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Melatonin
Pronunciation
Synonyms
Pharmacological Index
Use
Adverse Reactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Reference Range
Dosage Forms

Pronunciation
(mel ah TOE nin)

Synonyms
N-Acetyl-5-methoxytryptamine

Pharmacological Index

Hormone; Hypnotic, Miscellaneous


Use

Sleep disorders (insomnia), circadian rhythm disturbances (ie, jet lag); only FDA approval (as an orphan drug) is for treatment of circadian rhythm sleep disorders in blind people with no light perception


Adverse Reactions

Percentage unknown:

Dermatologic: Pruritus

Gastrointestinal: Nausea

Miscellaneous: Increase in alkaline phosphatase


Mechanism of Action

A hormone produced and secreted in the pineal gland causes an increase in hypothalamus aminobutyric acid and serotonin. Increased secretion occurs during dark hours; decreases neopterin release; counteracts apoptosis; increases thymus activity


Pharmacodynamics/Kinetics

Absorption: Rapid

Peak plasma level: 1 hour


Usual Dosage

Oral:

Hypnotic effects: Oral: 0.1-0.3 mg (daytime); 1-10 mg (nighttime)

Insomnia: 5-75 mg at night have been used


Reference Range

Mean baseline melatonin serum levels 80 pg/mL (range: 0-200) between 2-4 AM. Elevated endogenous levels seen after 9 AM; after a 2.5 mg oral dose, plasma melatonin level may be as high as 8.50 pg/mL.


Dosage Forms

Tablet: 3 mg

Tablet, sublingual: 2.5 mg


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