts with moderate or severe migraine.