Prednisolone

Prednisolone is a steroid medication used to treat certain types of allergies, inflammatory conditions, autoimmune disorders, and cancers.[2][3] Some of these conditions include adrenocortical insufficiency, high blood calcium, rheumatoid arthritis, dermatitis, eye inflammation, asthma, and multiple sclerosis.[3] It is used by mouth, injection into a vein, as a skin cream, and as eye drops.[4][5][3]

Not to be confused with Prednisone.

Prednisolone
Clinical data
Trade namesOrapred, PediaPred, Millipred, others
Other names11,17-Dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydrocyclopenta[a] phenanthren-3-one
AHFS/Drugs.comMonograph
MedlinePlusa615042
License data
Pregnancy
category
    Routes of
    administration    		By mouth, intravenous, topical, eye drop
    ATC code
    Legal status
    Legal status
    • UK: POM (Prescription only)
    • US: ℞-only
    • In general: ℞ (Prescription only)
    Pharmacokinetic data
    Elimination half-life2–3 hours
    Excretionurine
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.000.020
    Chemical and physical data
    FormulaC21H28O5
    Molar mass360.444 g/mol g·mol−1
    3D model (JSmol)
      (verify)

    Side effects with short-term use include nausea and feeling tired.[2] More severe side effects include psychiatric problems, which may occur in about 5% of people.[6] Common side effects with long term use include bone loss, weakness, yeast infections, and easy bruising.[3] While short-term use in the later part of pregnancy is safe, long-term use or use in early pregnancy is occasionally associated with harm to the baby.[1] It is a glucocorticoid made from hydrocortisone (cortisol).[7]

    Prednisolone was discovered and approved for medical use in 1955.[7] It is on the World Health Organization's List of Essential Medicines, the safest and most effective medicines needed in a health system.[8] It is available as a generic medication.[3] The wholesale cost in the developing world is about US$0.01 per 5 mg tablet.[9] In 2017, it was the 129th most commonly prescribed medication in the United States, with more than five million prescriptions.[10][11]

    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[12] such as asthma,[13] uveitis, pyoderma gangrenosum, rheumatoid arthritis, urticaria,[14] angioedema,[14] ulcerative colitis, pericarditis, temporal arteritis and Crohn's disease, Bell's palsy, multiple sclerosis,[15] cluster headaches, vasculitis, acute lymphoblastic leukemia and autoimmune hepatitis,[16] systemic lupus erythematosus, Kawasaki disease,[17] dermatomyositis,[4] and sarcoidosis.[18]

    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.[19][5][20] It has been explored as a treatment option for bacterial keratitis.[21]

    Prednisolone can also be used for allergic reactions ranging from seasonal allergies to drug allergic reactions.[22]

    Prednisolone can also be used as an immunosuppressive drug for organ transplants.[4][23]

    Prednisolone in lower doses can be used in cases of primary adrenal insufficiency (Addison's disease).[24][25]

    Corticosteroids inhibit the inflammatory response to a variety of inciting agents and, it is presumed, delay or slow healing.[26] They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation with inflammation.[27]

    Adverse effects

    Adverse reactions from the use of prednisolone include:[28][4]

    • Increased appetite, weight gain, nausea, and malaise
    • Increased risk of infection
    • Cardiovascular events
    • 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 increased 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, increased 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/muscle loss, osteoporosis (see steroid-induced osteoporosis), long bone fractures, tendon rupture, and back fractures
    • Neurological effects, including involuntary movements (convulsions), headaches, and vertigo
    • Behavioral disturbances [29]
    • Nasal septum perforation and bowel perforation (in some pathologic conditions).[30][31]

    Withdrawal from prednisolone after long-term or high-dose use can lead to adrenal insufficiency.[29]

    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.[29]

    Pharmacology

    As a glucocorticoid, the lipophilic structure of prednisolone 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 blocks the transcription of inflammatory genes.[32]

    Chemistry

    Prednisolone is a synthetic pregnane corticosteroid closely related to its cognate prednisone, having identical structure save for two fewer hydrogens near C11. It is also known as δ1-cortisol, δ1-hydrocortisone, 1,2-dehydrocortisol, or 1,2-dehydrohydrocortisone, as well as 11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione.[33][34]

    Society and culture

    Dosage forms

    In the United States:

    • Prednisolone sodium phosphate oral solution (Pediapred)[29]
    • Prednisolone acetate oral suspension (Flo-Pred)[28]
    • Prednisolone oral tablets (Millipred)[22]
    • Prednisolone sodium phosphate oral dissolving tablets (Orapred ODT)[4]
    • Prednisolone acetate ophthalmic suspension (Omnipred, Pred Forte)[5][19][20]

    Athletics

    As a glucocorticosteroid, unauthorized or ad-hoc use of prednisolone during competition via oral, intravenous, intramuscular or rectal routes is banned under World Anti-Doping Agency (WADA) anti-doping rules.[35]

    Veterinary uses

    Prednisolone is used in the treatment of inflammatory and allergic conditions in cats, dogs, and ferrets.

    See also

    References
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