Clinical Pharmacology of Propofol: An Intravenous Anesthetic Agent

Abstract

Propofol is a 2,6-diisopropylphenol with sedative-hypnotic properties. Because of its slight solubility in water, the drug is formulated as an emulsion for clinical use. It is highly lipophilic and distributes extensively in the body. The blood concentration-time profile of propofol after an iv bolus injection follows a three-compartment model with half-lives of 2-4 min, 30-45 min, and 3-63 h, respectively. Propofol is extensively metabolized by the liver prior to its elimination by the kidney. Following an iv dose of 2-2.5 mg/kg, loss of consciousness occurs in less than one minute and lasts for approximately five minutes. Hypnosis can be maintained by propofol blood concentrations of 1.5-6 micrograms/mL in the presence of N2O/O2 (60:40 ratio) or other anesthetic agents. During induction, propofol decreases the systolic and diastolic blood pressure by approximately 20-30 percent with minimal change in heart rate; apnea is also common. The cardiovascular and respiratory effects of propofol, however, should not cause major concern in otherwise healthy patients. By virtue of its pharmacokinetic profile, the drug lends itself to continuous infusion for maintenance of anesthesia. When used as the main anesthetic agent, it produces satisfactory anesthesia with rapid recovery and without major adverse effects in healthy individuals. In continuous infusion propofol can be used as an alternative to inhalation anesthetics.

Effects of Propofol on Electrocardiogram Measures in Mice

“…Decreases in blood pressure with propofol anesthesia are thought to be due in part to inhibition of sympathetic tonus (23). Propofol can also cause decreases in systemic vascular resistance, myocardial blood flow, and oxygen consumption, possibly through direct vasodilation (24).…”

Evaluation of Adeno-Associated Viral Vectors for Liver-Directed Gene Transfer in Dogs

“…The animals in our study received high doses of propofol during the procedure (total, 11.4 mg/kg for S473 and 14.5 mg/kg for S468). Propofol is well known for its ability to cause a decrease in blood pressure in humans (Grounds et al, 1985;Larijani et al, 1989;Muzi et al, 1992;Robinson et al, 1994Robinson et al, , 1997 as well as in dogs (Musk et al, 2005). In the latter study, four groups of 20 dogs each received propofol to establish blood propofol concentrations of 2.5, 3.0, 3.5, and 4.0 mg/ml.…”

Safety and Efficacy of Deep Sedation with Propofol Alone or Combined with Midazolam Administrated by Nonanesthesiologist for Gastric Endoscopic Submucosal Dissection

“…12,13 However, this agent occasionally decreases systemic vascular resistance, cardiac contractility, and ultimately cardiac output without a concomitant change in heart rate, and respiratory depression can also occur. 5,14,15 Recently, several studies have revealed most adverse events associated with propofol sedation were mild and often transient during advanced interventional endoscopic procedure. 12,[16][17][18] A randomized study in Japan, which compared continuous propofol infusion with intermittent midazolam injection during ESD for EGC, found that propofol is a safe and effective sedative agent and that patients treated with propofol had a quicker recovery than those who were treated with midazolam.…”