Drug intelligence / Profile preview

gabapentin + morphine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous, Intrathecal, Subcutaneous, Intramuscular, Epidural
01

Overview

Gabapentin + morphine is a combination therapy involving the anticonvulsant gabapentin and the opioid analgesic morphine. This combination is primarily used for the management of neuropathic pain and severe cancer pain, especially in cases where monotherapy with either agent is insufficient. Gabapentin acts by modulating voltage-gated calcium channels, reducing excitatory neurotransmitter release, while morphine exerts its effects as an agonist at the mu-opioid receptor to inhibit pain signaling in the central nervous system. Clinical studies have shown that combining these drugs can provide better analgesia at lower doses than either drug alone, potentially reducing opioid requirements[1][2][4][8]. However, this combination increases risks of central nervous system depression and respiratory depression due to additive effects[3][5]. The use of this combination should be carefully monitored due to these safety concerns.

02

Targets

CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)MOR (Mu opioid receptor)

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