Melatonin

Melatonin is a neurohormone naturally produced by the pineal gland in response to darkness, playing a fundamental role in regulating the body’s circadian rhythm and sleep-wake cycle. Supplemental melatonin is synthetically produced to mirror this endogenous compound and is widely utilized for managing sleep disorders and circadian misalignment. It serves as a chronobiotic agent, effectively resynchronizing the sleep phase in conditions such as jet lag, shift work sleep disorder, and delayed sleep-wake phase disorder. Available in various formulations including immediate-release tablets, extended-release capsules, and sublingual forms, it provides a non-prescription option for individuals seeking to improve sleep initiation and maintenance.

Features

• Synthetic analog of endogenous melatonin hormone
• Available in immediate-release, extended-release, and sublingual formulations
• Typical strengths range from 0.5 mg to 10 mg
• Often combined with complementary ingredients like magnesium or L-theanine
• Generally non-habit forming with a short half-life (20–50 minutes)
• Produced under cGMP (current Good Manufacturing Practices) standards

Benefits

• Facilitates faster sleep onset by reducing sleep latency
• Helps realign disrupted circadian rhythms due to jet lag or shift work
• May improve overall sleep quality and morning alertness
• Supports the management of non-24-hour sleep-wake disorder in blind individuals
• Provides a non-benzodiazepine alternative for sleep support
• Contributes to antioxidant and immune-modulating activity

Common use

Melatonin is primarily indicated for the short-term management of insomnia, particularly sleep onset insomnia. It is also widely used for alleviating symptoms of jet lag by accelerating adaptation to new time zones. Shift workers often use melatonin to improve daytime sleep quality and duration. In pediatric populations, it may be used under medical supervision for sleep disturbances associated with neurodevelopmental disorders such as autism spectrum disorder or attention-deficit/hyperactivity disorder (ADHD). Off-label uses include supporting sleep in individuals with tinnitus, reducing preoperative anxiety, and mitigating cluster headaches.

Dosage and direction

Dosage should be individualized based on the sleep disorder being treated and patient response. For jet lag, 0.5–5 mg taken close to the target bedtime at the destination is recommended, starting one day prior to travel. For insomnia, doses typically range from 1–10 mg taken 30–60 minutes before desired sleep time. Lower doses (0.5–1 mg) are often sufficient for circadian rhythm regulation, while higher doses may be used for sleep maintenance. Sublingual formulations should be placed under the tongue for rapid absorption. Use is generally recommended for short-term periods (up to 13 weeks) unless advised otherwise by a healthcare provider.

Precautions

Avoid activities requiring mental alertness, such as driving or operating machinery, for at least 4–5 hours after ingestion. Use with caution in patients with hepatic impairment, as melatonin is metabolized by the liver. May cause drowsiness the following day; patients should assess tolerance before engaging in hazardous tasks. Not recommended for long-term use without medical supervision. Discontinue use at least two weeks prior to elective surgery due to potential effects on coagulation and immune response. Store out of reach of children to prevent accidental ingestion.

Contraindications

Melatonin is contraindicated in individuals with known hypersensitivity to melatonin or any component of the formulation. Should not be used by patients with autoimmune diseases due to potential immunostimulatory effects. Contraindicated in those taking immunosuppressive therapy. Not recommended during pregnancy or breastfeeding due to insufficient safety data. Avoid use in patients with severe hepatic impairment. Use is contraindicated in individuals with epilepsy, as it may increase seizure frequency.

Possible side effects

Common side effects include daytime drowsiness, headache, and dizziness. Less frequently, patients may experience nausea, irritability, or mild anxiety. Hypothermia and reduced blood pressure have been reported at higher doses. Vivid dreams or nightmares may occur, particularly with extended-release formulations. In rare cases, melatonin may precipitate hormonal changes, including reduced sperm motility or alterations in prolactin secretion. Most side effects are dose-dependent and transient.

Drug interaction

Melatonin may interact with anticoagulants and antiplatelet drugs (e.g., warfarin, aspirin), increasing the risk of bleeding. Concurrent use with sedatives, including benzodiazepines, alcohol, or antihistamines, may potentiate sedation. It may reduce the effectiveness of antihypertensive medications. Melatonin can interact with fluvoxamine and other CYP1A2 inhibitors, increasing melatonin concentrations. Use with immunosuppressants (e.g., corticosteroids) is not advised. Caution is warranted with diabetes medications due to potential effects on glucose metabolism.

Missed dose

If a dose is missed, it should be skipped entirely. Do not double the next dose. Taking melatonin later in the night or early morning may result in residual drowsiness and disrupt the following night’s sleep cycle. Resume the regular dosing schedule the next evening.

Overdose

Symptoms of overdose may include severe drowsiness, confusion, and disorientation. In extreme cases, hypothermia and hypotension may occur. There is no specific antidote for melatonin overdose; treatment is supportive and symptomatic. Gastric lavage or activated charcoal may be considered if ingestion was recent. Patients should seek immediate medical attention if an overdose is suspected.

Storage

Store in a tightly closed container at room temperature (15–30°C or 59–86°F), away from light, moisture, and heat. Do not freeze. Keep out of reach of children and pets. Discard any product that has passed its expiration date or shows signs of degradation.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Individual responses to melatonin may vary. Consult a healthcare professional before starting any new supplement, especially if you have underlying health conditions or are taking other medications. Not evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease.

Reviews

Clinical studies and user reports generally indicate that melatonin is effective for reducing sleep onset latency and improving sleep quality in the short term. Many users report subjective improvements in jet lag symptoms and shift work adaptation. Critical reviews note that effects may diminish with prolonged use, and optimal dosing remains highly individualized. Some users report minimal effect, particularly those with long-term insomnia. Overall, it is considered a well-tolerated option for circadian rhythm regulation when used appropriately.