Pregabalin extended-release
Other products: Pregabalin
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Dosing in kidney impairment
Patients with Renal Impairment Use of pregabalin extended-release tablets is not recommended for patients with creatinine clearance (CLcr) less than 30 mL/min or who are undergoing hemodialysis. Those patients should receive LYRICA. In view of dose-dependent adverse reactions and because pregabalin is eliminated primarily by renal excretion, adjust the dose in patients with reduced renal function.
Base the dose adjustment in patients with renal impairment on CLcr, as indicated in Table 2. To use the dosing tables, an estimate of the patient's CLcr in mL/min is needed. CLcr in mL/min may be estimated from serum creatinine (mg/dL) determination using the Cockcroft and Gault equation: Next, refer to the Dosage and Administration section to determine the recommended total daily dose based on indication, for a patient with normal renal function (CLcr greater than or equal to 60 mL/min).
Then refer to Table 2 to determine the corresponding renal adjusted dose. (For example: A patient initiating pregabalin extended-release tablets therapy for postherpetic neuralgia with normal renal function [CLcr greater than or equal to 60 mL/min], receives a single daily dose of 165 mg/day pregabalin. Therefore, a renal impaired patient with a CLcr of 50 mL/min would receive a single daily dose of 82.5 mg.) [See table below.] PRINCIPAL DISPLAY PANEL - 50 mg/500 mg Tablet Bottle Label
| Creatinine Clearance (CLcr) (mL/min) | Total Pregabalin Extended-Release Tablets Daily Dose (mg/day) | Dose Regimen | |||
|---|---|---|---|---|---|
| greater than or equal to 60 | 165 | 330 | 495 495 mg = 3 × 165 mg tablets taken once a day. | 660 660 mg = 2 × 330 mg tablets taken once a day. | Once a day |
| 30–60 | 82.5 | 165 | 247.5 247.5 mg = 3 × 82.5 mg tablets taken once a day | 330 | Once a day |
| less than 30/hemodialysis | Dose with LYRICA | ||||
Preparation and administration
Important Dosage and Administration Instructions Pregabalin extended-release tablets should be administered once daily after an evening meal. Pregabalin extended-release tablets should be swallowed whole and should not be split, crushed, or chewed. When discontinuing pregabalin extended-release tablets, taper gradually over a minimum of 1 week.
Instruct patients that if they miss taking their dose of pregabalin extended-release tablets after an evening meal, then they should take their usual dose of pregabalin extended-release tablets prior to bedtime following a snack. If they miss taking the dose of pregabalin extended-release tablets prior to bedtime, then they should take their usual dose of pregabalin extended-release tablets following a morning meal.
If they miss taking the dose of pregabalin extended-release tablets following the morning meal, then they should take their usual dose of pregabalin extended-release tablets at the usual time that evening following an evening meal [see Patient Counseling Information] .
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- Pregabalin extended-release
Label text (3 paragraphs)
Since pregabalin is predominantly excreted unchanged in the urine, undergoes negligible metabolism in humans (less than 2% of a dose recovered in urine as metabolites), and does not bind to plasma proteins, its pharmacokinetics are unlikely to be affected by other agents through metabolic interactions or protein binding displacement. In vitro studies showed that pregabalin is unlikely to be involved in significant pharmacokinetic drug interactions [see Clinical Pharmacology (12) ] . The interactions of pregabalin extended-release tablets with co-administration of other drugs have not been systematically evaluated.
Co-administration of the prokinetic drug erythromycin with pregabalin extended-release tablets did not result in any clinically important changes in the pharmacokinetics of pregabalin extended-release tablets [see Clinical Pharmacology (12) ] . Additional studies have been performed with LYRICA. No pharmacokinetic interactions were observed between LYRICA and carbamazepine, gabapentin, lamotrigine, oral contraceptive, phenobarbital, phenytoin, topiramate, and valproic acid. A similar lack of pharmacokinetic interactions would be expected to occur with pregabalin extended-release tablets.
Pharmacodynamics Although no pharmacokinetic interactions were seen with LYRICA and ethanol, lorazepam, or oxycodone, additive effects on cognitive and gross motor functioning were seen when LYRICA was co-administered with these drugs. No clinically important effects on respiration were seen in studies of LYRICA.
Contraindications
Pregabalin extended-release tablets are contraindicated in patients with known hypersensitivity to pregabalin or any of its components. Angioedema and hypersensitivity reactions have occurred in patients receiving pregabalin therapy [see Warnings and Precautions (5.1 , 5.2) , Adverse Reactions (6) ] . Known hypersensitivity to pregabalin or any of its components. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
CLikelihood score C: Probable rare cause of clinically apparent liver injury.
Pregabalin is an inhibitor of neuronal activity used for therapy of painful neuropathy and as an anticonvulsant. Therapy with pregabalin is not associated with serum aminotransferase elevations, and clinically apparent liver injury from pregabalin has been reported but appears to be quite rare.
ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to pregabalin during pregnancy. To provide information regarding the effects of in utero exposure to pregabalin extended-release tablets, physicians are advised to recommend that pregnant patients taking pregabalin extended-release tablets enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry. This can be done by calling the toll free number 1-888-233-2334, and must be done by patients themselves. Information on the registry can also be found at the website http://www.aedpregnancyregistry.org/ .
Risk Summary There are no adequate and well-controlled studies with pregabalin extended-release tablets in pregnant women. However, in animal reproduction studies, increased incidences of fetal structural abnormalities and other manifestations of developmental toxicity, including skeletal malformations, retarded ossification, and decreased fetal body weight were observed in the offspring of rats and rabbits given pregabalin orally during organogenesis, at doses that produced plasma pregabalin exposures (AUC) greater than or equal to 18 times human exposure at the maximum recommended dose (MRD) of 660 mg/day [see Data ] .
In an animal development study, lethality, growth retardation, and nervous and reproductive system functional impairment were observed in the offspring of rats given pregabalin during gestation and lactation. The no-effect dose for developmental toxicity was approximately twice the human exposure at MRD. The background risk of major birth defects and miscarriage for the indicated populations are unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4% and of miscarriage is 15 to 20% of clinically recognized pregnancies. Advise pregnant women of the potential risk to a fetus.
Data Animal Data When pregnant rats were given pregabalin (500 mg/kg, 1250 mg/kg, or 2500 mg/kg) orally throughout the period of organogenesis, incidences of specific skull alterations attributed to abnormally advanced ossification (premature fusion of the jugal and nasal sutures) were increased at greater than or equal to 1250 mg/kg, and incidences of skeletal variations and retarded ossification were increased at all doses. Fetal body weights were decreased at the highest dose. The low dose in this study was associated with a plasma exposure (AUC) approximately 18 times human exposure at the MRD of 660 mg/day. A no-effect dose for rat embryo-fetal developmental toxicity was not…
Breastfeeding (LactMed)
Limited data indicate that amounts of pregabalin in breastmilk are low and one infant breastfed for 3 months with no discernable adverse effects. Pharmacokinetic model predicted that a maternal dosage of 150 mg daily would not result in a therapeutic level in an exclusively breastfed infant of any age. If pregabalin is required by the mother, it is not a reason to discontinue breastfeeding, but until more data become available, use caution while nursing a newborn or preterm infant. The manufacturer recommends that breastfeeding is not recommended during treatment with pregabalin because of the potential risk of tumorigenicity based on high-dose animal studies over a prolonged period. Pregabalin has been used to treat persistent nipple pain in a few women at an average starting dosage of 100 mg daily.
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