Serotonin releaser
- Reverses the serotonin transporter → serotonin floods out independent of firing
- High serotonin-toxicity risk, especially with MAO inhibition
- Serotonicity — how much a drug raises synaptic serotonin; distinction from “serotonergic”
Drugs with this mechanism (11)
- Mixed amphetamine salts XR — Extended-release stimulant for ADHD; long coverage with Schedule II misuse risk.
- Amphetamine XR-ODT — Extended-release orally disintegrating amphetamine for ADHD; no pill swallowing needed.
- Mixed amphetamine salts — Monoamine-releasing stimulant for ADHD and narcolepsy; effective but readily misused.
- Amphetamine XR suspension — Extended-release liquid amphetamine for ADHD; useful when pills are difficult.
- Amphetamine racemic (1:1) — Racemic amphetamine for ADHD; more peripheral sympathomimetic effect than dextro-rich products.
- Fenfluramine — Serotonin releaser once in "fen-phen"; now for Dravet seizures, valvulopathy risk.
- Methylenedioxymethamphetamine — Serotonin releaser (empathogen) under study for PTSD.
- Mephedrone — Synthetic cathinone ("meow meow") stimulant; a monoamine releaser.
- Methamphetamine — Potent, CNS-penetrant amphetamine; high addiction liability, rare medical use.
- Mixed amphetamine salts (triple-bead) — Triple-bead extended-release mixed amphetamine salts for all-day ADHD coverage.
- Phentermine — Amphetamine-like appetite suppressant for short-term weight loss.
Self-check
- Does serotonin release through transporter reversal depend on neuronal firing?
No. - Which co-mechanism especially increases serotonin-toxicity risk?
MAO inhibition.
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