Powerpoint presentation
Melatonin
Endogenous melatonin is a naturally occurring compound produced in the pineal gland that regulates the sleep-wake cycle, also acts as a cytoprotective and an immunostimulatory agent.
Exogenous melatonin in the form of an over-the-counter (OTC) supplement helps with occasional insomnia, disruption of circadian rhythm due to jet-lag or shift works.
Melatonin is the fourth most popular natural supplement taken by adults and second for children in the United States (Grigg-Damberger & Ianakieva, 2017, p. 163).
In the United States Melatonin regulated by Food and Drug Administration (FDA) as a dietary supplement, while in Australia and European Union it is classified as prescription drug (Andersen et al., 2016, p. 172).
Pharmacokinetics
Plasma concentration peak arises after sixty minutes after oral administration.
Plasma concentration diminution is biphasic with a half-life of two and twenty minutes
After oral intake of one to five mg of Melatonin, melatonin concentrations ten to one hundred times than the nocturnal physiological peak. Return to basal concentration occurs in four to eight hours after ingestion.
Melatonin supplement metabolized primarily in the liver by the CYP-450 enzyme system and secondarily in the kidney (Tordjman et al., 2017, p. 436).
Pharmacodynamics
Melatonin is a naturally made hormone in the pineal gland which released into the blood.
Melatonin synthesized from the essential amino acid L-tryptophan. It helps manage the circadian rhythm or sleep-wake cycles.
Melatonin is produced more during the night and is hindered by light.
Melatonin turns on two high-affinity G protein-coupled receptors, named MT1 and MT2, within the suprachiasmatic nucleus (SCN). SCN oversees the maintenance of the twenty-four-hour cycle, which controls sleep, immune functions, and other different functions of the organism (Liu et al., 2016, p. 381).
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Contraindications/ precautions/ side effects
Contraindicated with hypersensitivity, pregnancy and breastfeeding
Cautious use with seizure disorders, hypertension, and diabetes
Side effects may include headache, dizziness, drowsiness, nausea, vomiting, abdominal cramps
Drug interactions
May diminish effectiveness of Nifedipine
May increase bleeding risk with anticoagulant and antiplatelet medications
May prohibit blood glucose lowering if used with hypoglycemic medications
May inhibit sedation with CNS depressants
May alter effect of oral birth control medication
Patient teaching
Educate patient of importance of good sleep hygiene in addition to supplement therapy:
Go to sleep and set alarm to get up at the same time every day
Do not use electronic devices three hours prior bedtime
Avoid caffeinated beverages six hours prior bedtime
Instruct to use lowest effective dosage and take one-hour prior bedtime, since higher doses causes higher incidence of side effects such as next day grogginess, vivid dreams, headache.
Avoid driving, operating machinery, and drinking alcohol after taking the supplement
Instruct patient that it is acceptable to cut Melatonin pill in half if the lower formulated dose of Melatonin is not available, as long as it is not labeled as extended-release tablets or capsules.
Melatonin dosage
It is recommended to start with 0.5 mg (500 micrograms) or 1 mg of Melatonin 30-60 minutes prior bedtime. If dose is ineffective, the patient may increase it to 3–5 mg or follow the instructions on the supplement.
Melatonin doses of 0.5 mg and 5 mg are both effective, but people who have taken 5mg on average fall asleep 7 minutes faster and slept 8 minutes longer (Andersen et al., 2016).
Consider talking about:
Assessments
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Works cited
Andersen, L. P. H., Gögenur, I., Rosenberg, J., & Reiter, R. J. (2015). The Safety of Melatonin in Humans. Clinical Drug Investigation, 36(3), 169–175. https://doi.org/10.1007/s40261-015-0368-5
Grigg-Damberger, M. M., & Ianakieva, D. (2017). Poor Quality Control of Over-the-Counter Melatonin: What They Say Is Often Not What You Get. Journal of Clinical Sleep Medicine, 13(02), 163–165. https://doi.org/10.5664/jcsm.6434
Liu, J., Clough, S. J., Hutchinson, A. J., Adamah-Biassi, E. B., Popovska-Gorevski, M., & Dubocovich, M. L. (2016). MT1and MT2Melatonin Receptors: A Therapeutic Perspective. Annual Review of Pharmacology and Toxicology, 56(1), 361–383. https://doi.org/10.1146/annurev-pharmtox-010814-124742
Tordjman, S., Chokron, S., Delorme, R., Charrier, A., Bellissant, E., Jaafari, N., & Fougerou, C. (2017). Melatonin: Pharmacology, Functions and Therapeutic Benefits. Current Neuropharmacology, 15(3), 434–443. https://doi.org/10.2174/1570159x14666161228122115