What is the Difference Between Gabapentin and Pregabalin?

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Gabapentin and pregabalin are both anti-epileptic medications used to treat nerve pain, but they have some differences in their pharmacokinetic and pharmacodynamic properties, as well as their indications and side effects. Here are the main differences between the two:

  1. Brand names: Pregabalin is sold under the brand name Lyrica, while gabapentin is sold under brand names such as Neurontin, Gralise, and Horizant.
  2. Absorption: Pregabalin is absorbed faster and starts working more quickly than gabapentin. Pregabalin reaches its peak concentrations within an hour of being taken, whereas it takes 3 to 4 hours for gabapentin to reach its peak concentration.
  3. Binding affinity: Pregabalin has a stronger binding affinity to its target receptor, which may contribute to its increased potency.
  4. Pharmacokinetics: Pregabalin has more predictable pharmacokinetics, while gabapentin is more slowly and variably absorbed.
  5. Absorption location: Gabapentin is absorbed in the small intestine, while pregabalin is absorbed throughout the small intestine and extending to the ascending colon.
  6. Indications: Both drugs are used to treat nerve pain, but they have different specific uses and may not be interchangeable without consulting a doctor.
  7. Side effects: Some studies have found that pregabalin has fewer side effects and may be more effective for neuropathic pain than gabapentin. However, a randomized clinical trial found that gabapentin was superior to pregabalin in treating chronic sciatica, with fewer and less severe adverse events.
  8. Drug interactions: Neither drug is significantly affected by cytochrome (CYP) drug interactions, as neither is metabolized by CYP enzymes.

In summary, while pregabalin and gabapentin have similar uses and mechanisms, they differ in their absorption, binding affinity, pharmacokinetics, and specific indications. It is essential to consult a healthcare professional before switching between these medications or adjusting dosages.

Comparative Table: Gabapentin vs Pregabalin

Here is a table comparing the differences between gabapentin and pregabalin:

Property Gabapentin Pregabalin
Pharmacokinetics Less predictable More predictable
Binding Affinity Lower binding affinity for alpha-2-delta protein Higher binding affinity for alpha-2-delta protein
Potency Less potent More potent
Absorption Slower absorption Faster absorption
Blood Concentration Does not increase proportionally with increasing dose Increases proportionally with increasing dose
Indications Licensed for peripheral neuropathic pain only Licensed for peripheral and central neuropathic pain
Controlled Substance Not a controlled substance Controlled substance
Dose Equivalence Generally considered to be 6:1 ratio (total daily dose of gabapentin to pregabalin) -
Side Effects Dizziness, drowsiness, weight gain, edema (swelling), dry mouth, headache, nausea, diarrhea, blurred vision, fatigue, cognitive impairment, tremors Dizziness, drowsiness, weight gain, edema (swelling), dry mouth, headache, nausea, diarrhea, blurred vision, fatigue, cognitive impairment, tremors
Dependence Can lead to physical and psychological dependence, especially with high doses or long-term use Can lead to physical and psychological dependence, especially with high doses or long-term use

Please note that the dosage and dose equivalence may vary depending on individual preference and clinical characteristics. It is essential to consult a healthcare professional before making any changes to medication dosages.