药品详细
Prednisone(强的松)
化学结构式图
中文名
强的松
英文名
Prednisone
分子式
C21H26O5
化学名
(1S,2R,10S,11S,14R,15S)-14-hydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-diene-5,17-dione
分子量
Average: 358.4281
Monoisotopic: 358.178023942
Monoisotopic: 358.178023942
CAS号
53-03-2
ATC分类
A07E Intestinal Antiinflammatory Agents;H02A 未知;H02A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A synthetic anti-inflammatory glucocorticoid derived from cortisone. It is biologically inert and converted to prednisolone in the liver. [PubChem]
生产厂家
- American therapeutics inc
- Amneal pharmaceuticals ny llc
- Bayer pharmaceuticals corp
- Cadista pharmaceuticals inc
- Cm bundy co
- Contract pharmacal corp
- Duramed pharmaceuticals inc sub barr laboratories inc
- Elkins sinn div ah robins co inc
- Everylife
- Ferndale laboratories inc
- Halsey drug co inc
- Heather drug co inc
- Impax laboratories inc
- Inwood laboratories inc sub forest laboratories inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- John j ferrante
- Kv pharmaceutical co
- L perrigo co
- Lannett co inc
- Lederle laboratories div american cyanamid co
- Marshall pharmacal corp
- Muro pharmaceutical inc
- Mutual pharmaceutical co inc
- Nylos trading co inc
- Panray corp sub ormont drug and chemical co inc
- Parke davis div warner lambert co
- Pharmacia and upjohn co
- Pharmavite pharmaceuticals
- Phoenix laboratories inc
- Private formulations inc
- Purepac pharmaceutical co
- Rexall drug co
- Roxane laboratories inc
- Sandoz inc
- Scherer laboratories inc
- Schering corp sub schering plough corp
- Schwarz pharma inc
- Solvay pharmaceuticals
- Sperti drug products inc
- Superpharm corp
- Teva pharmaceuticals usa inc
- Udl laboratories inc
- Upsher smith laboratories inc
- Valeant pharmaceuticals international
- Vangard laboratories inc div midway medical co
- Vintage pharmaceuticals inc
- Vitarine pharmaceuticals inc
- Watson laboratories inc
- West ward pharmaceutical corp
- Whiteworth towne paulsen inc
- Wockhardt eu operations (swiss) ag
封装厂家
- Advanced Pharmaceutical Services Inc.
- Amend
- Amerisource Health Services Corp.
- Apotheca Inc.
- Apothecary Shop Wholesale
- AQ Pharmaceuticals Inc.
- A-S Medication Solutions LLC
- Breckenridge Pharmaceuticals
- Bryant Ranch Prepack
- C.O. Truxton Inc.
- Cadista Pharmaceuticals Inc.
- Cardinal Health
- Carlisle Laboratories Inc.
- Comprehensive Consultant Services Inc.
- Corepharma LLC
- Darby Dental Supply Co. Inc.
- Dept Health Central Pharmacy
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Innoviant Pharmacy Inc.
- Kaiser Foundation Hospital
- Keltman Pharmaceuticals Inc.
- Lake Erie Medical and Surgical Supply
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Mckesson Corp.
- Merz Pharmaceuticals LLC
- Murfreesboro Pharmaceutical Nursing Supply
- Mutual Pharmaceutical Co.
- Neuman Distributors Inc.
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Perrigo Co.
- Pharmacia Inc.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Prescription Dispensing Service Inc.
- Qualitest
- Rebel Distributors Corp.
- Redpharm Drug
- Remedy Repack
- Resource Optimization and Innovation LLC
- Roxane Labs
- Sandhills Packaging Inc.
- Southwood Pharmaceuticals
- St Mary's Medical Park Pharmacy
- Stat Rx Usa
- Stat Scripts LLC
- Tya Pharmaceuticals
- UDL Laboratories
- Vangard Labs Inc.
- Vedco Inc.
- Veratex Corp.
- Vintage Pharmaceuticals Inc.
- Wa Butler Co.
- Watson Pharmaceuticals
- West-Ward Pharmaceuticals
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For the treatment of drug-induced allergic reactions, perennial or seasonal allergic rhinitis, serum sickness, giant cell arteritis acute rheumatic or nonrheumatic carditis, systemic dermatomyositis, systemic lupus erythematosus, atopic dermatitis, contact dermatitis, exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe (Stevens-Johnson syndrome) erythema multiforme, mycosis fungoides, pemphigus, severe psoriasis, acute adrenocortical insufficiency, Addison's disease, secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia associated with neoplasms, nonsuppurative thyroiditis, ulceratice colitis, Crohn's disease, acquired hemolytic anemia, congenital hypoplastic anemia, erythroblastopenia, adult secondary thrombocytopenia, adult idiopathic thrombocytopenia purpura, acute or subacute bursitis, epicondylitis, acute nonspecific tenosynovitis, acute or chronic lymphocytic leukemia, Hodgkin's or non-Hodgkin's lynphomas, Waldenstrom's macroglobulinemia, primary brain tumors (adjunct), nephrotic syndrome, tuberculous meningitis, multiple sclerosis, myasthenia gravis. cerebral edema, chorioretinitis, diffuse posterior choroiditis, aleergic conjunctivitis, Herpes zoster ophthalmicus, anterior segment inflammation, iridocyclitis, iritis, keratitis, optoc neuritis, sympathetic ophthalmia, corneal marginal allergic ulcers, symptomatic sarcoidosis, Loeffler's syndrome not manageable by other means, berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy and aspiration pneumonitis. | ||||||||
| Pharmacodynamics | Prednisone, the most commonly-prescribed corticosteroid, is used to treat allograft rejection, asthma, systemic lupus erythematosus, and many other inflammatory states. Prednisone has some mineralocorticoid activity and thus may affect ion exchange in the kidney. | ||||||||
| Mechanism of action | Prednisone is a glucocorticoid receptor agonist. It is first metabolized in the liver to its active form, prednisolone. Prednisolone crosses cell membranes and binds with high affinity to specific cytoplasmic receptors. The result includes inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. 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. Prednisone can stimulate secretion of various components of gastric juice. Suppression of the production of corticotropin may lead to suppression of endogenous corticosteroids. Prednisone has slight mineralocorticoid activity, whereby entry of sodium into cells and loss of intracellular potassium is stimulated. This is particularly evident in the kidney, where rapid ion exchange leads to sodium retention and hypertension. | ||||||||
| Absorption | Readily absorbed from the gastrointestinal tract. Rayos, the delayed-release formulation, has a 4-hour release time. To compare, the delayed-release formulation has a Tmax of 6.0 - 6.5 hours in healthy male subjects, whereas the immediate-release formulation has a Tmax of 2.0 hours. The rate of absorption, Cmax, and exposure is comparable between formulations. | ||||||||
| Volume of distribution | Not Available | ||||||||
| Protein binding | Extensively bound to plasma proteins. | ||||||||
| Metabolism |
Prednisone is completely converted to the active metabolite prednisolone by 11β-hydroxysteroid dehydrogenases. It is then further metabolized mainly in the liver. The exposure of prednisolone is 4-6 fold higher than that of prednisone.
Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.
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| Route of elimination | Excreted in the urine as sulfate and glucuronide conjugates. | ||||||||
| Half life | Half life of both the immediate- and delayed- release formulation is 2 to 3 hours. | ||||||||
| Clearance | Not Available | ||||||||
| Toxicity | Not Available | ||||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | The corticosteroid, prednisone, alters the anticoagulant effect, acenocoumarol. |
| Acetylsalicylic acid | The corticosteroid, prednisone, may decrease the effect of the salicylate, acetylsalicylic acid. |
| Ambenonium | The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, ambenonium. |
| Amobarbital | The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisone. |
| Anisindione | The corticosteroid, prednisone, alters the anticoagulant effect of anisindione. |
| Aprobarbital | The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, prednisone. |
| Bismuth Subsalicylate | The corticosteroid, prednisone, may decrease the effect of the salicylate, bismuth subsalicylate. |
| Butabarbital | The barbiturate, butabarbital, may decrease the effect of the corticosteroid, prednisone. |
| Butalbital | The barbiturate, butalbital, may decrease the effect of the corticosteroid, prednisone. |
| Butethal | The barbiturate, butethal, may decrease the effect of the corticosteroid, prednisone. |
| Chlorotrianisene | The estrogenic agent, chlorotrianisene, may increase the effect of corticosteroid, prednisone. |
| Clomifene | The estrogenic agent, clomifene, may increase the effect of corticosteroid, prednisone. |
| Conjugated Estrogens | The estrogenic agent may increase the effect of corticosteroid, prednisone. |
| Dicumarol | The corticosteroid, prednisone, alters the anticoagulant effect of dicumarol. |
| Diethylstilbestrol | The estrogenic agent, diethylstilbestrol, may increase the effect of corticosteroid, prednisone. |
| Dihydroquinidine barbiturate | The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, prednisone. |
| Edrophonium | The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, edrophonium. |
| Estradiol | The estrogenic agent, estradiol, may increase the effect of corticosteroid, prednisone. |
| Estriol | The estrogenic agent, estriol, may increase the effect of corticosteroid, prednisone. |
| Estrone | The estrogenic agent, estrone, may increase the effect of corticosteroid, prednisone. |
| Estropipate | The estrogenic agent, estropipate, may increase the effect of corticosteroid, prednisone. |
| Ethinyl Estradiol | The estrogenic agent, ethinyl estradiol, may increase the effect of corticosteroid, prednisone. |
| Ethotoin | The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, prednisone. |
| F | decreases the effect of cortisone by metabolism alteration. |
| Fosphenytoin | The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, prednisone. |
| Glycerol Phenylbutyrate | Use of corticosteroids may cause the breakdown of body protein and increase plasma ammonia levels. Monitor ammonia levels closely when corticosteroids and glycerol pehnylbutyrate are used concomitantly. |
| Heptabarbital | The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, prednisone. |
| Hexobarbital | The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, prednisone. |
| Indacaterol | Concomitant therapy may increase the risk of hypokalemia via intracellular shunting. Monitor for adverse effects and especially for cardiovascular effects associated with hypokalemia. |
| Insulin Lispro | Concomitant therapy with corticosteriods may reduce the blood-glucose-lowering effect of insulin lispro. |
| Itraconazole | The imidazole, itraconazole, may increase the effect and toxicity of the corticosteroid, prednisone. |
| Ketoconazole | The imidazole, ketoconazole, may increase the effect and toxicity of the corticosteroid, prednisone. |
| Linagliptin | CYP3A4 inducers may decrease levels of linagliptin and diminish the hypoglycemic effect of antidiabetic agents. Monitor concomitant therapy closely. |
| Magnesium salicylate | The corticosteroid, prednisolone, may decrease the effect of magnesium salicylate. |
| Mephenytoin | The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, prednisone. |
| Mestranol | The estrogenic agent, mestranol, may increase the effect of corticosteroid, prednisone. |
| Methohexital | The barbiturate, methohexital, may decrease the effect of the corticosteroid, prednisone. |
| Methylphenobarbital | The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, prednisone. |
| Midodrine | Increased arterial pressure |
| Neostigmine | The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, neostigmine. |
| Pentobarbital | The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisone. |
| Phenobarbital | The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, prednisone. |
| Phenytoin | The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, prednisone. |
| Primidone | The barbiturate, primidone, may decrease the effect of the corticosteroid, prednisone. |
| Pyridostigmine | The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, pyridostigmine. |
| Quinestrol | The estrogenic agent, quinestrol, may increase the effect of corticosteroid, prednisone. |
| Quinidine barbiturate | The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, prednisone. |
| Rifampin | The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, prednisone. |
| Salicylate-sodium | The corticosteroid, prednisone, may decrease the effect of the salicylate, salicylate-sodium. |
| Salsalate | The corticosteroid, prednisone, may decrease the effect of the salicylate, salsalate. |
| Secobarbital | The barbiturate, secobarbital, may decrease the effect of the corticosteroid, prednisone. |
| Tacrine | Tacrine and Prednisone 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, prednisone. |
| Trastuzumab | Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
| Trisalicylate-choline | The corticosteroid, prednisone, may decrease the effect of the salicylate, trisalicylate-choline. |
| Vecuronium | Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Prednisone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy. |
| Warfarin | The corticosteroid, prednisone, alters the anticoagulant effect of warfarin. |
食物相互作用
- Avoid alcohol.
- Avoid taking with grapefruit juice.
- Take with food to reduce irritation.
- When Rayos, the delayed-release tablet, is taken without food, Cmax and bioavailability were lower compared to the fed state.
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