Ergonex (ergotamine/caffeine) / AC Farma - LARVOL DELTA

Interdigitation of lipids for vesosomal formulation of ergotamine tartrate with caffeine: A futuristic trend of intranasal route. (PubMed, Drug Dev Ind Pharm) - "Objective: This research work aimed to form vesosomes using combination of two drugs ergotamine and caffeine for synergistic activity when given intranasally resulting in faster absorption, steric stability and controlled release.Significance: The multicompartment vesicles viz., vesosomes of ergotamine tartrate proved to increase absorption of drugs post-intranasal administration, bypassing the blood-brain barrier via the olfactory pathway The phospholipids like soya lecithin, cholesterol and dipalmitoyl phosphatidylcholine were used to form a multicompartment structure called vesosomes using ethanol-induced interdigitation of lipids as the preparation method. The formulation showed low particle size of 315.48 ± 14.27 nm with zeta potential of -21.78 ± 4.72 mV, higher % EE of 91.13 ± 1.29% and controlled release kinetics, when assessed for in-vitro and ex-vivo studies as 97.64 ± 5.13% and 82.25 ± 3.27% release, respectively. Vesosomes displayed..."

Journal • CNS Disorders • Migraine • Pain

Potentially Inappropriate Use of Opioids in the Management of Migraine in Colombia. (PubMed, Biomedicines) - "The frequent use of opioids in the management of migraines is potentially inappropriate and can lead to problems of tolerance, abuse and dependence. This combined with the low prescription of triptans, offers an opportunity for improvements in medical practice."

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

Use of 3D applicator for intranasal microneedle arrays for combinational therapy in migraine. (PubMed, Int J Pharm) - "The novel 3D applicator effectively delivered the microneedle array into the nasal cavity for systemic action. Therefore, the fabricated rapid dissolving microneedles combining two drugs ergotamine and caffeine with use of 3D applicator proved to be a coherent technique for intranasal delivery of ergotamine in the treatment of migraine."

Journal • CNS Disorders • Migraine

Self-Assembled Lipid Polymer Hybrid Nanoparticles Using Combinational Drugs for Migraine Via Intranasal Route. (PubMed, AAPS PharmSciTech) - "Histopathological investigations and serotonin toxicity studies in animals confirmed the safe and non-toxic nature of the formulation while the acetic acid writhing test proved the anti-hyperalgesic activity. The PEGylated lipid polymer hybrid nanoparticles of ergotamine and caffeine showed synergistic activity with efficacious higher anti-migraine potential."

Journal • CNS Disorders • Migraine

Validated HPLC-DAD and Spectrophotometric Methods for Simultaneous Determination of Ternary Mixture of Analgin, Caffeine, and Ergotamine. (PubMed, J AOAC Int) - "The developed HPLC-DAD method has a high sensitivity for ergotamine. The spectrophotometric methods offer novelty, green solvent usage, and economic cost."

Journal • CNS Disorders • Migraine

2022 Taiwan Guidelines for Acute Treatment of Migraine. (PubMed, Acta Neurol Taiwan) - "Among them, migraine-specific triptans (oral or nasal spray formulations) and migraine-nonspecific acetaminophen and NSAIDs (diclofenac, ibuprofen, naproxen) are highly recommended because they are supported by strong evidence and demonstrate high efficacy. Prochlorperazine injection has been upgraded to a highly recommended level because of the rich clinical experience for this treatment...High-dose aspirin was downgraded to rescue treatment because of potential gastrointestinal side effects. Although evidence supports the combination of oral tramadol and acetaminophen, this combination should be used as a rescue treatment due to concerns about dependence. Evidence supporting the use of intravenous tramadol or morphine is insufficient; therefore, their use is not recommended...For moderate to severe attacks, oral or nasal spray triptans and ergotamine/caffeine compounds are recommended and should be administered in the early stage of migraine attacks...To prevent..."

Journal • CNS Disorders • Gastrointestinal Disorder • Migraine • Pain

Simultaneous determination of ergotamine, caffeine and dipyrone in their ternary mixture by applying double divisor and first derivative ratio spectra methods. (PubMed, Ann Pharm Fr) - "Regarding method B, the limits of detection and quantitation for EGT were 0.604 µg/mL and 1.829 µg/mL respectively: with corresponding values of 19.44 µg/mL and 58.92 µg/mL for CAF and 20.44 µg/mL and 61.9 µg/mL for DIP. The obtained results were compared to those obtained by published methods and were found to be in accordance."

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Acute Treatments for Episodic Migraine in Adults: A Systematic Review and Meta-analysis. (PubMed, JAMA) - "Compared with placebo, calcitonin gene-related peptide receptor antagonists (low to high SOE), lasmiditan (5-HT1F receptor agonist; high SOE), dihydroergotamine (moderate to high SOE), ergotamine plus caffeine (moderate SOE), acetaminophen (moderate SOE), antiemetics (low SOE), butorphanol (low SOE), and tramadol in combination with acetaminophen (low SOE) were significantly associated with pain reduction and increase in mild adverse events. Use of triptans, nonsteroidal anti-inflammatory drugs, acetaminophen, dihydroergotamine, calcitonin gene-related peptide antagonists, lasmiditan, and some nonpharmacologic treatments was associated with improved pain and function. The evidence for many other interventions, including opioids, was limited."

Clinical • Journal • Retrospective data • Review • Addiction (Opioid and Alcohol) • CNS Disorders • Immunology • Migraine • Pain

The effects of caffeine in adults with neurogenic orthostatic hypotension: a systematic review. (PubMed, Clin Auton Res) - "Caffeine should only be considered as a treatment for adults with neurogenic orthostatic hypotension when evidence-based treatments have been exhausted."

Clinical • Journal • Review • Hypotension

[VIRTUAL] Overt ergotism due to overuse of ergotamine-caffeine (AHS 2021) - "Ergotism is a rare but serious complication of ergotamine overuse. ergotamine exerts effects on multiple neurotransmitter pathways including norepinephrine and dopamine that can result in vasoconstriction and nausea/vomiting, respectively. The use of ergotamine is recommended only to a subset of patients given its significant side effect profile."

CNS Disorders • Depression • Migraine • Pain • Psychiatry

Greenness Profile Assessment of Selective Liquid Chromatographic Methods for Determination of a Quaternary Anti-migraine Combination Along with Three of Their Related Official Impurities. (PubMed, Biomed Chromatogr) - "Two selective, sensitive and environmentally safe liquid chromatographic methods were developed and validated for determination of paracetamol, caffeine, ergotamine tartrate and metoclopramide in co-formulated anti-migraine tablets along with P-aminophenol, P-nitro phenol and theophylline as officially specified impurities. The greenness profile evaluation was carried out using three tools; National Environmental Method Index, Analytical Eco-Scale, and Green Analytical Procedure Index tool and a comparative study was then conducted. Successful application of the developed methods for determination of the cited quaternary mixture in Metograine® tablets, affirms their suitability regarding the analytical performance and ecological impact in quality control assay and impurity profiling purposes."

Journal • CNS Disorders • Migraine

Validated ecofriendly chromatographic method for quantitative determination of anti migraine quaternary mixture. (PubMed, J Sep Sci) - "A novel ecofriendly, cost and time saving high performance thin layer chromatographic method was developed and validated for simultaneous determination of metoclopramide, ergotamine, caffeine and paracetamol in bulk and pharmaceutical formulation. The greenness profile assessment was achieved to the proposed method to evaluate its greenness characters to the environment with acceptable results. Validation parameters were checked according to International Conference of Harmonization guidelines to achieve the international requirements for quality control analysis of the proposed drugs."

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Drug-Drug Interaction of Ergotamine with a Combination of Darunavir, Abacavir, and Lamivudine Causing a Fatal Vasospastic Ischemia. (PubMed, Case Rep Emerg Med) - "...Clinicians were not aware that patient was self-medicating for years with medication containing ergotamine and caffeine for migraines...Treatment was started with intravenous nimodipine and intra-arterial sodium nitroprusside on the affected limbs. The patient developed severe limb ischemia, cerebral ischemia, and metabolic encephalopathy. Unfortunately no improvements were noticeable and due to evolving cerebral edema as a result of the ischemia, the patient developed brain herniation and died shortly after."

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