Drug intelligence / Profile preview

propofol + magnesium sulphate + nalbuphine

Development stage
Preclinical
Lead developer
AkzoNobel
Modality
Small Molecules
Administration
Intravenous, Intrathecal
01

Overview

This drug is a **combination of three agents: propofol, magnesium sulphate, and nalbuphine**. - **Propofol** is a short-acting intravenous anesthetic agent used for induction and maintenance of anesthesia and sedation. It exerts its effects primarily through positive allosteric modulation of GABA-A receptors, enhancing the inhibitory neurotransmission in the central nervous system. - **Magnesium sulphate** is an inorganic salt with analgesic and NMDA receptor antagonist properties, often used as an adjunct to anesthesia for its role in reducing perioperative pain and providing neuroprotection. - **Nalbuphine** is a synthetic opioid analgesic with agonist activity at kappa opioid receptors and antagonist/partial agonist activity at mu opioid receptors; it is used for moderate to severe pain, and also as an adjunct in anesthesia for its opioid-sparing and anti-shivering effects. This specific combination is used in clinical anesthesia for procedures requiring deep sedation or general anesthesia, where the synergistic effects can reduce propofol requirements, enhance analgesia, decrease opioid consumption, and minimize side effects such as injection pain and perioperative shivering[1][2][4][6].

02

Targets

KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)GABRB2 (GABA-A receptor subunit beta-2)MOR (Mu opioid receptor)GABRB3 (GABA-A receptor subunit beta-3)NMDAR (Glutamate receptor ionotropic, NMDA)

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