Pregabalin (LYRICA)
Pronunciation: pre GAB a lin / LEER ik uh
Mascot / Mnemonic phrase: “Preg gobblin’ Lyrics”
Year approved: 2005
❖ Antiepileptic
❖ Voltage-gated calcium channel blocker
❖ Glutamate ⇩
❖ DEA Schedule V
FDA-approved for:
❖ Focal seizures (adjunct)
❖ Neuropathic pain
❖ Fibromyalgia
❖ Post-herpetic neuralgia
Used off-label for:
❖ Generalized anxiety
❖ Social anxiety
❖ Alcohol dependence
❖ Alcohol or benzo withdrawal
Pregabalin, FDA-approved in 2005, is a voltage-gated calcium channel blocker, as is gabapentin (Neurontin). Gabapentin and pregabalin constitute the gabapentinoid class of medication. Their structure is similar to GABA, but neither bind GABA receptors.
Lyrica is not metabolized, but rather excreted unchanged in the urine. Half-life is 6 hours, similar to that of Neurontin. Lyrica is a Schedule V controlled substance (least restrictive) because euphoria is possible and it may potentiate the opioid "high". Generic pregabalin has been available since 2019.
It is approved for generalized anxiety in the UK. Large randomized-controlled trials supports its use (off-label) for generalized and social anxiety disorders. For these indications, evidence for pregabalin is more robust than evidence for gabapentin.
Side effects of pregabalin:
► Dizziness
► Sedation
► Headache
► Concentration problems
► Peripheral edema
► Weight gain (usually not)
► Angioedema (rare)
► Myoclonus (rare)
► Rhabdomyolysis (rare)
AEDs that are highly effective for neuropathic pain:
► Pregabalin (Lyrica)
► Gabapentin (Neurontin)
► Carbamazepine (Tegretol)
Although “preg” is in this drug’s name—consider avoiding use of pregabalin during pregnancy. Teratogenicity is not expected, but pregabalin was not good for fetuses of animals given double the recommended human dose.
Of 1,821 single-drug exposures to oxcarbazepine reported to Poison Control, there were 44 major serious outcomes but no deaths (Nelson & Spyker, 2017).
Comparison of gabapentin and pregabalin
In 2020 the FDA issued a warning of respiratory depression in individuals with respiratory risk factors (COPD, obesity, those taking opioids). The warning applied to gabapentin also.
Dynamic interactions:
❖ Sedation (mild)
❖ Respiratory depression
❖ May potentiate opioid “high”
Kinetic interactions:
❖ None significant because it is excreted unmetabolized in urine—“in a bubble”
Dosing of pregabalin
Capsules: 25, 50, 75, 100, 150, 200, 225 mg
For most indications, start 50 mg TID or 75 mg BID. May increase to total daily dose of 300 mg within one week; 300–600 mg/day in divided doses is an effective maintenance dose for generalized/social anxiety disorders; Maximum total daily dose is 600 mg.
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