Is pitolisant a stimulant?
What is Pitolisant? Pitolisant is a novel treatment for Narcolepsy
Persistent neurological disease that includes a diminished capacity to control sleep wake cycles.
and works as an inverse agonist/antagonist histamininergic agent, with selectivity for the Histamine H3 receptor
Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act as autoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release.
. Animal studies show that it acts as a stimulant.
What is the mechanism of action of Pitolisant? The mechanism of action of pitolisant is unclear, but may be mediated through its activity as an antagonist/inverse agonist at histamine-3 receptors. Metabolized by CYP2D6 and to a lesser extent by CYP3A4 to inactive metabolites
Are there any side effects to taking Pitolisant? Pitolisant Clinical Trial Results. In a recent clinical trial on 259 patients, the drug was found to be effective and relatively safe. The 109 patients treated with Pitolisant were observed to have decreased day time sleepiness and were more alert. The most common side effects observed in the trials were insomnia, nausea and headache.
How is Pitolisant used to treat narcolepsy? Pitolisant is used to treat excessive daytime sleepiness caused by narcolepsy (a condition that causes excessive daytime sleepiness) and to treat cataplexy (episodes of muscle weakness that begin suddenly and last for a short time) in adults with narcolepsy. Pitolisant is in a class of medications called H 3 blockers.
What kind of birth control can you use with Pitolisant? Pitolisant can make hormonal birth control less effective, including birth control pills, injections, implants, skin patches, and vaginal rings. To prevent pregnancy while using pitolisant, use a barrier form of birth control: condom, diaphragm, cervical cap, or contraceptive sponge.
How is Pitolisant used in the treatment of narcolepsy?
How is Pitolisant used in the treatment of narcolepsy? All narcolepsy patients show excessive daytime sleepiness, while approximately two-thirds of them experience catalepsy. Pitolisant is a potent and highly selective antagonist or inverse agonist of the histamine-3 (H 3) receptor.
When did the FDA approve the use of Pitolisant? Commonly marketed under the trade name Wakix, oral pitolisant was approved by the EMA in 2016 7 for the treatment of narcolepsy with or without cataplexy. 8 FDA approved the use of pitolisant in 2019 for excessive daytime sleepiness (EDS) associated with narcolepsy in adults. 10
What is the molecular formula of Pitolisant hydrochloride? Pitolisant is an antagonist/inverse agonist of the histamine-3 (H3) receptor. Pitolisant hydrochloride is a white or almost white crystalline powder with a molecular formula of C 17 H 26 ClNO•HCl and a molecular weight of 332.31.
What happens when Pitolisant is combined with adenosine? Adefovir dipivoxil may decrease the excretion rate of Pitolisant which could result in a higher serum level. Adenosine may increase the QTc-prolonging activities of Pitolisant. The serum concentration of Afatinib can be increased when it is combined with Pitolisant.