"Instant Sleep" or Health Red Light Signal! Pitolisant might be able to pull patients with narcolepsy out of the abyss of deep sleep

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Author : sarms4muscle
Update time : 2023-09-15 11:19:21

About one-third of our life time in sleep, as the maintenance of human life is extremely important physiological functions, sleep is vital to the human body. But "can't sleep" has become a common problem that plagues many modern people, survey data show that more than 300 million people in China have sleep disorders, the incidence of insomnia in adults nearly 40%. As a result, many people equate "sleeping in seconds" with quality sleep and consider it a sign of good health. However, this may also be one of the symptoms of episodic sleep disorder.

Episodic Narcolepsy is a rare form of central sleepiness, with the prevalence of Type 1 Episodic Narcolepsy ranging from 25 to 50 per 100,000 people and Type 2 Episodic Narcolepsy ranging from 20 to 34 per 100,000 people.


Episodic sleeping sickness is a disabling neurological disorder in which the patient is unable to properly regulate the sleep-wake cycle, resulting in symptoms of narcolepsy manifested by excessive daytime sleepiness or recurrent episodes of uncontrolled sleep during normal wakefulness, as well as sudden episodes of muscle weakness (sudden collapse). It is a globally recognized rare disorder, with published epidemiological data showing a worldwide prevalence of between 0.00023% and 0.05%.


Obstructive sleep apnea (OSA) is a severely underestimated chronic condition characterized by recurrent apnea and hypoventilation events due to partial or total collapse of the upper airway during sleep, leading to intermittent hypoxia and sleep fragmentation. The disease is prevalent in the elderly, men, obese and smokers, and it is likely that the prevalence of OSA will continue to rise, especially with the increase in obesity in recent years.


People with episodic Narcolepsy often fall asleep unknowingly and without warning during the day (daytime sleepiness), and often experience hallucinations and sleep paralysis before falling asleep at night. In addition, in type 1 episodic sleep disorder, the patient may also experience a sudden onset of localized or generalized muscle weakness and fall to the ground, which is referred to as "sudden collapse". Although Narcolepsy itself is not directly fatal, the symptoms of the disease can be as dangerous as some fatal diseases.


Currently, more than a dozen medications have been accumulated for the treatment of episodic sleep disorders, but they still have significant shortcomings and do not fully meet the needs of patients.


For example, Modafinil, a first-line drug, was ineffective in about 40% of patients in clinical trials despite its high efficacy, few side effects, and virtually no risk of abuse, and was ineffective against sudden collapse; Xywav, while effective against both daytime sleepiness and sudden collapse, has high side effects and is very expensive, with a one-month dose priced at about $13,000 (roughly 910,000 yuan), and is also highly addictive.


Against this background, Pitolisant cas: 903576-44-3 was introduced and became a market favorite with a variety of advantages such as effectiveness no less than first-line drugs, fewer side effects, non-addictive, and the ability to treat both daytime sleepiness and sudden collapse.


Pitolisant cas: 903576-44-3 is a psychotropic drug, a selective histamine 3-receptor antagonist/inverse agonist, which increases the synthesis and release of the arousal-promoting neurotransmitter histamine in the brain by potentiating the activity of histaminergic neurons, improving wakefulness and alertness in patients.


Pitolisant cas: 903576-44-3 is used for the treatment of episodic somnolence, one of the globally recognized rare disorders, which is a severe, chronic condition characterized by excessive daytime sleepiness


What is Pitolisant HCL pilLs tablet?

Pitolisant HCL pilLs tablet is not a hormone drug, in clinical practice Pitolisant HCL pilLs tablet belongs to the class of drugs called antihistamines. It generally has anti-allergic and anti-inflammatory effects and is often used to treat atopic dermatitis, chronic urticaria, allergic rhinitis, allergic conjunctivitis and other diseases.


Pitolisant is a histamine H3 receptor antagonist/inverse agonist that enhances histaminergic transmission in the brain, enhances the release of acetylcholine in the prefrontal cortex and hippocampus, and enhances the release of dopamine in the prefrontal cortex.


However, there is a possibility of drowsiness, fatigue, lack of concentration, dry mouth and nausea while taking this drug. Therefore, it is important not to drive, work at heights, or engage in delicate work while taking the drug, and not to take Valium drugs or alcohol at the same time as taking Cetirizine Hydrochloride Tablets.


Pitolisant cas: 903576-44-3 is a new FDA-approved, non-controlled drug for episodic somnambulism, a "first-in-class" selective histamine 3 (H3) receptor antagonist/inverse agonist, which works through a novel mechanism of action, i.e., by enhancing histaminergic neuronal activity, increasing the synthesis and release of the neurotransmitter histamine in the brain, which promotes wakefulness and alertness. It works through a new mechanism of action, i.e., by enhancing the activity of histaminergic neurons, it increases the synthesis and release of histamine, a neurotransmitter that promotes arousal in the brain, and thus improves patients' wakefulness and alertness, and it has been approved for marketing in Europe and the United States, with a certain degree of market potential.


DAUVILLIERS Y et al. conducted a clinical study of the efficacy of Pitolisant cas: 903576-44-3 versus Modafinil in the treatment of episodic somnambulism in which patients were randomly assigned to the Pitolisant group of 10 mg, 20 mg, or 40 mg versus the Modafinil group of 100 mg, 200 mg, or 400 mg (both doses determined at the discretion of the investigator) and the placebo group. groups (both drug doses were determined at the investigator's discretion) as well as a placebo group, and data were analyzed as between-group differences in mean ESS (a subjective scale evaluating the degree of somnolence) scores at the endpoint.

During the 8-week treatment period, the minimal mean reduction in ESS was 3.4 in the placebo group, 58 in the Pitolisant group, and 6.98 in the Modafinil group.The between-group differences in the endpoints showed superior efficacy of Pitolisant over placebo in the treatment of patients with episodic somnambulism; and there was a reduction in the frequency of sudden daily collapses in the Pitolisant group as compared with the placebo group, while the Modafinil had no anti-sudden collapse effect. This study suggests that Pitolisant, in addition to its wakefulness-promoting effects comparable to those of Modafinil, also has some anti-sudden collapse effects.


The KOLLB-SIELECKA M study, which focused on the efficacy of lower doses of Pitolisant in patients with episodic narcolepsy, found that the difference in the value of the change from baseline in the Epworth Sleepiness Scale scores in the Pitolisant group versus the placebo group was not statistically significant, but that, when assessing efficacy with the Maintenance of Wakefulness Test, an objective test for evaluating the degree of sleepiness, the Pitolisant group (1.14 min increase in awake time from baseline) was superior to the placebo group (1.39 min decrease in awake time from baseline). The Pitolisant group (1.14 min increase in awake time from baseline values) was superior to the placebo group (1.39 min decrease in awake time from baseline values). In terms of anti-snooze, the weekly rate of snooze improvement versus placebo was 0.512, which further supports the pro-arousal and anti-snooze effects of Pitolisant.


In a trial investigating the efficacy of Pitolisant in patients with episodic somnolence, SZAKACS Z et al. designed a 3-week flexible dosing period (Pitolisant doses of 5-20 mg/d) plus a subsequent 4-week stabilization dosing period (Pitolisant doses of 5-40 mg/d), and found that compared with the placebo group the Pitolisant group showed significant improvement in both the rate of sudden collapse and drowsiness scores. The safety and efficacy of high-dose Pitolisant (up to 40mg/d after the titration period) for the treatment of episodic sleepiness (with or without sudden collapse) in adults was also evaluated. The results of the study also showed that Pitolisant improved the main symptoms of episodic somnolence, including EDS, sudden collapse, and sleep onset hallucinations.


As a new drug for the treatment of episodic somnolence, there are fewer safety studies on Pitolisant. Romigi et al. conducted a meta-study of the drug for the treatment of episodic somnolence, which showed that the overall safety profile of Pitolisant was good, with the main side effects being mild headache (16%), insomnia (8%), anxiety (4%), depression (2%), hallucinations (2%) and vertigo ( 1%). And an important advantage of Pitolisant over other wakefulness-enhancing drugs is that there is no or very low potential for abuse.


As a new therapeutic strategy for episodic somnolence, Pitolisant offers new possibilities for the treatment of the disease with its improved EDS and anti-sudden collapse effects shown in clinical studies, but its long-term efficacy and safety still need to be corroborated by more clinical trials. In addition, the pathogenesis of episodic somnolence has not been fully elucidated, and the mechanism by which therapeutic agents improve the symptoms of episodic somnolence needs to be further investigated. Therefore, there is still a long way to go in the research of the treatment of episodic somnolence, and we need to invest more in the research of these issues, so that patients with episodic somnolence can be relieved of their pain and suffering as soon as possible.


How does schizophrenia develop?

The etiology of schizophrenia is still unclear. It mostly starts in young adults, and the course of the disease is prolonged and progresses slowly, with the possibility of developing into a recession. It is a class of psychotic disorders with basic personality changes, splitting of thinking, emotion and behavior, and incongruity between mental activities and the environment as the main manifestations. There are usually no consciousness disorders and intellectual disorders, and cognitive impairment may occur.


It may be related to the following factors:

1, genetic factors, current research has found that schizophrenia is a polygenic genetic disease.

2Environmental and psychosocial factors, including maternal pregnancy and perinatal infection comorbidities.

3Neurobiochemical studies, including the doctrine of dopamine hyperactivity and the 5-hydroxytryptamine hypothesis.

4, Studies of the pathologic anatomy and structure of the brain, including findings from magnetic resonance, CT, PAT, and others.

5, Neurodevelopmental models of pathogenesis, including studies in epidemiology, neuroectodermal studies, etc.

6. Neurophysiological studies, etc.