Tìm theo
Methylprednisolone
Các tên gọi khác (15 ) :
  • (6alpha,11beta)-11,17,21-Trihydroxy-6-methylpregna-1,4-diene-3,20-dione
  • (6α,11β)-11,17,21-trihydroxy-6-methylpregna-1,4-diene-3,20-dione
  • 1-dehydro-6alpha-Methylhydrocortisone
  • 1-dehydro-6α-methylhydrocortisone
  • 6alpha-Methyl-11beta,17alpha,21-triol-1,4-pregnadiene-3,20-dione
  • delta(1)-6alpha-Methylhydrocortisone
  • Medrate
  • Medrol
  • Medrone
  • Methylprednisolon
  • Methylprednisolone
  • Methylprednisolonum
  • Metilprednisolona
  • Solomet
  • Urbason
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 83-43-2
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C22H30O5
PTK: 374.4706
A prednisolone derivative with similar anti-inflammatory action. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H30O5
Phân tử khối
374.4706
Monoisotopic mass
374.20932407
InChI
InChI=1S/C22H30O5/c1-12-8-14-15-5-7-22(27,18(26)11-23)21(15,3)10-17(25)19(14)20(2)6-4-13(24)9-16(12)20/h4,6,9,12,14-15,17,19,23,25,27H,5,7-8,10-11H2,1-3H3/t12-,14-,15-,17-,19+,20-,21-,22-/m0/s1
InChI Key
InChIKey=VHRSUDSXCMQTMA-PJHHCJLFSA-N
IUPAC Name
(1S,2R,8S,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,8,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
Traditional IUPAC Name
methylprednisolone
SMILES
[H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])C[C@H](C)C2=CC(=O)C=C[C@]12C
Độ tan chảy
232.5 °C
Độ hòa tan
120 mg/L (at 25 °C)
logP
1.5
logS
-2.99
pKa (strongest acidic)
12.58
pKa (Strongest Basic)
-2.9
PSA
94.83 Å2
Refractivity
103.04 m3·mol-1
Polarizability
40.84 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Methylprednisolone and its derivatives, methylprednisolone sodium succinate and methylprednisolone acetate, are synthetic glucocorticoids used as antiinflammatory or immunosuppressive agents.
Cơ Chế Tác Dụng : A prednisolone derivative with similar anti-inflammatory action. [PubChem] Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
Dược Động Học :
▧ Absorption :
Oral bioavailability 80-99%
▧ Protein binding :
78%
▧ Metabolism :
Hepatic
▧ Half Life :
1-3 hours
Độc Tính : LD50=2000 mg/kg (orally in rat)
Chỉ Định : Adjunctive therapy for short-term administration in rheumatoid arthritis.
Tương Tác Thuốc :
  • Acetylsalicylic acid The corticosteroid, methylprednisolone, may decrease the effect of the salicylate, acetylsalicylic acid.
  • Aprepitant Increases the effect and toxicity of methylprednisolone
  • Clarithromycin The macrolide, clarithromycin, may increase the effect of corticosteroid, methylprednisolone.
  • Conivaptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Methylprednisolone. Consider methylprednisolone dose titration and/or adjustments in patients receiving strong CYP3A4 inhibitors (eg, azole antifungals, protease inhibitors) and monitor for increased steroid related adverse effects.
  • Erythromycin The macrolide, erythromycin, may increase the effect of corticosteroid, methylprednisolone.
  • Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, methylprednisolone.
  • Itraconazole The imidazole, itraconazole, may increase the effect and toxicity of the corticosteroid, methylprednisolone.
  • Ketoconazole The imidazole, ketoconazole, may increase the effect and toxicity of the corticosteroid, methylprednisolone.
  • Midodrine Increased arterial pressure
  • Phenobarbital The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, methylprednisolone.
  • Phenytoin The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, methylprednisolone.
  • Primidone The barbiturate, primidone, may decrease the effect of the corticosteroid, methylprednisolone.
  • Pyridostigmine The corticosteroid, methylprednisolone, may decrease the effect of the anticholinesterase, pyridostigmine.
  • Quinupristin This combination presents an increased risk of toxicity
  • Rifampicin The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, methylprednisolone.
  • Tacrine Tacrine and Methylprednisolone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
  • Tacrolimus Methylprednisone may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Methylprednisone therapy is initiated, discontinued or altered.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
  • Vecuronium Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Methylprednisolone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
Liều Lượng & Cách Dùng : Powder - Intramuscular
Powder - Intravenous
Powder, for solution - Intravenous
Suspension - Intramuscular
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : A-METHAPRED
  • Công ty :
    Sản phẩm biệt dược : Depo-Medrol
  • Công ty :
    Sản phẩm biệt dược : Medrate
  • Công ty :
    Sản phẩm biệt dược : Medrol
  • Công ty :
    Sản phẩm biệt dược : Medrone
  • Công ty :
    Sản phẩm biệt dược : Meprolone
  • Công ty :
    Sản phẩm biệt dược : Solomet
  • Công ty :
    Sản phẩm biệt dược : Solu-Medrol
  • Công ty :
    Sản phẩm biệt dược : Urbason
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00959
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6741
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504885
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00407
ChemSpider
http://www.chemspider.com/Chemical-Structure.6485.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0555-0301-02
PharmGKB
http://www.pharmgkb.org/drug/PA450466
Wikipedia
http://en.wikipedia.org/wiki/Methylprednisolone
RxList
http://www.rxlist.com/cgi/generic/methprd.htm
Drugs.com
http://www.drugs.com/methylprednisolone.html
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