Reversal Agents in Sedation and Anesthesia Practice for Dentistry

Abstract

Reversal agents are defined as any drug used to counteract the pharmacologic effects of another drug. Several pharmacologic antagonists serve as essential drugs in the contemporary practices of sedation providers and anesthesiologists. Reversal or “antidote” drugs, such as flumazenil and naloxone, are often used in unintentional overdose situations involving significant benzodiazepine- and/or opioid-induced respiratory depression. Within the context of skeletal muscle relaxation, neostigmine and sugammadex are routinely used to reverse the effects of nondepolarizing neuromuscular blocking agents. In addition, the alpha-adrenergic antagonist phentolamine is used in dentistry as a local anesthetic reversal agent, decreasing its duration of action by inducing vasodilation. This review article discusses the pharmacology, uses, practical implications, adverse effects, and precautions needed for flumazenil, naloxone, neostigmine, sugammadex, and phentolamine within the context of sedation and anesthesia practice for dentistry.

Effects of ketamine and propofol on muscarinic plateau potentials in rat neocortical pyramidal cells

“…Interestingly, cholinergic/muscarinic "arousal" has previously been used by anaesthesiologists to obtain faster awakening from anaesthesia, by giving cholinesterase inhibitor physostigmine intravenously, thus increasing the ACh level in the brain (Anderson 1988). The effect of this procedure was rather moderate, however, and it is now rarely used.…”

Antidotes in Clinical Toxicology—Critical Review

“…Flumazenil acts as a nonspecific competitive agonist on the GABA-benzodiazepine receptor (GABAA), competing with benzodiazepine and rapidly reversing its action by reducing the influx of afferent chloride ( Figure 4 ). The first effects can be noticeable within one minute of flumazenil administration and the maximum therapeutic effect is reached within 6 to 10 min and lasts 19 to 50 min, depending on the initial dose and plasma benzodiazepine concentration [ 102 , 103 ]. After using flumazenil, the patient should be closely monitored because its duration of action is shorter than benzodiazepines and may result in resedation [ 104 ].…”

“…Flumazenil is also used as an antisedation agent for benzodiazepines used to calm the patient during certain medical procedures. It also influences the restoration of proper respiratory and cardiovascular function by eliminating the central effect of benzodiazepine derivatives [ 103 , 107 ]. There are ongoing studies that indicate flumazenil as a potentially effective agent in the treatment of central disorders of excessive hypersomnolence resistant to treatment with available drugs that stimulate wakefulness [ 108 ] and studies on the use of flumazenil in the treatment of liver encephalopathy [ 109 ].…”