prednisolone sodium phosphate

WordNet

1. a salt of phosphoric acid (同)orthophosphate, inorganic_phosphate
2. carbonated drink with fruit syrup and a little phosphoric acid
3. a silvery soft waxy metallic element of the alkali metal group; occurs abundantly in natural compounds (especially in salt water); burns with a yellow flame and reacts violently in water; occurs in sea water and in the mineral halite (rock salt) (同)Na, atomic number 11
4. a glucocorticoid (trade names Pediapred or Prelone) used to treat inflammatory conditions (同)Pediapred, Prelone

PrepTutorEJDIC

1. 〈U〉リン酸塩 / 《複数形で》リン酸肥料
2. ソジウム,ナトリウム(金属元素;化学記号はNa)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/09/13 18:44:55」(JST)

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Not to be confused with Prednisolone.

Prednisone

Systematic (IUPAC) name
17,21-dihydroxypregna-1,4-diene-3,11,20-trione
Clinical data
AHFS/Drugs.com	Monograph
MedlinePlus	a601102
Pregnancy category	C
Routes of administration	Oral, Nasal, Rectal, Injection, IV
Legal status
Legal status	Rx Only (US)(AUS)
Pharmacokinetic data
Bioavailability	70%
Metabolism	prednisolone (liver)
Biological half-life	18 to 36 hours.
Excretion	Renal
Identifiers
CAS Number	53-03-2 Y
ATC code	A07EA03 (WHO) H02AB07 (WHO)
PubChem	CID 5865
IUPHAR/BPS	7096
DrugBank	DB00635 Y
ChemSpider	5656 Y
UNII	VB0R961HZT N
KEGG	C07370 Y
ChEBI	CHEBI:8382 Y
ChEMBL	CHEMBL635 Y
Synonyms	Deltasone, Liquid Pred, Orasone, Adasone, Deltacortisone, Prednisonum
Chemical data
Formula	C21H26O5
Molar mass	358.428 g/mol
SMILES O=C(CO)[C@@]3(O)CC[C@H]2[C@@H]4CC\C1=C\C(=O)\C=C/[C@]1(C)[C@H]4C(=O)C[C@@]23C
InChI InChI=1S/C21H26O5/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/h5,7,9,14-15,18,22,26H,3-4,6,8,10-11H2,1-2H3/t14-,15-,18+,19-,20-,21-/m0/s1 Y Key:XOFYZVNMUHMLCC-ZPOLXVRWSA-N Y
NY (what is this?)  (verify)

Micrograph of fatty liver, as may be seen due to long-term prednisone use. Trichrome stain.

Prednisone is a synthetic corticosteroid drug that is particularly effective as an immunosuppressant drug. It is used to treat certain inflammatory diseases (such as moderate allergic reactions), some autoimmune diseases, and (at higher doses) some types of cancer, but it has significant adverse effects.

Medical uses

Prednisone is used, at a usual adult dosage of 5–60 mg/day, for many different indications including: asthma, COPD, CIDP, rheumatic disorders, allergic disorders, ulcerative colitis and Crohn's disease, adrenocortical insufficiency, hypercalcemia due to cancer, thyroiditis, laryngitis, severe tuberculosis, urticaria (hives), lipid pneumonitis, pericarditis, multiple sclerosis, nephrotic syndrome, to relieve the effects of shingles, lupus, myasthenia gravis, poison oak exposure, Meniere's disease, and as part of a drug regimen to prevent rejection after organ transplant.

Prednisone has also been used in the treatment of migraine headaches and cluster headaches and for severe aphthous ulcer. Prednisone is used as an antitumor drug. It is important in the treatment of acute lymphoblastic leukemia, non-Hodgkin lymphomas, Hodgkin's lymphoma, multiple myeloma, and other hormone-sensitive tumors, in combination with other anticancer drugs.

Prednisone is also used for the treatment of the Herxheimer reaction, which is common during the treatment of syphilis. Prednisone is also used to delay the onset of symptoms of Duchenne muscular dystrophy and uveitis. The mechanism for the delay of symptoms is unknown. Because it suppresses the adrenal glands, it is the primary treatment for autoimmune disease, such as autoimmune hepatitis.

It is also sometimes used in the treatment of congenital adrenal hyperplasia. Prednisone is also used to treat sarcoidosis. Prednisone can be used in the treatment of decompensated heart failure to potentiate renal responsiveness to diuretics, especially in heart failure patients with refractory diuretic resistance with large dose of loop diuretics. In terms of the mechanism of action for this purpose: prednisone, a glucocorticoid, can improve renal responsiveness to atrial natriuretic peptide by increasing the density of natriuretic peptide receptor type A in the renal inner medullary collecting duct, inducing a potent diuresis.

Side effects

Short-term side effects, as with all glucocorticoids, include high blood glucose levels (especially in patients with diabetes mellitus or on other medications that increase blood glucose, such as tacrolimus) and mineralocorticoid effects such as fluid retention. The mineralocorticoid effects of prednisone are minor, which is why it is not used in the management of adrenal insufficiency, unless a more potent mineralocorticoid is administered concomitantly.

It can also cause depression or depressive symptoms and anxiety in some individuals.

Long-term side effects include Cushing's syndrome, steroid dementia syndrome, truncal weight gain, osteoporosis, glaucoma and cataracts, diabetes mellitus type 2, and depression upon dose reduction or cessation.

Major

• Increased blood sugar for diabetics
• Difficulty controlling emotion
• Difficulty in maintaining train of thought
• Weight gain
• Immunosuppression
• Facial swelling. Severe.
• Depression, mania, psychosis, or other psychiatric symptoms
• Unusual fatigue or weakness
• Mental confusion / indecisiveness
• Memory and attention dysfunction (Steroid dementia syndrome)
• Blurred vision
• Abdominal pain
• Peptic ulcer
• Painful hips or shoulders
• Steroid-induced osteoporosis
• Stretch marks
• Osteonecrosis – same as avascular necrosis
• Insomnia
• Severe joint pain
• Cataracts or glaucoma
• Anxiety
• Black stool
• Stomach pain or bloating
• Severe swelling
• Mouth sores or dry mouth
• Avascular necrosis
• Hepatic steatosis

Minor

• Nervousness
• Acne
• Skin rash
• Appetite gain
• Hyperactivity
• Increased thirst
• Frequent urination
• Diarrhea
• Reduced intestinal flora
• Leg pain/cramps
• Sensitive teeth

Dependency

Adrenal suppression will begin to occur if prednisone is taken for longer than seven days. Eventually, this may cause the body to temporarily lose the ability to manufacture natural corticosteroids (especially cortisol), which results in dependence on prednisone. For this reason, prednisone should not be abruptly stopped if taken for more than seven days; instead, the dosage should be gradually reduced. This weaning process may be over a few days, if the course of prednisone was short, but may take weeks or months if the patient had been on long-term treatment. Abrupt withdrawal may lead to an Addison crisis. For those on chronic therapy, alternate-day dosing may preserve adrenal function and thereby reduce side effects.

Glucocorticoids act to inhibit feedback of both the hypothalamus, decreasing corticotropin-releasing hormone [CRH], and corticotrophs in the anterior pituitary gland, decreasing the amount of adrenocorticotropic hormone [ACTH]. For this reason, glucocorticoid analogue drugs such as prednisone down-regulate the natural synthesis of glucocorticoids. This mechanism leads to dependence in a short time and can be dangerous if medications are withdrawn too quickly. The body must have time to begin synthesis of CRH and ACTH and for the adrenal glands to begin functioning normally again.

Withdrawal

The magnitude and speed of dose reduction in corticosteroid withdrawal should be determined on a case-by-case basis, taking into consideration the underlying condition being treated, and individual patient factors such as the likelihood of relapse and the duration of corticosteroid treatment. Gradual withdrawal of systemic corticosteroids should be considered in those whose disease is unlikely to relapse and have:

• received more than 40 mg prednisolone (or equivalent) daily for more than 1 week
• been given repeat doses in the evening;
• received more than 3 weeks' treatment
• recently received repeated courses (particularly if taken for longer than 3 weeks)
• taken a short course within 1 year of stopping long-term therapy
• other possible causes of adrenal suppression

Systemic corticosteroids may be stopped abruptly in those whose disease is unlikely to relapse and who have received treatment for 3 weeks or less and who are not included in the patient groups described above.

During corticosteroid withdrawal, the dose may be reduced rapidly down to physiological doses (equivalent to prednisolone 7.5 mg daily) and then reduced more slowly. Assessment of the disease may be needed during withdrawal to ensure that relapse does not occur.

Pharmacology

Prednisone has no substantial biological effects until converted via hepatic metabolism to prednisolone.

Industry

Prednisone 20 mg oral tablet

The pharmaceutical industry uses prednisone tablets for the calibration of dissolution testing equipment according to the United States Pharmacopeia (USP).

History

The first isolation and structure identifications of prednisone and prednisolone were done in 1950 by Arthur Nobile. The first commercially feasible synthesis of prednisone was carried out in 1955 in the laboratories of Schering Corporation, which later became Schering-Plough Corporation, by Arthur Nobile and coworkers. They discovered that cortisone could be microbiologically oxidized to prednisone by the bacterium Corynebacterium simplex. The same process was used to prepare prednisolone from hydrocortisone.

The enhanced adrenocorticoid activity of these compounds over cortisone and hydrocortisone was demonstrated in mice.

Prednisone and prednisolone were introduced in 1955 by Schering and Upjohn, under the brand names Meticorten and Delta-Cortef, respectively. These prescription medicines are now available from a number of manufacturers as generic drugs.

See also

• Chloroprednisone

References

Further reading

• Tsang, Sue Y.; Garovoy, Marvin R.; Benet, Leslie Z. (1985). "Immunosuppressive activity of prednisone and prednisolone and their metabolic interconversion in the mixed lymphocyte reaction". International Journal of Immunopharmacology. 7 (5): 731–737. doi:10.1016/0192-0561(85)90159-6. PMID 2931388. 

External links

• Kelly, Janis (July 2000). "Prednisone-related growth impairment persists in children with CF". Respiratory Reviews. 5 (7). 
• National Inventors Hall of Fame induction of Arthur Nobile
• U.S. National Library of Medicine: Drug Information Portal – Prednisone
• The National Center for Biotechnology Information: Prednisone

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

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English Journal

• Formulation Optimization of Freeze-Dried Long-Circulating Liposomes and In-Line Monitoring of the Freeze-Drying Process using an NIR Spectroscopy Tool.

• Sylvester B1, Porfire A1, Van Bockstal PJ2, Porav S3, Achim M1, Beer T2, Tomuță I4.
• Journal of pharmaceutical sciences.J Pharm Sci.2017 May 24. pii: S0022-3549(17)30381-7. doi: 10.1016/j.xphs.2017.05.024. [Epub ahead of print]
• PMID 28551424

• First in vivo MRI study on theranostic dendrimersomes.

• Filippi M1, Catanzaro V2, Patrucco D3, Botta M4, Tei L5, Terreno E6.
• Journal of controlled release : official journal of the Controlled Release Society.J Control Release.2017 Feb 28;248:45-52. doi: 10.1016/j.jconrel.2017.01.010. Epub 2017 Jan 7.
• PMID 28069551

• Promote Recurrent Aphthous Ulcer Healing with Low Dose Prednisolone Bilayer Mucoadhesive Buccal Film.

• Farid RM1, Wen MM.
• Current drug delivery.Curr Drug Deliv.2017;14(1):123-135. doi: 10.2174/1567201813666160316122548.
• PMID 26980427

Japanese Journal

• 肩関節拘縮に対するステロイド治療

• 永澤 雷太
• 肩関節 35(3), 975-978, 2011
• … We administered an injection of triamcinolone acetonide or dexamethasone sodium phosphate into the gleno-humeral joint. … We also prescribed prednisolone and NSAIDs for the inflammation. …
• NAID 130002103668

• ステロイド製剤により過敏性反応を呈したベル麻痺例

• 山村 一彦,森田 一郎,甲斐 智朗 [他],堀内 正敏
• 耳鼻咽喉科臨床 100(9), 757-760, 2007-09-01
• … A 40-year-old male consulted our out-patient clinic due to right peripheral facial palsy.As soon as he was injected with the hydrocortisone sodium succinate, he developed erythema all over his body, moderate itchiness and respiratory distress. … His condition was improved immediately after the cessation of infusion.The medication for facial palsy was altered from infusion to oral prednisolone. …
• NAID 10019531269

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★リンクテーブル★

リンク元	「prednisolone sodium succinate」「prednisolone farnesylate」「prednisolone succinate」「リン酸プレドニゾロンナトリウム」「PEDIAPRED」
関連記事	「phosphate」

「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

「prednisolone farnesylate」

　　[★]

• ファルネシル酸プレドニゾロン

関

prednisolone、prednisolone acetate、prednisolone sodium phosphate、prednisolone sodium succinate、prednisolone succinate、prednisolone tebutate、prednisolone valerate acetate

「prednisolone succinate」

　　[★]

• コハク酸プレドニゾロン

関

prednisolone、prednisolone acetate、prednisolone farnesylate、prednisolone sodium phosphate、prednisolone sodium succinate、prednisolone tebutate、prednisolone valerate acetate

「リン酸プレドニゾロンナトリウム」

　　[★]

英

prednisolone sodium phosphate

関

プレドニゾロン

「PEDIAPRED」

　　[★]

関

prednisolone sodium phosphate

「phosphate」

　　[★]

• n.

• (化合物)リン酸塩、リン酸エステル、ホスフェート、フォスフェート、リン酸

関

inorganic phosphate、orthophosphate、orthophosphoric acid、phospho、phosphoester、phosphoric、phosphoric acid、phosphoric acid ester、phosphorus