Pregabalin's abuse potential: a mini review focusing on the pharmacological profile.
Pregabalin, an analogue of the gamma-aminobutyric acid mammalian neurotransmitter and its structurally related compound gabapentin are known as α2δ ligands. They might act as inhibitory modulators of neuronal excitability that reduce ectopic neuronal activation of hyperexcited neurons while normal activation remains unchanged. However, the interaction with Ca²⁺ channel α2δ subunit is not sufficient to account for the broad clinical spectrum of pregabalin effects including the abuse potential. Pregabalin is approved for the treatment of partial epilepsy; generalized anxiety disorder; peripheral and central neuropathic pain and fibromyalgia. Its prescribing is rapidly increasing and total sales of the drug worldwide reached 4.6 billion US$ in 2012. Since entering widespread clinical use, reports of pregabalin abuse appeared more often, usually involving individuals with a history of abuse of other medications. The purpose of this mini review is to present available published data signaling pregabalin's abuse liability reflecting on the pharmacological characteristics that might enable this agent to trigger addictive behaviors.
Georgios
G
Papazisis
Dimitrios
D
Tzachanis
D000700:Analgesics / Q000009:adverse effects / Q000494:pharmacology*; D000818:Animals; D016739:Behavior, Addictive / Q000453:epidemiology; D006801:Humans; D009474:Neurons / Q000187:drug effects / Q000378:metabolism; D010818:Practice Patterns, Physicians' / Q000706:statistics & numerical data; D000069583:Pregabalin; D019966:Substance-Related Disorders / Q000453:epidemiology*; D005680:gamma-Aminobutyric Acid / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology
D000700:Analgesics; D000069583:Pregabalin; D005680:gamma-Aminobutyric Acid