By: Jill Weinstein, RPh, Ashley Addie, PharmD Candidate and Christopher Jackson, PharmD Candidate
Millions of Americans are affected every day by sleep disorders that range from acute transient sleep disturbances to long term chronic insomnia. Long-term consequences of sleep disorders include high blood pressure, increase risk of heart attack or stroke, emotional changes or weight gain. While there are many potential causes for sleep disorders, the main focus of treatment in long term chronic insomnia is to identify and correct the underlying cause. For acute transient sleep disturbances, many pharmacological treatment options including prescription and over the counter products are currently being marketed with FDA approval. However, for centuries people have successfully used herbal remedies and supplements despite minimal scientific evidence supporting their use. Recently, scientific studies have targeted melatonin, valerian root, kava, and 5-hydroxytryptophan (5-HTP) with relation to sleep disorders. This article focuses on evaluating these four herbal remedies and their potential use in acute sleep disturbances.
The U.S. Department of Health & Human Services reviewed the use of melatonin in sleep disorders and concluded that melatonin may have a modest benefit in people with delayed sleep phase syndrome4,11. Melatonin has FDA orphan drug status for treating sleep disorders in blind patients8. Dosing varies depending on use. Dosing for delayed sleep phase syndrome is 3 mg 1-2 hours before bedtime3. Blind patients with delayed sleep phase syndrome are instructed to take 5-10 mg at bedtime10. Dosing for the prevention of jet lag ranges from 3-6 mg 2200-2400 local time to help entrain the circadian rhythm. Caution should be used when taking melatonin with fluvoxamine, MAOI, and TCA, as these may increase concentrations of melatonin; benzodiazepines (BZDPs) and valproate have been shown to decrease nighttime concentrations. Melatonin has been shown to decrease the effects of nifedipine.
For centuries, people have used valerian root to treat anxiety and insomnia. Although not as many studies have been done evaluating the effectiveness of valerian root for sedation as compared to melatonin, some studies show that it may have some effective sedative properties2,7 . It is believed that the sedative and anxiolytic properties of this root come from its affinity for GABAA receptors in the brain, similar to that of benzodiazepines. Valerian root is generally well tolerated and has very few reported side effects. Although studies do not agree on a standard dose, doses ranging between 225 and 1215 mg per day have been studied1. One of the benefits of using valerian root compared to other herbals like melatonin is the lack of hangover effect, or sleepiness, the next morning2. Caution should be used when taking valerian root in conjunction with CNS depressants such as alcohol, opiates, barbiturates, and BZDPs due to an increased risk of CNS depression.
Kava (Piper methysticum) has also been used to help with sleeplessness and promote relaxation in patients suffering from Generalized Anxiety Disorder (GAD). While there is some evidence to support the use of kava in mild insomnia when taken 30-60 minutes before bedtime, patients should be cautious using this herb9,10. Kava has been linked to hepatotoxicity and may increase symptoms of Parkinson’s disease, interfere with INR, and potentiate the effects of other herbs including valerian13,14. Kava should not be recommended in patients with history of liver disease or taking medications that may increase risk of hepatotoxicity.
As a precursor to melatonin, 5-HTP is believed to help with sleep disorders6. Since 5-HTP is an immediate precursor for serotonin, it is also believed to help treat depression and regulate mood swings. After tryptophan was removed from the market in 1989 for serious risk of eosinophilia myalgia syndrome (EMS), 5-HTP was marketed as the safer alternative. There have been 10 cases reported worldwide associating 5-HTP with EMS; however, despite decades of use, none of these cases definitively link 5-HTP with EMS15. If used, doses should not exceed more than 150-300 mg/day. Other adverse effects include nausea, vomiting, diarrhea, and flatulence. Caution should be used in patients taking SSRIs, 5-HT1-agonists, and tramadol due to an increased risk of serotonin syndrome.
Given the research available, melatonin and valerian root are two possible options for patients wishing to treat acute sleep disturbances. Valerian root shows an additional benefit over melatonin as it does not result in a hangover effect, or sleepiness, the next morning. While there is some evidence to support the use of Kava and 5-HTP, due to the increased risk of hepatotoxicity and EMS, more studies are needed before these herbals can be recommended for use in sleep disorders. Based on historical use and limited scientific evidence, herbal medications can be used as an alternative to pharmacological medications in the treatment of sleep disorders. However, consideration must be given to potential side effects and adverse drug interactions.
Cortisol is secreted by the adrenal gland and influenced by circadian rhythm1. Since sleep inhibits the secretion of cortisol, studies show that patients suffering from insomnia may have elevated levels of cortisol16. Symptoms associated with high cortisol levels include weight gain, weakened immune system, acne and behavioral changes such as depression, anxiety, or mood swings. High cortisol levels in women can lead to irregularities in menstrual cycle, increase facial or body hair and infertility. In men, high cortisol levels may decrease libido. Cortisol levels can be checked with simple saliva test. Pharmacy Specialists provides cortisol testing and consultation for sleep disorders. Contact Pharmacy Specialists at 407-290-7002 and speak with a pharmacist today.
Ashley Addie, PharmD Candidate and Christopher Jackson, PharmD Candidate University of Florida are currently on rotation at Pharmacy Specialists. Jill Weinstein, RPh, graduated from University of Florida and is the clinical pharmacist who does hormone, nutrition and weight loss consultations at Pharmacy Specialists. Pharmacy Specialists is proud to be the only pharmacy in all of Central Florida and one of only 129 pharmacies in the country that are accredited by the Pharmacy Compounding Accreditation Board standards for sterile as well as non- sterile compounding and we are the only USP 797 and USP 795 vali- dated compliant pharmacy in all of central Florida. Currently, Sam Pratt, RPh at Pharmacy Specialists is the only Full Fellow of the Inter- national Academy of Compounding Pharmacists in the Central Florida area. Call Pharmacy Specialists to check with a clinical pharmacist for suggestions and recommendations. For additional information please call (407)260-7002, FAX (407) 260-7044, Phone (800) 224-7711, FAX (800) 224-0665.
