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

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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.
Thiamylal is a barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. Thiamylal, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia. Thiamylal 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:
SODIUM BUTABARBITAL by IVAX SUB TEVA PHARMS
(1973)
Source URL:
First approved in 1939

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Barbiturates are non-selective depressants of the central nervous system. Butabarbital is one of them, which is used under brand name butisol sodium as a sedative or hypnotic. Like other barbiturates, butabarbital is capable of producing all levels of CNS mood alteration from excitation to mild sedation, to hypnosis, and deep coma. The mechanism of action by which barbiturates exert their effect is not yet completely understood, but is assumed, that butabarbital 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.