Pentobarbitone
Pentobarbitone Uses, Dosage, Side Effects, Food Interaction and all others data.
A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)
Pentobarbitone, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
| Trade Name | Pentobarbitone |
| Availability | Prescription only |
| Generic | Pentobarbital |
| Pentobarbital Other Names | Pentobarbital, Pentobarbitone |
| Related Drugs | trazodone, hydroxyzine, lorazepam, diazepam, promethazine, fentanyl, Ativan, Valium, phenytoin, midazolam |
| Type | |
| Formula | C11H18N2O3 |
| Weight | Average: 226.2722 Monoisotopic: 226.131742452 |
| Groups | Approved, Investigational, Vet approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Pentobarbitone is a barbiturate drug used to induce sleep, cause sedation, and control certain types of seizures.
For the short-term treatment of insomnia.
Pentobarbitone is also used to associated treatment for these conditions: Insomnia, Severe Convulsion
How Pentobarbitone works
Pentobarbitone 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
No interactions found.Pentobarbitone 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.
Pentobarbitone 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.
Pentobarbitone 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
Pentobarbitone 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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