Drug intelligence / Profile preview

tolterodine + pregabalin

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Tolterodine + pregabalin is a combination of two pharmaceutical drugs, each with distinct mechanisms of action and primary indications. Tolterodine is a muscarinic receptor antagonist used to treat overactive bladder by relaxing bladder muscles and reducing urinary urgency, frequency, and incontinence. It acts primarily on M2 and M3 subtypes of muscarinic receptors in the lower urinary tract[3][4]. Pregabalin is an anticonvulsant that binds to the alpha2-delta subunit of presynaptic voltage-gated calcium channels in the central nervous system, thereby modulating the release of several excitatory neurotransmitters such as glutamate, substance P, norepinephrine, and calcitonin gene-related peptide. Pregabalin is indicated for neuropathic pain conditions (including diabetic neuropathy and post-herpetic neuralgia), fibromyalgia, partial-onset seizures (as adjunctive therapy), and pain from spinal cord injury[1][2][5][6]. There are no widely recognized fixed-dose combination products or specific brand names for this drug pairing; their use together would be off-label or based on individual clinical need.

02

Targets

CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)M1 (Muscarinic acetylcholine receptor M1)CHRM4 (M4)CHRM3 (M3)CHRM5 (M5)CHRM2 (M2)

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