Class Explorer · Neurology
Gabapentinoids
Bind the alpha-2-delta subunit of voltage-gated calcium channels and reduce excitatory transmitter release. Named after GABA and acting nowhere near it.
Members
Also in this class: Pregabalin. Full pages arrive as the library grows.
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Gabapentin
- Absorption
- Saturable, falls at higher doses
- Renal handling
- Entirely renal; dose tracks clearance
Shared across the class
- Indications
- Neuropathic pain · Focal seizures as adjunct · Restless legs syndrome · Generalised anxiety disorder (pregabalin)
- Adverse effects
- Sedation and dizziness · Peripheral oedema · Weight gain · Respiratory depression with opioids · Misuse potential
- Contraindications
- Known hypersensitivity
- Monitoring
- Renal function, which sets the dose · Sedation, gait and cognition, especially in older adults · Whether it is actually helping, judged after an adequate trial rather than continued indefinitely
What makes each agent different
- Pregabalin has linear, near-complete absorption; gabapentin's transporter saturates, so its bioavailability falls as the dose rises and splitting doses matters.
- Both are renally cleared and both accumulate quietly in kidney disease, which is where their confusion and myoclonus come from.
The ankle oedema is a drug effect, not heart failure. Answering it with furosemide is a textbook prescribing cascade.
Combined with opioids these drugs contribute meaningfully to respiratory depression, a risk that took years to be recognised.
Last reviewed 2026-08-16 · Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed.