In the animal fertility study with pregabalin in male rats, adverse reproductive and developmental effects were observed see Nonclinical Toxicology (13.1). Multiple oral doses of LYRICA were co-administered with oxycodone, lorazepam, or ethanol. Although no pharmacokinetic interactions were seen, additive effects on cognitive and gross motor functioning were seen when LYRICA was co-administered with these drugs.
- Only studies directly comparing pregabalin with gabapentin were included to address the specific research question.
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- Additionally, it selectively binds to the α2δ-1 subunit of calcium channels in the central nervous system, contributing to its analgesic effect and reducing the release of other neurotransmitters (46).
Choosing an OTC Pain Reliever: What to Consider
Ocular lesions (characterized by retinal atrophy including loss of photoreceptor cells and/or corneal inflammation/mineralization) were observed in two lifetime carcinogenicity studies in Wistar rats. These findings were observed at plasma pregabalin exposures (AUC) greater than or equal to 2 times those achieved in humans given the maximum recommended dose of 600 mg/day. Similar lesions were not observed in lifetime carcinogenicity studies in two strains of mice or in monkeys treated for 1 year. In the postmarketing experience, the most commonly reported adverse events observed with pregabalin when taken in overdose include reduced consciousness, depression/anxiety, confusional state, agitation, and restlessness. Deaths have been reported in the setting of lone LYRICA overdose and in combination with other CNS depressants.
Analysis by Dosage Form
After oral dosing administered in the fasted state, pregabalin absorption is rapid, and extensive. Pregabalin oral bioavailability is reported to be 90% regardless of the dose. Cmax is attained within 1.5 hours after single or multiple doses, and pregabalin in usa steady state is attained within hours with repeated administration.
In Ukraine, as of March 2025, pregabalin-containing drugs were included in the list of the most commonly used medicines 49. Overall, there were no significant differences in terms of total adverse events. However, when considering specific adverse events, gabapentin showed a higher incidence of nausea and vomiting compared to pregabalin. There were no significant differences in the occurrence of other specific adverse events.
