药品详细

Thiopental(硫喷妥钠)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

硫喷妥钠

英文名

Thiopental

分子式

C₁₁H₁₈N₂O₂S

化学名

5-ethyl-5-(pentan-2-yl)-2-sulfanylidene-1,3-diazinane-4,6-dione

分子量

Average: 242.338
Monoisotopic: 242.10889852

CAS号

76-75-5

ATC分类

N01A 未知;N05C 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

A barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration. It is also used for hypnosis and for the control of convulsive states. It has been used in neurosurgical patients to reduce increased intracranial pressure. It does not produce any excitation but has poor analgesic and muscle relaxant properties. Small doses have been shown to be anti-analgesic and lower the pain threshold. (From Martindale, The Extra Pharmacopoeia, 30th ed, p920)

生产厂家

Abbott laboratories hosp products div

封装厂家

参考

Synthesis Reference

Not Available

General Reference

Morgan DJ, Blackman GL, Paull JD, Wolf LJ: Pharmacokinetics and plasma binding of thiopental. II: Studies at cesarean section. Anesthesiology. 1981 Jun;54(6):474-80. Pubmed
Perez-Barcena J, Barcelo B, Homar J, Abadal JM, Molina FJ, de la Pena A, Sahuquillo J, Ibanez J: [Comparison of the effectiveness of pentobarbital and thiopental in patients with refractory intracranial hypertension. Preliminary report of 20 patients] Neurocirugia (Astur). 2005 Feb;16(1):5-12; discussion 12-3. Pubmed
WINTERS WD, SPECTOR E, WALLACH DP, SHIDEMAN FE: Metabolism of thiopental-S35 and thiopental-2-C14 by a rat liver mince and identification of pentobarbital as a major metabolite. J Pharmacol Exp Ther. 1955 Jul;114(3):343-57. Pubmed
Bory C, Chantin C, Boulieu R, Cotte J, Berthier JC, Fraisse D, Bobenrieth MJ: [Use of thiopental in man. Determination of this drug and its metabolites in plasma and urine by liquid phase chromatography and mass spectrometry] C R Acad Sci III. 1986;303(1):7-12. Pubmed

剂型

规格

化合物类型

Type	small molecule

Classes

Barbiturates
Lactams

Substructures

Barbiturates
Carbonyl Compounds
Amino Ketones
Carboxylic Acids and Derivatives
Pyrimidines and Derivatives
Ureas and Derivatives
Heterocyclic compounds
Carboxamides and Derivatives
Lactams

适应症

药理

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.
Pharmacodynamics	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 and anesthesia, but not analgesia. It produces hypnosis within 30 to 40 seconds of intravenous injection. Recovery after a small dose is rapid, with some somnolence and retrograde amnesia. Repeated intravenous doses lead to prolonged anesthesia because fatty tissues act as a reservoir; they accumulate Pentothal in concentrations 6 to 12 times greater than the plasma concentration, and then release the drug slowly to cause prolonged anesthesia
Mechanism of action	Thiopental binds at a distinct binding site associated with a Cl^- ionopore at the GABA_A 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.
Volume of distribution	Not Available
Protein binding	Approximately 80% of the drug in the blood is bound to plasma protein.
Metabolism	Primarily hepatic. Biotransformation products of thiopental are pharmacologically inactive and mostly excreted in the urine.
Route of elimination	Not Available
Half life	3-8 hours
Clearance	Not Available
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
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
logP	2.85	HANSCH,C ET AL. (1995)
logS	-3.36	ADME Research, USCD
pKa	7.55	SANGSTER (1994)

Predicted Properties

Property	Value	Source
water solubility	3.98e-02 g/l	ALOGPS
logP	3.05	ALOGPS
logP	2.78	ChemAxon
logS	-3.8	ALOGPS
pKa (strongest acidic)	7.2	ChemAxon
pKa (strongest basic)	-3	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	2	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	58.2	ChemAxon
rotatable bond count	4	ChemAxon
refractivity	65.99	ChemAxon
polarizability	25.7	ChemAxon

药物相互作用

Drug	Interaction
Acenocoumarol	Thiopental may increase the metabolism of the Vitamin K antagonist, Acenocoumarol. Acenocoumarol dose adjustment may be required.
Amlodipine	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Amlodipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Amlodipine if Thiopental is initiated, discontinued or dose changed.
Chloramphenicol	Chloramphenicol may increase the serum concentration of Thiopental by decreasing Thiopental metabolism. Thiopental may decrease the serum concentration of Chloramphenicol by increasing Chloramphenicol metabolism. Monitor for changes in therapeutic effects of both agents if concomitant therapy is initiated, discontinued or doses are adjusted.
Cyclosporine	Thiopental may increase the metabolism and clearance of Cyclosporine. Monitor for changes in the therapeutic/adverse effects of Cyclosporine if Thiopental is initiated, discontinued or dose changed.
Desogestrel	Thiopental may decrease the effect of Desogestrel. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Diltiazem	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Diltiazem, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Diltiazem if Thiopental is initiated, discontinued or dose changed.
Disopyramide	Thiopental may increase the metabolism and clearance of Disopyramide. Monitor for changes in therapeutic/adverse effects of Disopyramide if Thiopental is inititaed, discontinued or dose changed.
Doxycycline	Thiopental may decrease the serum levels of Doxycycline. A reduction in antimicrobial effects may occur. An alternative antibiotic may be considered.
Drospirenone	Thiopental may decrease the effect of Drospirenone. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Ethinyl Estradiol	Thiopental may decrease the effect of Ethinyl estradiol. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Ethynodiol Diacetate	Thiopental may decrease the effect of Ethynodiol diacetate. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Etonogestrel	Thiopental may decrease the effect of Etonogestrel. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Felodipine	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Felodipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Felodipine if Thiopental is initiated, discontinued or dose changed.
Isradipine	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Isradipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Isradipine if Thiopental is initiated, discontinued or dose changed.
Lamotrigine	Thiopental may increase the metabolism and clearance of Lamotrigine. Monitor for decreased therapeutic effect of Lamotrigine if Thiopental is initiated.
Levonorgestrel	Thiopental may decrease the effect of Levonorgestrel. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Medroxyprogesterone	Thiopental may decrease the effect of Medroxyprogesterone. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Mestranol	Thiopental may decrease the effect of Mestranol. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Methadone	Thiopental may decrease the effect of Methadone by increasing Methadone metabolism. Methadone withdrawal may occur.
Nicardipine	The 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.
Nifedipine	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nifedipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nifedipine if Thiopental is initiated, discontinued or dose changed.
Nimodipine	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nimodipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nimodipine if Thiopental is initiated, discontinued or dose changed.
Nisoldipine	The 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.
Nitrendipine	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nitrendipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nitrendipine if Thiopental is initiated, discontinued or dose changed.
Norethindrone	Thiopental may decrease the effect of Norethindrone. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Norgestimate	Thiopental may decrease the effect of Norgestimate. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
Propafenone	Thiopental may increase the metabolism and clearance of Propafenone. Monitor for decreased therapeutic effect of Propafenone if Thiopental is initiated.
Quinidine	Thiopental may increase the metabolism and clearance of Quinidine. Monitor for decreased therapeutic effect of Quinidine if Thiopental is initiated.
Trimipramine	The 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.
Triprolidine	The CNS depressants, Triprolidine and Thiopental, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Verapamil	Thiopental, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Thiopental is initiated, discontinued or dose changed.
Warfarin	Thiopental may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if thiopental is initiated, discontinued or dose changed.

食物相互作用

Not Available

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