Phenibut is commonly marketed in various OTC products, one specifically branded as “Za Za”. Ingredients of Za Za includes a proprietary blend of Phenibut, Tianeptine and Piper Methysticum (Kava). What are the mechanisms of actions of Tianeptine and Kava?
According to cited reference, tianeptine is an “efficacious μ-opioid receptor (MOR) and δ-opioid receptor (DOR) agonist”, although with much lower potency compared to MOR. Kava is a psychotropic plant indigenous to the South Pacific that has anxiolytic effects. Its mechanism is due to its “modulation of GABA activity via alteration of lipid membrane structure and sodium channel function, monoamine oxidase B inhibition, and noradrenaline and dopamine re-uptake inhibition.”
Gassaway, M M, et al. “The Atypical Antidepressant and Neurorestorative Agent Tianeptine Is a μ-Opioid Receptor Agonist.” Translational Psychiatry, 15 July 2014, www.ncbi.nlm.nih.gov/pmc/articles/PMC4119213/. and Sarris, Jerome, et al. “Kava: A Comprehensive Review of Efficacy, Safety, and Psychopharmacology.” Australian & New Zealand Journal of Psychiatry, vol. 45, no. 1, 1 Jan. 2011, pp. 27–35, https://doi.org/10.3109/00048674.2010.522554.
Contributed by Vincent Gao, Pharm D candidate