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QuickView for Thiopental (compound)


PubChem
Name: Thiopental
PubChem Compound ID: 3000715
Description: A barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration.
Molecular formula: C11H18N2O2S
Molecular weight: 242.339 g/mol
Synonyms:
Barbituric acid, 5-ethyl-5-(1-methylbutyl)-2-thio-; 59709-53-4; DEA No. 2100; Thiomebumal; 76-75-5; 4,6(1H,5H)-Pyrimidinedione, 5-ethyldihydro-5-(1-methylbutyl)-2-thioxo-; Thiopentobarbituric acid; 5-24-09-00172 (Beilstein Handbook Reference); AIDS018477; Thiopentobarbital.
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DrugBank
Identification
Name: Thiopental
Name (isomeric): DB00599
Drug Type: small molecule
Description: A barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration.
Synonyms:
Thiopentobarbitone; Thionembutal; Thiomebumal; Thiopentobarbituric acid; Penthiobarbital; Pentothal; Thiopentobarbital; Pentothiobarbital; Tiopentale [Italian]; Thiopentone
Brand: Farmotal, Thiothal, Trapanal, Nesdonal, Intraval
Brand name mixture: Thiotal 5g(Thiopental Sodium + Water)
Category: Anesthetics, Intravenous, GABA Modulators, Hypnotics and Sedatives, Anticonvulsants
CAS number: 76-75-5
Pharmacology
Indication: For use as the sole anesthetic agent for brief (15 minute) procedures, for induction of anesthesia prior to administration of other anesthetic agents, to supplement regional anesthesia, to provide hypnosis during balanced anesthesia with other agents for analgesia or muscle relaxation, for the control of convulsive states during or following inhalation anesthesia or local anesthesia, in neurosurgical patients with increased intracranial pressure, and for narcoanalysis and narcosynthesis in psychiatric disorders.
Pharmacology:
Thiopental, a barbiturate, is used for the induction of anesthesia prior to the use of other general anesthetic agents and for induction of anesthesia for short surgical, diagnostic, or therapeutic procedures associated with minimal painful stimuli. Thiopental is an ultrashort-acting depressant of the central nervous system which induces hypnosis a...
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Mechanism of Action: 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.
Absorption: Rapidly absorbed.
Protein binding: Approximately 80% of the drug in the blood is bound to plasma protein.
Biotransformation: Primarily hepatic. Biotransformation products of thiopental are pharmacologically inactive and mostly excreted in the urine.
Half Life: 3-8 hours
Toxicity: Overdosage may occur from too rapid or repeated injections. Too rapid injection may be followed by an alarming fall in blood pressure even to shock levels. Apnea, occasional laryngospasm, coughing and other respiratory difficulties with excessive or too rapid injections may occur. Lethal blood levels may be as low as 1 mg/100 mL for short-acting barbiturates; less if other depressant drugs or alcohol are also present.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
MestranolThiopental may decrease the effect of Mestranol. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
NicardipineThe CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nicardipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nicardipine if Thiopental is initiated, discontinued or dose changed.
TrimipramineThe barbiturate, Thiopental, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Thiopental is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required.
MethadoneThiopental may decrease the effect of Methadone by increasing Methadone metabolism. Methadone withdrawal may occur.
NisoldipineThe CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nisoldipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nisoldipine if Thiopental is initiated, discontinued or dose changed.
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Enzymes