Tìm theo
Almotriptan
Các tên gọi khác (1) :
  • 1-(((3-(2-(Dimethylamino)ethyl)indol-5-yl)methyl)sulfonyl)pyrrolidine
serotonin antagonists, serotonin receptor agonists, anti migraine agents
Thuốc Gốc
Small Molecule
CAS: 181183-52-8
ATC: N02CC05
ĐG : Janssen-Ortho Inc. , http://www.janssen-ortho.com
CTHH: C17H25N3O2S
PTK: 335.464
Almotriptan is a triptan drug for the treatment of migraine headaches. Almotriptan is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and stopping the release of certain natural substances that cause pain, nausea, and other symptoms of migraine. Almotriptan does not prevent migraine attacks.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H25N3O2S
Phân tử khối
335.464
Monoisotopic mass
335.166747749
InChI
InChI=1S/C17H25N3O2S/c1-19(2)10-7-15-12-18-17-6-5-14(11-16(15)17)13-23(21,22)20-8-3-4-9-20/h5-6,11-12,18H,3-4,7-10,13H2,1-2H3
InChI Key
InChIKey=WKEMJKQOLOHJLZ-UHFFFAOYSA-N
IUPAC Name
dimethyl(2-{5-[(pyrrolidine-1-sulfonyl)methyl]-1H-indol-3-yl}ethyl)amine
Traditional IUPAC Name
almotriptan
SMILES
CN(C)CCC1=CNC2=C1C=C(CS(=O)(=O)N1CCCC1)C=C2
Độ hòa tan
1.21e-01 g/l
logP
1.6
logS
-3.4
pKa (strongest acidic)
17.14
pKa (Strongest Basic)
9.55
PSA
56.41 Å2
Refractivity
94.52 m3·mol-1
Polarizability
37.01 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT1D family) having only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almotriptan also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Almotriptan in humans.
Cơ Chế Tác Dụng : Almotriptan is a triptan drug for the treatment of migraine headaches. Almotriptan is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and stopping the release of certain natural substances that cause pain, nausea, and other symptoms of migraine. Almotriptan does not prevent migraine attacks. Almotriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction.
Dược Động Học :

▧ Volume of Distribution :
* 180 to 200 L
▧ Protein binding :
35%
▧ Route of Elimination :
Almotriptan is eliminated primarily by renal excretion (about 75% of the oral dose), with approximately 40% of an administered dose excreted unchanged in urine. Approximately 13% of the administered dose is excreted via feces, both unchanged and metabolized.
▧ Half Life :
3-4 hours
▧ Clearance :
* 57 L/h [healthy] * 34.2 L/h [moderate renal impairment (creatinine clearance between 31 and 71 mL/min)] * 9.8 L/h [severe renal impairment (creatinine clearance between 10 and 30 mL/min)]
Chỉ Định : For the treatment of acute migraine headache in adults
Tương Tác Thuốc :
  • Citalopram Increased risk of CNS adverse effects
  • Conivaptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Almotriptan. Use an initial almotriptan dose of 6.25mg when using almotriptan with a strong CYP3A4 inhibitor, and do not exceed 12.5mg of almotriptan in any 24-hour period. Avoid concurrent use of almotriptan with a strong CYP3A4 inhibitor in patients with impaired hepatic or renal function.
  • Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Dihydroergotamine Possible severe and prolonged vasoconstriction
  • Ergonovine Possible severe and prolonged vasoconstriction
  • Ergotamine Possible severe and prolonged vasoconstriction
  • Escitalopram Increased risk of CNS adverse effects
  • Fluoxetine Increased risk of CNS adverse effects
  • Fluvoxamine Increased risk of CNS adverse effects
  • Isocarboxazid The MAO inhibitor, isocarboxazid, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, almotriptan. Concomitant therapy is contraindicated.
  • Itraconazole This potent CYP3A4 inhibitor increases the effect and toxicity of the triptan
  • Ketoconazole This potent CYP3A4 inhibitor increases the effect and toxicity of the triptan
  • Methylergometrine Possible severe and prolonged vasoconstriction
  • Methysergide Possible severe and prolonged vasoconstriction
  • Nefazodone Increased risk of CNS adverse effects
  • Paroxetine Increased risk of CNS adverse effects
  • Phenelzine The MAO inhibitor, phenelzine, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, almotriptan. Concomitant therapy is contraindicated.
  • Sertraline Increased risk of CNS adverse effects
  • Sibutramine Increased risk of CNS adverse effects
  • Tramadol Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Tranylcypromine The MAO inhibitor, Tranylcypromine, may reduce the metabolism and clearance of the serotonin 5-HT1D receptor agonist, Almotriptan. Risk of serotonin syndrome and Almotriptan toxicity. 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.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of almotriptan by decreasing its metabolism. The initial and maximum doses should not exceed 6.25 mg and 12.5 mg, respectively during concomitant therapy. Concomitant therapy should be avoided in patients with impaired hepatic or renal function.
  • Zolmitriptan Concomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and almotriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Almogran
  • Công ty :
    Sản phẩm biệt dược : Axert
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00918
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=123606
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505165
ChemSpider
http://www.chemspider.com/Chemical-Structure.110198.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0062-2080-06
PharmGKB
http://www.pharmgkb.org/drug/PA10246
Wikipedia
http://en.wikipedia.org/wiki/Almotriptan
RxList
http://www.rxlist.com/cgi/generic2/almotriptan.htm
Drugs.com
http://www.drugs.com/cdi/almotriptan.html
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