Tìm theo
Apomorphine
Các tên gọi khác (7 ) :
  • (-)-10,11-Dihydroxyaporphine
  • (−)-10,11-dihydroxyaporphine
  • (6AR)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol
  • (R)-5,6,6a,7-Tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol
  • Apomorphin
  • R-(-)-Apomorphine
  • R-(−)-apomorphine
Thuốc chống Parkinson
Thuốc Gốc
Small Molecule
CAS: 41372-20-7
ĐG : Ipsen Pharmaceuticals Inc. , http://www.ipsen.com
CTHH: C17H17NO2
PTK: 267.3224
A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H17NO2
Phân tử khối
267.3224
Monoisotopic mass
267.125928793
InChI
InChI=1S/C17H17NO2/c1-18-8-7-10-3-2-4-12-15(10)13(18)9-11-5-6-14(19)17(20)16(11)12/h2-6,13,19-20H,7-9H2,1H3/t13-/m1/s1
InChI Key
InChIKey=VMWNQDUVQKEIOC-CYBMUJFWSA-N
IUPAC Name
(9R)-10-methyl-10-azatetracyclo[7.7.1.0^{2,7}.0^{13,17}]heptadeca-1(16),2(7),3,5,13(17),14-hexaene-3,4-diol
Traditional IUPAC Name
apomorphine
SMILES
[H][C@]12CC3=C(C(O)=C(O)C=C3)C3=CC=CC(CCN1C)=C23
Độ hòa tan
1.66E+004 mg/L
logP
3.1
logS
-2.7
pKa (strongest acidic)
6.58
pKa (Strongest Basic)
13.25
PSA
43.7 Å2
Refractivity
79.99 m3·mol-1
Polarizability
29.7 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.92
Dược Lực Học : Apomorphine is a type of dopaminergic agonist, a morphine derivative which primarily affects the hypothalamic region of the brain. Drugs containing this substance are sometimes used in the treatment of Parkinson's disease or erectile dysfunction. In higher doses it is a highly effective emetic.
Cơ Chế Tác Dụng : A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. [PubChem] The precise mechanism of action of apomorphine as a treatment for Parkinson's disease is unknown, although it is believed to be due to stimulation of post-synaptic dopamine D2-type receptors within the brain. Apomorphine has been shown to improve motor function in an animal model of Parkinson's disease. In particular, apomorphine attenuates the motor deficits induced by lesions in the ascending nigrostriatal dopaminergic pathway with the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in primates.
Dược Động Học :
▧ Absorption :
100% following subcutaneous administration
▧ Volume of Distribution :
* 123 to 404 L
▧ Protein binding :
~50%-albumin
▧ Metabolism :
Hepatic
▧ Half Life :
40 minutes (range 30 - 60 minutes)
▧ Clearance :
* 223 L/hr
Độc Tính : LD50=0.6 mmoles/kg (mice, intraperitoneal)
Chỉ Định : For the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing off and unpredictable on/off episodes) associated with advanced Parkinson's disease.
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Entacapone Entacapone increases the effect and toxicity of the sympathomimetic, apomorphine.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Paliperidone The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, apomorphine. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Thiothixene may also antagonize the effects of the anti-Parkinsonian agent, Apomorphine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or doses changed.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). Antagonism may also occur between zuclopenthixol, a dopamine D2 receptor antagonist, and apomorphine, a dopamine agonist. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of both agents if concurrent therapy is initiated, discontinued or dose(s) changed.
Liều Lượng & Cách Dùng : Solution - Subcutaneous
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Mylan
    Sản phẩm biệt dược : Apokyn
  • Sản phẩm biệt dược : Ixense
  • Công ty :
    Sản phẩm biệt dược : Spontane
  • Sản phẩm biệt dược : Uprima
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00714
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6005
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508653
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07460
ChemSpider
http://www.chemspider.com/Chemical-Structure.5783.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/15054-0211-5
PharmGKB
http://www.pharmgkb.org/drug/PA164781163
Wikipedia
http://en.wikipedia.org/wiki/Apomorphine
RxList
http://www.rxlist.com/cgi/generic3/apokyn.htm
Drugs.com
http://www.drugs.com/cdi/apomorphine.html
... loading
... loading