pregabalin

pre-GAB-a-lin

Therapeutic Classification: analgesics, anticonvulsants

Pharmacologic Classification: gamma aminobutyric acid gaba analogues, nonopioid analgesics

REMS

Immediate-release and extended-release

Treatment of the following conditions:
- Neuropathic pain associated with diabetic peripheral neuropathy,
- Postherpetic neuralgia.

Immediate-release

Treatment of the following conditions:
- Fibromyalgia,
- Neuropathic pain associated with spinal cord injury,
- Partial-onset seizures (adjunctive therapy).

Binds to calcium channels in CNS tissues which regulate neurotransmitter release. Does not bind to opioid receptors.

Therapeutic effects:

Decreased neuropathic or postherpetic pain.
Decreased partial-onset seizures.

Absorption: Well absorbed (>90%) following oral administration.

Distribution: Well distributed to tissues; probably crosses the blood-brain barrier.

Metabolism/Excretion: Minimally metabolized; 90% excreted unchanged in urine.

Half-Life: 6 hr.

(↓ post–herpetic pain)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–4 wk	unknown

Contraindicated in:

Hypersensitivity;
Known/suspected myopathy;
Severe renal impairment (CCr <30 mL/min) (extended-release only);
Lactation: Lactation.

Use Cautiously in:

All patients (may ↑ risk of suicidal thoughts/behaviors);
Renal impairment (dose alteration recommended for CCr <60 mL/min);
HF;
History of drug dependence/drug-seeking behavior;
Respiratory impairment (↑ risk of respiratory depression);
OB: Safety not established in pregnancy;
Pedi: Children 1 mo (safety and effectiveness not established);
Geri: Consider age-related in renal function when determining dose in older adults.

CV: peripheral edema, PR interval prolongation

Derm: bullous pemphigoid, STEVENS-JOHNSON SYNDROME

EENT: blurred vision, double vision, vertigo

GI: dry mouth, abdominal pain, constipation, diarrhea, nausea, vomiting

Hemat: thrombocytopenia

Metab: ↑appetite, weight gain

MS: ↑creatine kinase

Neuro: dizziness, drowsiness, headache, impaired attention/concentration/thinking, SUICIDAL THOUGHTS/BEHAVIORS

Resp: RESPIRATORY DEPRESSION

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Drug-drug:

Concurrent use with pioglitazone may ↑ risk of fluid retention.
↑risk of CNS and respiratory depression with other CNS depressants including opioids, alcohol, benzodiazepines, or other sedatives/hypnotics.

Diabetic Neuropathic Pain

PO (Adults ): Immediate-release: 50 mg 3 times daily, ↑ over 7 days up to 100 mg 3 times daily. Extended-release: 165 mg once daily after an evening meal; ↑ to 330 mg once daily after an evening meal within 1 wk.

Renal Impairment

PO (Adults ): CCr 30–60 mL/min: Immediate-release: 75–300 mg/day in 2–3 divided doses; Extended-release: 82.5–330 mg once daily after an evening meal; CCr 15–30 mL/min: Immediate-release: 25–150 mg/day in 1–2 divided doses; CCr <15 mL/min: Immediate-release: 25–75 mg/day as a single daily dose.

Postherpetic Neuralgia

PO (Adults ): Immediate-release: 75 mg twice daily or 50 mg 3 times daily initially, may ↑ over 7 days to 300 mg/day in 2–3 divided doses; after 2–4 wk may ↑ to 600 mg/day in 2–3 divided doses. Extended-release: 165 mg once daily after an evening meal; ↑ to 330 mg once daily after an evening meal within 1 wk; if pain is persistent after 2–4 wk, may then ↑ dose of up to 660 mg once daily after an evening meal.

Renal Impairment

PO (Adults ): CCr 30–60 mL/min: Immediate-release: 75–300 mg/day in 2–3 divided doses; Extended-release: 82.5–330 mg once daily after an evening meal; CCr 15–30 mL/min: Immediate-release: 25–150 mg/day in 1–2 divided doses; CCr <15 mL/min: Immediate-release: 25–75 mg/day as a single daily dose.

Fibromyalgia

PO (Adults ): Immediate-release: 75 mg twice daily initially, may ↑ to 150 mg twice daily within 1 wk based on efficacy and tolerability. May ↑ to 225 twice daily.

Renal Impairment

PO (Adults ): CCr 30–60 mL/min: Immediate-release: 75–300 mg/day in 2–3 divided doses CCr 15–30 mL/min: Immediate-release: 25–150 mg/day in 1–2 divided doses; CCr <15 mL/min: Immediate-release: 25–75 mg/day as a single daily dose.

Spinal Cord Injury Neuropathic Pain

PO (Adults ): Immediate-release: 75 mg twice daily initially, may be ↑ to 150 mg twice daily within 1 wk based on efficacy and tolerability; if insufficient pain relief after 2–3 wk, may ↑ to 300 twice daily.

Renal Impairment

PO (Adults ): CCr 30–60 mL/min: Immediate-release: 75–300 mg/day in 2–3 divided doses; CCr 15–30 mL/min: Immediate-release: 25–150 mg/day in 1–2 divided doses; CCr <15 mL/min: Immediate-release: 25–75 mg/day as a single daily dose.

Partial Onset Seizures

PO (Adults ): Immediate-release: 75 mg twice daily or 50 mg 3 times daily initially; may gradually ↑ on a weekly basis up to a max dose of 600 mg/day (in 2–3 divided doses).
PO (Children ≥1 mo and ≥30 kg): Immediate-release: 2.5 mg/kg/day in 2–3 divided doses; may gradually ↑ on a weekly basis up to a max dose of 10 mg/kg/day in 2–3 divided doses (max = 600 mg/day).
PO (Children ≥1 mo and <30 kg): Immediate-release: 3.5 mg/kg/day in 2–3 divided doses for patients ≥4 yr old or in 3 divided doses for patients 1 mo-<4 yr old; may gradually ↑ on a weekly basis up to a max dose of 14 mg/kg/day in 2–3 divided doses for patients ≥4 yr old or in 3 divided doses for patients 1 mo-<4 yr old.

Renal Impairment

PO (Adults ): CCr 30–60 mL/min: Immediate-release: 75–300 mg/day in 2–3 divided doses; CCr 15–30 mL/min: Immediate-release: 25–150 mg/day in 1–2 divided doses; CCr <15 mL/min: Immediate-release: 25–75 mg/day as a single daily dose.

(Generic available)

Immediate-release capsules: 25 mg; 50 mg; 75 mg; 100 mg; 150 mg; 200 mg; 225 mg; 300 mg
Extended-release tablets: 82.5 mg; 165 mg; 330 mg
Oral solution: 20 mg/mL

Monitor closely for notable changes in behavior that could indicate the emergence or worsening of suicidal thoughts or behavior, or depression.
Diabetic Peripheral Neuropathy, Postherpetic Neuralgia, Fibromyalgia, and Spinal Cord Injury Pain: Assess location, characteristics, and intensity of pain periodically during therapy.
Seizures: Assess location, duration, and characteristics of seizure activity.

Lab Test Considerations:

May cause ↑ creatine kinase levels.
- May cause ↓ platelet count.

Do not confuse Lyrica with Lopressor or Hydrea.
Pregabalin should be discontinued gradually over at least 1 wk. Abrupt discontinuation may cause insomnia, nausea, headache, anxiety, sweating, and diarrhea when used for pain and may cause increase in seizure frequency when treating seizures.
PO: May be administered without regard to meals. Oral solution may be stored at room temperature.

Instruct patient to take medication as directed. Take missed doses as soon as remembered unless almost time for next dose; do not double doses. Do not discontinue abruptly. Advise patient to read the Patient Information Leaflet prior to taking pregabalin and with each Rx refill in case of changes.
May cause dizziness, drowsiness, and blurred vision. Caution patient to avoid driving or activities requiring alertness until response to medication is known. Advise patient to notify health care professional if changes in vision occur. Patients with seizures should not resume driving until health care professional gives clearance based on control of seizure disorder.
Instruct patient to promptly report unexplained muscle pain, tenderness, or weakness, especially if accompanied by malaise or fever. Discontinue therapy if myopathy is diagnosed or suspected or if markedly elevated creatine kinase levels occur.
Advise patient and family to notify health care professional if thoughts about suicide or dying, attempts to commit suicide; new or worse depression; new or worse anxiety; feeling very agitated or restless; panic attacks; trouble sleeping; new or worse irritability; acting aggressive; being angry or violent; acting on dangerous impulses; an extreme increase in activity and talking, other unusual changes in behavior or mood occur.
Inform patient that pregabalin may cause edema and weight gain.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Caution patient to avoid alcohol or other CNS depressants, including opioids, with pregabalin, may cause respiratory depression and overdose.
Instruct patient to notify health care professional of medication regimen before treatment or surgery.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. May impair male fertility. Encourage patients who become pregnant to enroll in the NAAED Pregnancy Registry by calling 1-800-233-2334. Information can be found at http://www.aedpregnancyregistry.org/.
Advise patient to carry identification describing disease process and medication regimen at all times.

Decrease in intensity of chronic pain.
Decrease in the frequency or cessation of seizures.

Lyrica, Lyrica CR

Schedule V (C-V)

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