Tìm theo
Selegiline
Các tên gọi khác (4 ) :
  • (−)-selegiline
  • L-Deprenalin
  • Selegilina
  • Selegilinum
Thuốc chống Parkinson
Thuốc Gốc
Small Molecule
CAS: 14611-51-9
ATC: N04BD01
ĐG : Alphapharm Party Ltd. , http://www.alphapharm.com.au
CTHH: C13H17N
PTK: 187.2808
A selective, irreversible inhibitor of Type B monoamine oxidase. It is used in newly diagnosed patients with Parkinson's disease. It may slow progression of the clinical disease and delay the requirement for levodopa therapy. It also may be given with levodopa upon onset of disability. (From AMA Drug Evaluations Annual, 1994, p385) The compound without isomeric designation is Deprenyl. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H17N
Phân tử khối
187.2808
Monoisotopic mass
187.136099549
InChI
InChI=1S/C13H17N/c1-4-10-14(3)12(2)11-13-8-6-5-7-9-13/h1,5-9,12H,10-11H2,2-3H3
InChI Key
InChIKey=MEZLKOACVSPNER-UHFFFAOYSA-N
IUPAC Name
methyl(1-phenylpropan-2-yl)(prop-2-yn-1-yl)amine
Traditional IUPAC Name
methyl(1-phenylpropan-2-yl)prop-2-yn-1-ylamine
SMILES
CC(CC1=CC=CC=C1)N(C)CC#C
Độ tan chảy
141-142 °C
Độ hòa tan
2.54e-02 g/l
logP
2.7
logS
-3.9
pKa (Strongest Basic)
8.67
PSA
3.24 Å2
Refractivity
61.35 m3·mol-1
Polarizability
22.48 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Dopamine is an essential chemical that occurs in many parts of the body. It is the premature degradation of dopamine that results in the symptoms of Parkinson's disease. Monoamine oxidase (MAO) is an enzyme which accelerates the breakdown of dopamine. Selegiline can prolong the effects of dopamine in the brain by preventing its breakdown through seletively blocking MAO-B. It also may prevent the removal of dopamine between nerve endings and enhance release of dopamine from nerve cells.
Cơ Chế Tác Dụng : A selective, irreversible inhibitor of Type B monoamine oxidase. It is used in newly diagnosed patients with Parkinson's disease. It may slow progression of the clinical disease and delay the requirement for levodopa therapy. It also may be given with levodopa upon onset of disability. (From AMA Drug Evaluations Annual, 1994, p385) The compound without isomeric designation is Deprenyl. [PubChem] Although the mechanisms for selegiline's beneficial action in the treatment of Parkinson's disease are not fully understood, the selective, irreversible inhibition of monoamine oxidase type B (MAO-B) is thought to be of primary importance. MAO-B is involved in the oxidative deamination of dopamine in the brain. Selegiline binds to MAO-B within the nigrostriatal pathways in the central nervous system, thus blocking microsomal metabolism of dopamine and enhancing the dopaminergic activity in the substantial nigra. Selegiline may also increase dopaminergic activity through mechanisms other than inhibition of MAO-B. At higher doses, selegiline can also inhibit monozmine oxidase type A (MAO-A), allowing it to be used for the treatment of depression.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from the gastrointestinal tract.
▧ Protein binding :
> 99.5%
▧ Half Life :
1.2-2 hours
Độc Tính : LD50=63 mg/kg (rats, IV)
Chỉ Định : Monotherapy for initial treatment of Parkinson's disease, as well as an adjunct therapy in patients with a decreased response to levodopa/carbadopa. Also used for the palliative treatment of mild to moderate Alzheimer's disease and at higher doses, for the treatment of depression.
Tương Tác Thuốc :
  • Bezafibrate MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like selegiline.
  • Brimonidine MAO Inhibitors like selegiline may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
  • Buprenorphine Buprenorphine may enhance the adverse/toxic effect of MAO Inhibitors like selegiline. When possible, avoid use of buprenorphine in patients who have used a monoamine oxidase inhibitor within the past 14 days due to possible severe adverse effects.
  • Citalopram Possible severe adverse reaction with this combination
  • Desvenlafaxine Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Concurrent therapy should be avoided.
  • Dextromethorphan Combination associated with possible serotoninergic syndrome
  • Escitalopram Possible severe adverse reaction with this combination
  • Fluoxetine Possible severe adverse reaction with this combination
  • Fluvoxamine Possible severe adverse reaction with this combination
  • Moclobemide Decrease in selectivity
  • Paroxetine Possible severe adverse reaction with this combination
  • Pethidine Potentially fatal adverse effects
  • Tapentadol Increases the toxicity of tapentadol by unknown mechanism. Discontinue selegiline at least 14 days prior to tapentadol administration.
  • Tetrabenazine Tetrabenazine may increase the adverse/toxic effects of Selegiline. Concomitant therapy is contraindicated.
  • Thiotepa Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Selegiline, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Selegiline if Thiotepa is initiated, discontinued or dose changed.
  • Tolcapone Tolcapone and Selegiline decrease the metabolism of endogenous catecholamines. Concomitant therapy may result in increased catecholamine effects. Consider alternate therapy or use cautiously and monitor for increased catecholamine effects.
  • Tramadol Tramadol increases the risk of serotonin syndrome and seizure induction by the MAO inhibitor, Selegiline.
  • Tranylcypromine Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome.
  • Trazodone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trimipramine Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Avoid combination or monitor for symptoms of serotonin syndrome and/or hypertensive crisis.
  • Venlafaxine Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Concurrent therapy should be avoided.
  • Vilazodone MAO Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Avoid combination.
  • Zolmitriptan The MAO inhibitor, selegiline, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing selegiline are contraindicated.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Carbex
  • Công ty :
    Sản phẩm biệt dược : Eldepryl
  • Công ty :
    Sản phẩm biệt dược : EmSam
  • Công ty :
    Sản phẩm biệt dược : Jumex
  • Công ty :
    Sản phẩm biệt dược : Zelapar
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01037
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07245
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03731
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=15579
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-9290-91
PharmGKB
http://www.pharmgkb.org/drug/PA451316
Wikipedia
http://en.wikipedia.org/wiki/Selegiline
RxList
http://www.rxlist.com/cgi/generic/seleg.htm
Drugs.com
http://www.drugs.com/cdi/selegiline.html
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