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Pagoclone
Pagoclone belongs to the cyclopyrrolone class,1 structurally related to zopiclone. It reduces anxiety with little sedation or memory impairment at low doses. It was investigated as a potential treatment for panic disorder1 and stuttering2, but was never commercialized after trials showed insufficient efficacy to support continued development. Its abuse potential has been assessed as similar to, or slightly lower than, that of diazepam.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Subjective Effects
Pharmacology
Pharmacodynamics
Pagoclone enhances GABA-A receptor activity through the benzodiazepine binding site.3 It binds with high affinity to receptors containing α1, α2, α3, or α5 subunits, acting as a partial agonist at α1-, α2-, and α5-containing receptors and an essentially full agonist at α3-containing receptors. Its affinity for receptors containing α4 or α6 subunits is low. Human receptor-occupancy and eye-movement findings are consistent with partial agonist activity.
Pharmacokinetics
Pagoclone forms hydroxypagoclone, a primary phase I metabolite, in humans.4 This metabolite was detected after incubation with hepatocytes and liver S-9 fractions, but not liver microsomes.4 In rats, its concentrations in brain and plasma were 10-20 times those of pagoclone; higher metabolite concentrations were also reported in squirrel monkeys.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Harm Potential
Addiction & Dependence
Psychological
ModeratePagoclone's abuse potential appears similar to or slightly less than diazepam, with development concerns related to abuse.
Physical
ModeratePhysical dependence probably develops over sufficient time, with tolerance and possible withdrawal symptoms such as anxiety and insomnia.
Toxicity
Reported acute effects include drowsiness, impairment, sedation, and reduced learning, memory, and alertness.
History & Culture
Origins and early development
Pagoclone was synthesized by a French team working for Rhone-Poulenc & Rorer S.A. A 1994 Rhone-Poulenc patent described the compound and its proposed therapeutic properties. Rhone-Poulenc subsequently licensed it to the American company Interneuron Pharmaceuticals, which later became…
Legality
By Country
References
Citations
Article Status
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