Prednisone
Clinical data | |
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Trade names | Deltasone, Liquid Pred, Orasone, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a601102 |
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Pregnancy category |
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Routes of administration | By mouth |
ATC code | |
Legal status | |
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Pharmacokinetic data | |
Bioavailability | 70% |
Metabolism | prednisolone (liver) |
Elimination half-life | 3 to 4 hours in adults. 1 to 2 hours in children[2] |
Excretion | Kidney |
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JSmol) | |
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Prednisone is a
Common side effects may include
Prednisone is a prodrug and must be converted to prednisolone by the liver before it becomes active.[6][7] Prednisolone then binds to glucocorticoid receptors, activating them and triggering changes in gene expression.[4]
Prednisone was patented in 1954 and approved for medical use in the United States in 1955.
Medical uses
Prednisone is used for many different
Prednisone has also been used in the treatment of
Prednisone is often also prescribed as a form of treatment for sudden sensorineural hearing loss (SSNHL).[17]
Prednisone can be used in the treatment of decompensated heart failure to increase renal responsiveness to diuretics, especially in heart failure patients with refractory diuretic resistance with large doses of loop diuretics.[18][19][20][21][22][23] 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, thereby inducing a potent diuresis.[24]
At high doses it may be used to prevent rejection following organ transplant.[3]
Side effects
Short-term side effects, as with all glucocorticoids, include high blood
It can also cause depression or depressive symptoms and anxiety in some individuals.[26][27]
Long-term side effects include
When used as treatment for sudden deafness or sudden sensorineural hearing loss, it can cause or exacerbate tinnitus or a ringing in the ears.[33][unreliable medical source?]
Major
Source:[25]
- Steroid myopathy
- Increased blood sugar for individuals with diabetes
- Difficulty in regulating emotion
- Difficulty in maintaining linear thinking
- Weight gain due to increased appetite
- Immunosuppression
- central obesity)
- Depression, mania, psychosis, or other psychiatric symptoms
- Unusual fatigue or weakness
- Mental confusion
- Memory and attention dysfunction (steroid dementia syndrome)
- Muscle atrophy[34]
- Blurred vision
- Abdominal pain
- Peptic ulcer
- Painful 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
- dry mouth
- Avascular necrosis
- Hepatic steatosis
- hiccups and burping
- weakening and breakage of tendons
Minor
Source:[25]
- Nervousness
- Acne
- Skin rash
- Appetite gain
- Hyperactivity
- Increased thirst
- Frequent urination
- Diarrhea
- Reduced intestinal flora
- Leg pain/cramps
- Sensitive teeth
- Headache
- Induced vomiting
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[35] if the patient had been on long-term treatment. Abrupt withdrawal may lead to an Addisonian crisis. For those on chronic therapy, alternate-day dosing may preserve adrenal function and thereby reduce side effects.[36]
Glucocorticoids act to inhibit feedback of both the
Prednisone may start to result in the suppression of the hypothalamic-pituitary-adrenal (HPA) axis if used at doses 7–10 mg or higher for several weeks. This is approximately equal to the amount of endogenous cortisol produced by the body every day. As such, the HPA axis starts to become suppressed and atrophy. If this occurs the patient should be tapered off prednisone slowly to give the adrenal gland enough time to regain its function and endogenous production of steroids.
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 prednisone (or equivalent) daily for more than one week
- been given repeat doses in the evening
- received more than three weeks of treatment
- recently received repeated courses (particularly if taken for longer than three weeks)
- taken a short course within one 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 three 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.[37]
Pharmacology
Prednisone is a synthetic glucocorticoid used for its anti-inflammatory and immunosuppressive properties.[38][39] Prednisone is a prodrug; it is metabolised in the liver by 11-β-HSD to prednisolone, the active drug. Prednisone has no substantial biological effects until converted via hepatic metabolism to prednisolone.[40]
Pharmacokinetics
Prednisone is absorbed in the gastrointestinal tract and has a half-life of 2–3 hours.[39] it has a volume of distribution of 0.4–1 L/kg.[41] The drug is cleared by hepatic metabolism using cytochrome P450 enzymes. Metabolites are excreted in the bile and urine.[41]
Lodotra
"Lodotra" is the brand name of an oral formulation, which releases prednisone four hours after ingestion. It is indicated for rheumatoid arthritis with morning stiffness. Taken at 10 p.m., it releases the drug at around 2 a.m. The plasmic peak level is reached at 4 a.m., which is considered to be the optimal time for relieving morning stiffness. The drug was approved in the European Union, in January 2009.[42][43]
Industry
The pharmaceutical industry uses prednisone tablets for the calibration of dissolution testing equipment according to the United States Pharmacopeia (USP).
Chemistry
Prednisone is a
History
The first isolation and structure identifications of prednisone and prednisolone were done in 1950 by Arthur Nobile.[46][47][48] 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.[49] 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.[50]
The enhanced adrenocorticoid activity of these compounds over cortisone and hydrocortisone was demonstrated in mice.[50]
Prednisone and prednisolone were introduced in 1955 by Schering and Upjohn, under the brand names Meticorten[51] and Delta-Cortef,[52] respectively.
References
- ^ "Product monograph brand safety updates". Health Canada. 7 July 2016. Retrieved 3 April 2024.
- S2CID 12218704.
- ^ a b c d e f g h i "Prednisone Monograph for Professionals". Drugs.com. AHFS. Retrieved 24 December 2018.
- ^ ISBN 978-1-25-958473-2.
- ^ "Prednisone Use During Pregnancy". Drugs.com. Retrieved 24 December 2018.
- ^ "Product Information Panafcort (prednisone) Panafcortelone (prednisolone)" (PDF). TGA eBusiness Services. St Leonards, Australia: Aspen Pharmacare Australia Pty Ltd. 11 July 2017. pp. 1–2. Retrieved 30 June 2018.
- S2CID 22720230.
- ISBN 9783527607495.
- hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
- ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Prednisone - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
- ^ Autoimmune Hepatitis~treatment at eMedicine
- )
- ^ "Prednisone". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.
- ISBN 9781607951773.
- ^ "Antineoplastic Agents, Hormonal". Medical Subject Headings. U.S. National Library of Medicine. 2009. Retrieved 11 November 2010.
- ^ "Steroid Treatments Equally Effective Against Sudden Deafness". National Institutes of Health (NIH). 22 May 2015. Retrieved 9 May 2022.
- PMID 13520608.
- PMID 13632954.
- PMID 18971570.
- PMID 17876376.
- S2CID 45800521.
- PMID 21406321.
- S2CID 1892149.
- ^ a b c "Prednisone and other corticosteroids: Balance the risks and benefits". Mayo Clinic. Retrieved 7 April 2017.
- ^ "Prednisone Information". Drugs.com.
- ^ "Prednisone". MedlinePlus Drug Information.
- S2CID 39340010.
- ^ "Steroids". Australian Department of Health & Human Services. April 2016. Retrieved 14 June 2018.
- S2CID 251774691. Retrieved 5 August 2022.
- PMID 34988356.
- ISBN 9780781748117.
- ^ "The Prednisone Tinnitus Connection". Tinnitus and You. 12 June 2021. Retrieved 9 May 2022.
- S2CID 21997662.
- ^ "Steroid Drug Withdrawal Symptoms, Treatment & Prognosis". MedicineNet. Retrieved 14 June 2018.
- ^ Bello CS, Garrett SD. "Therapeutic and Adverse Effects of Glucocorticoids". U.S. Pharmacist Continuing Education Program. Archived from the original on 11 July 2008.
- S2CID 72082017.
- PMID 23506281.
- ^ a b "Prednisone". DrugBank. Retrieved 29 January 2019.
- ^ "Prednisone". MedlinePlus. NIH U.S. National Library of Medicine.
- ^ PMID 29549463.
- ^ Wan Y (8 January 2009). "Delayed-release prednisone (Lodotra™) approved in EU for treatment of rheumatoid arthritis". Archived from the original on 9 July 2009. Retrieved 22 November 2009.
- S2CID 6197980.
- ISBN 978-1-4757-2085-3.
- ISBN 978-3-88763-075-1.
- OCLC 106716069.
- ^ "Inventor Profile: Arthur Nobile". National Inventors Hall of Fame. Archived from the original on 12 June 2012.
- ^ "Arthur Nobile". New Jersey Inventors Hall of Fame. Archived from the original on 1 September 2011.
- ISBN 978-0-911910-00-1.
- ^ PMID 13225767.
- ^ "Meticorten: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA).
- ^ "Delta-Cortef: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA).