Nembutal Sodium (pentobarbital sodium)
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.
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Indications
The following indications are listed for Nembutal 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.
Pentobarbital sodium may be administered by deep IM or slow IV injection. The drug also has been administered as a continuous IV infusion+ in the treatment of refractory status epilepticus; administration by continuous IV infusion requires assisted ventilation and cardiovascular monitoring.. IV administration of pentobarbital should usually be reserved for acute treatment, when other routes of administration are not feasible or immediate onset is necessary.
Because parenteral pentobarbital solution is highly alkaline, extreme caution should be taken to avoid perivascular extravasation or accidental intra-arterial injection of the drug. Extravascular injection of pentobarbital can cause local tissue damage and subsequent necrosis, while intra-arterial injection can lead to transient pain, or in severe cases, gangrene of the limb. If complaints of limb pain occur in patients receiving pentobarbital injection, the injection should be stopped.
Pentobarbital sodium injection should be stored at 20-25degreesC (excursions permitted from 15-30degreesC); freezing and exposure of the injection to extreme heat should be avoided. The drug should not be used if there is discoloration or precipitation.
No dosing information is available for this tab.
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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.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to barbiturates.
*History of manifest or latent porphyria.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
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).
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Animal data indicate that use of anesthetic and sedation drugs, including pentobarbital, that block NMDA receptors and/or potentiate GABA activity leads to increased neuronal apoptosis in the developing brain and results in long-term cognitive deficits when administered for >3 hours. Although the clinical importance of these findings have not been fully elucidated, the window of vulnerability to these neurodevelopmental changes is thought to correlate with exposure during the third trimester of pregnancy through the first year of life in humans, but may extend to approximately 3 years of age.
Some published evidence suggests that similar deficits in cognition and behavior may occur in children following repeated or prolonged exposure to anesthesia early in life, although there are substantial limitations to this data.
Anesthetic and sedation drugs are an essential component of care for children who require surgery or other procedures that cannot be delayed; no specific general anesthetic or sedation drug has been shown to be safer than any other such drug. When procedures requiring the use of general anesthetics or sedation drugs are considered for young children, clinicians should take into consideration the benefits, risks (including potential risk of adverse neurodevelopmental effects), and appropriate timing and duration of the procedure.
Based on animal data, repeated or prolonged use of general anesthetics and sedatives, including pentobarbital sodium, during the third trimester of pregnancy may result in adverse neurodevelopmental effects in the fetus. The clinical importance of these animal findings to humans is not known; the potential risk of adverse neurodevelopmental effects should be considered and discussed with pregnant women undergoing procedures requiring general anesthetics and sedation drugs.
Infants with long-term exposure to barbiturates in utero may exhibit an immediate or delayed onset of withdrawal symptoms (e.g., seizures, hyperirritability) up to 14 days after birth.
If pentobarbital is administered during pregnancy, or the patient becomes pregnant while receiving the drug, the patient should be informed of the potential fetal hazard.
Because barbiturates such as pentobarbital are excreted into the milk in small amounts, caution should be exerted when barbiturates are administered to nursing women.
Because geriatric patients may be more sensitive to barbiturates, the manufacturer recommends reducing the dosage of pentobarbital sodium.
In general, dosage selection for geriatric patients should be undertaken with caution and started at the lower end of the dosage range, taking into account the greater frequency of reduced hepatic, renal, or cardiac function and of concomitant diseases or drug therapy.
Clinical studies of pentobarbital did not include a sufficient number of patients >=65 years of age to assess differences compared to younger adults. Other reported clinical experiences with pentobarbital have also not identified differences in response between geriatric and younger adult patients.
Geriatric patients may be more sensitive to barbiturate therapy, and may frequently react to barbiturates with excitement, confusion, or depression.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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