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Gabapentin and Pregabalin

Andrew Street Top 100 Drugs Inglés 4 fichas

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  1. 1Indications 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)
  2. 2MOA 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.
  3. 3SE's of gabapentin & pregabalin.• Drowsiness
    • Dizziness
    • Ataxia
  4. 4CI'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.

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Top 100 drugs.
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Andrew Street
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