Aloja

Aloja

pregabalin

Manufacturer:

Mylan Healthcare

Distributor:

DKSH
Full Prescribing Info
Contents
Pregabalin.
Description
Aloja 75: Each Capsule contains: Pregabalin 75 mg, Excipients q.s.
Aloja 150: Each capsule contains Pregabalin 150 mg, Excipients q.s.
Excipients/Inactive Ingredients: Capsule content: Low substituted hydroxypropyl cellulose, Maize starch, Talc.
Capsules shell: Iron oxide yellow, Titanium dioxide, Erythrosine, Gelatin.
Imprinting Ink: Shellac, Ethanol Anhydrous, Isopropyl alcohol, Butyl alcohol, Propylene Glycol, Ammonia Solution Concentrated, Black Iron Oxide, Potassium Hydroxide, Purified Water.
Action
Pharmacotherapeutic Group: Anti-epileptics, other anti-epileptics. ATC Code: N03AX16.
Pharmacological classification: 13.1 Anticonvulsants.
The active substance, pregabalin, is a gamma-aminobutyric acid analogue [(S)-3-(aminomethyl)-5-methylhexanoic acid].
Pharmacology: Pharmacodynamics: Mechanism of action: Pregabalin binds to an auxiliary subunit (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.
Distribution: In humans, the apparent volume of distribution of pregabalin following oral administration is approximately 0.56 l/kg. Pregabalin is not bound to plasma proteins.
Biotransformation: Pregabalin undergoes negligible metabolism in humans. Following a dose of radiolabeled pregabalin, 98% of the radioactivity recovered in the urine was unchanged. The N-methylated derivative of pregabalin, the major metabolite of pregabalin found in urine.
Elimination: Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug.
Dose adjustment in patients with reduced renal function or undergoing haemodialysis is necessary.
Linearity/non-linearity: Pregabalin pharmacokinetics are linear over the recommended daily dose range. Inter-subject pharmacokinetic variability for pregabalin is low. Multiple dose pharmacokinetics are predictable from single-dose. Therefore, there is no need for routine monitoring of plasma concentrations of pregabalin.
Gender: Gender does not have a clinically significant influence on the plasma concentrations of pregabalin.
Renal impairment: Pregabalin clearance is directly proportional to creatinine clearance. In addition, pregabalin is effectively removed from plasma by haemodialysis. Because renal elimination is the major elimination pathway, dose reduction in patients with renal impairment and dose supplementation following haemodialysis is necessary.
Hepatic impairment: Since pregabalin does not undergo significant metabolism and is excreted predominantly as unchanged drug in the urine, impaired liver function would not be expected to significantly alter pregabalin plasma concentrations.
Elderly (over 65 years of age): Pregabalin clearance tends to decrease with increasing age. This decrease in pregabalin oral clearance is consistent with decreases in creatinine clearance associated with increasing age. Reduction of pregabalin dose may be required in patients who have age related compromised renal function.
Indications/Uses
Neuropathic pain: Pregabalin is indicated for the treatment of peripheral and central neuropathic pain in adults.
Epilepsy: Pregabalin is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalisation.
Generalised Anxiety Disorder: Pregabalin is indicated for the treatment of Generalised Anxiety Disorder (GAD) in adults.
Fibromyalgia: Pregabalin is indicated for the management of fibromyalgia.
Dosage/Direction for Use
Posology: The dose range is 150 to 600 mg per day given in either two or three divided doses.
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 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 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 1 week. The maximum dose of 600 mg per day may be achieved after an additional week.
Generalised Anxiety Disorder: The dose range is 150 to 600 mg per day given as two or three divided doses. The need for treatment should be reassessed 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.
Fibromyalgia: The recommended dose of pregabalin is 300-450 mg/day given in two divided doses. Dosing should begin at 75 mg 2 times a day (150 mg/ day) and may be increased to 150 mg 2 times a day (300 mg/day) within 1 week based on efficacy and tolerability. Patients who do not experience sufficient benefit with 300 mg/day may be further increased to 225 mg 2 times a day (450 mg/day). If needed, in some patients, based on individual response and tolerability, the dose may be increased to maximum dosage of 600 mg/day after an additional week.
Discontinuation of pregabalin: In accordance with current clinical practice, if pregabalin has to be discontinued, it is recommended this should be done gradually over a minimum of 1 week independent of the indication (see Precautions and Adverse Reactions).
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 (see Pharmacology: Pharmacokinetics under Actions), dose reduction in patients with compromised renal function must be individualised according to creatinine clearance (CLcr), as indicated in Table 1 determined using the following formula: (see Equation).

Click on icon to see table/diagram/image

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).

Click on icon to see table/diagram/image

Patients with hepatic impairment: No dose adjustment is required for patients with hepatic impairment (see Pharmacology: Pharmacokinetics under Actions).
Paediatric population: The safety and efficacy of Pregabalin in children below the age of 12 years and in adolescents (12-17 years of age) have not been established. Currently available data are described in Adverse Reactions, Pharmacology: Pharmacodynamics and Pharmacokinetics under Actions but no recommendation on a posology can be made.
Elderly (over 65 years of age) population: Elderly patients may require a dose reduction of pregabalin due to a decreased renal function (see patients with renal impairment).
Method of administration: Pregabalin may be taken with or without food. Pregabalin is for oral use only.
Overdosage
Patient may experience the most commonly adverse reactions when pregabalin was taken in overdose included somnolence, confusional state, agitation, and restlessness.
In rare occasions, cases of coma might be experience.
Treatment of pregabalin overdose should include general supportive measures and may include haemodialysis if necessary (see Dosage & Administration Table 1).
Contraindications
Hypersensitivity to the active substance or to any of the excipients listed in Description.
Special Precautions
Diabetic patients: Some diabetic patients who gain weight on pregabalin treatment may need to adjust hypoglycaemic medicinal products.
Hypersensitivity reactions: Pregabalin should be discontinued immediately if experienced symptoms hypersensitivity reaction include angioedema, such as facial, perioral, or upper airway swelling occur.
Dizziness, somnolence, loss of consciousness, confusion and mental impairment: Pregabalin treatment has been associated with dizziness and somnolence, which could increase the occurrence of accidental injury (fall) in the elderly population. There have chances to experience of loss of consciousness, confusion and mental impairment. Therefore, patients should be advised to exercise caution until they are familiar with the potential effects of the medicinal product.
Vision-related effects: In the postmarketing experience, 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.
Renal failure: Reversible renal failure may occur with discontinuation of pregabalin.
Withdrawal of concomitant anti-epileptic medicinal products: 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.
Withdrawal symptoms: After discontinuation of short-term and long-term treatment with pregabalin, withdrawal symptoms have been observed in some patients. The following events have been mentioned: insomnia, headache, nausea, anxiety, diarrhoea, flu syndrome, nervousness, depression, pain, convulsion, hyperhidrosis and dizziness, suggestive of physical dependence. The patient should be informed about this at the start of the treatment.
Convulsions, including status epilepticus and grand mal convulsions, may occur during pregabalin use or shortly after discontinuing pregabalin.
Concerning discontinuation of long-term treatment of pregabalin, data suggest that the incidence and severity of withdrawal symptoms may be dose-related.
Congestive heart failure: There have been postmarketing reports of congestive heart failure in some patients receiving pregabalin. These reactions are mostly seen in elderly cardiovascular compromised patients during pregabalin treatment for a neuropathic indication. Pregabalin should be used with caution in these patients. Discontinuation of pregabalin may resolve the reaction.
Treatment of central neuropathic pain due to spinal cord injury: In the treatment of central neuropathic pain due to spinal cord injury the incidence of adverse reactions in general, central nervous system adverse reactions and especially somnolence was increased. This may be attributed to an additive effect due to concomitant medicinal products (e.g. anti-spasticity agents) needed for this condition. This should be considered when prescribing pregabalin in this condition.
Suicidal ideation and behaviour: Suicidal ideation and behaviour have been reported in patients treated with anti-epileptic agents in several indications. The mechanism of this risk is not known and the available data do not exclude the possibility of an increased risk for pregabalin.
Therefore patients should be monitored for signs of suicidal ideation and behaviours and appropriate treatment should be considered. Patients (and caregivers of patients) should be advised to seek medical advice should signs of suicidal ideation or behaviour emerge.
Potential for an increase in risk of suicidal thoughts or behavior.
Reduced lower gastrointestinal tract function: Reduced lower gastrointestinal tract function (e.g. Intestinal obstruction, paralytic ileus, constipation) when pregabalin was co-administered with medications that have the potential to produce constipation, such as opioid analgesics. When pregabalin and opioids will be used in combination, measures to prevent constipation may be considered (especially in female patients and elderly).
Misuse, abuse potential or dependence: Caution should be exercised in patients with a history of substance abuse and the patient should be monitored for symptoms of pregabalin misuse, abuse or dependence (development of tolerance, dose escalation, drugseeking behaviour have been reported).
Encephalopathy: Patients with underlying conditions that may precipitate encephalopathy are at risk to develop encephalopathy.
Effects on ability to drive and use machines: Pregabalin may have minor or moderate influence on the ability to drive and use machines. Pregabalin may cause dizziness and somnolence and therefore may influence the ability to drive or use machines. Patients are advised not to drive, operate complex machinery or engage in other potentially hazardous activities until it is known whether this medicinal product affects their ability to perform these activities.
Use In Pregnancy & Lactation
Women of childbearing potential/Contraception in males and females: As the potential risk for humans is unknown, effective contraception must be used in women of child bearing potential.
Pregnancy: There are no adequate data from the use of pregabalin in pregnant women.
The potential risk for humans is unknown, although reproductive toxicity is reported in animals.
Pregabalin should not be used during pregnancy unless clearly necessary (if the benefit to the mother clearly outweighs the potential risk to the foetus).
Breast-feeding: Pregabalin is excreted into human milk. The effect of pregabalin on newborns/infants is unknown. A decision must be made whether to discontinue breast-feeding or to discontinue pregabalin therapy taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman.
Fertility: There are no clinical data on the effects of pregabalin on female fertility.
Adverse Reactions
The most commonly reported adverse reactions were dizziness and somnolence. Adverse reactions were usually mild to moderate in intensity. The most common adverse reactions resulting in discontinuation from pregabalin treatment groups were dizziness and somnolence.
The adverse reactions listed may also be associated with the underlying disease and/or concomitant medicinal products.
In the treatment of central neuropathic pain due to spinal cord injury the incidence of adverse reactions in general, CNS adverse reactions and especially somnolence was increased.
Infections and infestations: Common: Nasopharyngitis.
Blood and lymphatic system disorders: Uncommon: Neutropaenia.
Immune system disorders: Uncommon: Hypersensitivity. Rare: Angioedema, allergic reaction.
Metabolism and nutrition disorders: Common: Appetite increased. Uncommon: Anorexia, hypoglycaemia.
Psychiatric disorders: Common: Euphoric mood, confusion, irritability, disorientation, insomnia, libido decreased. Uncommon: Hallucination, panic attack, restlessness, agitation, depression, depressed mood, elevated mood, aggression, mood swings, depersonalisation, word finding difficulty, abnormal dreams, libido increased, anorgasmia, apathy. Rare: Disinhibition.
Nervous system disorders: Very Common: Dizziness, somnolence, headache. Common: Ataxia, coordination abnormal, tremor, dysarthria, amnesia, memory impairment, disturbance in attention, paraesthesia, hypoaesthesia, sedation, balance disorder, lethargy. Uncommon: Syncope, stupor, myoclonus, loss of consciousness, psychomotor hyperactivity, dyskinesia, dizziness postural, intention tremor, nystagmus, cognitive disorder, mental impairment, speech disorder, hyporeflexia, hyperaesthesia, burning sensation, ageusia, malaise. Rare: Convulsions, parosmia, hypokinesia, dysgraphia.
Eye disorders: Common: Vision blurred, diplopia. Uncommon: Peripheral vision loss, visual disturbance, eye swelling, visual field defect, visual acuity reduced, eye pain, asthenopia, photopsia, dry eye, lacrimation increased, eye irritation. Rare: Vision loss, keratitis, oscillopsia, altered visual depth perception, mydriasis, strabismus, visual brightness.
Ear and labyrinth disorders: Common: Vertigo. Uncommon: Hyperacusis.
Cardiac disorders: Uncommon: Tachycardia, atrioventricular block first degree, sinus bradycardia, congestive heart failure. Rare: QT prolongation, sinus tachycardia, sinus arrhythmia.
Vascular disorders: Uncommon: Hypotension, hypertension, hot flushes, flushing, peripheral Coldness.
Respiratory, thoracic and mediastinal disorders: Uncommon: Dyspnoea, epistaxis, cough, nasal congestion, rhinitis, snoring, nasal dryness. Rare: Pulmonary oedema, throat tightness.
Gastrointestinal disorders: Common: Vomiting, nausea, constipation, diarrhoea, flatulence, abdominal distension, dry mouth. Uncommon: Gastrooesophageal reflux disease, salivary hypersecretion, hypoaesthesia oral. Rare: Ascites, pancreatitis, swollen tongue, dysphagia.
Skin and subcutaneous tissue disorders: Uncommon: Rash papular, urticaria, hyperhidrosis, pruritus. Rare: Stevens Johnson syndrome, cold sweat.
Musculoskeletal and connective tissue disorders: Common: Muscle cramp, arthralgia, back pain, pain in limb, cervical spasm. Uncommon: Joint swelling, myalgia, muscle twitching, neck pain, muscle stiffness. Rare: Rhabdomyolysis.
Renal and urinary disorders: Uncommon: Urinary incontinence, dysuria. Rare: Renal failure, oliguria, urinary retention.
Reproductive system and breast disorders: Common: Erectile dysfunction. Uncommon: Sexual dysfunction, ejaculation delayed, dysmenorrhoea, breast pain. Rare: Amenorrhoea, breast discharge, breast enlargement, gynaecomastia.
General disorders and administration site conditions: Common: Oedema peripheral, oedema, gait abnormal, fall, feeling drunk, feeling abnormal, fatigue. Uncommon: Generalised oedema, face oedema, chest tightness, pain, pyrexia, thirst, chills, asthenia.
Investigations: Common: Weight increased. Uncommon: Blood creatine phosphokinase increased, alanine aminotransferase increased, aspartate aminotransferase increased, blood glucose increased, platelet count decreased, blood creatinine increased, blood potassium decreased, weight decreased. Rare: White blood cell count decreased.
After discontinuation of short-term and long-term treatment with pregabalin withdrawal symptoms have been observed in some patients.
The following reactions have been mentioned: insomnia, headache, nausea, anxiety, diarrhoea, flu syndrome, convulsions, nervousness, depression, pain, hyperhidrosis and dizziness, suggestive of physical dependence. The patient should be informed about this at the start of the treatment.
Concerning discontinuation of long-term treatment of pregabalin, data suggest that the incidence and severity of withdrawal symptoms may be dose-related.
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.
In vivo studies and population pharmacokinetic analysis: Accordingly, no 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.
Oral contraceptives, norethisterone and/or ethinyl oestradiol: Co-administration of pregabalin with the oral contraceptives norethisterone and/or ethinyl oestradiol does not influence the steady-state pharmacokinetics of either substance.
Central nervous system influencing medical products: Gross motor function caused by oxycodone. Pregabalin may potentiate the effects of ethanol and lorazepam. Multiple oral doses of pregabalin co-administered with oxycodone, lorazepam, or ethanol did not result in clinically important effects on respiration. Patients may experience respiratory failure and coma in taking pregabalin and other central nervous system (CNS) depressant medicinal products. Pregabalin appears to be additive in the impairment of cognitive and gross motor function caused by oxycodone.
Interactions and the elderly: No specific pharmacodynamics interaction studies in elderly volunteers. Interaction studies have only been performed in adults.
Caution For Usage
Special precautions for disposal and other handling: No special requirements for disposal.
Incompatibilities: Not applicable.
Storage
Do not Store above 30°. Store in Original Container.
Shelf-Life: 24 months.
ATC Classification
N03AX16 - pregabalin ; Belongs to the class of other antiepileptics.
Presentation/Packing
Hard cap 75 mg (a no. 4, light peach opaque cap and light peach opaque body, hard-shell gelatin capsule filled with white to off white powder. The capsule is axially printed with MYLAN over PB75 in black ink on cap and body) x 3 x 10's. 150 mg (a no. 2, light peach opaque cap and white opaque body, hard-shell gelatin capsule filled with white to off-white powder. The capsule is axially printed with MYLAN over PB150 in black ink on cap and body) x 3 x 10's.
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