Drug intelligence / Profile preview

propofol + rocuronium + caffeine + acetaminophen + bupivacaine

Development stage
Phase 4
Lead developer
AkzoNobel
Modality
Small Molecules
Administration
Intravenous, Oral, Topical, Regional (e.g. Epidural, Nerve Block)
01

Overview

This is a **combination of five pharmaceutical agents**: propofol, rocuronium, caffeine, acetaminophen, and bupivacaine. Such a formulation does not correspond to any marketed fixed-dose combination or branded product, but each component is widely used in clinical settings. - **Propofol** is an intravenous anesthetic agent primarily used for induction and maintenance of general anesthesia and sedation. Its main mechanism is potentiation of GABA_A receptor activity, leading to CNS depression and rapid loss of consciousness[6][7]. - **Rocuronium** is a non-depolarizing neuromuscular blocker (muscle relaxant) used to facilitate endotracheal intubation and muscle relaxation during surgery. It acts as an antagonist at the nicotinic acetylcholine receptor at the neuromuscular junction[2][3]. - **Caffeine** is a central nervous system stimulant, commonly used to increase alertness and counteract sedative effects. In medicine, it may be used for apnea of prematurity and as an adjuvant in some analgesic combinations. It acts as an antagonist of adenosine receptors. - **Acetaminophen** (paracetamol) is an analgesic and antipyretic agent used for pain and fever reduction. Its mechanism is not fully understood but is thought to involve inhibition of central prostaglandin synthesis. - **Bupivacaine** is a long-acting local anesthetic used for regional anesthesia, including nerve blocks and epidural anesthesia. It works as a sodium channel blocker, inhibiting nerve signal conduction. No evidence was found for a fixed commercial or investigational product containing all five ingredients. In clinical practice, combinations of some of these agents (especially propofol with rocuronium) are used in anesthesia, but not with all five in a single preparation[1][4][5].

02

Targets

ADOR (Adenosine receptors)GABRR (GABA-A receptor subunit rho)Muscle-type nicotinic acetylcholine receptorCOXGABRB3 (GABA-A receptor subunit beta-3)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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