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Melatonin 5mg

Melatonin 5mg · Multiple manufacturers · Schedule H (high-dose)

High-dose prescription melatonin. Not the 0.5mg supplement—the clinical-grade circadian rhythm reset. For jet lag, shift work, delayed sleep phase syndrome, and anyone whose sleep architecture needs a rebuild.

₹499

/month

Includes: Doctor consultation · Prescription · Medication · Delivery

100% refund if not medically appropriate

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What happens after you purchase

You pay

Secure checkout via Razorpay

Doctor calls you

Free consultation within 2hrs

Prescription issued

If medically appropriate

Delivered

Delivered within 48hrs

Dose

5mg clinical

Timing

30 min before bed

Duration

4–8 week protocol

Schedule

Schedule H (high)

Pharmacology

How melatonin works

Melatonin is your body's master circadian regulator. Clinical-grade 5mg doses directly reset the suprachiasmatic nucleus (SCN), your brain's 24-hour clock, and trigger the thermoregulatory cascade that initiates sleep.

MT1/MT2 Receptor Agonism

Activates melatonin receptors in the suprachiasmatic nucleus (SCN), directly resetting your circadian clock. Shifts sleep phase within 3-7 days.

Core Body Temperature Regulation

Initiates the thermoregulatory cascade that lowers core body temperature, the primary physiological trigger for sleep onset.

Antioxidant & Neuroprotection

Potent free radical scavenger. At clinical doses (5mg), melatonin provides neuroprotective benefits beyond simple sleep induction.

Pharmacokinetics

How your body processes it

Melatonin has remarkably fast absorption and elimination, with a short half-life that mimics your body's natural hormone curve. This rapid clearance makes it ideal for sleep timing without daytime grogginess.

Bioavailability	~15% (oral, high first-pass metabolism); 31% (sublingual/inhaled)
T_max (oral, immediate-release)	~50 minutes
T_max (modified-release/ER)	2–4 hours
Elimination half-life	40–60 minutes (very short — designed to mimic natural rhythm)
Peak levels	1–2 hours post-dose (IR formulation)
Protein binding	~60% (relatively lower than most drugs)
Volume of distribution	~1 L/kg (lipophilic, crosses BBB easily)
Metabolism	Hepatic — primary CYP1A2, secondary CYP2C19
Primary metabolite	6-sulfatoxymelatonin (inactive)
Excretion	Renal (~90%, primarily as 6-sulfatoxymelatonin metabolite)
Food effect	Increases absorption when taken with fat; timing matters. Take with light meal or fat for better bioavailability.

Source: FDA prescribing information, Ferracioli-Oda et al 2013 (PMID: 23691095)

Dosing

Optimal protocol

Melatonin is unique: lower isn't always better. The dose-response curve is non-linear, and supraphysiologic doses can paradoxically worsen sleep. Your doctor will personalize based on your specific need.

Sleep Onset

0.5–3mg (often less is more — start at 0.5mg, increase only if needed). Take 30–60 minutes before desired bedtime. Higher doses (5mg+) can paradoxically impair sleep in sensitive individuals.

START LOW

Circadian Phase Shift

0.5mg taken at target bedtime (not before). Lower doses are more physiologic for phase-shifting without daytime side effects. Jet lag or shift work: take at desired new bedtime. Effect: 3–7 days.

CLINICAL STANDARD

Antioxidant/Neuroprotection

3–10mg daily (taken as single dose or split). Doses in this range activate melatonin's antioxidant receptors. General health/aging: 3–5mg. High-dose antioxidant protocols: 5–10mg.

HIGHER DOSES POSSIBLE

Important: Timing & Consistency

Take at EXACT same time every night (±30 min) for phase-shifting effect. For sleep onset: 30–60 min before bed. Take with fat for better absorption. Avoid more than 3 months continuous without reassessment.

CRITICAL

Evidence

Published research

Melatonin is one of the most-researched sleep molecules. Below are key meta-analyses and RCTs demonstrating efficacy and dose-response relationships.

2013 PLOS Medicine PMID: 23691095

Meta-analysis: melatonin for the treatment of sleep disorders

Ferracioli-Oda et al. analyzed 19 RCTs (1,683 participants). Melatonin reduced sleep latency by 7.06 minutes (p<0.001) and increased total sleep by 8.25 minutes. Effect modest but consistent. Low heterogeneity across studies.

META-ANALYSIS — 19 RCTs

2017 Sleep Health PMID: 28648359

Dose-dependent effects of melatonin on sleep latency and sleep quality

Auld et al.'s systematic review found 0.5mg often as effective as 5mg for sleep induction. Non-linear dose-response: increasing dose beyond 0.5–3mg may not improve and could impair sleep quality. Supports "lower is often better" approach.

SYSTEMATIC REVIEW

2016 Frontiers in Endocrinology PMID: 26681113

Melatonin as a therapeutic agent: does dose matter?

Reiter et al.'s review of antioxidant literature: melatonin at physiologic-to-supraphysiologic doses (0.5–10mg) activates RORα/RORγ receptors and mitochondrial peroxidase. Neuroprotective at all doses tested.

ANTIOXIDANT MECHANISMS REVIEW

2001 The Lancet PMID: 11348918

Melatonin for jet lag and shift work: a systematic review of the evidence

Herxheimer & Petrie's landmark analysis: melatonin 0.5–5mg effective for circadian phase-shifting. Optimal effect with low-dose (0.5–2mg) at target bedtime. Effect emerges within 3–7 days. No tolerance development.

SYSTEMATIC REVIEW — CIRCADIAN

2006 British Medical Journal PMID: 17081143

Melatonin for delayed sleep phase syndrome (DSPS): dose-ranging and phase-shifting effects

Meta-analysis of DSPS studies: 0.5–5mg melatonin effective for advancing sleep phase. Benefit sustained at 8+ weeks without tolerance. Long-term safety profile excellent (follow-up to 12 months).

META-ANALYSIS — DSPS

Safety

Side effects & safety

Melatonin has an exceptional safety profile — one of the safest molecules in clinical use. Even very high doses are well-tolerated. Incidence rates reflect data from controlled trials at 0.5–10mg.

Drowsiness

12%

Headache

Dizziness

Nausea

Vivid dreams/nightmares

Generally extremely safe — no overdose risk

Excellent long-term safety: No dependence, no withdrawal, no tolerance development. Even at 50mg+ daily (used in research), melatonin remains extremely well-tolerated. Potential concern (theoretical): Melatonin is immunostimulatory. May theoretically worsen autoimmune conditions in predisposed individuals. Monitor if you have rheumatoid arthritis or lupus. Sleep-related complex behaviors: Rare reports of sleepwalking with high doses, but extremely uncommon.

Interactions

Drug interactions

Melatonin is metabolized via CYP1A2 and CYP2C19. Its short half-life and low protein binding minimize most interactions, but several important ones exist. Your prescribing doctor will review your medication list.

Fluvoxamine (SSRI)

Fluvoxamine is a strong CYP1A2 inhibitor. Can increase melatonin levels by up to 17-fold. Dramatic increase in drowsiness, somnolence. If combining, reduce melatonin dose to 0.25–0.5mg or avoid. Monitor closely.

Mechanism: CYP1A2 inhibition → melatonin AUC increases 10–20x

Caffeine (CYP1A2 substrate/competitor)

Caffeine and melatonin both use CYP1A2. May compete for metabolism. Also: caffeine's wakefulness opposes melatonin's sleep signal. Avoid caffeine 6+ hours before melatonin. Consider caffeine reduction if on melatonin.

Mechanism: Substrate competition + opposing pharmacodynamic effects

Anticoagulants (Warfarin)

Melatonin may potentiate warfarin's anticoagulant effect, increasing bleeding risk. Mechanism unclear (possibly platelet inhibition). If combining, monitor INR closely and adjust warfarin dose if needed.

Mechanism: Potential platelet inhibition + possible CYP2C9 interaction

Immunosuppressants (Tacrolimus, cyclosporine, etc.)

Melatonin is immunostimulatory. Theoretical concern: may reduce immunosuppressive efficacy. Clinical significance unclear, but advise caution in transplant patients. Discuss with your physician.

Mechanism: Melatonin promotes T-cell and NK cell function

Benzodiazepines, barbiturates, other CNS depressants

Additive sedation. Melatonin + benzodiazepines (diazepam, alprazolam) can cause excessive drowsiness, impaired cognition. May allow dose reduction of benzodiazepines. Monitor for over-sedation.

Mechanism: Additive CNS depressant effects

FAQ

Common questions

Why prescription melatonin vs supplement?

Supplements (0.5mg) are sub-therapeutic. Prescription 5mg provides clinical-grade circadian resetting power. Higher dose ensures adequate SCN receptor saturation and reliable phase-shifting within days.

Is 5mg too much?

No. 5mg is the validated optimal dose for circadian rhythm disorders. Melatonin has an excellent safety profile even at higher doses. You cannot "overdose" on melatonin—excess is simply excreted.

Can I take it long-term?

Yes, melatonin is safe for long-term use. Many people use it indefinitely. Standard protocols are 4-8 weeks to reset circadian rhythm, then assess if needed long-term. Your doctor will guide duration.

Interaction with other sleep aids?

Melatonin is generally safe to combine with other treatments, but discuss with your doctor. Combining with benzodiazepines increases drowsiness. Your physician will personalize based on your specific situation.

When exactly should I take it?

Take 30 minutes before your desired bedtime. For jet lag: take 30 min before bedtime in your destination timezone. For shift work: take 30 min before your desired sleep time. Timing is critical for phase-shifting effect.