Thiopental

Các tên gọi khác (16 ) :

(+-)-Thiopental
2-Thio-5-ethyl-5-sec-pentylbarbituric acid
5-Ethyl-5-(1-methyl-butyl)-2-thioxo-dihydro-pyrimidine-4,6-dione
Bitaryl
Omexolon
Penthiobarbital
Pentothiobarbital
Sodium Pentothal
Thiomebumalum
Thiopental
Thiopentobarbital
Thiopentobarbitone
Thiopentobarbituric acid
Thiopentone
Tiopentale
Trapanal

Thuốc gây tê, mê

Thuốc Gốc

Small Molecule

CAS: 76-75-5

ATC: N01AF03, N05CA19

ĐG : Baxter International Inc. , http://www.baxter.com

CTHH: C₁₁H₁₈N₂O₂S

PTK: 242.338

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)

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₁H₁₈N₂O₂S

Phân tử khối

242.338

Monoisotopic mass

242.10889852

InChI

InChI=1S/C11H18N2O2S/c1-4-6-7(3)11(5-2)8(14)12-10(16)13-9(11)15/h7H,4-6H2,1-3H3,(H2,12,13,14,15,16)

InChI Key

InChIKey=IUJDSEJGGMCXSG-UHFFFAOYSA-N

IUPAC Name

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

Traditional IUPAC Name

thiopental

SMILES

CCCC(C)C1(CC)C(=O)NC(=S)NC1=O

Độ hòa tan

3.98e-02 g/l

logP

2.85

logS

-3.36

pKa (strongest acidic)

7.2

pKa (Strongest Basic)

-3

PSA

58.2 Å²

Refractivity

65.99 m³·mol^-1

Polarizability

25.7 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Ghose Filter

true

pKa

7.55

Dược Lực Học : 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

Cơ Chế Tác Dụng : 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) 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.

Dược Động Học :

▧ Absorption :
Rapidly absorbed.
▧ 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.
▧ Half Life :
3-8 hours

Độc Tính : 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.

Chỉ Định : 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.

Tương Tác Thuốc :

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 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 Acetate 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.

Liều Lượng & Cách Dùng : Powder, for solution - Intravenous

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Incepta

Sản phẩm biệt dược : Anestho
Công ty : Fada

Sản phẩm biệt dược : Bensulf
Công ty : Brookes

Sản phẩm biệt dược : Bitol Sodium
Công ty : Tüm Ekip

Sản phẩm biệt dược : Ekipental
Công ty : Marvecs Pharma Services

Sản phẩm biệt dược : Farmotal
Công ty : Abbott

Sản phẩm biệt dược : Intraval Sodium
Công ty : I.E. Ulagay

Sản phẩm biệt dược : Pental Sodyum
Công ty : Swiss Parenterals

Sản phẩm biệt dược : Pentazol
Công ty : Oboi

Sản phẩm biệt dược : Penthal
Công ty : Abbott

Sản phẩm biệt dược : Penthotal Sodium
Công ty : Choong Wae

Sản phẩm biệt dược : Pentotan
Công ty : Rotexmedica

Sản phẩm biệt dược : Pentotex
Công ty : Hospira

Sản phẩm biệt dược : Pentothal
Công ty : Ravonal

Sản phẩm biệt dược : Ravonal
Công ty : ACI

Sản phẩm biệt dược : Thiopen
Công ty : Richmond

Sản phẩm biệt dược : Tiopental
Công ty : Nycomed

Sản phẩm biệt dược : Trapanal

Đóng gói

Công ty : Baxter International Inc.

Website : http://www.baxter.com
Công ty : Hospira Inc.

Website : http://www.hospira.com
Công ty : Teva Pharmaceutical Industries Ltd.

Website : http://www.tevapharm.com

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00599

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3000715

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504621

KEGG Compound

http://www.genome.jp/dbget-bin/www_bget?cpd:C07521

ChemSpider

http://www.chemspider.com/Chemical-Structure.2272258.html

PharmGKB

http://www.pharmgkb.org/drug/PA451664

Wikipedia

http://en.wikipedia.org/wiki/Thiopental

RxList

http://www.rxlist.com/cgi/generic3/thiopental.htm

Drugs.com

http://www.drugs.com/cdi/thiopental.html

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