U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1 - 10 of 17 results


Class (Stereo):
CHEMICAL (MIXED)


Conditions:

Methohexital is an ultrashort-acting barbiturate widely used in dentistry because of its rapid onset, predictable effects, and short duration of action. It was marked under the name brevital sodium for the intravenous anaesthesia. It has also been commonly used to induce deep sedation. Like other barbiturates, methohexital exerts its effects through the gamma-aminobutyric acid (GABA) receptor complex. By binding to its own receptor on the complex, methohexital augments the inhibitory effect of GABA on neurons and additionally can exert a similar effect independent of GABA.
Status:
US Previously Marketed
Source:
Medomin by Geigy
(1955)
Source URL:
First approved in 1954
Source:
Heptabarbital by Ciba-Geigy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

HEPTABARBITAL is an intermediate or short term barbiturate. It binds to the GABAA receptor at either the alpha or the beta subunit. 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. HEPTABARBITAL was formerly used as a sedative and hypnotic drug.
Status:
US Previously Marketed
First approved in 1954

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Talbutal is a short to intermediate-acting barbiturate, which had been used under brand name Latusate as a sedative and hypnotic, but then this usage was discontinued. It was found, that talbutal binds at a distinct binding site at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. Thus, the post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Status:
US Previously Marketed
First marketed in 1934

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Sodium thiopental (also known as Sodium Pentothal, thiopental) was discovered in 1930s by investigators working for Abbott Laboratories. Thiopental sodium was used for the induction of general anesthesia and is used as an adjunct to provide hypnosis during balanced anesthesia with other anesthetic agents, including analgesics and muscle relaxants. Thiopental sodium was also used as an adjunct for control of convulsive disorders of various etiology, including those caused by local anesthetics. Finally, thiopental sodium had been used to reduce the intracranial pressure in patients with increased intracranial pressure, if controlled ventilation is provided. Nevertheless, these prescriptions of drug were discontinued. In addition, this drug was banned for use in US executions. Thiopental sodium acts through the CNS with particular activity in the mesencephalic reticular activating system. It was shown, that mechanism of action of sodium thiopental via GABAA receptor. Thiopental 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.
Status:
US Previously Marketed
Source:
amobarbital
(1923)
Source URL:
First marketed in 1923

Class (Stereo):
CHEMICAL (ACHIRAL)



AMOBARBITAL is a barbiturate derivative with hypnotic and sedative properties. In an in vitro study in rat thalamic slices amobarbital worked by activating GABAA receptors, which decreased input resistance, depressed 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 increased both the amplitude and decay time of inhibitory postsynaptic currents. Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high.
Status:
US Previously Marketed
Source:
butobarbital
(1923)
Source URL:
First marketed in 1923
Source:
butobarbital
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Butethal is a sedative and a hypnotic drug indicated for the treatment of severe intractable insomnia. It acts on receptors in the brain (GABA A receptors) causing the release of the chemical GABA. This chemical inhibits certain areas of the brain resulting in sleepiness. Common side effects are: drowsiness, sedation, unsteadiness, vertigo and inco- ordination. Also, hangover effect, paradoxical excitement, confusion, memory defects and skin rashes. Interactions may occur with the following: adrenocorticoids (cortisone-like medicine), anticoagulants (blood thinners), carbamazepine, corticotropin (barbiturates may decrease the effects of these medicines), central nervous system (CNS) depressants (using these medicines with barbiturates may result in increased CNS depressant effects), divalproex sodium, valproic acid (using these medicines with barbiturates may change the amount of either medicine that you need to take), and oral contraceptives containing estrogens (barbiturates may decrease the effectiveness of these oral contraceptives, and you may need to change to a different type of birth control).
Status:
US Previously Marketed
Source:
ALLONAL APROBARBITAL by ROCHE
(1961)
Source URL:
First marketed in 1921
Source:
ALLONAL APROBARBITAL by ROCHE
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Aprobarbital is a barbiturate derivative. Aprobarbital have been used for the short-term treatment of insomnia and for routine sedation to relieve anxiety, tension, and apprehension however, barbiturates generally have been replaced by benzodiazepines.
Status:
US Previously Marketed
Source:
Veronal by Friedr. Bayer 8: Co., Elberfeld, Germany, and E. Merck, Darmstadt, Germany.
(1903)
Source URL:
First marketed in 1903
Source:
Veronal by Friedr. Bayer 8: Co., Elberfeld, Germany, and E. Merck, Darmstadt, Germany.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Barbital, the one of the series of barbiturates, has hypnotic, sedative, and anticonvulsant properties and used under the trade name Veronal. It calmed manic patients and helped melancholic patients to sleep and was an effective inducer of sleep in insomniacs, but at the same time compound could induced dependence. It was substituted by the butyl analog, butobarbital, which was three times stronger and its period of action was much shorter due to its lipophilicity. Barbital is a ligand of GABA-receptor complex and in addition, it could have another target, a creatine kinase.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Vinylbital is a barbiturate derivative. It was introduced into therapy in 1963 and used as a sedative and in the treatment of insomnia.

Showing 1 - 10 of 17 results