Natural alternatives for sleeping tablets

When you’re lying awake at night, running through your to-do list, or composing a mental email to John from accounting, you can blame glutamate.

Glutamate is the primary stimulating neurotransmitter responsible for wakefulness, cognition, learning and memory. Research suggests that around 70% of synapses, which carry information between cells in your brain, or from your brain to your body are facilitated by glutamate.

Glutamate is produced by brain cells– and when it’s running riot, ferrying messages around, it prevents the neurons responsible for sleepiness from releasing calming neurotransmitters like GABA.

GABA downregulates arousal in wakeful areas of the brain like the hypothalamus and the brainstem. When GABA floods your brain, it inhibits the production of glutamate, allowing you to fall asleep.  When GABA is released, it inhibits the production of glutamate.

Balance between GABA and glutamate is essential for healthy HPA axis regulation – a bodily system which influences sleep quality. Dysregulation of the HPA axis is caused by chronic stress, sometimes related to trauma, and can result in an overactive fight or flight response, disrupting sleep. 

Sleeping problems are multi-factorial and usually more complex than this singular pathway, but targeting GABA and glutamate offers some reprieve for those plagued by sleepless nights. 
Hypnotic sleeping medications like benzodiazepines (Xanax, Valium, Ativan, Klonopin) and Z drugs (zopiclone, lorazepam, diazepam) work by enhancing the effects of GABA, binding to receptors, which upon activation shift the body into sleepy mode. 

Dangers of benzodiazepines and Z drugs

Use of benzodiazepines (BZD) and Z drugs are on the rise in Hong Kong, despite them being highly addictive and affecting daytime cognition. Studies show that current BZD use is associated with lower brain volume of the parts responsible for memory. Current research hasn’t reached consensus on the effects of BZDs and Z drugs on memory long term. Physical dependency to both classes of drug are common and can develop over a short time, even when used exactly as prescribed.

Dependency can develop in as little as 4 weeks, but studies from Hong Kong show that of those prescribed BZDs and Z drugs between 2014 and 2023, 44.9% and 62.4% respectively exceeded the recommended limit of a 30 day prescription. One study found that 49.8% of those who had been taking benzodiazepines for 12 weeks or more, had developed physical and psychological dependency.

Withdrawal is common and experienced by between 20 and 50% of those who discontinue use. Sleeping problems are a symptom of withdrawal – the exact reason people are often prescribed the drug in the first place.

Withdrawal can also cause sweating, intense anxiety – as well as more severe and potentially fatal consequences. Weaning yourself off benzodiazepines or Z drugs should always be overseen by a medical professional.

If you’re spending long nights awake, don’t lose hope. Benzodiazepines and Z drugs aren’t the only substances that support the function of GABA – there are natural alternatives that support GABAergic signalling, for better sleep.

Magnesium, a natural alternative

Magnesium helps block the receptors for glutamate, quieting the mind at night time. Its effect on the glutamate pathway means magnesium also helps calm anxiety and relieve low mood, two factors which often contribute to poor sleep.

Magnesium supports GABA receptors, which has an indirect effect of upregulating GABA transmission, inhibiting the parts of the brain responsible for wakefulness so that you can sleep.
Magnesium inhibits other neurotransmitters known to stimulate the fight or flight response. Instead, it helps activate your parasympathetic nervous system, also known as your rest and digest response, during which you sleep and heal.

Low levels of magnesium cause HPA axis dysfunction and have been directly linked to sleeping problems.

Studies show that those with a higher intake of magnesium sleep for longer, have less disturbed sleep and fall asleep faster. One study demonstrated that magnesium threonate improved deep sleep, REM sleep, light sleep, energy upon waking and daytime productivity.

Our practitioners’ favourite magnesium formula is Magnesium Glycinate / Malate by Vital Nutrients – featuring a well-absorbed, therapeutic form of magnesium. Magnesium glycinate is created by binding magnesium to glycine (more on glycine later) which is an amino acid that acts as a calming neurotransmitter, supporting better relaxation and sleep.

Ashwagandha (Withania somnifera)

Ashwagandha is a herbal adaptogen which regulates your stress response. It’s been used traditionally in Ayurvedic medicine and a mounting body of evidence proves its ability to support better sleep and mental health. Its namesake reflects its therapeutic properties, as ‘somnifera’ translates from Latin to ‘sleep inducing’.

Studies have shown that Ashwagandha activates GABA. One study found that ashwagandha helps stimulate GABA receptors, calming arousal in the central nervous system for better sleep.

Drugs like benzodiazepines have been found to reduce deep sleep phases (also known as stage 3 and REM sleep) which are essential for you to wake feeling rested.

On the other hand, a study on those who experience non-restorative sleep, found that when taking ashwagandha for 6 weeks, a 72% increase in sleep quality was reported. The participants also slept for longer, fell asleep faster, and were less likely to wake after they started sleeping. Those taking the supplement reported increased quality of life.

Just like magnesium, ashwagandha helps regulate the HPA axis, which is key for sleep and mental health. A meta-analysis (a review of 22 studies on 1391 adults) found that ashwagandha significantly improved stress and low mood – two factors which influence your ability to fall asleep. The analysis showed that the best results occurred when ashwagandha was taken at a lower dose over a longer period of time – longer than 8 weeks.

Sereni-Pro by Bioclinic Naturals features a standardised, therapeutic form of ashwagandha, blended with other herbal adaptogens to ease stress and support better energy throughout the day, including Rhodiola Rosea, Siberian Ginseng and lavender.

Saffron

Research shows that Saffron has neuroprotective qualities, regulating HPA axis function, increasing resilience to stress and supporting better mental wellbeing.

Saffron has been shown in studies to increase levels of GABA in the brain. Multiple studies show that saffron increases sleep quality and duration by binding to and blocking glutamate receptors. The benefits of saffron were felt in as few as 7 days of treatment.

Additional research demonstrates its ability to reduce the time it takes to fall asleep in bed, as well as improving sleep quality and duration.

One of the ways in which saffron supports better sleep is by reducing pain.

Saffron Bioactive by Natroceutics features Affron® - the world’s leading saffron extract, favoured by scientists in their research. Affron® has been proven to reduce stress and low mood while improving sleep. This formula offers superior bioavailability and is absorbed within the hour.

L-theanine

L-theanine is an amino acid found naturally in green tea. It inhibits glutamate receptors to downregulate arousal, while upregulating GABA receptors.

Studies show that it can reduce stress 30 – 40 minutes after consuming it, lowering blood pressure and heart rate. It stimulates alpha brain waves – the same kind which are produced during meditation, which help create a feeling of relaxation and ease.

A meta-analysis on the effects of L-theanine on sleep examined 19 studies featuring 897 participants. It confirmed that the amino acid improves sleep efficiency and quality.

In addition the meta-analysis showed that L-theanine helped reduce daytime dysfunction – in contrast to benzodiazepines which cause problems like fatigue, irritability, memory problems and co-ordination impairment.

L-theanine by Vital Nutrients is the formula favoured by our naturopaths.

Glycine

Like GABA, glycine is an amino acid that functions as an inhibitory neurotransmitter, downregulating arousal to prepare you for better sleep.

While GABA works on the brain, glycine works on the brainstem and spinal cord, dampening sensory perception in the body and controlling movement-based reflexes.

Research shows that when given 3mg of glycine, people experience better sleep quality, reduced fatigue and improved cognitive function during the day.

Our naturopaths use Glycine Powder by Vital Nutrients to support sleep and relaxation.

Valerian

Rather than having an indirect effect on GABA, like the previously named natural remedies, valerian has a direct effect on GABA, increasing its production. This makes you feel sleepy, helping relax muscles and the mind.

Valerian is proven to reduce the amount of time it takes for you to fall asleep, improving sleep quality, increasing stage 3 and REM sleep which is essential for healing, cognitive function and emotional health.

Valerian is a non-addictive natural substance that will cause drowsiness. It’s best taken 30 minutes to an hour before bed. Long-term use has not been studied, so it’s recommended to limit your use to 6 weeks, before taking a break.

Tension Ease by Vital Nutrients is a herbal blend designed to help you get into a sleepy headspace before bed. It contains ashwagandha, valerian, L-theanine, passionflower, lemon balm and poppy extract.

Passionflower

Passionflower has high levels of GABA, leading to increased levels in the brain. Like valerian, passionflower is sedating, so is best taken just before you go to sleep.

Studies show that passionflower helps increase sleep duration and time spent in therapeutic slow wave sleep. It also helps reduce sleep disturbances.

To benefit from passionflower’s lulling properties, turn to Tension Ease by Vital Nutrients.

In summary

There are many natural alternatives for sleeping medications that come without the negative side-effects, like addiction and withdrawal.

Magnesium, ashwagandha, saffron, L-theanine, glycine, valerian and passionflower affect glutamate and GABA, helping induce sleepiness. They calm excited neurotransmitters in the brain, oh so keen to remind you of that email you forgot to send to Karen, or the bill that has gone unpaid.

Our world is full of demands on our attention – so sometimes, we need a little extra help quieting the mind so that we can have the restful sleep we need to face tomorrow’s challenges.

Sleep problems can be much more complex than the GABA-glutamate pathway. External pressures can increase time spent in fight or flight, making it hard to shift into a more relaxed state. Alongside these natural remedies, lifestyle changes like taking the time before bed to calm your mind and body can make a big difference. 

Our naturopaths undertake a careful exploration of your symptoms, referring you for testing to understand the complete landscape of your sleeping problems. Once they’ve identified the origin of your sleepless nights, they develop a personalised treatment plan, incorporating lifestyle changes to restore your rest. 

Traditional Chinese Medicine offers a different route for resolving sleeping problems, analysing your constitution and using Chinese Herbs and acupuncture to protect your sleep.

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