Flupirtina Winthrop
Flupirtina Winthrop Uses, Dosage, Side Effects, Food Interaction and all others data.
Flupirtina Winthrop is a pyridine derivative that is in clinical use as a nonopioid analgesic. It was approved for the treatment of pain in 1984 in Europe. It is not approved for use in the U.S. or Canada, but is currently in phase II trials for the treatment of fibromyalgia.
| Trade Name | Flupirtina Winthrop |
| Generic | Flupirtine |
| Flupirtine Other Names | Flupirtine, Flupirtino, Flupirtinum |
| Type | |
| Formula | C15H17FN4O2 |
| Weight | Average: 304.3195 Monoisotopic: 304.133554013 |
| Groups | Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Portugal |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Investigated for use/treatment in fibromyalgia.
How Flupirtina Winthrop works
Flupirtina Winthrop upregulates Bcl-2, increases glutathione levels, activates an inwardly rectifying potassium channel, and delays loss of intermitochondrial membrane calcium retention capacity. Flupirtina Winthrop acts like a NMDA receptor antagonists, but does not bind to the receptor. One study concluded that the discriminative effects of flupirtine are neither of opioid nor of alpha-1 adrenergic type, but are primarily mediated through alpha-2 adrenergic mechanisms [PMID: 2901483].
Toxicity
Oral, mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50 = 980 mg/kg.
Elimination Route
Bioavailability: 90% (oral), 70% (rectal)
Half Life
6.5 hrs (average), 11.2-16.8 hrs (average 14 hrs) (elderly), 8.7-10.9 hrs (average 9.8 hrs) (in those with moderate-level renal impairment).
Elimination Route
72% of flupirtine and its metabolites appear in urine and 18% appear in faeces.
Innovators Monograph
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