Pregabalin is an anticonvulsant and analgesic medication closely related to gabapentin, developed in the 1990s and marketed under the brand name Lyrica. It is a structural analogue of GABA but does not bind to GABA receptors. Its primary action is binding with high affinity to the α2δ subunit of voltage-gated calcium channels in the central nervous system. By reducing calcium influx into presynaptic neurons, pregabalin decreases the release of excitatory neurotransmitters including glutamate, norepinephrine, and substance P. This stabilises neuronal hyperexcitability and dampens pain signalling.
Pregabalin has greater bioavailability and more predictable pharmacokinetics than gabapentin. Oral bioavailability is ≥90% across therapeutic doses, and peak plasma levels occur about 1 hour after administration. Unlike gabapentin, absorption is not saturable. Pregabalin is not metabolised in the liver and is excreted unchanged in urine, meaning kidney function is the main determinant of clearance. Its half-life is about 6 hours, requiring twice or three times daily dosing depending on indication.
Approved worldwide, pregabalin is indicated for neuropathic pain, epilepsy, and generalised anxiety disorder (in Europe, not the US). It is widely used for fibromyalgia and is considered by many guidelines as first-line for neuropathic pain syndromes. Due to reports of misuse and dependence, pregabalin is controlled in the UK (Schedule 3) and many other jurisdictions, though it remains a valuable therapy when prescribed judiciously.
Pregabalin should be tapered gradually over at least 1 week when discontinuing to avoid withdrawal symptoms such as anxiety, insomnia, nausea, and pain rebound.
Most side effects are dose-related and improve with dose adjustment. Slow titration reduces risk. Patients should be counselled to report mood changes, swelling, breathing difficulties, or vision problems promptly.
Patients should be informed about the potential for weight gain and swelling, and clinicians may monitor renal function periodically.
Pregabalin has fewer pharmacokinetic interactions than most antiepileptics, but several important interactions exist:
Pregabalin does not significantly interact with the cytochrome P450 system, so it does not alter levels of most common drugs (e.g., statins, anticoagulants, antibiotics). However, clinical vigilance is still required, especially in polypharmacy.
Overdose: Symptoms include profound drowsiness, agitation, confusion, restlessness, double vision, slurred speech, and, in severe cases, coma. Fatal outcomes are rare but have occurred particularly with co-ingestion of CNS depressants. Treatment is supportive; haemodialysis effectively removes pregabalin in renal impairment.
Accidental double dose: May cause transient dizziness, drowsiness, or confusion. Patients should rest, avoid hazardous tasks, and contact a clinician if symptoms are severe.
Missed dose: Take as soon as remembered unless close to the next scheduled dose. If so, skip the missed dose. Do not double up doses. Consistency is important for effectiveness in pain and seizure control.
When travelling internationally, check pregabalin’s controlled status in the destination country. Carry it in original packaging with a copy of the prescription.
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