Drug intelligence / Profile preview

lidocaine + adrenaline + ketamine + midazolam

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Subcutaneous, Local (infiltration)
01

Overview

This is a **combination drug** consisting of four active pharmaceutical ingredients: - **Lidocaine**: A local anesthetic that works by blocking sodium channels (mainly Sodium channel protein type 1 subunit alpha) on neuronal cell membranes, resulting in inhibition of nerve impulse conduction to produce anesthesia and analgesia. - **Adrenaline (epinephrine)**: A sympathomimetic that acts primarily on adrenergic receptors, leading to vasoconstriction, which can reduce local bleeding, slow systemic absorption of local anesthetics, and prolong their effect. - **Ketamine**: A dissociative anesthetic that acts as an antagonist at the N-methyl-D-aspartate (NMDA) receptor, producing anesthesia, analgesia, and amnesia. - **Midazolam**: A short-acting benzodiazepine with rapid onset, acting as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA-A) receptor to provide sedation, anxiolysis, amnesia, and muscle relaxation[3][7][4][2][8]. This combination is not a standard, widely-marketed proprietary product but individual or partial combinations of these drugs are frequently used in procedural sedation, analgesia, and anesthesia, especially in emergency and perioperative settings to achieve rapid onset, potent analgesia, sedation, muscle relaxation, and reduced local bleeding[2][6][4][5][8][9]. The combination leverages their complementary mechanisms for synergistic effect in pain control and sedation, while adrenaline serves to prolong lidocaine's local action and reduce bleeding.

02

Targets

ADRA1A (α1A)NaV (Voltage-gated sodium channels)GABAA (Gamma-aminobutyric acid receptor)ADRB1 (β1)NMDAR (Glutamate receptor ionotropic, NMDA)

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