Tìm theo
Buspirone
Các tên gọi khác (5 ) :
  • 8-(4-(4-(2-Pyrimidinyl)-1-piperizinyl)butyl)-8-azaspiro(4,5)decane-7,9-dione
  • Buspiron
  • Buspirona
  • Buspirone
  • Buspironum
Thuốc chống lo âu, hoảng sợ
Thuốc Gốc
Small Molecule
CAS: 36505-84-7
ATC: N05BE01
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C21H31N5O2
PTK: 385.5031
An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H31N5O2
Phân tử khối
385.5031
Monoisotopic mass
385.247775261
InChI
InChI=1S/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2
InChI Key
InChIKey=QWCRAEMEVRGPNT-UHFFFAOYSA-N
IUPAC Name
8-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione
Traditional IUPAC Name
buspirone
SMILES
O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)C1=NC=CC=N1
Độ tan chảy
201.5-202.5 °C
Độ hòa tan
21.4 mg/L
logP
2.63
logS
-2.8
pKa (Strongest Basic)
7.62
PSA
69.64 Å2
Refractivity
108.89 m3·mol-1
Polarizability
44.12 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
6
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.
Cơ Chế Tác Dụng : An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam. [PubChem] Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced.
Dược Động Học :
▧ Absorption :
Rapidly absorbed in man. Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism.
▧ Protein binding :
95% (approximately 70% bound to albumin, 30% bound to alpha 1 -acid glycoprotein)
▧ Metabolism :
Metabolized hepatically, primarily by oxidation by cytochrome P450 3A4 producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP)
▧ Route of Elimination :
In a single-dose study using 14C-labeled buspirone, 29% to 63% of the dose was excreted in the urine within 24 hours, primarily as metabolites; fecal excretion accounted for 18% to 38% of the dose.
▧ Half Life :
2-3 hours (although the action of a single dose is much longer than the short halflife indicates).
Độc Tính : Oral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.
Chỉ Định : For the management of anxiety disorders or the short-term relief of the symptoms of anxiety, and also as an augmention of SSRI-treatment against depression.
Tương Tác Thuốc :
  • Clarithromycin Clarithromycin may increase the effect and toxicity of buspirone.
  • Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Diltiazem The calcium channel blocker, diltiazem, increases the effect and toxicity of buspirone.
  • Erythromycin The macrolide, erythromycin, may increase the effect and toxicity of buspirone.
  • Isocarboxazid Possible blood pressure elevation
  • Josamycin The macrolide, josamycin, may increase the effect and toxicity of buspirone.
  • Nefazodone Nefazodone increases the effect of buspirone
  • Phenelzine Possible blood pressure elevation
  • Rasagiline Possible blood pressure elevation
  • Rifabutin Rifabutin decreases the effect of buspirone
  • Rifampicin Rifampin decreases the effect of buspirone
  • Ritonavir Ritonavir increases the effect and toxicity of buspirone
  • Telithromycin Telithromycin may reduce clearance of Buspirone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Buspirone if Telithromycin is initiated, discontinued or dose changed.
  • Tranylcypromine Buspirone may increase the adverse effects of Tranylcypromine. Elevation of blood pressure may occur. Concomitant therapy also may increase the risk of serotonin syndrome. Concomitant therapy should be avoided.
  • Trazodone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trimipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Venlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Verapamil Verapamil may increase the serum concentration of Buspirone. The likely occurs via Verapamil-mediated CYP3A4 inhibition resulting in decreased Buspirone metabolism. Monitor for changes in the therapeutic/adverse effects of Buspirone if Verpamil is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole may increase the serum concentration of buspirone likely by decreasing its metabolism via CYP3A4. Monitor for changes in the therapeutic and adverse effects of buspirone if voriconazole is initiated, discontinued or dose changed.
  • Zolmitriptan Use of two serotonin modulators, such as zolmitriptan and buspirone, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Rontag
    Sản phẩm biệt dược : Ansial
  • Công ty : Valeant
    Sản phẩm biệt dược : Anxiron
  • Công ty : Eisai
    Sản phẩm biệt dược : Anxut
  • Công ty :
    Sản phẩm biệt dược : Bespar
  • Công ty : Wockhardt
    Sản phẩm biệt dược : Buscalm
  • Công ty : Hexal
    Sản phẩm biệt dược : Busp
  • Sản phẩm biệt dược : Buspar
  • Công ty : Deva
    Sản phẩm biệt dược : Buspon
  • Công ty : Biotech
    Sản phẩm biệt dược : Dalpas
  • Công ty : Coup
    Sản phẩm biệt dược : Epsilat
  • Công ty : Aspen Pharmacare
    Sản phẩm biệt dược : Pasrin
  • Công ty : Anpharm
    Sản phẩm biệt dược : Spamilan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00490
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2477
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508113
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06861
ChemSpider
http://www.chemspider.com/Chemical-Structure.2383.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-1140-01
PharmGKB
http://www.pharmgkb.org/drug/PA448689
Wikipedia
http://en.wikipedia.org/wiki/Buspirone
RxList
http://www.rxlist.com/cgi/generic/buspir.htm
Drugs.com
http://www.drugs.com/buspirone.html
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