Tìm theo
Zaleplon
Các tên gọi khác (1) :
  • 3'-(3-Cyanopyrazolo(1,5-a)pyrimidin-7-yl)-N-ethylacetanilide
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 151319-34-5
ATC: N05CF03
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C17H15N5O
PTK: 305.3339
Zaleplon is a sedative/hypnotic, mainly used for insomnia. It is known as a nonbenzodiazepine hypnotic. Zaleplon interacts with the GABA receptor complex and shares some of the pharmacological properties of the benzodiazepines. Zaleplon is a schedule IV drug in the United States.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H15N5O
Phân tử khối
305.3339
Monoisotopic mass
305.127660127
InChI
InChI=1S/C17H15N5O/c1-3-21(12(2)23)15-6-4-5-13(9-15)16-7-8-19-17-14(10-18)11-20-22(16)17/h4-9,11H,3H2,1-2H3
InChI Key
InChIKey=HUNXMJYCHXQEGX-UHFFFAOYSA-N
IUPAC Name
N-(3-{3-cyanopyrazolo[1,5-a]pyrimidin-7-yl}phenyl)-N-ethylacetamide
Traditional IUPAC Name
zaleplon
SMILES
CCN(C(C)=O)C1=CC=CC(=C1)C1=CC=NC2=C(C=NN12)C#N
Độ tan chảy
157-159 °C
Độ hòa tan
4.03e-02 g/l
logP
0.9
logS
-3.9
pKa (Strongest Basic)
0.3
PSA
74.29 Å2
Refractivity
97.24 m3·mol-1
Polarizability
32.09 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Zaleplon is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Zaleplon is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zaleplon also binds selectively to the CNS GABAA-receptor chloride ionophore complex at benzodiazepine(BZ) omega-1 (BZ1, ο1) receptors.
Cơ Chế Tác Dụng : Zaleplon is a sedative/hypnotic, mainly used for insomnia. It is known as a nonbenzodiazepine hypnotic. Zaleplon interacts with the GABA receptor complex and shares some of the pharmacological properties of the benzodiazepines. Zaleplon is a schedule IV drug in the United States. Zaleplon exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex. Zaleplon also binds selectively to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding.
Dược Động Học :
▧ Absorption :
Absorption Zaleplon is rapidly and almost completely absorbed following oral administration.
▧ Volume of Distribution :
* 1.4 L/kg
▧ Protein binding :
Approximately 60% (in vitro plasma protein binding).
▧ Metabolism :
Zaleplon is primarily metabolized by aldehyde oxidase.
▧ Route of Elimination :
Zaleplon is metabolized primarily by the liver and undergoes significant presystemic metabolism. After oral administration, zaleplon is extensively metabolized, with less than 1% of the dose excreted unchanged in urine. Renal excretion of unchanged zaleplon accounts for less than 1% of the administered dose.
▧ Half Life :
Approximately 1 hour
▧ Clearance :
* 1 L/h/kg
Độc Tính : Side effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss, menstrual pain, nausea, sleepiness, tingling, weakness
Chỉ Định : For the treatment of short-term treatment of insomnia in adults.
Tương Tác Thuốc :
  • Cimetidine Cimetidine may increase the serum concentration of zaleplon by decreasing its metabolism. Reduce the initial dose of zaleplon to 5 mg in patients receiving cimetidine.
  • Methotrimeprazine Additive CNS depressant effects may occur. A dose reduction of zaleplon may be required. Monitor for increased CNS depression during concomitant therapy.
  • Rifampicin Rifampin decreases the effect of zaleplon
  • Triprolidine The CNS depressants, Triprolidine and Zaleplon, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Zaleplon 10 mg capsule
    Giá bán buôn : USD >2.09
    Đơn vị tính : capsule
  • Biệt dược thương mại : Zaleplon 5 mg capsule
    Giá bán buôn : USD >2.13
    Đơn vị tính : capsule
  • Biệt dược thương mại : Sonata 5 mg capsule
    Giá bán buôn : USD >5.26
    Đơn vị tính : capsule
  • Biệt dược thương mại : Sonata 10 mg capsule
    Giá bán buôn : USD >6.83
    Đơn vị tính : capsule
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Sonata
  • Công ty :
    Sản phẩm biệt dược : Zalaplon
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00962
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5719
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508267
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07484
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00530
ChemSpider
http://www.chemspider.com/Chemical-Structure.5517.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0832-0400-00
PharmGKB
http://www.pharmgkb.org/drug/PA451952
Wikipedia
http://en.wikipedia.org/wiki/Zaleplon
RxList
http://www.rxlist.com/cgi/generic3/zaleplon.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/son1537.shtml
Drugs.com
http://www.drugs.com/cdi/zaleplon.html
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