Lyrica (pregabalin)
Medication Class: anticonvulsant, analgesic
Manufacturer: Pfizer Inc.
FDA Approval date: December 2004

What is Lyrica and its mechanism of action?

Lyrica is a synthetic form of gamma-aminobutyric acid (GABA). GABA is a chemical messenger that transmits inhibitory signals in the brain. GABA reduces the transmission of nerve impulses and calms excitable nerve cells in the nervous system. The exact mechanism of action of Lyrica in the treatment of neuropathy and seizures is unknown. Lyrica binds to calcium channels in the CNS (central nervous system) tissues reducing the release of neurotransmitters (chemical messengers) between nerves. Blocking the release of neurotransmitters may reduce the sensation of pain caused by neuropathic pain and help control seizure episodes.

What is Lyrica used for treating?

Lyrica is FDA approved for treating the following conditions:

• Management of diabetic neuropathic pain
• Neuropathic pain associated with spinal cord injury
• Fibromyalgia
• Postherpetic neuralgia (nerve pain due to damage from shingles) 
• Partial onset seizures

The American Academy of Neurology (AAN) recommends Lyrica as the preferred treatment for diabetic neuropathy.

Lyrica is the first drug approved by the FDA for the treatment of fibromyalgia.

Lyrica is also used for generalized anxiety disorder (GAD), but this is not an FDA approved indication the for Lyrica.

How effective is Lyrica?

Neuropathic pain (nerve pain) (diabetes-associated)

Lyrica 25 mg, 100 mg and 200 mg three times a day were compared to a placebo in patients with neuropathic pain (nerve pain). After 5 weeks of treatment Lyrica 100 mg or 200 mg, reduced pain scores better than placebo and more patients had at least 50% or greater improvement in pain when compared to placebo. There was no significant difference in efficacy between the Lyrica 100 mg and Lyrica 200 mg.

Postherpetic neuralgia (shingles-associated)

Lyrica 100 mg and 200 mg three times a day were compared to placebo in patients with neuralgia persisting for at least 3 months following healing of herpes zoster rash. Patients also experienced pain levels of at least ≥4 on a numerical pain rating scale ranging from 0 (no pain) to 10 (worst possible pain). After an 8-week treatment period there was a significantly better reduction in the levels of pain and more patients had at least a 50% reduction in pain compared to placebo.

Interesting Facts about Lyrica

• Lyrica is a schedule V controlled substance because.
• Lyrica is used as an add-on medication to help in the treatment of seizures.
• When discontinuing Lyrica, patients must taper the dose gradually over a minimum of 1 week. 

What are side effects of Lyrica?

Some common side effects of Lyrica include:

• dizziness
• blurred eyesight 
• weight gain
• feeling sleepy
• not able to focus
• headache
• dry mouth
• fatigue
• constipation
• increase in appetite

Some serious side effects include:

• hypersensitivity reactions
• increased creatine kinase levels
• suicidal thoughts 
• angioedema

What is the dosage of Lyrica?

Lyrica can be taken without regard to meals. It is available in 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg and 300 mg oral capsules.

Lyrica is also available as a 20 mg/ml oral Solution.

Lyrica dosage differs based on the indication. The following are the dosages for each indication:

Neuropathic pain associated with diabetic peripheral neuropathy: Start with 50 mg taken 3 times daily and may increase to the maximum dosage of 100 mg taken 3 times daily. 

Neuropathic pain associated with spinal cord injury: The starting dose is 75 mg two times a day (150 mg/day). The dose may be increased to 150 mg two times a day (300 mg/day) within 1 week. The dose may be increased up to 300 mg two times a day (600 mg/day) after 2 to 3 weeks.

Postherpetic neuralgia (shingles-associated): Start dosing at 75 mg two times a day, or 50 mg three times a day (150 mg/day). The dose may be increased to 300 mg/day within 1 week based on efficacy and tolerability. The maximum dose is 600 mg/day.

Fibromyalgia: The recommended dose for fibromyalgia is 300 to 450 mg/day. Start dosing at 75 mg two times a day (150 mg/day). Increase the dose to 150 mg two times a day (300 mg/day) within 1 week if needed. The dose may be may be increased to 225 mg two times a day (450 mg/day) if needed.

Partial-onset seizures (adjunctive therapy): Start with 75 g twice daily or 50 mg taken 3 times daily and may increase to100 mg taken 3 times daily based on tolerability and as needed. The maximum dose is 600 mg daily.

What are Lyrica drug interactions?

Lyrica may increase the effect of buprenorphine, clobazam, droperidol, fentanyl, hydrocodone, methotrimeprazine, sodium oxybate, SSRIs, suvorexant, tapentadol, thalidomide, and zolpidem on brain function.

What are warnings and precautions for Lyrica?

Some contraindications, warnings, and precautions for Lyrica include:

• Lyrica may increase the risk of suicidal behavior or thoughts, therefore monitoring behavior of patients are important.
• Lyrica is linked to angioedema. It must be discontinued immediately if symptoms develop.
• Lyrica may cause dizziness and drowsiness. Operating machinery or other dangerous tasks should be avoided when taking Lyrica.
• Lyrica must be discontinued slowly over a week because abrupt discontinuation of may cause seizures.
• Patients with poor kidney function require a dose a dose adjustment.
• Rhabdomyolysis (muscle breakdown) can occur when taking Lyrica. Patients should report muscle pain.
• Lyrica may cause heart problems in patients with a history of heart failure or heart problems.

Pregnancy: Lyrica may harm the fetus. 

Nursing: It is not known if Lyrica is excreted in human milk. Breastfeeding is not recommended.

What is the cost of Lyrica?

The average wholesale price of a bottle of 90 capsules of Lyrica 25 mg to 300 mg is about $474. One tablet cost about $5.27. The average wholesale price of Lyrica oral solution 20 mg per mL (473 mL) is about $663.

How to obtain prescription assistance for Lyrica?

A Lyrica Co-pay Savings Card is available for prescription assistance. 

References

Lyrica Prescribing Information (package insert)