Butisol
Butisol Uses, Dosage, Side Effects, Food Interaction and all others data.
Butisol, or Butisol, is a fast onset barbiturate with short duration of action compared to other barbiturates. This makes butabarbital a useful drug for treating severe insomnia and pre-operative anxiety. Butisol is less commonly used in recent years, as more patients are typically prescribed benzodiazepines. Its short duration of action gives butabarbital a high abuse potential, comparable to secobarbital.
Butisol was granted FDA approval on 5 June 1939.
Butisol potentiates GABAergic neurons while inhibiting neuronal acetylcholine and glutamate receptors to produce sedation. Butisol is an intermediate acting barbiturate with a duration of action of approximately 6-8 hours. The therapeutic index is quite wide as doses vary considerably from patient to patient. Patients should be counselled regarding the risk of worsening insomnia, drowsiness, falls, and complex behaviour while not fully awake.
| Trade Name | Butisol |
| Availability | Discontinued |
| Generic | Butabarbital |
| Butabarbital Other Names | Butabarbital, Secbutabarbital, Secbutabarbitale, Secbutabarbitalum |
| Related Drugs | trazodone, hydroxyzine, lorazepam, promethazine, fentanyl, Ativan |
| Type | Tablet and solution |
| Formula | C10H16N2O3 |
| Weight | Average: 212.2456 Monoisotopic: 212.116092388 |
| Protein binding | Data regarding the protein binding of butbarbital is not readily available. However, barbiturates generally bind to serum albumin. |
| Groups | Approved, Illicit |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Butisol is a barbiturate drug used as a sedative and hypnotic.
Butisol is indicated for use as a sedative or hypnotic. Butisol should not be used to treat insomnia for longer than 2 weeks.
Butisol is also used to associated treatment for these conditions: Insomnia
How Butisol works
Barbiturates like butabarbital potentiate GABA-A receptors and inhibit receptors for neuronal acetylcholine, and kainate. GABA-A receptors are predominantly on the post-synaptic membrane, and upon activation, open chloride channels to hyperpolarize the neuron and decreased firing rate. Potentiation of GABAergic neurons produces sedation. Inhibition of neuronal acetylcholine receptors and glutamate receptors of the kainate subtype desensitize their respective neurons, producing sedation.
Toxicity
Patients experiencing an overdose may present with unsteady gait, slurred speech, nystagmus, confusion, poor judgement, irritability, and insomnia. Acute overdoses may present as CNS depression, respiratory depression, oligouria, tachycardia, hypotension, low body temperature, coma, and shock. An extreme overdose can lead to a flat EEG, resembling death, that is reversible provided there is no hypoxic brain damage. Overdose can be treated with symptomatic and supportive treatment.
Food Interaction
- Avoid alcohol. Concomitant use of alcohol and barbiturates may lead to increased.
Butisol Alcohol interaction
[Major] GENERALLY AVOID:
Concurrent acute use of barbiturates and ethanol may result in additive CNS effects,
including impaired coordination, sedation, and death.
Tolerance of these agents may occur with chronic use.
The mechanism is related to inhibition of microsomal enzymes acutely and induction of hepatic microsomal enzymes chronically.
The combination of ethanol and barbiturates should be avoided.
Butisol Drug Interaction
Major: acetaminophen / hydrocodone, acetaminophen / hydrocodoneModerate: duloxetine, duloxetine, amitriptyline, amitriptyline, acetaminophen / butalbital / caffeine, acetaminophen / butalbital / caffeine, escitalopram, escitalopram, pregabalin, pregabalin, montelukast, montelukast, cholecalciferol, cholecalciferolUnknown: docusate, docusate, cyanocobalamin, cyanocobalamin
Half Life
Butisol has a half life of 100 hours but its duration of action is only 6-8 hours.
Elimination Route
Barbiturates such as butabarbital are predominantly eliminated in the urine. In dogs, 3-5% of the dose is eliminated in the urine as the unchanged parent compound.
Innovators Monograph
You find simplified version here Butisol
