Pentobarbital Sodium (pentobarbital sodium)

Advertisement

Last reviewed · Source: First Databank (FDB) drug data

Overview

Pentobarbital sodium is a short-acting barbiturate that has sedative-hypnotic properties and anticonvulsant activities at anesthetic doses.

Pentobarbital, a barbiturate, is a nonselective CNS depressant that is primarily used as a sedative hypnotic, and at subhypnotic doses, as an anticonvulsant. At high enough therapeutic dosages, barbiturates induce anesthesia and exhibit anticonvulsant activity. At lower dosages not sufficient to induce anesthesia, barbiturates have little analgesic activity, and instead may increase reactions to painful stimuli.

The CNS effects of pentobarbital are related to the blockage of N-methyl-d-aspartic acid (NMDA) receptors and/or potentiation of gamma-aminobutyric acid (GABA) activity. Barbiturates can produce varying levels of CNS mood alteration, including excitation to mild sedation, hypnosis, and deep coma. Barbiturate activity includes depression of the sensory cortex, decreased motor activity, and altered cerebellar function, which produce drowsiness, sedation, and hypnosis.

Barbiturates also cause respiratory depression, which is dose dependent. At large hypnotic dosages, the respiratory depression produced by barbiturates is similar to the slight decrease in blood pressure and heart rate experienced during physiologic sleep.

Although pentobarbital has been used for the short term treatment of insomnia, barbiturate-induced sleep differs from physiological sleep. Barbiturates such as pentobarbital reduce the amount of time spent in the rapid eye movement (REM) phase of sleep or dreaming, and the amount of time spent in stages III and IV sleep.

The onset of action of pentobarbital occurs within 1 minute following IV administration. The duration of action of barbiturates, related to rate of redistribution throughout the body, is highly variable and can vary in the same patient. Maximal CNS depression may not occur until 15 minutes or more after IV administration.

Plasma pentobarbital concentrations in the therapeutic range of 0.5-3 mcg/mL generally produce sedation and calm, and plasma concentrations of 10-15 mcg/mL produce significant respiratory depression and coma; plasma concentrations of >15 mcg/mL are potentially lethal.

Pentobarbital is rapidly distributed into all tissues and fluids with high concentrations in the brain, liver, and kidneys. The drug crosses the placenta and distributes into milk. Pentobarbital is metabolized primarily by hepatic microsomal enzymes.

Metabolites of pentobarbital are primarily excreted into the urine, and less commonly into the feces. The amount of unchanged pentobarbital that is excreted into the urine is considered negligible. Inactive metabolites undergo excretion as conjugates of glucuronic acid.

The elimination half-life of pentobarbital ranges from 15-50 hours and is dose dependent.

Generic name: pentobarbital sodium

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

Today’s intelligence on Pentobarbital Sodium

Intelligence content is not available yet.

Indications

The following indications are listed for Pentobarbital Sodium:

  • General Anesthesia Adjunct
  • Sedation As Adjunct To Anesthesia
  • Status Epilepticus

Also known as: Adjunct General Anesthesia, Adjunct Sedation.

Dosing

Dosage of pentobarbital sodium must be individualized for each patient, taking into consideration the patient's age, weight, and condition. Dosage of pentobarbital sodium is expressed in terms of the sodium salt.

Drug interactions

Pentobarbital is metabolized by, and induces hepatic microsomal enzymes. Although most reported drug interaction experience has involved the use of phenobarbital, these interactions are applicable to other barbiturates such as pentobarbital.

Contraindications

*Known hypersensitivity to barbiturates.

*History of manifest or latent porphyria.

Adverse reactions

The most common adverse effect reported in up to 3% of patients receiving pentobarbital is somnolence. Other less common adverse effects reported in <1% of patients receiving pentobarbital include agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness, psychiatric disturbance, hallucinations, insomnia, anxiety, dizziness, thinking abnormalities, hypoventilation, apnea, bradycardia, hypotension, syncope, nausea and vomiting, constipation, headache, injection site reactions, hypersensitivity reactions (angioedema, skin rash, exfoliative dermatitis), fever, liver damage, and megaloblastic anemia (following chronic use).

Precautions

No enhanced messaging available.

ICD codes

No ICD codes are available for this drug.

Formulary status

Search health-plan coverage for this drug by ZIP code.

Enter a ZIP code to view available health plans.

Last reviewed · Source: First Databank (FDB) drug data