Asibalin binds presynaptically to the alpha-2-delta subunit of the voltage-gated calcium channels in central nervous system tissues located in the brain and spinal cord. The mechanism of action has not been fully elucidated but studies suggest that pregabalin produces a disruption of calcium channel traficking or a reduction of calcium currents. The inhibition of subunits of voltage-gated calcium channels reduces calcium release which in order inhibits the release of several neurotransmitters. Studies also suggest that the descending noradrenergic and serotonergic pathways originating from the brainstem may be involved with the mechanism of pregabalin. Interestingly, although pregabalin is a structural derivative of inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors.
Asibalin is used for the management of neuropathic pain associated with diabetic peripheral neuropathy and management of post-herpetic neuralgia. It is also used for the adjunctive therapy for adult patients with partial onset seizures. It can be used for the management of fibromyalgia and neuropathic pain associated with spinal cord injury.
Asibalin is also used to associated treatment for these conditions: Diabetic Peripheral Neuropathic Pain (DPN), Epilepsies, Fibromyalgia, Generalized Anxiety Disorder (GAD), Neuropathic Pain, Partial-Onset Seizures, Peripheral Neuropathic Pain, Peripheral neuropathy, Postherpetic Neuralgia
|Other Names||3-Isobutyl GABA, Pregabalin, Pregabalina|
|Weight||75mg, 25mg, 50mg|
Pregabalin is not plasma protein bound.
|Therapeutic Class||Adjunct anti-epileptic drugs|
|Manufacturer||Asiatic Laboratories Ltd|
|Last Updated:||June 23, 2021 at 11:24 am|
Table Of contents
Neuropathic pain associated with diabetic peripheral neuropathy: The maximum recommended dose of Asibalin 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) and may be increased to 300 mg/day within 1 week based on efficacy and tolerability.
Post-herpetic neuralgia: The recommended dose of Asibalin 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) and may be increased to 300 mg/day within 1 week based on efficacy and tolerability.
Adjunctive therapy for adult patients with partial onset seizures: Asibalin 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. The total daily doseshould be divided and given either two or three times daily. 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.
Management of Fibromyalgia: The recommended dose of Asibalin for fibromyalgia is 300 to 450 mg/day. Dosing should begin at 75 mg two times a day (150 mg/day) and 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: The recommended dose range 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 treatment with 300 mg/day and who tolerate pregabalin may be treated with up to 300 mg two times a day. Neurolin® capsules can be taken without regards to meals.
The most common side effects include dizziness, somnolence, dry mouth, edema, blurred vision, weight gain, and abnormal thinking.
Discontinuation of Asibalin without tapering may produce insomnia, nausea, headache and diarrhea. So it should be tapered gradually over a minimum of 1 week rather than discontinued abruptly. Creatinine kinase may be elevated if treated with Asibalin. It should be discontinued rapidly if myopathy is diagnosed or suspected or if creatinine kinase is elevated markedly.
- Avoid alcohol. Alcohol may increase CNS effects.
- Take with or without food. Food alters drug absorption, but not to a clinically significant extent.
Volume of Distribution
After oral administration of pregabalin, the reported apparent volume of distribution is roughly 0.5 L/kg.
Although pregabalin is not very lipophilic, it is able to cross the blood brain barrier(BBB). System L transporters facilitate the transport of large amino acids across the BBB and it has been confirmed that pregabalin is a substrate. This information suggests that system L transporters are responsible for pregabalin uptake into the BBB.
In rat models, pregabalin has been shown to cross the placenta.
The elimination half life of pregabalin is 6.3 hours.
In young healthy subjects the mean renal clearance is estimated to be 67.0 to 80.9 mL mL/min. Given pregabalin's lack of plasma protein binding, this clearance rate suggests that renal tubular reabsorption is involved.
Pregnancy & Breastfeeding use
Pregnancy category C. So it should only used if potential benefit justifies the potential risks to the fetus.
Nursing mother: It is not known if pregabalin is excreted in human milk; it is, however, present in the milk of rats. So it should be used in nursing mother only if there is a clear benefit over the risk.
Asibalin is contraindicated in patients with known hypersensitivity to Asibalin or any of its components.
Use in children & adolescents: The safety and effectiveness of Asibalin have not been established in patients below the age of 18 years.
Use in elderly (Over 65 years of age): No dosage adjustment is necessary in elderly patients. Overdose: In overdoses up to 15 g, no unexpected adverse effects were reported.
Paediatric use: The safety and efficacy of pregabalin in paediatric patients have not been established.
Store at a cool & dry place, protected from light and moisture. Keep out of reach of the children.