Drug intelligence / Profile preview

amitriptyline + gabapentin

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

Overview

Amitriptyline + gabapentin is a fixed-dose combination of two pharmaceutical agents used primarily for the management of neuropathic pain. Amitriptyline is a tricyclic antidepressant that increases levels of serotonin and noradrenaline in the brain, thereby modulating pain signal transmission. Gabapentin is an anticonvulsant that binds to voltage-gated calcium channels in the central nervous system, reducing neuronal excitability and relieving nerve pain. The combination provides additive or synergistic analgesic effects, particularly beneficial in chronic neuropathic conditions such as diabetic neuropathy and chronic pelvic pain[2][4][5]. This combination may increase side effects like dizziness, drowsiness, confusion, and difficulty concentrating due to additive central nervous system depressant effects[1][3].

Other names
gabapentin + amitriptyline
02

Targets

NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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