PREGABALIN is indicated as a treatment for peripheral neuropathic pain and as an adjunctive therapy for partial seizures in patients with epilepsy. The dose range is 150 to 600 mg per day given in either two or three divided doses. Pregabalin is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalisation. Pregabalin may be taken with or without food.
Neuropathic pain: Pregabalin treatment can be started at a dose of 150 mg per day. Based on individual patient response and tolerability, the dosage may be increased to 300 mg per day after an interval of 3 to 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. Based on individual patient response and tolerability, the dosage may be increased to 300 mg per day after 1 week. The maximum dosage of 600 mg per day may be achieved after an additional week. Discontinuation of pregabalin: In accordance with current clinical practice, if pregabalin has to be discontinued either in neuropathic pain or epilepsy, it is recommended this should be done gradually over a minimum of 1 week.
Pregabalin binds to an auxiliary subunit (a2-d protein) of voltage-gated calcium channels in the central nervous system, potently displacing [3H]-gabapentin.
The most commonly reported adverse reactions of PREGABALIN are dizziness and somnolence. Other commonly reported side effects include Appetite increased, Euphoric mood, confusion, libido decreased, irritability,
Dizziness, somnolence, Vision blurred, diplopia, Vertigo, Dry mouth, constipation, vomiting, flatulence, fatigue, oedema peripheral, feeling drunk, oedema, gait abnormal.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. In accordance with current clinical practice, some diabetic patients who gain weight on pregabalin treatment may need to adjust hypoglycaemic medications.
Pregabalin treatment has been associated with dizziness and somnolence, which could increase the occurrence of accidental injury (fall) in the elderly population. Therefore, patients should be advised to exercise caution until they are familiar with the potential effects of the medication. There are insufficient data for the withdrawal of concomitant antiepileptic medicinal products, once seizure control with pregabalin in the add-on situation has been reached, in order to reach monotherapy on pregabalin.
Since pregabalin is predominantly excreted unchanged in the urine, undergoes negligible
metabolism in humans (<2% of a dose recovered in urine as metabolites), does not inhibit drug metabolism in vitro, and is not bound to plasma proteins, it is unlikely to produce, or be subject to, pharmacokinetic interactions. Accordingly, in in vivo studies no clinically relevant pharmacokinetic interactions were observed between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol. Population pharmacokinetic analysis indicated that oral antidiabetics, diuretics, insulin, phenobarbital, tiagabine and topiramate had no clinically significant effect on pregabalin clearance.
Co-administration of pregabalin with the oral contraceptives norethisterone and/or ethinyl oestradiol does not influence the steady-state pharmacokinetics of either substance.
Multiple oral doses of pregabalin co-administered with oxycodone, lorazepam, or ethanol did not result in clinically important effects on respiration. Pregabalin appears to be additive in the impairment of cognitive and gross motor function caused by oxycodone. Pregabalin may potentiate the effects of ethanol and lorazepam.
No specific pharmacodynamic interaction studies were conducted in elderly volunteers.
Pregabalin is an effective, rapidly acting, and safe treatment for generalized anxiety disorder. In short-term treatment, pregabalin does not appear to have the withdrawal symptoms associated with the benzodiazepines.
PREGABALIN is a 3-substituted analogue of gamma-amino butyric acid (GABA) and a compound related to the antiepileptic drug gabapentin. PREGABALIN will be indicated as adjunctive therapy for partial seizures in epilepsy, for treatment of neuopathic pain, including diabetic peripheral neuropathy, and for treatment of generalised anxiety disorder. PREGABALIN is binds to calcium channels and modulates calcium influx as well as influencing GABergic neurotransmission. This mode of action translates into anti-epileptic, analgesic and anxiolytic effects. Because it is more potent than its predacessor Neurontin (gabapentin), Pregabalin achieves efficacy at lower doses. This increases its therapeutic index with respect to gabapentin and should lead to fewer dose-related side effects.
List of excipients include:
Capsule content:
Lactose monohydrate
Maize starch
Talc
Capsule shell:
Gelatin
Titanium Dioxide (E171)
Sodium Laurilsulfate
Silica, colloidal anhydrous
Purified water
75 mg, 100 mg, 200 mg and 300 mg shells only:
Red Iron Oxide (E172)
Printing Ink :
Shellac
Black Iron Oxide (E172)
Propylene Glycol
Potassium Hydroxide