Overview of Butabarbital Sodium
Butabarbital sodium, commonly known by the brand name Butisol, is a barbiturate drug used as a sedative and hypnotic. It is characterized by its fast onset and short duration of action compared to other barbiturates, making it useful for treating severe insomnia and pre-operative anxiety[1][5].
Clinical Trials and Current Status
FDA Approval and Historical Use
Butabarbital sodium was granted FDA approval on June 5, 1939. Despite its long history, it is less commonly used today due to the preference for benzodiazepines in clinical practice[1].
Ongoing and Completed Trials
There are no recent clinical trials specifically focused on butabarbital sodium listed in the available sources. The drug has been well-established for decades, and most of the current research is not centered around new clinical trials for butabarbital itself. Instead, research often compares barbiturates to newer classes of sedatives and hypnotics, such as benzodiazepines[1][5].
Safety Concerns and Long-term Effects
While butabarbital sodium is not the subject of new clinical trials, studies on other barbiturates, like phenobarbital, highlight potential long-term neurodevelopmental risks. For example, phenobarbital has been associated with negative neurodevelopmental outcomes in infants, including lower cognitive and motor scores. However, these findings are specific to phenobarbital and not directly applicable to butabarbital sodium[3].
Mechanism of Action and Pharmacodynamics
Butabarbital sodium acts by potentiating GABA-A receptors and inhibiting neuronal acetylcholine and glutamate receptors. This action results in sedation by hyperpolarizing neurons and decreasing their firing rate. The drug is classified as an intermediate-acting barbiturate with a duration of action of approximately 6-8 hours[1][5].
Market Analysis
Current Market Status
The market for barbiturates, including butabarbital sodium, has declined in recent years due to the increased use of benzodiazepines and other newer sedatives. Benzodiazepines offer similar therapeutic effects with potentially fewer side effects and lower abuse potential, making them a preferred choice for many clinicians[1].
Market Projections
Given the trend towards using newer classes of sedatives, the market for butabarbital sodium is not expected to grow significantly. The global market for sedatives and hypnotics is evolving, with a focus on safer and more effective alternatives. However, butabarbital sodium may still maintain a niche presence in certain clinical scenarios where its specific pharmacokinetic profile is advantageous[2].
Competitive Landscape
The competitive landscape for sedatives and hypnotics is dominated by benzodiazepines and non-benzodiazepine hypnotics. These drugs offer a broader therapeutic index and lower risk of dependence compared to barbiturates. The market is also seeing the introduction of new drugs with innovative mechanisms of action, further reducing the market share of traditional barbiturates like butabarbital sodium[4].
Dosage and Administration
Butabarbital sodium is available in oral forms, including tablets and an oral solution. The dosage is typically adjusted based on the patient's response, with plasma concentrations of 2-3 μg/mL producing sedation and concentrations above 30 μg/mL potentially leading to coma or lethality[5].
Side Effects and Contraindications
Common side effects of butabarbital sodium include drowsiness, falls, and complex behaviors while not fully awake. Patients should be counseled about the risks of worsening insomnia and other adverse effects. The drug has a high abuse potential due to its short duration of action, similar to secobarbital[1][5].
Elimination and Metabolism
Butabarbital sodium is primarily eliminated in the urine, with approximately 1-2% of the oral dose excreted unchanged. The plasma half-life varies, with reports ranging from 34-42 hours to an average of 100 hours in adults[5].
Key Takeaways
- Clinical Trials: There are no recent clinical trials specifically focused on butabarbital sodium.
- Market Status: The market for butabarbital sodium is declining due to the preference for benzodiazepines and other newer sedatives.
- Mechanism of Action: Butabarbital sodium potentiates GABA-A receptors and inhibits neuronal acetylcholine and glutamate receptors.
- Dosage and Administration: Available in oral forms, with dosages adjusted based on patient response.
- Side Effects: Includes drowsiness, falls, and complex behaviors; high abuse potential.
FAQs
What is butabarbital sodium used for?
Butabarbital sodium is used as a sedative or hypnotic to treat anxiety and short-term insomnia, as well as for pre-operative sedation[1][5].
Why is butabarbital sodium less commonly used today?
Butabarbital sodium is less commonly used today due to the preference for benzodiazepines, which offer similar therapeutic effects with potentially fewer side effects and lower abuse potential[1].
What is the mechanism of action of butabarbital sodium?
Butabarbital sodium acts by potentiating GABA-A receptors and inhibiting neuronal acetylcholine and glutamate receptors, leading to sedation[1][5].
What are the common side effects of butabarbital sodium?
Common side effects include drowsiness, falls, and complex behaviors while not fully awake. Patients should also be aware of the risk of worsening insomnia[1][5].
How is butabarbital sodium eliminated from the body?
Butabarbital sodium is primarily eliminated in the urine, with approximately 1-2% of the oral dose excreted unchanged[5].
What is the typical duration of action for butabarbital sodium?
The duration of action for butabarbital sodium is approximately 6-8 hours, classifying it as an intermediate-acting barbiturate[1][5].
Sources
- DrugBank: Butabarbital: Uses, Interactions, Mechanism of Action.
- Market Research Reports: Global Pentobarbital Sodium Injection Market Research Report 2024.
- FDA: 215910Orig1s000 OTHER REVIEW(S).
- DailyMed: NEMBUTAL SODIUM- pentobarbital sodium injection.
- PharmaCompass: Butabarbital | Drug Information, Uses, Side Effects, Chemistry.
