Beta-Blockers Cause Insomnia

Q: My doctor prescribed atenolol (Tenormin®) to treat my high blood pressure. Ever since I started taking it, I constantly feel fatigued and lethargic, yet at night I don’t get any restful sleep. Why is this and what can I do?

A: Atenolol is a beta-blocker commonly prescribed for patients with cardiovascular disease and hypertension (high blood pressure). Beta-blockers, also known as beta-adrenergic blocking agents, reduce the effects of catecholamines (norepinephrine and epinephrine, the fight-or-flight hormones). This in turn slows the heart rate, relaxes blood vessels, and improves conduction signals in the heart, thereby lowering blood pressure.^1,2

Unfortunately, these changes, including the slowed heart rate, can lead to adverse side effects since beta-receptors affect multiple metabolic and physiologic functions.^3,4 Common side effects associated with the use of this medication include symptoms of fatigue as well as sleep disturbances including insomnia.^5-7

Beta-Blocker Side Effect: Fatigue Symptoms due to CoQ10 Deficiency

Beta-blockers have been shown to block the biological pathway of coenzyme Q10-dependent enzymes in the body.⁸ This interferes with energy production and protection against free radicals, contributing to fatigue.^8,9 This drug-induced depletion may be particularly serious in the elderly, who already suffer from a natural age-related CoQ10 deficiency. CoQ10 is a mitochondrial enzyme essential for the production of adenosine triphosphate (ATP), the core of cellular energy processes.^10-13 A 2009 clinical study showed a close correlation between lowered levels of CoQ10 and its role in the pathophysiology of chronic fatigue as a direct result of mitochondrial dysfunction.¹⁴

Levels of CoQ10 naturally decline with age. While adults over the age of 30 can benefit from taking CoQ10 supplements, they are especially important for people with cardiovascular concerns, and those who take certain blood pressure medications like beta-blockers.^15-18 Ubiquinol (the active form of CoQ10) has a much greater bioavailability than ubiquinone (the oxidized form), helping to improve metabolic efficiency of the cardiovascular system to maintain heart health.¹⁹ Based on a meta-analysis of published scientific research, therapeutic doses of ubiquinol range between 100 to 200 mg daily, but may be increased if conditions warrant.⁹

Beta-Blockers Side Effect: Insomnia due to Reduced Melatonin Levels

Beta blockers have long been associated with sleep disturbances such as difficulty falling asleep, staying asleep, and insomnia. They have been shown to reduce the production of melatonin via specific inhibition of beta-1 adrenergic receptors. Melatonin is a hormone secreted by the pineal gland in the brain, and helps in maintaining normal circadian rhythms.^6,20-21 People with hypertension already have a lower melatonin production rate than those with normal blood pressure.²²

Depression, Cancer and Obesity: Why Insomnia Is Concerning

According to the Centers for Disease Control and Prevention, insufficient sleep is a public health epidemic. Persons experiencing sleep insufficiency are also more likely to suffer from chronic diseases such as hypertension, high blood sugar and diabetes, depression, obesity, and cancer. People with insomnia are also at risk of increased mortality and reduced quality of life and productivity.²³

Melatonin and Circadian Rhythms

Clinical data indicates melatonin not only plays a significant role in regulating our sleep-wake cycle or circadian rhythms, it also plays a part in protecting against cardiovascular disease, neurological disease, and other diseases related to aging.²⁴ Melatonin’s universal action on oxidative stress through its scavenging and antioxidant effects plays a role in several metabolic functions influencing virtually every living cell. Scientific evidence from the last 15 years has suggested that melatonin has positive effects on the cardiovascular system. Melatonin administration typically involves dosages ranging from 500 mcg to 5 mg nightly to promote sleep.^25-27

Beta-blocking medications deplete nutrients that are essential to the metabolic activities of every cell in the body. The bottom line here is that we need to be aware of medications that could potentially create an imbalance in your nutritional status and correct them.

Note: Altering your dose or discontinuing any of your prescription medications should always be done under the care and supervision of your physician. If you experience chest pain, seek immediate medical attention.

Kimmi Stultz is a member of the American Pharmacists Association Foundation, American Academy of Anti-Aging Medicine, and a clinical pharmacy educator for the Life Extension Foundation®.

If you have any questions on the scientific content of this article, please call a Life Extension® Wellness Specialist at 1-866-864-3027.

References

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19. Frei B, Kim MC, Ames BN. Ubiquinol-10 is an effective lipid-soluble antioxidant at physiological concentrations. Proc Natl Acad Sci USA. 1990 Jun;87(12): 4879-83.
20. Fares A. Night-time exogenous melatonin administration may be a beneficial treatment for sleeping disorders in beta blockers patients. J Cardiovasc Dis Res. 2011 Jul;2(3):153-5.
21. Stoschitzky K, Sakotnik A, Lercher P, et al. Influence of beta-blockers on melatonin release. Eur J Clin Pharmacol. 1999 Apr;55(2):111-5.
22. Zeman M, Dulkova K, Bada V, Herichova I. Plasma melatonin concentrations in hypertensive patients with the dipping and non-dipping blood pressure profile. Life Sci. 2005;76:1795-803.
23. Available at: https://www.cdc.gov/sleep/about_sleep/chronic_disease.html. Accessed May 12, 2022.
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Newly Added References

28. Neel, AB. 10 Types of Meds That Can Cause Insomnia. Available at: https://www.aarp.org/health/drugs-supplements/info-04-2013/medications-that-can-cause-insomnia.html. Accessed May 3, 2022.
29. Chang C, Yang Y et al. Risk of insomnia attributable to β-blockers in elderly patients with newly diagnosed hypertension. Drug Metab Pharmacokinet. 2013;28(1):53-8. Available at: https://pubmed.ncbi.nlm.nih.gov/22813717/. Published July 17, 2012. Accessed May 3, 2022.
30. Beta-blockers not likely to cause depression yet may contribute to sleep disturbances. Available at: https://newsroom.heart.org/news/beta-blockers-not-likely-to-cause-depression-yet-may-contribute-to-sleep-disturbances. Published March 15, 2021. Accessed May 3, 2022.