Prednisolone

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Prednisolone
Systematic (IUPAC) name
(11β)-11,17,21-trihydroxypregna-1,4-diene-3,20-dione
Identifiers
CAS number	50-24-8
ATC code	A07EA01 C05AA04, D07AA03, D07XA02, H02AB06, R01AD02, S01BA04, S01CB02, S02BA03, S03BA02
PubChem	5755
DrugBank	APRD00197
ChemSpider	5552
Chemical data
Formula	C₂₁H₂₈O₅
Mol. mass	360.444 g/mol
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
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	2-3 hours
Excretion	Prednisolone is excreted via urine
Therapeutic considerations
Pregnancy cat.	A(AU) C(US)
Legal status	POM(UK) ℞-only(US)
Routes	?

Prednisolone is the active metabolite of prednisone.^[1]

[edit] Uses

Prednisolone is a corticosteroid drug with predominantly glucocorticoid and low mineralocorticoid activity, making it useful for the treatment of a wide range of inflammatory and auto-immune conditions^[2] such as asthma^[3], uveitis, rheumatoid arthritis, ulcerative colitis and Crohn's disease, Bell's palsy, multiple sclerosis^[4], cluster headaches, systemic lupus erythematosus, acute lymphoblastic leukemia^[5] and Dermatomyositis.

It can also be used as an immunosuppressive drug for organ transplants and in cases of adrenal insufficiency (Addison's). Prednisolone acetate ophthalmic suspension is an adrenocortical steroid product, prepared as a sterile ophthalmic suspension and used to reduce swelling, redness, itching, and allergic reactions affecting the eye.

Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation with inflammation.

There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A₂ inhibitory proteins, collectively called lipocortins (annexins). It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A₂. Corticosteriods are capable of producing a rise in intraocular pressure.

[edit] Adverse effects

Possible side effects include fluid retention of the face (moon face, Cushing's syndrome), acne, constipation, and mood swings.

A lengthy course of prednisolone can cause bloody or black tarry stools; filling or rounding out of the face; muscle cramps or pain; muscle weakness; nausea; pain in back, hips, ribs, arms, shoulders, or legs; reddish-purple lines on arms, face, legs, trunk or groin; thin and shiny skin; unusual bruising; urinating at night; rapid weight gain; and wounds that will not heal.

Swelling of the pancreas has also been reported.

Prednisolone can cause increased blood sugar levels for diabetics.

Other effects include decreased or blurred vision, increased eye pressure, increased thirst, confusion, rare cases of dementia in otherwise healthy elderly patients and nervousness.

It also is reported to cause insomnia when taken.

[edit] Banned status in athletics

As a glucocorticosteroid, prednisolone is banned under WADA anti-doping rules.

[edit] 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. PMID 656293.
^ Czock D, Keller F, Rasche FM, Häussler U. Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. Review. PMID: 15634032
^ Fiel SB, Vincken W. Systemic corticosteroid therapy for acute asthma exacerbations. J Asthma. 2006 Jun-Jul;43(5):321-31. Review. PMID: 16801135
^ Thrower BW. Relapse management in multiple sclerosis. Neurologist. 2009 Jan;15(1):1-5. Review. PMID: 19131851
^ Lambrou GI, Vlahopoulos S, Papathanasiou C, Papanikolaou M, Karpusas M, Zoumakis E, Tzortzatou-Stathopoulou F. Prednisolone exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells: Relation to early gene expression. Leuk Res. 2009 May 16. [Epub ahead of print] PMID: 19450877

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[Davis-0] 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. PMID 656293.

[1] Czock D, Keller F, Rasche FM, Häussler U. Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. Review. PMID: 15634032

[2] Fiel SB, Vincken W. Systemic corticosteroid therapy for acute asthma exacerbations. J Asthma. 2006 Jun-Jul;43(5):321-31. Review. PMID: 16801135

[3] Thrower BW. Relapse management in multiple sclerosis. Neurologist. 2009 Jan;15(1):1-5. Review. PMID: 19131851

[4] Lambrou GI, Vlahopoulos S, Papathanasiou C, Papanikolaou M, Karpusas M, Zoumakis E, Tzortzatou-Stathopoulou F. Prednisolone exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells: Relation to early gene expression. Leuk Res. 2009 May 16. [Epub ahead of print] PMID: 19450877

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Prednisolone

From Wikipedia, the free encyclopedia

Contents

[edit] Uses

[edit] Adverse effects

[edit] Banned status in athletics

[edit] References

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