The prevalence of sleep-related disorders is one of the increasing challenges among individuals of all ages, causing a heightened desire in the affected individuals to use sleep aids and over-the-counter (OTC) medications. However, prescription and OTC medications can provide short-term relief from sleep issues, both types of medications can pose significant risks and concerns regarding patient safety. This blog explores the necessary knowledge to support patients and care professionals in choosing appropriate sleep medication options and obtaining safe, effective sleep solutions.
What are Sleep Medications: Classification & Pharmacology
- How Sleep Medications Work
Sleep medications work through modulating neuro chemical pathways that control the circadian timing, cognitive arousal and state of alertness.
- GABAergic modulation
Prescription hypnotics including benzodiazepines or Z-drugs elevates the effect of Gamma-aminobutyric acid modulation, a primary inhibitory neurotransmitter. This causes sedation and calming brain activities for optimal sleep.
- Melatonin receptor agonism
The consumption of certain sleep drugs like remelteon can aid in mimicking melatonin by stimulating MT1 or MT2 receptors, regulating the circadian rhythm and facilitates sleep harmony.
- Orexin (hypocretin) system inhibition
Orexin is responsible neuropeptide for the state of wakefulness. Certain medications can suppress the orexin system and reduce the impact of nighttime arousal, promoting good, uninterrupted sleep.
- Histamine receptor blockade
Histamine is a neurotransmitter that contributes to a state of alertness. OTC antihistamines or some antidepressants like doxepin in a small dosage, can help block the H1 histamine receptors as a result of sedation and drowsiness.
- Serotonergic modulation in off-label uses
Some anti depressants such as trazodone can improve sleep quality by inhibiting serotonin or histamine receptors, especially in scenarios of patients having mood disorders and insomnia.
Safety Risks and Characteristics of Sleep Medications
- Benzodiazepines
Strong effects on GABAA receptors facilitate quick onset of sleep. These medications are especially beneficial for individuals experiencing severe forms of insomnia or insomnia treatment due to anxiety. It has been widely utilized in various conventional practices with the background of extensive research into its pharmacological action. The three drug types are; short acting (triazolam), intermediate (temazepam), and slow to act (diazepam)
Risks
- Loss of tolerance can develop with a prolonged period of continuous consumption
- May lead cognitive impairment
- Drowsiness during day time and decreased reaction frequency
- Increased falling risk, mainly for the older person
- Occurrence of withdrawal symptoms post discontinuation
- Z-Drugs (Zolpidem, Zopiclone, Eszopiclone)
Z=drugs mainly target GABAA receptors more selectively outperforming benzodiazepines. These are effective for initiating sleep and in some scenarios used for maintaining sleep quality. Generally shorter-half lives than benzodiazepines; thus, less effect on the next day. Typically, prescribed for curing short-term insomnia issues.
Risks
- Sleepwalking, driving in a sleep state, or other complex behaviors while asleep
- With higher doses, the impacts can lead to cognitive impairment and excessive sleepiness for the following day
- When used for an extended period of time, they have the potential to lead to a dependence or risks of cardiovascular disease
- When stopped suddenly, rebound insomnia may likely to occur
- Older adults can have problems with coordination
- Melatonin & Melatonin Receptor Agonists
Regulates the body’s biological clock rather than acts as a sedative. The drug is used for issues like phase delays, jet lag, and shift-work disorder. It does not influence over dependence and has little to no tolerance. Most patients can prefer for long term use based on the clinicians recommendation.
Risks
- May have mild headaches, dizziness, and vivid dreams with the use of higher doses.
- When taken with anticoagulants and some immunosuppressive drugs, there may be an interaction.
- Not all OTC Melatonin supplements are consistent in quality.
- Potentially leading hormonal changes for those taking long periods of time and at high doses.
- Dual Orexin Receptor Antagonists (DORAs)
Example: Suvorexant, Lemborexant, Daridorexant
These can aid in decreasing awake time, as opposed to induce sleep. It has less respiratory depression than GABA Receptor Agonists. Dual orexin receptors can be advantageous for those who have trouble maintaining sleep throughout the night.
Risks
- Some patients may experience sleepiness the next day if taken too close to bed time
- Mild sleep paralysis in some cases or chances of seeing abnormal dreams
Safe Use Guidelines for Patients
- Follow prescriptions
Follow up medications exactly as the doctor’s prescription. Avoid changing the dosage without professional consultation. Schedule periodic assessment with a healthcare professional to validate the necessity, dosage and side effects checks.
- Monitor adverse effects
Evaluate symptoms like daytime drowsiness, cognitive slowing, balance problems, unusual sleep behaviors regularly. Patients may recommend professional advice for reevaluation.
- Avoid alcohol, opioids, or CNS depressants
Some drugs have adverse complications with the consumption of alcohol. It include complications like high blood pressure, respiratory suppression, cognitive impairment, lasting sleepiness or sedation.
Conclusion
The use of sleeping pills has a range of risk factors such as addiction or dependence, cognitive dysfunction, decreased alertness, unusual behaviors during sleep (such as sleepwalking), and consecutive long-term changes in how much we sleep and the type of sleep we experience.
Therefore, its necessary for both the healthcare professionals and consumers alike to conduct a potential risk assessment of sleep aid or medication drug applications, along with evaluating the patient’s age, gender, medical conditions and overall health history. If pharmacotherapy is chosen as the treatment option, the prescribing clinician must select the safest and most effective class of sleep aids, at the lowest prescribed dose for the shortest value time in order to minimize any potential risk to the patient.
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