almotriptan / 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

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

Eight-teen years of triptan use in Korea: A nationwide population-based study (AHS 2024) - "The triptans available in Korea, listed in order of their release, are sumatriptan, naratriptan, zolmitriptan, almotriptan, and frovatriptan. Despite the exponential growth in the volume of triptan prescriptions, the proportion of migraine patients receiving triptans remains low, and there is significant variability in prescribing practices across medical specialties. Efforts to reduce the gap in treatment approaches among doctors through more education are needed."

Clinical • CNS Disorders • Migraine • Pain • Psychiatry

Rizatriptan as an Over-the-Counter Triptan in the Treatment of Migraine Attacks. (PubMed, Pain Ther) - "The results show that rizatriptan at a dose of 5 mg is more effective than the triptans naratriptan 2.5 mg, almotriptan 12.5 mg and sumatriptan 50 mg, which were previously available for self-medication in Germany. From a clinical care perspective, it is desirable for affected patients to have other options available for self-medication. Non-responders to other substances also have a further treatment option with rizatriptan 5 mg, with the same or even better risk-benefit profile, to treat migraine attacks safely, effectively and in a tolerable manner as part of self-medication."

Journal • Review • CNS Disorders • Migraine • Pain

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

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

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

QuEChERS-assisted ion pair chromatography/fluorescence detection method for determination of antimigraine combination therapy in rabbit plasma samples: Application to a pharmacokinetic study. (PubMed, J Pharm Biomed Anal) - "The presented study was conducted to investigate the pharmacokinetic profile of almotriptan (ALM), a serotonin (5-HT) receptor agonist used to treat migraine, when coadministered with timolol (TIM) or verapamil (VER) which are considered as an adjuvant therapy in migraine prevention. This newly proposed method offers a faster alternative to existing chromatographic methods for extraction and determination of ALM in binary mixtures with TIM or VER in rabbit plasma and provides a platform for studying pharmacokinetic parameters. The coadministration of either TIM or VER with ALM resulted in a notable rise in C (maximum plasma concentration) and AUC (area under the plasma concentration-time curve) of ALM, implying possible alterations in the absorption and overall exposure of ALM."

Combination therapy • Journal • PK/PD data • Preclinical • CNS Disorders • Migraine • Ophthalmology • 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

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

In Vivo Evaluation of Almotriptan malate Formulation through Intranasal Route for the Treatment of Migraine: Systematic Development and Pharmacokinetic Assessment. (PubMed, AAPS PharmSciTech) - "For this, the LC-MS/MS bioanalytical method was developed and used for the determination of plasma almotriptan malate concentrations. Results of a pharmacokinetic study revealed that intranasal administration of optimized almotriptan malate formulation enabled an almost five-fold reduction in T and about seven-fold increase in bioavailability in comparison to the currently available oral tablet formulation, suggesting the potential of developed almotriptan malate intranasal formulation in producing a rapid onset of action as well as enhanced bioavailability."

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

ATOM: Evaluation of the Efficacy of Almotriptan and Ubrogepant for the Acute Treatment of Migraine (clinicaltrials.gov) - P4 | N=645 | Recruiting | Sponsor: Messoud Ashina, MD | Not yet recruiting ➔ Recruiting | Initiation date: Feb 2022 ➔ Jun 2022

Enrollment open • Trial initiation date • CNS Disorders • Migraine

Information on migraine drugs in commonly available Indian drug information sources - Whether we satisfied the community needs? (PubMed, Indian J Pharmacol) - "The scores for the completeness of drug information about the selected antimigraine drugs are 18.37% for CIMS (Ergotamine, Sumatriptan, Rizatriptan, and Zolmitriptan), 21.1% for NFI (Dihydroergotamine, Sumatriptan), 72.79% for MIMS (Ergotamine tartrate, Sumatriptan, Rizatriptan, Naratriptan, zolmitriptan, Almotriptan) and 21.77% for CDSCO (Ergotamine tartrate, Sumatriptan, Rizatriptan, Naratriptan, Zolmitriptan, eletriptan and almotriptan). The information for the antimigraine drugs available from various sources found to so much deficient. Necessary steps need to be taken in case of government public or hard documents to streamline drug information available with them as well the commercial documents as to provide reliable drug information uniformly for promoting rational use of the drug."

Journal • CNS Disorders • Migraine

Re-writing Oral Pharmacokinetics Using Physiologically Based Finite Time Pharmacokinetic (PBFTPK) Models. (PubMed, Pharm Res) - "The PBFTPK models are a powerful tool for the analysis of oral pharmacokinetic data since they rely on the physiologically sound concept of finite absorption time."

Journal • PK/PD data

ATOM: Evaluation of the Efficacy of Almotriptan and Ubrogepant for the Acute Treatment of Migraine (clinicaltrials.gov) - P4 | N=645 | Not yet recruiting | Sponsor: Messoud Ashina, MD

New P4 trial • CNS Disorders • Migraine

[VIRTUAL] Pharmacokinetic and pharmacodynamic variability of triptans. A review and some clinical implications (AHS 2021) - "In contrast, the distribution of 40% CVs can be estimated for 5 triptans, and the variability is low for almotriptan and sumatriptan, medium for rizatriptan, and high for eletriptan and zolmitriptan. Based on the lowest pharmacokinetic variability among triptans, almotriptan and sumatriptan, are probably most likely to result in reproducible efficacy. In addition to the pharmacokinetic variability, probably mainly due to genetic differences in metabolizing enzymes, potential explanations for the total variability of triptans could be genetic variations in transporters mediating blood-cell transport, and brain drug disposition where uptake and efflux transporters possibly play a role. Finally, variations in target function, pharmacodynamics, most likely play a large role."

Clinical • PK/PD data • Review • CNS Disorders • Migraine

Transfer of triptans into human breast milk and estimation of infant drug exposure through breastfeeding. (PubMed, Basic Clin Pharmacol Toxicol) - "Twenty-two breast milk sample sets were obtained for sumatriptan (n=8), rizatriptan (n=5), zolmitriptan (n=4), eletriptan (n=3), almotriptan (n=1) and naratriptan (n=1). Infant drug exposure through breastfeeding appears to be low and indicates that use of the triptans in this study is compatible with breastfeeding. Naratriptan may not be first choice in breastfeeding mothers initiating triptans during the neonatal period."

Journal • CNS Disorders • Migraine

Pharmacokinetic drug interactions between antiseizure medications and drugs for comorbid diseases in children with epilepsy. (PubMed, Expert Opin Drug Metab Toxicol) - "Most important DDIs are between some ASMs and omeprazole and pantoprazole (drugs for gastrointestinal disorders), ibuprofen and cyclobenzaprine (drugs for musculoskeletal disorders), loratidine, lumacaftor/ivacaftor, montelukast, and theophylline (drugs for respiratory system), levothyroxine, liothyronine and several corticosteroids (systemic hormonal preparations), almotriptan, dihydroergotamine, ergotamine, and several antipsychotics, antidepressants and anxiolytics (drugs for nervous diseases). Clinical evidence of the predicted DDIs was found in a minority of cases. : Treatment of children with epilepsy should be decided considering treatment of both seizures and comorbid diseases and aimed at minimizing the risk of DDIs between ASMs and NON-ASMs."

Clinical • Journal • PK/PD data • CNS Disorders • Epilepsy • Gastroenterology • Gastrointestinal Disorder • Migraine • Musculoskeletal Diseases • Respiratory Diseases

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

Journal • CNS Disorders • Migraine • Pain

Twenty-five years of triptans - a nationwide population study. (PubMed, Cephalalgia) - "In a cohort with access to free clinical consultations and low medication costs, we observed low rates of triptan adherence, likely due to disappointing efficacy and/or unpleasant side effects rather than economic considerations. Triptan success continues to be hindered by poor implementation of clinical guidelines and high rates of treatment discontinuance."

Clinical • Journal • CNS Disorders • Migraine • Pain

Effects of new generation triptans - frovatriptan and almotriptan - on hemodynamic parameters in intact male and female rats. (PubMed, Acta Pharm) - "Male and female rats showed reduction in all hemodynamic parameters, but only male rats showed an increase in the heart rate. In general, we could say that both almotriptan and frovatriptan potentiate cardiovascular safety."

Journal • Preclinical • Cardiovascular • CNS Disorders • Migraine