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
Pentobarbitone
Pentobarbitone

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.

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

You find simplified version here Pentobarbitone

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0000002
http://classyfire.wishartlab.com/tax_nodes/C0001346
http://classyfire.wishartlab.com/tax_nodes/C0000075
http://classyfire.wishartlab.com/tax_nodes/C0000291
http://classyfire.wishartlab.com/tax_nodes/C0002202
http://classyfire.wishartlab.com/tax_nodes/C0000364
http://classyfire.wishartlab.com/tax_nodes/C0003633
http://classyfire.wishartlab.com/tax_nodes/C0004139
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0000278
http://classyfire.wishartlab.com/tax_nodes/C0003940
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://classyfire.wishartlab.com/tax_nodes/C0001831
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:7983
http://www.hmdb.ca/metabolites/HMDB0014457
http://www.genome.jp/dbget-bin/www_bget?drug:D00499
http://www.genome.jp/dbget-bin/www_bget?cpd:C07422
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4737
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508399
https://www.chemspider.com/Chemical-Structure.4575.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50055935
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=8004
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=7983
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL448
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000671
http://www.pharmgkb.org/drug/PA450859
http://www.rxlist.com/cgi/generic2/pentob.htm
https://www.drugs.com/mtm/pentobarbital.html
https://en.wikipedia.org/wiki/Pentobarbital
*** Taking medicines without doctor's advice can cause long-term problems.
Share