Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Two-hundred-and-seventy-eight patients with acute migraine attacks with or without aura were treated in 17 centers with 1.8 g lysine acetylsalicylate i.v. (Aspisol; = 1 g acetylsalicylic acid), 6 mg sumatriptan s.c. or placebo using a double-blind, double-dummy, randomized, multicenter parallel group study design. Two-hundred-and-seventy-five of them fulfilled the criteria for efficacy analysis, corresponding to 119 patients treated with lysine acetylsalicylate (L-ASA), 114 with sumatriptan and 42 with placebo injections. Both treatments were highly effective compared to placebo (p < 0.0001) in decreasing headache from severe or moderate to mild or none (verbal rating scale, VRS, placebo = 23.8%). Sumatriptan showed a significantly (p = 0.001) better response (91.2%) compared to L-ASA (response 73.9%). Of the patients in the L-ASA-group, 43.7% were pain-free after 2 h; 76.3% after sumatriptan and 14.3% after placebo. It took patients on average 12.6 (L-ASA), 8.2 (sumatriptan), and 19.4 h (placebo) to be able to work again. There was no significant difference between treatment groups in recurrence of headache in responders within 24 h (18.2% L-ASA, 23.1% sumatriptan, 20% placebo). Accompanying symptoms (nausea, vomiting; photophobia, phonophobia, and visual disturbances) improved with both verum treatments to a similar extent. L-ASA was significantly better tolerated than sumatriptan (adverse events L-ASA 7.6%, sumatriptan 37.8%). In conclusion, subcutaneous sumatriptan and lysine acetylsalicylate i.v. are effective treatments for patients suffering from migraine attacks. Sumatriptan is more effective, but resulted in more adverse events.
Cephalalgia 1999 Jul
PMID:Efficacy and safety of intravenous acetylsalicylic acid lysinate compared to subcutaneous sumatriptan and parenteral placebo in the acute treatment of migraine. A double-blind, double-dummy, randomized, multicenter, parallel group study. The ASASUMAMIG Study Group. 1044 45

Migraine is a paroxysmal disorder characterized by attacks of headache, nausea, vomiting, photophobia, phonophobia, and malaise. This review summarizes new treatment options for therapy of the acute attack. Mild or moderate migraine attacks are treated with antiemetics followed by analgesics such as aspirin, paracetamol, nonsteroidal anti-inflammatory drugs, or antiemetics combined with ergotamine or dihydroergotamine. Sumatriptan, a specific serotonin (5-HT)1B/D agonist is used when attacks do not respond to ergotamine, or when intolerable side effects occur. The new migraine drugs zolmitriptan, naratriptan, rizatriptan, and eletriptan differ slightly in their pharmacological profiles, which translates into minor differences in efficacy, headache recurrence, and side effects. New drugs in migraine prophylaxis include cyclandelate, valproic acid and magnesium.
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PMID:Antimigraine drugs. 1046 49

This review summarizes data on the effectiveness of various symptomatic migraine pharmacotherapies and makes recommendations for treatment. A wide variety of agents are available for the symptomatic treatment of migraine headache, including over-the-counter analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs), combination products, opiates, ergot alkaloids, corticosteroids, dopamine antagonists, and triptans. In the stepped-care approach, simple analgesics and NSAIDs are the recommended first step for the treatment of mild-to-moderate migraine headaches. Patients who do not respond to first-step treatments may be given ergots, combination products, dopamine antagonists, or triptans as the second step. Corticosteroids or opiates may be used as rescue treatment in patients who do not respond to second-step treatment. A stratified approach to care individualizes treatment based on the severity of the headache and other patient-specific factors. In a stratified approach, dihydroergotamine or triptans may be the first-step treatment for patients who present with a history of severe migraines that have responded poorly to previous treatments. Sumatriptan was the first triptan approved for the symptomatic treatment of migraine headache; newer triptans include zolmitriptan, naratriptan, and rizatriptan. Since sumatriptan is rapidly absorbed by the subcutaneous route, its time to onset of effect is shortest. Among triptan drugs that are administered orally, the relative time to onset may be shorter with rizatriptan than sumatriptan. Naratriptan has a longer time to onset but is associated with a lower rate of migraine recurrence than other triptans. graine headache, ergot alkaloids, triptans,
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PMID:Symptomatic pharmacotherapy of migraine. 1046 12

Sumatriptan is a novel drug for the treatment of acute migraine attacks. The aim of this study was to assess the efficacy of a 6 mg s.c. Sumatriptan in the early acute treatment of migraine. Patients were recruited with a current history of migraine with and without aura. 58 patients treated 1 migraine attacks at home using an autoinjector with a dose 6 mg of sumatriptan. Patient assessed headache severity and other migraine symptoms 1 and 4 h after treatment. 55% patients reported headache relief after 1 h and 77% patients after 4 h. Adverse events were reported by 11% of patients. In conclusion, sumatriptan were effective and well tolerated in the acute treatment of migraine.
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PMID:[The efficacy of subcutaneous sumatriptan for the treatment of migraine attack]. 1048 46

Migraine is a paroxysmal disorder characterized by attacks of headache, nausea, vomiting, photophobia and phonophobia, and malaise. This review summarizes new treatment options for the therapy of acute attacks. Sumatriptan was the first specific serotonin-1B/D agonist for the treatment of acute migraine attacks. Apart from the oral and subcutaneous formulation, it is also available as nasal spray and suppository. The other new migraine drugs zolmitriptan, naratriptan, rizatriptan and eletriptan differ in their pharmacological profiles, which translates into minor differences in efficacy, headache recurrence and side-effects. Importantly, in clinical practice individual patients may show a preference for one treatment over another. New drugs in migraine treatment include substance-P antagonists, nitric oxide synthetase inhibitors and calcitonin gene-related peptide antagonists.
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PMID:Acute management of migraine: triptans and beyond. 1049 71

Sumatriptan is indicated for the treatment of migraine attack and cluster headache; it is currently marketed as a subcutaneous injection, nasal spray, and oral tablet. New formulations are under consideration. The knowledge of sumatriptan absorption, combined with PK/PD information would help the design of more efficient formulations. In this perspective, we attempted to model the absorption of sumatriptan by population PK analysis. Data following administration by the intravenous (i.v.), the subcutaneous (s.c.), and the oral (po) route in healthy subjects were analyzed. A large database with full kinetic profiles was constituted. Sumatriptan was administered to 215 healthy subjects (i.v., s.c., and po) and to 143 migraine sufferers (po). The mean age was 31 years (18-86 years) in healthy subject population and was 38 years (18-65 years) in migraine patients. The mean weights were 74 kg (54-104 kg) and 66 kg (38-136 kg) in healthy subjects and migraine patients, respectively, and the mean heights were 176 cm (157-193 cm) and 164 cm (152-183 cm) in healthy subjects and migraine patients, respectively. A NONMEN analysis was performed using a two-compartment disposition model. Oral absorption was modeled with a first-order input followed by a zero-order input. Less biased results were obtained using the FOCE method. The total clearance and the distribution volume at steady state were 71.2 L/hr and 94.5 L after i.v. dosing and 68.7 L/hr and 109 L after inclusion of the s.c. and po data. The absorption phase appeared to last for about 5 hr. The interindividual variability of the main PK parameters was low: It was around 20% for the total clearance and around 30% for the distribution volume at steady state. Although significant, the combination of age and height on clearance did not decrease considerably the interindividual variability of this parameter (decrease of 2.2%); nor was it possible to establish clearly if a migraine attack has an effect on drug absorption because of the sampling scheme during absorption. Simulations have shown that it would have been possible to estimate all the PK parameters with a data set reduced to one quarter of its actual number of samples.
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PMID:Mixed effect modeling of sumatriptan pharmacokinetics during drug development: II. From healthy subjects to phase 2 dose ranging in patients. 1056 53

Sumatriptan nasal spray is a single-dose device that delivers 5 mg, 10 mg, or 20 mg of sumatriptan (dosage availability dependent upon country) in a 0.1 ml aqueous solution to one nostril. The efficacy and tolerability of sumatriptan nasal spray have been assessed in a number of studies. It has been demonstrated that administering sumatriptan as a divided dose in both nostrils confers no advantage over administration in a single nostril. It appears from these studies that sumatriptan nasal spray is rapidly effective (with an onset of efficacy as early as 15 min postdose). The 20 mg dose is superior to the lower doses (5 mg, 10 mg) in terms of both time to onset of efficacy and the extent of migraine symptom relief. Sumatriptan nasal spray is consistently effective in the treatment of multiple migraine attacks (with 67% of patients treated with the 20 mg dose responding in at least two of three treated attacks) and with long-term use for up to 1 year. Apart from a bitter taste, the adverse event profile of sumatriptan nasal spray is comparable to that of placebo.
Cephalalgia 1999 Nov
PMID:Sumatriptan nasal spray in the acute treatment of migraine: a review of clinical studies. 1096 73

The purpose of this study was to assess the sensitivity of 5-HT1D receptors in migraine using sumatriptan as a pharmacological probe. The drug stimulates the release of growth hormone (GH) and this effect may be used to explore the function of cerebral serotonergic systems in vivo. We administered sumatriptan and placebo to 15 migraineurs and to 10 controls. Blood samples were collected -15, 0, 15, 30, 45, 60 and 90 min after injection. Placebo had no effect on hormone concentrations. Sumatriptan induced a significant (P<0.01) increase in GH concentrations both in migraine patients and healthy controls. The GH increase was not significantly different in the two groups. Our results suggest that cerebral serotonergic functions mediated by 5-HT1D receptors are not altered in migraine. Sumatriptan overuse could lead to adverse effects mediated by its neuroendocrine activity.
Cephalalgia 2000 May
PMID:Effects of subcutaneous sumatriptan on plasma growth hormone concentrations in migraine patients. 1099 71

The use of sumatriptan for the treatment of migraine and cluster headache is well established. Sumatriptan has also been reported to be effective for the treatment of postdural puncture headache, postictal headache, and headache related to intravenous immunoglobulin infusion. We report two patients with headache caused by locally invasive head and neck cancer relieved by oral sumatriptan.
Headache 2000 Oct
PMID:Sumatriptan for headache caused by head and neck cancer. 1109 Dec 98

Triptans are a new class of compounds developed for the treatment of migraine attacks. The first of the class, sumatriptan, and the newer triptans (zolmitriptan, naratriptan, rizatriptan, eletriptan, almotriptan and frovatriptan) display high agonist activity at mainly the serotonin 5-HT1B and 5-HT1D receptor subtypes. As expected for a class of compounds developed for affinity at a specific receptor, there are minor pharmacodynamic differences between the triptans. Sumatriptan has a low oral bioavailability (14%) and all the newer triptans have an improved oral bioavailability and for one, risatriptan, the rate of absorption is faster. The half-lives of naratriptan, eletriptan and, in particular, frovatriptan (26 to 30h) are longer than that of sumatriptan (2h). These pharmacokinetic improvements of the newer triptans so far seem to have only resulted in minor differences in their efficacy in migraine. Double-blind, randomised clinical trials (RCTs) comparing the different triptans and triptans with other medication should ideally be the basis for judging their place in migraine therapy. In only 15 of the 83 reported RCTs were 2 triptans compared, and in 11 trials triptans were compared with other drugs. Therefore, in all placebo-controlled randomised clinical trials, the relative efficacy of the triptans was also judged by calculating the therapeutic gain (i.e. percentage response for active minus percentage response for placebo). The mean therapeutic gain with subcutaneous sumatriptan 6mg (51%) was more than that for all other dosage forms of triptans (oral sumatriptan 100mg 32%; oral sumatriptan 50mg 29%: intranasal sumatriptan 20mg 30%; rectal sumatriptan 25mg 31%; oral zolmitriptan 2.5mg 32%; oral rizatriptan 10mg 37%; oral eletriptan 40mg 37%; oral almotriptan 12.5mg 26%). Compared with oral sumatriptan 100mg (32%), the mean therapeutic gain was higher with oral eletriptan 80mg (42%) but lower with oral naratriptan 2.5mg (22%) or oral frovatriptan 2.5mg (16%). The few direct comparative randomised clinical trials with oral triptans reveal the same picture. Recurrence of headache within 24 hours after an initial successful response occurs in 30 to 40% of sumatriptan-treated patients. Apart from naratriptan, which has a tendency towards less recurrence, there appears to be no consistent difference in recurrence rates between the newer triptans and sumatriptan. Rizatriptan with its shorter time to maximum concentration (tmax) tended to produce a quicker onset of headache relief than sumatriptan and zolmitriptan. The place of triptans compared with non-triptan drugs in migraine therapy remains to be established and further RCTs are required.
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PMID:Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. 1115 11


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