What is Pregabalin - Meaning and definition

Published by Roberto Wenk. Reviewed by Alison Ramsey. Last updated date: January 27, 2019.

A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anticonvulsant, anti-epileptic, anxiolytic, and analgesic activities.
Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished.
Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation.

National Cancer Institute. NCI Drug Dictionary. Internet. September 15, 2009.

Published by Roberto Wenk. Reviewed by Alison Ramsey. Last updated date: January 27, 2019.

Adult
PO
Adjunct in partial seizures. Initial: 150 mg/day, may increase to 300 mg/day after a wk. Max: 600 mg/day.
Anxiety. Initial: 150 mg/day, may increase in increments of 150 mg wkly. Max: 600 mg/day.
Neuropathic pain. Initial: 150 mg/day, may increase to 300 mg/day after 3-7 days. Max: 600 mg/day after a 7-day interval.
Fibromyalgia. Initial: 150 mg/day, may increase to 300 mg/day after a wk. Max: 450 mg/day, if needed. All doses to be given in 2 or 3 divided doses.

Adverse drug reactions: somnolence, dizziness, headache, blurred vision, vertigo, fatigue, irritability, arthralgia, muscle cramp, disorientation, insomnia, sedation, weight gain, confusion, reduced libido, attention, memory, coordination, gait disturbances.

Adapted from CIMS Drug Information System. Internet. Accessed on January 10, 2016.

Pregabalin

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