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pregabalin + tizanidine
- Development stage
- Unknown
- Lead developer
- Beijing Tiantan Hospital
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Pregabalin + tizanidine is a combination pharmacological intervention being evaluated for the treatment of fibromyalgia. Pregabalin, a gabapentinoid, exerts its effect by binding to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, thereby modulating the release of several excitatory neurotransmitters such as glutamate and substance P. Tizanidine is a centrally acting alpha-2 adrenergic receptor agonist primarily used as a muscle relaxant; it is thought to reduce spasticity by increasing presynaptic inhibition of motor neurons and may also possess antinociceptive properties. The combination is being studied by Beijing Tiantan Hospital in the PROBE trial to determine if the dual mechanism of action provides enhanced efficacy in managing the complex symptoms of fibromyalgia, including widespread pain and sleep disturbances, compared to pregabalin monotherapy.
- Other names
- Pregabalin/Tizanidine
02
Targets
CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)I1R (Nischarin)CACNA2D2 (α2δ-2)ADRA2A (α2A)
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