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Common otology viva topics
Published in Joseph Manjaly, Peter Kullar, Advanced ENT Training, 2019
Betahistine: A histamine H3 receptor antagonist and weak H1 agonist. Postulated to work by reducing endolymphatic hydrops through improvements in microcirculation. The drug is generally well tolerated and is effective in some patients however the BEMED trial found no difference in symptom control between betahistine and placebo groups.
Third Histamine Receptor: From Discovery to Clinics, Long-Lasting Love Story at INSERM and Bioprojet
Published in Divya Vohora, The Third Histamine Receptor, 2008
For these reasons, we decided to embark on a medicinal chemistry H3 project in a purely academic environment. However, although we had in hands a model to test new molecules on the novel target, we had neither the know-how nor the facilities to prepare such molecules in the laboratory. At this time, I participated with Jeanne-Marie in a dopamine symposium that took place in Beerse, in Paul Janssen’s laboratory, during which one of his collaborators showed 3D formulas of neuroleptics and discussed their analogy with the structure of dopamine. This gave me the very straightforward idea that we could, in a parallel way, imagine obtaining an H3-receptor antagonist, starting from the structure of histamine, maintaining its imidazole ring, and replacing the ethylamine chain by a piperidine residue. We submitted the idea to Max Robba, a professor of medicinal chemistry at the University of Caen, in Normandy, that we both knew because he had given pharmacochemistry courses to both of us at the Parisian Faculty of Pharmacy, and, even more, Jeanne-Marie had prepared her PhD in his laboratory. Max accepted enthusiastically to collaborate on this project; Bioprojet provided him a salary for a technician who started to synthesize molecules according to the line imagined in Beerse, and these molecules were tested on brain slices of rat against histamine at our INSERM laboratory. After no more than a few dozen molecules prepared and tested in this way, structure—activity relationships had become quite clear, and we obtained thioperamide, a compound displaying low nanomolar affinity as a competitive antagonist, as revealed by Schild plot analysis. Thioperamide was not only the first selective H3-receptor ligand in vitro, but we rapidly showed that, given systemically in low dosage to rats, it also enhanced markedly the turnover of histamine in brain as measured by pulse-labeling the endogenous pool with 3H-histidine, a very reliable technique that we had developed a few years before. We were quite excited by this result because we realized that we had designed the first drug able to activate histaminergic neurons in brain, that is, an important tool to characterize their functional role, a tool that was lacking at this time.
Current and emerging pharmacotherapeutic strategies for Tourette syndrome
Published in Expert Opinion on Pharmacotherapy, 2022
There are a few recent studies on emerging treatments for TS that modulate histaminergic, noradrenergic, and serotonergic pathways [33]. A trial investigating atomoxetine, a noradrenaline reuptake inhibitor which might improve response inhibition parameters in patients with TS, has been registered. An H3-receptor antagonist called AZD5213 has been assessed for safety and tolerability in patients with TS, however it has not shown any significant difference compared to placebo. Pimavanserin is a serotonin receptor inverse agonist (without dopamine receptor antagonist properties) which is approved for the treatment of Parkinson’s disease psychosis. The results of a recent open-label phase 1 pilot study to evaluate pimavanserin in the treatment of motor and behavioral symptoms in adults with TS were encouraging and warranted further research by larger, placebo-controlled, trials [92]. Of note, the adverse effects of pimavanserin were reported to be common but not severe (headache, bloating, dizziness, drowsiness, nausea, and dysgeusia. A significant degree of tic reduction was demonstrated when D-cycloserine, an antibiotic with learning enhancing properties, was administered to patients with TS undergoing habit reversal training (as compared to patients treated with habit reversal training and placebo) [93]. A follow-up study of D-cycloserine augmented habit reversal training for youth with tic disorders has been registered.
Pitolisant for treating patients with narcolepsy
Published in Expert Review of Clinical Pharmacology, 2020
Pitolisant is an H3 receptor antagonist/inverse agonist. It was approved by the European Medicines Agency (EMA) for the treatment of narcolepsy with or without cataplexy in March 2016 [40,46], and was approved by the US FDA for the treatment of EDS in adult patients with narcolepsy in August 2019. The recommended dosage range for pitolisant is 17.8 mg to 35.6 mg, administered orally once daily in the morning upon wakening. Pitolisant is contraindicated in patients with severe hepatic impairment. Pitolisant prolongs the QT interval, it should be avoided in patients with a history of cardiac arrhythmias [12,13].
Strategies to counter antipsychotic-associated weight gain in patients with schizophrenia
Published in Expert Opinion on Drug Safety, 2019
Wade Marteene, Karl Winckel, Sam Hollingworth, Steve Kisely, Erin Gallagher, Margaret Hahn, Bjørn H Ebdrup, Joseph Firth, Dan Siskind
More recently betahistine has shown promising results. This is a centrally acting histamine H1 receptor agonist and H3 receptor antagonist that reverses olanzapine-induced weight gain in mice [129]. It is relatively well tolerated and is used to treat vestibular disorders [130]. A study in 48 healthy female patients demonstrated that pre-treatment with betahistine as monotherapy for one week prior to coadministration of betahistine and olanzapine for two weeks reduced weight gain compared to placebo and olanzapine (1.24 kg gain vs 1.93 kg gain) [131].