Tìm theo
Zolmitriptan
Các tên gọi khác (6 ) :
  • (S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one
  • 311C90
  • 4-[[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]methyl]oxazolidin-2-one
  • Zolmitriptan
  • Zolmitriptanum
  • Zomig
serotonin antagonists, serotonin 5 ht1 receptor agonists, serotonin receptor agonists, anti migraine ag
Thuốc Gốc
Small Molecule
CAS: 139264-17-8
ATC: N02CC03
ĐG : AstraZeneca Inc. , http://www.astrazeneca.ca
CTHH: C16H21N3O2
PTK: 287.3568
Zolmitriptan is a synthetic tryptamine derivative and appears as a white powder that is readily soluble in water. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H21N3O2
Phân tử khối
287.3568
Monoisotopic mass
287.163376931
InChI
InChI=1S/C16H21N3O2/c1-19(2)6-5-12-9-17-15-4-3-11(8-14(12)15)7-13-10-21-16(20)18-13/h3-4,8-9,13,17H,5-7,10H2,1-2H3,(H,18,20)/t13-/m0/s1
InChI Key
InChIKey=ULSDMUVEXKOYBU-ZDUSSCGKSA-N
IUPAC Name
(4S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one
Traditional IUPAC Name
zolmitriptan
SMILES
CN(C)CCC1=CNC2=CC=C(C[C@H]3COC(=O)N3)C=C12
Độ hòa tan
1.90e-01 g/l
logP
1.6
logS
-3.2
pKa (strongest acidic)
13
pKa (Strongest Basic)
9.55
PSA
57.36 Å2
Refractivity
82.44 m3·mol-1
Polarizability
31.65 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Zolmitriptan 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 Zolmitriptan 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 Zolmitriptan in humans.
Cơ Chế Tác Dụng : Zolmitriptan is a synthetic tryptamine derivative and appears as a white powder that is readily soluble in water. [Wikipedia] Zolmitriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
Dược Động Học :
▧ Absorption :
Mean absolute oral bioavailability is approximately 40%. Food has no affect on the rate and extent of absorption.
▧ Volume of Distribution :
* 8.4±3.3 L/kg
▧ Protein binding :
25%
▧ Metabolism :
Hepatic. There have been three metabolites identified: indole acetic acid, N -oxide, and N-desmethyl metabolites. However, the N-desmethyl is the only active metabolite.
▧ Half Life :
The mean elimination half-life of zolmitriptan and of the active N-desmethyl metabolite is 3 hours.
▧ Clearance :
* 25.9 mL/min/kg
Chỉ Định : For the acute treatment of adult migraine with or without auras.
Tương Tác Thuốc :
  • Almotriptan 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.
  • Amitriptyline Use of two serotonin modulators, such as zolmitriptan and amitriptyline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Amoxapine Use of two serotonin modulators, such as zolmitriptan and amoxapine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Bromocriptine Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, bromocriptine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. Use of two serotonin modulators, such as zolmitriptan and bromocriptine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Buspirone 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.
  • Cabergoline Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, carbergoline, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. Use of two serotonin modulators, such as zolmitriptan and carbergoline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Citalopram The use of two serotonin modulators, such as zolmitriptan and citalopram, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Clomipramine Use of two serotonin modulators, such as zolmitriptan and clomipramine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • D-Tryptophan Use of two serotonin modulators, such as zolmitriptan and D-tryptophan, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Desipramine Use of two serotonin modulators, such as zolmitriptan and desipramine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Dextromethorphan Use of two serotonin modulators, such as zolmitriptan and dextromethorphan, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Dihydroergotamine Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, dihydroergotamine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Doxepin Use of two serotonin modulators, such as zolmitriptan and doxepin, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Duloxetine Use of two serotonin modulators, such as zolmitriptan and duloxetine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Eletriptan Concomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and eletriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Ergoloid mesylate Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergoloid mesylate, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Ergonovine Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergonovine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Ergotamine Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergotamine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Escitalopram Use of two serotonin modulators, such as zolmitriptan and escitalopram, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Fluoxetine Use of two serotonin modulators, such as zolmitriptan and fluoxetine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Fluvoxamine Use of two serotonin modulators, such as zolmitriptan and fluvoxamine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Frovatriptan Concomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and frovatriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Furazolidone The MAO inhibitor, furazolidine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing furazolidine are contraindicated.
  • Imipramine Use of two serotonin modulators, such as zolmitriptan and imipramine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Isocarboxazid The MAO inhibitor, isocarboxazid, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing isocarboxazid are contraindicated.
  • L-Tryptophan Use of two serotonin modulators, such as zolmitriptan and L-tryptophan, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Linezolid The MAO inhibitor, linezolid, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing linezolid are contraindicated.
  • Lithium Use of two serotonin modulators, such as zolmitriptan and lithium, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Maprotiline Use of two serotonin modulators, such as zolmitriptan and maprotiline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Methylergometrine Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, methylergonovine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Methysergide Possible severe and prolonged vasoconstriction
  • Milnacipran Use of two serotonin modulators, such as zolmitriptan and milnacipran, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Mirtazapine Use of two serotonin modulators, such as zolmitriptan and mirtazapine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Moclobemide The MAO inhibitor, moclobemide, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing moclobemide are contraindicated.
  • Naratriptan Concomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and naratriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Nefazodone Use of two serotonin modulators, such as zolmitriptan and nafazodone, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Nortriptyline Use of two serotonin modulators, such as zolmitriptan and nortriptyline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Paroxetine Use of two serotonin modulators, such as zolmitriptan and paroxetine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Pergolide Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, pergolide, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Pethidine Use of two serotonin modulators, such as zolmitriptan and meperidine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Phenelzine The MAO inhibitor, phenelzine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing phenelzine are contraindicated.
  • Procarbazine The MAO inhibitor, procarbazine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing procarbazine are contraindicated.
  • Promethazine Use of two serotonin modulators, such as zolmitriptan and promethazine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Protriptyline Use of two serotonin modulators, such as zolmitriptan and protriptyline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Rasagiline The MAO inhibitor, rasagiline, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing rasagiline are contraindicated.
  • Rizatriptan 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.
  • S-Adenosylmethionine Use of two serotonin modulators, such as zolmitriptan and S-adenosylmethionine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Selegiline 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.
  • Sertraline Use of two serotonin modulators, such as zolmitriptan and sertraline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Sibutramine Use of sibutramine, which inhibits serotonin reuptake, and zolmitriptan, a serotonin 5-HT1D receptor agonist, may cause serotonin syndrome. Concomitant therapy is contraindicated.
  • St. John's Wort Use of two serotonin modulators, such as zolmitriptan and St. John's Wort, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Sumatriptan Concomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and sumatriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
  • Tapentadol Use of two serotonin modulators, such as zolmitriptan and tapentadol, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Tramadol The use of two serotonin modulators, such as zolmitriptan and tramadol, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Tranylcypromine The MAO inhibitor, tranylcypromine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing tranylcypromine are contraindicated.
  • Trazodone Use of two serotonin modulators, such as zolmitriptan and trazodone, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Trimipramine Use of two serotonin modulators, such as zolmitriptan and trimipramine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
  • Venlafaxine Use of two serotonin modulators, such as zolmitriptan and venlafaxine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
Liều Lượng & Cách Dùng : Spray - Nasal
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : AscoTop
  • Công ty : Square
    Sản phẩm biệt dược : Nomi
  • Công ty : Actavis
    Sản phẩm biệt dược : Zolmiles
  • Công ty :
    Sản phẩm biệt dược : zolmiptriptan
  • Công ty : Beximco
    Sản phẩm biệt dược : Zolmit
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Zomig
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Zomig Rapimelt
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Zomigon
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Zomigoro
  • Công ty : Incepta
    Sản phẩm biệt dược : Zomitan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00315
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07218
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00415
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0310-0208-60
PharmGKB
http://www.pharmgkb.org/drug/PA451975
Wikipedia
http://en.wikipedia.org/wiki/Zolmitriptan
RxList
http://www.rxlist.com/cgi/generic2/zolmit.htm
Drugs.com
http://www.drugs.com/cdi/zolmitriptan.html
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