NationMaster - Encyclopedia: Disulfiram

Disulfiram is a drug used to support the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Trade names for disulfiram in different countries are Antabuse and Antabus manufactured by Odyssey Pharmaceuticals. Disulfiram is also being studied as a treatment for cocaine dependence, as it prevents the breakdown of dopamine (a neurotransmitter whose release is stimulated by cocaine); the excess dopamine results in increased anxiety, higher blood pressure, restlessness and other unpleasant symptoms. The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... It has been suggested that Blockbuster drug be merged into this article or section. ... Alcoholism is the consumption of, or preoccupation with, alcoholic beverages to the extent that this behavior interferes with the drinkers normal personal, family, social, or work life, and may lead to physical or mental harm. ... Ethanol, also known as ethyl alcohol, drinking alcohol or grain alcohol, is a flammable, colorless, slightly toxic chemical compound, and is best known as the alcohol found in alcoholic beverages. ... Cocaine is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. ... Dopamine is a phenethylamine naturally produced by the human body. ...

Interaction with alcohol

Under normal metabolism, alcohol is broken down in the liver by the enzyme alcohol dehydrogenase to acetaldehyde, which is then converted by the enzyme acetaldehyde dehydrogenase to the harmless acetic acid. Disulfiram blocks this reaction at the intermediate stage by blocking the enzyme acetaldehyde dehydrogenase. After alcohol intake under the influence of disulfiram, the concentration of acetaldehyde in the blood may be 5 to 10 times higher than that found during metabolism of the same amount of alcohol alone. As acetaldehyde is one of the major causes of the symptoms of a "hangover" this produces immediate and severe negative reaction to alcohol intake. Some 5-10 minutes after alcohol intake, the patient may experience the effects of a severe hangover for a period of 30 minutes up to several hours. Symptoms include flushing of the skin, accelerated heart rate, shortness of breath, nausea, and vomiting. A few of the metabolic pathways in a cell. ... The liver is an organ present in vertebrates and some other animals. ... Ribbon diagram of the enzyme TIM, surrounded by the space-filling model of the protein. ... Alcohol Dehydrogenase Alcohol dehydrogenases are a group of dehydrogenase enzymes that occur in many organisms and facilitate the interconversion between alcohols and aldehydes or ketones. ... R-phrases , , S-phrases , , , Flash point âˆ’39 Â°C Autoignition temperature 185 Â°C RTECS number AB1925000 Supplementary data page Structure and properties n, Îµr, etc. ... Acetaldehyde dehydrogenase Acetaldehyde dehydrogenase (EC 1. ... Acetic acid, also known as ethanoic acid, is an organic chemical compound with the formula CH3COOH best recognized for giving vinegar its sour taste and pungent smell. ... A hangover (veisalgia) describes the sum of unpleasant physiological effects following heavy consumption of drugs, particularly alcoholic beverages. ... A hangover (veisalgia) describes the sum of unpleasant physiological effects following heavy consumption of drugs, particularly alcoholic beverages. ... Look up flushing in Wiktionary, the free dictionary. ... Dyspnea (Latin dyspnoea, Greek dyspnoia from dyspnoos - short of breath) or shortness of breath (SOB) is perceived difficulty breathing or pain on breathing. ... For the Beck song, see Nausea (song). ... Vomiting (also throwing up or emesis) is the forceful expulsion of the contents of ones stomach through the mouth and sometimes the nose. ...

Disulfiram should not be taken if alcohol has been consumed in the last 12 hours. There is no tolerance to disulfiram: the longer it is taken, the stronger its effects. As disulfiram is absorbed slowly through the digestive tract and eliminated slowly by the body the effects may last for up to 2 weeks after the initial intake; consequently, medical ethics dictate that patients must be fully informed about the disulfiram-alcohol reaction. Possible side effects while taking Disulfiram are numbness or tingling of the lower legs and shortness of breath. Medical ethics is primarily a field of applied ethics, the study of moral values and judgments as they apply to medicine. ...

Dosage

Disulfiram is supplied in 200 mg, 250 mg and 500 mg tablets. The usual initial dose is 500 mg for 1 to 2 weeks, followed by a maintenance dose of 250 mg (range 125 mg - 500 mg) per day. The total daily dosage should not exceed 500 mg.

History

The drug's action was discovered by accident in the 1948 by the researchers Erik Jacobsen and Jens Hald at the Danish drug company Medicinalco. The substance was intended to provide a remedy for parasitic infestations; however, workers testing the substance on themselves reported severe symptoms after alcohol consumption. Year 1948 (MCMXLVIII) was a leap year starting on Thursday (link will display the 1948 calendar) of the Gregorian calendar. ...

Limitations

From a practical standpoint, disulfiram is not a "cure" for alcoholism, since it is easier for an alcoholic to stop taking disulfiram than alcohol; if the treatment is not supervised, an alcoholic may abandon the treatment — and even when disulfiram therapy is strictly enforced, the negative effects are rarely enough to break the drinking patterns of a chronic alcoholic. In some extreme cases, patients with subcutaneous disulfiram tablet implants have been known to cut or dig out the tablet to avoid its effects. For these reasons, disulfiram is usually only indicated for select patients who wish to remain in an enforced state of sobriety during other forms of treatment, such as support groups and psychotherapy. Alcoholism is the consumption of, or preoccupation with, alcoholic beverages to the extent that this behavior interferes with the drinkers normal personal, family, social, or work life, and may lead to physical or mental harm. ... The subcutis is the layer of tissue directly underlying the cutis. ... Support groups exist to combat or legitimise conditions or behaviours. ... Psychotherapy is an interpersonal, relational intervention used by trained psychotherapists to aid clients in problems of living. ...

Similarly acting substances

Coprine (N5-1-hydroxycyclopropyl-L-glutamine) which metabolises to 1-aminocyclopropanol, a closely-related chemical having the same metabolic effects, occurs naturally in several edible mushroom species, such as the Common Ink Cap. Mushroom(s) are the fleshy, spore-bearing fruiting bodies of fungi typically produced above ground on soil or on their food sources. ... Binomial name Coprinopsis atramentaria (Bull. ...

Temposil, or citrated calcium carbamide, has the same function as disulfiram, but is weaker and safer. Calcium carbamide, sold under the trade name TemposilÂ®, is an alcohol sensitizing agent. ...

Dangerous drug interactions

Disulfiram should not be administered to patients who take certain stimulant drugs and antidepressants. Disulfiram has been found to inhibit the enzyme dopamine-beta-hydroxylase, blocking the metabolism of dopamine into norepinephrine. Combined with the dopamine agonist and/or reuptake effect of stimulants, this can cause a dramatic rise in synaptic dopamine levels, resulting in sleeplessness, paranoia, and, in extreme cases, stimulant psychosis. Dopamine Î²-hydroxylase (DBH) is an enzyme that converts dopamine to norepinephrine: In the peripheral nervous system, it is located predominantly within sympathetic nerve vesicles, but it is also present in preganglionic motor nerve fibers of the vagus nerve. ... Dopamine is a phenethylamine naturally produced by the human body. ... Norepinephrine (INN)(abbr. ... Dopamine is a phenethylamine naturally produced by the human body. ... Reuptake, or re-uptake, is the reabsorption of a neurotransmitter by the neurotransmitter transporter of a pre-synaptic neuron after it has performed its function of transmitting a neural impulse. ... Stimulants are drugs that temporarily increase alertness and wakefulness. ... Amphetamine psychosis is a form of psychosis which can result from amphetamine or methamphetamine use. ...

Drugs that are known to interfere with the dopamine / norepinephrine system include, but are not limited to:

The metabolism of other drugs may be inhibited by disulfiram, increasing their potential for toxic effects. Drugs known to have adverse effects when used concurrently with disulfiram include amitriptyline, isoniazid, and metronidazole (all with acute changes in mental state), phenytoin, some benzodiazepines, morphine, pethidine, and barbiturates. Bupropion (INN; also amfebutamone,[1] brand names Wellbutrin, Zyban, Budeprion and Buproban) is an atypical antidepressant, which acts as a norepinephrine reuptake inhibitor and dopamine reuptake inhibitor,[2] and a nicotinic antagonist. ... Amphetamine or Amfetamine (Alpha-Methyl-PHenEThylAMINE), also known as, beta-phenyl-isopropylamine, and benzedrine, is a prescription stimulant commonly used to treat Attention-deficit hyperactivity disorder (ADHD) in adults and children. ... Vitamin R redirects here. ... Cocaine is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. ... Amitriptyline (or Amitryptyline) hydrochloride (sold as Elavil, Tryptanol, Endep, Elatrol, Tryptizol, Trepiline, Laroxyl) is a tricyclic antidepressant drug. ... Isoniazid (also called isonicotinyl hydrazine or isonicotinic acid hydrazide); abbreviated INH or just H. Isoniazid is a first-line antituberculous medication used in the prevention and treatment of tuberculosis. ... Metronidazole (INN) (IPA: ) is a nitroimidazole anti-infective drug used mainly in the treatment of infections caused by susceptible organisms, particularly anaerobic bacteria and protozoa. ... Phenytoin sodium (marketed as DilantinÂ® in the USA and as EpanutinÂ® in the UK, by Parke-Davis, now part of Pfizer) is a commonly used antiepileptic. ... Benzodiazepine tablets The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsant, amnestic and muscle relaxant properties. ... Morphine (INN) (IPA: ) is a highly potent opiate analgesic drug and is the principal active agent in opium and the prototypical opiate. ... Pethidine (INN) or meperidine (USAN) (also referred to as: isonipecaine; lidol; pethanol; piridosal; AlgilÂ®; AlodanÂ®; CentralginÂ®; DemerolÂ®; DispadolÂ®; DolantinÂ®; DolarganÂ® (in Poland);[1] DolestineÂ®; DolosalÂ®; DolsinÂ®; MefedinaÂ®) is a fast-acting opioid analgesic drug. ... Barbiturates are drugs that acts as central nervous system (CNS) depressants, and by virtue of this they produce a wide spectrum of effects, from mild sedation to anesthesia. ...

Organic chemistry

Disulfiram is an example of a thiuram disulfide, that is the oxidized derivative of diethyldithiocarbamate. In chemistry, a disulfide is an ion formed by sulfur atoms. ... Sodium diethyldithiocarbamate is the chemical compound with the formula NaS2CN(C2H5)2. ...

See also

Naltrexone is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. ...

External links

Categories: Alcohol abuse | Drugs | Thiuram disulfides Addiction is an uncontrollable compulsion to repeat a behavior regardless of its negative consequences. ... A section of the Anatomical Therapeutic Chemical Classification System. ... Nicotine is an alkaloid found in the nightshade family of plants (Solanaceae), predominantly in tobacco, and in lower quantities in tomato, potato, eggplant (aubergine), and green pepper. ... Nicotine is an alkaloid found in the nightshade family of plants (Solanaceae), predominantly in tobacco, and in lower quantities in tomato, potato, eggplant (aubergine), and green pepper. ... Bupropion (INN; also amfebutamone,[1] brand names Wellbutrin, Zyban, Budeprion and Buproban) is an atypical antidepressant, which acts as a norepinephrine reuptake inhibitor and dopamine reuptake inhibitor,[2] and a nicotinic antagonist. ... Varenicline (trade name Chantix in the USA and Champix in Europe and Canada, manufactured by Pfizer, usually in the form of varenicline tartrate) is a prescription medication used to treat smoking addiction. ... This article needs cleanup. ... Calcium carbamide, sold under the trade name TemposilÂ®, is an alcohol sensitizing agent. ... acamprosate ... Naltrexone is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. ... Opioid dependence is a medical diagnosis characterized by an individuals inability to stop using opioids even when objectively in his or her best interest to do so. ... Buprenorphine, is an opioid drug with partial agonist and antagonist actions. ... Methadone is a synthetic opioid, used medically as an analgesic and in the treatment of narcotic addiction. ... Levacetylmethadol (INN, or methadyl acetate) is a drug used in treating opioid addiction. ... Lofexidine is an alpha2-adrenergic receptor agonist, can be used as a short acting (short half life) anti-hypertensive, but mostly used to help with relief from symptoms of heroin or opiate withdrawal in opiate dependency. ... Naltrexone is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. ... A section of the Anatomical Therapeutic Chemical Classification System. ... Lindane is an insecticide, also known as gamma-Hexachlorocyclohexane (HCH) and benzene hexachloride (BHC). ... Pyrethrum refers to several Old World plants of the genus Chrysanthemum (e. ... Phenothrin is a synthetic pyrethroid that kills adult fleas and ticks. ... Permethrin is a common synthetic chemical, widely used as an insecticide and acaricide and as an insect repellent. ... This page may meet Wikipedias criteria for speedy deletion. ... Malathion is a organophosphate parasympathomimetic which binds irreversibly to cholinesterase. ... Species See text Quassia is a genus of about 40 species of tropical evergreen trees and shrubs native to Asia. ...

Contents

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