ArticleCephalalgia : an international journal of headache2020
Ultra-rapid brain uptake of subcutaneous sumatriptan in the rat: Implication for cluster headache treatment.
Article in Cephalalgia : an international journal of headache, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13 citing papers in PubMed, 34 citations in OpenAlex.
- Targeting GCell reports. Medicine · 2026Article
- Early life stress induces brain-wide electrical network predisposition to migraine.The journal of headache and pain · 2026Article
- Beyond symptom: Exploring the analgesic properties of vomiting in patients with migraine.Headache · 2026Article
- Mechanistic intersections between migraine and major depressive disorder.The journal of headache and pain · 2025Review
- Regional distribution of unbound eletriptan and sumatriptan in the CNS and PNS in rats: implications for a potential central action.The journal of headache and pain · 2024Article
- The putative proton-coupled organic cation antiporter is involved in uptake of triptans into human brain capillary endothelial cells.Fluids and barriers of the CNS · 2024Article
- Advances in functional lipid nanoparticles: from drug delivery platforms to clinical applications.3 Biotech · 2024Review
- Article
- Cluster headache pathophysiology - insights from current and emerging treatments.Nature reviews. Neurology · 2021Review
- Cluster headache and TACs: state of the art.Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2020Review
- Lasmiditan mechanism of action - review of a selective 5-HTThe journal of headache and pain · 2020Review
- Rapid uptake of sumatriptan into the brain: An ongoing question of blood-brain barrier permeability.Cephalalgia : an international journal of headache · 2020Article
- Functional Hybrid Nanoemulsions for Sumatriptan Intranasal Delivery.Frontiers in chemistry · 2020Article
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8 authors at 3 institutions in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
backgroundIn spite of the substantial therapeutic efficacy of triptans, their site of action is still debated. Subcutaneous sumatriptan is the most efficacious symptomatic treatment for cluster headache (CH) patients, showing therapeutic onset within a few minutes after injection even in migraine patients. However, whether subcutaneous sumatriptan is able to reach the CNS within this short time frame is currently unknown.
methodsHere, by means of liquid chromatography/mass spectrometry, we investigated peripheral and brain distribution of subcutaneous sumatriptan soon after injection in rats at a dose equivalent to that used in patients. Tissue sumatriptan contents were compared to those of oxazepam, a prototypical lipophilic, neuroactive drug.
resultsWe report that sumatriptan accumulated within brain regions of relevance to migraine and CH pathogenesis such as the hypothalamus and the brainstem as soon as 1 and 5 minutes after injection. Notably, sumatriptan brain distribution was faster than that of oxazepam, reaching concentrations exceeding its reported binding affinity for 5HT1
conclusionOur findings indicate that sumatriptan distributes within the CNS soon after injection, and are in line with prompt pain relief by parenteral sumatriptan in CH patients.
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