Gabapentin and Pregabalin

Question	Answer
Indications for gabapentin & pregabalin.	• Focal epilepsies - usually as an add-on Rx when other antiepileptic drugs aren't adequate • Neuropathic P • Migraine prophylaxis (gabapentin) • GAD (pregabalin)
MOA of gabapentin & pregabalin.	From a structural point of view, gabapentin is closely related to γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the brain. However, its MOA, although not completely understood, appears largely unrelated to GABA. It binds with voltage-sensitive calcium (Ca2+) channels, where it presumably prevents inflow of Ca2+ &, in so doing, inhibits neurotransmitter release. This interferes with synaptic transmission & reduces neuronal excitability. Pregabalin is a structural analogue of gabapentin that probably has a similar mechanism of action.
SE's of gabapentin & pregabalin.	• Drowsiness • Dizziness • Ataxia
CI's, cautions, & important interactions of gabapentin & pregabalin.	CI's: • None Cautions: • Renal impairment (reduce dose) Important interactions: The sedative effects of gabapentin & pregabalin may be enhanced when combined with other sedating drugs (eg benzodiazepines). Other than this, gabapentin & pregabalin are notable in having relatively few drug interactions – in stark contrast to most other antiepileptic drugs. This makes them particularly useful where combination regimens are considered necessary.

Resource summary

	Created by Andrew Street over 8 years ago