Pregabalin is the first drug to receive approved labelling from FDA for the treatment of painful diabetic neuropathy, post herpetic neuralgia & antiepileptic. It is structurally similar to gamma- amino butyric acid (GABA) an inhibitory neurotransmitter.
Absorption: absorbed from the small intestine and proximal colon. The bioavailability is reduced if taken on an empty stomach. The AUC is approximately 30%.
Plasma protein binding: It doesn’t bind to plasma proteins
Volume of distribution: 0.5L/kg
Metabolism: It undergoes negligible metabolism in humans
Half life: 6.3 hours
Elimination: eliminated from the systemic circulation primarily by renal excretion as unchanged drug
Paglin binds with high affinity to the alpha 2-delta site (an auxiliary subunit of voltage gated calcium channels) in central nervous system tissues thereby reduces calcium influx at the nerve terminals which inhibits the release of excitatory neurotransmitters such as glutamate and Ach which finally modulates nerve impulses involved in the transmission of pain.
- Diabetic peripheral neuropathy: the approved starting dose is 50mg t.i.d.
- Post herpetic neuralgia: the starting dosage is 75mg BID daily or 50mg t.i.d.
- Painful neurological conditions & fibromyalgia: the recommended dose is 50-75 mg b.i.d.
- Trouble with memory
- Poor coordination
- Dry mouth
- Problem with vision
- Weight gain
- Hypersensitivity reactions
- Suicidal behaviour and ideation
- Peripheral edema