pregabalin

Pregabalin is a prescription medication that belongs to the class of gabapentinoids. It is used to treat neuropathic pain conditions such as diabetic peripheral neuropathy and postherpetic neuralgia, and as an adjunctive therapy for partial-onset seizures. In some countries, it is also approved for other conditions such as fibromyalgia and generalized anxiety disorder.

The mechanism of action involves binding with high affinity to the alpha-2-delta subunit of presynaptic voltage-gated calcium channels in the central nervous system. This reduces the release of several neurotransmitters and helps to dampen neuronal excitability. Pregabalin does not directly activate GABA receptors, despite structural similarity to the neurotransmitter GABA.

Pharmacokinetics are favorable for clinical use. Pregabalin is taken orally and is rapidly absorbed with relatively high bioavailability. It exhibits linear pharmacokinetics and is eliminated primarily by the kidneys, with a half-life of about six hours. Because renal clearance is important, dose adjustments are recommended in individuals with impaired kidney function. It is not extensively bound to plasma proteins.

Common adverse effects include dizziness, somnolence, peripheral edema, weight gain, dry mouth, and blurred vision. There is potential for misuse and for withdrawal symptoms if therapy is stopped abruptly. Caution is advised with alcohol and other central nervous system depressants. Pregnancy is typically managed with caution due to limited safety data, and breastfeeding should be discussed with a clinician.

Regulatory status varies by country. Pregabalin is a prescription drug and is regulated as a controlled substance in some jurisdictions owing to concerns about abuse potential.