Pharmaceutical

AFOBAZOL

Fabomotizole

Evidence TierCWADA NOT PROHIBITED

tuneTypical Dose

10–30 mg per day (divided TID)

watchEffect Window

5–7 days onset, full benefit at 4 weeks

check_circleCompliance

WADA NOT PROHIBITED

Overview

Clinical Summary

Afobazol (fabomotizole) is a regionally marketed anxiolytic used for anxiety and stress symptoms. Limited clinical data suggest less sedation than diazepam, but the evidence base is narrow and geographically concentrated.

Small mostly Russian clinical studies report reductions in anxiety symptoms and stress-related somatic complaints, often with fewer sedative adverse effects than diazepam. Some trials suggest improved sleep quality via reduced hyperarousal. Minority research explores support for nicotine withdrawal and stress resilience, but evidence remains regionally concentrated, lightly replicated, and methodologically uneven.

Sigma-1 receptor agonist with reversible MAO-A inhibition and indirect GABA-A modulation. Does not bind the benzodiazepine site, avoiding sedation and dependence.

Outcomes

What This Is Expected To Influence

Primary Outcomes

Anxiolysis comparable to diazepam without sedation (Russian trials)
No withdrawal syndrome on discontinuation

Secondary Outcomes

Potential neuroprotective and cognitive-preserving effects under stress

Safety

Contraindications and Interactions

Contraindications

Pregnancy
Lactation
Severe hepatic or renal impairment

Side effects

Mild headache (infrequent)
Allergic skin reactions (rare)
Mild GI upset/dry mouth (rare)

Interactions

Diazepam (potentiates anxiolytic/sedative effect, useful for taper, requires dose adjustment)
Carbamazepine (may enhance anticonvulsant effect)
SSRIs/SNRIs (theoretical serotonergic overlap from MAO-A component)
Phenibut (avoid due to unpredictable GABAergic overlap)

Avoid if

Pregnancy
Lactation
Children under 18
Individuals seeking acute panic relief (5–7 day onset)

Evidence

Study-level References

afobazol-SRC-001RCT

Sourceopen_in_new

Syunyakov TS, Neznamov GG. Evaluation of the therapeutic efficacy and safety of the selective anxiolytic afobazole in generalized anxiety disorder and adjustment disorders. Ter Arkh. 2016;88(8):73-86. doi:10.17116/terarkh201688873-86. PMID:27636931.

Population: Adult patients with generalized anxiety disorder (GAD) and adjustment disorders (AD)

Dose protocol: 30 mg/day for 30 days (n=100 afobazol, n=50 diazepam)

Key findings: Afobazol was reported as non-inferior to diazepam for anxiety reduction, with fewer adverse events and no withdrawal syndrome reported during follow-up.

Paper content

This multicenter, randomized phase III trial compared the selective anxiolytic afobazole to diazepam in patients with generalized anxiety disorder and adjustment disorders. Afobazole demonstrated non-inferiority to diazepam in treating both conditions while showing a superior safety profile. The study supports afobazole as an effective and safer alternative to benzodiazepines for anxiety management.

afobazol-SRC-002Animal study (controlled experiment) with in silico docking

Sourceopen_in_new

Voronin MV, Vakhitova YV, Tsypysheva IP, et al. Involvement of Chaperone Sigma1R in the Anxiolytic Effect of Fabomotizole. Int J Mol Sci. 2021;22(11):5455. doi:10.3390/ijms22115455. PMID:34064275.

Population: Male BALB/c mice tested in elevated plus maze

Dose protocol: Fabomotizole (2.5 mg/kg i.p.) administered 30 min prior to elevated plus maze, with or without Sigma1R antagonist pretreatment (BD-1047 or NE-100 at 1.0 mg/kg i.p.)

Key findings: Fabomotizole's anxiolytic effect was blocked by Sigma1R antagonists BD-1047 and NE-100 in elevated plus-maze, confirming sigma-1 receptor chaperone agonism as the primary anxiolytic mechanism. Binding affinity comparable to (+)-pentazocine.