A crystalline barbiturate, C12H12N2O3, used medicinally as a sedative, a hypnotic, and an anticonvulsant.
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Neurological Disorder:
Phenobarbital
Definition
Phenobarbital is a barbiturate, a drug that has sedative and hypnotic effects. The drug is classed as a central nervous system agent and subclassed as an anticonvulsant (antiseizure).
Purpose
Phenobarbital is used to control the seizures that occur in epilepsy, and can relieve anxiety. For short-term use, phenobarbital can help those with insomnia fall asleep.
Description
Phenobarbital is available in tablet or capsule form, and as a liquid. All three forms are taken orally one to three times each day with or without food. When taken once a day, the drug is typically taken near bedtime.
Recommended dosage
The dosage is prescribed by a physician. Typically, the total daily dose ranges 30–120 mg. For treatment of seizures, the dosage can be 60–200 mg daily. The daily dosage for children is typically 3–6 mg per 2.2 lb (1 kg) of body weight.
Dosages should not be exceeded. It is also important to adhere to the proper timetable for use of the medication. Use of the drug should not be discontinued without consulting a physician.
Precautions
Phenobarbital is potentially habit forming if taken over an extended period of time. When being prescribed to overcome insomnia, the drug should not be used for a period longer than two weeks. Furthermore, phenobarbital should not be taken in a dose that exceeds the prescribed amount. Ingestion of more than the recommended dosage can result in unsteadiness, slurred speech, and confusion. More serious results of overdose include unconsciousness and breathing difficulty.
Long-term use can lead to tolerance, making it necessary to take increased amounts of the drug to achieve the desired effect. This poses a risk of habitual use; however, it should be noted that people with seizure disorders seldom have problems with phenobarbital dependence. Nevertheless, with chemical dependency, symptoms of withdrawal from phenobarbital begin eight to 12 hours after the last dose, and progress in severity. Initial symptoms may include anxiousness, insomnia, and irritability. Twitching and tremors in the hands and fingers precludes increasing weakness, dizziness, nausea, and vomiting. Symptoms can sometimes become severe or life-threatening, with seizures, delirium, or coma.
While there is evidence of risk to a fetus, the benefits of phenobarbital for a pregnant woman can sometimes warrant its use. This must be determined by a physician.
Side effects
Common side effects include drowsiness, headache, dizziness, depression, stomachache, and vomiting. More severe side effects include nightmares, constipation, and pain in muscles and joints. Side effects that require immediate medical attention occur rarely, and include seizures, profuse nosebleeds, fever, breathing or swallowing difficulties, and a severe skin rash.
Interactions
Phenobarbital can interact with a number of prescription and nonprescription medications including acetaminophen, anticoagulants such as warfarin, chloramphenicol, monoamine oxidase inhibitors (MAOIs), antidepressants, asthma medicine, cold medicine, anti-allergy medicine, sedatives, steroids, tranquilizers, and vitamins. Interactions with these medications can increase the drowsiness caused by phenobarbital. Decreased efficiency of anticoagulants can increase the risk of bleeding. Phenobarbital can also react with oral contraceptives, which can decrease the effectiveness of the birth control medication.
Resources
PERIODICALS
Beghi, E. "Overview of Studies to Prevent Posttraumatic Epilepsy." Epilepsia (2003; Suppl): 21–26.
Galindo, PA., et al. "Anticonvulsant Drug Hypersensitivity." Journal of Investigative Allergological and Clinical Immunology (December 2002): 299–304.
Kokwaro, GO., et al. "Pharmacokinetics and Clinical Effect of Phenobarbital in Children with Severe Falciparum Malaria and Convulsions." British Journal of Clinical Pharmacology (October 2003): 453–457.
Pennell, P. B. "Antiepileptic Drug Pharmacokinetics during Pregnancy and Lactation." Neurology (September 2003): S35–42.
OTHER
U.S. National Library of Medicine. Drug Information: Phenobarbital. MEDLINEplus Health Information. December 28, 2003 (May 23, 2004). http://www.nlm.nih.gov/medlineplus/print/druginfo/medmaster/a682007.html.
ORGANIZATIONS
The Epilepsy Foundation. 4351 Garden City Drive, Landover, MD 20785-7223. (800) 332-1000. http://www.epilepsyfoundation.org/.
Brian Douglas Hoyle, PhD
Drug Info:
Phenobarbital
Brand names: Luminal®
Chemical formula:
- Drug Forms:
- Phenobarbital tablets or capsules (below)
- Phenobarbital oral elixir
- Phenobarbital injection
Phenobarbital tablets or capsules
What are phenobarbital tablets or capsules?
PHENOBARBITAL (Solfoton®) is a barbiturate that acts by slowing down the activity of the brain and nervous system. Phenobarbital has sedative and hypnotic properties, which will help make you relaxed and sleepy before surgery or help you to sleep. It also reduces or controls seizures or convulsions, except for absence (petit mal) seizures. Federal law prohibits the transfer of phenobarbital to any person other than the patient for whom it was prescribed. Do not share this medicine with any one else. Generic phenobarbital tablets are available, but not capsules.
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
• heart disease
• kidney disease or undergoing dialysis
• liver disease
• low blood pressure
• lung disease, chest infection or breathing difficulties
• mental depression or mental problems
• osteoporosis or other bone diseases
• porphyria
• seizures or convulsions
• shock
• suicidal thoughts, plans, or attempt; a previous suicide attempt by you or a family member
• an unusual or allergic reaction to phenobarbital, other barbiturates or seizure medications, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should I take this medicine?
Take phenobarbital tablets or capsules by mouth. Follow the directions on the prescription label. Swallow the tablets or capsules with a drink of water. If phenobarbital upsets your stomach, take it with food or milk. Take your doses at regular intervals. Do not take your medicine more often than directed.
Elderly patients over age 65 years may have a stronger reaction to this medicine and need smaller doses.
Contact your pediatrician or health care professional regarding the use of this medication in children. Special care may be needed.
What if I miss a dose?
If you are on a regular schedule and miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Try not to miss doses if you are taking phenobarbital for epilepsy. Do not take double or extra doses.What drug(s) may interact with phenobarbital?
Phenobarbital can interact with many different types of medications. You should check with your prescriber or pharmacist before taking other medications with phenobarbital. The following list includes some of the types of medications that may interact:
• acetaminophen
• alcohol
• alosetron
• antifungal drugs like fluconazole, griseofulvin, itraconazole or ketoconazole
• caffeine
• cancer-treating medications
• chloramphenicol
• cyclophosphamide
• cyclosporine
• digoxin
• disopyramide
• doxycycline
• female hormones, including contraceptive or birth control pills
• hormones such a prednisone or cortisone
• levothyroxine
• medicines for sleeping problems
• medicines for mental depression, anxiety or other mood problems
• medicines for treating HIV infection or AIDS
• metronidazole
• mexiletine
• prescription pain medications
• quinidine
• quinine
• riluzole
• sevelamer
• sirolimus
• tacrolimus
• tamoxifen
• other seizure (convulsion) or epilepsy medicine
• 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 phenobarbital?
Visit your prescriber or health care professional for regular checks on your progress. If you are taking this medicine for epilepsy, take it at the same time each day. It may be 2 to 3 weeks before the full effects in controlling seizures are apparent. If you have been taking this medicine regularly and suddenly stop taking it, you may increase the risk of seizures. Your prescriber or health care professional may want to gradually reduce the dose. Do not stop taking except on your prescriber's advice.
If you are taking this medicine for epilepsy, wear a Medic Alert bracelet or necklace. Carry an identification card with information about your condition, medications, and prescriber or health care professional.
In general this medicine should not be taken for longer than 1 or 2 weeks as a sleep aid. If sleep medicine is taken every night for a long time it may no longer help you to sleep. Consult your prescriber or health care professional if you still have difficulty in sleeping.
After taking this medicine you may feel drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine 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.
The use of this medicine may increase the chance of suicidal thoughts or actions. Pay special attention to how you are responding while on this medicine. Any worsening of mood, or thoughts of suicide or dying should be reported to your health care professional right away.
This medicine can reduce the effectiveness of birth control pills (oral contraceptives) or other hormonal birth control drugs. Talk to your prescriber about alternatives or use of additional birth control methods while taking this drug.
If you are going to have surgery, tell your prescriber or health care professional that you are taking this medicine.
What side effects may I notice from taking phenobarbital?
Side effects that you should report to your prescriber or health care professional as soon as possible:
• bone tenderness
• changes in behavior, mood, or mental ability
• changes in the frequency or severity of seizures
• confusion, agitation
• difficulty breathing or shortness of breath
• eye problems, very small or enlarged centers to the eyes
• fever, sore throat
• hallucinations
• lightheadedness or fainting spells
• redness, blistering, peeling or loosening of the skin, including inside the mouth
• 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
• worsening of mood, thoughts or actions of suicide or dying
• 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):
• constipation
• clumsiness, unsteadiness, or a 'hang-over' effect
• difficulty sleeping or nightmares
• drowsiness, dizziness
• headache
• irritability, nervousness
• nausea or vomiting
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed. 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:
phenobarbital
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Phenobarbital
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| Systematic (IUPAC) name | |
| 5-ethyl-5-phenyl-1,3-diazinane-2,4,6-trione | |
| Identifiers | |
| CAS number | |
| ATC code | N05 N03AA02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C12H12N2O3 |
| Mol. mass | 232.235 g/mol |
| Pharmacokinetic data | |
| Bioavailability | >95% |
| Protein binding | 20 to 45% |
| Metabolism | Hepatic (mostly CYP2C19) |
| Half life | 53 to 118 hours |
| Excretion | Renal and fecal |
| Therapeutic considerations | |
| Pregnancy cat. |
D(US) |
| Legal status | |
| Routes | Oral, rectal, parenteral (intramuscular and intravenous) |
Phenobarbital (INN) or phenobarbitone (former BAN) is a barbiturate, first marketed as Luminal by Farbwerke Fr. Bayer and Co. It is the most widely used anticonvulsant worldwide and the oldest still in use. It also has sedative and hypnotic properties but, as with other barbiturates, has been superseded by the benzodiazepines for these indications. The World Health Organization recommends its use as first-line for partial and generalized tonic–clonic seizures in developing countries. It is a core medicine in the WHO Model List of Essential Medicines, which is a list of minimum medical needs for a basic health care system.[1] In more affluent countries, it is no longer recommended as a first or second-line choice anticonvulsant for most seizure types,[2][3] though it is still commonly used to treat neonatal seizures.[4]
History
The first barbiturate drug, barbital, was synthesized in 1902 by German chemists Emil Fischer and Joseph von Mering at Bayer. By 1904 several related drugs, including phenobarbital, had been synthesized by Fischer. Phenobarbital was brought to market in 1912 by the drug company Bayer using the brand Luminal. It remained a commonly prescribed sedative and hypnotic until the introduction of benzodiazepines in the 1950s.[5]
Phenobarbital's soporific, sedative and hypnotic properties were well known in 1912, but nobody knew it was also an effective anticonvulsant. The young doctor Alfred Hauptmann gave it to his epilepsy patients as a tranquiliser and discovered that their epileptic attacks were susceptible to the drug. Hauptmann performed a careful study of his patients over an extended period. Most of these patients were using the only effective drug then available, bromide, which had terrible side effects and limited efficacy. On phenobarbital, their epilepsy was much improved: the worse patients suffered fewer and lighter seizures and some patients became seizure free. In addition, they improved physically and mentally as bromides were removed from their regime. Patients who had been institutionalised due to the severity of their epilepsy were able to leave and, in some cases, resume employment. Hauptman dismissed concerns that its effectiveness in stalling epileptic attacks could lead to patients suffering a build-up that needed to be "discharged". As he expected, withdrawal of the drug lead to an increase in seizure frequency – it was not a cure. The drug was quickly adopted as the first widely effective anticonvulsant, though World War I delayed its introduction in the U.S.[6]
Phenobarbital was used to treat neonatal jaundice by increasing liver metabolism and thus lowering bilirubin levels. In the 1950s, phototherapy was discovered, and became the standard treatment.[7]
In 1940, Winthrop Chemical produced sulfathiazole tablets that were contaminated with phenobarbital. This occurred because both tablets were produced side-by-side and equipment could be interchanged. Each antibacterial tablet contained more than twice the required dose of phenobarbital necessary to induce sleep. Hundreds of patients died or were injured as a result. A U.S. Food and Drug Administration investigation was highly critical of Winthrop and the scandal lead to the introduction of Good Manufacturing Practice for drugs.[7]
The drug itself through predated FDA approval processes and has failed to be formally cleared for use in subsequent years. Guidance was issued in June 2006 of plans to enforce US approval for unapproved drugs.[8]
Phenobarbital was used for over 25 years as prophylaxis in the treatment of febrile seizures.[9] Although an effective treatment in preventing recurrent febrile seizures, it had no positive effect on patient outcome or risk of developing epilepsy. The treatment of simple febrile seizures with anticonvulsant prophylaxis is no longer recommended.[10][11]
Indications
Phenobarbital is indicated in the treatment of all types of seizures except absence seizures.[2][12] Phenobarbital is no less effective at seizure control than more modern drugs such as phenytoin and carbamazepine. It is, however, significantly less well tolerated.[13][14]
The first line drugs for treatment of status epilepticus are fast acting benzodiazepines such as diazepam or lorazepam. If these fail then phenytoin may be used, with phenobarbital being an alternative in the U.S. but used only third line in the UK.[15] Failing that, the only treatment is anaesthesia in intensive care.[12][16]
Phenobarbital is the first line choice for the treatment of neonatal seizures.[4][17][18] Concerns that neonatal seizures in themselves could be harmful make most physicians treat them aggressively. There is, however, no reliable evidence to support this approach.[19]
Side effects
Sedation and hypnosis are the principal side effects of phenobarbital. Central nervous system effects like dizziness, nystagmus and ataxia are also common. In elderly patients, it may cause excitement and confusion while in children, it may result in paradoxical hyperactivity.
Contraindications
Acute intermittent porphyria, oversensitivity for barbiturates, prior dependence on barbiturates, severe respiratory insufficiency and hyperkinesia in children.
Overdose
| ICD-10 | T42.3 |
|---|---|
| eMedicine | med/207 |
Phenobarbital causes a "depression" of the body's systems, mainly the central and peripheral nervous systems; thus, the main characteristic of phenobarbital overdose is a "slowing" of bodily functions, including decreased consciousness (even coma), bradycardia, bradypnea, hypothermia, and hypotension (in massive overdoses). Overdose may also lead to pulmonary edema and acute renal failure as a result of shock.
The electroencephalogram of a person with phenobarbital overdose may show a marked decrease in electrical activity, to the point of mimicking brain death. This is due to profound depression of the central nervous system, and is usually reversible.[20]
Treatment of phenobarbital overdose is supportive, and consists mainly in the maintenance of airway patency (through endotracheal intubation and mechanical ventilation), correction of bradycardia and hypotension (with intravenous fluids and vasopressors, if necessary) and removal of as much drug as possible from the body. Depending on how much time has elapsed since ingestion of the drug, this may be accomplished through gastric lavage (stomach pumping) or use of activated charcoal. Hemodialysis is effective in removing phenobarbital from the body, and may reduce its half-life by up to 90%.[20] There is no specific antidote for barbiturate poisoning.
Pharmacokinetics
Phenobarbital has an oral bioavailability of approximately 90%. Peak plasma concentrations are reached 8 to 12 hours after oral administration. It is one of the longest-acting barbiturates available – it remains in the body for a very long time (half-life of 2 to 7 days) and has very low protein binding (20 to 45%). Phenobarbital is metabolized by the liver, mainly through hydroxylation and glucuronidation, and induces most isozymes of the cytochrome P450 system. Cytochrome P450 2B6 System is more specifically induced by Phenobarbital. It is excreted primarily by the kidneys.
Veterinary uses
Phenobarbital is one of the initial drugs of choice to treat epilepsy in dogs, and is the initial drug of choice to treat epilepsy in cats.[21]
It may also be used to treat seizures in horses when benzodiazepine treatment has failed or is contraindicated.[22]
Illicit Use
The High Incident Bandits used phenobarbitol prior to committing the North Hollywood shootout.
Phenobarbital was mixed with vodka and consumed by the Heaven's Gate Cult members to commit suicide on March 26, 1997.
References
- Ole Daniel Enersen. Alfred Hauptmann.
- Kwan P, Brodie M (2004). "Phenobarbital for the treatment of epilepsy in the 21st century: a critical review.". Epilepsia 45 (9): 1141-9. PMID 15329080.
Footnotes
- ^ WHO Model List of Essential Medicines (PDF). World Health Organization (March 2005). Retrieved on 2006-03-12.
- ^ a b NICE (2005-10-27). CG20 Epilepsy in adults and children: NICE guideline. NHS. Retrieved on 2006-09-06.
- ^ Phenobarbital. Epilepsy Foundation. Retrieved on 2006-09-07.
- ^ a b British Medical Association, Royal Pharmaceutical Society of Great Britain, Royal College of Paediatrics and Child Health and Neonatal and Paediatric Pharmacists Group (2006). "4.8.1 Control of epilepsy", British National Formulary for Children, 255-6. ISBN 0-85369-676-4.
- ^ Sneader, Walter (2005-06-23). Drug Discovery. John Wiley and Sons, 369. ISBN 0-471-89979-8.
- ^ Scott,, Donald F (1993-02-15). The History of Epileptic Therapy. Taylor & Francis, 59-65. ISBN 1-85070-391-4.
- ^ a b Rachel Sheremeta Pepling (06 2005). "Phenobarbital". Chemical and Engineering News 83 (25). Retrieved on 2006-09-06.
- ^ Michelle Meadows (January-February 2007). The FDA Takes Action Against Unapproved Drugs. FDA Consumer magazine. Retrieved on 2007-09-27.
- ^ John M. Pellock, W. Edwin Dodson, Blaise F. D. Bourgeois (2001-01-01). Pediatric Epilepsy. Demos Medical Publishing, 169. ISBN 1-888799-30-7.
- ^ Robert Baumann (2005-02-14). Febrile Seizures. eMedicine. WebMD. Retrieved on 2006-09-06.
- ^ various (March 2005). Diagnosis and management of epilepsies in children and young people 15. Scottish Intercollegiate Guidelines Network. Retrieved on 2006-09-07.
- ^ a b British National Formulary 51
- ^ Taylor S, Tudur Smith C, Williamson PR, Marson AG (2003). "Phenobarbitone versus phenytoin monotherapy for partial onset seizures and generalized onset tonic-clonic seizures.". Cochrane Database Systematic Reviews (2). DOI:10.1002/14651858.CD002217. PMID 11687150. Retrieved on 2006-09-06.
- ^ Tudur Smith C, Marson AG, Williamson PR (2003). "Carbamazepine versus phenobarbitone monotherapy for epilepsy". Cochrane Database of Systematic Reviews (1). DOI:10.1002/14651858.CD001904. PMID 12535420. Retrieved on 2006-09-06.
- ^ British Medical Association, Royal Pharmaceutical Society of Great Britain, Royal College of Paediatrics and Child Health and Neonatal and Paediatric Pharmacists Group (2006). "4.8.2 Drugs used in status epilepticus", British National Formulary for Children, 269. ISBN 0-85369-676-4.
- ^ Kälviäinen R, Eriksson K, Parviainen I (2005). "Refractory generalised convulsive status epilepticus : a guide to treatment.". CNS Drugs 19 (9): 759-68. PMID 16142991.
- ^ John M. Pellock, W. Edwin Dodson, Blaise F. D. Bourgeois (2001-01-01). Pediatric Epilepsy. Demos Medical Publishing, 152. ISBN 1-888799-30-7.
- ^ Raj D Sheth (2005-03-30). Neonatal Seizures. eMedicine. WebMD. Retrieved on 2006-09-06.
- ^ Booth D, Evans DJ (2004). "Anticonvulsants for neonates with seizures". Cochrane Database of Systematic Reviews (3). DOI:10.1002/14651858.CD004218.pub2. PMID 15495087. Retrieved on 2006-09-06.
- ^ a b Rania Habal (2006-01-27). Barbiturate Toxicity. eMedicine. WebMD. Retrieved on 2006-09-14.
- ^ Thomas, WB (2003). Seizures and narcolepsy. In: Dewey, Curtis W. (ed.) A Practical Guide to Canine and Feline Neurology. Ames, Iowa: Iowa State Press. ISBN 0-8138-1249-6.
- ^ (February 8, 2005) in Kahn, Cynthia M., Line, Scott, Aiello, Susan E. (ed.): The Merck Veterinary Manual, 9th ed., John Wiley & Sons. ISBN 0-911910-50-6.
| Barbiturates (N01AF, N03AA, N05CA) |
|---|
|
Allobarbital • Amobarbital • Aprobarbital • Alphenal • Barbexaclone • Barbital • Brallobarbital • Butabarbital • Butalbital • Butobarbital • Butallylonal • Crotylbarbital • Cyclobarbital • Cyclopal • Ethallobarbital • Febarbamate • Hexethal • Heptabarbital • Hexobarbital • Mephobarbital • Metharbital • Methohexital • Methylphenobarbital • Narcobarbital • Pentobarbital • Phenobarbital • Probarbital • Propallylonal • Proxibarbal • Proxibarbital • Reposal • Secbutabarbital • Secobarbital • Talbutal • Thialbarbital • Thiamylal • Thiobarbital • Thiobutabarbital • Thiopental • Valofane • Vinbarbital • Vinylbital |
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Translations:
Translations for:
Phenobarbital
Nederlands (Dutch)
sedatief (m.n. gebruikt tegen epilepsie)
Français (French)
n. - gardénal, phénobarbital
Deutsch (German)
n. - (Med.) Phenobarbital
Ελληνική (Greek)
n. - φαινοβαρβιτάλη, λουμινάλη, φαινυλαιθυλοβαρβιτουρικό οξύ
Italiano (Italian)
fenobarbital
Português (Portuguese)
n. - fenobarbital (m) (remédio) (Med.)
Русский (Russian)
фенобарбитал
Español (Spanish)
n. - fenobarbital
Svenska (Swedish)
n. - fenemal (farm.)
中文（简体） (Chinese (Simplified))
镇静安眠剂
中文（繁體） (Chinese (Traditional))
n. - 鎮靜安眠劑
العربيه (Arabic)
(الاسم) بنبارتين : أسم كيماوي مطلق على نوع من العقاقير
עברית (Hebrew)
n. - פנוברביטל (סם שינה)
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Copyrights:
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 | Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2007. Published by Houghton Mifflin Company. All rights reserved. Read more |
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| Neurological Disorder. Gale Encyclopedia of Neurological Disorders. Copyright © 2005 by The Gale Group, Inc. All rights reserved. Read more |
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| Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved. Read more |
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