MedPath

Melatonin

Generic Name
Melatonin
Brand Names
Circadin, Slenyto, Melatonin Neurim
Drug Type
Small Molecule
Chemical Formula
C13H16N2O2
CAS Number
73-31-4
Unique Ingredient Identifier
JL5DK93RCL

Overview

Melatonin is a biogenic amine that is found in animals, plants and microbes. Aaron B. Lerner of Yale University is credited for naming the hormone and for defining its chemical structure in 1958. In mammals, melatonin is produced by the pineal gland. The pineal gland is small endocrine gland, about the size of a rice grain and shaped like a pine cone (hence the name), that is located in the center of the brain (rostro-dorsal to the superior colliculus) but outside the blood-brain barrier. The secretion of melatonin increases in darkness and decreases during exposure to light, thereby regulating the circadian rhythms of several biological functions, including the sleep-wake cycle. In particular, melatonin regulates the sleep-wake cycle by chemically causing drowsiness and lowering the body temperature. Melatonin is also implicated in the regulation of mood, learning and memory, immune activity, dreaming, fertility and reproduction. Melatonin is also an effective antioxidant. Most of the actions of melatonin are mediated through the binding and activation of melatonin receptors. Individuals with autism spectrum disorders (ASD) may have lower than normal levels of melatonin. A 2008 study found that unaffected parents of individuals with ASD also have lower melatonin levels, and that the deficits were associated with low activity of the ASMT gene, which encodes the last enzyme of melatonin synthesis. Reduced melatonin production has also been proposed as a likely factor in the significantly higher cancer rates in night workers.

Indication

Used orally for jet lag, insomnia, shift-work disorder, circadian rhythm disorders in the blind (evidence for efficacy), and benzodiazepine and nicotine withdrawal. Evidence indicates that melatonin is likely effective for treating circadian rhythm sleep disorders in blind children and adults. It has received FDA orphan drug status as an oral medication for this use. A number of studies have shown that melatonin may be effective for treating sleep-wake cycle disturbances in children and adolescents with mental retardation, autism, and other central nervous system disorders. It appears to decrease the time to fall asleep in children with developmental disabilities, such as cerebral palsy, autism, and mental retardation. It may also improve secondary insomnia associated with various sleep-wake cycle disturbances. Other possible uses for which there is some evidence for include: benzodiazepine withdrawal, cluster headache, delayed sleep phase syndrome (DSPS), primary insomnia, jet lag, nicotine withdrawal, preoperative anxiety and sedation, prostate cancer, solid tumors (when combined with IL-2 therapy in certain cancers), sunburn prevention (topical use), tardive dyskinesia, thrombocytopenia associated with cancer, chemotherapy and other disorders.

Associated Conditions

  • Insomnia

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/06/25
Phase 2
Not yet recruiting
2025/06/24
Phase 4
Active, not recruiting
2025/05/30
Not Applicable
Recruiting
CMH Kharian Medical College
2025/04/29
Phase 1
Recruiting
Mian Muhammad Hassan Ahmed
2025/04/20
Phase 2
Not yet recruiting
2025/03/27
Phase 4
Completed
Konya City Hospital
2025/03/25
Early Phase 1
Recruiting
2025/03/25
Phase 3
Recruiting
2025/03/05
Phase 3
Not yet recruiting
Bart Koes
2025/02/20
Not Applicable
Active, not recruiting

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
BioActive Nutritional, Inc.
43857-0020
ORAL
6 [hp_X] in 1 mL
5/14/2025

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
CIRCADIN™ PROLONGED RELEASE TABLETS 2MG
SIN13954P
TABLET, EXTENDED RELEASE
2 mg
5/4/2011

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

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