Recently, I was skimming the coupons from the Sunday papers and found the inspiration for this Healthful Hints column.

I saw an ad from a “big-box” pharmacy for three different brands of over-the-counter “sleep aids.” I am familiar with the brands Tylenol PM and Advil PM, but not the ones advertised in the coupons. So, I went label shopping.

The two mentioned above are combinations of those pain relievers with 25 mg of an antihistamine called diphenhydramine (DPH, die-fen-HI-dra-meen), the longtime brand Benadryl first formulated in 1946, which I have even tried myself, personally experiencing mild morning-after grogginess. Another older first-generation antihistamine in one product was doxylamine.

Melatonin is also a common ingredient. It is a hormone whose production fluctuates with exposure to light or dark conditions that we secrete from our pineal gland. Less often found is a fourth choice, valerian, which has been used for centuries. A chemical used in conjunction with others occasionally is L-theanine (THEE-ah-neen). In the bottles snuggled up on that shelf I found another option, L-tryptophan (nothing to do with feet) only once.

A brief explanation of these might help. By far, DPH is the most frequently used hypnotic or sleep inducer. Originally synthesized in Cincinnati by Fred Huber in 1943 in the lab of professor George Rieveschl (who gets credit for the discovery), it binds to cell surface receptors for both histamine (antihistamine) and acetylcholine, a chemical transferring signals from one nerve to another in parts of both central and peripheral nerve systems. The latter seems to yield the hypnotic effect. The resulting drowsiness can hang on a bit for some of us. On rare occasion, it can produce a paradoxical (not two doctors) effect of excitation and anxiety.

Doxylamine is another first-generation antihistamine synthesized in 1949. It has a similar biological profile to DPH, but has a half-life 10-12 hours instead of 4-9 like DPH. One reference called it “stronger” because of that. Not really.

Valerian is a powder from the roots of the plant. It was written about by Hippocrates, the Greek doctor, and prescribed for insomnia by Galen, the famous Roman physician. The name is derived from the Latin verb valere, to be healthy, strong. While it is advocated as an “all natural” remedy, the studies done with it on an objective basis haven’t demonstrated a significant effect for insomnia or anxiety disorders. For what it’s worth, it also attracts cats like catnip.

Theanine (THE-ah-neen), chemically known as L-theanine, was found in green tea leaves in 1949. It is related to glutamate and glutamine, neurotransmitter chemicals. It has been marketed as a nutritional supplement, especially in Japan, to reduce stress, produce feelings of relaxation and improve mood.

Let’s not forget L-tryptophan, first isolated in 1901, which has enjoyed a reputation for being the chemical that makes for sleepy folks after a big meal such as the stereotypical Thanksgiving turkey feast. Supplements are sold to promote sleep. Our body does metabolize it into serotonin, which can help control mood and sleep. It also is made into melatonin.

Melatonin is secreted by your pineal gland, a pea-sized hormone producer between your two brain halves, and shaped like a pinecone, giving it its name.

The pineal is activated by lack of light reaching brain during the sleep-wake cycle. As its blood level increases, you feel less alert (like going to bed earlier when days are shorter?). The theory behind taking it is to create that feeling to allow easier snorking off.

When shopping for any these, you must read for ingredients, not brand names. One brand had different drugs in different boxes with the same name. Combining stuff can make sense, such as pain relievers and antihistamines. Sometimes it’s sort of curious. One brand had melatonin, l-tryptophan, and valerian with other ground-up weeds. One brand had melatonin with soy germ and pumpkin for alleged bladder control.

You need to ask your doc if any drug interactions might take place if you’re chucking down other pills. You have to be honest when trying to decide how beneficial any one is for you.

My personal vote for the best OTC sleep aid is a boring class or lecture.

My favorite personal example is from medical school in lectures by an excellent surgeon who nevertheless droned on so much in class that he became famous for putting students to sleep.

I returned some 30 years later to a meeting where he lectured. I was out in about 10 minutes like the old days. I often thought if I could have recorded some of those talks to sell for curing insomnia, I could have made big bucks.


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