Horse Chestnut

Chloe Sullivan, BSPS Student Spring 2023

What is horse chestnut?

Definition & history: A tree native to the Balkan Peninsula that was brought to the United Kingdom during the 16th century and has been used medicinally for its anti inflammatory properties for centuries. The reason it’s called horse chestnut is most likely because it used to be fed to horses with respiratory problems.

Other names: aesculus hippocastanum, buckeye, conker tree, European chestnut

Uses

Dosing: capsules

Take 300-600mg daily for 8-12 weeks

Adverse effects

• Dizziness

• Upset GI

• Headache

• Itching

Today, horse chestnut is primarily used to treat CVI (chronic vein insufficiency) by improving circulation and reducing the related symptoms including:

• Varicose veins

• Pain

• Tiredness

• Swelling of legs

• Itching

• Water retention

Other uses: treatment of IBS, treatment of male infertility, general anti-inflammatory treatment

Dudek - Makuch M, Studzi ń ska - Sroka E. Horse chestnut – efficacy and safety in chronic venous insufficiency: An overview. Revista Brasileira de Farmacognosia 2015;25(5):533 - 541. doi:10.1016/j.bjp.2015.05.009

Horse chestnut. National Center for Complementary and Integrative Health. https://www.nccih.nih.gov/health/horse - chestnut.

Horse chestnut. Uses, Interactions, Mechanism of Action | DrugBank Online. https:// go.drugbank.com /drugs/DB13195. Woodland Trust. Horse Chestnut (aesculus hippocastanum). Woodland Trust. https://www.woodlandtrust.org.uk/trees - woods- and - wildli fe/british - trees/a - zof- british - trees/horse- chestnut/.

Mechanism of action

The active component to horse chestnut is called aescin, which has several different effects in the body:

• Anti-inflammatory activity: inhibition of phospholipase A2, an enzyme that has a role inflammatory mediator synthesis

• Anti-oedematous activity: inhibition of adhesion and aggregation of neutrophils, which increase vascular permeability and increase tissue fluid retention

• Vascular tension: increased production of prostaglandin F2, which stimulates vasoconstriction and inhibits vascular tissue catabolism, improving blood flow

Note: There is little research currently available regarding the precise mechanisms of aescin in horse chestnut. This list summarizes just one article.

Safety & toxicity

Horse chestnut contains esculin, which is poisonous if eaten raw and must be removed before consumption. Horse chestnut should not be taken with anticoagulant/antiplatelet drugs.

Efficacy

Based on the current available research, horse chestnut has been proven to produce beneficial therapeutic effects in the treatment of CVI. Its effects are comparable to those of hydroethylrutoside, pycnogenol, or compression therapy.

Professional opinion

Professional opinion: Overall, there is simply a lack of research available for horse chestnut, as well as many other supplements or nonpharmaceutical forms of treatment. I believe that horse chestnut possesses properties than can be beneficial to someone suffering from poor circulation, but more research should be done in order to fully understand the extent of its mechanisms and effectiveness. ~C.

Sullivan

Anya Wappler, Student Pharmacist, Spring 2023

Melatonin is a hormone produced by the pineal gland. Melatonin production is stimulated by darkness, and begins around 9 PM. Secretion peaks between 2 and 4 AM. Melatonin secretion levels decrease with age. Melatonin is a dietary supplement derived as a synthetic product from animals, and it has not been FDA-approved. It was first discovered in 1958. By the 1990s, studies led to increased use of melatonin for insomnia, jet lag, preventing pregnancy in large doses, boosting the immune system, preventing cancer, extending life, and protecting cells from free-radical damage4 .

Pharmacology

Melatonin is produced from tryptophan in the pineal gland. The tryptophan is converted to 5hydroxytryptophan, then to serotonin, then to Nacetylserotonin, then to melatonin (N-Acetyl-5methoxytryptamine). Once synthesized, melatonin is collected by the venous capillary system and secreted into cerebrospinal fluid and venous systemic circulation. In the brain, melatonin increases the binding of GABA to its receptors. Melatonin regulates the body’s circadian rhythm, endocrine secretions, and sleep patterns. It can also aid with growth hormone secretion, sexual maturation, pain control, balance, and sexual activity5 .

Drug Interactions

• Anticoagulants may increase risk of bleeding

Dosing

Common Uses:

• Jet Lag

• Delayed sleep-wake phase disorder

• Sleep disorders in children

• Anxiety before and after surgery 6

• For Analgesia: 3-10mg per day by mouth for various durations

• For Insomnia: 3-5mg per day by mouth in the evening over 4 weeks; 1-2 mg before bedtime for elderly patients

2mg by mouth preflight; 5mg by mouth postflight over a period of up to 4 days4

• Anticonvulsants may increase frequency of seizures

• Antidiabetic drugs may increase risk of hypoglycemia cannabis, and tobacco 4 AdornThemes. Neuriva Sleep Think Bigger. Schiff Vitamins. Melatonin Bottle.

• Antihypertensive drugs may increase risk of hypo/hypertension

• Caffeine may increase melatonin levels

• CNS depressants may increase sedative effects of CNS depressants

• Contraceptive drugs may increase effects and adverse effects of melatonin5

Dosage Forms

• Tablet

• Chewable tablet

• Sublingual tablet4

Effectiveness

• Delayed Sleep Phase Syndrome Melatonin has been shown to shorten the time needed to fall asleep in children and adults with DSPS

• Improves non-24-hour sleep wake disorder in blind children and adults5

Melatonin

Side Effects

• Dizziness

• Drowsiness

Safety

• Can safely use up to 8mg every day for up to 6 months

• Can safely use up to 10mg every day for up to 2 months

• Do not use frequently or in high doses if pregnant5

• Do not use in patients with autoimmune diseases4

Warnings

• Usually melatonin supplements are made in a lab, but in some cases it may be derived from animal pineal gland. This should be avoided due to risk of contamination.

• Some supplements have been found to be contaminated with serotonin

• Many supplement labels do not show the correct dose that is actually contained in the supplement

• Do not drive or operate machinery for 4-5 hours after taking melatonin5

• Headache

• Nausea

• Increased risk for seizure (rare)5

I believe that Melatonin is beneficial for its indicated uses when used correctly. However, I think that people who are just taking Melatonin in whatever doses they deem best fit for them is unsafe. Practicing good sleep takes time, but in the long run it is better to try to naturally fix your sleep cycle rather than just pop a pill every night before bed ~A Wappler~

Since the pandemic, studies have shown that more adults are taking higher doses of melatonin to help them fall asleep. Melatonin can have negative side effects when used in too high of a dose too frequently. Some of these side effects include headache, nausea, confusion, mild anxiety, depression, tremors, and low blood pressure. It is also dangerous, because many melatonin pills have been found to contain much larger amounts of melatonin than what is advertised. This is due to the fact that the FDA doesn’t fully regulate melatonin, so the pills do not have to be tested. Unfortunately, many adults do not fully realize that melatonin is not just a supplement, but that it is actually a hormone that regulates the body’s sleep cycles. Studies have found that there actually isn’t much benefit from melatonin and that other methods of training your brain to sleep are more effective2

References

1. AdornThemes. Neuriva Sleep Think Bigger. Schiff Vitamins. Accessed February 24, 2023. https://www.schiffvitamins.com/pages/ neuriva-sleep-think-bigger?&utm_source=bing&utm_medium=cpc&utm_campaign=_CN%7CSLEEP-SUPPLEMENTS_CC% 7CPROD_KC%7CGEN_MT%7CPHR&utm_term=supplements%20to%20help% 20sleep&utm_content=Supplements&gclid=3e67acee4b2e1b02b222cf19e6b42080&gclsrc=3p.ds

2. CNN SL. Using melatonin for sleep is on the rise, study says, despite potential health harms. CNN. https://www.cnn.com/2022/02/01/ health/melatonin-overuse-wellness/index.html

3. Markham Heid. Is Melatonin Safe to Take Every Night? Time. Published October 2019. https://time.com/5672106/melatonin-safety/

4. Melatonin. Lexi-Drugs. Lexicomp. Wolters Kluwer Health, Inc. Riverwoods, IL. Accessed February 24, 2023. http://online.lexi.com

5. Melatonin. Natural Medicines. Therapeutic Research Center. Stockton, CA. Accessed February 24, 2023. http://online.lexi.com

6. National Center for Complementary and Integrative Health. Melatonin: What You Need To Know. NCCIH. Published January 2021. https://www.nccih.nih.gov/health/melatonin-what-you-need-to-know

7. 购买Melatonin (NSC 113928) | MT Receptor agonist | 价格 | IC50 | 只能用于研究 Selleck.cn. Published 2016. Accessed February 24, 2023. https://www.selleck.cn/products/Melatonin.html