Prescription Sleeping Pills and Natural Remedies for Rest

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Prescription Sleeping Pills and Natural Remedies for Rest

“Dear Pharmacist,

What are the best medications to help me sleep? I’ve tried all the natural remedies, I need something stronger!”
 –V.E., Sacramento, California

Answer: Why, as a nation, do we have trouble sleeping? It should be such a natural act. I urge you to find the underlying cause of your chronic insomnia and to change your sleep habits because you can’t rely on medication forever.

Chronic insomnia may be caused by sleep apnea, and sleeping pills in this case, are dangerous. For some of you, a deficiency of your sleep hormone, melatonin, causes you to wake up very early. The point is that sleep disorders aren’t always related to neurotransmitter imbalances, so sleeping pills are not a ‘wet blanket’ like everyone thinks. You can take them for awhile, but they just mask the underlying problem. Here are the most popular medications:

Ambien (zolpidem)- Introduced in 1992, this helps put you to sleep, and keep you asleep. Many people reported having morning grogginess, so the makers came out with a controlled-release version in 2005 that works longer. Ambien usually puts you to sleep within 15 to 30 minutes. There are other brand names containing the same chemical ingredients such as a sublingual low-dose tablet called “Intermezzo” that you can take in the middle of the night. There’s “Zolpimist,” an oral spray. Every now and then you hear a report of someone sleep-driving, having sex, making phone calls, sleep-walking and cooking meals.

Lunesta (eszopiclone)- Everything I said about Ambien applies to this drug; it is similar in mechanism of action, as well of duration of action.

Sonata (Zaleplon)- Again, this is similar to Ambien. However, it has a very short duration of action. The advantage is you won’t have morning grogginess, however, the disadvantage is you may be staring at the alarm clock by 3 a.m.

Rozerem (Ramelteon)- This is my favorite sleep medication because it affects your melatonin receptors, increasing the length of time you sleep. You can start and stop as often as you wish, since there is no physical dependence. The drug may affect prolactin and testosterone levels, so if you use it long-term (greater than 3 or 4 months), have these levels evaluated.

Silenor (Doxepine)- Introduced in 2010, this medication blocks histamine receptors. It contains the same active ingredient as a popular antidepressant, but in a much lower dose. I like that it does not have addictive potential.

Benzodiazepine drugs (temazepam, alprazolam, clonazepam, lorazepam and others)- Very affordable, and used for decades, these drugs have strong addictive potential and may cause daytime drowsiness. This category helps with some seizures.

Insurance companies may have restrictions on which sleeping pills are covered, and will obviously expect you to buy generic; they often require you to try other approaches to your insomnia first.

Some of you are interested in natural herbs or vitamins to help you sleep, so I’m going to talk about that now. Keep in mind that there are many causes for poor sleep, among them low melatonin, low GABA, high glutamate, high quinolinic acid and pain that is unrelieved in your body. I can’t cover everything here, it would require a book, so I’ll cover the most important and common supplements that could address some of these problems.

5-HTP: This is a dietary supplement that can often cause drowsiness within an hour or two. But evening dosing isn’t right for everyone because 5-HTP creates energy before it causes drowsiness. Think of a roller coaster –you have to go uphill before you coast downward.

My advice is to try taking 5-HTP around dinnertime and if it stimulates you during the sleep hours (ie you get up to mow the lawn, do dishes and pay bills) then come over to my house. Just kidding. Seriously, if this happens to you, then here’s what you should do: Take 5-HTP at tea time (or even earlier, like at lunch) and this should allow you to enjoy the temporary lift in energy before the lull to la la land.

Why does it do that? Because 5-HTP undergoes a chemical reaction in the body to form serotonin, a ‘happy’ brain chemical, and serotonin is stimulating. Think of those popular anti-depressants like Prozac, Zoloft and Paxil that increase serotonin levels. Eventually, the serotonin breaks down to another chemical called melatonin, a powerful sleep hormone that your brain normally produces when night falls. The melatonin is what makes you fall asleep. You can also take melatonin all by itself, as this natural hormone declines after the age of 40.

Can 5-HTP replace Ambien, Lunesta or Sonata? No, and sometimes, with very low doses, the supplement can be taken with the drugs but not everyone can do that. Ask your doctor what is right for you. Ambien, Lunesta and Sonata increase GABA, they don’t affect melatonin.

GABA- Some of you want to substitute a supplement for the sleeping drugs. You can buy GABA at any health food store and online. GABA quiets down the excitotoxin glutamate which is probably keeping many of you awake and overstimulated. GABA and glutamate are on a see-saw. At low dosages, GABA may relieve anxiety, panic attacks and irritability.  In larger doses, GABA induces sleep. Remember, the prescription drugs are pushing GABA too, so don’t combine. Many say GABA doesn’t get into the brain, and that may be true for some people, but others have poor permeability in their blood brain barrier, in which case GABA gets into your brain. You’ll know if it gets in because when you take it, you get calm and sleepy, depending on the dose. I like GABA because it can improve memory and protect the brain.

Melatonin- For many night-time thrashers, it’s a question of how much melatonin you secrete from your pineal gland. Melatonin production can be augmented if you supplement, because the pills (or sublingual sprays) get absorbed into your bloodstream and trigger the same sleep reaction as if you had made the hormone yourself. Fluoride can harm your pineal gland, which is supposed to make melatonin. For some, melatonin supplements are highly effective. For others, it must be combined with glycine, hops, valerian root or kava. I always suggest low dosages, about 0.2 to 0.3 mg per night, but you will find many supplements containing more. Be very careful with yourself, this is a hormone. Too much melatonin and you will suppress cortisol to the point that you feel bad getting up every morning (when cortisol is supposed to be peaking). That said, melatonin has a widespread (wonderful) effect on the immune system and is specifically awesome for people with auto-immune disorders and chronic infections.

Glycine- This also helps people suffering with Huntington’s, certain seizure disorders and memory loss. Like a blanket of calm, it helps you achieve deeper stages of sleep. Unlike most sleeping pills, glycine should not give you a groggy ‘morning hangover’ until noon, nor will it result in dry mouth (very common with diphenhydramine sleep aids).  Usually two to three grams taken an hour before bed time allows sleep to crawl into bed with you. As an interesting aside, research points to glycine’s use as an antibiotic, specifically against H. pylori, an organism associated with ulcers and stomach cancer. Even though glycine is found in meat, you won’t get enough of its sleep-inducing effects unless you supplement. Capsules are available, but powders may be better if you want to titrate your dose.

Green Tea- It contains theanine, an amino acid that is relaxing. Green tea and its other active ingredient EGCG help to quiet down quinolinic acid which is very active in some of you. It’s also a neurotoxin, and contributes to insomnia. It’s especially high in people with Lyme, but also dozens of other disorders which you can look up on your own. I just want you to know that green tea helps to quell this. For some people, it creates a heightened alertness and insomnia, so if you try green tea, please drink it early, like around 5 or 6pm. I don’t advise drinking it much later than that because it may cause you to feel alert, and actually cause insomnia. For others, it puts them to sleep, but that’s more the minority.  I love recommending green tea but like everything, timing and dosage is everything. Also, curcumin reduces quinolinic acid, and helps relieve pain too. Supplements of that are sold everywhere.

Hops- It’s in beer, one of the bittering ingredients called Humulus lupulus, or Hops. Without hops, beer would be sweet. (Hey, maybe I would like it then?!) Anyway, hops helps people fall asleep faster, and is one of the best insomnia remedies I can think of. It’s been used for centuries. While Hops is safe for human consumption, it can be quite harmful for dogs, so keep it away from Fido! The FDA gave hops GRAS status which means it is “generally recognized as safe.” There’s an ingredient in hops called 8-prenylnaringenin or 8-PN which reduces the incidence of hot flashes. Aside from helping with menopausal concerns and insomnia, hops is touted to ease anxiety, earaches and cramps. An ingredient in it works as a COX 2 inhibitor, similar to the drug Celebrex so if you are in pain, and have trouble sleeping, Hops is a natural herb to talk about with your practitioners.

If you take thyroid medicine, do not take it at night; it must be taken in the morning. I’ve heard people experiencing insomnia because they were not told this, so if you take thyroid medicine, it’s best taken upon arising every morning, on an empty stomach. Take it at night and you’ll be wired! 

Finally, I want you to know about a chemical pathway called methylation that happens in your body.  Methylation also plays a role in making and breaking down various neurotransmitters, such as energy producing epinephrine and sleep producing melatonin. If there’s a problem breaking neurotransmitters down, then they will hang around in excess, which may cause unwanted issues such as insomnia. It can also cause other “hyper or irritable and stimulating” types of conditions like seizures, agitation, combativeness, panic attacks and so forth. Please go read my article on methylation to learn what to do. I know you are busy, but this is one article worth the extra 10 minutes in your day. The feedback for this has been tremendous and filled with gratitude. Poor methylation may be the cause of your insomnia and other problems, and no drug can correct that, only vitamins/minerals and foods that support it.

All of the supplements discussed today are sold at health food stores and some pharmacies, but always ask your doctor what’s right for you. If you enjoyed my article, please share it with loved ones and friends.