zolmitriptan / Generic mfg. - LARVOL DELTA

Mendelian Randomization Uncovers Potential Repurposable Medications for Neuropsychiatric Disorders. (PubMed, Curr Neuropharmacol) - "MR-based drug repurposing is a promising approach for the treatment of neuropsychiatric disorders. Further validation is necessary to effectively integrate these medications into clinical practice."

Journal • Alzheimer's Disease • Cardiovascular • CNS Disorders • Dementia • Epilepsy • Hematological Disorders • Mental Retardation • Mood Disorders • Multiple Sclerosis • Psychiatry • Subarachnoid Hemorrhage

Variant angina associated with a CGRP receptor antagonist: a case report. (PubMed, BMC Neurol) - "This case suggests that atogepant may be associated with coronary vasospasm in patients with cardiovascular risk factors. Given CGRP's role as a potent vasodilator, its blockade may predispose to vasospasm in vulnerable individuals. Caution and close monitoring are warranted when prescribing CGRP receptor antagonists, particularly in those with cardiovascular comorbidities."

Journal • Cardiovascular • CNS Disorders • Glomerulonephritis • Hematological Disorders • Hypertension • IgA Nephropathy • Migraine • Pain • Renal Disease • Thrombosis

Pharmacodynamic and Physicochemical Evaluation of Intranasal Zolmitriptan-Loaded Nanostructured Lipid Carriers: for Enhanced Antimigraine Potential. (PubMed, Assay Drug Dev Technol) - "NLCs offer improved bioavailability and targeted brain therapy for effective migraine management. The findings suggest that NLCs are a promising approach for enhancing the therapeutic efficacy of ZMP."

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

Substrate-specific inhibition of organic cation transporter 1 revealed using a multisubstrate drug cocktail. (PubMed, Drug Metab Dispos) - "Here, we describe a multisubstrate drug cocktail that allows for the simultaneous testing of drug-drug interactions using 8 different victim drugs: fenoterol, salbutamol, sumatriptan, zolmitriptan, ipratropium, trospium, methylnaltrexone, and metformin...Group 1 comprised verapamil, quinidine, fenoterol, and ipratropium, and group 2 comprised metformin, sumatriptan, and trimethoprim...Here, we demonstrate this for organic cation transporter 1 (OCT1, SLC22A1) and presents a drug cocktail designed to identify varying inhibitory potencies in vitro and prevent false-negative drug-drug interaction results during early drug development. This approach can be extended to other polyspecific drug transporters."

Journal • SLC22A1

Extracts of Chuanxiong and Baizhi Attenuate Neuroinflammation in Chronic Migraine Rats by Inhibiting TLR4/MyD88/Nuclear Factor Kappa B Signal Pathway. (PubMed, J Physiol Investig) - "This study investigates the mechanism by which a compound mixture of Chuanxiong and Baizhi (CMCB) modulates the TLR4/MyD88/nuclear factor kappa B (NF-κB) pathway to alleviate neuroinflammation in nitroglycerin (NTG)-induced chronic migraine (CM) rat models...Results showed that CMCB concentrations below 16 μM were nontoxic to BV2 cells and effectively reduced cell apoptosis and inflammation, akin to the effects of a TLR4 pathway inhibitor, TAK-242...In vivo experiments demonstrated that both zolmitriptan and CMCB treatment ameliorated symptoms like red ear, head scratching, and cage climbing in CM rat models. High dosages of CMCB exhibited comparable efficacy to zolmitriptan in reducing inflammatory responses, indicating that CMCB alleviates neuroinflammation in CM rat models through the inhibition of the TLR4/MyD88/NF-κB signaling pathway."

Journal • Preclinical • CNS Disorders • Inflammation • Migraine • Pain • MYD88 • TLR4

Optimizing Transdermal Drug Delivery with Novasome Nanocarriers: A Quality by Design (QbD) Framework. (PubMed, Curr Drug Deliv) - "It has been shown that novasome technology may be used to deliver various drugs, such as vaccines, niflumic acid, zolmitriptan, and terconazole...These may be applied for both scale-up and lab-scale applications. This manuscript includes a detailed view of novasomes and the involvement of QBD."

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Enhanced skin adhesion of transdermal drug delivery systemviaa semi-IPN strategy:in vitro/in vivoevaluation and drug release mechanism. (PubMed, Colloids Surf B Biointerfaces) - "Meanwhile, rivastigmine, etodolac, ketoprofen, propranolol, pirfenidone, and zolmitriptan were used to evaluate drug release rates from the semi-IPN PSA. The release rates of different drugs were negatively correlated with drug polarizability, suggesting dipole-dipole interactions as the key mechanism. In summary, the semi-IPN strategy offers a robust solution for high-performance transdermal patches by improving adhesion without compromising drug release."

Journal • Preclinical

Advances in Migraine Treatment: A Comprehensive Clinical Review. (PubMed, Curr Protein Pept Sci) - "Second-generation triptans have reduced side effects and administration issues, however, Zolmitriptan and Sumatriptan still treat migraines. A holistic and multidisciplinary approach is needed to manage migraines, taking into consideration present and future therapy developments and new challenges. Research, collaboration, and ethics can improve migraine outcomes and quality of life."

Journal • CNS Disorders • Depression • Gene Therapies • Migraine • Pain • Psychiatry

Cocaine and Zolmitriptan (clinicaltrials.gov) - P1 | N=12 | Completed | Sponsor: William Stoops | Recruiting ➔ Completed | N=20 ➔ 12 | Trial completion date: Nov 2025 ➔ Jan 2025 | Trial primary completion date: Nov 2025 ➔ Jan 2025

Enrollment change • Trial completion • Trial completion date • Trial primary completion date

Real-world study of adverse events associated with triptan use in migraine treatment based on the U.S. Food and Drug Administration (FDA) adverse event reporting system (FAERS) database. (PubMed, J Headache Pain) - "Analyses have demonstrated that AEs are present in a range of systems, including cardiac, nervous, gastrointestinal, and musculoskeletal disorders. It should be noted, however, that the incidence and signal intensity of these AEs vary depending on the specific drug in question. In clinical practice, the selection of an appropriate drug and the monitoring of AEs should be tailored to the individual patient's and specific characteristics."

Adverse events • Journal • Real-world • Real-world evidence • Retrospective data • CNS Disorders • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Migraine • Musculoskeletal Diseases • Pain • Pulmonary Disease

Effects of ligustrazine on energy metabolism in migraine rats based on mitochondria-inflammation pathway. (PubMed, Neurosci Lett) - "The mitochondria-inflammation pathway plays a critical role in regulating migraine. Lig exerts anti-migraine effects primarily by modulating the mitochondria-inflammation pathway providing a novel perspective on migraine research that is beneficial for its clinical application."

Journal • Preclinical • CNS Disorders • Inflammation • Migraine • Pain • IL1B • TRPA1

Zolmitriptan niosomal transdermal patches: combating migraine via epigenetic and endocannabinoid pathways and reversal of migraine hypercoagulability. (PubMed, Drug Deliv Transl Res) - "In-vivo ZOL-patch application in rats with nitroglycerin-induced migraine showed significant management of migraine pain symptoms and photophobia assessed behaviorally, decreased brain levels of the trigeminal neuronal activation marker (c-fos), the migraine pain neurotransmitter (CGRP) and the serum levels of different migraine pain markers (substance P, nitric-oxide, and TNF-α). Additionally, this nanoformulation significantly opposed migraine-induced platelet activation and hypercoagulable status in both central and peripheral circulations as evidenced by the significant decrease in adenosine diphosphate, thrombin, factor X, CD41, and Von-Willebrand factor levels assessed peripherally and centrally. TPFsp60/6-1:1 significantly improved ZOL efficacy and accessibility to brain-receptors to a much greater extent than conventional ZOL-solution.KeywordsEndocannabinoid receptors; Epigenetically-altered genes; Hemostatic pathways; Niosomal patch; Transdermal; Zolmitriptan."

Journal • CNS Disorders • Migraine • Pain • FOS • ITGA2B • miR-382 • TNFA

Cardiovascular adverse events associated with triptans for treatment of migraine: a pharmacovigilance study of the FDA adverse event reporting system (FAERS). (PubMed, Can J Physiol Pharmacol) - "The patients prescribed sumatriptan or zolmitriptan were at a higher risk of reporting CV events for chest pain and chest discomfort, compared to rizatriptan. This finding may provide support for the clinical observation and risk evaluation of triptan treatment."

Adverse events • Journal • Cardiovascular • CNS Disorders • Migraine • Pain

Zolmitriptan, a 5-HT1B/1D receptor agonist, reduces the acquisition of methamphetamine preference in male and female adolescent Sprague-Dawley rats (Neuroscience 2024) - "Results indicated that zolmitriptan reduced the rewarding effects of METH in male and female adolescent rats. Overall, the findings demonstrate that 5-HT1B receptors play a central role in the effects of methamphetamine across development (i.e., adolescent and adult) and that this receptor system is a viable pharmacological target for the treatment of METH use disorder."

Preclinical • CNS Disorders

Zolmitriptan, a 5-HT1B receptor agonist, attenuates the acquisition of ethanol preference in adolescent female Sprague-Dawley rats (Neuroscience 2024) - "Our findings indicate that activating 5-HT1B receptors through administering zolmitriptan reduced the rewarding effects of ethanol in adolescent female rats, providing further evidence of the role of 5-HT1B receptors in modulating the rewarding effects of various drugs of abuse. Future research will examine the preference for zolmitriptan, as evident in the present study, using a wider range of doses in male and female adolescent rats."

Preclinical • Addiction (Opioid and Alcohol) • CNS Disorders

Buspirone/zolmitriptan combination exerts synergistic reduction in dyskinesia without worsening Parkinson disease motor symptomatology (MDS Congress 2024) - P2 | "In this short, proof-of-concept pilot study, addition of buspirone/zolmitriptan to the patients PD medication regimen significantly reduced LID severity without worsening Parkinsonian motor function. The buspirone/zolmitriptan oral formulation (JM-010) has been modified in ongoing multi-center clinical trials investigating PD patients with LID (in the EU: NCT03956979; in the US: NCT04377945)."

CNS Disorders • Parkinson's Disease

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

Validated green and white RP-HPLC method for the estimation of Zolmitriptan in marketed dosage form. (PubMed, Ann Pharm Fr) - "- The developed and validated method has several advantages compared to the reported HPLC methods and is useful in the systematic analysis of Zolmitriptan in its dosage form."

Journal • Cerebral Hemorrhage • CNS Disorders • Migraine • Pain

Many human pharmaceuticals are weak inhibitors of the cytochrome P450 system in rainbow trout (Oncorhynchus mykiss) liver S9 fractions. (PubMed, Front Toxicol) - "The inhibitory impacts (IC50) of atomoxetine, atorvastatin, azelastine, bimatoprost, clomethiazole, clozapine, desloratadine, disulfiram, esomeprazole, felbinac, flecainide, orphenadrine, prazosin, quetiapine, sulpiride, and zolmitriptan toward the EROD and BFCOD activities in RT-S9 were determined using the IC50 shift assay, capable of identifying time-dependent inhibitors (TDI). The IC50 concentrations are however many orders of magnitude higher than average environmental concentrations of pharmaceuticals. The time-dependent EROD inhibition by esomeprazole could warrant further research to evaluate its possible interlinkages with hepatotoxic impacts on fish."

Journal • Hepatology • CYP1A1

Pharmacological treatment of cluster headache (EAN 2024) - "Acute therapy is useful for aborting individual attacks of cluster headache and primarily involves oxygen inhalation, subcutaneous sumatriptan, or intranasal sumatriptan/zolmitriptan...Verapamil is the medication of choice for the prevention of episodic and chronic cluster headache...Alternative agents such as lithium, topiramate, or melatonin may also be beneficial. Galcanezumab has recently emerged as an additional option for episodic cases. Noninvasive neurostimulation techniques and deep brain stimulation offer potential avenues for medically refractory cases. This presentation will comprehensively review cluster headache treatment options, ensuring an evidence- based and up- to- date approach to patient care."

Chronic Cluster Headache • 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

Cocaine and Zolmitriptan (clinicaltrials.gov) - P1 | N=20 | Recruiting | Sponsor: William Stoops | Trial completion date: Jul 2024 ➔ Nov 2025 | Trial primary completion date: Jul 2024 ➔ Nov 2025

Trial completion date • Trial primary completion date

A pro-reparative bioelectronic device for controlled delivery of ions and biomolecules. (PubMed, Wound Repair Regen) - "The device incorporates ion pumps for the targeted delivery of H+ and zolmitriptan to the wound site...Overall, this bioelectronic ion pump demonstrates potential for accelerating wound healing via targeted and controlled delivery of therapeutic agents to wounds. Continued optimization and development of this device could not only lead to significant advancements in tissue repair and wound healing strategies but also reveal new physiological information about the dynamic wound environment."

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