Pharm

Pregabalin

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Pregabalin, Lyrica

  • See Also
  1. Gabapentin
  • Indications
  1. Anticonvulsant
    1. Adjunct for partial-onset Seizures
  2. Neuropathic Pain Management
    1. Fibromyalgia
    2. Peripheral Neuropathy
      1. Diabetic Peripheral Neuropathy
      2. Postherpetic Neuralgia
  • Mechanism
  1. Lipophilic (greater diffusion across blood brain barrier)
  2. Binds alpha2-delta1 subunit of Central Nervous System voltage-gated Calcium channels
  3. GABA Receptor Agonist, but does not bind GABA Receptors or Benzodiazepine receptors
  1. Regular Release
    1. Start 50 mg orally three times daily or 75 mg orally twice daily
      1. May start at 25 mg orally three times daily to maximize tolerability
    2. May increase after 1 week to 100 mg orally three times daily or 150 mg orally twice daily
    3. Maximum dose: 300 mg (Diabetic Neuropathy), 450 mg (Fibromyalgia), 600 mg/day (Postherpetic Neuralgia)
  2. Extended Release (Pregabalin XR, Lyrica CR)
    1. Start 165 mg orally daily after evening meal
    2. May increase after 1 week to 330 mg orally daily
    3. Maximum: 660 mg/day
      1. Maximum 330 mg if CrCl 30 to 60 ml/min
      2. Avoid CR if CrCl <30 ml/min (use regular release capsules instead)
  3. Stopping
    1. Taper off agent over 1 week or more
    2. Avoid stopping abruptly due to withdrawal symptoms
  1. Adult
    1. Start 50 mg orally three times daily or 75 mg orally twice daily
    2. Maximum: 600 mg/day
  2. Child (over age 1 month)
    1. Weight > 30 kg
      1. Start 2.5 mg/kg/day divided 2-3 times per day
      2. Titrate as needed to 10 mg/kg/day in divided doses (maximum 600 mg/day)
    2. Weight <30 kg
      1. Start 3.5 mg/kg/day divided 3 times per day
      2. Titrate as needed to 14 mg/kg/day in divided doses (maximum 600 mg/day)
  • Metabolism
  1. Decrease Pregabalin dosing in Creatinine Clearance <60 ml/min
  • Safety
  1. Unknown Safety in Lactation
  2. First trimester use linked to possible birth defects
    1. Winterfeld (2016) Neurology 86(24): 2251-7 [PubMed]
  • Adverse effects
  1. Common adverse effects
    1. Weight gain
    2. Peripheral Edema
    3. Dizziness or Ataxia
    4. Somnolence
    5. Headache
    6. Xerostomia
    7. Tremor
    8. Blurred Vision or Diplopia
  2. Severe but uncommon adverse effects
    1. Angioedema
    2. Hypersensitivity Reaction
    3. Rhabdomyolysis or Myopathy (rare)
  3. Other adverse effects
    1. Thrombocytopenia
    2. Prolonged PR Interval
  4. Risk of Abuse
    1. Gabapentin and Pregabalin (Lyrica) are abused by patients on Opiates to potentiate CNS Opiate effects
    2. More than one quarter of Opiate patients have abused Gabapentin
    3. Pregabalin (Lyrica) is more potent with faster onset and has higher abuse potential than Gabapentin
    4. Smith (2012) Br J Gen Pract 62(601):406-7 +PMID:22867659 [PubMed]
  5. Cardiovascular Events
    1. Single retrospective EHR chart review associated Gabapentin and Pregabalin with cardiovascular events
    2. Higher quality confirmatory studies are needed
    3. Pan (2022) Cardiovasc Diabetol 21(1):170 +PMID: 36050764 [PubMed]
  • Resources
  1. Pregabalin (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=60185c88-ecfd-46f9-adb9-b97c6b00a553
  • References
  1. (2022) Presc Lett, Resource #361206, Antiseizure Medications
  2. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 56-7
  3. Hamilton (2020) Tarascon Pocket Pharmacopoeia