Busetal
Busetal Uses, Dosage, Side Effects, Food Interaction and all others data.
A carbamate derivative used as an alcohol deterrent. It is a relatively nontoxic substance when administered alone, but markedly alters the intermediary metabolism of alcohol. When alcohol is ingested after administration of disulfiram, blood acetaldehyde concentrations are increased, followed by flushing, systemic vasodilation, respiratory difficulties, nausea, hypotension, and other symptoms (acetaldehyde syndrome). It acts by inhibiting aldehyde dehydrogenase.
Busetal produces a sensitivity to alcohol which results in a highly unpleasant reaction when the patient under treatment ingests even small amounts of alcohol. Busetal blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake, the concentration of acetaldehyde occurring in the blood may be 5 to 10 times higher than that found during metabolism of the same amount of alcohol alone. Accumulation of acetaldehyde in the blood produces a complex of highly unpleasant symptoms referred to hereinafter as the disulfiram-alcohol reaction. This reaction, which is proportional to the dosage of both disulfiram and alcohol, will persist as long as alcohol is being metabolized. Busetal does not appear to influence the rate of alcohol elimination from the body. Prolonged administration of disulfiram does not produce tolerance; the longer a patient remains on therapy, the more exquisitely sensitive he becomes to alcohol.
Trade Name | Busetal |
Availability | Prescription only |
Generic | Disulfiram |
Disulfiram Other Names | Disulfiram, Tetraethylthioperoxydicarbonic diamide, Tetraethylthiuram disulfide, Tetraethylthiuram disulphide |
Related Drugs | Vivitrol, naltrexone, acamprosate, Antabuse, Campral, Revia |
Type | |
Formula | C10H20N2S4 |
Weight | Average: 296.539 Monoisotopic: 296.05093141 |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | Peru |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Busetal is a carbamate derivative used to treat alcohol addiction.
For the treatment and management of chronic alcoholism
Busetal is also used to associated treatment for these conditions: Chronic Alcoholism
How Busetal works
Busetal blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake causing an accumulation of acetaldehyde in the blood producing highly unpleasant symptoms. Busetal blocks the oxidation of alcohol through its irreversible inactivation of aldehyde dehydrogenase, which acts in the second step of ethanol utilization. In addition, disulfiram competitively binds and inhibits the peripheral benzodiazepine receptor, which may indicate some value in the treatment of the symptoms of alcohol withdrawal, however this activity has not been extensively studied.
Toxicity
LD50=8.6g/kg (orally in rats). Symptoms of overdose include irritation, slight drowsiness, unpleasant taste, mild GI disturbances, and orthostatic hypotension.
Food Interaction
- Avoid alcohol. Avoid alcohol for up to 14 days after discontinuation.
- Take with or without food. The absorption is unaffected by food.
Busetal Alcohol interaction
[Major] CONTRAINDICATED:
Consumption of ethanol during treatment with disulfiram may cause flushing, nausea, blurred vision, dyspnea, tachypnea, tachycardia, and hypotension.
Death has been reported.
The mechanism is probably related to inhibition of aldehyde dehydrogenase, the enzyme responsible for the oxidation of acetaldehyde to acetyl CoA.
Accumulation of acetaldehyde probably results.
Ethanol should be avoided in patients receiving disulfiram.
Busetal Drug Interaction
Moderate: clonazepam, clonazepam, alprazolam, alprazolamUnknown: duloxetine, duloxetine, lamotrigine, lamotrigine, lurasidone, lurasidone, escitalopram, escitalopram, fluoxetine, fluoxetine, quetiapine, quetiapine, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Busetal Disease Interaction
Major: alcohol intoxication, cardiac disease, disulfiram reaction, psychosesModerate: hepatotoxicity
Elimination Route
Busetal is absorbed slowly from the gastrointestinal tract (80 to 90% of oral dose).
Innovators Monograph
You find simplified version here Busetal