Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
269.164045633
InChI
InChI=1S/C15H19N5/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3
InChI Key
InChIKey=ULFRLSNUDGIQQP-UHFFFAOYSA-N
IUPAC Name
dimethyl({2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethyl})amine
Traditional IUPAC Name
rizatriptan
SMILES
CN(C)CCC1=CNC2=C1C=C(CN1C=NC=N1)C=C2
Độ hòa tan
42 mg/mL (for free base)
pKa (strongest acidic)
17.24
pKa (Strongest Basic)
9.56
Refractivity
93.13 m3·mol-1
Dược Lực Học :
Rizatriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists and has 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 Rizatriptan 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 Rizatriptan in humans.
Cơ Chế Tác Dụng :
Rizatriptan is a triptan drug used for the treatment of migraine headaches. It is a selective 5-hydroxytryptamine1 receptor subtype agonist.
Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.
Dược Động Học :
▧ Absorption :
Rapid following oral administration. Bioavailability is 45%. Food has no effect on the bioavailability of rizatriptan. However, administering rizatriptan with food will delay by 1 hour the time to reach peak plasma concentration. The rate of absorption is not affected by the presence of a migraine attack.
▧ Volume of Distribution :
* 140 L [male]
* 110 L [female]
▧ Protein binding :
14%
▧ Metabolism :
Rizatriptan is metabolized by monoamine oxidase A isoenzyme (MAO-A) to an inactive indole acetic acid metabolite. In addition, several other inactive metabolites are formed. An active metabolite, N-monodesmethyl-rizatriptan, with pharmacological activity similar to that of the parent compound has been identified in small concentrations (14%) in the plasma.
▧ Route of Elimination :
Approximately 14% of an oral dose is excreted in urine as unchanged rizatriptan while 51% is excreted as indole acetic acid metabolite, indicating substantial first pass metabolism.
▧ Half Life :
2-3 hours
Độc Tính :
Symptoms of overdose include dizziness, fainting, heart and blood vessel problems, high blood pressure, loss of bowel and bladder control, slow heartbeat, and vomiting.
Chỉ Định :
For treatment of acute migraine attacks with or without aura.
Tương Tác Thuốc :
-
Citalopram
Increased risk of CNS adverse effects
-
Desvenlafaxine
Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
-
Dihydroergotamine
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, rizatriptan. Concomitant therapy is contraindicated.
-
Methysergide
Possible severe and prolonged vasoconstriction
-
Moclobemide
The MAO inhibitor, moclobemide, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, rizatriptan. Concomitant therapy is contraindicated.
-
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, rizatriptan. Concomitant therapy is contraindicated.
-
Propranolol
Propranolol increases the effect and toxicity of rizatriptan
-
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, Rizatriptan. Risk of serotonin syndrome and Rizatriptan 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.
-
Zolmitriptan
Concomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and rizatriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
Liều Lượng & Cách Dùng :
Tablet - Oral
Wafer - Oral
Dữ Kiện Thương Mại
Giá thị trường
-
Giá bán buôn : USD >22.98
Đơn vị tính : tablet
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Giá bán buôn : USD >25.31
Đơn vị tính : tablet
-
Giá bán buôn : USD >26.7
Đơn vị tính : tablet
-
Giá bán buôn : USD >26.7
Đơn vị tính : tablet
-
Giá bán buôn : USD >83.32
Đơn vị tính : box
-
Giá bán buôn : USD >107.44
Đơn vị tính : box
-
Giá bán buôn : USD >203.46
Đơn vị tính : box
-
Giá bán buôn : USD >286.96
Đơn vị tính : box
-
Giá bán buôn : USD >333.27
Đơn vị tính : box
-
Giá bán buôn : USD >333.27
Đơn vị tính : box
Nhà Sản Xuất
-
Sản phẩm biệt dược : Maxalt
-
Sản phẩm biệt dược : Maxalt MLT
-
Sản phẩm biệt dược : Maxalt-MLT
Tài Liệu Tham Khảo Thêm
National Drug Code Directory