Zeneo Sumatriptan (sumatriptan needle-free injection) / Crossject - LARVOL DELTA

Effects of Olcegepant, Sumatriptan, and Ibuprofen on Migraine-Like Behavior Induced by Repetitive Restraint Stress in Mice (Neuroscience 2025) - "These injections were repeated for sumatriptan on Day 3, while olcegepant was injected on Day 2, and Day 3. We showed that restraint stress can cause migraine-like behaviors that are responsive to several migraine therapeutics. These data further validate this model as being translationally relevant for testing migraine therapeutics and they provide insight into the mechanisms by which stress causes behavioral features consistent with migraine."

Preclinical • CNS Disorders • Migraine • Pain

Pain intensity in cluster headache - Case Report (IHC 2025) - "Results A 44-year-old white male patient, diagnosed six years earlier with chronic cluster headache, which had become refractory to preventive treatments, but remained responsive to injectable sumatriptan and/ or inhalation of moist oxygen during attacks. This case is unique in that it allowed a direct comparison between two concomitant painful conditions. The patient experienced the pain from cluster headache as significantly more intense than that of the open fracture, reinforcing existing literature on the extreme severity of cluster headache pain."

Case report • Clinical • Migraine

Cluster Headache vs. Labor: A Comparative Perspective on Acute Pain During and After Delivery (IHC 2025) - "She self-treated with her home injectable sumatriptan, successfully aborting the attack and then delivered a healthy boy. It does not care if you are already trialed with another difficulty, hospitalized for another condition, taking shelter in a war zone, have just lost your job, or are delivering a newborn child. CH is like an unwanted guest; it shows up uninvited, makes a mess of the place, and then leaves only threatening to come back later – and on its time, not yours."

Migraine

Effects of olcegepant, sumatriptan, and ibuprofen on migraine-like behavior induced by repetitive restraint stress in mice (AHS 2025) - "These injections were repeated for sumatriptan on Day 3, while olcegepant was injected on Day 2, and Day 3. We showed that repeated restraint stress in mice can cause migraine-like behaviors that are responsive to several migraine therapeutics. These data further validate this model as being translationally relevant for testing migraine therapeutics and they provide insight into the mechanisms by which stress causes behavioral features consistent with migraine."

Preclinical • CNS Disorders • Migraine • Pain

Reduction of opioid withdrawal symptoms and opioid-induced hyperalgesia by subcutaneous sumatriptan reveals central neuromodulation. (PubMed, J Pain) - "We also found that at the time of naloxone injection sumatriptan reached contents of 294±19 and 371±30 pg/mg of tissue in the RVM and locus coeruleus, respectively. PERSPECTIVE: This article reports that sumatriptan reduces symptoms of morphine withdrawal and morphine-induced hyperalgesia. Data suggests that triptans exert their antinociceptive effects through central mechanisms."

Journal • Addiction (Opioid and Alcohol) • CNS Disorders • Migraine • Pain

Development of a hydrophilic transdermal patch for combined delivery of sumatriptan and metoclopramide in migraine therapy. (PubMed, Drug Deliv Transl Res) - "The target therapeutic dose, equivalent to 4 mg subcutaneous injection of sumatriptan succinate and 10 mg oral metoclopramide HCL, was achieved within 8 h using a 60 cm2 patch of the optimized formulation. Based on these findings, the developed transdermal patch could serve as a promising alternative for migraine management, potentially improving patient compliance and therapeutic outcomes."

Journal • CNS Disorders • Migraine • Pain

Abhd6 partially reversed medication overuse headache induced allodynia induced by sumatriptan (Neuroscience 2024) - "In rats with headache like behaviors, those that received the ABHD6 inhibitor had periorbital allodynia thresholds statistically higher than those receiving vehicle, suggesting that targeting ABHD6 for MOH attenuation is a potential strategy. Targeting ABHD6 with the inhibitor KT-182 mitigated periorbital allodynia in sumatriptan induced MOH animals, indicating a potential intervention for the reversal of MOH.Late-Breaker Justification: Data collection was still underway during the initial timeframe o fAbstract submission; therefore, results could not be completed until now.This study is supported by NIH R01-NS126752-01A1"

CNS Disorders • Depression • Migraine • Pain • Psychiatry

Grimace scale as a robust metric for nociception in a nitroglycerin (NTG)-induced mouse migraine model (Neuroscience 2023) - "In acute and chronically NTG-treated mice, the grimace scale analysis showed a strong increase in nociceptive responses that can be alleviated by co-injection of sumatriptan, similarly to what has been observed in humans. These results affirm the NTG-induced migraine model as a valid and fast system to study migraine pathology in mice. The grimace scale proved to be a strong indicator of nociception in NTG-treated animals."

Preclinical • CNS Disorders • Migraine • Pain • FOS

Glassy Carbon Electrode Modified with CB/TiO Layer for Sensitive Determination of Sumatriptan by Means of Voltammetry and Flow Injection Analysis. (PubMed, Sensors (Basel)) - "Amperometric and voltammetric measurements of SUM under the flow injection conditions were also performed to indicate the possibility of its fast and accurate determination with a time of single analysis of approx. 30 s."

Journal • CNS Disorders • Migraine • Pain

Activation of the microglial P2X7R/NLRP3 inflammasome mediates central sensitization in a mouse model of medication overuse headache. (PubMed, Front Mol Neurosci) - "Repeated intraperitoneal injection of sumatriptan (SUMA) was used to establish a mouse model of MOH...To elucidate the effect of microglial activation and the P2X7/NLRP3 signaling pathway on central sensitization in MOH, we evaluated whether the microglia-specific inhibitor minocycline, the P2X7R-specific antagonist BBG and the NLRP3-specific inhibitor MCC950 altered SUMA-caused mechanical hyperalgesia...Based on the current findings, inhibiting microglial activation could reduce central sensitization caused by chronic SUMA treatment via the P2X7R/NLRP3 signaling pathway. The clinical management of MOH may benefit from a novel strategy that inhibits microglial activation."

Journal • Preclinical • Inflammation • Pain • FOS • NLRP3

The role of ATP-sensitive potassium channels in a preclinical stress-induced migraine model (Neuroscience 2022) - "Co-injection of sumatriptan (0.01 μg) with levcromakalim (1 μg) on the dura effectively alleviated levcromakalim-induced migraine-like behavior. Importantly, they demonstrate that opening of KATP channels within the dura contributes to migraine-related behavior, suggesting that the dura is one location where these channels contribute to the disorder. Together, these data and future studies using this model may help to further investigate the potential of KATP channel blockers as novel migraine therapeutics."

Preclinical • CNS Disorders • Migraine

Network meta-analysis of therapies for cluster headache: Effects of acute therapies for episodic and chronic cluster. (PubMed, Headache) - "Our findings suggest that high flow oxygen is more efficacious when compared to low flow oxygen for headache relief. When low flow oxygen fails in patients who can tolerate oxygen, increased flow rates should be tried. Additionally, high flow oxygen is likely more effective than zolmitriptan nasal spray, nVNS, and octreotide. Sumatriptan injectable is more likely to be effective when compared to zolmitriptan nasal spray, octreotide, and nVNS."

Journal • Retrospective data • Pain

A prolactin-dependent sexually dimorphic mechanism of migraine chronification. (PubMed, Cephalalgia) - "We identified a sexually dimorphic mechanism of migraine chronification that involves down-regulation of PRLR-L and increased signaling of circulating prolactin at PRLR-S. These studies reveal a previously unrecognized neuroendocrine mechanism linking the hypothalamus to nociceptor sensitization that increases the risk of migraine pain in females and suggest opportunities for novel sex-specific therapies including gene editing through nasal delivery of CRISPR/Cas9 constructs."

Journal • CNS Disorders • Migraine • Ophthalmology • Pain • PRLR

[VIRTUAL] LasmiGepant: A case report of simultaneous administration of lasmiditan and rimegepant (AHS 2021) - "Gepants are small molecule CGRP receptor antagonists, and this class of medications includes rimegepant and ubrogepant, which are both FDA approved for the abortive treatment of migraine...In terms of abortive therapy, she has used caffeine-containing over-the-counter analgesics, butalbital-containing analgesics, ibuprofen, naproxen, indomethacin, injectable sumatriptan, intranasal sumatriptan, rizatriptan, naratriptan, eletriptan, zolmitriptan, isometheptene mucate/dichloralphenazone/acetaminophen, ondansetron, hydroxyzine, promethazine, prochlorperazine, metoclopramide, ketamine, and non-invasive vagus nerve stimulation with inconsistent benefit... While the mechanisms underlying migraine are complex and not fully understood, extensive data support the interplay of neurotransmitters, neuropeptides, cellular channels, electrical signaling, and the collective activity of neural networks. New treatments target specific migraine pathways with potentially less impact on..."

Clinical • CNS Disorders • Migraine • Pain • Restless Legs Syndrome • Sleep Disorder

[VIRTUAL] Central sensitization and migraine treatments impact on thalamic metabolism: MR study at 21.1 T (AHS 2021) - "For treatment groups, drugs were injected (0.3 mg/kg sumatriptan, 0.3 mg/kg telcagepant or 0.1 mg/kg ouabain) prophylactically 5 min prior to NTG. Thalamic metabolite concentrations during migraine onset reveal that recruited neural structures undergo a state of ATP deprivation possibly due to NKAT over-activity at the CP, which may be mitigated by migraine treatments. The neuroprotective response (elevated Gly and Tau) to NTG-triggered sensitization is reduced but not eliminated by treatment with either sumatriptan, telcagepant or ouabain."

CNS Disorders • Migraine

[VIRTUAL] Cerebral hemodynamics with migraine onset and intervention (AHS 2021) - "While anesthetized in the MR scanner, the rats (n=6/group) were administered an in situ IP injection of either NTG (10 mg/kg) to trigger the migraine or saline to serve as control, with and without the prior injection (5 min) of either sumatriptan or telcagepant (both 0.3 mg/kg). Cerebral microcirculation showed altered perfusion significantly impacting the NTG-triggered brainstem, an integrating gateway to nociceptive inputs. However, CBF increases are largely subsequent to both ionic and metabolic changes. Prophylactic drugs impact early perfusion only in the brainstem, reversing the CBF enhancement of NTG alone."

CNS Disorders • Migraine • Pain

Levcromakalim, an Adenosine Triphosphate-Sensitive Potassium Channel Opener, Dilates Extracerebral but not Cerebral Arteries. (PubMed, Headache) - "Levcromakalim dilated the MMA but not MCA. The MMA dilation was associated with headache. Future studies should investigate whether opening of K channels can activate and sensitize the perivascular nociceptors."

Journal • CNS Disorders • Giant Cell Arteritis • Migraine

Association Between Sumatriptan Treatment During a Migraine Attack and Central 5-HT1B Receptor Binding. (PubMed, JAMA Neurol) - "All participants were scanned 3 times: (1) during an experimentally induced migraine attack, (2) after a subcutaneous injection of 6-mg subcutaneous sumatriptan, and (3) on a migraine attack-free day. Furthermore, during migraine attacks, as compared with outside of attacks, 5-HT1B receptor binding was statistically significantly associated with reduced in pain-modulating regions (mean [SD] binding potential, 1.36 [0.22] vs 1.20 [0.20]; P = .02). Treatment with sumatriptan during migraine attacks appeared to be associated with a decrease in 5-HT1B receptor binding, a finding that is most likely associated with the binding of sumatriptan to central 5-HT1B receptors, but the contribution of ongoing cerebral serotonin release to the lower binding cannot be excluded; the migraine attack-associated decrease in binding could indicate that migraine attacks are associated with increases in endogenous serotonin."

Journal • CNS Disorders • Migraine • Pain

Repetitive stress in mice causes migraine-like behaviors and CGRP-dependent hyperalgesic priming to a migraine trigger. (PubMed, Pain) - "Following return to baseline, the NO-donor sodium nitroprusside (SNP; 0.1 mg/kg) elicited mechanical hypersensitivity in stressed but not in control animals, demonstrating the presence of hyperalgesic priming...Finally, mice received either the CGRP monoclonal antibody ALD405 (10 mg/kg) 24 hours prior to SNP or a co-injection of sumatriptan (0.6 mg/kg). ALD405, but not sumatriptan, blocked the facial hypersensitivity due to SNP. This stress paradigm in mice and the subsequent primed state caused by stress, allow further preclinical investigation of mechanisms contributing to migraine, particularly those caused by common triggers of attacks."

Journal • Preclinical • CNS Disorders • Immunology • Migraine

A Pre-Existing Myogenic Temporomandibular Disorder Increases Trigeminal Calcitonin Gene-Related Peptide and Enhances Nitroglycerin-Induced Hypersensitivity in Mice. (PubMed, Int J Mol Sci) - "Systemic injection of sumatriptan inhibited the MMTL-enhanced migraine-like hypersensitivity. MMTL pretreatment significantly upregulated the protein level of CGRP in the spinal trigeminal nucleus caudalis after NTG injection. Our results indicate that a pre-existing myogenic TMD can upregulate NTG-induced trigeminal CGRP and enhance migraine-like hypersensitivity."

Journal • Preclinical • CNS Disorders • Immunology • Migraine • Pain

Inflammation induces developmentally regulated sumatriptan inhibition of spinal synaptic transmission. (PubMed, Br J Pharmacol) - "These findings indicate that inflammation induces a developmentally regulated 5-HT1B/D presynaptic inhibition of excitatory transmission into the rat superficial dorsal horn. Thus, triptans could potentially act as spinal analgesic agents for inflammatory pain in the juvenile setting."

Journal • CNS Disorders • Immunology • Migraine • Pain

Gi-coupled receptor activation potentiates Piezo2 currents via Gβγ. (PubMed, EMBO Rep) - "Local injection of sumatriptan, an agonist of the Gi-coupled serotonin 1B/1D receptors, increases mechanical sensitivity in mice, and the effect is abolished by inhibiting PI3K and MAPK. Hence, our studies illustrate an indirect mechanism of action of Gβγ to sensitize Piezo2 currents and alter mechanosensitivity after activation of Gi-coupled receptors."

Journal

Non-invasive dural stimulation in mice: A novel preclinical model of migraine. (PubMed, Cephalalgia) - "Systemic injection of sumatriptan at the time of dural stimulation with inflammatory soup decreased the resulting cutaneous hypersensitivity. Trigeminal ganglion cell bodies retrogradely labeled from the dura had low pH-evoked currents similar to those generated by acid-sensing ion channels. Conclusion Non-invasive dural stimulation in mice can be used as a model of migraine in the absence of injury."

Journal • Preclinical

Protective effects of sumatriptan on ischaemia/reperfusion injury following torsion/detorsion in ipsilateral and contralateral testes of rat. (PubMed, Andrologia) - "Male Wistar rats (n = 42) were allocated into a sham-operated group, a control group and treatment groups which were injected sumatriptan (0.1, 0.3 and 1 mg/kg), GR-127935 (0.01 mg/kg)-5-HT1B/1D receptors antagonist-and sumatriptan (0.1 mg/kg) + GR-127935 (0.01 mg/kg). Interestingly, co-administration of sumatriptan with GR-127935 reversed the beneficial impacts of sumatriptan on macroscopic appearance, microscopic pattern and biochemical markers. It is concluded that sumatriptan presumably via stimulation of 5-HT receptors decreased inflammation, oxidative stress and deteriorations induced by ischaemia/reperfusion injury following testicular torsion/detorsion."

Journal • Preclinical

Ultra-rapid brain uptake of subcutaneous sumatriptan in the rat: Implication for cluster headache treatment. (PubMed, Cephalalgia) - "Our 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."

Journal • Preclinical