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topiramate + flunarizine
- Development stage
- Unknown
- Lead developer
- Janssen Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Topiramate + flunarizine is a fixed-dose combination of two small molecule drugs used primarily for migraine prophylaxis. Topiramate is an anticonvulsant that acts by blocking voltage-dependent sodium channels, enhancing GABA-A receptor activity, inhibiting AMPA/kainate glutamate receptors, and weakly inhibiting carbonic anhydrase. Flunarizine is a selective calcium channel blocker with calmodulin binding properties and histamine H1 antagonism; it also exhibits antidopaminergic effects. The combination has demonstrated efficacy and good tolerability in reducing the frequency and severity of migraines compared to either agent alone[1][2][5]. Topiramate may mitigate the weight gain commonly associated with flunarizine[1][2].
- Other names
- topiramate + flunarizine
02
Targets
GABRR (GABA-A receptor subunit rho)iGluR (Ionotropic receptor 76b (Ir76b))NaV (Voltage-gated sodium channels)HRH1 (Histamine H1 Receptor)VDCC (L-type voltage-dependent calcium channel (often specified further as subunits such as CaV1.2 in humans))DRD2 (Dopamine D2 Receptor)CA2 (Carbonic Anhydrase 2)
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