Neufar

Neufar

pregabalin

Manufacturer:

Fahrenheit
Full Prescribing Info
Contents
Pregabalin.
Description
Each capsule contains Pregabalin 75 mg.
Each capsule contains Pregabalin 150 mg.
Action
Pharmacology: The active substance, pregabalin, is a gamma-aminobutyric acid analogue ((S)-3-(aminomethyl)-5- methylhexanoic acid).
Mechanism of action: Pregabalin binds to an auxiliary subunit (α2-δ protein) of voltage-gated calcium channels in the central nervous system, potently displacing [3H]-gabapentin.
Pharmacokinetics: Absorption: Although the mechanism of Pregabalin absorption is unknown, it has been proposed that, as for Gabapentin, Pregabalin should be a substrate for the L-amino acid transport system. Bioavailability studies with Pregabalin single dose in healthy volunteers showed proportional values of maximum concentration (Cmax) and area under the curve (AUC), a time to maximum concentration (T½) of about 1 hour, a half life (t½) of about 5-7 hours and an oral bioavailability of 90%.
The simultaneous consumption of food with Pregabalin can reduce Cmax, by 25 - 30%, and increase the Tmax to 3 hours. The serum concentrations for healthy volunteers obtained with a single dose of 200 mg of Pregabalin was 5.96 mg/ml. The drug does not bind to protein.
Distribution: An apparent volume of distribution following oral administration approximately 0.5 l/kg.
Elimination: Pregabalin does not bind to proteins plasma and it is not substantially metabolized in humans. Its only N-methylated metabolite is found in urine at 0.9% of the dose. and is not expected to be an inducer of liver enzymes.
Indications/Uses
Neuropathic pain: Pregabalin is indicated for the treatment of peripheral neuropathic pain in adults.
Epilepsy: Pregabalin is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalization.
Dosage/Direction for Use
The dose range is 150 to 600 mg per day given in either two or three divided doses.
Pregabalin is given with or without food.
Neuropathic pain: The recommended starting dose for pregabalin is 75 mg BID (150 mg/day), with or without food. In clinical trials, the efficacy of pregabalin was demonstrated in patients dosed in a range of 150 to 600 mg/day. For the majority of patients, 150 mg BID will be the optimal dose. Efficacy of pregabalin has been demonstrated within the first week. However, based on individual patient response and tolerability, the dose may be increased to 150 mg BID after an interval of 3 to 7 days, and if needed, to a maximum dose of 300 mg BID after an additional week.
Epilepsy: The recommended effective starting dose for pregabalin is 75 mg BID (150 mg/day), with or without food. In clinical trials, the efficacy of pregabalin was demonstrated in patients dosed in a range of 150 to 600 mg/day. Efficacy of pregabalin has been demonstrated as early as 1 week. However, based on individual patient response and tolerability, the dose may be increased to 150 mg BID after 1 week, and if needed, to a maximum dose of 300 mg BID 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.
Patients with renal impairment: Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. As pregabalin clearance is directly proportional to creatinine clearance, dosage reduction in patients with compromised renal function must be individualized according to creatinine clearance (CLcr), as indicated in Table 1 determined using the following formula:


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Pregabalin is removed effectively from plasma by haemodialysis (50% of drug in 4 hours). For patients receiving haemodialysis, the pregabalin daily dose should be adjusted based on renal function. In addition to the daily dose, a supplementary dose should be given immediately following every 4-hour haemodialysis treatment (see Table 1).


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Use in patients with hepatic impairment: No dosage adjustment is required for patients with hepatic impairment.
Use in Children and adolescents (12 to 17 years of age): The safety and effectiveness of pregabalin in pediatric patients below the age of 12 years and adolescent has not been established.
The use in children is not recommended.
Use in elderly (over 65 years of age): Elderly patients may require dose reduction of pregabalin due to a decreased renal function.
Overdosage
In overdoses up to 15 g, no unexpected adverse reactions were reported. Treatment of pregabalin overdose should include general supportive measures and may include haemodialysis if necessary (see Dosage & Administration).
Contraindications
Hypersensitivity to the active substance or to any of the excipients.
Special Precautions
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 hypoglycemic 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 effect 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.
Effects on ability to drive and use machines: Pregabalin may cause dizziness and somnolence. Therefore patients are advised not to drive, operate complex machinery or engage in other potentially hazardous activities until it is known whether this medication affects their ability to perform these activities.
Use In Pregnancy & Lactation
There are no adequate data on the use of pregabalin in pregnant women.
Studies in animals have shown reproductive toxicity. The potential risk to humans is unknown. Therefore, pregabalin should not be used during pregnancy unless the benefit to the mother clearly outweighs the potential risk to the foetus.
It is not known if pregabalin is excreted in the breast milk of humans; however, it is present in the milk of rats. Therefore, breast-feeding is not recommended.
Effective contraception may be used in women of child bearing potential
Adverse Reactions
In the table as follows, all adverse reactions, which occurred at an moidence greater than placebo and in more than one patient, are listed by class and frequency {very common (>1/10), common (>1/100, < /10), uncommon (>1/1000, <1/100) and rare (<1/100)}.
The adverse reactions listed may also be associated with the underlying disease and/or concomitant medications. (See Table 2.)


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The following adverse events were reported during post-Marketing Surveillance: Nervous system disorders: Headache.
Gastrointestinal disorders: Rare cases of swollen tongue have been reported. Nausea.
Skin and subcutaneous tissue disorders: Rare cases of face swelling have been reported.
Drug Interactions
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.
No clinically relevant pharmacokinetic interactions were observed between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol. 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 agent.
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.
Storage
Store below 30°C.
MIMS Class
ATC Classification
N03AX16 - pregabalin ; Belongs to the class of other antiepileptics.
Presentation/Packing
Cap 75 mg x 3 x 10's. 150 mg x 3 x 10's.
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