pregabalin

Pregabalin is an anticonvulsant (antiepileptic) and a pain-relieving (analgesic) medication. Pregabalin is used to treat seizures and for nerve pain (neuralgia) associated with neurological disorders that include diabetic neuropathy, postherpetic neuralgia and fibromyalgia. Pregabalin prevents seizures and neuralgia by blocking the transmission of electrical signals in the brain.

Pregabalin works by binding to a subunit of the calcium channels in nerve cells (neurons) and preventing the inflow of calcium ions. Blockage of calcium influx into the neurons prevents the conduction of electrical impulses by excitatory neurotransmitters such as glutamate and norepinephrine, and reduces the transmission of pain signals and/or seizure activity in the brain.

Pregabalin is used to treat the following conditions:

• Diabetic peripheral neuropathic pain
• Postherpetic neuralgia, a complication of shingles
• Fibromyalgia, a condition of heightened pain sensitivity and abnormal pain processing
• Neuropathic pain with spinal cord injuries
• Adult and pediatric partial onset seizure, a type of seizure that starts with abnormal electrical activity in one part of the brain

• Do not take pregabalin if you are hypersensitive to pregabalin or any of its components.
• Pregabalin may impair the ability to drive or perform hazardous tasks.
• Antiepileptic drugs increase the risk of suicidal thoughts or behavior in patients taking these drugs.
• Use with caution in cardiovascular disease (heart failure) and renal impairment.
• May cause prolongation of PR interval.
• Muscle wasting (rhabdomyolysis) may occur.
• Pregabalin may potentiate the effects of other sedatives.

Common side effects of pregabalin include:

• Dizziness
• Drowsiness (somnolence)
• Vertigo
• Headache
• Balance disorder
• Constipation
• Nausea
• Joint swelling
• Inflammation of nose and throat (nasopharyngitis)
• Increase in liver enzymes ALT and AST
• Diarrhea
• Peripheral edema
• Difficulty with balance, coordination and speech (ataxia)
• Fatigue
• Dry mouth (xerostomia)
• Weight gain
• Tremor
• Blurred vision
• Double vision (diplopia)
• Lack of energy (asthenia)
• Swelling (edema)
• Facial edema
• Low blood pressure (hypotension)
• Nerve damage (neuropathy)
• Pain
• Disorientation
• Accidental injury
• Abnormal thinking
• Confusion
• Memory loss (amnesia) and difficulty concentrating

Less common side effects of pregabalin include

• Addiction
• Anemia
• Breast enlargement in males (gynecomastia) and females
• Inflammation of epididymis, the coiled tube in the testicle that carries the sperm (epididymitis)
• Inflammation of the esophagus (esophagitis)
• Menstrual cramps (dysmenorrhea)
• Involuntary muscle contractions (dystonia)
• Heart failure
• Abnormal male-pattern hair growth in women (hirsutism)
• Inflammation of uvea, a layer in the eye (uveitis)

Postmarketing reports

• Swelling in the tissue under the skin or mucous membranes (angioedema)
• Suicidal behavior and ideation
• Abnormal creatinine kinase
• Decreased platelet count
• Pneumonia
• Viral infection
• Skin reaction with blistering, hives and itching (bullous pemphigoid)
• Respiratory depression

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

Capsule: Schedule V

• 25mg
• 50mg
• 75mg
• 100mg
• 150mg
• 200mg
• 225mg
• 300mg

Oral solution: Schedule V

• 20mg/mL

Extended-release tablet: Schedule V

• 82.5 mg
• 165 mg
• 330 mg

Adult

Diabetic Peripheral Neuropathic Pain

Regular release capsules

• Initial: 50 mg orally every 8 hours
• Maintenance: May increase to 100 mg orally every 8 hours within 1 week, as needed; not to exceed 300 mg/day

Extended-release tablets

• Initial: 165 mg orally once a day
• Maintenance: May increase to 330 mg orally once a day within 1 week based on response and tolerability; not to exceed 330 mg orally once a day

Postherpetic Neuralgia

• Regular release capsules
• Initial: 150-300 mg/day orally divided every 8-12 hours
• Maintenance: May increase to 300 mg/day divided every 8-12 hours after 1 week, as needed

Extended-release tablets

• Initial: 165 mg orally once a day
• Maintenance: May increase to 330 mg orally once a day within 1 week based on response and tolerability; not to exceed 330 mg orally once a day
• Patients experiencing insufficient pain relief following 2-4 weeks of treatment with 330 mg orally once a day and tolerating the ER tablets, may be treated with up to 660 mg orally once a day

Fibromyalgia

• Regular-release capsules and oral solution only
• Adult, Initial: 150 mg/day orally divided every 12 hours
• Adult, Maintenance: May increase to 300-450 mg/day divided every 12 hours after 1 week, as needed

Partial onset seizures

• Initial: 150 mg/day divided every 8-12 hours orally
• Maintenance: May increase to 600 mg/day orally divided every 8-12 hours, as needed

Neuropathic Pain With Spinal Cord Injury

• Initial: 150 mg/day orally divided every 12 hours; may increase within 1 week to 300 mg/day orally divided every 12 hours
• If there is insufficient pain relief after 2-3 weeks and 300 mg/day dose is tolerated, may increase the dose again up to 600 mg/day orally divided every 12 hours

Dosage Modifications

• Renal impairment (CrCl 30-60 mL/min)
• Decrease dose by 50% divided two to three times daily

Renal impairment (CrCl 15-30 mL/min)

• If 150 mg/day in normal renal function: Decrease dose to 25-50 mg/day; administer once/day or divided twice daily
• If 300 mg/day in normal renal function: Decrease dose to 75 mg/day; administer once/day or divided twice daily
• If 450 mg/day in normal renal function: Decrease dose to 100-150 mg/day; administer once/day or divided twice daily
• If 600 mg/day in normal renal function: Decrease dose to 150 mg/day; administer once/day or divided twice daily

Renal impairment (CrCl less than 15 mL/min)

• If 150 mg/day in normal renal function: Decrease dose to 25 mg/day; single daily dose
• If 300 mg/day in normal renal function: Decrease dose to 25-50 mg/day; single daily dose
• If 450 mg/day in normal renal function: Decrease dose to 50-75 mg/day; single daily dose or divided twice daily
• If 600 mg/day in normal renal function: Decrease dose to 75 mg/day; single daily dose

Renal impairment (supplemental dosage following hemodialysis)

• 25 mg once/day regimen: Take 1 supplemental dose of 25 mg or 50 mg
• 25-50 mg once/day regimen: Take 1 supplemental dose of 50 mg or 75 mg
• 50-75 mg once/day regimen: Take 1 supplemental dose of 75 mg or 100 mg
• 75 mg once/day regimen: Take 1 supplemental dose of 100 mg or 150 mg

Conversion from capsules or oral solution (Lyrica) to ER tablets (Lyrica CR)

• Lyrica total daily dose (TDD) 75 mg/day = Lyrica CR 82.5 mg/day
• Lyrica TDD 150 mg/day = Lyrica CR 165 mg/day
• Lyrica TDD 225 mg/day = Lyrica CR 247.5 mg/day
• Lyrica TDD 300 mg/day = Lyrica CR 330 mg/day (3 × 82.5 mg tablets)
• Lyrica TDD 450 mg/day = Lyrica CR 495 mg/day (3 × 165 mg tablets)
• Lyrica TDD 600 mg/day = Lyrica CR 660 mg/day (2 × 330 mg tablets)

Pediatric

Partial Onset Seizures

Regular-release capsules and oral solution only

• Children below 1 month: Safety and efficacy not established
• Children from 1 month up to 17 years of age:
• Children of weight 11 kg up to 30 kg
• Initial: 3.5 mg/kg/day orally divided every 8 hours (for 1 month to 4 years) or every 8-12 hours (for children of 4 years or more)
• Maintenance: Based on clinical response and tolerability, may increase dose in weekly increments, not to exceed 14 mg/kg/day
• Children of weight 30 kg and above
• Initial: 2.5 mg/kg/day orally divided every 8-12 hours
• Maintenance: Based on clinical response and tolerability, may increase dose in weekly increments up to 10 mg/kg/day (not to exceed 600 mg/day)

Children above 17 years of age:

• Initial: 150 mg/day orally divided every 8-12 hours
• Maintenance: Based on clinical response and tolerability, may increase dose in weekly increments, not to exceed 600 mg/day

Fibromyalgia

• Safety and efficacy not established
• A 15-week, placebo-controlled trial (n=107) was conducted in pediatric patients with fibromyalgia aged 12-17 years with pregabalin (75-450 mg/day)
• The primary efficacy endpoint of change from baseline to Week 15 in mean pain intensity (derived from an 11-point numeric rating scale) showed numerically greater improvement for the pregabalin-treated patients compared to placebo-treated patients but did not reach statistical significance

• Renal impairment: Use in children with compromised renal function has not been studied

• Along with its benefits, this medication may very rarely cause abnormal drug-seeking behavior (addiction). This risk may be increased if you have abused alcohol or drugs in the past. Take this medication exactly as prescribed to lessen the risk of addiction.
• Monitor for physical dependence and withdrawal symptoms.
• In case of overdose, get medical help or contact a Poison Control Center immediately.

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

Pregabalin has no known severe interactions with other drugs.

• Benazepril
• Captopril
• Enalapril
• Everolimus
• Fosinopril
• Imidapril
• Lisinopril
• Perindopril
• Quinapril
• Ramipril
• Sirolimus

• Clobazam
• Deutetrabenazine
• Lurasidone
• Orlistat

Pregabalin has no known mild interactions with other drugs.

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

• Use pregabalin with caution during pregnancy if benefits outweigh risks. Animal studies show risk and there are no adequate and well-controlled studies with pregabalin in pregnant women.
• Small amounts of pregabalin have been detected in the milk of lactating women; it is not recommended for use while breastfeeding.

• Do not discontinue anticonvulsants abruptly because that may increase seizure frequency. Discontinue gradually at least over a week.
• Discontinue if hypersensitivity or angioedema occurs and institute appropriate therapy immediately.