Home Drug Guide Pregabalin

Drug Guide

Generic Name

Pregabalin

Brand Names Lyrica, Lyrica CR

Classification

Therapeutic: Anticonvulsant, Neuropathic pain agent

Pharmacological: Alpha2-delta ligand

FDA Approved Indications

Neuropathic pain associated with diabetic peripheral neuropathy
Postherpetic neuralgia
Fibromyalgia
Adjunctive therapy for partial-onset seizures

Mechanism of Action

Pregabalin binds to the alpha2-delta site in the central nervous system, reducing calcium influx at nerve terminals, which diminishes the release of excitatory neurotransmitters and stabilizes hyperexcited neural activity, thereby exerting its anticonvulsant and analgesic effects.

Dosage and Administration

Adult: Start with 150 mg/day in 2 to 3 divided doses, titrate gradually based on efficacy and tolerability, up to a maximum of 600 mg/day.

Pediatric: Not approved for use in children.

Geriatric: Start at lower doses due to potential renal impairment; dose adjustments required.

Renal Impairment: Reduce dose based on creatinine clearance; detailed dosing guidelines are available.

Hepatic Impairment: No specific adjustment needed; use with caution.

Pharmacokinetics

Absorption: Well absorbed orally, with bioavailability >90%.

Distribution: Widely distributed in body tissues; volume of distribution approximately 0.5 L/kg.

Metabolism: Minimal hepatic metabolism; primarily excreted unchanged by the kidneys.

Excretion: Renal excretion; unchanged in urine.

Half Life: Approximately 6.3 hours in healthy individuals; may be prolonged in renal impairment.

Contraindications

Hypersensitivity to pregabalin or its components.

Precautions

History of angioedema, hypersensitivity reactions.
Renal impairment: dose adjustment required.
Suicidal thoughts and behaviors: monitor closely.
CNS depression: caution when operating machinery; avoid alcohol.

Adverse Reactions - Common

Dizziness (Frequently)
Somnolence (Frequently)
Peripheral edema (Frequently)
Dry mouth (Often)

Adverse Reactions - Serious

Anaphylaxis (Rare)
Angioedema (Rare)
Erythema multiforme (Rare)
Suicidal ideation (Monitor closely)

Drug-Drug Interactions

CNS depressants (e.g., opioids, benzodiazepines) – additive CNS depression.

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor for signs of CNS depression, peripheral edema, and mood changes.

Diagnoses:

Risk for injury due to dizziness or sedation
Ineffective airway clearance if CNS depression occurs

Implementation: Administer doses as prescribed; titrate gradually. Monitor renal function periodically. Educate patient on avoiding activities requiring alertness initially.

Evaluation: Assess patient’s pain relief, seizure frequency, and adverse effects regularly.

Patient/Family Teaching

Do not stop medication abruptly to avoid withdrawal seizures.
Be cautious when driving or operating machinery until effects are known.
Report any swelling, difficulty breathing, or severe side effects promptly.
Avoid alcohol as it may increase CNS depression.

Special Considerations

Black Box Warnings:

Suicidal thoughts and behaviors: Patients should be closely monitored for mood changes.
Risks related to depression and suicidality.

Genetic Factors: Pharmacogenomic data not yet well established.

Lab Test Interference: Minimal; no significant interference expected with common lab tests.

Overdose Management

Signs/Symptoms: Severe drowsiness, confusion, agitation, hallucinations, vomiting, tachycardia.

Treatment: Supportive care; gastric lavage or activated charcoal if ingestion was recent; hemodialysis may be considered in severe cases, especially in renal impairment.

Storage and Handling

Storage: Store at room temperature 20°C to 25°C (68°F to 77°F). Keep container tightly closed.

Stability: Stable when stored properly; discard after expiration date.