Pregabalin
A gabapentinoid for neuropathic pain, fibromyalgia (US) and generalized anxiety disorder (EU and UK), and as add-on for focal seizures.
Drug card
- Class
- Gabapentinoid
- How it works
- Binding the alpha-2-delta calcium channel subunit to cut transmitter release
- Used for
- Neuropathic pain: diabetic, postherpetic, spinal cord injury
- Fibromyalgia (US license)
- Generalized anxiety disorder (EU and UK license)
- Focal seizures, as add-on treatment
- Known for
- Dizziness
- Drowsiness
- Swelling of the legs and feet (peripheral edema)
- Its name
- -gab- means a GABA analogue (gabapentin type)
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does pregabalin work?
Pregabalin, a GABA derivative, binds the alpha-2-delta subunit of voltage-gated calcium channels with high affinity; in nerve-injury models it cuts the calcium-triggered release of pain-signaling transmitters in the spinal cord. It does not act on GABA or benzodiazepine receptors. Unlike gabapentin, 90% or more of every dose is absorbed, so levels rise linearly.
Like other gabapentinoids: Gabapentinoids bind the alpha-2-delta subunit of the voltage-gated calcium channels found in the brain and spinal cord. This cuts calcium entry into overactive nerve endings and so the release of glutamate, norepinephrine and substance P, damping pain signals and seizure spread, though the full mechanism is not settled. Although built like GABA, they do not act on GABA receptors or change GABA levels.
Uses
What is pregabalin used for?
- Neuropathic pain: diabetic, postherpetic, spinal cord injury
- Fibromyalgia (US license)
- Generalized anxiety disorder (EU and UK license)
- Focal seizures, as add-on treatment
Side effects
Side effects of pregabalin
- DizzinessKnown for
- DrowsinessKnown for
- Swelling of the legs and feet (peripheral edema)Known for
- Breathing depression, mainly with opioidsSerious
- Misuse, euphoria and dependenceSerious
- Severe skin reactions (SJS, TEN)Serious
- Heart failure, mainly in older heart patientsSerious
- Birth defects after first-trimester useSerious
- Kidney failure (rare)Serious
- Falls in older peopleSerious
- Erectile dysfunction and lower libido
- Muscle breakdown (rhabdomyolysis), rareSerious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Opioids, other CNS depressants, lung or nerve disease, kidney impairment and age over 65 raise the risk of severe breathing depression.
- It can cause dependence even at usual doses and is misused; screen for drug misuse. It is Schedule V in the US and Class C in the UK.
- First-trimester use slightly raises the risk of major birth defects, so it is avoided in pregnancy unless clearly needed.
- Doses are cut in kidney impairment; stop gradually over at least a week to avoid withdrawal symptoms and seizures.
Good to know: UK reports of abuse and dependence with pregabalin far outnumber those with gabapentin, and its US label records euphoria in some patients.
Remember it
A way to remember it
Gabapentinoids look like GABA but act on calcium.
They are built like the neurotransmitter GABA yet do not bind GABA receptors; instead they bind the alpha-2-delta subunit of voltage-gated calcium channels and cut transmitter release.
Written for biofideX
Its name
-gab- means GABA analogue (gabapentin type)
Gabapentin and pregabalin are modeled on GABA, but both bind the alpha-2-delta subunit of calcium channels, and gabapentin leaves GABA binding and breakdown untouched.
- Every drug name stem
Its class
Gabapentinoids
Other gabapentinoids with a card:
Easily mixed up with benzodiazepines, tricyclic antidepressants and serotonin-norepinephrine reuptake inhibitors.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
- Pregabalin capsules: label (DailyMed)
- Pregabalin: product information (EMA)
- Pregabalin (NCI Thesaurus)
- About pregabalin (NHS)
- Pregabalin: reports of severe respiratory depression (MHRA)
- Pregabalin, gabapentin and risk of abuse and dependence: new scheduling requirements (MHRA)
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Epilepsy and nerve pain
Pregabalin is one of 8 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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