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Combined hormonal contraception
Published in John Guillebaud, Contraception Today, 2016
This applies chiefly to epileptic women and women being treated for tuberculosis. This situation is WHO 3, meaning that an alternative method of contraception such as an IUC is preferable – especially for women taking rifampicin or rifabutin, whose effects on the efficacy of CHCs are so strong that long term users should use another method (WHO 4). Moreover, with the teratogenic anti-epileptic drugs (e.g. rufinamide), pregnancy could be catastrophic.
A reappraisal of atypical absence seizures in children and adults: therapeutic implications
Published in Expert Opinion on Pharmacotherapy, 2019
Francesco Brigo, Pasquale Striano, Vicenzo Belcastro
Adjunctive stiripentol was found to be able to reduce by 70% (range 5–95%) atypical absence seizures in 10 patients with uncontrolled seizures (more than one seizure a day). The tolerability was good, with only some patients experiencing dose-related adverse effects (anorexia, nausea, vomiting, and sedation) [42]. Stiripentol is currently authorized in the European Union and in the United States as adjunctive treatment of seizures associated with DS.Rufinamide was also reported to be effective in the treatment atypical absence seizures, and in a randomized, placebo-controlled trial on LGS conducted in 138 patients, this drug administered as adjunctive treatment decreased the atypical absence frequency by 50.6% compared to 29.8% in the placebo group [43]. Rufinamide is currently authorized in the European Union and in the United States for adjunctive therapy in the treatment of seizures associated with LGS.
Evaluation of WO2014121383 A1: a process for preparation of rufinamide and intermediates
Published in Expert Opinion on Therapeutic Patents, 2019
Barnali Maiti, Balamurali M M, Kaushik Chanda
The patent mentioned in this manuscript only described about processes for the synthesis of rufinamide and intermediates thereof. Since it is already having US FDA approval in 2008, so all the patent processes described in the literature mainly discussed about the different synthetic routes. The precise mechanism(s) by which rufinamide exerts its antiepileptic effect is unknown[18]. Rufinamide is used as a drug for the treatment of epileptic disorders. In general, it acts by slowing down the activation of sodium channels and thus negatively influences the sodium-dependent action potentials in neurons[19]. This also helps in the prediction of efficacy towards determining the seizure types and epileptic syndromes. As indicated by patch clamp technique, rufinamide acts on the inactive sodium ion channels and slows down its activation [3,20]. This might help to block the spread of seizure activity in epileptogenesis. The results of in vitrostudies suggest that rufinamide may prolong the inactive state of plasma membrane sodium channels. In vitro studies have shown that rufinamide reduces the frequency of sodium-dependent actions potentials in the neurons of animal models. This could aid to block the spread of seizure activity during epileptogenisis. Rufinamide did not significantly interact with a number of neurotransmitter systems, including GABA, benzodiazepine, monoaminergic and cholinergic binding sites, NMDA, and other excitatory amino acid binding sites. In vivo anti-convulsant studies examined the ability of rufinamide to suppress both electrically and chemically induced seizures as well as partial seizures. Following oral or intraperitoneal administration, rufinamide potently suppressed maximal electroshock-induced seizures. Rufinamide was also effective, but comparably less potent, in antagonizing chemically induced clonic seizures. The protective index and safety ratio of rufinamide were comparable to or better than other Antiepileptic drugs.
Novel investigational therapeutics for generalized anxiety disorder (GAD)
Published in Expert Opinion on Investigational Drugs, 2019
Bella Schanzer, Ana Maria Rivas-Grajales, Aamir Khan, Sanjay J Mathew
Cannabidiol exerts its effect through the endocannabinoid system. It has a variety of receptors that are found throughout the body, the most well-described ones are G protein-coupled receptors CB1 and CB2 [66]. Cannabidiol is being studied for use in multiple therapeutic indications including anxiety, pain management, seizures, sleep and a number of others. Processes related to cannabinoids may be involved in cognition, memory, inflammation, and immune responses [67–69].Echinacea angustifolia is a plant from North America that is thought to have anxiolytic effects via alkamides that binds cannabinoid CB1 and CB2 receptors [70]. There is an ongoing trial studying the effects of this plant on sub-threshold and mild anxiety in subjects that are not eligible for anxiolytic medications. This was driven by preliminary findings demonstrating the positive effects of this root extract in healthy participants [71].Rufinamide is a medication initially developed for epilepsy which functions through the protection against excitotoxic neuronal damage possibly through anti-oxidant and anti-inflammatory activities. It is a triazole derivative that is structurally unique amongst anti-epileptic medications [72]. In addition, rufinamide has been found to increase neurogenesis through increasing immunoreactivity of insulin-like growth factor-1, its receptor, and phosphorylated cAMP neurotrophic factor and its receptor [73].BNC210 is an anxiolytic drug that works via negative allosteric modulation of the α7-nicotinic acetylcholine receptor. Preliminary evidence showed attenuation of amygdala responses to fearful faces in 24 patients with GAD who received BNC210, which demonstrates the role of the cholinergic system in this disorder [74].