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PregabalinAka: Lyrica

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  1. 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
  2. Mechanism
    1. Alpha2-delta1 Ligand agent
    2. Binds alpha2-delta1 subunit of Central Nervous System voltage-gated calcium channels
    3. Does not bind GABA receptors or Benzodiazepine receptors
  3. 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 (rare)
  4. Dosing
    1. Starting: 25 mg orally three times daily (starting low dose maximizes tolerability)
    2. Titrate to effective dose in increments on weekly basis based on tolerability
    3. Maximum dose: 450 mg/day divided 2-3 times daily
      1. Fibromyalgia may require the maximum dose
    4. Stopping: Taper off agent (Do not stop abruptly due to withdrawal symptoms)

pregabalin (C0657912)

Definition (NCI)A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic and analgesic activities. Pregabalin selectively binds to alpha2delta (A2D) subunit of the presynaptic voltage-gated calcium channels located in the central nervous system (CNS). Binding of A2D subunits prevent calcium influxes and the subsequent calcium-dependent releases of various neurotransmitters from presynaptic nerve terminals in hyperexcited neurons, including glutamate, norepinephrine, serotonin, dopamine, and substance P. This leads to an inhibition of synaptic transmission and reduces neuronal excitability. Pregabalin does not bind directly to GABA-A, GABA-B receptors and does not alter GABA uptake or degradation.
ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
Englishpregabalin
Spanishpregabalina
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Lyrica (C1570232)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishLyrica
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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