Trazodone
SARI antidepressant widely used at low doses as a sleep aid via 5-HT2A antagonism.
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Pharmacology
Contents
WHAT IS TRAZODONE?
Detailed overview
Trazodone is a serotonin antagonist and reuptake inhibitor (SARI) antidepressant that is used more often at low doses as a sleep aid than at the higher doses used to treat depression. Its main action is potent antagonism of the serotonin 5-HT2A receptor, complemented by weaker 5-HT2C blockade and moderate serotonin reuptake inhibition. Blockade of histamine H1 and alpha-1 adrenergic receptors produces its characteristic sedation and sleep-promoting effect. The hypnotic dose (typically 25-100 mg at bedtime) is a fraction of the antidepressant dose. It is an FDA-approved prescription medicine studied in humans for decades and in extensive clinical trials.
Mechanism
5-HT2A antagonist + H1/alpha-1 blockade
Half-life
About 7-10 hours
Legal status
Prescription medicine (FDA-approved)
Receptor profile
- 5-HT2A receptor (antagonist)Strong
- Serotonin transporter (SERT)Moderate
- Histamine H1 / alpha-1 adrenergic receptorModerate
- 5-HT1A receptor (partial agonist)Weak
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Daytime drowsiness, sedation and next-day grogginess, especially when starting treatment
- Orthostatic hypotension and dizziness from alpha-1 adrenergic blockade (fall risk in the elderly)
- Dry mouth, blurred vision, constipation, nausea
- Priapism (prolonged, painful erection): rare but a medical emergency
- QT prolongation and arrhythmia risk, particularly with other QT-prolonging drugs
- Theoretical serotonin syndrome when combined with other serotonergic agents
Contraindications · 5
- Concurrent or recent MAO inhibitor use (risk of serotonin syndrome)
- Recovery after recent myocardial infarction; known QT prolongation or serious arrhythmia
- Pregnancy and breastfeeding: only under clear medical indication and supervision
- Alcohol and other CNS depressants taken together intensify the sedation
- Prescription medicine: not to be taken without medical supervision
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Trazodone improves sleep parameters in Alzheimer disease patients: a randomized, double-blind, and placebo-controlled study
Camargos EF, Louzada LL, Quintas JL, Naves JO, Louzada FM, Nobrega OT
Trazodone changed the polysomnographic sleep architecture in insomnia disorder: a systematic review and meta-analysis
Zheng Y, Lv T, Wu J, Lyu Y
Antidepressants for insomnia in adults
Everitt H, Baldwin DS, Stuart B, Lipinska G, Mayers A, Malizia AL, Manson CC, Wilson S
The effects of trazodone on human cognition: a systematic review
La AL, Walsh CM, Neylan TC, Vossel KA, Yaffe K, Krystal AD, Miller BL, Karageorgiou E
Treatment of Alzheimer's Disease: Trazodone, Sleep, Serotonin, Norepinephrine, and Future Directions
La AL, Walsh CM, Neylan TC, Vossel KA, Yaffe K, Krystal AD, Miller BL, Karageorgiou E
FAQ
FAQ
SARI antidepressant widely used at low doses as a sleep aid via 5-HT2A antagonism.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.