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The apparent volume of distribution of pregabalin following oral administration is approximately 0.5 L/kg. Pregabalin is a substrate for system L transporter which is responsible for the transport of large amino acids across the blood brain barrier. Although there are no data in humans, pregabalin has been shown to cross the blood brain barrier in mice, rats, and monkeys. In addition, pregabalin has been shown to cross the placenta in rats and is present in the milk of lactating rats. 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.
Safety and effectiveness in pediatric patients have not been established. There are no adequate and well-controlled studies with LYRICA in pregnant women. Because there are limited data on congestive heart failure patients with New York Heart Association (NYHA) Class III or IV cardiac status, exercise caution when using LYRICA in these patients. LYRICA is contraindicated in patients with known hypersensitivity to pregabalin or any of its pregabalin in usa components.
Do not stop taking this medication without consulting your doctor. Some conditions (such as seizures) may become worse when this drug is suddenly stopped. Also, you may experience symptoms such as difficulty sleeping, nausea, headache and diarrhea. To prevent these symptoms while you are stopping treatment with this drug, your doctor may reduce your dose gradually. This drug works best when the amount of medicine in your body is kept at a constant level.
Patients were permitted up to 4 grams of acetaminophen per day as needed for pain, in addition to pregabalin. Pregabalin pharmacokinetics were evaluated in 358 pediatric patients 3 months to less than 17 years of age with partial-onset seizures at dose levels of 2.5, 5, 10, and 15 mg/kg/day after single and multiple oral administration of pregabalin. Following oral administration, pregabalin reaches peak plasma concentration at 0.5 hours to 2 hours in the fasted state. Both apparent clearance (CL/F) and apparent volume of distribution increase as body weight increases. A weight-based dosing regimen is necessary to achieve pregabalin exposures in pediatric patients 1 month to less than 17 years of age similar to those observed in adults treated for partial-onset seizures at effective doses see Dosage and Administration (2.4). The mean t½ is 3 to 4 hours in pediatric subjects up to 6 years of age, and 4 to 6 hours in those 7 years of age and older.


