Prescribing Details
Description
Gabarol ® is the preparation of Pregabalin, which is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). It does not bind directly to GABA., GABA, or benzodiazepine receptors. Pregabalin binds with high affinity to the alpha-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Although the mechanism of action of Pregabalin has not been fully elucidated, results in animal studies suggest that binding to the alpha-delta subunit may be involved in Pregabalin's anti-nociceptive and antiseizure effects.
Uses
No Data
Indications
Gabarol® is indicated for:
• Neuropathic pain associated with diabetic peripheral neuropathy (DPN)
• Postherpetic neuralgia (PHN)
• Adjunctive therapy for the treatment of partial onset seizures in patients month of age and older
• Fibromyalgia
• Neuropathic pain associated with spinal cord injury
Gabarol® CR is indicated for:
•Neuropathic pain associated with diabetic peripheral neuropathy (DPN)
• Postherpetic neuralgia (PHN)
Dosage and administration
Route of administration: Gabarol® is taken in oral route. It can be taken with or without food. Gabarol® CR tablet should be administered after an evening meal. It should be swallowed whole and should not be split, crushed or chewed. If patients miss taking their dose of Gabarol® CR after an evening meal, then they should take their usual dose of Gabarol® CR prior to bedtime following a snack. If they miss taking the dose of Gabarol® CR prior to bedtime, then they should take their usual dose of Gabarol® CR following a morning meal. If they miss taking the dose of Gabarol® CR following the morning meal. then they should take their usual dose of Gabarol® CR at the usual time that evening following an evening meal. When discontinuing both Gabarol® and Gabarol® CR, it should be gradually tapered over a minimum of 1 week.
Neuropathic pain associated with diabetic peripheral neuropathy in adults (DPN)
The maximum recommended dose of Gabarol® is 100 mg three times a day (300 mg/day) in patients with creatinine clearance of at least 60 ml/min. Dosing should begin at 50 mg three times a day (150 mg/day). The dose may be increased to 300 mg/day within week based on efficacy and tolerability. Begin dosing of Gabarol® CR at 165 mg once daily and increase to 330 mg once daily within week based on individual patient response and tolerability. The maximum recommended dose of Gabarol® CR is 330 mg once daily.
Postherpetic neuralgia in adults (PHN)
The recommended dose of Gabarol® 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. Dosing should begin 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 week based on efficacy and tolerability. 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 Gabarol, may be treated with up to 300 mg two times a day or 200 mg three times a day (600 mg/day).
Begin dosing of Gabarol® CR at 165 mg once daily and increase to 330 mg once daily within 1 week based on individual patient response and tolerability. Patients who do not experience sufficient pain relief following 2 to 4 weeks of treatment with 330 mg once daily and who are able to tolerate Gabarol® CR, may be treated with up to 660 mg once daily. In view of the dose-dependent adverse reactions and the higher rate of treatment discontinuation due to adverse reactions, dosing above 330 mg/day should be reserved only for those patients who have on-going pain and are tolerating 330 mg daily. The maximum recommended dose of Gabarol® CR is 660 mg once daily.)
Adiunctive therapy for partial onset seizures in patients 1 month of age and older
| Recommended dosage for adults and pediatric patients 1 month and older | |||
|---|---|---|---|
| Age and body weight | Recommended initial dosage | Recommended maximum dosage | Recommended administration |
| Pediatric patients weighing 30 kg or more | 2.5 mg/kg/day | 10 mg/kg/day (not to exceed 600 mg/day) | 2 or 3 divided doses |
| Weeks 3 and 4 | 25 mg daily | 50 mg daily | 100 mg daily, in divided doses |
| Pediatric patients weighing less than 30 kg | 3.5 mg/kg/day | 14 mg/kg/day | 1 month to less than 4 years of age: 3 divided doses 4 years of age and older: 2 or 3 divided doses |
Management of fibromyalgia in adults
The recommended dose of Gabarol® is 300 to 450 mg/day. Dosing should begin 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).
Neuropathic pain associated with spinal cord injury in adults
The recommended dose range of Gabarol 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 Gabarol may be treated with up to 300 mg two times a day.
Dosing for adult patients with renal impairment
Gabarol®
| Gabarol dosage adjustment based on renal function | |||||
|---|---|---|---|---|---|
| Creatine Clearance (CLcr) (ml/min) | Total Gabarol daily dose (mg/day)* | Dose regimen | |||
| Greater than or equal to 60 | 150 | 300 | 450 | 600 | BID or TID |
| 30-60 | 75 | 150 | 225 | 300 | BID or TID |
| 15-30 | 25-50 | 75 | 100-150 | 150 | QD or BID |
| Less than 15 | 25 | 25-50 | 50-75 | 75 | QD |
| Supplementary dosage following hemodialysis (mg)** | |||||
| Patients on the 25 mg QD regimen: take one supplemental dose of 25 mg or 50 mg Patients on the 25-50 mg QD regimen: take one supplemental dose of 50 mg or 75 mg Patients on the 50-75 mg QD regimen: take one supplemental dose of 75 mg or 100 mg Patients on the 75 mg QD regimen: take one supplemental dose of 100 mg or 150 mg |
|||||
| TID= Three divided doses; BID = Two divided doses; QD = Single daily dose. | |||||
| *Total daily dose (mg/day) should be divided as indicated by dose regimen to provide mg/dose. | |||||
| **Supplementary dose is a single additional dose | |||||
Gabarol® CR
| Gabarol dosage adjustment based on renal function | |||||
|---|---|---|---|---|---|
| Creatine Clearance (CLcr) (ml/min) | Total Gabarol daily dose (mg/day)* | Dose regimen | |||
| Greater than or equal to 60 | 165 | 330 | 495 | 660 | Once a Day |
| 30-60 | 82.5 | 165 | 247.5 | 330 | Once a Day |
| Less than 30/hemodialysis | Dose with Gabarol® | ||||
Conversion from Gabarol Capsules to GabarolⓇ CR
When switching from GabarolⓇ to GabarolⓇ CR on the day of the switch, instruct patients to take their morning dose of GabarolⓇ as prescribed and initiate GabarolⓇ CR therapy after an evening meal.
| Gabarol total daily dose (dosed 2 or 3 times daily) | Gabarol CR dose (dosed once a day) |
|---|---|
| 75 mg/daily | 82.5 mg/day |
| 150 mg/daily | 165 mg/day |
| 225 mg/daily | 247.5 mg/day |
| 300 mg/daily | 330 mg/day |
| 450 mg/daily | 495 mg/day |
| 600 mg/daily | 660 mg/day |
Use in pregnancy & lactation
Pregnancy: There are no adequate and well controlled studies with pregabalin in pregnant women. Pregnant women should be advised of the potential risk to a fetus.
Lactation: Small amounts of pregabalin have been detected in the milk of lactating women. Because of the potential risk of tumorigenicity, breastfeeding is not recommended during treatment with pregabalin.
Use in children and adolescents
Safety and effectiveness in pediatric patients have not been established for management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, neuropathic pain associated with spinal cord injury and fibromyalgia. In case of adjunctive therapy for partial onset seizures, safety and effectiveness in pediatric patients below the age of 1 month have not been established. The safety and effectiveness of pregabalin extended release tablet in pediatric patients have not been established.
Geriatric use
Precautions
Angioedema (e.g., swelling of the throat, head and neck) can occur and may be associated with life threatening respiratory compromise requiring emergency treatment. Pregabalin should be discontinued immediately in these cases. Pregabalin should also be discontinued immediately if hypersensitivity reactions (e.g., hives, dyspnea and wheezing) occur. Antiepileptic drugs, including pregabalin, increase the risk of suicidal thoughts or behavior. Respiratory depression may occur with pregabalin when used with concomitant CNS depressants or in the setting of underlying respiratory impairment. Patients need to be monitored and dosage adjusted as appropriate. Pregabalin may cause dizziness and somnolence and impair patients ability to drive or operate machinery. Increased seizure frequency or other adverse reactions may occur if pregabalin is rapidly discontinued. Pregabalin should be withdrawn gradually over a minimum of 1 week. Pregabalin may cause peripheral edema. Caution should be exercised when coadministering pregabalin and thiazolidinedione antidiabetic agents.
Side effects
Most common side effects in adults are dizziness, somnolence, dry mouth, edema, blurred vision, weight gain and thinking abnormal (primarily difficulty with concentration/attention). Most common side effects in pediatric patients for the treatment of partial onset seizures are increased weight and increased appetite.
Contraindications
Pregabalin is contraindicated in patients with known hypersensitivity to pregabalin or any other components of this product.
Drug interactions
Drug interaction with medication: Pregabalin is unlikely to be involved in significant pharmacokinetic drug interactions. Drug interaction with food and others: Not applicable.
Overdose
In overdose up to 15 mg, no unexpected adverse reactions were reported. The most common adverse events are affective disorder, somnolence, confusional state, depression, agitation and restlessness. Elimination of unabsorbed drug may be attempted by emesis or gastric lavage or hemodialysis if necessary.
Preparation
No Data
Pharmaceutical precautions
In case of overdose with pregabalin, sign and symptoms are reduced consciousness, depression/anxiety, confusional state, agitation and restlessness. Seizures and heart block have also been reported. There is no specific antidote. If indicated, elimination of unabsorbed drug may be attempted by emesis or gastric lavage; usual precautions should be observed to maintain the airway. General supportive care of the patient is indicated including monitoring of vital signs and observation of the clinical status of the patient.
Presentation
Gabarol 25 mg capsule: Carton of 30 capsules in blister pack.
Gabarol 50 mg capsule: Carton of 30 capsules in blister pack.
Gabarol® 75 mg capsule: Carton of 30 capsules in blister pack.
Gabarol® 100 mg capsule: Carton of 20 capsules in blister pack.
Gabarol 150 mg capsule: Carton of 20 capsules in blister pack.
Gabarol® CR 82.5 mg tablet: Carton of 30 tablets in blister pack. Gabarol® CR 165 mg tablet: Carton of 20 tablets in blister pack.
Package quantitie
Gabarol® 25 mg capsule: Carton of 30 capsules in blister pack.
Gabarol® 50 mg capsule: Carton of 30 capsules in blister pack.
Gabarol® 75 mg capsule: Carton of 30 capsules in blister pack.
Gabarol® 100 mg capsule: Carton of 20 capsules in blister pack.
Gabarol® 150 mg capsule: Carton of 20 capsules in blister pack.
