II. Precautions: Risk of Abuse

  1. Gabapentin and Pregabalin (Lyrica) is 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]

III. 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

IV. Mechanism

  1. Lipophilic (greater diffusion across blood brain barrier)
  2. Binds alpha2-delta1 subunit of Central Nervous System voltage-gated Calcium channels
  3. Does not bind GABA receptors or Benzodiazepine receptors

V. Safety

  1. First trimester use linked to possible birth defects
    1. Winterfeld (2016) Neurology 86(24): 2251-7 [PubMed]

VI. Adverse effects

VII. Dosing

  1. Starting
    1. Dose: 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
    1. Taper off agent over 1 week or more
    2. Avoid stopping abruptly due to withdrawal symptoms

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Related Studies

Cost: Medications

lyrica (on 6/1/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
LYRICA 100 MG CAPSULE $6.62 each
LYRICA 150 MG CAPSULE $6.62 each
LYRICA 200 MG CAPSULE $6.62 each
LYRICA 225 MG CAPSULE $6.62 each
LYRICA 25 MG CAPSULE $6.62 each
LYRICA 300 MG CAPSULE $6.62 each
LYRICA 50 MG CAPSULE $6.62 each
LYRICA 75 MG CAPSULE $6.64 each

Ontology: pregabalin (C0657912)

Definition (NCI_NCI-GLOSS) A drug used to treat nerve pain caused by diabetes or herpes zoster infection and certain types of seizures. It is being studied in the prevention and treatment of nerve pain in the hands and feet of cancer patients given chemotherapy. Pregabalin is a type of anticonvulsant.
Definition (NCI) A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished. Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation.
Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH C080245
SnomedCT 415159003, 415160008
LNC LP61621-6, MTHU021880
English 3-(Aminomethyl)-5-methyl-hexanoic Acid, 3-Isobutyl GABA, pregabalin (medication), PREGABALIN, pregabalin [Chemical/Ingredient], (S+)-3-isobutyl GABA, 3-(aminomethyl)-5-methylhexanoic acid, (R-)-3-isobutyl GABA, (S)-3-(aminomethyl)-5-methylhexanoic acid, Pregabalin (product), Pregabalin (substance), Pregabalin, 3-isobutyl GABA, pregabalin
Spanish pregabalina (producto), pregabalina (sustancia), pregabalina

Ontology: Lyrica (C1570232)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C080245
English Lyrica, Pfizer brand of pregabalin