A crystalline barbiturate, C12H12N2O3, used medicinally as a sedative, a hypnotic, and an anticonvulsant.
Dictionary:
phe·no·bar·bi·tal (fē'nō-bär'bĭ-tôl', -tăl') ![]() |
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:

Phenobarbital Oral tablet
What is this medicine?
PHENOBARBITAL (fee noe BAR bi tal) is a barbiturate. It may be used to help you sleep or may be used to help control seizures.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•drug abuse or addiction
•if you frequently drink alcohol containing drinks
•kidney disease
•liver disease
•lung disease or breathing problems
•porphyria
•suicidal thoughts, plans, or attempt; a previous suicide attempt by you or a family member
•an unusual or allergic reaction to phenobarbital, other barbiturates, other medicines, lactose, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a full glass of water. Follow the directions on the prescription label. Take your medicine at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your doctor's advice. If you have been taking this medicine regularly and suddenly stop taking it, you may increase the risk of seizures. Your doctor may gradually reduce the dose.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Patients over 65 years old may have a stronger reaction and need a smaller dose.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What if I miss a dose?
Try not to miss a dose, you will have an injection once a week. Keep your scheduled appointments and notify your prescriber or health care professional if you are unable to keep an appointment.What may interact with this medicine?
Do not take this medicine with any of the following medications:
•other barbiturates
•primidone
•voriconazole
This medicine may also interact with the following medications:
•alcohol or medicines that contain alcohol
•antihistamines
•medicines for depression, anxiety, or psychotic disturbances
•medicines for pain including pentazocine, buprenorphine, butorphanol, nalbuphine, tramadol, and propoxyphene
•medicines for sleep
•muscle relaxants
•steroid medicines like prednisone or cortisone
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress.
If you are taking this medicine for seizures, wear a medical identification bracelet or chain to say you have seizures, and carry a card that lists all your medications.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.
Birth control pills may not work properly while you are taking this medicine. Talk to your doctor about using an extra method of birth control.
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.
Women who become pregnant while using this medicine may enroll in the North American Antiepileptic Drug Pregnancy Registry by calling 1-888-233-2334. This registry collects information about the safety of antiepileptic drug use during pregnancy.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•fever, chills, or sore throat
•redness, blistering, peeling or loosening of the skin, including inside the mouth
•unusual bleeding or bruising
•unusually weak or tired
•worsening of mood, thoughts or actions of suicide or dying
•yellowing of the eyes or skin
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•dizziness
•drowsiness
•headache
•irritability or nervousness
•nausea
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children. This medicine can be abused. Keep your medicine in a safe place to protect it from theft. Do not share this medicine with anyone. Selling or giving away this medicine is dangerous and against the law.
Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Keep container tightly closed. Protect from light. 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-phenylpyrimidine-2,4,6(1H,3H,5H)-trione | |
| Identifiers | |
| CAS number | 50-06-6 |
| ATC code | N05CA24 N03 |
| PubChem | 4763 |
| DrugBank | APRD00184 |
| ChemSpider | 4599 |
| 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) |
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Phenobarbital (INN) or phenobarbitone (former BAN) is a barbiturate, first marketed as Luminal by Friedr. Bayer et comp. It is the most widely used anticonvulsant worldwide [1] and the oldest still commonly used.[2] 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 (those formerly known as Grand Mal) 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.[3] In more affluent countries, it is no longer recommended as a first or second-line choice anticonvulsant for most seizure types,[2][4] though it is still commonly used to treat neonatal seizures.
How supplied: Phenobarbital (and phenobarbital sodium) is manufactured and supplied in various forms: In Tablets of 15, 30, 60 and 100 mg (though not all are available in all countries: for example, in Australia only the 30 mg strength tablets are available); in an oral elixir (commonly 3 mg/mL in strength); and in a form for injection (as phenobarbital sodium - usually 200 mg/mL). The injectable form is used principally to control status epilepticus, while the oral forms are used for prophylactic and maintenance therapy. The dose range for epilepsy is 60–320 mg/day; its very long active half-life means that for some patients, doses do not have to be taken every day, particularly once the dose has been stabilised over a period of several weeks or months and seizures are effectively controlled. It is occasionally still used as a sedative/hypnotic in anxious or agitated patients who may be intolerant of or do not have access to benzodiazepines, neuroleptics and other, newer drugs. For this purpose phenobarbital has a lower dose range - around 30–120 mg/day; however this practice is uncommon in developed countries.
Contents |
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.[6]
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[7] 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 worst 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 led 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.[8]
Between 1934-1945 Phenobarbital, under the brand name Luminal, was used by German doctors under the Nazi party endorsed policy of eugenics to remove children born with disease or deformities from the population so that they would not suffer. Many of the medical staff involved were later to transfer to Nazi hospitals.[9] [10]
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.[11]
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 led to the introduction of Good Manufacturing Practice for drugs.[11]
The drug predates the 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.[12]
Phenobarbital was used for over 25 years as prophylaxis in the treatment of febrile seizures.[13] 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.[14][15]
Phenobarbital is indicated in the treatment of all types of seizures except absence seizures.[4][16] Phenobarbital is no less effective at seizure control than more modern drugs such as phenytoin and carbamazepine. It is, however, significantly less well tolerated.[17][18]
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.[19] Failing that, the only treatment is anaesthesia in intensive care.[16][20]
Phenobarbital is the first line choice for the treatment of neonatal seizures.[5][21][22] 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.[23]
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.
Caution in children. Of anticonvulsant drugs behavioural disturbances occur most frequently with clonazepam and phenobarbital.[24]
Acute intermittent porphyria, oversensitivity for barbiturates, prior dependence on barbiturates, severe respiratory insufficiency and hyperkinesia in children.
See barbiturates.
| Poisoning by barbiturates | |
|---|---|
| Classification and external resources | |
| 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.[25]
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%.[25] There is no specific antidote for barbiturate poisoning.
British veterinarian Donald Sinclair, better known as "Siegfried Farnon" in the "All Creatures Great and Small" books of James Herriot committed suicide at the age of 84 by injecting himself with an overdose of phenobarbital. Activist Abbie Hoffman also committed suicide by consuming phenobarbital, combined with alcohol, on April 12, 1989; the residue of around 150 pills was found in his body at autopsy.[26]
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 many isozymes of the cytochrome P450 system. Cytochrome P450 2B6 (CYP2B6) is specifically induced by Phenobarbital via the CAR/RXR nuclear receptor heterodimer. It is excreted primarily by the kidneys.
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.[27]
It may also be used to treat seizures in horses when benzodiazepine treatment has failed or is contraindicated.[28]
The High Incident Bandits used phenobarbital prior to committing the North Hollywood Bank of America robbery.[29]
The Heaven's Gate cult used phenobarbital mixed with vodka to commit a mass suicide in 1997.
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| Translations: 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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| Atropine; Hyoscyamine; Phenobarbital; Scopolamine | |
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| phenobarbitone |
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Copyrights:
![]() | Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved. Read more | |
![]() | Neurological Disorder. Gale Encyclopedia of Neurological Disorders. Copyright © 2005 by The Gale Group, Inc. All rights reserved. Read more | |
![]() | Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved. Read more | |
![]() | Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Phenobarbital". Read more | |
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