Tìm theo
Prednisolone
Các tên gọi khác (15 ) :
  • (11beta)-11,17,21-Trihydroxypregna-1,4-diene-3,20-dione
  • 1,4-Pregnadiene-11beta,17alpha,21-triol-3,20-dione
  • 1,4-Pregnadiene-3,20-dione-11beta,17alpha,21-triol
  • 3,20-dioxo-11beta,17alpha,21-Trihydroxy-1,4-pregnadiene
  • delta-dehydrocortisol
  • delta-dehydrohydrocortisone
  • delta-hydrocortisone
  • delta(1)-Dehydrocortisol
  • delta(1)-Dehydrohydrocortisone
  • delta(1)-Hydrocortisone
  • Hydroretrocortine
  • Metacortandralone
  • PRDL
  • Prednisolona
  • Prednisolonum
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 50-24-8
ATC: A07EA01, C05AA04, D07AA01, D07AA03, D07AC14, D07XA02, D10AA02, H02AB04, H02AB06, R01AD02, S01BA04, S01CB02, S02BA03, S03BA02
ĐG : Adamis Laboratories , http://www.adamispharmaceuticals.com
CTHH: C21H28O5
PTK: 360.444
A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
360.444
Monoisotopic mass
360.193674006
InChI
InChI=1S/C21H28O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h5,7,9,14-16,18,22,24,26H,3-4,6,8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1
InChI Key
InChIKey=OIGNJSKKLXVSLS-VWUMJDOOSA-N
IUPAC Name
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
Traditional IUPAC Name
prednisolone
Độ tan chảy
235 °C
Độ hòa tan
223 mg/L (at 25 °C)
logP
1.62
logS
-3.21
pKa (strongest acidic)
12.58
pKa (Strongest Basic)
-2.9
PSA
94.83 Å2
Refractivity
98.49 m3·mol-1
Polarizability
38.78 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 : Prednisolone is a synthetic glucocorticoid used as antiinflammatory or immunosuppressive agent. Prednisolone is indicated in the treatment of various conditions, including congenital adrenal hyperplasia, psoriatic arthritis, systemic lupus erythematosus, bullous dermatitis herpetiformis, seasonal or perennial allergic rhinitis, allergic corneal marginal ulcers, symptomatic sarcoidosis, idiopathic thrombocytopenic purpura in adults, leukemias and lymphomas in adults, and ulcerative colitis. Glucocorticoids are adrenocortical steroids and cause profound and varied metabolic effects. In addition, they modify the body's immune responses to diverse stimuli.
Cơ Chế Tác Dụng : A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states. [PubChem] Glucocorticoids such as Prednisolone can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of glucocorticoids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Prednisolone reduces inflammatory reaction by limiting the capillary dilatation and permeability of the vascular structures. These compounds restrict the accumulation of polymorphonuclear leukocytes and macrophages and reduce the release of vasoactive kinins. Recent research suggests that corticosteroids may inhibit the release of arachidonic acid from phospholipids, thereby reducing the formation of prostaglandins. Prednisolone is a glucocorticoid receptor agonist. On binding, the corticoreceptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing an increase or decrease in expression of specific target genes, including suppression of IL2 (interleukin 2) expression.
Dược Động Học :
▧ Absorption :
Readily absorbed by gastrointestinal tract, peak plasma concentration is reached 1-2 hours after administration.
▧ Protein binding :
Very high (>90%)
▧ Metabolism :
Excreted in the urine as either free or glucoconjugate.
▧ Half Life :
2-3 hours
Độc Tính : LD50=500 mg/kg (oral, rat), short-term side effects include high blood glucose levels and fluid retention. Long term side effects include Cushing's syndrome, weight gain, osteoporosis, glaucoma, type II diabetes and adrenal suppression.
Chỉ Định : For the treatment of primary or secondary adrenocortical insufficiency, such as congenital adrenal hyperplasia, thyroiditis. Also used to treat psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, bursitis, acute gouty arthritis and epicondylitis. Also indicated for treatment of systemic lupus erythematosus, pemphigus and acute rhematic carditis. Can be used in the treatment of leukemias, lymphomas, thrombocytopenia purpura and autoimmune hemolytic anemia. Can be used to treat celiac disease, insulin resistance, ulcerative colitis and liver disorders.
Tương Tác Thuốc :
  • Acenocoumarol The corticosteroid, prednisolone, alters the anticoagulant effect, acenocoumarol.
  • Acetylsalicylic acid The corticosteroid, prednisolone, may decrease the effect of the salicylate, acetylsalicylic acid.
  • Ambenonium The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, ambenonium.
  • Amobarbital The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Anisindione The corticosteroid, prednisolone, alters the anticoagulant effect of anisindione.
  • Aprobarbital The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Bismuth Subsalicylate The corticosteroid, prednisolone, may decrease the effect of the salicylate, bismuth subsalicylate.
  • Butabarbital The barbiturate, butabarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Butalbital The barbiturate, butalbital, may decrease the effect of the corticosteroid, prednisolone.
  • Butethal The barbiturate, butethal, may decrease the effect of the corticosteroid, prednisolone.
  • Chlorotrianisene The estrogenic agent, chlorotrianisene, may increase the effect of the corticosteroid, prednisolone.
  • Clomifene The estrogenic agent, clomifene, may increase the effect of the corticosteroid, prednisolone.
  • Conjugated Estrogens The estrogenic agent may increase the effect of the corticosteroid, prednisolone.
  • Dicoumarol The corticosteroid, prednisolone, alters the anticoagulant effect of dicumarol.
  • Diethylstilbestrol The estrogenic agent, diethylstilbestrol, may increase the effect of the corticosteroid, prednisolone.
  • Dihydroquinidine barbiturate The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, prednisolone.
  • Edrophonium The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, edrophonium.
  • Estradiol The estrogenic agent, estradiol, may increase the effect of the corticosteroid, prednisolone.
  • Estriol The estrogenic agent, estriol, may increase the effect of the corticosteroid, prednisolone.
  • Estrone The estrogenic agent, estrone, may increase the effect of the corticosteroid, prednisolone.
  • Estropipate The estrogenic agent, estropipate, may increase the effect of the corticosteroid, prednisolone.
  • Ethinyl Estradiol The estrogenic agent, ethinyl estradiol, may increase the effect of the corticosteroid, prednisolone.
  • Ethotoin The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, prednisolone.
  • Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, prednisolone.
  • Heptabarbital The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Hexobarbital The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Itraconazole The imidazole, itraconazole, may increase the effect and toxicity of the corticosteroid, prednisolone.
  • Ketoconazole The imidazole, ketoconazole, may increase the effect and toxicity of the corticosteroid, prednisolone.
  • Magnesium salicylate The corticosteroid, prednisolone, may decrease the effect of magnesium salicylate.
  • Mephenytoin The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, prednisolone.
  • Mestranol The estrogenic agent, mestranol, may increase the effect of the corticosteroid, prednisolone.
  • Methohexital The barbiturate, methohexital, may decrease the effect of the corticosteroid, prednisolone.
  • Methylphenobarbital The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Midodrine Increased arterial pressure
  • Neostigmine The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, neostigmine.
  • Pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Phenobarbital The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Phenytoin The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, prednisolone.
  • Primidone The barbiturate, primidone, may decrease the effect of the corticosteroid, prednisolone.
  • Pyridostigmine The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, pyridostigmine.
  • Quinestrol The estrogenic agent, quinestrol, may increase the effect of the corticosteroid, prednisolone.
  • Quinidine barbiturate The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, prednisolone.
  • Rifampicin The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, prednisolone.
  • Salicylate-sodium The corticosteroid, prednisolone, may decrease the effect of the salicylate, salicylate-sodium.
  • Salsalate The corticosteroid, prednisolone, may decrease the effect of the salicylate, salsalate.
  • Secobarbital The barbiturate, secobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Tacrine Tacrine and Prednisolone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
  • Talbutal The barbiturate, talbutal, may decrease the effect of the corticosteroid, prednisolone.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
  • Trisalicylate-choline The corticosteroid, prednisolone, may decrease the effect of the salicylate, trisalicylate-choline.
  • Vecuronium Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Prednisolone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
  • Warfarin The corticosteroid, prednisolone, alters the anticoagulant effect of warfarin.
Liều Lượng & Cách Dùng : Liquid - Oral
Solution - Oral
Solution / drops - Ophthalmic
Suspension - Ophthalmic
Tablet - Oral
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