Methohexital

Các tên gọi khác (9 ) :

(+-)-5-Allyl-1-methyl-5-(1-methyl-2-pentynyl)barbituric acid
5-Allyl-1-methyl-5-(1-methyl-2-pentynyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
5-Allyl-1-methyl-5-(1-methyl-pent-2-ynyl)-pyrimidine-2,4,6-trione
5-Allyl-5-(3-hexyn-2-yl)-1-methylbarbituric acid
alpha-DL-1-Methyl-5-allyl-5-(1'-methylpentyn-2-yl)barbituric acid
Methohexital
Methohexitalum
Methohexitone
Metohexital

anesthetics intravenous, barbiturates

Thuốc Gốc

Small Molecule

CAS: 151-83-7

ATC: N01AF01, N05CA15

ĐG : JHP Pharmaceuticals LLC , http://www.jhppharma.com

CTHH: C₁₄H₁₈N₂O₃

PTK: 262.3043

An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia. [PubChem]

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₄H₁₈N₂O₃

Phân tử khối

262.3043

Monoisotopic mass

262.131742452

InChI

InChI=1S/C14H18N2O3/c1-5-7-8-10(3)14(9-6-2)11(17)15-13(19)16(4)12(14)18/h6,10H,2,5,9H2,1,3-4H3,(H,15,17,19)

InChI Key

InChIKey=NZXKDOXHBHYTKP-UHFFFAOYSA-N

IUPAC Name

5-(hex-3-yn-2-yl)-1-methyl-5-(prop-2-en-1-yl)-1,3-diazinane-2,4,6-trione

Traditional IUPAC Name

methohexital

SMILES

CCC#CC(C)C1(CC=C)C(=O)NC(=O)N(C)C1=O

Độ hòa tan

5.24e-02 g/l

logP

1.8

logS

-3.7

pKa (strongest acidic)

8.73

PSA

66.48 Å²

Refractivity

71.51 m³·mol^-1

Polarizability

27.4 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

Dược Lực Học : Methohexital, 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. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.

Cơ Chế Tác Dụng : An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia. [PubChem] Methohexital 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 :
The absolute bioavailability following rectal administration of methohexital is 17%.
▧ Protein binding :
73%
▧ Metabolism :
Metabolism occurs in the liver through demethylation and oxidation. Side-chain oxidation is the most important biotransformation involved in termination of biologic activity.
▧ Route of Elimination :
Excretion occurs via the kidneys through glomerular filtration.
▧ Half Life :
5.6 ± 2.7 minutes

Độc Tính : The onset of toxicity following an overdose of intravenously administered methohexital will be within seconds of the infusion. If methohexital is administered rectally or is ingested, the onset of toxicity may be delayed. The manifestations of an ultrashort-acting barbiturate in overdose include central nervous system depression, respiratory depression, hypotension, loss of peripheral vascular resistance, and muscular hyperactivity ranging from twitching to convulsive-like movements. Other findings may include convulsions and allergic reactions. Following massive exposure to any barbiturate, pulmonary edema, circulatory collapse with loss of peripheral vascular tone, and cardiac arrest may occur.

Chỉ Định : Methohexital is indicated for use as an intravenous anaesthetic. It has also been commonly used to induce deep sedation.

Tương Tác Thuốc :

Aminophylline The barbiturate, methohexital, decreases the effect of aminophylline.
Betamethasone The barbiturate, methohexital, may decrease the effect of the corticosteroid, betamethasone.
Clomifene The enzyme inducer, methohexital, decreases the effect of the hormone agent, clomifene.
Conjugated Estrogens The enzyme inducer, methohexital, decreases the effect of the hormone agent, conjugated estrogens.
Cyclosporine The barbiturate, methohexital, increases the effect of cyclosporine.
Dexamethasone The barbiturate, methohexital, may decrease the effect of the corticosteroid, dexamethasone.
Diethylstilbestrol The enzyme inducer, methohexital, decreases the effect of the hormone agent, diethylstilbestrol.
Doxycycline The anticonvulsant, methohexital, decreases the effect of doxycycline.
Estradiol The enzyme inducer, methohexital, decreases the effect of the hormone agent, estradiol.
Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
Felodipine The barbiturate, methohexital, decreases the effect of felodipine.
Fludrocortisone The barbiturate, methohexital, may decrease the effect of the corticosteroid, fludrocortisone.
Folic Acid Folic acid decreases the effect of anticonvulsant, methohexital.
Gefitinib The CYP3A4 inducer, methohexital, may decrease the serum concentration and therapeutic effects of gefitinib.
Griseofulvin The barbiturate, methohexital, decreases the effect of griseofulvin.
Hydrocortisone The barbiturate, methohexital, may decrease the effect of the corticosteroid, hydrocortisone.
Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
Medroxyprogesterone Acetate The enzyme inducer, methohexital, decreases the effect of the hormone agent, medroxyprogesterone.
Megestrol acetate The enzyme inducer, methohexital, decreases the effect of the hormone agent, megestrol.
Methadone The barbiturate, methohexital, decreases the effect of methadone.
Metronidazole The barbiturate, methohexital, decreases the effect of metronidazole.
Nifedipine The barbiturate, methohexital, decreases the effect of the calcium channel blocker, nifedipine.
Norethindrone This product may cause a slight decrease of contraceptive effect
Oxtriphylline The barbiturate, methohexital, decreases the effect of oxtriphylline.
Prednisolone The barbiturate, methohexital, may decrease the effect of the corticosteroid, prednisolone.
Prednisone The barbiturate, methohexital, may decrease the effect of the corticosteroid, prednisone.
Quinidine The anticonvulsant, methohexital, decreases the effect of quinidine.
Theophylline The barbiturate, methohexital, decreases the effect of theophylline.
Triamcinolone The barbiturate, methohexital, may decrease the effect of the corticosteroid, triamcinolone.
Trimipramine The barbiturate, Methohexital, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Methohexital is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required.
Triprolidine The CNS depressants, Triprolidine and Methohexital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Verapamil Methohexital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Methohexital is initiated, discontinued or dose changed.
Warfarin Methohexital may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if methohexital is initiated, discontinued or dose changed.

Liều Lượng & Cách Dùng : Injection, powder, for solution - Intramuscular
Injection, powder, for solution - Intravenous

Dữ Kiện Thương Mại

Giá thị trường

Biệt dược thương mại : Brevital sodium 2.5 gm vial

Giá bán buôn : USD >221.2

Đơn vị tính : vial

Nhà Sản Xuất

Công ty :

Sản phẩm biệt dược : Brevital
Công ty :

Sản phẩm biệt dược : Brietal

Đóng gói

Công ty : JHP Pharmaceuticals LLC

Website : http://www.jhppharma.com
Công ty : Physicians Total Care Inc.

Website : http://www.physicianstotalcare.com

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00474

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=9034

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507954

KEGG Compound

http://www.genome.jp/dbget-bin/www_bget?cpd:C07844

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D04985

ChemSpider

http://www.chemspider.com/Chemical-Structure.8683.html

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/42023-105-01

PharmGKB

http://www.pharmgkb.org/drug/PA164784030

Wikipedia

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

RxList

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

Drugs.com

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

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