Tofisopam
Daytime, non-sedating 2,3-benzodiazepine anxiolytic that works by phosphodiesterase inhibition.
Pharmacology
Contents
WHAT IS TOFISOPAM?
Detailed overview
Tofisopam (Grandaxin) is an atypical 2,3-benzodiazepine anxiolytic that differs structurally from classic 1,4- and 1,5-benzodiazepines and also differs in mechanism: it does not potentiate GABA and binds only negligibly to the benzodiazepine site, so it is not sedating, not muscle-relaxing and does not impair psychomotor performance. Its main action is selective inhibition of phosphodiesterase isoenzymes (PDE2, PDE4, PDE10A), which raises cyclic AMP/GMP signaling, alongside dopaminergic and autonomic modulation. Clinically it targets the physical, autonomic symptoms of anxiety (racing heart, sweating, tension) without causing drowsiness, so it is used as a daytime anxiolytic. It is a marketed prescription drug in several countries (Hungary, Russia, Japan) but has never been approved by the FDA.
Mechanism
PDE inhibitor (non-GABAergic, non-sedating)
Half-life
About 6 to 8 hours
Legal status
Prescription (HU: Grandaxin), not FDA-approved
Receptor profile
- Phosphodiesterase isoenzymes (PDE2, PDE4, PDE10A)Moderate
- Dopaminergic signalingModerate
- Sympathetic autonomic toneModerate
- GABA-A benzodiazepine binding siteWeak
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Headache, the most commonly reported side effect
- Nausea, stomach upset, loss of appetite
- Restlessness, irritability, occasionally tension or agitation
- Sleep disturbance if dosed late in the evening (a corollary of its daytime, non-sedating profile)
- Rarely confusion, muscle tension or skin rash
Contraindications · 5
- Pregnancy and breastfeeding: avoid based on teratologic data
- Severe respiratory insufficiency or decompensated respiratory failure
- Galactose intolerance or lactase deficiency (due to the tablet's lactose content)
- Caution with CYP3A4-metabolized drugs (e.g. alprazolam): interaction risk
- Prescription medicine; not to be taken without medical supervision
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis
Rundfeldt C, Socała K, Wlaź P
Application of drug repositioning strategy to TOFISOPAM
Bernard P, Dufresne-Favetta C, Favetta P, Do QT, Himbert F, Zubrzycki S, Scior T, Lugnier C
Effect of tofisopam on the single-oral-dose pharmacokinetics and pharmacodynamics of the cyp3a4 probe drug alprazolam
Drabant S, Tóth M, Bereczki A, Bajnógel J, Tömlö J, Klebovich I
A population-based case-control teratologic study of nitrazepam, medazepam, tofisopam, alprazolum and clonazepam treatment during pregnancy
Eros E, Czeizel AE, Rockenbauer M, Sørensen HT, Olsen J
Immunomodulating effects of tofizopam (Grandaxin) and diazepam in vitro
Kalashnikov SV, Kalashnikova EA, Kokarovtseva SN
FAQ
FAQ
Daytime, non-sedating 2,3-benzodiazepine anxiolytic that works by phosphodiesterase inhibition.
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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.