Pregabur-75/Pregabur-150

Pregabur-75/Pregabur-150

pregabalin

Manufacturer:

Rhydburg

Distributor:

Ambica
Full Prescribing Info
Contents
Pregabalin.
Description
Pregabur-75: Each hard gelatin capsule contains: Pregabalin 75 mg.
Pregabalin is an anticonvulsant drug used for neuropathic pain and as an adjunct therapy for partial seizures with or without secondary generalization in adults. Its chemical name is (S)-3-(aminomethyl)-5-methylhexanoic acid. Its empirical formula is C8H17NO2 and its molecular weight is 159.23.
Pregabur 150: Each hard gelatin capsule contains: Pregabalin 150 mg; Excipients q.s.
Action
Pregabur-75: Pharmacology: Pharmacodynamics: Mechanism of Action: Pregabalin binds to an auxiliary subunit (α2-δ protein) of voltage-gated calcium channels in the central nervous system tissues. Although the mechanism of action of pregabalin has not been fully elucidated, results with genetically modified mice and with compounds structurally related to pregabalin (such as gabapentin) suggest that binding to the alpha2-delta subunit may be involved in pregabalin’s antinociceptive and antiseizure effects in animals. In animal models of nerve damage, pregabalin has been shown to reduce calcium dependent release of pronociceptive neurotransmitters in the spinal cord, possibly by disrupting alpha2-delta containing calcium channel trafficking and/or reducing currents. Evidence from other animal models of nerve damage and persistent pain suggest the antinociceptive activities of pregabalin may also be mediated through interactions with descending noradrenergic and serotonergic pathways originating from the brainstem that modulate pain transmission in the spinal cord.
While pregabalin is a structural derivative of the inhibitory neurotransmitter gammaaminobutyric acid (GABA), it does not bind directly to GABAA, GABAB, or benzodiazepine receptors, does not augment GABAA responses in cultured neurons, does not alter rat brain GABA concentration or have acute effects on GABA uptake or degradation. However, in cultured neurons prolonged application of pregabalin increases the density of GABA transporter protein and increases the rate of functional GABA transport. Pregabalin does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity. It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake.
Pharmacokinetics: Oral bioavailability of Pregabalin is estimated to be ≥90% and is independent of dose. 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. Following a dose ratio labeled pregabalin approximately 98% of the administered dose recovered in the urine was unchanged pregabalin. Its mean elimination half-life is 6.3 hours
Indications/Uses
Pregabur-75: Pregabalin is indicated for the management of neuropathic pain with diabetic peripheral neuropathy, management of postherpetic neuralgia, adjunctive therapy for adult patients with partial onset seizures, management of fibromyalgia, and management of neuropathic pain associated with spinal cord injury.
Pregabur 150: Used to treat epilepsy, neuropathic pain and Generalized Anxiety Disorder (GAD) in adults.
Peripheral and central neuropathic pain: is used to treat long lasting pain caused by damage to the nerves. A variety of diseases can cause peripheral neuropathic pain, such as diabetes or shingles. Pain sensations may be described as hot, burning, throbbing, shooting, stabbing, sharp, cramping, aching, tingling, numbness, pins and needles. Peripheral and central neuropathic pain may also be associated with mood changes, sleep disturbance, fatigue (tiredness), and can have an impact on physical and social functioning and overall quality of life.
Epilepsy: is used to treat a certain form of epilepsy (partial seizures with or without secondary generalization) in adults. The doctor will prescribe Pregabalin to help treat the epilepsy when the current treatment is not controlling the condition. Patient should take Pregabalin in addition to the current treatment. It is not intended to be used alone, but should always be used in combination with other anti-epileptic treatment.
Generalized Anxiety Disorder: is used to treat Generalized Anxiety Disorder (GAD). The symptoms of GAD are prolonged excessive anxiety and worry that are difficult to control. GAD can also cause restlessness or feeling keyed up or on edge, being easily fatigued (tired), having difficulty concentrating or mind going blank, feeling irritable, having muscle tension or sleep disturbance. This is different to the stresses and strains of everyday life.
Dosage/Direction for Use
Pregabur-75: Pregabalin is given orally without food.
Neuropathic Pain Associated with Diabetic peripheral Neuropathy: The maximum recommended dose of Pregabalin is 100 mg three times a day (9300 mg/day). In patients with creatinine clearance of at least 60 mL/min, begin dosing at 50 mg three times a day (9150 mg/day). The dose may be increased to 300 mg/day within 1 week based on efficacy and tolerability because Pregabalin is eliminated primarily by renal excretion. Adjust the dose in patients with reduced renal function.
Postherpetic Neuralgia: The recommended dose of Pregabalin is 75 to 150 mg two times a day, or 50 to 100 mg three times a day (150 to 300 mg/day). In patients with creatinine clearance of at least 60 mL/min, begin dosing at 75 mg two times a day, or 50 mg three times a day (150 mg/day). The dose may be increased to 300 mg/day within 1 week based on efficacy and tolerability, because Pregabalin is eliminated primarily by renal excretion, adjust the dose in patients with reduced renal function.
Patients who do not experience sufficient pain relief following 2 to 4 weeks of treatment with 300 mg/day, and who are able to tolerate Pregabalin, may be treated with up to 300 mg two times a day, or 200 mg three times a day (600 mg/day). In view of the dose-dependent adverse reactions and the higher rate of treatment discontinuation due to adverse reactions, reserve dosing above 300 mg/day for those patients who have on-going pain are tolerating 300 mg daily.
Adjunctive Therapy for Adult Patients with Partial Onset Seizures: Pregabalin at doses of 150 to 600 mg/day has been shown to be effective as adjunctive therapy in the treatment of partial onset seizures in adults. Administer the total daily dose in two or three divided doses. In general, it is recommended that patients be started on a total daily dose no greater than 150 mg/day (75 mg two times a day, or 50 mg three times a day). Based on individual patient response and tolerability, the dose may be increased to a maximum dose of 600 mg/day, because Pregabalin is eliminated primarily by renal excretion. Adjust the dose in patients with reduced renal function. The effect of dose escalation rate on the tolerability of Pregabalin has not been formally studied. The efficacy of add-on Pregabalin in patients taking gabapentin has not been evaluated in controlled trials. Consequently, the dosing recommendations for the use of Pregabalin with gabapentin cannot be offered.
Management of Fibromyalgia: The recommended dose of Pregabalin for fibromyalgia is 300 to 450 mg/day. Begin dosing at 75 mg two times a day (150 mg/day). The dose may be increased to 150 mg two 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 two times a day (450 mg/day). Although Pregabalin was also studied at 600 mg/day, there is no evidence that this dose confers additional benefit and this dose is less well-tolerated. In view of the dose-dependent adverse reactions, treatment with doses above 450 mg/day is not recommended, because Pregabalin is eliminated primarily by renal excretion. Adjust the dose in patients with reduced renal function.
Neuropathic Pain Associated with Spinal Cord Injury: The recommended dose range of Pregabalin for the treatment of neuropathic pain associated with spinal cord injury is 150 to 600 mg/day. The recommended starting dose is 75 mg two times a day (150 mg/day). The dose may be increased to 150 mg two times a day (300 mg/day) within 1 week based on efficacy and tolerability. Patients who do not experience sufficient pain relief after 2 to 3 weeks of treatment with 150 mg two times a day and who tolerate Pregabalin may be treated with up to 300 mg two times a day because Pregabalin is eliminated primarily by renal excretion. Adjust the dose in patients with reduced renal function.
Patients with Renal Impairment: In view of dose-dependent adverse reactions and since Pregabalin is eliminated primarily by renal excretion, adjust the dose in patients with reduced renal function. Base the dose adjustment in patients with renal impairment on creatinine clearance (CrCl), as indicated in the table. Next, refer to Dosage & Administration to determine the recommended total daily dose based on indication, for a patient with normal renal function (CrCl ≥60 mL/min). Then refer to the table to determine the corresponding renal adjusted dose.
For patients undergoing hemodialysis, adjust the pregabalin daily dose based on renal function. In addition to the daily dose adjustment, administer a supplemental dose immediately following every 4-hour hemodialysis treatment (see table).

Click on icon to see table/diagram/image

Pregabur 150: Pregabalin is given orally in 2 or 3 divided doses daily.
The initial dose in the treatment of epilepsy is 150 mg daily increased after 1 week according to response to 300 mg daily and then to 600 mg daily after another week.
In the treatment of generalized anxiety disorder, the initial dose is 150 mg daily; this maybe increased at weekly intervals in steps of 150 mg to a maximum of 600 mg daily.
For neuropathic pain the initial dose is 150 mg daily increased after 3 to 7 days according to the response to 300 mg daily and then to 600 mg daily after another 7 days.
For fibromyalgia the initial dose is 150 mg daily increased after 1 week according to response to 300 mg daily and then to 450 mg daily if necessary.
Directions for Use: Pregabalin capsules may be taken with or without food.
It is advised not to drink alcohol while taking.
Overdosage
Pregabur-75: Symptoms include somnolence, confusional state, agitation, and restlessness. Treatment of pregabalin overdose should include general supportive measures and may include haemodialysis, if necessary.
Pregabur 150: If the patient took more Pregabalin than needed. Call a doctor or go to the nearest hospital emergency unit immediately. Take the box or bottle of Pregabalin capsules. Patient may feel sleepy, confused, agitated, or restless as a result of taking more than needed.
Contraindications
Pregabur-75: Hypersensitivity to the active substance or to any of the excipients.
Special Precautions
Pregabur-75: Angioedema: There have been postmarketing reports of angioedema in patients during initial and chronic treatment with Pregabalin. Specific symptoms included swelling of the face, mouth (tongue, lips, and gums), and neck (throat and larynx). There were reports of life-threatening angioedema with respiratory compromise requiring emergency treatment. Discontinue Pregabalin immediately in patients with these symptoms.
Exercise caution when prescribing Pregabalin to patients who have had a previous episode of angioedema. In addition, patients who are taking other drugs associated with angioedema (e.g. angiotensin converting enzyme inhibitors [ACE-inhibitors]) may be at increased risk of developing angioedema.
Hypersensitivity: There have been postmarketing reports of hypersensitivity in patients shortly after initial of treatment with Pregabalin. Adverse reactions included skin redness, hives, rash, dyspnea, and wheezing. Discontinue Pregabalin immediately in patients with these symptoms.
Withdrawal of Antiepileptic Drugs (AEDs): As with all AEDs, withdraw Pregabalin gradually to minimize the potential of increased seizure frequency in patients with seizure disorders. If pregabalin is discontinued, taper the drug gradually over a minimum of 1 week.
Suicidal Behavior and Ideation: Antiepileptic drugs (AEDs), including Pregabalin, increase the risk of suicidal thoughts or behavior in patients taking drugs for any indication. Monitor patients treated with AEDs for any indication of the emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior.
Pregabur 150: Some patients taking Pregabalin have reported symptoms suggesting an allergic reaction. These symptoms include swelling of the face, lips, tongue, and throat, as well as diffuse skin rash.
Should patient experience any of these reactions, contact a physician immediately.
It has been associated with dizziness and somnolence, which could increase the occurrence of accidental injury (fall) in elderly patients. Therefore, patient should be careful until used to any effect the medicine might have.It may cause blurring or loss of vision, or other changes in eyesight, many of which are temporary. Patient should immediately tell the doctor if any changes in vision is experienced.
Some patients with diabetes who gain weight while taking Pregabalin may need an alteration in diabetic medicines.
Certain side effects may be more common, such as sleepiness, because patients with spinal cord injury may be taking other medicines to treat, for example, pain or spasticity, that have similar side effects to Pregabalin and the severity of these effects may be increased when taken together.
There have been reports of kidney failure in some patients when taking Pregabalin; these patients were mostly elderly with cardiovascular conditions. Before taking this medicine advise the doctor about any history of heart disease.
There have been reports of kidney failure in some patients when taking Pregabalin. If while taking patient noticed decreased urination, tell the doctor as stopping the medicine may improve this.
A small number of people being treated with anti-epileptics such as Pregabalin have had thoughts of harming or killing themselves. If at any time patient has these thoughts, immediately contact a doctor.
When Pregabalin is taken with other medicines that may cause constipation (such as some types of pain medicines) it is possible that gastrointestinal problems may occur (e.g. constipation, blocked or paralysed bowel). Tell the doctor if constipation is experienced, especially if patient is prone to this problem.
Before taking this medicine patient should tell the doctor if he/she has a history of alcoholism or any drug abuse or dependence. Do not take more medicine than prescribed.
There have been reports of convulsions when taking Pregabalin or shortly after stopping. If patient experience a convulsion, contact a doctor immediately.
There have been reports of reduction in brain function (encephalopathy) in some patients taking Pregabalin when they have other conditions. Tell the doctor in case of history of any serious medical conditions, including liver or kidney disease.
Contains lactose monohydrate: If the patient has been told by the doctor that patient has intolerance to some sugars, contact a doctor before taking this medicinal product.
Driving and using machines: Pregabalin may produce dizziness, sleepiness and decreased concentration. Patient should not drive, operate complex machinery or engage in other potentially hazardous activities until it is known whether this medicine affects the ability to perform these activities.
Use in Children: The safety and efficacy in children and adolescents (under 18 years of age) has not been established and therefore, pregabalin should not be used in this age group.
Use In Pregnancy & Lactation
Pregabur 150: Pregabalin should not be taken during pregnancy or when breast-feeding, unless told otherwise by the doctor. Effective contraception must be used by women of child-bearing potential. If patient is pregnant or breast-feeding, think that may be pregnant or planning to have a baby, ask the doctor or pharmacist for advice before taking this medicine.
Adverse Reactions
Pregabur-75: Hypersensitivity, angioedema, allergic reaction, increased appetite, euphoric mood, confusion, irritability, decreased libido, disorientation and insomnia.
Pregabur 150: Like all medicines, this medicine can cause side effects, although not everybody gets them.
Very common: may affect more than 1 in 10 people: Dizziness, drowsiness, headache.
Common: may affect up to 1 in 10 people: Increased appetite; Feeling of elation, confusion, disorientation, decrease in sexual interest, irritability; Disturbance in attention, clumsiness, memory impairment, loss of memory, tremor, difficulty with speaking, tingling feeling, numbness, sedation, lethargy, insomnia, fatigue, feeling abnormal; Blurred vision, double vision; Vertigo, problems with balance, fall; Dry mouth, constipation, vomiting, flatulence, diarrhea, nausea, swollen abdomen; Difficulties with erection; Swelling of the body including extremities; Feeling drunk, abnormal style of walking; Weight gain; Muscle cramp, joint pain, back pain, pain in limb; Sore throat.
Uncommon: may affect up to 1 in 100 people: Loss of appetite, weight loss, low blood sugar, high blood sugar; Change in perception of self, restlessness, depression, agitation, mood swings, difficulty in finding word, hallucinations, abnormal dreams, panic attack, apathy, aggression, elevated mood, mental impairment, difficulty with thinking, increase in sexual interest, problems with sexual functioning including inability to achieve a sexual climax, delayed ejaculation; Changes in eyesight, unusual movement, changes in vision including tunnel vision, flashes of light, jerky movements, reduced reflexes, increased activity, dizziness on standing, sensitive skin, loss of taste, burning sensation, tremor on movement, decreased consciousness, loss of consciousness, fainting, increased sensitivity to noise, feeling unwell; Dry eyes, eye swelling, eye pain, weak eyes, watery eyes, eye irritation; Heart rhythm disturbances, increased heart rate, low blood pressure, high blood pressure, changes in heart beat, heart failure; Flushing, hot flushes; Difficulty breathing, dry nose, nasal congestion; Increased saliva production, heartburn, numb around mouth; Sweating, rash, chills, fever; Muscle twitching, joint swelling, muscle stiffness, pain including muscle pain, neck pain; Breast pain; Difficulty with or painful urination, incontinence; Weakness, thirst, chest tightness; Changes in blood and liver test results (blood creatinine phosphokinase increased, alanine amino transferase increased, aspartate aminotransferase increased, platelet count decreased, neutropenia, increase in blood creatinine, decrease in blood potassium); Hypersensitivity, swollen face, itchiness, hives, runny nose, nose bleed, cough, snoring; Painful menstrual periods; Coldness of hands and feet.
Rare: may affect up to 1 in 1,000 people: Abnormal sense of smell, swinging vision, altered perception of depth, visual brightness, vision loss; Dilated pupils, cross eyes; Cold sweat, tightness of the throat, swollen tongue; Inflammation of the pancreas; Difficulty in swallowing; Slow or reduced movement of the body; Difficulty with writing properly; Increased fluid in the abdomen; Fluid in the lungs; Convulsions; Changes in the recording of electrical changes (ECG) in the heart which correspond to heart rhythm disturbances; Muscle damage; Breast discharge, abnormal breast growth, breast growth in males; Interrupted menstrual periods; Kidney failure, reduced urine volume, urinary retention; Decrease in white blood cell count; Inappropriate behavior; Allergic reactions (which may include difficulty in breathing, inflammation of the eyes (keratitis) and serious skin reaction characterized by rash, blisters, peeling skin and pain).
If patient experiences swollen face or tongue or if skin turns red and starts to blister or peel, seek immediate medical advice.
Certain side effects may be more common, such as sleepiness, because patients with spinal cord injury may be taking other medicines to treat, for example, pain or spasticity, that has similar side effects to Pregabalin and the severity of these effects may be increased when taken together.
Drug Interactions
Pregabur 75: In vivo studies and population pharmacokinetic analysis show that no pharmacokinetic interactions were observed between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol and oral contraceptives, such as norethisterone and/or ethinyl oestradiol.
Pregabur 150: Pregabalin and certain other medicines may influence each other (interaction). When taken with certain other medicines, it may potentiate the side effects seen with these medicines, including respiratory failure and coma. The degree of dizziness, sleepiness and decreased concentration may be increased if it is taken together with medicinal products containing: Oxycodone-(used as a pain-killer); Lorazepam-(used for treating anxiety); Alcohol; may be taken with oral contraceptives; with food, drink and alcohol.
Storage
Store at temperatures not exceeding 30°C.
ATC Classification
N03AX16 - pregabalin ; Belongs to the class of other antiepileptics.
Presentation/Packing
Pregabur-75: Cap 75 mg x 10's. Pregabur-150: Cap 150 mg x 10's.
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