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 that 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.

(↓ postherpetic pain)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–4 wk	unknown

Contraindicated in:

Hypersensitivity;
Known/suspected myopathy;
Severe renal impairment (extended release only);
Lactation: Lactation.

Use Cautiously in:

All patients (may ↑ risk of suicidal thoughts/behaviors);
Renal impairment (↓ dose if 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: ↑CK

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

Resp: RESPIRATORY DEPRESSION

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Drug-drug:

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 ↑ 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.
Monitor for hypersensitivity reactions (angioedema, hives, dyspnea, wheezing). Discontinue immediately and implement supportive measures if indicated.
Monitor for respiratory depression (respiratory rate and oxygen saturation). Implement supportive measures if needed.
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 ↑ CK.
- May ↓ platelets.

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

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy. 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 notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
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 provider if changes in vision occur. Patients with seizures should not resume driving until health care provider 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 ↑ CK levels occur.
Advise patient and caregiver to notify health care provider 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 ↑ in activity and talking, or other unusual changes in behavior or mood occur.
Inform patient that pregabalin may cause edema and weight gain.
Advise patient to notify health care provider if hypersensitivity reactions, respiratory depression, or rash occurs. Advise to seek immediate medical attention if needed.
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 provider of medication regimen before treatment or surgery.
Advise patient to carry identification describing disease process and medication regimen at all times.
Rep: Advise women of reproductive potential to notify health care provider 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 or visiting https://www.aedpregnancyregistry.org/.

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

Lyrica, Lyrica CR

Schedule V (C-V)

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Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

Contr. Subst. Schedule ⬆ ⬇

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