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Sleep Medications – the Good, the Bad and the Ugly

Written By M. Ryan Odom, MD

Sleep Medications – the Good, the Bad and the Ugly

May 9, 2022

To recap, we have discussed the mainstay of treatment for insomnia: sleep hygiene and non-medication techniques. Today, I am going to address medications and supplements. It is important to recognize that all substances we put into our body have side effects. Often the medications we use for sleep are habit forming or addicting, have a hung over feeling in the morning, have small impact on total sleep, and can have significant side effects. The best use of these medications is to help establish a healthy routine for sleep at the lowest effective dose for a brief amount of time. This is a lot of information, but it is intended to be a good resource if you struggle with sleep or are using sleep aids.

Supplements:


Melatonin:
RISK OF DEPENDENCE: LOW
CONTROLLED SUBSTANCE: NO – OVER THE COUNTER
This is by far the most common supplement used to help with sleep. It is a natural occurring hormone that spikes during sleep. By supplementing with melatonin (ideally under 5mg), we believe it helps the brain to get into the mood to sleep. It is best taken approximately two hours before bedtime.

It has recently come under scrutiny for being poorly regulated and likely overused without fully understanding the impact on increased melatonin in our bodies. It still remains one of the first interventions for the low amount of side effects.

https://www.nccih.nih.gov/health/melatonin-what-you-need-to-know

WebMD has put together a good list of 14 other supplements that may be of benefit for sleep with their side effects and possible benefits.

https://www.webmd.com/sleep-disorders/ss/slideshow-natural-sleep-remedies

Medications:


Medications for sleep fall into a few broad categories that I will discuss in generalities. Each medication in these classes will have similar but also unique characteristics that are best to discuss with your physician.

The Z Drugs (hypnotics) – Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta)
RISK OF DEPENDENCE: Moderate
CONTROLLED SUBSTANCE: Schedule IV
COST: $$-$$$
These medications often improve sleep initiation by 10-20 minutes and sleep length by 20-45 minutes depending on the specific drug. They work on the GABA receptors similar to alcohol. Some of the most concerning adverse effects include sleep driving, eating, working or intercourse. There is abuse potential for these drugs, and they are controlled substances. These are often used for sleep cycle changes or travel related sleep challenges. There is a dependence that can develop to these medications over time as well. We will often use these to help get someone’s sleep cycle on track for brief periods of time (usually 2 weeks).

Benzodiazepines – Temazepam (Restoril), Quazepam (Doral) Ect
RISK OF DEPENDENCE: HIGH – up to 40% of regular users will have withdrawal symptoms
CONTROLLED SUBSTANCE: Schedule IV
COST: $
These Induce sleep through the same mechanism as alcohol affecting the GABA receptors. Chronic use disrupts the quality of sleep by distorting sleep architecture and diminishing deep sleep time. People who use this class for a prolonged amount of time report much greater fatigue than self-reported good sleepers. Because of the risk of abuse, the long-term affect on fatigue, these medications are not recommended for long term use and we very rarely prescribe them.

Tricyclic/quatracyclic antidepressants – Doxepin (Silenor), Mirtazapine (Remeron), Trazodone
RISK OF DEPENDENCE: MILD
CONTROLLED SUBSTANCE: NO
COST: $$
It is uncertain in the exact mechanism of action for this class of medications, but it is thought to be similar to antihistamines. It can improve sleep initiation and length by about 20 minutes each. Overall, these tend to be well tolerated, but at higher doses patients will often complain of a groggy feeling in the morning. They do not tend to create a dependence but if they are titrated up, they should be weaned off as well. Doxepin is the only FDA approved medication in this class for insomnia; the remainder are used off-label. These medications are often the safest in older adults.

Orexin Receptor Antagonist – Suvorexant (Belsomra)
RISK OF DEPENDENCE: MILD
CONTROLLED SUBSTANCE: Schedule IV
COST: $$$$
This is by far the newest (and most expensive) medication to treat insomnia. The orexin system regulates the sleep arousal cycle that promotes wakefulness. It decreased sleep latency up to 9.4 minutes and improved length of sleep by approximately 20 minutes. The most common side effect in fatigue but otherwise is well tolerated with low risk of dependence. Given cost and risk for abuse it is not first line at this time.

Antihistamines – Diphenhydramine (Benadryl), Doxylamine, Hydroxyzine
RISK OF DEPENDENCE: MILD
CONTROLLED SUBSTANCE: NO
COST: $
These medications are the most common sleep aids that are available over the counter. By affecting the histamine receptors, they induce a drowsiness that often leads to sleep. They are first line medications in pregnancy because they may be effective for nausea and insomnia, and they are thought to be relatively safe for the developing fetus. There have been some reports that prolonged use may increase your risk of dementia. Found in most medications that have a PM on them (AdvilPM, TylenolPM, ect). I recommend these in the setting of trying to reset a sleep cycle.

Antipsychotics – Olanzapine, Quetiapine, Risperidone
RISK OF DEPENDENCE: Not reported
CONTROLLED SUBSTANCE: NO
COST: $
All of these medications are used off-label to treat insomnia. The evidence for their use is weak, and in general should be avoided unless there is another indication to utilize. There are significant side effects and an increase risk of death. These are not first line, and I will rarely use these medications solely for sleep.

Anticonvulsants – Gabapentin, Pregabalin
RISK OF DEPENDENCE: MILD
CONTROLLED SUBSTANCE: Depends on state – Schedule IV
COST: $$
These medications have been found to improve sleep but the mechanism of action is not clear. The seem to improve sleep length by up to 45 minutes. Gabapentin is especially useful in patients with restless leg syndrome. The most common complaint of these medications is a hung over feeling in the morning at higher doses. These are reasonable to try as well to help control someone’s sleep. They are anticonvulsants, so coming off of them quickly can lower your seizure threshold.

That is a lot of medications for sleep. As I stated at the beginning, the best therapy for your insomnia is the non-pharmalogic techniques. If you are suffering from insomnia, please call our clinic to set up an appointment with Dr. Silakoski or myself to talk about it.

Sleep well,
M. Ryan Odom, MD
North Idaho DPC

References: https://www.aafp.org/afp/2017/0701/p29.html

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