Obstructive sleep apnea is caused by difficulty in the passage of air in the upper respiratory tract during sleep, which causes a lack of oxygen and fragmented and poor quality sleep. The disorder is caused by a certain anatomical structure and a decrease in muscle tension (tone) during sleep. This is a serious problem: the lack of oxygen during sleep may lead for cardiovascular diseases also to cognitive declineto metabolic disorders and even premature death. It is customary to count the number of breathing pauses during one hour of sleep for reception A quantitative measure of the severity of the condition – The higher the number, the more severe the condition: up to five breath pauses per hour are considered normal, five to 15 pauses – mild, between 15 and thirty pauses – moderate and over thirty pauses per hour – severe. The standard treatment today is the use of a device called cPAP – Abbreviation of Continuous Positive Airway Pressure. It is a kind of small blower, which flows high-pressure air during sleep through a face mask or even into the airways. The device is not invasive and its treatment is painless, but many patients do not persist in the treatment because it is uncomfortable. In 2017 Apnimed was founded with the aim of offering a more convenient alternative, and developed A treatment called AD109 which is based on two drugs approved by the FDA, the American Food and Drug Administration, for use in other conditions. After promising findings in an initial trial, a large clinical trial began in 2023, and last May was published Press release regarding his positive findings.
The two went together
The first drug Atomoxetine (atomoxetine), originally intended for the treatment of attention deficit hyperactivity disorder (ADHD), and is marketed in Israel under the trade names Atomic and Strattera. Atomoxetine inhibits the reabsorption of the neurotransmitter norepinephrine in synapses – the meeting points between nerve cells. The delay causes the neurotransmitter to continue activating the muscles of the throat and pharynx and, among other things, the muscles that pull the tongue forward and prevent it from falling back, which contributes to greater stability of the airways during sleep. However, atomoxetine may have a negative effect on sleep: patients take longer to fall asleep, and the quality of their sleep decreases.
dictation Originally published on the Davidson Institute for Science Education website
The new treatment combines atomoxetine with a derivative of Oxybutynin (oxybutinin), an old medicine for the treatment of irritable bladder. The drug blocks receptors for the neurotransmitter Acetylcholine in the nerve cells, thus reducing excess nerve activity in the areas of the brain that are responsible for tongue movements. in research In rats, it was found that oxybutynin stabilizes the activity pattern of the nerve cells that activate the tongue muscles, thus preventing abnormal oscillations or vibrations, which could damage the stability of the air passage.
For the new treatment, the company produced an experimental version of oxybutynin called Aroxybutynin (aroxybutinin), which allows for improved oral absorption and is expected to cause fewer side effects. The researchers estimate that the combination of the drugs creates a synergy: atomoxetine strengthens the tension of the muscles that keep the airways open, while eroxibutinin helps them work smoothly and stably and without “jumps”, which will allow continuous and continuous passage of air.
The combination of the drugs creates a synergy: atomoxetine increases muscle tension and pulling the tongue forward and eroxibutinin stabilizes the activity and prevents unwanted vibrations. On the right is a person with obstructive sleep apnea and on the left normal breathing during sleep Pixel-Shot, Shutterstock
A clinical trial showed that the combination of the two drugs reduces the number of sleep interruptions, that is, reduces the severity of the phenomenon, in 51 percent of the patients. 22 percent of them even reached a state of less than five breath pauses per hour – which is defined as a normal state. The company plans to submit to the FDA a new approval request for the drug treatment by the beginning of 2026, alongside the publication of the full results in a scientific article and conference, and continues In another clinical trial for a year.
The main advantage of the new drug treatment over the existing cPAP device treatment is that it will certainly be easier for patients to persist in taking oral drug therapy compared to being connected to the device all night.
This is not the only drug that has been studied in recent years for obstructive sleep apnea. medicine called tirzepatide For type 2 diabetes and weight reduction, approved in the United States under the name Zepbound for patients with obesity-related apnea. In contrast, the drug treatment AD109 directly targets the muscles of the airways and is also intended for patients who are not suitable for treatment based on weight loss. It is important to note that the drug has not yet been approved, and that long-term follow-up, of months and even years, is required in order to assess side effects, risks and benefits for patients. However, the results raise hope that this development could offer an alternative to the existing treatment and allow many to sleep better quality sleep, be less tired and avoid a variety of health problems that endanger those suffering from sleep apnea.
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