What is Lyrica (pregabalin) used for?

Lyrica (Pregabalin) Uses and Indications

Lyrica (pregabalin) is primarily used for treating neuropathic pain conditions, including diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia, and neuropathic pain associated with spinal cord injury, as well as serving as adjunctive therapy for partial-onset seizures in patients 17 years and older. 1

Primary FDA-Approved Indications

Pregabalin is officially indicated for:

• Management of neuropathic pain associated with diabetic peripheral neuropathy
• Management of postherpetic neuralgia
• Management of fibromyalgia
• Management of neuropathic pain associated with spinal cord injury
• Adjunctive therapy for partial-onset seizures in patients 17 years of age and older 1

Mechanism of Action

Pregabalin works by binding to the alpha-2-delta (α2δ) subunit of voltage-gated calcium channels in the central nervous system. This binding:

• Inhibits calcium influx at nerve terminals
• Reduces the release of excitatory neurotransmitters involved in pain signaling
• Decreases neuronal hyperexcitability that contributes to both pain and seizures 2

Unlike many other pain medications, pregabalin:

• Does not bind to GABA receptors
• Does not affect GABA uptake or metabolism
• Is not converted to GABA or a GABA agonist

Efficacy in Neuropathic Pain Conditions

Diabetic Peripheral Neuropathy

Pregabalin has demonstrated significant efficacy in treating painful diabetic neuropathy:

• Doses of 150-600 mg/day (in divided doses) are recommended
• Number needed to treat (NNT) of 4.04 for 600 mg/day and 5.99 for 300 mg/day 2

Postherpetic Neuralgia

For postherpetic neuralgia, pregabalin has shown:

• NNT of 4.93 for clinically meaningful pain reduction
• May be considered if patients have inadequate response to gabapentin 2

Fibromyalgia

Pregabalin is one of the few medications specifically approved for fibromyalgia:

• Effective at reducing pain intensity compared to placebo
• NNT of 6-9 for meaningful pain relief 2

Advantages of Pregabalin

Pregabalin offers several pharmacokinetic advantages:

• Rapid and almost complete absorption (90% bioavailability)
• Linear pharmacokinetics
• No protein binding
• No significant drug interactions (lacks hepatic metabolism)
• No enzyme induction 3

Common Side Effects

The most common adverse effects include:

• Dizziness
• Somnolence
• Peripheral edema
• Headache
• Weight gain
• Ataxia
• Diplopia 2, 3

Dosing Considerations

Dosing must be adjusted based on:

• Renal function (pregabalin is eliminated primarily unchanged through the kidneys)
• Specific indication being treated
• Patient tolerance of side effects

Starting with lower doses and titrating upward can help minimize adverse effects. For neuropathic pain associated with diabetic peripheral neuropathy, the starting dosage is typically 50 mg three times daily, which may be increased to 300 mg daily within one week based on efficacy and tolerability 4.

Important Clinical Considerations

1. Pregabalin is classified as a Schedule V controlled substance due to potential for abuse and dependence
2. It should not be discontinued abruptly due to risk of withdrawal symptoms
3. It may cause swelling of hands, legs, and feet, which can be problematic for patients with heart conditions
4. Pregabalin can cause dizziness and sleepiness that may impair driving and operation of machinery

When to Consider Pregabalin

Pregabalin is often considered a first-line treatment for:

• Neuropathic pain conditions, particularly diabetic neuropathy and postherpetic neuralgia
• Fibromyalgia when other treatments have failed
• As adjunctive therapy for partial seizures

For neuropathic pain, pregabalin and gabapentin are considered first-line anticonvulsants, preferred over older generation agents due to better tolerability and more predictable pharmacokinetics 2.