Amobarbital

What is Amobarbital?

• Amobarbital (Amytal), is a nonselective central nervous system (CNS) depressant that are primarily used as sedative hypnotics.
• In subhypnotic doses, they are also used as anticonvulsants.

Amobarbital

Amobarbital2

Amobarbital ball-and-stick

What are the uses of this medicine?

Amobarbital (Amytal), is used as a:

• Sedative
• Hypnotic, for the short-term treatment of insomnia, since it appears to lose its effectiveness for sleep induction and sleep maintenance after 2 weeks (see CLINICAL PHARMACOLOGY).
• Preanesthetic

How does this medicine work?

• Amobarbital, also known as amobarbital sodium, is a barbiturate medication that acts as a central nervous system depressant.
• It is primarily used as a sedative-hypnotic agent to induce sleep or for short-term treatment of insomnia.
• The mechanism of action of amobarbital involves enhancing the inhibitory effects of gamma-aminobutyric acid (GABA), the primary inhibitory neurotransmitter in the brain.
• Amobarbital acts by binding to specific sites on GABA-A receptors, which are ligand-gated chloride channels located in the cell membranes of neurons.

When amobarbital binds to these receptors, it enhances the effects of GABA, leading to increased chloride ion influx into the neuron. The increased chloride conductance hyperpolarizes the neuron, making it less excitable and reducing neuronal activity.

• By increasing the inhibitory effects of GABA, amobarbital produces various pharmacological effects, including sedation, hypnosis, anxiolysis (anxiety reduction), and anticonvulsant activity.
• These effects make amobarbital useful in the treatment of insomnia and certain seizure disorders.
• It is important to note that amobarbital, like other barbiturates, has a narrow therapeutic index and can cause respiratory depression and central nervous system depression at high doses or with prolonged use.
• The use of amobarbital should be closely monitored, and it should be prescribed at the lowest effective dose for the shortest duration possible to minimize the risk of adverse effects.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• who are hypersensitive to barbiturates
• with a history of manifest or latent porphyria
• with marked impairment of liver function or respiratory disease in which dyspnea or obstruction is evident.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking.

Be sure to mention any of the following:

• Anticoagulants
• Corticosteroids
• Griseofulvin
• Doxycycline
• Phenytoin, Sodium Valproate, Valproic Acid
• CNS Depressants
• Monoamine Oxidase Inhibitors (MAOIs)
• Estradiol, Estrone, Progesterone, and Other Steroidal Hormones
• Theophylline
• Anticonvulsants

Is this medicine FDA approved?

• Amobarbital (am" oh bar' bi tal) and butabarbital (bue' ta bar' bi tal) are currently available, but only as solutions for parenteral administration, being used largely as preanesthetic agents.
• Secobarbital is available as a 100 mg capsule generically and under the brand name Seconal.
• Pentobarbital is no longer available in the United States.

How should this medicine be used?

Recommended dosage:

In Adults:

• As Sedative: 30 to 50 mg given 2 or 3 times daily.
• As Hypnotic: 65 to 200 mg at bedtime.

• The maximum single dose for an adult is 1 g.

• Dosage should be reduced in the elderly or debilitated because these patients may be more sensitive to barbiturates.
• Dosage should be reduced for patients with impaired renal function or hepatic disease.
• Ordinarily, an IV dose of 65 mg to 0.5 g may be given to a child 6 to 12 years of age.

Administration:

• Vials of amobarbital sodium are for parenteral administration.
• Amobarbital injectable solution is usually administered by healthcare professionals in a healthcare setting, such as a hospital or clinic.
• The injection is typically given into a muscle (intramuscularly) or a vein (intravenously), as directed by the healthcare provider.
• The dosage, concentration, and rate of administration will be determined by the healthcare provider based on the specific condition being treated.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As vials contain 500 mg (2 mmol) amobarbital sodium as a sterile lyophilized powder.

This medicine is available in fallowing brand namesː

• Amytal

What side effects can this medication cause?

The most common side effects of this medicine include: Somnolence

Less common, side effects may include:

• Nervous System: Agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness, psychiatric disturbance, hallucinations, insomnia, anxiety, dizziness, abnormality in thinking
• Respiratory System: Hypoventilation, apnea, postoperative atelectasis
• Cardiovascular System: Bradycardia, hypotension, syncope
• Digestive System: Nausea, vomiting, constipation
• Other Reported Reactions: Headache, injection site reactions, hypersensitivity reactions (angioedema, skin rashes, exfoliative dermatitis), fever, liver damage, megaloblastic anemia following chronic phenobarbital use.

What special precautions should I follow?

• Amobarbital sodium may be habit forming. Abrupt cessation after prolonged use in a person who is dependent on the drug may result in withdrawal symptoms, including delirium, convulsions, and possibly death. Barbiturates should be withdrawn gradually from any patient known to be taking excessive doses over long periods of time.
• Too rapid administration may cause respiratory depression, apnea, laryngospasm, or vasodilation with fall in blood pressure.
• Caution should be exercised when barbiturates are administered to patients with acute or chronic pain because paradoxical excitement could be induced or important symptoms could be masked.
• Barbiturates can cause fetal damage when administered to a pregnant woman. If amobarbital sodium is used during pregnancy or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
• The concomitant use of alcohol or other CNS depressants may produce additive CNS depressant effects.
• Parenteral solutions of barbiturates are highly alkaline. Therefore, extreme care should be taken to avoid perivascular extravasation or intra-arterial injection.
• Barbiturates may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks, such as driving a car or operating machinery. The patient should be cautioned accordingly.
• Alcohol should not be consumed while taking barbiturates. The concurrent use of the barbiturates with other CNS depressants (e.g., alcohol, narcotics, tranquilizers, and antihistamines) may result in additional CNS depressant effects.
• Caution should be exercised when amobarbital sodium is administered to a nursing woman because small amounts of barbiturates are excreted in the milk.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Symptoms of oral overdose may occur within 15 minutes beginning with CNS depression, absent or sluggish reflexes, underventilation, hypotension, and hypothermia and may progress to pulmonary edema and death.
• Hemorrhagic blisters may develop, especially at pressure points.
• In extreme overdose, all electrical activity in the brain may cease.
• Complications such as pneumonia, pulmonary edema, cardiac arrhythmias, congestive heart failure, and renal failure may occur.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Protect the patient’s airway and support ventilation and perfusion.
• Monitor and maintain, within acceptable limits, the patient’s vital signs, blood gases, serum electrolytes, etc.
• Absorption of drugs from the gastrointestinal tract may be decreased by giving activated charcoal, which, in many cases, is more effective than emesis or lavage; consider charcoal instead of or in addition to gastric emptying. Repeated doses of charcoal over time may hasten elimination of some drugs that have been absorbed.
• Safeguard the patient’s airway when employing gastric emptying or charcoal.
• Diuresis and peritoneal dialysis are of little value; hemodialysis and hemoperfusion enhance drug clearance and should be considered in serious poisoning.
• If the patient has chronically abused sedatives, withdrawal reactions may be manifest following acute overdose.

Can this medicine be used in pregnancy?

• Barbiturates can cause fetal damage when administered to a pregnant woman.
• If amobarbital sodium is used during pregnancy or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Can this medicine be used in children?

• Safety and effectiveness have not been established in children below the age of 6 years.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• amobarbital sodium

Inactive ingredients:

• none

Who manufactures and distributes this medicine?

Distributed by:

• Bausch Health US, LLC
• Bridgewater, NJ USA

Manufactured by:

• Alcami Carolinas Corporation
• North Charleston, SC USA

• AMYTAL is a trademark of Bausch Health Companies Inc. or its affiliates.

What should I know about storage and disposal of this medication?

• Store at (15° to 30°C) (59° to 86°F).

• Dailymed label info on Amobarbital
• FDA Amobarbital

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