WordNet

a glucocorticoid (trade names Pediapred or Prelone) used to treat inflammatory conditions (同)Pediapred, Prelone
be earlier in time; go back further; "Stone tools precede bronze tools" (同)precede, forego, forgo, antecede, antedate
establish something as being earlier relative to something else (同)antedate, foredate

PrepTutorEJDIC

…‘を'実際の日付より前にする / …‘わり'早く起こる

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/09/03 03:07:01」(JST)

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Prednisolone is a synthetic glucocorticoid, a derivative of cortisol, used to treat a variety of inflammatory and autoimmune conditions and some cancers. It is the active metabolite of the drug prednisone^[1] and is used especially in patients with liver failure, as these individuals are unable to metabolize prednisone into active prednisolone; it is primarily metabolized via the liver enzyme, 11-β-hydroxydehydrogenase.^[2] Adverse effects are not generally seen with short term therapy, but weight gain, impaired immune response, and behavioral disturbances commonly occur with longer durations of treatment.^[2]

It is on the WHO Model List of Essential Medicines, the most important medications needed in a basic health system.^[3]

Medical uses

Prednisolone is a corticosteroid drug with predominant glucocorticoid and low mineralocorticoid activity, making it useful for the treatment of a wide range of inflammatory and autoimmune conditions^[4] such as asthma,^[5] uveitis, pyoderma gangrenosum, rheumatoid arthritis, ulcerative colitis, pericarditis, temporal arteritis and Crohn's disease, Bell's palsy, multiple sclerosis,^[6] cluster headaches, vasculitis, acute lymphoblastic leukemia and autoimmune hepatitis,^[7] systemic lupus erythematosus, Kawasaki disease,^[8] dermatomyositis,^[9] and sarcoidosis.^[10]

Prednisolone acetate ophthalmic suspension (eye drops) is an adrenocortical steroid product, prepared as a sterile ophthalmic suspension and used to reduce swelling, redness, itching, and allergic reactions affecting the eye.^[11]^[12]

Prednisolone can also be used for allergic reactions ranging from seasonal allergies to drug allergic reactions.^[13]

Prednisolone can also be used as an immunosuppressive drug for organ transplants.^[9]^[14]

Prednisolone in lower doses can be used in cases of primary adrenal insufficiency (Addison's disease).^[15]^[16]

Corticosteroids inhibit the inflammatory response to a variety of inciting agents and, it is presumed, delay or slow healing.^[17] They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation with inflammation.^[18]

Adverse effects

There are several adverse reaction from the use of prednisolone:

Increase appetite, weight gain, nausea, and malaise
Increase risk of infection
Cardiovascular events in children
Dermatological effects including reddening of face, bruising/ skin discoloration, impaired wound healing, thinning of skin, skin rash, fluid build up and abnormal hair growth
Hyperglycemia; patients with diabetes may need increase insulin or diabetic therapies
Menstrual abnormalities
Less response to hormones especially during stressful instances such as surgery or illness.
Change in electrolytes: rise in blood pressure, increase sodium and low potassium leading to alkalosis
GI system effects: Swelling of stomach lining, reversible increase in liver enzymes and risk of stomach ulcers
Muscular and skeletal abnormalities such as muscle weakness and loss, osteoporosis, long bone fractures, tendon rupture and back fractures.
Neurological effects include involuntary movements (convulsions), headaches, and vertigo
Behavioral disturbances ^[19]

Nasal septum perforation and bowel perforation are also notable adverse effects that restrict steroids' use in some pathologic conditions.^[20]^[21]

Withdrawal from prednisolone after long term or high dose use can lead to adrenal insufficiency.^[19]

Pregnancy and breastfeeding

Although there are no major human studies of prednisolone use in pregnant women, studies in several animals show that it may cause birth defects including increase cleft palate. Prednisolone should be used in pregnant women when benefits outweigh the risks and children born from mothers using prednisolone during pregnancy should be monitored for impaired adrenal function.

Prednisolone is found in breast milk of mothers taking prednisolone.^[19]

Mechanism of action

As a synthetic glucocorticoid (GC), its lipophilic structure allows for easy passage through the cell membrane where it then binds to its respective glucocorticoid receptor (GCR) located in the cytoplasm. Upon binding, formation of the GC/GCR complex causes dissociation of chaperone proteins from the glucocorticoid receptor enabling the GC/GCR complex to translocate inside the nucleus. This process occurs within 20 minutes of binding. Once inside the nucleus, the homodimer GC/GCR complex binds to specific DNA binding-sites known as glucocorticoid response elements (GREs) resulting in gene expression or inhibition. Complex binding to positive GREs leads to synthesis of anti-inflammatory proteins while binding to negative GREs block the transcription of inflammatory genes.^[22]

Society and culture

Dosage forms

In the United States

Prednisolone sodium posphate oral solution (Pediapred)^[19]
Prednisolone acetate oral suspension (Flo-Pred)^[23]
Prednisolone oral tablets (Millipred)^[13]
Prednisolone sodium phosphate oral dissolving tablets (Orapred)^[24]

Athletics

As a glucocorticosteroid, unauthorized or ad-hoc use of prednisolone during competition via oral, intravenous, intramuscular or rectal routes is banned under WADA anti-doping rules.^[25] The drug may be used in competition with a TUE (Therapeutic Use Exemption), in compliance with WADA regulations. Local or topical use of prednisolone during competition as well as any use out of competition is not regulated.^[25]

References

^ Davis M, Williams R, Chakraborty J, et al. (June 1978). "Prednisone or prednisolone for the treatment of chronic active hepatitis? A comparison of plasma availability". British Journal of Clinical Pharmacology. 5 (6): 501–5. doi:10.1111/j.1365-2125.1978.tb01664.x. PMC 1429358. PMID 656293.
^ ^a ^b Frey, Brigitte (March 1985). "Pharmacokinetics of 3 prednisolone prodrugs. Evidence of therapeutic inequivalence in renal transplant patients with rejection.". Transplantation. 39: 270–4. doi:10.1160/TH11-09-0672. PMID 3883592.
^ "19th WHO Model List of Essential Medicines (April 2015)" (PDF). WHO. April 2015. Retrieved May 10, 2015.
^ Czock D, Keller F, Rasche FM, Häussler U (2005). "Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids". Clin Pharmacokinet. 44 (1): 61–98. doi:10.2165/00003088-200544010-00003. PMID 15634032.
^ Fiel SB, Vincken W (Jun 2006). "Systemic corticosteroid therapy for acute asthma exacerbations". J Asthma. 43 (5): 321–31. doi:10.1080/02770900600567163. PMID 16801135.
^ Thrower BW (Jan 2009). "Relapse management in multiple sclerosis". Neurologist. 15 (1): 1–5. doi:10.1097/NRL.0b013e31817acf1a. PMID 19131851.
^ Lambrou GI, Vlahopoulos S, Papathanasiou C, Papanikolaou M, Karpusas M, Zoumakis E, Tzortzatou-Stathopoulou F (2009). "Prednisolone exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells: Relation to early gene expression". Leuk Res. 33 (12): 1684–95. doi:10.1016/j.leukres.2009.04.018. PMID 19450877.
^ Miura M, Tamame T, Naganuma T, Chinen S, Matsuoka M, Ohki H (2011). "Steroid pulse therapy for Kawasaki disease unresponsive to additional immunoglobulin therapy". Paediatrics & Child Health. 16 (8): 479–84. PMC 3202387. PMID 23024586.
^ ^a ^b Product Information: ORAPRED ODT(TM) orally disintegrating tablets, prednisolone sodium phosphate orally disintegrating tablets. Cima Labs Inc, Alpharetta, GA, 2006.
^ Gera, Kamal; Gupta, Nitesh; Ahuja, Anuradha; Shah, Ashok (2014-04-30). "Acute alveolar sarcoidosis presenting with hypoxaemic respiratory failure". BMJ Case Reports. 2014: bcr2013202247. doi:10.1136/bcr-2013-202247. ISSN 1757-790X. PMC 4024548. PMID 24789154.
^ "Pred Forte Package Insert" (PDF).
^ Product Information: OMNIPRED(TM) ophthalmic suspension, prednisolone acetate ophthalmic suspension. Alcon Laboratories Inc, Fort Worth, TX, 2005
^ ^a ^b "Millipred tablets package insert" (PDF).
^ Vethe, Nils; Midtvedt, Karsten; Åsberg, Anders; Amundsen, Rune; Bergan, Stein. "Legemiddelinteraksjoner og immunsuppresjon hos organtransplanterte". Tidsskrift for Den norske legeforening. 131 (20): 2000–2003. doi:10.4045/tidsskr.11.0138.
^ Husebye, E. S.; Allolio, B.; Arlt, W.; Badenhoop, K.; Bensing, S.; Betterle, C.; Falorni, A.; Gan, E. H.; Hulting, A.-L. (2014-02-01). "Consensus statement on the diagnosis, treatment and follow-up of patients with primary adrenal insufficiency". Journal of Internal Medicine. 275 (2): 104–115. doi:10.1111/joim.12162. ISSN 1365-2796.
^ AMA Department of Drugs: AMA Drug Evaluations, 6th. American Medical Association, Chicago, IL, 1986.
^ Schwiebert, L. M.; Beck, L. A.; Stellato, C.; Bickel, C. A.; Bochner, B. S.; Schleimer, R. P.; Schwiebert, L. A. (1996-01-01). "Glucocorticosteroid inhibition of cytokine production: relevance to antiallergic actions". The Journal of Allergy and Clinical Immunology. 97 (1 Pt 2): 143–152. doi:10.1016/s0091-6749(96)80214-4. ISSN 0091-6749. PMID 8568145.
^ Lee, Sang Hag (2015). "Mechanisms of Glucocorticoid Action in Chronic Rhinosinusitis". Allergy, Asthma & Immunology Research. 7 (6): 534–7. doi:10.4168/aair.2015.7.6.534. PMC 4605925. PMID 26333699.
^ ^a ^b ^c ^d "PEDIAPRED" (PDF).
^ "Bowel Perforation in Steroid-Treated Patients"
^ "Intranasal steroids and septum perforation--an overlooked complication?"
^ Stahn, Cindy (17 May 2007). "Molecular mechanisms of glucocorticoid action and selective glucocorticoid receptor agonists" (PDF). Molecular and Cellular Endocrinology. 275: 71–78. doi:10.1016/j.mce.2007.05.019.
^ "Flo-Pred Package Insert" (PDF).
^ "Package Insert for Orapred ODT" (PDF).
^ ^a ^b "The 2011 Prohibited List".

UpToDate Contents

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English Journal

Clinical features and outcomes of delayed facial palsy after head trauma.

Li Q1, Jia Y2, Feng Q3, Tang B1, Wei N1, Zhang Y1, Li Y4, Zhang X5.
Auris, nasus, larynx.Auris Nasus Larynx.2016 Oct;43(5):514-7. doi: 10.1016/j.anl.2015.12.017. Epub 2016 Feb 1.
OBJECTIVE: To investigate clinical features and outcomes of delayed facial palsy after head trauma.METHODS: The cases who had delayed facial palsy after head trauma treated from March 2008 to March 2013 at our hospital were enrolled in the study, and their clinical features and outcomes were analyze
PMID 26837868

Calcium pectinate gel beads obtained from callus cultures pectins as promising systems for colon-targeted drug delivery.

Günter EA1, Popeyko OV2.
Carbohydrate polymers.Carbohydr Polym.2016 Aug 20;147:490-9. doi: 10.1016/j.carbpol.2016.04.026. Epub 2016 Apr 8.
Low methyl-esterified pectins obtained from the cell walls of the campion (SV, SV>300), tansy (TV, TV>300) and duckweed (LM, LM>300) callus cultures and apple pectin (AP, Classic AU 701) were used as the carriers for colon delivery of prednisolone. The pectins with molecular weight more tha
PMID 27178956

Prediction of high risk for death in patients with follicular lymphoma receiving rituximab plus cyclophosphamide, doxorubicin, vincristine, and prednisolone in first-line chemotherapy.

Murakami S1, Kato H1, Higuchi Y1, Yamamoto K1, Yamamoto H1, Saito T1, Taji H1, Yatabe Y2, Nakamura S2,3, Kinoshita T4.
Annals of hematology.Ann Hematol.2016 Aug;95(8):1259-69. doi: 10.1007/s00277-016-2690-2. Epub 2016 May 25.
Risk stratification of patients with relapsed and refractory follicular lymphoma (FL) remains challenging. Recently, much attention has been paid to the impact of early progression of disease within 2 years of diagnosis (early POD) on subsequent survival. The aim of this study was to clarify the cl
PMID 27220639

Japanese Journal

Preparation of Enteric-coated Capsules of Beclomethasone Dipropionate for Patients with Intestinal Graft-versus-Host Disease and a Case Study

Murakawa Kiminaka,Sato Tomoaki,Maeda Yoshinobu,Kitamura Yoshihisa,Tanimoto Mitsune,Sendo Toshiaki
Acta Medica Okayama 67(5), 319-324, 2013-10-00
… In addition, we were able to decrease the prednisolone equivalent dose. …
NAID 120005341865

A case of refractory cutaneous polyarteritis nodosa in a patient with hepatitis B carrier status successfully treated with tumor necrosis factor alpha blockade

Zoshima Takeshi,Matsumura Masami,Suzuki Yasunori,Kakuchi Yasushi,Mizushima Ichiro,Fujii Hiroshi,Yamada Kazunori,Yamagishi Masakazu,Kawano Mitsuhiro
Modern Rheumatology 23(5), 1029-1033, 2013-09-00
… prednisolone dose-sparing; …
NAID 120004966632

Management of postoperative hemorrhage associated with factor VIII inhibitor: report of a case

Onishi Ichiro,Kayahara Masato,Munemoto Masayoshi,Sakai Seisyo,Makino Isamu,Hayashi Hironori,Nakagawara Hisatoshi,Tajima Hidehiro,Takamura Hiroyuki,Kitagawa Hirohisa,Tani Takashi,Ohta Tetsuo
Surgery Today 43(9), 1058-1061, 2013-09-00
… Inhibitor elimination was started using prednisolone on POD 20; …
NAID 120004754695

Related Pictures

★リンクテーブル★

リンク元	「糖質コルチコイド」「ベタメタゾン」「デキサメタゾン」「プレドニゾロン」「prednisolone sodium succinate」
拡張検索	「methylprednisolone aceponate」「methylprednisolone hemisuccinate」「6α-methylprednisolone」「methylprednisolone」「fluoxyprednisolone」

「糖質コルチコイド」

Prednisolone
Systematic (IUPAC) name
	(11β)-11,17,21-Trihydroxypregna-1,4-diene-3,20-dione
Clinical data
AHFS/Drugs.com	Monograph
MedlinePlus	a682794
License data	US FDA: prednisolone;
Pregnancy; category	AU: A; US: C (Risk not ruled out); ;
Legal status
Legal status	UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Biological half-life	2-3 hours
Excretion	urine
Identifiers
CAS Number	50-24-8
ATC code	A07EA01 (WHO) C05AA04 (WHO), D07AA03 (WHO), H02AB06 (WHO), R01AD02 (WHO), S01BA04 (WHO), S02BA03 (WHO), S03BA02 (WHO)
PubChem	CID 5755
IUPHAR/BPS	2866
DrugBank	DB00860
ChemSpider	5552
UNII	9PHQ9Y1OLM
KEGG	D00472
ChEBI	CHEBI:8378
ChEMBL	CHEMBL131
Synonyms	11,17-Dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydrocyclopenta[a] phenanthren-3-one
Chemical data
Formula	C21H28O5
Molar mass	360.444 g/mol
	SMILES O=C\1\C=C/[C@]4(/C(=C/1)CC[C@@H]2[C@@H]4[C@@H](O)C[C@@]3([C@@](O)(C(=O)CO)CC[C@@H]23)C)C ;
	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 ; Key:OIGNJSKKLXVSLS-VWUMJDOOSA-N ;
(verify)

　　[★]

英: glucocorticoid (Z), glucocorticoids
関: グルココルチコイド
関: 副腎皮質、副腎皮質ホルモン

以下、内的に合成される糖質コルチコイドについて述べる

種類

ステロイドホルモン

分類

副腎皮質ホルモン

性状

ステロイド

産生組織

副腎皮質索状層

標的組織

生理作用

1. エネルギー代謝

糖新生においてグルコースの前駆体となるアミノ酸を肝臓に供給すべく動員する作用 (SP.894)

a. 糖代謝作用

糖新生の亢進

血糖上昇

肝細胞以外のグルコースの取り込みを抑制 (SP.894) ←　末梢でインスリンの作用に拮抗

グルコース-6-ホスファターゼの活性亢進 (SP.894)

グリコーゲンの合成亢進

血糖値の上昇に伴い、肝臓などでグルコースからグリコーゲンが作られる (SP.894)

b. タンパク質代謝作用

肝臓での糖新生の基質を末梢から供給する作用

肝細胞以外でのアミノ酸取り込み阻害 (SP.894)

特定のアミノ酸合成を阻害 (SP.894)

生理的範囲：(肝臓)同化作用が起こる、(肝臓以外)異化作用が起こる

ステロイド大量投与時：ほとんど異化作用が起こる→副作用につながる

c. 脂質代謝作用

脂肪細胞に対して、インスリンの拮抗作用を持つが、一方で糖質コルチコイドにより血糖値が上昇する

脂肪分解↑→血糖値↑　…(1)

脂肪細胞に対してグルコースの取り込みを抑制し、中性脂肪の生合成を抑制し、さらに大量の遊離脂肪酸とグリセロールを放出させる。肝臓でグリセロールからグルコースが合成される。 (SP.894)

血糖値↑→脂肪合成↑　…(2)

血糖値の上昇によりインスリンが分泌され、脂肪細胞で脂肪の合成が促進される (SP.894)

(1)、(2)のいずれの反応が起こるかは体の部位によって異なり、脂肪分布の変化が生じる。

中心性肥満、満月様顔貌、バッファローハンプ

2. 電解質代謝作用

糖質コルチコイドの電解質コルチコイド様作用。

Na+再吸収↑、K+排泄↑

コルチゾールの電解質作用はアルドステロンの約１／４００

コルチゾールの量　　　　はアルドステロンの約　２００倍

ゆえに、電解質コルチコイドの１／２の作用力を持つ

3. 水代謝作用

GFR↑、ADHに拮抗、細胞内への水移動の抑制→水利尿作用を有する。　　尿崩症 + 副腎不全　→　多尿がいくらか改善されると考えて良いと思われる。仮面尿崩症

4. 骨・軟骨に対する作用

a. ビタミンDと拮抗して腸管からのCa吸収阻害 (SP.894)
b. 腎尿細管におけるCa再吸収阻害 (SP.894)
c. 骨芽細胞の分化・増殖を抑制 (SP.894)

糖質コルチコイドの大量投与→軟骨↓骨成長↓(活性型ビタミンD₃に拮抗・尿細管Ca再吸収↓→PTH↑、骨芽細胞の分化抑制、タンパク質の異化作用↑)→骨粗鬆症、骨壊死 or 骨端線閉鎖を促進(←？要調査)

b.の機序で尿に排泄されるカルシウムが増加　　→　　高カルシウム尿症　→　尿路結石

5. 抗炎症作用

胸腺やリンパ組織を萎縮させる　→　炎症反応や免疫反応を抑制

リンパ球数の減少、白血球の遊走抑制、抗体産生低下、ヒスタミン放出抑制(局所の毛細血管拡張抑制) (SP.894)

末梢好中球数は増加する(YN.F-78)　→　白血球増多症

SPC.330

a) 核内受容体を介してlipocortinを発現させ、これがphospholipase A2を阻害する。これにより、アラキドン酸の産生が抑制され、炎症を促進するロイコトリエンの産生も抑制される。
b) 末梢血Tリンパ球、単球、好酸球、好塩基球：骨髄からの放出減少と再分配(?)のため末梢血中では減少する。
c) 末梢血好中球：炎症部位への集合が抑制され(血管外への遊走が抑制される(GOO.1600))、末梢血中では増加する。
d) Bリンパ球はヘルパーT細胞が抑制されるために抗体産生能が減少する。
e) リンパ球などの細胞表面の立体構造を換えて抗体や補体の結合を抑制する。
f) 毛細血管(毛細管)の収縮により、血管の透過性は低下する。

6. 循環器

カテコールアミン・アンジオテンシンIIによる血管収縮作用の許容作用　→　糖質コルチコイドなしではその作用を十分に及ぼし得ない

欠乏症では血管のカテコールアミン・アンジオテンシンIIに対する感受性低下

7. 中枢神経系

認知機能や情動を修飾 (SP.895)

8. 成長発達

胎児期の消化酵素・リン脂質(肺胞表面の張力に関与)の合成に関与 (SP.895)
小児期で骨や熱強訴域に直接作用して身長の伸びを抑制する (SP.895)

作用機序

免疫抑制(GOO. 657,674,1600)

COX-2の抑制
phospholipase A₂の抑制

糖質コルチコイドはリポコルチンを産生→リポコルチンはホスホリパーゼA₂の活性を修飾→アラキドン酸産生↓

分泌調節

1. 概日リズム
2. フィードバック制御
- 糖質コルチコイドがACTHやCRHを抑制
3. ストレス反応

臨床関連

クッシング症候群(糖質コルチコイド過剰) (SP.894)

合成ステロイドホルモン

用量

低用量から中等量：40mg未満

Low-to-moderate doses — Doses of 1 mg/kg per day of prednisone in children or 40 mg per day in adults may be considered an approximate threshold at which significant toxicities begin to appear with extended use in most individuals.

副作用

副腎皮質ホルモン剤

副腎機能の低下、骨粗鬆症(無菌性大腿骨頭壊死)、高脂血症、高血圧、筋力低下、筋肉痛、白内障、緑内障
ニューモシスチス肺 PCP

Patients receiving a glucocorticoid dose equivalent to ≥20 mg of prednisone daily for one month or longer who also have another cause of immunocompromise (eg, certain hematologic malignancies or a second immunosuppressive drug)

https://www.uptodate.com/contents/treatment-and-prevention-of-pneumocystis-pneumonia-in-hiv-uninfected-patients?

0.5mg/kg以上のプレドニゾロン(PSL)を3週間以上投与され、かつST予防投与されていない間質性肺炎74例中7例(9.5％)でPCPを発症(榎本達治，他．ステロイド療法中の間質性肺炎患者に発症したニューモシスチス肺炎の臨床的検討．日呼吸会誌 2005: 43: 725-30)

Table 59–2 Relative Potencies and Equivalent Doses of Representative Corticosteroids
COMPOUND	ANTIINFLAMMATORY POTENCY	Na+-RETAINING POTENCY	DURATION OF ACTION*	EQUIVALENT DOSE, MG
cortisol	1	1	S	20
cortisone	0.8	0.8	S	25
fludrocortisone	10	125	I	‡
prednisone	4	0.8	I	5
prednisolone	4	0.8	I	5
6α-methylprednisolone	5	0.5	I	4
triamcinolone	5	0	I	4
betamethasone	25	0	L	0.75
dexamethasone	25	0	L	0.75

「ベタメタゾン」

　　[★]

英: betamethasone
同: ベタメサゾン
化: ベタメタゾンリン酸エステルナトリウム、リン酸ベタメタゾンナトリウム betamethasone sodium phosphate; 酢酸ベタメタゾン betamethasone acetate; 吉草酸ベタメタゾン betamethasone valerate。ベタメタゾン吉草酸エステル; ベタメタゾンジプロピオン酸エステル、ジプロピオン酸ベタメタゾン betamethasone dipropionate; ベタメタゾン酪酸エステルプロピオン酸エステル
商: リンデロン Rinderon、アンテベート。Celestone; アンテベート、アンフラベート、エンペラシン、ケリグロール、サクコルチン、サレックス、サンベタゾン、ステロネマ、セレスタミン、ダイプロセル、ディーピーポロン、デキサンVG、デルモゾールＤＰ、デルモゾールＧ、デルモゾール、トクダーム、トチプロベタゾン、ノルコット、ハイコート、ヒスタブロック、ヒズボット、フロダーム、プラデスミン、ベクトミラン、ベタセレミン、ベトネベートＮ、ベトネベート、ベトノバールＧ、ベルベゾロンF、ベルベゾロン、リダスロン、リネステロン、リノロサール、リンデロン-DP、リンデロン-VG、リンデロン-V、リンデロン、リンベタPF、ルリクールVG、リンデロンA
関: 鎮痛，鎮痒，収歛，消炎剤

GOO.1594

Table 59–2 Relative Potencies and Equivalent Doses of Representative Corticosteroids
COMPOUND	ANTIINFLAMMATORY POTENCY	Na+-RETAINING POTENCY	DURATION OF ACTION	EQUIVALENT DOSE, MG
prednisone	4	0.8	I	5
prednisolone	4	0.8	I	5
betamethasone	25	0	L	0.75
dexamethasone	25	0	L	0.75

「デキサメタゾン」

　　[★]

英: dexamethasone
ラ: dexamethasonum
化: プロピオン酸デキサメタゾン？JAN
同: デキサメサゾン
商: Decadron; (点眼・点耳・点鼻)DMゾロン、コンドロンデキサ、ビジュアリン、テイカゾン、D・E・X、オルガドロン、サンテゾーン; (口腔内用)アフタゾロン、デルゾン、エースミン、デキサルチン、デルゾン; (軟膏)ビスオ、メインベート、デルムサット、プロメタゾン、メサデルム、オイラゾン、グリメサゾン、ザルックス、デキサA、ヒフメタ、プロメタゾン、ボアラ; (注射液)デキサート、オルガドロン(デキサメタゾンリン酸エステルナトリウム)、ソルコート、デカドロン、メサドロン、リメタゾン; (服用)エリザス、レナデックス; (吸入)ストメリンD
関: 糖質コルチコイド、デキサメタゾン抑制試験、コルチコイド; 鎮痛，鎮痒，収歛，消炎剤

[show details]

デキサメタゾン : 約 103,000 件
デキサメサゾン : 約 37,800 件

GOO.1594

Table 59–2 Relative Potencies and Equivalent Doses of Representative Corticosteroids
COMPOUND	ANTIINFLAMMATORY POTENCY	Na+-RETAINING POTENCY	DURATION OF ACTION	EQUIVALENT DOSE, MG
prednisone	4	0.8	I	5
prednisolone	4	0.8	I	5
betamethasone	25	0	L	0.75
dexamethasone	25	0	L	0.75

「プレドニゾロン」

　　[★]

英: prednisolone, PSL
化: コハク酸プレドニゾロン、コハク酸プレドニゾロンナトリウム, prednisolone sodium succinate、酢酸プレドニゾロン
商: プレドニゾロン、プレドニン, Predonine、Delta Cortef、Hydeltrasol、Predalone; PSゾロン、クロマイ-P、コールタイジン、コハクサニン、スピラゾン、ハイセチンP、ビスオ、ファルネゾン、プレドニン、プレドネマ、プレドハン、プレロン、ユーメトン、リドメックスコーワ
関: 副腎皮質ホルモン、糖質コルチコイド。プレドニゾン

概念

合成糖質副腎皮質ホルモン
ヒドロコルチゾンの誘導体

"prednisone" is a prodrug that is converted by the liver into "prednisolone", which is the active drug and also a steroid.

添付文書

※プレドニゾロン錠5mg「トーワ」

http://www.info.pmda.go.jp/go/pack/2456001F1400_1_03/2456001F1400_1_03?view=body

「prednisolone sodium succinate」

　　[★]

コハク酸プレドニゾロンナトリウム

関: predate、prednisolone、prednisolone acetate、prednisolone farnesylate、prednisolone sodium phosphate、prednisolone succinate、prednisolone tebutate、prednisolone valerate acetate

「methylprednisolone aceponate」

　　[★]

アセ・ン酸メチルプレドニゾロン

関: methylprednisolone、methylprednisolone acetate、methylprednisolone sodium succinate

「methylprednisolone hemisuccinate」

　　[★]

ヘミコハク酸メチルプレドニゾロン

関: methylprednisolone sodium succinate、methylprednisolone succinate、Solumedrol

「6α-methylprednisolone」

　　[★]

同: 6α-メチルプレドニゾロン
関: メチルプレドニゾロン

「methylprednisolone」

　　[★] メチルプレドニゾロン

同: Depo-Medrol, Medrol, Solu- Medrol

「fluoxyprednisolone」

　　[★] トリアムシノロン、フルオキシプレドニゾロン

[Davis-1] Davis M, Williams R, Chakraborty J, et al. (June 1978). "Prednisone or prednisolone for the treatment of chronic active hepatitis? A comparison of plasma availability". British Journal of Clinical Pharmacology. 5 (6): 501–5. doi:10.1111/j.1365-2125.1978.tb01664.x. PMC 1429358. PMID 656293.

[:3-2] Frey, Brigitte (March 1985). "Pharmacokinetics of 3 prednisolone prodrugs. Evidence of therapeutic inequivalence in renal transplant patients with rejection.". Transplantation. 39: 270–4. doi:10.1160/TH11-09-0672. PMID 3883592.

[WHO2015E-3] "19th WHO Model List of Essential Medicines (April 2015)" (PDF). WHO. April 2015. Retrieved May 10, 2015.

[4] Czock D, Keller F, Rasche FM, Häussler U (2005). "Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids". Clin Pharmacokinet. 44 (1): 61–98. doi:10.2165/00003088-200544010-00003. PMID 15634032.

[5] Fiel SB, Vincken W (Jun 2006). "Systemic corticosteroid therapy for acute asthma exacerbations". J Asthma. 43 (5): 321–31. doi:10.1080/02770900600567163. PMID 16801135.

[6] Thrower BW (Jan 2009). "Relapse management in multiple sclerosis". Neurologist. 15 (1): 1–5. doi:10.1097/NRL.0b013e31817acf1a. PMID 19131851.

[7] Lambrou GI, Vlahopoulos S, Papathanasiou C, Papanikolaou M, Karpusas M, Zoumakis E, Tzortzatou-Stathopoulou F (2009). "Prednisolone exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells: Relation to early gene expression". Leuk Res. 33 (12): 1684–95. doi:10.1016/j.leukres.2009.04.018. PMID 19450877.

[8] Miura M, Tamame T, Naganuma T, Chinen S, Matsuoka M, Ohki H (2011). "Steroid pulse therapy for Kawasaki disease unresponsive to additional immunoglobulin therapy". Paediatrics & Child Health. 16 (8): 479–84. PMC 3202387. PMID 23024586.

[Cima_Labs_Inc_2006-9] Product Information: ORAPRED ODT(TM) orally disintegrating tablets, prednisolone sodium phosphate orally disintegrating tablets. Cima Labs Inc, Alpharetta, GA, 2006.

[10] Gera, Kamal; Gupta, Nitesh; Ahuja, Anuradha; Shah, Ashok (2014-04-30). "Acute alveolar sarcoidosis presenting with hypoxaemic respiratory failure". BMJ Case Reports. 2014: bcr2013202247. doi:10.1136/bcr-2013-202247. ISSN 1757-790X. PMC 4024548. PMID 24789154.

[11] "Pred Forte Package Insert" (PDF).

[12] Product Information: OMNIPRED(TM) ophthalmic suspension, prednisolone acetate ophthalmic suspension. Alcon Laboratories Inc, Fort Worth, TX, 2005

[:0-13] "Millipred tablets package insert" (PDF).

[14] Vethe, Nils; Midtvedt, Karsten; Åsberg, Anders; Amundsen, Rune; Bergan, Stein. "Legemiddelinteraksjoner og immunsuppresjon hos organtransplanterte". Tidsskrift for Den norske legeforening. 131 (20): 2000–2003. doi:10.4045/tidsskr.11.0138.

[15] Husebye, E. S.; Allolio, B.; Arlt, W.; Badenhoop, K.; Bensing, S.; Betterle, C.; Falorni, A.; Gan, E. H.; Hulting, A.-L. (2014-02-01). "Consensus statement on the diagnosis, treatment and follow-up of patients with primary adrenal insufficiency". Journal of Internal Medicine. 275 (2): 104–115. doi:10.1111/joim.12162. ISSN 1365-2796.

[16] AMA Department of Drugs: AMA Drug Evaluations, 6th. American Medical Association, Chicago, IL, 1986.

[17] Schwiebert, L. M.; Beck, L. A.; Stellato, C.; Bickel, C. A.; Bochner, B. S.; Schleimer, R. P.; Schwiebert, L. A. (1996-01-01). "Glucocorticosteroid inhibition of cytokine production: relevance to antiallergic actions". The Journal of Allergy and Clinical Immunology. 97 (1 Pt 2): 143–152. doi:10.1016/s0091-6749(96)80214-4. ISSN 0091-6749. PMID 8568145.

[18] Lee, Sang Hag (2015). "Mechanisms of Glucocorticoid Action in Chronic Rhinosinusitis". Allergy, Asthma & Immunology Research. 7 (6): 534–7. doi:10.4168/aair.2015.7.6.534. PMC 4605925. PMID 26333699.

[:2-19] "PEDIAPRED" (PDF).

[20] "Bowel Perforation in Steroid-Treated Patients"

[21] "Intranasal steroids and septum perforation--an overlooked complication?"

[22] Stahn, Cindy (17 May 2007). "Molecular mechanisms of glucocorticoid action and selective glucocorticoid receptor agonists" (PDF). Molecular and Cellular Endocrinology. 275: 71–78. doi:10.1016/j.mce.2007.05.019.

[23] "Flo-Pred Package Insert" (PDF).

[24] "Package Insert for Orapred ODT" (PDF).

[:1-25] "The 2011 Prohibited List".

v t e Antidiarrheals, intestinal anti-inflammatory and anti-infective agents (A07)

Rehydration	Oral rehydration therapy

Intestinal anti-infectives	Antibiotics Amphotericin B Colistin Fidaxomicin Kanamycin Natamycin Neomycin Nystatin Paromomycin Polymyxin B Rifaximin Streptomycin Vancomycin Sulfonamides Phthalylsulfathiazole Succinylsulfathiazole Sulfaguanidine Nitrofuran Nifuroxazide Nifurzide Imidazole Miconazole Arsenical Acetarsol Oxyquinoline Broxyquinoline

Intestinal adsorbents	Charcoal Bismuth Pectin Kaolin Crospovidone Attapulgite Diosmectite

Antipropulsives (opioids)	Opium tincture (laudanum) Codeine Morphine Camphorated opium tincture (paregoric) crosses BBB: Diphenoxylate (Diphenoxylate/atropine) Difenoxin does not cross BBB: Eluxadoline Loperamide

Intestinal anti-inflammatory agents	corticosteroids acting locally Prednisolone Hydrocortisone Prednisone Betamethasone Tixocortol Budesonide Beclometasone antiallergic agents, excluding corticosteroids Cromoglicic acid aminosalicylic acid and similar agents Sulfasalazine Mesalazine Olsalazine Balsalazide

Antidiarrheal micro-organisms	Saccharomyces boulardii

Other antidiarrheals	Albumin tannate Ceratonia Crofelemer Octreotide Racecadotril

v t e Drugs used for diseases of the ear (S02)

Infection	Acetic acid Aluminium acetotartrate Boric acid Chloramphenicol Chlorhexidine Ciprofloxacin Clioquinol Gentamicin Hydrogen peroxide Miconazole Neomycin Nitrofurazone Ofloxacin Polymyxin B Rifamycin Tetracycline

Corticosteroids	Betamethasone Dexamethasone Fluocinolone acetonide Hydrocortisone Prednisolone

Analgesics and anesthetics	Lidocaine Cocaine Phenazone

匿名

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案内

prednisolone

WordNet

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Wikipedia preview

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Contents

Medical uses

Adverse effects

Pregnancy and breastfeeding

Mechanism of action

Society and culture

Dosage forms

Athletics

See also

References

UpToDate Contents

English Journal

Japanese Journal

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Related Pictures

★リンクテーブル★

「糖質コルチコイド」

種類

分類

性状

産生組織

標的組織

生理作用

1. エネルギー代謝

a. 糖代謝作用

b. タンパク質代謝作用

c. 脂質代謝作用

2. 電解質代謝作用

3. 水代謝作用

4. 骨・軟骨に対する作用

5. 抗炎症作用

SPC.330

6. 循環器

7. 中枢神経系

8. 成長発達

作用機序

免疫抑制(GOO. 657,674,1600)

分泌調節

臨床関連

用量

副作用

「ベタメタゾン」

GOO.1594

「デキサメタゾン」

GOO.1594

「プレドニゾロン」

概念

添付文書

「prednisolone sodium succinate」

「methylprednisolone aceponate」

「methylprednisolone hemisuccinate」

「6α-methylprednisolone」

「methylprednisolone」

「fluoxyprednisolone」