Pregabalin (PGB, LYRICA®) was initially approved as an adjunctive treatment for partial seizures. Additional indications for PGB include anxiety, fibromyalgia, postherpetic neuralgia, diabetic peripheral neuropathy, and spinal cord injury-related neuropathic pain. It is also used for treating sciatica, irritable bowel syndrome, and postoperative pain. The recommended PGB dosage is 150–600 mg/day in patients 17 years of age and older, 2.5–10 mg/kg/day (not to exceed 600 mg/day) in pediatric patients weighing 30 kg or more, and 3.5–14 mg/kg/day in pediatric patients weighing between 11 kg to less than 30 kg.13 The structure and mechanism of action of PGB are similar to those of gabapentin (GBP). They potently bind to the auxiliary alpha-2-delta (α2δ) subunit of voltage-gated calcium channels, which reduces the calcium influx and mediates pharmacological activity by inhibiting the release of various neurotransmitters, such as noradrenaline and glutamate. 

Most common adverse reactions of PGB in adults and children are somnolence and dizziness, which are dose-dependent in their severity and incidence. The mean oral bioavailability PGB is approximately 90% or more, of which approximately 98% is renally excreted unchanged and less than 2% is metabolized to N-methyl-pregabalin.18 Pharmacokinetic (PK) studies of PGB in healthy people demonstrated that its PK characteristics are linear, and the maximum plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC) are proportional to the dose. PGB reaches the maximal plasma concentration (Tmax) approximately 1 h after administration and has a mean plasma elimination half-life (t1/2) of approximately 6 h in adult patients; both parameters are dose-independent. The apparent volume of distribution at steady state (Vss) is approximately 0.5 L/kg.19 PGB has low drug-drug interactions potential, as it is barely metabolized and does not bind to plasma proteins.15,19 As indicated in a previous study, PGB clearance is proportional to creatinine clearance (CLcr), and therefore, dose adjustments are recommended for adult patients with renal impairment (RI).

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Mishita
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Journal of Clinical & Experimental Nephrology