Mirogabalin: could it be the next generation gabapentin or pregabalin?
| Autor: | Salahadin Abdi, Billy K. Huh, Jae Yeon Kim, Kyung-Hoon Kim |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Sleepiness
Gabapentin medicine.medical_treatment Pregabalin Review Article Pharmacology Dizziness 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Mirogabalin 030202 anesthesiology Cerebellum Ganglia Spinal medicine business.industry Carbamazepine Equianalgesic Anesthesiology and Pain Medicine Anticonvulsant chemistry Neuropathic pain Neuralgia Anticonvulsants Ataxia Calcium Channels Analgesia business 030217 neurology & neurosurgery medicine.drug Gabapentinoid |
| Zdroj: | The Korean Journal of Pain |
| ISSN: | 2093-0569 2005-9159 |
| DOI: | 10.3344/kjp.2021.34.1.4 |
| Popis: | Except for carbamazepine for trigeminal neuralgia, gabapentinoid anticonvulsants have been the standard for the treatment of neuropathic pain. Pregabalin, which followed gabapentin, was developed with the benefit of rapid peak blood concentration and better bioavailability. Mirogabalin besylate (DS-5565, Tarlige®) shows greater sustained analgesia due to a high affinity to, and slow dissociation from, the α2δ-1 subunits in the dorsal root ganglion (DRG). Additionally, it produces a lower level of central nervous system-specific adverse drug reactions (ADRs), due to a low affinity to, and rapid dissociation from, the α2δ-2 subunits in the cerebellum. Maximum plasma concentration is achieved in less than 1 hour, compared to 1 hour for pregabalin and 3 hours for gabapentin. The plasma protein binding is relatively low, at less than 25%. As with all gabapentinoids, it is also largely excreted via the kidneys in an unchanged form, and so the administration dose should also be adjusted according to renal function. The equianalgesic daily dose for 30 mg of mirogabalin is 600 mg of pregabalin and over 1,200 mg of gabapentin. The initial adult dose starts at 5 mg, given orally twice a day, and is gradually increased by 5 mg at an interval of at least a week, to 15 mg. In conclusion, mirogabalin is anticipated to be a novel, safe gabapentinoid anticonvulsant with a greater therapeutic effect for neuropathic pain in the DRG and lower ADRs in the cerebellum. |
| Databáze: | OpenAIRE |
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