Lyrica: Targeted Neuropathic Pain Relief with Pregabalin
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Synonyms | |||
Lyrica (pregabalin) is a prescription medication specifically formulated for the management of neuropathic pain, a complex condition arising from damaged or dysfunctional nerves. As a potent anticonvulsant and anxiolytic agent, its primary mechanism of action involves binding to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system. This binding modulates the release of several neurotransmitters, including glutamate, norepinephrine, and substance P, resulting in a reduction of neuronal excitability. Clinically, this translates to a significant decrease in pain signals and seizure activity, offering a targeted therapeutic approach for various neurological disorders. It is a cornerstone in the pharmacological management of chronic pain conditions where first-line treatments have proven insufficient or intolerable.
Features
- Active Pharmaceutical Ingredient (API): Pregabalin.
- Pharmacological Class: Gabapentinoid; Anticonvulsant.
- Available Formulations: Oral capsules (25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, 300 mg) and an oral solution (20 mg/mL).
- Mechanism of Action: Binds potently to the alpha2-delta subunit of voltage-gated calcium channels, reducing the release of excitatory neurotransmitters.
- Bioavailability: Greater than 90% and independent of food intake.
- Half-life: Approximately 6.3 hours in individuals with normal renal function.
- Primary Excretion: Renal, predominantly as unchanged drug.
Benefits
- Provides significant reduction in pain scores for diabetic peripheral neuropathy and postherpetic neuralgia, improving overall quality of life.
- Effective as adjunctive therapy for managing partial-onset seizures in adults, reducing seizure frequency.
- Offers a non-opioid, non-NSAID option for chronic pain management, mitigating risks associated with those drug classes.
- Demonstrated efficacy in managing fibromyalgia, reducing widespread pain and improving sleep quality and physical function.
- Approved for the management of neuropathic pain associated with spinal cord injury.
- Can be effective in treating generalized anxiety disorder (GAD) in some regions, though not a universal indication.
Common use
Lyrica is FDA-approved for the treatment of multiple specific conditions. Its most prominent use is in the management of neuropathic pain, including diabetic peripheral neuropathy, a burning or shooting pain in the extremities caused by nerve damage from diabetes, and postherpetic neuralgia, the persistent nerve pain that can follow a shingles (herpes zoster) outbreak. It is also a well-established adjunctive therapy for adults with partial-onset seizures, meaning it is used alongside other antiepileptic drugs to achieve better seizure control. Furthermore, it is indicated for the management of fibromyalgia, a chronic disorder characterized by widespread musculoskeletal pain, fatigue, and tenderness. An additional approved use is for the treatment of neuropathic pain associated with spinal cord injury. Off-label, it is sometimes used for other types of chronic pain and certain anxiety disorders, though such use should be strictly supervised by a physician.
Dosage and direction
Dosage must be individualized based on renal function and therapeutic response. The drug is administered orally, with or without food.
- Neuropathic Pain (Diabetic Peripheral Neuropathy/Postherpetic Neuralgia): The starting dose is 150 mg/day, administered in two or three divided doses (e.g., 75 mg twice daily or 50 mg three times daily). Based on efficacy and tolerability, the dose may be increased to 300 mg/day within one week. If needed, and if tolerated, the dose can be further increased to a maximum of 600 mg/day after 2–4 weeks.
- Adjunctive Therapy for Partial-Onset Seizures: The starting dose is 150 mg/day, given in two or three divided doses. The dose may be increased to a maximum of 600 mg/day based on clinical response.
- Fibromyalgia: The starting dose is 150 mg/day (75 mg twice daily). The dose should be increased to 300 mg/day within one week, based on patient response and tolerability. Patients who do not experience sufficient benefit may be further increased to 450 mg/day, and if needed, to a maximum of 600 mg/day.
- Neuropathic Pain Associated with Spinal Cord Injury: The recommended starting dose is 150 mg/day (75 mg twice daily). The dose may be increased to 300 mg/day after one week. Based on response and tolerability, the dose may be further increased to a maximum of 600 mg/day.
Renal Impairment: Dosage must be adjusted for patients with reduced creatinine clearance. Please refer to the full prescribing information for detailed dosing tables. Abrupt discontinuation should be avoided; the dose should be tapered gradually over a minimum of one week.
Precautions
Patients should be closely monitored for the emergence or worsening of depression, suicidal thoughts or behavior, or any unusual changes in mood or behavior. Lyrica may cause dizziness and somnolence, which could impair the ability to perform potentially hazardous activities such as driving or operating complex machinery. Patients should be advised not to drive until they have sufficient experience to gauge whether Lyrica impairs their abilities. Concurrent use with other central nervous system (CNS) depressants (e.g., opioids, benzodiazepines, alcohol) may potentiate these effects. There is a potential for weight gain and peripheral edema; caution is advised in patients with a history of congestive heart failure. Lyrica may cause blurry vision or other visual disturbances. Patients with a history of angioedema should be monitored closely. Routine monitoring of creatine kinase levels is recommended in patients treated for fibromyalgia.
Contraindications
Lyrica is contraindicated in patients with a known hypersensitivity to pregabalin or any of the excipients in the formulation. Hypersensitivity reactions have included cases of angioedema.
Possible side effect
The most common adverse reactions observed in controlled clinical trials are CNS-related and dose-dependent.
- Very Common (≥1/10): Dizziness, somnolence (sleepiness).
- Common (≥1/100 to <1/10): Dry mouth, blurred vision, diplopia (double vision), disturbance in attention, euphoric mood, weight gain, peripheral edema, constipation, vomiting, flatulence, erectile dysfunction, fatigue, balance disorder, headache, tremor, nystagmus.
- Uncommon (≥1/1,000 to <1/100): Loss of consciousness, confusion, disorientation, insomnia, irritability, decreased libido, myalgia, arthralgia, nephrolithiasis, hypoglycemia, thrombocytopenia.
- Rare but Serious: Angioedema, hypersensitivity reactions (e.g., skin redness, blisters, hives, wheezing), rhabdomyolysis, suicial ideation and behavior, severe dizziness and balance problems leading to falls.
Drug interaction
Lyrica has a low potential for pharmacokinetic drug interactions as it is not metabolized in the liver and does not inhibit or induce major CYP450 enzymes. It is eliminated renally largely unchanged. However, pharmacodynamic interactions are significant.
- CNS Depressants: Concomitant use with opioids (e.g., oxycodone), benzodiazepines (e.g., lorazepam), barbiturates, or alcohol may potentiate effects on cognitive and motor function, increasing the risk of severe dizziness, somnolence, and respiratory depression. Dose adjustments may be necessary.
- Angiotensin-Converting Enzyme (ACE) Inhibitors: Concomitant use has been associated with a higher risk of developing angioedema.
- Thiazolidinedione Antidiabetic Agents (e.g., pioglitazone): Co-administration may lead to an increased risk of weight gain and peripheral edema.
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. The patient should not take a double dose to make up for the missed one. Maintaining a consistent dosing schedule is important for stable therapeutic effects.
Overdose
There is no specific antidote for pregabalin overdose. Standard supportive measures should be employed as required. Overdose symptoms are expected to be an exaggeration of the drug’s adverse effects, including severe somnolence, profound sedation, confusion, restlessness, agitation, and depression. In massive overdose, coma and respiratory depression are possible. Hemodialysis significantly removes pregabalin from the blood (approximately 50% removal over 4 hours) and should be considered in cases of life-threatening overdose, especially in patients with renal impairment.
Storage
Lyrica capsules and oral solution should be stored at room temperature, between 20°C to 25°C (68°F to 77°F), with excursions 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. Do not use after the expiration date printed on the packaging. The oral solution can be stored for up to 45 days after first opening the bottle.
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 before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from publicly available sources but may not be comprehensive or fully up-to-date.
Reviews
Clinical trials and post-marketing surveillance demonstrate that Lyrica (pregabalin) is generally well-tolerated and effective for its approved indications when used appropriately. Many patients with refractory neuropathic pain report a meaningful reduction in pain intensity and an associated improvement in sleep and daily functioning. However, the side effect profile, particularly dizziness, somnolence, and cognitive blunting, is a significant consideration and a common reason for discontinuation in some patients. The potential for weight gain can also be a limiting factor for long-term use. Efficacy is highly individual, and a period of dose titration is almost always required to find the optimal balance between therapeutic benefit and adverse effects. Patient reviews in real-world settings often reflect this dichotomy, highlighting its life-changing pain relief for some, while others cite intolerable side effects. Consistent themes in expert reviews underscore its value as a non-opioid analgesic but emphasize the necessity of careful patient selection, thorough education on side effects, and vigilant monitoring, especially during the initiation and titration phases.