Tìm theo
Modafinil
Các tên gọi khác (5 ) :
  • Modafinil
  • Modafinilo
  • Modafinilum
  • Moderateafinil
  • Provigil
central nervous system stimulants, appetite depressants, neuroprotective agents, stimulants
Thuốc Gốc
Small Molecule
CAS: 68693-11-8
ATC: N06BA07
ĐG : Bryant Ranch Prepack , http://bryantranchprepack.com
CTHH: C15H15NO2S
PTK: 273.35
Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H15NO2S
Phân tử khối
273.35
Monoisotopic mass
273.082349419
InChI
InChI=1S/C15H15NO2S/c16-14(17)11-19(18)15(12-7-3-1-4-8-12)13-9-5-2-6-10-13/h1-10,15H,11H2,(H2,16,17)
InChI Key
InChIKey=YFGHCGITMMYXAQ-UHFFFAOYSA-N
IUPAC Name
2-(diphenylmethane)sulfinylacetamide
Traditional IUPAC Name
2-diphenylmethanesulfinylacetamide
SMILES
NC(=O)CS(=O)C(C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
164-166 °C
Độ hòa tan
Slightly soluble
logP
0.6
logS
-2.6
pKa (strongest acidic)
8.84
pKa (Strongest Basic)
-4.4
PSA
60.16 Å2
Refractivity
77.39 m3·mol-1
Polarizability
28.71 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. Modafinil is not indicated for complaints of lack of energy or fatigue; but it appears to be very helpful for some patients. Also, it has been used in the treatment of hypersomnia, a disorder in which patients lack the capacity for meaningful sleep and may require ten or more hours per day. Recent studies have have found that modafinil may help recovering cocaine addicts fight their addiction.
Cơ Chế Tác Dụng : Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA. The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA. Modafinil is thought to have less potential for abuse than other stimulants due to the absence of any significant euphoric or pleasurable effects. It is possible that modafinil acts by a synergistic combination of mechanisms including direct inhibition of dopamine reuptake, indirect inhibition of noradrenalin reuptake in the VLPO and orexin activation. Modafinil has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors.
Dược Động Học :
▧ Absorption :
Rapid following oral administration.
▧ Volume of Distribution :
* 0.9 L/kg
▧ Protein binding :
60%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
The major route of elimination is metabolism (~90%), primarily by the liver, with subsequent renal elimination of the metabolites.
▧ Half Life :
23-215 hours
Chỉ Định : To improve wakefulness in patients with excessive daytime sleepiness (EDS) associated with narcolepsy.
Tương Tác Thuốc :
  • Carisoprodol Strong CYP2C19 inhibitors such as modafinil may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Clozapine Modafinil increases the effect and toxicity of clozapine
  • Cyclosporine Modafinil decreases the effect of cyclosporine
  • Ethinyl Estradiol Modafinil may decrease the contraceptive effect of ethinyl estradiol. Hormonal contraception should not be solely relied on during concomitant therapy with modafinil.
  • Mestranol Modafinil decreases the effect of the contraceptive
  • Roflumilast Affects CYP1A2 metabolism; decreases level or effect of roflumilast.
  • Telithromycin Telithromycin may reduce clearance of Modafinil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Modafinil if Telithromycin is initiated, discontinued or dose changed.
  • Triazolam Modafinil decreases the effect of triazolam
  • Trimipramine The strong CYP2C19 inhibitor, Modafinil, may decrease the metabolism and clearance of Trimipramine, a CYP2D6 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Modafinil is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of modafinil by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of modafinil if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Provigil 100 mg tablet
    Giá bán buôn : USD >13.58
    Đơn vị tính : tablet
  • Biệt dược thương mại : Provigil 200 mg tablet
    Giá bán buôn : USD >15.33
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty : Shire
    Sản phẩm biệt dược : Alertec
  • Công ty : Saval
    Sản phẩm biệt dược : Alertex
  • Công ty : Medochemie
    Sản phẩm biệt dược : Aspendos
  • Công ty : LKM
    Sản phẩm biệt dược : Forcilin
  • Công ty : Royal Pharma
    Sản phẩm biệt dược : Mentix
  • Công ty : Cephalon
    Sản phẩm biệt dược : Modasomil
  • Công ty : CSL
    Sản phẩm biệt dược : Modavigil
  • Công ty : Cephalon
    Sản phẩm biệt dược : Modiodal
  • Công ty : Ranbaxy
    Sản phẩm biệt dược : Provake
  • Công ty : Cephalon
    Sản phẩm biệt dược : Provigil
  • Công ty : Drugtech
    Sản phẩm biệt dược : Resotyl
  • Công ty : Cephalon
    Sản phẩm biệt dược : Sparlon
  • Công ty : Libbs
    Sản phẩm biệt dược : Stavigile
  • Công ty : Beta
    Sản phẩm biệt dược : Vigicer
  • Công ty : Cephalon
    Sản phẩm biệt dược : Vigil
  • Công ty :
    Sản phẩm biệt dược : Zalux
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00745
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4236
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504648
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01832
ChemSpider
http://www.chemspider.com/Chemical-Structure.4088.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50156055
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0339-4168-11
PharmGKB
http://www.pharmgkb.org/drug/PA450530
Wikipedia
http://en.wikipedia.org/wiki/Modafinil
RxList
http://www.rxlist.com/cgi/generic2/modafinil.htm
PDRhealth
http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=pro1544.html&contentName=Provigil&contentId=631
Drugs.com
http://www.drugs.com/cdi/modafinil.html
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