eletriptan / Generic mfg. - LARVOL DELTA

The impact of headache specialist density and the introduction of gepants and lasmitidan on prescriptions for acute migraine treatments: a regression and interrupted time series analysis. (PubMed, Front Neurol) - "In our interrupted time-series analysis, the introduction of the gepants and lasmiditan was linked to decreases in triptan utilization, except for eletriptan which remained stable, and rizatriptan which rose at a slower rate...Our study suggests increased headache provider availability is associated with more prescriptions for naratriptan, eletriptan, and almotriptan. Additionally, the introduction of the gepants and lasmiditan broadly decreased the utilization of triptans. Critically, there was a strong association between a pharmaceutical company's, Pfizer, payments to physicians and utilization of their medication, rimegepant."

Journal • CNS Disorders • Migraine • Pain

Curvilinear regression analysis and ranking of migraine treatment drugs using degree-based topological indices and the WASPAS method. (PubMed, Comput Biol Med) - "In this study, we calculate several degree-based topological indices for a range of migraine treatment medications, including aspirin, caffeine, eletriptan, ergotamine, sumatriptan, rizatriptan, verapamil, diclofenac, frovatriptan, and droperidol. This research emphasizes the application of curvilinear regression techniques and performs extensive testing using these models to enhance the understanding of drug properties. The Weighted Aggregated Sum Product Assessment (WASPAS) method is applied to evaluate and rank these drugs based on various topological indices attributes, integrating both the weighted sum model and the weighted product model to provide a comprehensive assessment."

Journal • CNS Disorders • Migraine • Pain

A Pilot Study on the Drug Price Revision Strategy in Japan: A Comparison Among Fiscal Years 2018, 2020, and 2022. (PubMed, Hosp Pharm) - "In FY2020, sumatriptan and eletriptan were cost-effective, and rizatriptan was extended-dominated; nevertheless, the other triptans were dominated by sumatriptan. In FY2022, naratriptan and eletriptan were cost-effective; however, the other triptans were dominated by naratriptan...The variations could be problematic because in Japan, formulary management of triptans, for example, those for migraine, may face revaluation every other year. Discussions regarding this issue will be further explored in the future."

Journal • CNS Disorders • Migraine • Pain

eSpine: Phase 1b/2a Clinical Trial to Determine the Safety, Tolerability and Efficacy of TZ-161 in Spinal Cord Injury (clinicaltrials.gov) - P1/2 | N=28 | Not yet recruiting | Sponsor: Technophage, SA

New P1/2 trial • CNS Disorders • Orthopedics

Regional distribution of unbound eletriptan and sumatriptan in the CNS and PNS in rats: implications for a potential central action. (PubMed, J Headache Pain) - "This study suggests that despite low BBB transport, both eletriptan and sumatriptan achieve unbound concentrations sufficient to stimulate 5-HT1B, 5-HT1D, and 5-HT1F receptors not only in the trigeminal ganglion, but also in the CNS. Further research is needed to determine whether central mechanisms contribute to triptan's antimigraine effect and/or side effects."

Journal • Preclinical • CNS Disorders • Migraine • Pain

Advancing migraine therapy with novel mucoadhesive eletriptan formulations (Neuroscience 2024) - "Additionally, analytical methods for eletriptan estimation using UV-visible spectroscopy and HPLC with UV detection were developed and validated. Results demonstrated the potential of mucoadhesive formulations to enhance drug absorption and efficacy, offering a promising avenue for improving migraine therapy outcomes."

Late-breaking abstract • CNS Disorders • Migraine • Pain

Comparative effects of drug interventions for the acute management of migraine episodes in adults: systematic review and network meta-analysis. (PubMed, BMJ) - "Overall, eletriptan, rizatriptan, sumatriptan, and zolmitriptan had the best profiles and they were more efficacious than the recently marketed drugs lasmiditan, rimegepant, and ubrogepant. Although cost effectiveness analyses are warranted and careful consideration should be given to patients with a high risk cardiovascular profile, the most effective triptans should be considered as preferred acute treatment for migraine and included in the WHO List of Essential Medicines to promote global accessibility and uniform standards of care."

Clinical • Journal • Retrospective data • Review • Cardiovascular • CNS Disorders • Migraine • Pain

Recent Development of Zolmitriptan Formulation in Migraine Therapy: Production, Metabolism and Pharmaceutical Aspects. (PubMed, CNS Neurol Disord Drug Targets) - "At the moment, naratriptan, eletriptan, zolmitriptan, rizatriptan, almotriptan, and frovatriptan are the seven types of triptans available on the market. Among these are the FDA-approved triptans, Zolmitriptan and Sumatriptan, which are selective serotonin (5-hydroxytryptamine) agonists...The only known antimigraine drugs that were widely utilized before the triptan period were ergotamine and dihydroergotamine...Researchers have looked into fresh ideas for solving this issue and innovations to overcome its pharmacokinetic difficulties. This article emphasizes the role of zolmitriptan in the treatment of migraines, highlighting its pharmacological properties, production, metabolism, and structural features."

Journal • CNS Disorders • Migraine • Pain

Triptan non-response in a London tertiary headache centre: What can we learn? A retrospective study. (PubMed, Cephalalgia) - "Our findings highlight an alarming prevalence of triptan non-response among adult migraineurs receiving treatment in a London-based tertiary headache service. It is imperative for clinicians to explore methods to optimize acute medication efficacy, whether this comprises changing to a triptan with a superior response rate, advocating for early intervention or considering alternative acute medication classes, such as gepants or ditans."

Journal • Retrospective data • CNS Disorders • Migraine • Pain

Variations in prescribing patterns for acute and preventive migraine medications in young adults: A retrospective, observational study (AHS 2024) - "Fifteen preventive medications were analyzed, of which only onabotulinumtoxinA showed a statistically significant difference in rate of utilization between age groups (41.4% in adults vs. 32.3% in young adults, p = 0.001). Ten acute medications were evaluated with statistically significant differences in prescription rates demonstrated in eletriptan (8.0% vs. 3.5%, p = 0.001) and frovatriptan (4.7% vs. 1.3%, p = 0.001). We demonstrate statistically significant differences in prescription rates of common acute and preventive migraine medications when analyzing by age group."

Observational data • Retrospective data • CNS Disorders • Migraine • Pain

Changing migraine patterns in a transgender man assigned female at birth undergoing gender-affirming hormone therapy (AHS 2024) - "At this appointment, his abortive regimen was changed from sumatriptan 25 mg as needed to eletriptan 40 mg as needed. He was also started on duloxetine 60 mg daily as migraine preventive, with additional benefit of anxiety management... There exists well-established data about how certain patient populations with migraines have migraine patterns that respond to hormonal changes. For other patient populations, such as for transgender men receiving gender-affirming care, there is a lack of data in this regard. In this patient, we establish that his migraines began concurrently with initiation of gender-affirming hormone therapy with intramuscular testosterone."

CNS Disorders • Migraine • Mood Disorders • Pain • Psychiatry

The putative proton-coupled organic cation antiporter is involved in uptake of triptans into human brain capillary endothelial cells. (PubMed, Fluids Barriers CNS) - "We have demonstrated that the triptan family of compounds possesses affinity for the H+/OC antiporter proposing that the putative H+/OC antiporter plays a role in the BBB transport of triptans, particularly eletriptan. Our in vivo studies indicate that eletriptan is subjected to simultaneous brain uptake and efflux, possibly facilitated by the putative H+/OC antiporter and P-gp, respectively. Our findings offer novel insights into the potential central site of action involved in migraine treatment with triptans and highlight the significance of potential transporter related drug-drug interactions."

Journal • CNS Disorders • Migraine • Pain • ABCB1

Facile and green chemistry-compatible fluorescence spectroscopic applications of acid red 87 used to evaluate eletriptan, antimigraine, in its pharmaceutical and biological samples. (PubMed, Spectrochim Acta A Mol Biomol Spectrosc) - "This approach proficiently evaluated the pharmaceutical and biological samples of ETR. Finally, the proposed approach not only simplifies the analysis process but also limits the badimpact on the environment, making it a promising technique for analytical applications."

Journal • CNS Disorders • Migraine • Pain

The 5-HT and 5-HT agonists in acute migraine therapy: Ergotamine, dihydroergotamine, and the triptans. (PubMed, Handb Clin Neurol) - "There is extensive evidence that the seven triptans available today, sumatriptan, zolmitriptan, rizatriptan, eletriptan, naratriptan, almotriptan, and frovatriptan, are effective in the acute treatment of migraine. For optimal benefit, therapy needs to be individualized for a given patient both regarding the triptan chosen and the formulation. This chapter discusses the ergot alkaloids and the triptans, including mechanism of action, evidence for efficacy, clinical use, and adverse effects."

Journal • CNS Disorders • Migraine • Pain

Simultaneous Comparisons of 25 Acute Migraine Medications Based on 10 Million Users' Self-Reported Records From a Smartphone Application. (PubMed, Neurology) - "Using a big-data approach, we analyzed patient-generated real-time records of 10 million migraine attacks and conducted simultaneous head-to-head comparisons of 25 acute migraine medications. Our findings that triptans, ergots and anti-emetics are the most effective classes of medications align with the guideline recommendations and offer generalizable insights to complement clinical practice."

Journal • CNS Disorders • Migraine • Pain

Statistically Optimized Polymeric Buccal Films of Eletriptan Hydrobromide and Itopride Hydrochloride: An In Vivo Pharmacokinetic Study. (PubMed, Pharmaceuticals (Basel)) - "The drug was found to rapidly permeate across the buccal mucosa, leading to increased bioavailability of the drug: C of 130 and 119 ng/mL of ITHC and EHBR, respectively, as compared to 96 (ITHC) and 90 ng/mL (EHBR) of oral solution. The conclusion can be drawn that possible reasons for the enhanced bioavailability could be the increased surface area in the form of buccal films, its rapid disintegration, and faster dissolution, which led toward the rapid absorption of the drug into the blood stream."

Journal • PK/PD data • Preclinical • CNS Disorders • Migraine • Pain

Unravelling the role of the putative proton-coupled organic cation antiporter in triptan transport across the blood-brain barrier (Neuroscience 2023) - "We applied human brain capillary endothelial cells (hCMEC/D3) to investigate uptake characteristics of prototypical H+/OC antiporter substrates and triptans (almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan and zolmitriptan). J Headache Pain. 2010; 11(1):5-12."

CNS Disorders • Migraine • Pain • ABCB1

Triptan non-response in specialized headache care: cross-sectional data from the DMKG Headache Registry. (PubMed, J Headache Pain) - "In the present setting (specialized headache care in Germany), 13.1% of the patients had failed ≥ 2 triptans. Triptan failure was associated with increased migraine severity and disability, emphasizing the importance of establishing an effective and tolerable acute migraine medication. Acute treatment optimization might include switching to one of the triptans with the highest responder rates and/or to a different acute medication class."

Journal • CNS Disorders • Migraine • Pain

Prior migraine treatments among patients initiating rimegepant for acute migraine treatment in the United States (AHS 2023) - "Prior migraine treatments evaluated during the 60-month pre-index period included recommended acute and preventative treatments for migraine, including: anticonvulsants (topiramate, divalproex sodium, valproic acid), antidepressants (amitriptyline, duloxetine, venlafaxine, nortriptyline, imipramine), beta-blockers (propranolol, metoprolol, atenolol, nadolol, bisoprolol, timolol), botulinum toxin A, CGRP antagonist monoclonal antibodies (galcanezumab, erenumab, fremanezumab, eptinezumab), other CGRP antagonists (ubrogepant, atogepant), and triptans (sumatriptan, rizatriptan, eletriptan, naratriptan, zolmitriptan, frovatriptan, almotriptan). Patients initiating rimegepant for acute treatment had significant prior experience with other migraine-specific treatments, although the time period may not fully capture migraine treatment history. Most patients had tried at least one prevention agent, with more than half having tried two or more in the prior 5 years. Similarly,..."

Clinical • CNS Disorders • Migraine • Pain

Primary Care Provider Approach to Triptan Selection and Optimal Use of Triptans (AHS 2023) - "The second generation triptans (e.g., almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, and zolmitriptan) were designed to have improved oral bioavailability, increased duration of half-life, and/or faster onset of action compared with the first-generation medication, sumatriptan. Our study suggests that sumatriptan remains the first choice triptan in primary care with more than 50% of providers using it, followed closely by rizatriptan in about 40% of providers. Most providers are not familiar with almotriptan, frovatriptan, and naratriptan, despite their improved pharmacokinetic profiles. Primary care providers were not aware that naratriptan and frovatriptan are longer-acting agents which may be helpful as bridge therapy and for menstrual migraine."

Clinical • CNS Disorders • Migraine • Pain

Real World Evidence for the Effect of the Introduction of the Gepants and Lasmiditan on the Prescribing of Triptans for the Acute Treatment of Migraine at a Tertiary Headache Center (AHS 2023) - "The introduction of gepants and lasmiditan was not associated with an overall change in triptan prescribing patterns among providers at a tertiary headache center, but was linked to a decrease in naratriptan prescriptions...The introduction of lasmiditan, ubrogepant, and rimegepant in the winter of 2019-2020 presented the first potential alternatives to the triptans...Rizatriptan, sumatriptan, zolmitriptan, frovatriptan, eletriptan, and almotriptan showed no statistically significant change in prescriptions (Figure 1). The gepants and lasmiditan provide additional tools for providers and their patients but have not taken the place of triptans. Future studies should examine the continued evolution of the prescription of acute treatments for migraine."

Clinical • HEOR • Real-world • Real-world evidence • CNS Disorders • Migraine • Pain

Drugs for migraine. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • CNS Disorders • Migraine • Pain

Comparison table: Triptans. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • CNS Disorders • Migraine • Pain

Three-Dimensional Oral Mucosal Equivalents as Models for Transmucosal Drug Permeation Studies. (PubMed, Pharmaceutics) - "Using eletriptan hydrobromide as a model drug, we found that the full-thickness OME had similar drug flux to EpiOral™ (28.8 vs. 29.6 µg/cm/h), suggesting that the model had the same permeation barrier properties...Following the 3R principles, we found that the addition of Ca, retinoic acid, linoleic acid, epidermal growth factor and bovine pituitary extract was important but not sufficient to fully replace the fetal bovine serum. Finally, the OME models presented here offer a longer shelf-life than the pre-existing models, which paves the way for the further investigation of broader pharmaceutical applications (i.e., long-term drug exposure, effect on the keratinocytes' differentiation and inflammatory conditions, etc.)."

Journal • Oncology

The Efficacy of Different Triptans for the Treatment of Acute Headache in Pediatric Migraine: A Systematic Review. (PubMed, Indian Pediatr) - "We found that rizatriptan (good tolerability profile with a dose of 5 mg) and sumatriptan (oral administration) had higher efficiency as compared to other triptans. Regardless of type or dose, all triptans are generally well tolerated by patients, but a few adverse effects such as light-headedness (sumatriptan), nasopharyngitis, and, muscular spasms (sumatriptan/ naproxen), somnolence, and dry mouth (rizatriptan), and dizziness (zolmitriptan group) were reported with the triptans."

Journal • Review • CNS Disorders • Infectious Disease • Migraine • Pain • Pediatrics • Xerostomia