Melatonin (N-acetyl-5-methoxytryptamine, pineal hormone melatonin)

Suggested dosing of N-acetyl-5-methoxytryptamine, pineal hormone melatonin (melatonin)

 

Benzodiazepine Withdrawal in Elderly with Insomnia

2 mg controlled-release PO qHS for up to 6 months; taper dose over 6 weeks

 

Cancer, Adjunctive Therapy

10-50 mg PO daily

 

Cluster Headache, Prevention

10 mg PO qHs

 

Migraine Headache

3 mg PO Hs

 

Insomnia

3-5 mg PO qHs

Difficulty falling asleep

• 5 mg PO 3-4 hour before sleep period x 4 weeks

Difficulty maintaining sleep

• Use controlled release formulation

 

Thrombocytopenia, Chemo-related

20 mg PO qHs

 

Jet Lag

0.5-5 mg PO Hs

Eastbound

• Preflight, early evening dose followed by HS dosing x 4days

Westbound

• Treat HS x 4days when in new time zone

 

Chronic Fatique Syndrome

5 mg PO Hs

 

Nicotine Withdrawal

0.3 mg PO 3.5 hours after stopping smoking

 

Winter Depression

0.125 mg PO twice daily

 

Premedication for Surgery

0.5 mg/kg SL

 

Tardive Dyskinesia

10 mg controlled-release PO qDay

 

Sleep Disorders (Orphan)

Treatment of circadian rhythm sleep disorders in blind people without light perception

Orphan indication sponsor

• Neurim Pharmaceuticals, Ltd; 8 Hanechoshet St; Tel-Aviv, Israel
• Sack, Robert, M.D.; Oregon Health Sciences University, 3181 S.W. Sam Jackson Park Road; Portland, OR 97201

 

Encephalopathy (Orphan)

Orphan designation for treatment of neonatal hypoxic ischemic encephalopathy

Orphan sponsor

• Scharper S.p.A.; Viale Ortles 12; Milan 20139, Italy

 

Suggested uses of N-acetyl-5-methoxytryptamine, pineal hormone melatonin (melatonin)

Alzheimer's disease, benzodiazepine or nicotine withdrawal, cancer (adjunctive treatment), headache (prevention), insomnia, jet lag, shift-work disorder, sleep disorders , thrombocytopenia (chemo-induced), winter depression, tardive dyskinesia

 

Efficacy

Circadian rhythm sleep disorders: FDA orphan drug status

Insomnia: Helpful for sleep-wake cycle disorders

Research is continuing

 

N-acetyl-5-methoxytryptamine, pineal hormone melatonin (melatonin) adverse (side) effects

Frequency not defined

Abdominal cramps

Alertness decreased

Circadian rhythm disruption

Daytime fatigue

Depression (transient)

Dizziness

Drowsiness

Dysphoria in depressed patients

Headache

Irritability

 

Warnings

Contraindications

Concurrent immunosuppressive treatment

 

Cautions

Age <20 years old, depression, hypertension, impaired liver function, seizure disorder

 

Pregnancy and lactation

Pregnancy category: avoid use

Lactation: avoid use

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of N-acetyl-5-methoxytryptamine, pineal hormone melatonin (melatonin)

Mechanism of action

Hormone produced by pineal gland; regulates sleep cycle

 

Pharmacokinetics

Not studied