Drug intelligence / Profile preview

propofol + remifentanil + sevoflurane

Development stage
Unknown
Lead developer
AkzoNobel
Modality
Small Molecules
Administration
Intravenous, Inhalation
01

Overview

The combination of propofol, remifentanil, and sevoflurane is a frequently used anesthetic regimen in modern surgical practice. This combination leverages the complementary properties of these three agents to provide effective anesthesia with favorable pharmacokinetic profiles. **Propofol** is an intravenous anesthetic agent with rapid onset and short duration of action. It produces its effects through interaction with neurotransmitter receptors, constricting cerebral vessels and protecting the auto-regulated function of cerebral vessels[5]. Propofol is commonly used for both induction and maintenance of anesthesia. **Remifentanil** is a potent, short-acting synthetic opioid analgesic marketed under the brand name Ultiva. It has an extremely rapid onset and short context-sensitive half-life, making it ideal for providing analgesia during surgical procedures[3]. Remifentanil is used as an adjunct to anesthetics and for sedation, allowing for high-dose opioid and low-dose hypnotic anesthesia due to synergism with various hypnotic drugs and volatile anesthetics[3]. **Sevoflurane** is an inhaled anesthetic agent used for induction and maintenance of general anesthesia. It is a volatile, non-flammable compound with low solubility and blood/gas partition coefficient. Unlike other volatile anesthetics, sevoflurane has a pleasant odor and doesn't irritate the airways, making it suitable for inhalational induction in both adults and children[4]. ## Clinical Applications This combination is used in various surgical procedures, including: - Radical gastrectomy[1] - Craniotomy and neurosurgery[5] - Tracheal intubation without neuromuscular blocking agents[2] - Electroconvulsive therapy (when propofol and remifentanil are used together)[3] ## Efficacy and Safety Studies have shown that the addition of sevoflurane to propofol and remifentanil can improve intubation conditions and provide hemodynamic stability[2]. In one study, the addition of 7% sevoflurane to propofol (2 mg/kg) and remifentanil (1 μg/kg) provided satisfactory intubation conditions without hemodynamic compromise in healthy premedicated patients with favorable airway anatomy[2]. When comparing propofol combined with remifentanil versus propofol combined with sevoflurane for patients undergoing radical gastrectomy, research has shown that propofol combined with sevoflurane anesthesia had less effect on respiration and circulation of patients[1]. For neurosurgery specifically, both sevoflurane-remifentanil and propofol-remifentanil combinations have shown good anesthetic effects, though propofol-remifentanil was more likely to cause lactic acidosis and hypertension in some studies[5]. The combination of these three agents allows clinicians to leverage their complementary properties while potentially reducing the required doses of each individual agent, thereby potentially minimizing side effects.

02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)MOR (Mu opioid receptor)GABRR (GABA-A receptor subunit rho)

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