Nevraxa 200
International non-proprietary name:
Pregabalin.
Ingredients:
Each hard gelatin capsule contains 150, 200 and 300 mg of pregabalin.
Pharmacotherapeutic group:
Analgesics, Other analgesics and antipyretics, Gabapentinoids.
Pharmacological properties
Pharmacodynamics
The active substance is pregabalin, a derivative of gamma-aminobutyric acid [(S)-3-(aminomethyl)-5-methylhexane acid)] is an analogue .
Mechanism of action
Pregabalin binds to an auxiliary subumit (α2-δ protein) of voltage-gated calcium channels in the central nervous system.
Pharmacokinetics
Pregabalin steady-state pharmacokinetics are similar in healthy volunteers, patients with epilepsy receiving anti-epileptic drugs and patients with chronic pain.
Absorption
Pregabalin is rapidly absorbed when administered in the fasted state, with peak plasma concentrations occurring within 1hour following both single and multiple dose administration. Pregabalin oral bioavailability is estimated to be ≥ 90% andis independent of dose. Following repeated administration, steady state is achieved within 24 to 48 hours. The rate ofpregabalin absorption is decreased when given with food resulting in a decrease in Cmax by approximately 25-30% anda delay in tmax to approximately 2.5 hours. However, administration of pregabalin with food has no clinically significanteffect on the extent of pregabalin absorption.
Distribution
In preclinical studies, pregabalin has been shown to cross the blood brain barrier in mice, rats, and monkeys. Pregabalinhas been shown to cross the placenta in rats and is present in the milk of lactating rats. In humans, the apparent volumeof distribution of pregabalin following oral administration is approximately 0.56 l/kg. Pregabalin is not bound to plasmaproteins..
Biotransformation
Pregabalin undergoes negligible metabolism in humans. Following a dose of radiolabelled pregabalin, approximately 98% of the radioactivity recovered in the urine was unchanged pregabalin. The N-methylated derivative of pregabalin,the major metabolite of pregabalin found in urine, accounted for 0.9% of the dose. In preclinical studies, there was noindication of racemisation of pregabalin S-enantiomer to the R-enantiomer.
Elimination
Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. Pregabalin meanelimination half-life is 6.3 hours. Pregabalin plasma clearance and renal clearance are directly proportional to creatinineclearance.
Dose adjustment in patients with reduced renal function or undergoing haemodialysis is necessary.
Instructions for use
Neuropathic pain
Nevraxa® is indicated for the treatment of peripheral and central neuropathic pain in adults.
Epilepsy
Nevraxa® is indicated as adjunctive therapy in adults with partial seizures with or without secondarygeneralisation.
Generalised Anxiety Disorder
Nevraxa® is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
Contraindications
Hypersensitivity to the active substance or any of the excipients included in the composition of the drug.
Directions for use and dosage
Dosage regimen
The drug is prescribed in a dose range of 150-600 mg in two or three doses daily.
Neuropathic pain
Pregabalin treatment can be started at a dose of 150 mg per day given as two or three divided doses.
Based on individual patient response and tolerability, the dose may be increased to 300 mg per day after an interval of 3to 7 days, and if needed, to a maximum dose of 600 mg per day after an additional 7-day interval.
Epilepsy
Pregabalin treatment can be started with a dose of 150 mg per day given as two or three divided doses. Based onindividual patient response and tolerability, the dose may be increased to 300 mg per day after 1 week. The maximumdose of 600 mg per day may be achieved after an additional week.
Generalized anxiety disorder
The dose range is 150 to 600 mg per day given as two or three divided doses. The need for treatment should bereassessed regularly.
Pregabalin treatment can be started with a dose of 150 mg per day. Based on individual patient response and tolerability,the dose may be increased to 300 mg per day after 1 week. Following an additional week the dose may be increased to 450 mg per day. The maximum dose of 600 mg per day may be achieved after an additional week.
Method of administration
Nevraxa ® may be taken with or without food.
Nevraxa ® is for oral use only.
Release form
Hard gelatin capsules No.7, in Alu-PVC blisters . No. 4 blisters are packed in a cardboard box together with an insert leaflet.
Storage conditions
Store at a temperature below 25℃. Protect from light and moisture
Pharmacy discharge condition
It is available on prescription.
Manufactured for:
OPES HEALTHCARE UK LIMITED 71-75 Shelton Street, London, England, United Kingdom, WC2H 9JQ at OPES HEALTHCARE PRIVATE LIMITED Ahmedabad, Gujarat, India.