Rapid Oral Transmucosal Absorption of Sumatriptan, and Pharmacodynamics in Acute Migraine

Migraine is a common and highly disabling neurological disorder associated with a high socioeconomic burden. Effective migraine management depends on adequate patient education: to avoid unrealistic expectations, the condition must be carefully explained to the patient soon as it is diagnosed. The range of available acute treatments has increased over time. At present, abortive migraine therapy can be classed as specific (ergot derivatives and triptans) or non-specific (analgesics and non-steroidal anti-inflammatory drugs). Even though acute symptomatic therapy can be optimised, migraine continues to be a chronic and potentially progressive condition. In addition to the drugs officially approved for migraine prevention by international governmental regulatory agencies, numerous different agents are commonly used for this indication, showing various levels of evidence of efficacy and tolerability. Guidelines published in recent years, based on evidence-based medicine data on migraine prophylaxis, are a useful source of guidance, especially for primary care physicians and neurologists without specific expertise in headache medicine. Although the field of pharmacological migraine prevention has seen few advances in recent years, potential novel approaches are now being developed. This review looks at emerging pharmacological strategies for acute and preventive migraine treatment that are nearing or have already entered the clinical trial phase. Specifically, it discusses preclinical and clinical data on compounds acting on calcitonin gene-related peptide or its receptor, the serotonin 5-HT1F receptor, nitric oxide synthase, and acid-sensing ion channel blockers.

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“…A sumatriptan lingual spray, currently under development, has shown a good bioequivalence with oral sumatriptan 50 mg (Dilone et al 2009 ).…”

Section: Specific Anti-migraine Drugsmentioning

confidence: 99%

Recent advances in migraine therapy

et al. 2016

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“…The AUCs showed greater efficiency of systemic exposure with lingual spray as compared to the tablet formulation. The data show that absorption of sumatriptan across the oral mucosa is faster as compared to the tablets, and transmucosal delivery is a promising alternative [32].…”

Section: Lingual Spraymentioning

confidence: 97%

“…In order to check the feasibility of increasing the absorption of sumatriptan from the oral cavity, a lingual spray formulation was developed [32]. Pharmacokinetic parameters, such as T max and AUC have been evaluated for comparison with other delivery routes.…”

Section: Lingual Spraymentioning

confidence: 99%

Tablets and Other Solid Dosage Forms for Systemic Oral Mucosal Drug Delivery

Rane¹,

Moe²

2015

Advances in Delivery Science and Technology

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Efficacy of Parecoxib, Sumatriptan, and Rizatriptan in the Treatment of Acute Migraine Attacks

Müller¹,

Lohse²

2011

Clinical Neuropharmacology

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Triptans and analgetic nonsteroidal inflammatory drugs reduce acute pain syndromes in migraine. A further treatment option for an acute headache attack in patients with migraine may be the application of cyclooxygenase-2-specific inhibitors, as they have anti-inflammatory and analgesic properties. The objective of this pilot study was to investigate the effects of an oral fast-dissolving tablet of 10 mg of rizatriptan, an intravenous infusion of 40 mg of parecoxib, and a subcutaneous pen injection of sumatriptan (6 mg/0.5 mL) on pain relief in 3 cohorts of patients with episodic migraine. They were treated owing to the acute onset of a pain attack as a case of emergency. They were randomized to treatment with sumatriptan, rizatriptan, or parecoxib. The participants completed a visual analog scale for pain intensity at baseline before the drug administration and then after intervals of 20, 30, 60, and 120 minutes. Rizatriptan, parecoxib, and sumatriptan reduced pain symptoms. Twenty and 30 minutes after drug intake, rizatriptan was more efficacious than parecoxib and sumatriptan, and parecoxib was more effective than sumatriptan. Only a significant difference between rizatriptan and sumatriptan was found after 60 and 120 minutes. This trial demonstrates the effectiveness of a parecoxib infusion in the treatment of acute migraine and that the circumvention of the first pass effect of the liver by rizatriptan may be beneficial for fast pain relief.

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Rapid Oral Transmucosal Absorption of Sumatriptan, and Pharmacodynamics in Acute Migraine

Cited by 7 publications

References 6 publications

Recent advances in migraine therapy

Recent advances in migraine therapy

Tablets and Other Solid Dosage Forms for Systemic Oral Mucosal Drug Delivery

Efficacy of Parecoxib, Sumatriptan, and Rizatriptan in the Treatment of Acute Migraine Attacks

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