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Melatonin

Generic Medicine
Indications

Melatonin is used for several conditions, but it is most effective for short-term regulation of sleep patterns, including jet lag.

Insomnia: Melatonin helps induce sleep in individuals with:

  • Disrupted circadian rhythm (e.g., jet lag, night shift workers, or visual impairment)
  • Low melatonin levels (e.g., some elderly patients and patients with schizophrenia)
  • Children with learning disabilities associated with insomnia

Other uses include:

Osteoporosis: stimulates osteoblast activity, supporting bone formation

Menopause: helps peri- and postmenopausal women regulate sleep cycles

Eating disorders: may be involved in anorexia-related symptoms

ADHD: may improve sleep disturbances in children

Sarcoidosis

Description

Melatonin is a hormone produced by the pineal gland in the brain that regulates other hormones and maintains the body’s circadian rhythm (sleep–wake cycle). It responds to light exposure: darkness increases melatonin secretion, while light suppresses it. It plays a key role in adapting to daily light–dark cycles, seasonal changes, and environmental light intensity. Disruption of normal melatonin production may occur in jet lag, shift work, and visual impairment. Melatonin also influences reproductive hormone timing, and research suggests it may be linked to aging. In addition to hormonal effects, it has strong antioxidant properties and supports immune function.

Pharmacology

After administration, melatonin binds to specific receptors known as MT1 and MT2 receptors. These receptors are found in the brain and peripheral tissues. MT1 receptors are located in the pituitary gland and suprachiasmatic nucleus of the hypothalamus. MT2 receptors are mainly found in the retina. Activation of these receptors regulates neurotransmitters such as serotonin, GABA, and dopamine. Increased melatonin promotes sleep initiation and maintenance while stabilizing the circadian rhythm.

Dosage Administration

Adult:

Insomnia: 3-6 mg one hour before bedtime

Jet lag:

  • 0.50 to 5 mg one hour prior to bedtime at final destination or, 1 to 5 mg 1 hour before bedtime for 2 days prior to departure and for 2 to 3 days upon arrival at final destination.
  • Eastbound travel- Take a preflight early evening treatment followed by treatment at bedtime for 4 days after arrival.
  • Westbound travel- Take for 4 days at bedtime when in the new time zone

Sarcoidosis: 20 mg per day for 4 to 12 months.

Depression: 0.125 mg twice in the late afternoon, each dose 4 hours apart.

Difficulty falling asleep: 5 mg 3 to 4 hours before an imposed sleep period over a 4-weeks period.

Children (6 months to 14 years of age): For sleep disorders 0.30 mg/day

Interactions

Melatonin may interact with several medicines and substances:

Antidepressants: Melatonin may reduce the effect of desipramine and fluoxetine. Fluoxetine may also lower natural melatonin levels in the body.

Antipsychotics: In patients with schizophrenia or tardive dyskinesia, melatonin combined with antipsychotic drugs may reduce abnormal mouth movements.

Benzodiazepines: Combination with triazolam may improve sleep quality. Melatonin may also help some patients discontinue long-term benzodiazepine use.

Antihypertensive drugs: Melatonin may reduce the effectiveness of drugs like methoxamine and clonidine. Calcium channel blockers (e.g., nifedipine, verapamil, diltiazem, amlodipine, etc.) may lower melatonin levels. Beta-blockers (e.g., propranolol, atenolol, metoprolol, etc.) may reduce melatonin production.

Anticoagulants: Melatonin may increase bleeding risk when used with warfarin and similar blood thinners.

Interleukin-2: Combined use may improve tumor response and survival in some cancer patients.

NSAIDs: Drugs like ibuprofen may reduce melatonin levels.

Steroids & immunosuppressants: May reduce the effectiveness of these medicines.

Tamoxifen: Possible beneficial effect in certain cancer patients when used together.

Other substances: Caffeine, tobacco, and alcohol may reduce melatonin levels, while cocaine and amphetamines may increase it.

Contraindications

Melatonin should not be used in patients with autoimmune diseases.

Side Effects

Common side effects include headache and mild depression. Drowsiness may occur within 30 minutes of intake and can last for about 1 hour, which may affect driving or alertness.

Pregnancy & Lactation

There is insufficient information regarding the safety and effectiveness of melatonin during pregnancy and breastfeeding.

Precautions & Warnings

Caffeine and fluvoxamine may increase the effects of melatonin. Melatonin may reduce the blood pressure-lowering effect of nifedipine.

Overdose Effects

There is little evidence of serious toxicity even at high doses of melatonin.

Therapeutic Class

Hormonal preparations / Sleep-regulating agents / Nutritional supplements

Storage Conditions

Store below 30°C, protected from light. Keep all medicines out of reach of children.

Common Questions

What is Melatonin for?

What does Melatonin do?

What are the side effects of Melatonin?

What happens if you take too much Melatonin?

Can Melatonin be taken during pregnancy?

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