Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter. It may be used to manage neuropathic pain, postherpetic neuralgia, and fibromyalgia among other conditions.

Therapeutic Indication
● Neuropathic Pain
● Diabetic Peripheral Neuropathic Pain (DPN)
● Effectively supports brain and nerve function
● Treatment of fibromyalgia


Mechanism of Action:
Pregabalin is structural analogue of gamma-aminobutyric acid (GABA), it does not bind to GABA receptors. Instead, it binds the alpha2-delta subunit of presynaptic voltage-gated calcium channels in the central nervous system. By binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin modulates the release of several excitatory neurotransmitters including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide. In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn, which may also contribute to the mechanism of action Pregabalin does not modulate dopamine receptors, serotonin receptors, opiate receptors, sodium channels or cyclooxygenase activity.

Absorption: Absorption of Pregabalin extended release formulation is limited by permeability with absorption occurring in upper gastrointestinal tract, with little or no drug absorption occurring beyond hepatic flexure giving the absorption window of 6 hours for drugs to be absorbed.
Volume of Distribution:
Volume of Distribution is approximately 0.56 L/kg
It is not bound to plasma proteins
Metabolism: Negligible amount is metabolised
Excretion: Excreted unchanged mainly from urine

Side Effects
Common side effects include:
● Dizziness
● Drowsiness
● Dry mouth
● Constipation

Some products that may interact with this drug include:
● Amitriptyline
● Aspirin
● Celecoxib
● Codeine
● Duloxetine
● Diazepam
● Fish Oil (omega-3 polyunsaturated fatty acids)
● Fluoxetine
● Morphine
● Tramadol
● Alprazolam

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