Pregabalin
Pregabalin is an oral gabapentinoid used in adults for neuropathic pain, generalised anxiety disorder, fibromyalgia (in some markets) and as adjunctive therapy for partial-onset seizures. It binds the alpha-2-delta subunit of voltage-gated calcium channels.
- Chemical formula
- C8H17NO2
- CAS number
- 148553-50-8
- ATC code
- N03AX16
- Molecular weight
- 159.23 g/mol
- Drug class
- Gabapentinoid (alpha-2-delta ligand)
- Also known as
- CI-1008, Pregabalina
What is it?
Pregabalin is a structural analogue of gamma-aminobutyric acid (GABA) and a successor to gabapentin, with improved pharmacokinetics. It was approved in 2004 and is supplied as oral capsules, oral solution and extended-release tablets. Pregabalin is dispensed only on prescription and is classified as a controlled substance in some jurisdictions because of its abuse and dependence potential.
Mechanism of action
Pregabalin binds the alpha-2-delta auxiliary subunit of voltage-gated calcium channels in the central nervous system, reducing presynaptic calcium influx and the release of excitatory neurotransmitters such as glutamate, noradrenaline and substance P. Despite its structural similarity to GABA, it does not bind GABA receptors. The result is anticonvulsant, anxiolytic and analgesic effects, particularly in neuropathic pain pathways.
Pharmacokinetics
Pregabalin is rapidly and almost completely absorbed orally, with bioavailability greater than 90% — substantially higher than gabapentin, which is non-linear. Plasma protein binding is negligible. The drug is excreted predominantly unchanged in urine, and renal impairment requires substantial dose reduction. The terminal half-life is approximately six hours, supporting two or three daily doses. Linear pharmacokinetics simplify dose adjustment.
Indications
Pregabalin is approved in adults for neuropathic pain associated with diabetic peripheral neuropathy, post-herpetic neuralgia, spinal cord injury and other forms of central neuropathic pain (some markets), for generalised anxiety disorder, for fibromyalgia (in the United States and some other markets) and as adjunctive therapy for partial-onset seizures. According to international guidelines, pregabalin is one of the recommended first-line agents in neuropathic pain.
Safety profile
Common adverse effects include drowsiness, dizziness, peripheral oedema, weight gain, dry mouth and blurred vision. Pregabalin can impair driving and cognitive function, particularly during initiation. Tolerance, physical dependence and abuse have been reported, especially in patients with substance use disorders. According to regulatory communications, pregabalin combined with opioids increases the risk of respiratory depression. Renal impairment requires substantial dose reduction.
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Frequently asked questions
How is pregabalin different from gabapentin? ▾
Both bind the alpha-2-delta calcium channel subunit and are used in similar indications, but pregabalin has linear pharmacokinetics and higher bioavailability than gabapentin, which has saturable absorption at higher doses. As a result, pregabalin reaches effective plasma levels more reliably and at lower doses, although clinical efficacy in neuropathic pain at adequate doses is broadly comparable. According to international guidelines, the choice is made by the prescriber.
Is pregabalin addictive? ▾
Pregabalin has been associated with tolerance, physical dependence and abuse, especially in patients with previous substance use disorders. It is a controlled substance in some jurisdictions. Withdrawal symptoms can include anxiety, insomnia, sweating and gastrointestinal symptoms after abrupt discontinuation. According to the prescribing information, the medication should be tapered gradually, particularly after long-term use, and the medical history must be reviewed before any prescription.
Why must the dose be reduced in kidney disease? ▾
Pregabalin is excreted predominantly unchanged in urine, so renal impairment substantially increases plasma concentrations and the risk of adverse effects, including sedation, ataxia and cognitive impairment. According to the prescribing information, the dose is reduced based on creatinine clearance, including in patients on dialysis where supplemental doses are given after sessions. Renal function should be assessed before treatment and periodically thereafter.
Does pregabalin cause weight gain? ▾
Weight gain is a common adverse effect of pregabalin, more pronounced at higher doses and with longer treatment. The mechanism is not fully understood and may relate to fluid retention and increased appetite. According to the prescribing information, weight should be monitored during treatment, and dose adjustment or alternative agents should be considered if weight gain becomes problematic, with the regimen tailored by the prescriber.
What are the main contraindications for pregabalin? ▾
Pregabalin is contraindicated in known hypersensitivity to pregabalin or its excipients. Caution is required in renal impairment (with mandatory dose adjustment), in concurrent CNS depressants including opioids and alcohol, in patients with previous substance use disorders, in suicidal ideation and during pregnancy and breastfeeding. According to the prescribing information, the medical history must be reviewed by a clinician before any prescription.
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