Drug intelligence / Profile preview

flunarizine + pregabalin

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Flunarizine + pregabalin is a combination of two small molecule drugs, each with distinct mechanisms of action. Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity, primarily used for migraine prophylaxis, vertigo (of central and peripheral origin), occlusive peripheral vascular disease, and as an adjuvant in epilepsy therapy[1][6]. Pregabalin is an analog of the neurotransmitter GABA that binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing neurotransmitter release; it is indicated for neuropathic pain (including diabetic neuropathy and postherpetic neuralgia), fibromyalgia, partial-onset seizures (as adjunctive therapy), and neuropathic pain associated with spinal cord injury[2]. The combination may be considered when both migraine/vertigo symptoms and neuropathic pain or seizure disorders coexist or are refractory to monotherapy. There are pharmacodynamic interactions between these agents; some sources suggest flunarizine efficacy can be increased by pregabalin[1], while others note possible decreased efficacy[4].

02

Targets

HRH1 (Histamine H1 Receptor)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)DRD2 (Dopamine D2 Receptor)LTCC (Voltage-gated calcium channel (L-type))

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