Drug intelligence / Profile preview

pregabalin

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Pregabalin is an anticonvulsant and analgesic small molecule medication used to treat neuropathic pain, fibromyalgia, and as adjunctive therapy for partial-onset seizures. It is a gabapentinoid structurally related to gamma-aminobutyric acid (GABA), but it does not act directly on GABA receptors. Instead, pregabalin binds with high affinity to the α2δ subunit of voltage-gated calcium channels in the central nervous system. This binding reduces calcium influx at nerve terminals, thereby decreasing the release of several excitatory neurotransmitters such as glutamate, norepinephrine, serotonin, dopamine, substance P, and calcitonin gene-related peptide. The net effect is a reduction in neuronal excitability and abnormal pain signaling[1][2][4][5]. Pregabalin was developed by Pfizer and first approved for medical use in 2004[5]. Its primary indications include neuropathic pain associated with diabetic peripheral neuropathy or postherpetic neuralgia; fibromyalgia; neuropathic pain due to spinal cord injury; and as adjunctive therapy for partial-onset seizures[1][2].

Brand names
LyricaLyrica CR
Other names
pragaPrega 75mg CapsulePrega75mg CapsulePrega-75mg CapsulePregabalin-AFT
02

Targets

CACNA2D2 (α2δ-2)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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