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amobarbital (Amytal Sodium)

 

Classes: Barbiturates; Sedative/Hypnotics

Dosing and uses of Amytal Sodium (amobarbital)

 

Adult dosage forms and strengths

powder for injection: Schedule II

  • 500mg

 

Sedative

30-50 mg IV q8-12hr

 

Hypnotic

Used as a hypnotic, for short-term treatment of insomnia; effectiveness for sleep induction and sleep maintenance is lost after 2 weeks

65-200 mg IV qHs

 

Pediatric dosage forms and strengths

powder for injection: Schedule II

  • 500mg

 

Sedative

<6 years: Safety and effectiveness not established

6-12 years: 65 mg-500 mg IV/Im

>12 years: 30-50 mg IV q8-12hr

 

Hypnotic

Used as a hypnotic, for short-term treatment of insomnia; effectiveness for sleep induction and sleep maintenance is lost after 2 weeks

<6 years: Safety and effectiveness not established

6-12 years: 2-3 mg/kg; not to exceed 500 mg IV/Im

>12 years: 65-200 mg IV qHs

 

Geriatric dosage forms and strengths

Reduce dose in the elderly or debilitated because these patients may be more sensitive to barbiturates

Elderly and debilitated patients may react with marked excitement, depression, or confusion

 

Amytal Sodium (amobarbital) adverse (side) effects

1-10%

Somnolence

 

<1%

Nervous system: agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness, psychiatric disturbance, hallucinations, insomnia, anxiety, dizziness, abnormality in thinking

Cardiovascular system: Bradycardia, hypotension, syncope

Respiratory system: apnea, hypoventilation, postoperative atelectasis

Digestive system: Constipation, vomiting, nausea

Other adverse effects: Headache, injection site reactions, hypersensitivity reactions, fever, liver damage, megaloblastic anemia following chronic phenobarbital use

 

Warnings

Contradindications

Hypersensitivity

Patients with history of manifest or latent porphyria

Significant impairment of liver function

Respiratory disease in which dyspnea or obstruction is evident

 

Cautions

Habit forming; tolerance and psychological dependence may occur with continued use

Caution in patients that are mentally depressed, have suicide ideation or history of drug abuse and hepatic damage

Rapid administration may cause respiratory depression, apnea, laryngospasm, or vasodilatation with decrease in blood pressure

Parenteral solutions of barbiturates are highly alkaline; care should be taken to avoid perivascular extravasation or intra-arterial injection

Amobarbital may diminish systemic effects of exogenous and endogenous corticosteroids. Administer with caution to patients with borderline hypoadrenal function, regardless of whether it is of pituitary or of primary adrenal origin

Possible impairment of mental and/or physical abilities required for the performance of potentially hazardous tasks, such as driving a car or operating machinery

Concurrent use of barbiturates with other CNS depressants (eg, alcohol, narcotics, tranquilizers, antihistamines) may result in increased CNS-depressant effects

Extravascular injection may cause local tissue damage with subsequent necrosis; consequences of intra-arterial injection may vary from transient pain to gangrene of the limb; any complaint of pain in the limb warrants stopping the injection

 

Pregnancy and lactation

Pregnancy category: d

Lactation: small amounts of barbiturates are excreted in the milk; use caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Amytal Sodium (amobarbital)

Mechanism of action

Depress the sensory cortex by interfering with transmission of impulses from thalamus. This results in decreased motor activity, altered cerebellar function, drowsiness, sedation, and hypnosis

 

Onset of Action

Within 5 minutes

 

Metabolism

Primarily hepatic via microsomal enzymes

 

Elimination

Half-Life: 15-40 hours in adults (mean 25 hours)

Excretion: feces, urine

 

Administration

IV Administration

Slow IV injection is essential; observe patients carefully during administration

Blood pressure, respiration, and cardiac function must be maintained, vital signs be recorded and equipment for resuscitation and artificial ventilation be available

The rate of IV injection for adults should not exceed 50 mg/min to prevent sleep or sudden respiratory depression

Final dosage is determined largely by the patient’s reaction to the slow administration of the drug

 

IM Administration

IM injection of the sodium salts of barbiturates should be made deeply into a large muscle

Average IM dose ranges from 65 mg-500 mg; volume of 5 mL (irrespective of concentration) should not be exceeded at any one site because of possible tissue irritation

Twenty percent solutions may be used so that a small volume can contain a large dose; monitor vital signs after IM injection of hypnotic dose

Superficial IM or subcutaneous injections may be painful and may produce sterile abscesses or sloughs