MedlinePlus a682417 Biological half-life 100 hours. | ATC code none Excretion Urine | |
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AHFS/Drugs.com Consumer Drug Information Legal status CA: Schedule IV
DE: Anlage II (Prohibited)
US: Schedule III | ||
Butabarbital (trade name Butisol) is a prescription barbiturate sleep aid. Butabarbital has a particularly fast onset of effects and short duration of action compared to other barbiturates, which makes it useful for certain applications such as treating severe insomnia and relieving anxiety before surgical procedures; however it is also relatively dangerous particularly when combined with alcohol, and so is now rarely used, although it is still prescribed in some Eastern European and South American countries. Its intermediate duration of action gives butabarbital an abuse potential slightly lower than secobarbital.
Contents
- History
- Treatment Clinical Uses
- Administration
- Clinical Effects Elimination
- Overdose Abuse
- Side Effects
- References
Butabarbital is also sold in combination with belladonna alkaloids under the brand name Butibel. The belladonna is added for antispasmodic effect. This product contains a low dose of butabarbital combined with a standardised mix of belladonna alkaloids and is used as an antispasmodic taken to relieve cramping and spasms of the stomach and intestines. They are used also to decrease the amount of acid formed in the stomach. Another similar product is Donnatal, which contains belladonna alkaloids combined with phenobarbital.
History
Barbiturates were first discovered to have medical use in 1903, when a research at Bayer showed barbital to be an effective sedative for dogs. It was not until the mid 20th century that the habit forming nature of barbiturates and behavioral side effects were first noted
Butabarbital was approved for medical use in 2007 under the brand name Butisol Sodium. Butisol sodium is manufactured by Meda Pharmaceuticals as a Schedule III controlled substance due to its high risk for abuse and dependence. Benzodiazapines are more commonly administered today for their similar sedative and hypnotic properties, and reduced risk of physical dependence. Barbiturate drugs such as butabarbital sodium are used now for short-term and acute treatment under strict doctor supervision only
Treatment & Clinical Uses
Barbiturates are non-selective depressants of the central nervous system, inducing drowsiness and mild sedative effects. Barbiturate hypnotics are used in the treatment of sleep and anxiety disorders for their calming and sedative properties, however are usually restricted to short term use due to risk of dependency.
Butabarbital, most commonly known as Butisol commercially, is an approved Schedule III drug in the US and Canada used in the short term treatment of anxiety disorders and as a pre-surgical sedative aid. Approved commercial forms are available in tablet or elixir forms.
Administration
It is most often administered orally as either sodium solution or tablet, however can also be given by intravenous injection. Tablets contain either 30 mg or 50 mg of butabarbital sodium, or 30 mg/5mL with 7% alcohol/vol in solution. For preoperative sedation, adults are administered 50–100 mg 60-90min prior to surgery, with varying doses for pediatric and geriatric patients.
Clinical Effects & Elimination
Effects from oral doses often are felt within an hour of administration, lasting somewhere from six to eight hours in effect. A non-selective depressant of the CNS, Butabarbital sodium is used as a sedative hypnotic, depending on dose, to induce drowsiness or sleep, or reduce anxiety and tension. Butabarbital sodium can be used as a pre-surgical anesthetic aid or in the short-term treatment of sleep and anxiety disorders. For short term sleep maintenance and induction butabarbital sodium treatment is recommended to be limited to two weeks, after which it begins to lose efficacy. The half life is approximately 100hrs, eliminated primarily by hepatic microsomal enzymes and excreted in the urine.
Overdose & Abuse
Butabarbital sodium is a Schedule III controlled substance in the US and Canada due to risk of abuse and dependence. A psychoactive substance, butabarbital drugs are often abused with risk of acute intoxication and addiction. Barbiturates such as butabarbital are thought to be habit-forming and addictive, and have severe risks from withdrawal including death. Due the high risk of dependence and overdose, use of butabarbital is highly regulated and has become less common in clinical application.
Side Effects
Those taking Butabarbital are asked to watch out for signs of severe allergic reaction, such as swelling or difficulty breathing. Less serious side effects include dizziness or drowsiness, excitation, headache, nausea, vomiting, or constipation. Psychiatric disturbances (hallucinations, agitation, confusion, depression, or memory problems), ataxia, difficulty breathing, or slow heartbeat could be signs of serious adverse effects and should be brought to the attention of a doctor immediately.
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