pregabalin (Rx)

Brand and Other Names:Lyrica, Lyrica CR
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule: Schedule V

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

oral solution: Schedule V

  • Lyrica
  • 20mg/mL

tablet, extended-release: Schedule V

  • Lyrica CR
  • 82.5 mg
  • 165 mg
  • 330 mg
more...

Diabetic Peripheral Neuropathic Pain

Regular-release capsules

  • Initial: 50 mg PO q8hr
  • Maintenance: May increase to 100 mg PO q8hr within 1 week, as needed; not to exceed 300 mg/day

Extended-release tablets

  • Initial: 165 mg PO qDay
  • Maintenance: May increase to 330 mg PO qDay within 1 week based on response and tolerability; not to exceed 330 mg PO qDay
  • See also Administration

Postherpetic Neuralgia

Regular-release capsules

  • Initial: 150-300 mg/day PO divided q8-12hr
  • Maintenance: May increase to 300 mg/day divided q8-12hr after 1 week, as needed

Extended-release tablets

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

Fibromyalgia

Regular-release capsules and oral solution only

Initial: 150 mg/day PO divided q12hr

Maintenance: May increase to 300-450 mg/day divided q12hr after 1 week, as needed

Partial Onset Seizures

Indicated as adjunctive therapy for treatment of partial onset seizures in adults aged ≥17 yr

Regular-release capsules and oral solution only

Initial: 150 mg/dday PO divided q8-12hr

Maintenance: Based on clinical response and tolerability, may increase dose in weekly increments, not to exceed 600 mg/day

Neuropathic Pain With Spinal Cord Injury

Regular-release capsules and oral solution only

Initial: 150 mg/day PO divided q12hr; may increase within 1 week to 300 mg/day PO divided q12hr

If there is insufficient pain relief after 2-3 weeks and 300 mg/day dose is tolerated, may increase dose again up to 600 mg/day PO divided q12hr

Dosage Modifications

Renal impairment (capsules/oral solution)

  • CrCl 30-60 mL/min
    • Decrease dose by 50% divided bid/tid
  • CrCl 15-30 mL/min
    • If 150 mg/day in normal renal function: Decrease dose to 25-50 mg/day; administer qDay or divided bid
    • If 300 mg/day in normal renal function: Decrease dose to 75 mg/day; administer qDay or divided bid
    • If 450 mg/day in normal renal function: Decrease dose to 100-150 mg/day; administer qDay or divided bid
    • If 600 mg/day in normal renal function: Decrease dose to 150 mg/day; administer qDay or divided bid
  • CrCl <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 of divided bid
    • If 600 mg/day in normal renal function: Decrease dose to 75 mg/day; single daily dose
  • Supplemental dosage following hemodialysis
    • 25 mg qDay regimen: Take 1 supplemental dose of 25 mg or 50 mg
    • 25-50 mg qDay regimen: Take 1 supplemental dose of 50 mg or 75 mg
    • 50-75 mg qDay regimen: Take 1 supplemental dose of 75 mg or 100 mg
    • 75 mg qDay regimen: Take 1 supplemental dose of 100 mg or 150 mg

Renal impairment (ER tablets)

  • CrCl 30-60 mL/min
    • If 165 mg/day in normal renal function: Decrease dose to 82.5 mg/day
    • If 330 mg/day in normal renal function: Decrease dose to 165 mg/day
    • If 495 mg/day in normal renal function: Decrease dose to 247.5 mg/day
    • If 660 mg/day in normal renal function: Decrease dose to 330 mg/day
  • CrCl <30 mL/min or hemodialysis
    • Not recommended
    • Patients should only receive capsules or oral solution

Dosing Considerations

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)

Dosage Forms & Strengths

capsule: Schedule V

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

oral solution: Schedule V

  • Lyrica
  • 20mg/mL
more...

Partial Onset Seizures

Indicated as adjunctive therapy for treatment of partial onset seizures in patients aged ≥4 yr

Regular-release capsules and oral solution only

11 kg to <30 kg

  • Initial: 3.5 mg/kg/day PO divided q8-12hr
  • Maintenance: Based on clinical response and tolerability, may increase dose in weekly increments, not to exceed 14 mg/kg/day

≥30 kg

  • Initial: 2.5 mg/kg/day PO divided q8-12hr
  • 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)

Aged ≥17 years

  • Initial: 150 mg/day PO divided q8-12hr
  • 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 yr 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

Dosage Modifications

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

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Interactions

Interaction Checker

and pregabalin

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Dose-dependent; percentages according to highest reported

            >10%

            Lyrica CR

            • Dizziness (3.4-17.1%)
            • Somnolence (0.5-11.4%)

            Lyrica

            • Dizziness (8-45%)
            • Somnolence (4-36%)
            • Peripheral edema (16%)
            • Ataxia (1-20%)
            • Fatigue (5-11%)
            • Xerostomia (1-15%)
            • Weight gain (16%)
            • Tremor (11%)
            • Blurred vision (1-12%)
            • Diplopia (12%)

            1-10%

            Lyrica CR

            • Vertigo (1-3.9%)
            • Headache (1.9-3.9%)
            • Vision blurred (0.5-3.7%)
            • Balance disorder (0.5-2.6%)
            • Weight increased (2.5-3.8%)
            • Fatigue (2.4-3.9%)
            • Constipation (2.7%)
            • Dry mouth (0.5-3.7%)
            • Nausea (3-3.4%)
            • Peripheral edema (3.8-4.9%)
            • Fatigue (1.4 -3.9%)
            • Joint swelling (1.9%)
            • Nasopharyngitis (1.4-1.5%)
            • ALT/AST increased (0.2-1.4%)
            • Diarrhea (1-1.4%)

            Lyrica

            • Asthenia (5%)
            • Edema (8%)
            • Facial edema (<3%)
            • Hypotension (2%)
            • Neuropathy (2-9%)
            • Pain (5%)
            • Disorientation (<2%)
            • Constipation (5%)
            • Weight gain (4%)
            • Accidental injury (4%)
            • Abnormal thinking (2%)
            • Confusion (<7%)
            • Amnesia (<6%)
            • Vertigo (1-4%)

            <1%

            Addiction

            Anemia

            Diarrhea

            Gynecomastia and breast enlargement

            Epididymitis

            Esophagitis

            Dysmenorrhea

            Dystonia

            Heart failure

            Hirsutism

            Uveitis

            Postmarketing Reports

            Angioedema

            Suicidal behavior and ideation

            Creatinine kinase

            Decreased platelet count

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            Warnings

            Contraindications

            Hypersensitivity

            Cautions

            Peripheral edema may occur; higher frequencies of weight gain and peripheral edema were observed in patients taking both pregabalin and a thiazolidinedione antidiabetic agent compared to patients taking either drug alone; monitor these patients for possible exacerbation of congestive heart failure symptoms when using pregabalin

            Pregabalin may cause dizziness and somnolence; inform patients that pregabalin may impair their ability to perform tasks such as driving or operating machinery; concomitant use of pregabalin with other central nervous system (CNS) depressants may exacerbate these effects

            Weight gain may occur; long-term cardiovascular effects of pregabalin-associated weight gain are unknown

            Symptoms including, insomnia, nausea, headache, anxiety, and diarrhea were reported following abrupt or rapid discontinuation of treatment; increased seizure frequency may occur in patients with seizure disorders and have rapid discontinued treatment; taper pregabalin gradually over a minimum of 1 week rather than discontinuing the drug abruptly

            Unexpectedly high incidence of hemangiosarcoma was identified in 2 different strains of mice; the clinical significance of this finding is unknown

            In controlled studies, blurred vision and other vision-related events were reported with treatment; clinical significance of the ophthalmologic findings is unknown, inform patients to notify their physician if changes in vision occur; if visual disturbance persists, consider further assessment

            Creatine kinase elevations has been associated with treatment; monitor for symptoms (eg, unexplained muscle pain, tenderness, or weakness, particularly if these muscle symptoms are accompanied by malaise or fever); discontinue treatment if myopathy is diagnosed or suspected or if markedly elevated creatine kinase levels occur

            Monitor for decreased platelet count (rare)

            May cause prolongation of PR interval

            Suicidal thoughts or behaviors

            • Antiepileptic drugs increase risk of suicidal thoughts or behavior in patients taking these drugs for any indication; monitor for emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior
            • Inform patients, their caregivers, and families of the increase the risk of suicidal thoughts and behavior; advise to be alert for the emergence or worsening of signs and symptoms

            Angioedema

            • Angioedema of the face, extremities, lips, tongue, glottis, and larynx has been reported during initial and chronic treatment, including reports of life-threatening angioedema with respiratory compromise requiring emergency intervention
            • If laryngeal stridor or angioedema of the face, tongue, or glottis occurs, discontinue therapy and institute appropriate therapy immediately
            • Coadministration of ACE inhibitors or mTOR (mammalian target of rapamycin) inhibitors (eg, temsirolimus, sirolimus, everolimus), or previous history of angioedema may increase risk
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            Pregnancy & Lactation

            Pregnancy

            There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to pregabalin during pregnancy

            North American Antiepileptic Drug (NAAED) Pregnancy Registry

            1-888-233-2334

            http://www.aedpregnancyregistry.org/

            There are no adequate and well-controlled studies with pregabalin in pregnant women

            In the animal fertility study with pregabalin in male rats, adverse reproductive and developmental effects were observed

            In animal reproduction studies, increased incidences of fetal structural abnormalities and other manifestations of developmental toxicity, including skeletal malformations, retarded ossification, and decreased fetal body weight were observed in the offspring of rats and rabbits given pregabalin orally during organogenesis, at doses that produced plasma pregabalin exposures (AUC) greater than or equal to 18 times human exposure at the maximum recommended dose (MRD) of 660 mg/day

            Lactation

            Small amounts of pregabalin have been detected in the milk of lactating women

            Based on animal studies, there is a potential risk of tumorigenicity with pregabalin exposure via breast milk to the breastfed infant

            Available clinical study data in patients greater than 12 years of age do not provide a clear conclusion about the potential risk of tumorigenicity with pregabalin

            Because of the potential risk of tumorigenicity, breastfeeding is not recommended during treatment

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Precise mechanism of action unknown but is a GABA analogue that binds to a subunit of voltage-gated calcium channels in CNS; does not affect sodium channels, opiate receptors, or cyclo-oxygenase enzyme activity; interactions with descending noradrenergic and serotonergic pathways originating from the brain stem appear to reduce neuropathic pain transmission from spinal cord

            Absorption

            Bioavailability: >90%

            AUC (24 hr): 31.5 mcg·h/mL (75 mg capsule BID); 29.4 mcg·h/mL (165 mg ER tablet)

            Peak plasma concentration: 3.2 mcg/mL (75 mg capsule BID); 2 mcg/mL (165 mg ER tablet)

            Peak plasma time, fasting: 1.5 hr (capsule)

            Peak plasma time, with food: 3 hr (ER tablet)

            Distribution

            Vd: 0.5 L/kg

            Protein bound: None

            Although there are no data in humans, pregabalin has been shown to cross the blood brain barrier in mice, rats, and monkeys

            Metabolism

            Minimal

            Elimination

            Half-life: 6.3 hr

            Clearance: 67-80.9 mL/min

            Excretion: Urine

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            Administration

            Oral Administration

            Capsules/oral solution

            • Take orally with or without food
            • When discontinuing treatment, taper gradually over a minimum of 1 week

            ER tablets

            • Take once daily after an evening meal
            • Swallow whole and should not be split, crushed, or chewed
            • When discontinuing treatment, taper gradually over a minimum of 1 week
            • Missed dose after an evening meal, then take usual dose prior to bedtime following a snack
            • Missed dose prior to bedtime, then take usual dose following a morning meal
            • Missed dose following the morning meal, then take usual dose at the usual time that evening following an evening meal

            Storage

            Store at 20-25°C (68-77°F), excursions permitted between 15-30°C (between 59-86°F) in the original package

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.