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NEUREXAL
PREGABALIN
DESCRIPTION
Each hard capsule contains 75 or 150 mg of pregabalin
Excipients: Lactose monohydrate, Cornstarch, Talc.
NEUREXAL 75 mg: Capsule shell contains erythrosine, indigo carmine, gelatin and titanium dioxide
NEUREXAL 150 mg: Capsule shell contains indigotine, titanium dioxide and gelatin.
PHARMACOLOGICAL PROPERTIES
Pregabalin, is a gramma-aminobutyric acid analogue ((S)-3-(aminomethyl)-5-methylhexanoic acid). Pregabalin binds to an auxiliary
subunit (α2-δ protein) of voltage-gated calcium channels in the central nervous system, potently displacing [3H]-gabapentin.
Pregabalin steady-state pharmacokinetics are similar in healthy volunteers, patients with epilepsy receiving anti-epileptic drugs and
patients with chronic pain. Pregabalin oral bioavailability is estimated to be ≥ 90% and is independent of dose. Pregabalin is eliminated
from the systemic circulation primarily by renal excretion as unchanged drug. Pregabalin mean elimination half-life is 6.3 hours.
Pregabalin pharmacokinetics are linear over the recommended daily dose range. Therefore there is no need for routine monitoring
of plasma concentration of pregabalin.
THERAPEUTIC INDICATIONS
- Treatment for peripheral and central neuropathic pain in adults
- As adjunctive therapy in adults with partial seizures with or without secondary generalization
- Treatment of Generalized Anxiety Disorder in adults
POSOLOGY AND METHOD OF ADMINISTRATION
The dose range is 150 to 600 mg per day given by mouth in either two or three divided doses. NEUREXAL may be taken with or
without food.
Neuropathic pain
Treatment can be started at 150mg per day. Based on individual patient response and tolerability, the dose 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
Treatment can be started at 150mg per day. Based on individual patient response and tolerability, the dose may be increased to 300
mg per day after 1 week. The maximum dose of 600 mg per day may be achieved after an additional week.
Generalized Anxiety Disorder
The need for treatment should be reassessed regularly.
Treatment can be started at 150mg 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.
Discontinuation of Pregabalin
If Pregabalin has to be discontinued it is recommended this should be done gradually over a minimum of 1 week independent of the
indication.
Patients with renal impairment
Dose reduction in patients with compromised renal function must be individualized according to creatinine clearance, as indicated in
Table 1.
Pregabalin is removed effectively from plasma by hemodialysis (about 50% decrease in plasma concentration in 4 hours). For
patients undergoing hemodialysis, adjust the pregabalin daily dose based on renal function. In addition to the daily dose, administer
a supplementary dose immediately following every 4-hour hemodialysis treatment (see Table 1).
Table 1. Pregabalin Dose Adjustment Based on Renal Function
Creatinine Clearance
(CLcr) (ml/min)
Total Pregabalin Daily Dose
(mg/day)*
Dose Regimen
Starting Dose
Maximum Dose
≥ 60
150
600
BID or TID
≥ 30 - < 60
75
300
BID or TID
≥15 - < 30
25 - 50
150
Once Daily or BID
<15
25
75
Once Daily
100
Single Dose†
Supplementary dosage following hemodialysis (mg)
25
TID= Three divided doses
BID = Two divided doses
* Total daily dose (mg/day) should be divided as indicated by dose regimen to provide mg/dose.
† Supplementary dose is a single additional dose.
Patients with hepatic impairment
No dose adjustment is required.
Use in children (< 12 years old) and adolescents ( 12 - 17 years old)
Not recommended.
Use in the elderly over 65 years
May require a dose reduction due to a decreased renal function. (Refer to Table 1)
CONTRAINDICATIONS
Hypersensitivity to the active substance or to any of the excipients.
SPECIAL WARNINGS AND PRECAUTIONS FOR USE
- Some diabetic patients who gain weight on Pregabalin treatment may need to adjust hypoglycemic medications.
- Hypersensitivity reactions, including cases of angioedema have been reported after the use of pregabalin. Pregabalin should be
discontinued immediately if symptoms of angioedema, such as facial, perioral, or upper airway swelling occur.
- Visual adverse reactions have also been reported, including loss of vision, visual blurring or other changes of visual acuity, many of
which were transient. Discontinuation of pregabalin may result in resolution or improvement of these visual symptoms.
- Convulsions, including status epilepticus and grand mal convulsions, may occur during pregabalin use or shortly after discontinuing
pregabalin.
- Congestive heart failure in some patients receiving pregabalin has been reported, mostly in elderly cardiovascular compromised
patients during treatment for a neuropathic indication. Discontinuation of pregabalin may resolve the reaction.
- Patients with a history of substance abuse should be monitored for symptoms of pregabalin abuse.
- Cases of encephalopathy have been reported, mostly in patients with underlying conditions that may precipitate encephalopathy.
- Pregabalin treatment has been associated with dizziness and somnolence, which could increase the occurrence of accidental injury
in elderly population. Cases of loss of consciousness, confusion and mental impairment have also been reported. 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 medical products, once seizure control with pregabalin in
the add-on situation has been reached, in order to reach monotherapy on pregabalin.
- After discontinuation of short-term and long-term treatment with pregabalin withdrawal symptoms have been observed in some
patients, (e.g. insomnia, headache, nausea, diarrhoea, flu syndrome, nervousness, depression, pain, sweating and dizziness). The
patient should be informed about this at the start of the treatment. Concerning discontinuation of long-term treatment of pregabalin
there are no data of the incidence and severity of withdrawal symptoms in relation to duration of use and dosage of pregabalin.
- Patients with rare hereditary problems of galatose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption
should not take this medicine.
- In the treatment of central neuropathic pain due to spinal cord injury the incidence of adverse events in general, central nervous
system adverse events and especially somnolence was increased. This may be attributed to an additive effect due to concomitant
medication (e.g. anti-spasticity agents) needed for this condition.
- Cases of renal failure have been reported. Some cases were reversible upon discontinuation of treatment.
- Patients should be monitored for signs of suicidal ideation and behaviors. Appropriate treatment should be considered.
- When pregabalin and opioids are co-administered, measures to prevent constipation may be considered (especially in female
patients and elderly).
Interaction with other medicinal products and other forms of interaction
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 as well as other central nervous system depressant medicinal products.
No specific pharmacodynamic interaction data is available in elderly volunteers.
Pregnancy and lactation
Neurexal should not be used during pregnancy unless clearly necessary (if the benefit to the mother clearly outweighs the potential
risk to the foetus). Effective contraception must be used in women of child bearing potential. Breast-feeding is not recommended
during treatment with pregabalin.
Effects on ability to drive and use machines
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.
UNDESIRABLE EFFECTS
Adverse reactions are usually mild to moderate in intensity.
Very Common adverse reactions: dizziness and somnolence.
Common adverse reactions: appetite increase, psychiatric disorders (euphoric mood, confusion, irritability, libido decrease,
disorientation, insomnia), nervous system disorders (ataxia, coordination abnormal, tremor, dysarthria, memory impairment,
disturbance in attention, paraesthesia, sedation, balance disorder, lethargy), eye disorders (vision blurred, diplopia), vertigo,
gastro-intestinal disorders (vomiting, dry mouth, constipation, flatulence) , erectile dysfunction, gait abnormal, feeling drunk, fatigue,
oedema peripheral, oedema, weight increase.
Uncommon adverse reactions: nasopharyngitis, anorexia, hypoglycaemia, psychiatric disorders (hallucination, panic attack,
restlessness, agitation, depression, depressed mood, mood swings, depersonalisation, word finding difficulty, abnormal dreams,
libido increased, anorgasmia, apathy), nervous system disorders (syncope, stupor, myoclonus, psychomotor hyperactivity, ageusia,
dyskinesia,
dizziness postural, intention tremor, nystagmus, cognitive disorder, speech disorder, hyporeflexia, hypoaesthesia,
amnesia, hyperaesthesia, burning sensation), eye disorders (visual disturbance, eye swelling, visual field defect,
visual acuity reduced, eye pain, asthenopia, dry eye, lacrimation increase), hyperacusis, tachycardia, atrioventricular
block first degree, flushing, hot flushes, hypotension, hypertension, dyspnoea, nasal dryness, gastrointestinal
disorders (abdominal distension, gastrooesophageal reflux disease, salivary hypersecretion,
hypoaesthesia oral), rash papular, sweating, muscle twitching,
joint swelling, muscle cramp, myalgia, arthralgia, back pain, pain in limb, muscle stiffness, urinary incontinence, dysuria,
ejaculation delay, sexual dysfunction, fall, chest tightness, asthenia, thirst, pain, feeling abnormal, chills, blood creatine
phosphokinase increase, alanine aminotransferase increase, aspartate aminotransferase increase, platelet count decrease.
Rare adverse reactions: neutropenia, disinhibition, elevated mood, hypokinesia, parosmia, dysgraphia, eye disorders
(peripheral vision loss, oscillopsia, altered visual depth perception, photopsia, eye irritation, mydriasis, strabismus, visual brightness),
sinus tachycardia, sinus bradycardia, sinus arrhythmia, peripheral coldness, epistaxis, throat tightness, cough, nasal congestion,
rhinitis, snoring, ascites, pancreatitis, dysphagia, urticaria, cold sweat, rhabdomyolysis, cervical spasm, neck pain, renal failure,
oliguria, amenorrhoea, breast discharge, breast pain, dysmenorrhoea, hypertrophy breast, generalised oedema, pyrexia, blood
glucose increase, blood potassium decrease, white blood cell count decrease, blood creatinine increase, weight decrease.
Adverse reactions with unknown frequency: hypersensitivity, angioedema, allergic reaction, aggression, loss of
consciousness, mental impairment, convulsions, headache, malaise, vision loss , keratitis, congestive heart failure, QT prolongation,
pulmonary oedema, swollen tongue, diarrhoea, nausea, Stevens Johnson syndrome, pruritus, urinary retention, face oedema.
The adverse reactions mentioned may also be associated with the underlying disease and / or concomitant medications.
OVERDOSE
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.
HOW SUPPLIED
Neurexal 75 mg: Box of 14 capsules, each containing pregabalin 75 mg, excipient q.s. 1 capsule. Reg. Nº Lebanon 167719/10
Neurexal 150 mg: Box of 30 capsules, each containing pregabalin 150 mg, excipient q.s. 1 capsule. Reg. Nº Lebanon 167720/10
- Do not store above 30ºC. Do not refrigerate. Keep away from light and humidity.
- Keep out of the reach of children.
- Do not use after the expiry date shown on the blister and the outer packaging.
- Do not use if there is visible sign of deterioration.
- To be dispensed only by or on the prescription of a physician.
This is a medicament
- A medicament is a product which affects your health, and its consumption contrary to instructions is dangerous for you.
- Follow strictly the doctor’s prescription, the method of use and the instructions of the pharmacist who sold the medicament.
- The doctor and the pharmacist are experts in medicine, its benefits and risks.
- Do not by yourself interrupt the period of treatment prescribed for you.
- Do not repeat the same prescription without consulting your doctor.
Keep medicaments out of reach of children
Pharmaline - Lebanon
NEUREXAL is a Registered Trademark
Council of Arab Health Ministers Union of Arab Pharmacists
Rev. Nº 02/2011
905083-A