Drug intelligence / Profile preview

diclofenac + baclofen + orphenadrine + bupivacaine

Development stage
Preclinical
Lead developer
Transdermal Therapeutics
Modality
Small Molecules
Administration
Topical, Intravenous, Intramuscular, Subcutaneous, Oral, Infiltration, Nerve Block, Intrathecal
01

Overview

This is a **combination drug** composed of four distinct active pharmaceutical ingredients: **diclofenac**, **baclofen**, **orphenadrine**, and **bupivacaine**, each with different mechanisms of action targeting pain and muscle spasm. - **Diclofenac** is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) enzymes, primarily COX-2, reducing prostaglandin synthesis and thus decreasing inflammation and pain. - **Baclofen** is a centrally acting skeletal muscle relaxant, a gamma-aminobutyric acid (GABA)-B receptor agonist, reducing excitatory neurotransmitter release and causing muscle relaxation. - **Orphenadrine** is a muscle relaxant with anticholinergic and antihistaminic properties, believed to reduce pain via NMDA receptor antagonism, inhibition of norepinephrine reuptake, and sodium channel blockade. - **Bupivacaine** is an amide-type local anesthetic that blocks voltage-gated sodium channels, inhibiting nerve impulse transmission to produce sensory and motor neuronal blockade and thus local or regional anesthesia. This combination is experimental for multimodal analgesia, mainly in the form of compounded topical pain creams or as separate injections/infusions for acute or postoperative pain, targeting both inflammatory and neuropathic mechanisms. No fixed-dose commercial product containing all four drugs is marketed or approved, but there are compounded formulations and research interest in using such combinations for enhanced pain relief, including for neuropathic and musculoskeletal pain, particularly where both muscle spasm and severe pain are present.[7][3][5][6][1][2]

Other names
Topical Diclofenac, Baclofen, Orphenadrine, and Bupivacaine Cream
02

Targets

NET (Norepinephrine Transporter)NaV (Voltage-gated sodium channels)HRH1 (Histamine H1 Receptor)PGHS-1 (Prostaglandin G/H Synthase 1)M1 (Muscarinic acetylcholine receptor M1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NMDAR (Glutamate receptor ionotropic, NMDA)GABA-B (Gamma-aminobutyric acid receptor type B)

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