Amobarbital

Amobarbital Uses, Dosage, Side Effects, Food Interaction and all others data.

A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565)

Trade Name Amobarbital
Availability Prescription only
Generic Amobarbital
Amobarbital Other Names Amobarbital, Amobarbitale, Amylobarbitone, Barbamil, Barbamyl
Related Drugs trazodone, hydroxyzine, lorazepam, promethazine, fentanyl, Ativan
Type
Formula C11H18N2O3
Weight Average: 226.2722
Monoisotopic: 226.131742452
Groups Approved, Illicit
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Amobarbital
Amobarbital

Uses

Amobarbital is a barbiturate derivative used for the induction of sedation during procedures, short-term management of insomnia, and acute management of refractory tonic-clonic seizures.

How Amobarbital works

Amobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Amobarbital also appears to bind neuronal nicotinic acetylcholine receptors.

Food Interaction

  • Avoid alcohol. Ingesting alcohol may increase the CNS depressant effects of amobarbital.
  • Take on an empty stomach. Taking oral amobarbital sodium on an empty stomach increases the rate of absorption.

Amobarbital 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.

Amobarbital 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.

Innovators Monograph

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https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:2673
http://www.hmdb.ca/metabolites/HMDB0015440
http://www.genome.jp/dbget-bin/www_bget?drug:D00555
http://www.genome.jp/dbget-bin/www_bget?cpd:C07536
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2164
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508165
https://www.chemspider.com/Chemical-Structure.2079.html
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=719
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=2673
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL267894
https://zinc.docking.org/substances/ZINC000004811698
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000686
http://www.pharmgkb.org/drug/PA448401
https://en.wikipedia.org/wiki/Amobarbital
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