Pregabalin Lyrica: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Pregabalin is also used in people with epilepsy to treat and prevent seizures, sometimes called convulsions. Keep a list of them with you to show your healthcare provider and pharmacist each time you get a new medicine. Do not start a new medicine without talking with your healthcare provider.

What should I tell my healthcare provider before using pregabalin?

However, these analyses cannot be considered definitive because of the limited number of patients in these categories. Inform patients that pregabalin-related dizziness and somnolence may impair their ability to perform tasks such as driving or operating machinery see Patient Counseling Information (17). Pregabalin capsules 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 (5.2). Your doctor will probably start you on a low dose of pregabalin and may gradually increase your dose during the first week of treatment. This medicine may cause some people to be agitated, irritable, or display other abnormal behaviors.

Based on clinical response and tolerability, dosage may be increased, approximately weekly. In the first study (E1), there was evidence of a dose-response relationship for Pregabalin Oral Route Description total daily doses of pregabalin capsules between 150 mg and 600 mg/day; a dose of 50 mg/day was not effective. In the first study (E1), each daily dose was divided into two equal doses (twice a day dosing). In the second study (E2), each daily dose was divided into three equal doses (three times a day dosing).

Inform patients that pregabalin capsules-related dizziness and somnolence may impair their ability to perform tasks such as driving or operating machinery see Patient Counseling Information (17). Dizziness and somnolence generally began shortly after the initiation of pregabalin capsules therapy and occurred more frequently at higher doses. Dizziness and somnolence were the adverse reactions most frequently leading to withdrawal (4% each) from controlled studies. In pregabalin capsules-treated patients reporting these adverse reactions in short-term, controlled studies, dizziness persisted until the last dose in 30% and somnolence persisted until the last dose in 42% of patients see Drug Interactions (7). Pediatric use information is approved for Pfizer’s LYRICA (pregabalin) Capsules and Oral Solution products.

1 Clinical Trials Experience

Pregabalin is also used for postherpetic neuralgia (pain that occurs after shingles) and pain caused by nerve damage from diabetes or a spinal cord injury. • If you take too much pregabalin, call your healthcare provider or poison control center, or go to the nearest emergency room right away. • Do not drive a car, work with machines, or do other dangerous activities until you know how pregabalin capsules affects you. Your healthcare provider will tell you how much pregabalin to take and when to take it. Pediatric Pharmacokinetics Pediatric use information is approved for Pfizer’s LYRICA (pregabalin) Capsules and Oral Solution products.

What should I do if I accidentally use too much pregabalin?

• Check with your doctor right away if you have pale or blue lips, fingernails, or skin, difficulty or trouble breathing, or irregular, fast or slow, or shallow breathing.
• The following figure displays responder rate by dose for two of the studies.
• Contact a Certified Poison Control Center for up-to-date information on the management of overdose with pregabalin.
• Subset evaluations of the antiseizure efficacy of pregabalin showed no clinically important differences as a function of age, gender, or race.

Similar lesions were not observed in lifetime carcinogenicity studies in two strains of mice or in monkeys treated for 1 year. In view of dose-dependent adverse reactions and since pregabalin is eliminated primarily by renal excretion, adjust the dose in adult patients with reduced renal function. The use of pregabalin capsules in pediatric patients with compromised renal function has not been studied. The recommended dosages for adult patients 17 years of age and older is included in Table 1. Administer the total daily dosage orally in two or three divided doses as indicated in Table 1.

The highest reported accidental overdose of pregabalin during the clinical development program was 8,000 mg, and there were no notable clinical consequences. In the prenatal-postnatal study in rats, pregabalin prolonged gestation and induced dystocia at exposures greater than or equal to 50 times the mean human exposure (AUC(0 to 24) of 123 mcg•hr/mL) at the MRD. Subgroup analyses did not identify an increased risk of PR prolongation in patients with baseline PR prolongation or in patients taking other PR prolonging medications.

• Dizziness and somnolence were the adverse reactions most frequently leading to withdrawal (4% each) from controlled studies.
• Stopping pregabalin suddenly can increase your risk for seizures or withdrawal reactions such as anxiety, diarrhea, headache, trouble sleeping, and nausea.
• Pregabalin capsules, 50 mg are supplied as white, hard gelatin capsule printed with black ink “AN” on cap & “1311” on body.
• There are no adequate studies in women for determining infant risk when using this medication during breastfeeding.

Pediatric

Based on animal studies, there is a potential risk of tumorigenicity with pregabalin exposure via breast milk to the breastfed infant see Nonclinical Toxicology (13.1). Available clinical study data in patients greater than 12 years of age do not provide a clear conclusion about the potential risk of tumorigenicity with pregabalin see Warnings and Precautions (5.8). Because of the potential risk of tumorigenicity, breastfeeding is not recommended during treatment with pregabalin. In clinical studies, following abrupt or rapid discontinuation of pregabalin capsules, some patients reported symptoms including insomnia, nausea, headache or diarrhea see Warnings and Precautions (5.3),consistent with physical dependence. In the postmarketing experience, in addition to these reported symptoms there have also been reported cases of anxiety and hyperhidrosis. Counsel patients that pregabalin may cause edema and weight gain.

Following is a list of treatment-emergent adverse reactions reported by patients treated with pregabalin during all clinical trials. In standard preclinical in vivo lifetime carcinogenicity studies of pregabalin capsules, an unexpectedly high incidence of hemangiosarcoma was identified in two different strains of mice see Nonclinical Toxicology (13.1). Clinical experience during pregabalin capsules premarketing development provides no direct means to assess its potential for inducing tumors in humans. In clinical studies across various patient populations, comprising 6,396 patient-years of exposure in patients greater than 12 years of age, new or worsening-preexisting tumors were reported in 57 patients. Without knowledge of the background incidence and recurrence in similar populations not treated with pregabalin capsules, it is impossible to know whether the incidence seen in these cohorts is or is not affected by treatment.

Although pregabalin capsules were also studied at 600 mg/day, there is no evidence that this dose confers additional significant benefit and this dose was less well tolerated. In view of the dose-dependent adverse reactions, treatment with doses above 300 mg/day is not recommended see Adverse Reactions (6.1). Dizziness and somnolence generally began shortly after the initiation of pregabalin therapy and occurred more frequently at higher doses. In pregabalin-treated patients reporting these adverse reactions in short-term, controlled studies, dizziness persisted until the last dose in 30% and somnolence persisted until the last dose in 42% of patients see Drug Interactions (7).

There have been postmarketing reports of hypersensitivity in patients shortly after initiation of treatment with pregabalin capsules. Adverse reactions included skin redness, blisters, hives, rash, dyspnea, and wheezing. Discontinue pregabalin capsules immediately in patients with these symptoms.

Antiepileptic drugs (AEDs), including pregabalin, increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication. Monitor patients treated with any AED for any indication for the emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior. Pregabalin, at concentrations that were, in general, 10-times those attained in clinical trials, does not inhibit human CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 enzyme systems.

Missed Dose

Pregabalin binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. However, in cultured neurons prolonged application of pregabalin increases the density of GABA transporter protein and increases the rate of functional GABA transport. Pregabalin does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity. It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake. Pregabalin can cause slow or shallow breathing, especially if you are taking another medicine that can cause slowed breathing, such as the opioid medicines codeine or oxycodone, or if you already have breathing problems.

Pregabalin elimination is nearly proportional to creatinine clearance (CLcr) see Dosage and Administration (2.7). Following oral administration of pregabalin capsules under fasting conditions, peak plasma concentrations occur within 1.5 hours. Pregabalin oral bioavailability is greater than or equal to 90% and is independent of dose. Following single- (25 mg to 300 mg) and multiple-dose (75 to 900 mg/day) administration, maximum plasma concentrations (Cmax) and area under the plasma concentration-time curve (AUC) values increase linearly. Following repeated administration, steady-state is achieved within 24 to 48 hours.