Pentobarbital

Uses

Pentobarbital is a barbiturate drug used to induce sleep, cause sedation, and control certain types of seizures.

For the short-term treatment of insomnia.

Pentobarbital is also used to associated treatment for these conditions: Insomnia, Severe Convulsion

How Pentobarbital works

Pentobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.

Toxicity

Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.

Food Interaction

Pentobarbital Alcohol interaction

[Major] GENERALLY AVOID:

Concurrent acute use of barbiturates and ethanol may result in additive CNS effects,

including impaired coordination, sedation, and death.

Tolerance of these agents may occur with chronic use.

The mechanism is related to inhibition of microsomal enzymes acutely and induction of hepatic microsomal enzymes chronically.

The combination of ethanol and barbiturates should be avoided.

Pentobarbital Hypertension interaction

[Major] The intravenous administration of barbiturates may produce severe cardiovascular reactions such as bradycardia, hypertension, or vasodilation with fall in blood pressure, particularly during rapid infusion.

Parenteral therapy with barbiturates should be administered cautiously in patients with hypertension, hypotension, or cardiac disease.

The intravenous administration of barbiturates should be reserved for emergency treatment of acute seizures or for anesthesia.

Pentobarbital Drug Interaction

Major: fentanyl, oxycodone, acetaminophen / oxycodoneModerate: zolpidem, methohexital, clonidine, clozapine, prochlorperazine, duloxetine, dexamethasone, secobarbital, quetiapine, vortioxetineUnknown: phentermine, aspirin, ipratropium, onabotulinumtoxinA, multivitamin with minerals, docusate, methylphenidate

Pentobarbital Disease Interaction

Major: acute alcohol intoxication, drug dependence, liver disease, porphyria, rash, respiratory depression, cardiovascular, prolonged hypotensionModerate: adrenal insufficiency, depression, hematologic toxicity, osteomalacia, paradoxical reactions

Elimination Route

Barbiturates are absorbed in varying degrees following oral, rectal, or parenteral administration.

Half Life

5 to 50 hours (dose dependent)

Elimination Route

Barbiturates are metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine, and less commonly, in the feces. Approximately 25 to 50 percent of a dose of aprobarbital or phenobarbital is eliminated unchanged in the urine, whereas the amount of other barbiturates excreted unchanged in the urine is negligible.

Innovators Monograph

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