Methohexital Sodium, a barbiturate derivative, is often administered under the trade names Brevital and Brevital Sodium. It is primarily used as an anesthetic for inducing sedation and anesthesia during various medical procedures. Methohexital Sodium is a central nervous system depressant that targets the brain's
GABA receptors, facilitating fast onset sedation. Originally developed in the mid-20th century, Methohexital Sodium has undergone extensive research to validate its efficacy and safety. Institutions such as the American Society of Anesthesiologists and various pharmaceutical companies have extensively studied this drug to establish its clinical applications. Methohexital Sodium is primarily indicated for short-term anesthesia, especially in outpatient settings, pediatric anesthesia, and during electroconvulsive therapy (ECT).
The mechanism of action for Methohexital Sodium is similar to other barbiturates but is distinctly rapid in its onset and short in its duration. It works by enhancing the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) at the
GABA-A receptor. This interaction increases the flow of chloride ions into neurons, making them hyperpolarized and less likely to fire action potentials, thus leading to depressant effects on the central nervous system. This potent action on GABA receptors results in quick sedation, making the drug particularly useful for procedures that require rapid onset and short duration of anesthesia. Methohexital's potent and immediate effect on GABA receptors is the cornerstone of its anesthetic properties.
Methohexital Sodium is administered intravenously, typically as a single bolus or through continuous infusion depending on the procedural requirements. It can also be administered rectally in pediatric patients. For intravenous administration, the onset time is remarkably fast, often within 30 seconds to a minute. This rapid onset makes Methohexital ideal for procedures requiring quick sedation and recovery. The drug's effect peaks within a few minutes and wears off relatively quickly, which is beneficial for outpatient procedures where patients are expected to regain consciousness and motor function promptly after the procedure. The duration of action is approximately 5-7 minutes, although this can vary slightly depending on individual patient factors such as age, weight, and overall health.
Despite its efficacy, Methohexital Sodium has a range of side effects and contraindications. Common side effects include
respiratory depression,
hypotension, and
myocardial depression. Patients may also experience
dizziness,
nausea,
vomiting, or
allergic reactions, although these are relatively rare. Due to its potent central nervous system depressant effects, Methohexital Sodium should be used with caution in patients with compromised respiratory function or
cardiovascular instability. It is contraindicated in patients with a known hypersensitivity to barbiturates,
severe asthma, or
porphyria. Furthermore, care must be taken when administering Methohexital Sodium to elderly patients or those with liver or kidney impairment, as these conditions can alter the drug's pharmacokinetics and dynamics, potentially leading to prolonged sedation or adverse effects.
The interaction of Methohexital Sodium with other drugs is an important consideration to ensure patient safety and drug efficacy. This drug can potentiate the effects of other central nervous system depressants, such as benzodiazepines, opioids, and alcohol, leading to increased risk of respiratory depression and hypotension. It can also interact with certain antihypertensive medications, leading to enhanced hypotensive effects. Additionally, drugs that induce hepatic enzymes, such as
phenytoin or
rifampin, can decrease the efficacy of Methohexital Sodium by increasing its metabolic rate. Conversely, inhibitors of hepatic enzymes, such as
cimetidine, may prolong the effects of Methohexital Sodium by slowing its metabolism. It is crucial for healthcare providers to assess a patient's current medications and health status to avoid potentially dangerous drug interactions or side effects.
In summary, Methohexital Sodium is a highly effective anesthetic agent with a rapid onset and short duration of action, making it suitable for a variety of medical procedures requiring quick sedation. Its mechanism of action largely hinges on its interaction with GABA receptors in the brain, resulting in potent central nervous system depression. While generally safe when used appropriately, it does have potential side effects and contraindications that must be carefully considered. Moreover, its interactions with other drugs necessitate a thorough evaluation of the patient's medication regimen and overall health status to ensure its safe and effective use.
How to obtain the latest development progress of all drugs?
In the Synapse database, you can stay updated on the latest research and development advances of all drugs. This service is accessible anytime and anywhere, with updates available daily or weekly. Use the "Set Alert" function to stay informed. Click on the image below to embark on a brand new journey of drug discovery!


