amobarbital
Dictionary:
am·o·bar·bi·tal (ăm'ō-bär'bĭ-tăl', -tôl') 
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n.
A barbiturate, C11H18N2O3, used as a sedative and a hypnotic.
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| Drug Info: Amobarbital |
Brand names: Amytal®
Chemical formula:
- Español:
- Inyección de amobarbital
Amobarbital injection
What does amobarbital injection do?
AMOBARBITAL (Amytal®) is a barbiturate that slows down activity of the brain and nervous system. Amobarbital has both sedative and hypnotic properties which means it will help you to relax and sleep. Amobarbital can help produce relaxation and drowsiness before surgery. Amobarbital also can help reduce or control seizures (convulsions). It is not for the long-term control or prevention of seizures. Federal law prohibits the transfer of amobarbital to any person other than the patient for whom it was prescribed. Do not share your medicine with anyone else. Generic amobarbital injections are available.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
• an alcohol or drug abuse problem
• breathing difficulties or lung disease
• attempted suicide
• heart disease
• liver disease
• low blood pressure
• mental depression or mental problems
• porphyria
• an unusual or allergic reaction to amobarbital, other barbiturates, medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should I use this medicine?
Amobarbital is for injection into a muscle or into a vein. It is given by a health-care professional in a hospital or clinic setting.
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
Elderly patients over age 65 years may have a stronger reaction to this medicine and need smaller doses.
What if I miss a dose?
This does not apply.What drug(s) may interact with amobarbital?
• alcohol
• caffeine
• chloramphenicol
• chlorpromazine
• cyclophosphamide
• cyclosporine
• digitoxin
• doxorubicin
• doxycycline
• female hormones, including contraceptive or birth control pills
• methoxyflurane
• metronidazole
• medicines for anxiety or sleeping problems
• medicines for hay fever and other allergies
• medicines for high blood pressure
• medicines for mental depression
• medicines for pain
• medicines that help the heart to beat regularly
• quinine
• seizure (convulsion) or epilepsy medicine
• steroid medicines such as prednisone or cortisone
• theophylline
• warfarin
Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking amobarbital?
Your condition will be monitored closely if you are receiving amobarbital for an immediate need. If you do receive amobarbital regularly, visit your prescriber or health care professional for regular checks on your progress.
After receiving amobarbital you may get a residual hangover effect that leaves you drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how amobarbital affects you. To reduce dizzy or fainting spells, do not sit or stand up quickly, especially if you are an older patient. Alcohol can increase possible unpleasant effects. Avoid alcoholic drinks.
Amobarbital can stop birth control pills (oral contraceptives) working properly. Use another method of birth control while you are using amobarbital.
If you are going to have surgery, tell your prescriber or health care professional that you are receiving amobarbital.
What side effects may I notice from receiving amobarbital?
Side effects that you should report to your prescriber or health care professional as soon as possible:
• bone tenderness
• confusion, agitation, changes in mood, or mental ability
• depression
• eye problems, very small or enlarged centers to the eyes
• lightheadedness, fainting spells
• fever, sore throat
• hallucinations
• redness, blistering, peeling or loosening of the skin, including inside the mouth
• shortness of breath, or difficulty breathing
• skin rash, itching, hives
• slow heartbeat
• swelling of the face or lips
• unusual bleeding or bruising; pinpoint red spots on the skin
• unusual tiredness or weakness
• weight loss
• yellowing of skin or eyes
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• clumsiness, unsteadiness, or a "hangover" effect
• constipation
• difficulty sleeping or nightmares
• drowsiness, dizziness
• headache
• irritability, nervousness
• nausea or vomiting
• pain, redness or irritation at the injection site
Where can I keep my medicine?
Keep out of the reach of children.
Use the injection solution within 30 minutes of preparation. Do not use the solution unless quite clear. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
| Wikipedia: Amobarbital |
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Amobarbital
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| Systematic (IUPAC) name | |
| 5-ethyl-5-(3-methylbutyl)-1,3-diazinane-2,4,6-trione | |
| Identifiers | |
| CAS number | 57-43-2 64-43-7 (sodium salt) |
| ATC code | N05CA02 |
| PubChem | 2164 |
| DrugBank | none |
| ChemSpider | 2079 |
| Chemical data | |
| Formula | C11H18N2O3 |
| Mol. mass | 226.272 |
| SMILES | eMolecules & PubChem |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | Hepatic |
| Half life | 8-42 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | Oral, IM, IV, Rectal |
 (what is this?) (verify) |
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Amobarbital (formerly known as amylobarbitone) is a drug that is a barbiturate derivative. It has sedative-hypnotic and analgesic properties. It is a white crystalline powder with no odor and a slightly bitter taste. It was first synthesized in Germany in 1923. If amobarbital is taken for extended periods of time, physical and psychological dependence can develop.
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Pharmacology
According to an in vitro study conducted at the University of British Columbia, amobarbital works by activating GABAA receptors, which decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents.[1]
It has an LD50 in mice of 212 mg/kg s.c.
Metabolism
Amobarbital undergoes both hydroxylation to form 3'-hydroxyamobarbital,[2] and N-glucosidation[3] to form 1-(beta-D-glucopyranosyl)amobarbital.[4]
Indications
Approved
Unapproved/Off-Label
- When given slowly by an intravenous route, sodium amobarbital has a reputation for having activity as a so-called truth serum. A person under the influence of the drug in this circumstance will relate information that he or she would otherwise "block." As such, the drug was first employed clinically by Dr. William Bleckwenn at the University of Wisconsin to circumvent inhibitions in psychiatric patients.[5] It has been used to convict alleged murderers such as Andres English-Howard, who strangled his girlfriend to death but claimed innocence. He was surreptitiously administered the drug, by his attorney, and under the influence of it he revealed why he strangled her and under which circumstances. A year later he confessed, on the stand, and was convicted on the basis of these statements; he later committed suicide in his cell.[6] The use of amobarbital as a truth serum has lost credibility due to the discovery[citation needed] that the subject can be coerced into having a 'false memory' of the event. In controlled doses, it is used in the Narco Analysis test to trace crime and criminals in modern forensics.[citation needed]
- The drug may be used intravenously to interview patients with Catatonic mutism, sometimes combined with caffeine to prevent sleep.[7]
- It was used by the U.S. Army during World War II's Battle of the Bulge to get shell-shocked GI's back to the frontline.[8]
Contraindications
The following drugs should be avoided when taking amobarbital:
- Alcohol
- Caffeine[citation needed]
- Chloramphenicol
- Chlorpromazine
- Cyclophosphamide
- Ciclosporin
- Digitoxin
- Doxorubicin
- Doxycycline
- Methoxyflurane
- Metronidazole
- Quinine
- Theophylline
- Warfarin
- Benzodiazepines, such as diazepam, clonazepam or nitrazepam
- Antiepileptics, such as phenobarbital or carbamazepine
- Antihistamines, such as doxylamine and clemastine
- Narcotic analgesics, such as morphine and oxycodone
- Steroids, such as prednisone and cortisone
- Antidepressants[citation needed]
- Antihypertensives, such as atenolol and propranolol
- Antiarrhythmics, such as verapamil and digoxin
Amobarbital has been known to decrease the effects of hormonal birth control, sometimes to the point of uselessness. Being chemically related to phenobarbital, it might also do the same thing to digitoxin, a cardiac glycoside.
In 1988, Miller et al. reported that amobarbital increases benzodiazepine receptor binding in vivo with less potency than secobarbital and pentobarbital (in descending order), but greater than phenobarbital and barbital (in ascending order).[9]
Overdose
Some side effects of overdose include confusion (severe); decrease in or loss of reflexes; drowsiness (severe); fever; irritability (continuing); low body temperature; poor judgment; shortness of breath or slow or troubled breathing; slow heartbeat; slurred speech; staggering; trouble in sleeping; unusual movements of the eyes; weakness (severe). Death can be a result, as in the case of the Hollywood actor, Robert Walker.
See also
References and End Notes
- ^ Kim HS, Wan X, Mathers DA, Puil E. "Selective GABA-receptor actions of amobarbital on thalamic neurons." British Journal of Pharmacology. 2004 Oct;143(4):485-94. Epub 2004 Sep 20. PMID 15381635
- ^ Maynert EW. "The alcoholic metabolites of pentobarbital and amobarbital in man." Journal of Pharmacology and Experimental Therapeutics. 1965 Oct;150(1):118-21. PMID 5855308
- ^ Tang BK, Kalow W, Grey AA. "Amobarbital metabolism in man: N-glucoside formation." Research Communications in Chemical Pathology and Pharmacology. 1978 Jul;21(1):45-53. PMID 684279
- ^ Soine PJ, Soine WH. "High-performance liquid chromatographic determination of the diastereomers of 1-(beta-D-glucopyranosyl)amobarbital in urine." Journal of Chromatography. 1987 Nov 27;422:309-14. PMID 3437019
- ^ Bleckwenn WJ Sodium amytal in certain nervous and mental conditions. Wis Med J 1930; 29: 693-696.
- ^ Truth Serum: A Possible Weapon, 60 Minutes, April 23, 2003.
- ^ McCall WV. "The addition of intravenous caffeine during an amobarbital interview." Journal of Psychiatry & Neuroscience. 1992 Nov;17(5):195-7. PMID 1489761
- ^ Use of sodium amytal during WWII
- ^ Miller LG, Deutsch SI, Greenblatt DJ, Paul SM, Shader RI (1988). "Acute barbiturate administration increases benzodiazepine receptor binding in vivo". Psychopharmacology (Berl) 96 (3): 385–90. doi:. PMID 2906155
- Controlled Substances in Schedule II Office of Diversion Control, Drug Enforcement Administration.
- Controlled Substances in Schedule III Office of Diversion Control, Drug Enforcement Administration.
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