Lyrica (pregabalin) is a prescription medication indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, and as an adjunctive therapy for adult patients with partial-onset seizures. It is also approved for the management of fibromyalgia. As a Schedule V controlled substance, it works by binding to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, thereby modulating the release of several excitatory neurotransmitters. This mechanism of action is central to its efficacy in calming overactive nerve signals that cause chronic pain and reducing neuronal hyperexcitability involved in seizure activity. Proper diagnosis and a treatment plan supervised by a healthcare professional are essential for its safe and effective use.

Features

• Active Ingredient: Pregabalin.
• Pharmacologic Class: Gabapentinoid; Analog of gamma-aminobutyric acid (GABA).
• Available Strengths: 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, and 300 mg oral capsules; 20 mg/mL oral solution.
• Mechanism of Action: Binds potently to the alpha2-delta subunit of voltage-gated calcium channels, reducing the excessive release of neurotransmitters such as glutamate, norepinephrine, and substance P.
• Bioavailability: Greater than 90% and is independent of dose.
• Half-life: Approximately 6.3 hours.
• Excretion: Primarily renally excreted unchanged.

Benefits

• Provides significant reduction in the sharp, burning, and shooting pain characteristic of neuropathic conditions.
• Offers improved sleep quality and overall patient-reported outcomes in fibromyalgia management.
• Contributes to a reduction in seizure frequency when used concomitantly with other antiepileptic drugs.
• Demonstrates a rapid onset of action for pain relief, often within the first week of therapy at effective doses.
• May help alleviate anxiety symptoms associated with certain medical conditions due to its anxiolytic-like effects in clinical studies.

Common use

Lyrica is commonly prescribed for several FDA-approved conditions. Its primary use is for neuropathic pain, specifically diabetic peripheral neuropathy (nerve pain in the extremities caused by diabetes) and postherpetic neuralgia (persistent nerve pain following a shingles outbreak). It is a well-established therapy for fibromyalgia, helping to reduce widespread pain and improve function. In neurology, it is used as an adjunctive therapy for partial-onset seizures in adults, meaning it is added to a patient’s existing regimen of antiepileptic drugs to achieve better seizure control. It is also approved for the management of neuropathic pain associated with spinal cord injury. Off-label, it is sometimes used for generalized anxiety disorder and other chronic pain syndromes, though such use should be carefully considered by a specialist.

Dosage and direction

Dosage must be individualized according to the patient’s renal function and therapeutic response. The drug can be taken with or without food.

• Neuropathic Pain (DPN/PHN), Fibromyalgia: The recommended starting dose is 150 mg/day, given as 75 mg two times a day (75 mg BID). Based on efficacy and tolerability, the dose may be increased to 300 mg/day (150 mg BID) within one week. For patients who require additional pain relief, the dose may be increased to a maximum of 300 mg BID (600 mg/day).
• Adjunctive Therapy for Seizures: The starting dose is 150 mg/day, given as 75 mg BID. The dose may be increased to a maximum of 600 mg/day (300 mg BID) based on clinical response and tolerability.
• Renal Impairment: Dosage adjustment is critical for patients with reduced creatinine clearance. Dosing frequency and total daily dose must be reduced. Refer to the full prescribing information for specific dosing tables based on CrCl.
• Discontinuation: To minimize the potential for increased seizure frequency or withdrawal symptoms, Lyrica should be tapered gradually over a minimum of one week rather than discontinued abruptly.

Precautions

• Angioedema: Serious allergic reactions involving angioedema (swelling of the face, mouth, tongue, lips, and throat) have been reported. This requires immediate medical attention and discontinuation of the drug.
• Hypersensitivity Reactions: Discontinue Lyrica if a patient develops signs of hypersensitivity, including skin blistering, rash, or wheezing.
• Dizziness and Somnolence: Lyrica may cause significant dizziness and drowsiness, which could increase the risk of accidental injury. Patients should be cautioned about operating machinery, driving, or engaging in hazardous activities until they experience how the drug affects them.
• Peripheral Edema: Swelling of the extremities can occur and may be dose-related. Caution is advised in patients with pre-existing cardiac conditions or those taking drugs associated with edema (e.g., thiazolidinediones).
• Weight Gain: Weight gain has been observed and may be problematic for some patients, particularly those with diabetes or other comorbidities. Monitoring weight is recommended.
• Blurred Vision and Other Visual Effects: Patients may experience blurred vision or other visual changes. A baseline and periodic eye exams should be considered.
• Suicidal Thoughts and Behavior: Antiepileptic drugs, including Lyrica, increase the risk of suicidal thoughts or behavior. Patients should be monitored for the emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior.

Contraindications

Lyrica is contraindicated in patients with known hypersensitivity to pregabalin or any of its inactive components. Reactions have included cases of angioedema.

Possible side effect

The most common adverse reactions are central nervous system-related and are often dose-dependent.

• Very Common (>10%): Dizziness, somnolence (sleepiness), dry mouth, peripheral edema, blurred vision, weight gain, disturbances in attention.
• Common (1% to 10%): Euphoria, ataxia (loss of coordination), balance disorder, tremor, lethargy, diplopia (double vision), increased appetite, constipation, vomiting, flatulence, erectile dysfunction, feeling drunk, headache.
• Uncommon (0.1% to 1%): Syncope (fainting), hypotension, heart failure, myalgia, arthralgia, nephrolithiasis, neutropenia, thrombocytopenia, rhabdomyolysis.
• Rare (<0.1%): Rashes including Stevens-Johnson syndrome, toxic epidermal necrolysis, hepatitis, pancreatitis, anaphylaxis.

Drug interaction

• CNS Depressants: Additive effects on cognitive and motor function can occur when Lyrica is taken with other agents that cause dizziness or somnolence, such as opioids, benzodiazepines, barbiturates, alcohol, and sedating antihistamines. This significantly increases the risk of severe sedation, respiratory depression, and accidental injury.
• Angiotensin-Converting Enzyme (ACE) Inhibitors: Coadministration may increase the risk and severity of angioedema.
• Pioglitazone/Other Thiazolidinediones: May potentiate peripheral edema and weight gain.
• Other Antiepileptic Drugs (e.g., gabapentin): While often co-prescribed, the combined effects on the CNS must be carefully monitored.

Missed dose

If a dose is missed, it should be taken as soon as it is remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. The patient should not take a double dose to make up for a missed one.

Overdose

There is no specific antidote for pregabalin overdose. Signs of acute overdose may include severe drowsiness, lethargy, restlessness, agitation, confusion, depression, and seizures. In massive overdose, coma and respiratory depression are possible. General supportive measures should be instituted, including monitoring of vital signs and observation of the clinical status of the patient. Hemodialysis may be effective in removing pregabalin from the blood (removing approximately 50% of the drug over 4 hours) and should be considered in cases of life-threatening overdose.

Storage

Store Lyrica capsules and oral solution at room temperature, between 20°C to 25°C (68°F to 77°F). Excursions are permitted between 15°C and 30°C (59°F and 86°F). The medication must be kept in its original container, tightly closed, and out of reach of children and pets. Any unused medication should be disposed of properly via a drug take-back program.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The author does not recommend or endorse any specific tests, physicians, products, procedures, opinions, or other information that may be mentioned.

Reviews

• Clinical Efficacy (Neurology): “As an adjunctive therapy for refractory partial-onset seizures, pregabalin has demonstrated a statistically significant reduction in seizure frequency in multiple randomized, double-blind, placebo-controlled trials. Its predictable pharmacokinetics are a notable advantage in a polypharmacy setting.”
• Pain Management Perspective: “For postherpetic neuralgia and diabetic neuropathy, Lyrica is a first-line option. The number needed to treat (NNT) for substantial pain relief is favorable. However, the side effect profile, particularly dizziness and edema, requires careful patient selection and dose titration.”
• Patient Report (Fibromyalgia): “Many of my patients with fibromyalgia report a marked improvement in sleep quality and a reduction in the overall ‘pain burden,’ which significantly enhances their quality of life. The weight gain can be a limiting factor for long-term adherence.”
• Safety Review: “The potential for misuse and dependence, while lower than Schedule II substances, is real and necessitates that prescribers remain vigilant, especially in patients with a history of substance use disorder. The boxed warning for suicidal ideation is a critical component of the risk-benefit discussion.”