Blog | Stages of Life

Over the Counter Sleep Aids: What You Need to Know to relieve Insomnia. Four products for a natural approach.

David S Klein, MD

Dec 16, 20243 min read

Insomnia affects about 30% of all adults — Sleep Deprivation or Insomnia is a common complaint

Insomnia is a symptoms, not a disease

Insomnia is a common sleep complaint. Insomnia, can be divided into 3 main types: early insomnia (difficulty falling asleep) mid-insomnia (difficulty staying asleep) and late insomnia (difficulty with early morning awakening.)

You may have trouble falling asleep, staying asleep, or getting good quality sleep, or some combination of all three. This happens even if you have the time and the right environment to sleep well. Insomnia can get in the way of your daily activities and may make you feel sleepy during the day.

Diseases that can cause sleep disorders

Obstructive sleep apnea
Heart conditions – such as angina or heart failure.
Neurological conditions – such as Alzheimer's disease or Parkinson's disease.
Kidney disease
Diabetes
Chronic pain
Opiate induced insomnia
Adrenal Failure
Post traumatic stress disorder, depression

We will discuss the disease states individually, at a later date, as each one is worthy of focus. For purposes here, we will assume that we are dealing with mild, situational insomnia, not due to major medical illness.

Theanine (l-theanine) is an amino acid found in tea leaves. In addition to providing benefits as an anti-oxidant, theanine is useful in sleep induction, as well.

L-Theanine provides an interesting combination of salutary benefits. It acts as a non-sedating relaxant by enhancing alpha wave production in the brain. It improves mental focus during wakeful hours, yet it enhances sleep quality. The alpha-wave enhancing effect is very useful for students, promoting concentration, yet it does not cause sleep disturbances that result from the use of caffeine and amphetamines. The effective dosage range of L-Theanine ranges between 50 and 200 mg, or more, per day.

While 3 or 4 cups of tea would be expected to contain 100-200mg of l-theanine, this same volume of tea contains a great deal of caffeine. The caffeine itself will improve concentration, but headache can occur as the caffeine wears off, and sleep disorders are common with caffeine ingestion. Decaffeinated tea would be a good choice, but the decaffeinating process destroys the L-theanine.

After ingestion of capsular or tablet forms of l-theanine, blood levels will reach maximum peak blood levels in about 30 mins, and peak in 2-4 hours. For maximal effect, it is best taken in the morning to enhance concentration, and immediately before bed to enhance sleep.

I have my patients use one of our Green Tea Extract Capsules at bed time, combined with a melatonin 10 mg capsule. This is a very gentle approach to sleep induction.

In patients with anxiety and/or depression, the addition of 5-HTP can be added. Dosage is discussed, below.

Sleep Disorder is remarkably common. For a general idea as to how prevalent this problem might be, simply watch television and count the number of commercials that pop up for prescription sleep medications.

The Problems:

Sleep Dysfunction or insomnia is a symptom, not a primary disease state.
Without sorting through WHY a person has difficulty sleeping, it is impossible to correct the underlying problem.
Taking a medication that is ‘new to nature’ rarely corrects any underlying problem. That is, a medication that is formulated from chemicals that are not native to the organism (human, in this case) cannot by nature correct an imbalance. Only restoration of the missing piece, chemical or nutrient will restore proper balance.
It is unclear, in most cases, which chemical is out of balance or inadequate.

My approach to correcting sleep problems begins with teaching correct sleep habits, but it includes interventions such as L-Theanine, Melatonin, and colostrum. I will use 5-HTP, as well, if the clinical situation is appropriate.

We will discuss 'Sleep Hygiene' in another blog, or two........ Comprehensive topic, to be certain.

Damage to the Inner Lining of the Blood Vessels May Lead to Heart Attack and Stroke: The GLYCOCALYX. Treat inflammation to reduce your risk!

bkreinbrink

Dec 16, 20243 min read

Stages of Life Vitamins — Stages of Life Functional Medicine

The Glycocalyx: The inner lining of the blood vessel as well as the inner lining of the GUT

glycocalyx Mend — The glycocalyx is the innermost and most delicate part of the arteries

The following discussion is a bit technical, but it is extremely important. Even if you do not entirely understand microbiology.

The endothelial glycocalyx is a vital structure found on the luminal surface of endothelial cells lining blood vessels throughout the body. Composed of a complex meshwork of glycoproteins, proteoglycans, glycosaminoglycans (GAGs), and associated plasma proteins, the glycocalyx forms a gel-like layer that coats the endothelial surface. This structure plays a crucial role in regulating vascular permeability, blood flow dynamics, and interactions between blood components and the vessel wall.

Protecting the lining of the arteries, blood vessels and gut inner wall

One of the primary functions of the endothelial glycocalyx is to act as a selective barrier between the circulating blood and the endothelial cells. Its dense and negatively charged composition repels negatively charged molecules such as proteins and blood cells, while allowing smaller molecules like water and ions to pass through.

This selective permeability helps maintain the proper balance of fluid and solutes within the blood vessel lumen. Moreover, the endothelial glycocalyx serves as a dynamic sensor of mechanical forces exerted on the blood vessel wall. Shear stress, generated by blood flow, can influence the structure and function of the glycocalyx. In response to changes in shear stress, the glycocalyx may undergo alterations in thickness and composition, thereby modulating vascular tone and blood flow distribution.

Additionally, the glycocalyx plays a crucial role in mediating interactions between circulating cells, such as leukocytes and platelets, and the endothelium. Specific molecules within the glycocalyx, such as selectins and adhesion receptors, facilitate the tethering, rolling, and firm adhesion of these cells to the endothelial surface during processes like inflammation and hemostasis.

Furthermore, the endothelial glycocalyx is involved in regulating vascular homeostasis by modulating the release of vasoactive substances such as nitric oxide (NO) and endothelin-1. NO, produced by endothelial cells, promotes vasodilation and inhibits platelet aggregation, while endothelin-1 acts as a potent vasoconstrictor.

The glycocalyx helps maintain the balance between these opposing vasomotor factors, thereby influencing vascular tone and blood pressure regulation.

Moreover, the glycocalyx functions as a reservoir for various bioactive molecules, including growth factors, cytokines, and enzymes. These molecules are sequestered within the glycocalyx, where they can be released in response to physiological stimuli, such as inflammation or tissue injury, to modulate cellular responses and tissue repair processes.

Diseases of the Glycocalyx

The endothelial glycocalyx has been implicated in the pathophysiology of various cardiovascular diseases, including atherosclerosis, hypertension, and diabetes. Damage to the glycocalyx, caused by factors such as oxidative stress, inflammation, and hyperglycemia, can lead to increased vascular permeability, endothelial dysfunction, and accelerated atherogenesis.

Additionally, loss or impairment of the glycocalyx has been associated with adverse outcomes in critically ill patients, such as increased capillary leakage, tissue edema, and organ dysfunction.

Strategies aimed at preserving or restoring glycocalyx integrity, such as administration of exogenous glycocalyx components or modulation of glycocalyx-degrading enzymes, hold promise for improving vascular function and clinical outcomes in various disease settings.

Glycocalyx Mend

Treatment for vasculitis, kidney failure, stroke — Glycocalyx Mend: 3 capsules every morning

We have treated patients with stroke, angina, chronic kidney failure using 3 capsules every morning. Laboratory data including C-RP, eGFR have demonstrated measurable improvement in 3 to 4 weeks. A positive response response is followed by continued, chronic administration.

Conclusion

The endothelial glycocalyx is a dynamic and multifunctional structure that plays a critical role in vascular physiology and pathophysiology. Its selective barrier function, mechano-sensory properties, role in cell adhesion and signaling, and involvement in vascular homeostasis make it a key determinant of vascular health and function. Further research into the structure, function, and regulation of the glycocalyx may uncover new therapeutic strategies for treating cardiovascular diseases and other vascular disorders.

Functional Medicine Doctor Orlando Florida — Practicing Functional Medicine for 42 years

David S. Klein, MD, FACA, FACPM

1917 Boothe Circle

Longwood, Florida 32750

Tel: 407-679-3337

Fax: 407-678-7246

The Health Benefits of Huperzine: An Evidence-Based Overview

David S. Klein, MD FACA FACPM

Dec 12, 20244 min read

Many benefits from this naturally occurring substance, Huperzine A

The Health Benefits of Huperzine: An Evidence-Based Overview

Huperzine A, a compound extracted from the Chinese club moss Huperzia serrata, has garnered attention for its potential neuroprotective and cognitive-enhancing properties. Research highlights its effects in promoting mental clarity, improving memory, and combating neurological disorders. Below, we explore its health benefits through evidence-backed findings.

How does Huperzine A work?

Well, through effect on the PDE neuro-receptors through a chemical called 'Nitric Oxide.'

The Huperzine stimulates the receptor causing the blood vessels to open up, increasing blood flow.

1. Memory Enhancement

Huperzine A is widely known for its ability to enhance memory. Studies suggest that it inhibits acetylcholinesterase, an enzyme responsible for breaking down acetylcholine, a neurotransmitter involved in memory and learning. Increased acetylcholine levels are associated with improved cognitive functions, especially in individuals with memory impairments (Wang et al., 2006).

2. Neuroprotective Properties

Huperzine A offers neuroprotection by reducing oxidative stress and inflammation in the brain. Research indicates that it may help shield neurons from damage caused by amyloid-beta plaques, a hallmark of Alzheimer's disease (Zhao et al., 2004). This protective effect may extend to individuals without neurological disorders, supporting general brain health.

3. Potential Role in Alzheimer’s Disease

Clinical trials have shown that Huperzine A can improve cognitive function and quality of life in patients with Alzheimer’s disease. A meta-analysis of randomized controlled trials reported that the compound significantly improved cognitive scores compared to placebo treatments (Yang et al., 2013).

4. Cognitive Enhancement in Healthy Individuals

Beyond its therapeutic applications, Huperzine A has been explored as a nootropic for healthy individuals. A study by Sun et al. (1999) found that students who took Huperzine A experienced better memory retention and academic performance, suggesting potential benefits for learning and memory consolidation.

5. Support for Age-Related Cognitive Decline

Huperzine A may be beneficial for age-related cognitive decline, even in the absence of diagnosable neurodegenerative diseases. Its ability to modulate acetylcholine levels helps maintain cognitive functions in older adults (Xu et al., 1995).

6. Treatment of Myasthenia Gravis

Myasthenia gravis, an autoimmune neuromuscular disorder, is characterized by muscle weakness due to impaired communication between nerves and muscles. Huperzine A has been investigated for its potential to improve muscle function by enhancing acetylcholine signaling (He et al., 1990).

7. Antioxidant Properties

The compound's antioxidant properties may contribute to its neuroprotective effects. Huperzine A has been shown to reduce oxidative damage in brain cells, which is linked to aging and neurodegenerative diseases (Liu et al., 2007).

8. Mental Fatigue Reduction

Some evidence suggests that Huperzine A can alleviate mental fatigue. This benefit is attributed to its ability to optimize neurotransmitter function, which may enhance mental clarity and sustained focus (Zhang et al., 1999).

9. Safety and Tolerability

Huperzine A is generally well-tolerated, with mild side effects such as nausea and dizziness reported in some studies. Its safety profile, combined with its potential cognitive benefits, makes it an attractive option for both clinical and non-clinical use (Liang et al., 2008).

10. Future Directions in Research

Emerging research continues to explore Huperzine A's potential applications beyond cognitive health. Preliminary findings suggest that it may have therapeutic roles in other conditions involving neurotransmitter dysregulation, including schizophrenia and depression (Li et al., 2020).

Notes from Doctor Klein:

How do I take Huperzine A? This is a remarkable product, the goal is to improve blood flow in the microvasculature. The net effect is most profound in the kidney, eyes, ears, brain, heart and the small blood vessels of the extremities, to include the male genitalia. It was first a prescription product used to treat microvascular dementia.

Note well: I have found that it can benefit patient with mild to moderately decreased kidney function, and it is my second line therapy for patients with CKD IIIa, early renal failure.

I like to start slowly, recommending 1 tablet taken twice daily, increase to 3 per day, and then 4 per day in divided dosages. Advance until you get a headache, then back off 1/2 tablet, wait another week and try pushing ahead. Some individuals benefit by using a pill cutter, and starting with 1/2 tablets.

It increases the blood flow to the brain, and this may be the reason behind the headache. It does not increase blood pressure, but the increase in blood flow can be disturbing, at first.

As it is with everything, individual needs and tolerances will dictate the dosage, and this can be apparent over the course of a month, or so.

Huperzine A for memory issues, erectile dysfunction, and more....

References

Wang, B. S., Wang, H., Wei, Z. H., Song, Y. Y., & Zhang, L. (2006). Effects of Huperzine A on memory deficits and brain oxidative stress in senescent mice. Brain Research, 1123(1), 187–195.
Zhao, Q., Zhou, D. M., & Li, L. (2004). Neuroprotective effects of Huperzine A against oxidative injury in rat pheochromocytoma PC12 cells. Acta Pharmacologica Sinica, 25(3), 341-345.
Yang, G., Wang, Y., Sun, J., & Zhang, K. (2013). Huperzine A for Alzheimer’s disease: A systematic review and meta-analysis of randomized clinical trials. PLoS ONE, 8(9), e74916.
Sun, X. M., & Tang, X. C. (1999). Effects of Huperzine A on memory deficits in aged rats and young students. Acta Pharmacologica Sinica, 20(7), 601-605.
Xu, S. S., Gao, Z. X., Weng, Z., & Du, Z. Y. (1995). Efficacy of Huperzine A on age-related memory decline. Chinese Journal of Clinical Pharmacology and Therapeutics, 1(4), 21-23.
He, Y., Zhu, M. Y., & Zhang, Y. (1990). Huperzine A as a treatment for myasthenia gravis: A double-blind trial. Chinese Medical Journal, 103(7), 486-491.
Liu, J. S., Wang, C. Y., & Xu, P. Y. (2007). Antioxidant effects of Huperzine A on aging brain. Experimental Gerontology, 42(8), 787-794.
Zhang, R. W., Li, Z., & Wang, Z. (1999). The effects of Huperzine A on cognitive and mental fatigue in healthy volunteers. Acta Pharmacologica Sinica, 20(9), 847-851.
Liang, J., Yuan, Q., & Liu, H. (2008). Safety and tolerability of Huperzine A in humans. Journal of Clinical Pharmacy and Therapeutics, 33(5), 623-627.
Li, Q., Wang, H., & Wei, Z. (2020). Investigating the therapeutic potential of Huperzine A in neuropsychiatric disorders. Frontiers in Pharmacology, 11, 345.