Prednisone is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, prednisone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations.
Mechanism of Action of Prednisone
Prednisone is a glucocorticoid receptor agonist. It is first metabolized in the liver to its active form, prednisolone. Prednisolone crosses cell membranes and binds with high affinity to specific cytoplasmic receptors. The result includes inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The anti-inflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Prednisone can stimulate secretion of various components of gastric juice. Suppression of the production of corticotropin may lead to suppression of endogenous corticosteroids. Prednisone has slight mineralocorticoid activity, whereby entry of sodium into cells and loss of intracellular potassium is stimulated. This is particularly evident in the kidney, where rapid ion exchange leads to sodium retention and hypertension.
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In physiologic doses, corticosteroids are administered to replace deficient endogenous hormones. In larger (pharmacologic) doses, glucocorticoids decrease inflammation by stabilizing leukocyte lysosomal membranes, preventing release of destructive acid hydrolases from leukocytes; inhibiting macrophage accumulation in inflamed areas; reducing leukocyte adhesion to capillary endothelium; reducing capillary wall permeability and edema formation; decreasing complement components; antagonizing histamine activity and release of kinin from substrates; reducing fibroblast proliferation, collagen deposition, and subsequent scar tissue formation; and possibly by other mechanisms as yet unknown. The drugs suppress the immune response by reducing activity and volume of the lymphatic system, producing lymphocytopenia, decreasing immunoglobulin and complement concentrations, decreasing passage of immune complexes through basement membranes, and possibly by the depressing reactivity of tissue to antigen-antibody interactions. Glucocorticoids stimulate erythroid cells of bone marrow, prolong survival time of erythrocytes and platelets, and produce neutrophilia and eosinopenia. Glucocorticoids promote gluconeogenesis, redistribution of fat from peripheral to central areas of the body, and protein catabolism, which results in negative nitrogen balance. They reduce intestinal absorption and increase renal excretion of calcium.
Indications of Prednisone
Most common or FDA approved uses are listed.
- Inflammatory Conditions
- Asthma
- Allergic Reactions
- Acute Lymphocytic Leukemia
- Rheumatoid Arthritis
- Adrenocortical Insufficiency
- Adrenogenital Syndrome
- Allergic Rhinitis
- Ankylosing Spondylitis
- Aspiration Pneumonia
- Atopic Dermatitis
- Autoimmune Hemolytic Anemia
- Berylliosis
- Bullous Pemphigoid
- Bursitis
- COPD
- Chorioretinitis
- Cluster Headaches
- Cogan’s Syndrome
- Conjunctivitis, Allergic
- Corneal Ulcer
- Dermatitis Herpetiformis
- Dermatomyositis
- Diffuse Large B-Cell Lymphoma
- Eczema
- Epicondylitis, Tennis Elbow
- Erythroblastopenia
- Fibromyalgia
- Gouty Arthritis
- Graft-versus-host disease
- Atopic Dermatitis (AD)
- Bell’s Palsy
- Berylliosis
- Bullous dermatitis herpetiformis
- Congenital Adrenal Hyperplasia (CAH)
- Congenital Hypoplastic Anemia
- Herpes Zoster
- Herpes Zoster Iridocyclitis
- Hypercalcemia of Malignancy
- Idiopathic Thrombocytopenic Purpura
- Immunosuppression
- Inflammatory Bowel Disease
- Iridocyclitis
- Iritis
- Juvenile Rheumatoid Arthritis
- Keratitis
- Leukemia
- Lymphoma
- Mixed Connective Tissue Disease
- Multiple Sclerosis
- Mycosis Fungoides
- Nephrotic Syndrome
- Neurosarcoidosis
- Osteoarthritis
- Pemphigoid
- Pemphigus
- Pharyngitis
- Polymyositis/Dermatomyositis
- Psoriasis
- Psoriatic Arthritis
- Ramsay Hunt Syndrome
- Sarcoidosis
- Scleroderma
- Seborrheic Dermatitis
- Sinusitis
- Skin Rash
- Synovitis
- Systemic Lupus Erythematosus
- Systemic Sclerosis
- Thrombocytopenia
- Toxic Epidermal Necrolysis
- Tuberculosis
- Tuberculous Meningitis
- Ulcerative Colitis
- Uveitis, Posterior
- Crohn’s disease
- Systemic lupus
- Allergic reactions
- Asthma
- Severe psoriasis
- Symptomatic Sarcoidosis
- Synovitis of osteoarthritis
- Systemic Dermatomyositis
- Varicella-zoster virus acute retinal necrosis
It also is used the treatment of
- Leukemias
- Lymphomas
- Idiopathic thrombocytopenic purpura
- Autoimmune hemolytic anemia
- Bronchitis
FDA Approval: Indications of Prednisone
- Prednisone is approved to be used to reduce inflammation and suppress (lower) the body’s immune response. It is used with other drugs to treat the following types of cancer: Acute lymphoblastic leukemia.
- Chronic lymphocytic leukemia.
- Hodgkin lymphoma.
- Mycosis fungoides.
- Non-Hodgkin lymphoma.
- Prednisone is also used alone or with other drugs to prevent or treat the following conditions related to cancer: Anemia.
- Drug hypersensitivity (allergic reactions).
- Hypercalcemia (high blood levels of calcium).
- Thrombocytopenia (low platelet levels).
- Prednisone is also used alone or with other drugs to treat many other diseases and conditions. The drug continues to be studied in the treatment of many types of cancer and other conditions.
Therapeutic Indications of Prednisone
- Prednisone is usually considered the oral glucocorticoid of choice for anti-inflammatory or immunosuppressant effects. Because it has only minimal mineralocorticoid properties, the drug is inadequate alone for the management of adrenocortical insufficiency. If prednisone is used in the treatment of this condition, concomitant therapy with a mineralocorticoid is also required.
- Prednisone tablets and solutions are indicated in the following conditions: Endocrine Disorders: Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the first choice: synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy mineralocorticoid supplementation is of particular importance); congenital adrenal hyperplasia; hypercalcemia associated with cancer; nonsuppurative thyroiditis.
- Prednisone tablets and solutions are indicated in the following conditions: Rheumatic Disorders: As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in: psoriatic arthritis, rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy), ankylosing spondylitis, acute and subacute bursitis, acute nonspecific tenosynovitis, acute gouty arthritis, post-traumatic osteoarthritis, synovitis of osteoarthritis, epicondylitis.
- Prednisone tablets and solutions are indicated in the following conditions: Collagen Diseases: During an exacerbation or as maintenance therapy in selected cases of systemic lupus erythematosus, systemic dermatomyositis (polymyositis), acute rheumatic carditis.
- Prednisone tablets and solutions are indicated in the following conditions: Dermatologic Diseases: Pemphigus; bullous dermatitis herpetiformis; severe erythema multiforme (Stevens-Johnson syndrome); exfoliative dermatitis; mycosis fungoides; severe psoriasis; severe seborrheic dermatitis.
- Prednisone tablets and solutions are indicated in the following conditions: Allergic States: Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment: seasonal or perennial allergic rhinitis; bronchial asthma; contact dermatitis; atopic dermatitis; serum sickness; drug hypersensitivity reactions.
- Prednisone tablets and solutions are indicated in the following conditions: Ophthalmic Diseases: Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as: allergic corneal marginal ulcers, herpes zoster ophthalmicus, anterior segment inflammation, diffuse posterior uveitis and choroiditis, sympathetic ophthalmia, allergic conjunctivitis, keratitis, chorioretinitis, optic neuritis, iritis and iridocyclitis.
- Prednisone tablets and solutions are indicated in the following conditions: Respiratory Diseases: Symptomatic sarcoidosis; Loeffler’s syndrome not manageable by other means; berylliosis; fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy; aspiration pneumonitis.
- Prednisone tablets and solutions are indicated in the following conditions: Hematologic Disorders: Idiopathic thrombocytopenic purpura in adults; secondary thrombocytopenia in adults; acquired (autoimmune) hemolytic anemia; erythroblastopenia (RBC anemia); congenital (erythroid) hypoplastic anemia.
- Prednisone tablets and solutions are indicated in the following conditions: Neoplastic Diseases: For palliative management of leukemias and lymphomas in adults, acute leukemia of childhood.
- Prednisone tablets and solutions are indicated in the following conditions: Edematous States: To induce a diuresis or remission of proteinuria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus.
- Prednisone tablets and solutions are indicated in the following conditions: Gastrointestinal Diseases: To tide the patient over a critical period of the disease in ulcerative colitis.
- Prednisone tablets and solutions are indicated in the following conditions: Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculous chemotherapy; trichinosis with neurologic or myocardial involvement.
- Systemic glucocorticoids have been used to reduce the pain, fever, and inflammation of pericarditis, including that associated with myocardial infarction.
- Systemic conventional glucocorticoids (e.g., prednisone ) have been used in pediatric patients with mild esophageal or gastroduodenal Crohn’s disease. In addition, glucocorticoids (e.g., prednisone or methylprednisolone ) are recommended for the management of moderately to severely active Crohn’s disease, in children.
- Glucocorticoids (e.g., prednisone) are used in the management of myasthenia gravis, usually in patients who have had an inadequate response to anticholinesterase therapy.
- Glucocorticoid therapy has been used as an adjunct to anti-infective therapy in the treatment of anthrax in an attempt to ameliorate toxin-mediated effects associated with Bacillus anthracis infections. Some experts suggest that glucocorticoids may be indicated in the treatment of cutaneous anthrax if there are signs of systemic involvement or extensive edema involving the neck and thoracic region. Glucocorticoid therapy also has been used as an adjunct in the treatment of anthrax meningitis.
Contra-Indications of Prednisone
Depending on the indication and the general situation, peptic ulcers, osteoporosis, psychoses, infections, diabetes, and hypertension can represent contraindications.
- Serious infections
- Herpetic eye infections
- Hypersensitivity to the Prednisone
- HBsAg-positive chronic active hepatitis
- Two months before and fourteen days after prophylactic vaccination
- Herpes simplex infection
- Herpes zoster infection
- Other viral infections
- Ulcers in the stomach and duodenum
- Acute and chronic bacterial infections
- Fungal infections affecting the skin and internal organs
- Infections caused by parasites
- Unstable hypertension
- Osteoporosis
- Neuropsychiatric disorders
- Glaucoma
- Diverticulitis
- Cushing’s disease
Dosage of Prednisone
Strengths: 1 mg, 2.5 mg, 5 mg, 10 mg, 20 mg, 50 mg
Rheumatoid Arthritis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.
Gouty Arthritis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.
Psoriatic Arthritis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.
Ankylosing Spondylitis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Osteoarthritis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.
Psoriasis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.
Asthma
- Short-course “burst” therapy: 40 to 80 mg orally once a day or in 2 divided doses until peak expiratory flow (PEF) reaches 70% of predicted or personal best
- For OUTPATIENT “burst” therapy: 40 to 60 mg orally once a day or in 2 divided doses for a total of 5 to 10 days
Aspiration Pneumonia
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained
Hemolytic Anemia
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Rheumatic Heart Disease
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Immunosuppression
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained
Ulcerative Colitis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained
Adrenocortical Insufficiencyency
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained
Iritis
- Initial dose: 5 to 60 mg orally per day
Allergic Reaction
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Bursitis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Synovitis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Dermatitis Herpetiformis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.
Hypercalcemia of Malignancy
- Initial dose: 5 to 60 mg orally per day
Thrombocytopenic Purpura
- Initial dose: 5 to 60 mg orally per day
Pediatric
Ankylosing Spondylitis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Pediatric Aspiration Pneumonia
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Bursitis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain initial dose until a satisfactory response is obtained;
Hypercalcemia of Malignancy
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Osteoarthritis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained
Psoriasis
- Initial dose: 5 to 60 mg orally per day
- Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;
Side Effects of Prednisone
The most common
- heartburn or indigestion (severe and continuous)
- Fluid retention
- Weight gain,
- Mouth sores,
- Drying of the skin
- Change in skin color
- Diarrhea
- Any signs of infection, or a skin rash.
- Stomach pain, especially if it comes along with fever and diarrhea or constipation
- Yellowing of the skin or eyes
- Loss of appetite
- Constipation
- Sleepiness or unusual drowsiness
- Clumsiness or unsteadiness
- Dizziness
- Drowsiness
- Dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- Headache.
- Skin rashes.
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Jaundice.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Rare
- agitation
- anxiety
- behavioral changes, including aggressiveness, angry outbursts, bizarre behavior, or decreased inhibitions
- confusion
- increased trouble sleeping
- memory problems
- muscle spasms
- shortness of breath
Drug Interactions of Prednisone
Prednisone may interact with following drugs, supplements, & may change the efficacy of drugs
- abatacept
- anakinra
- Amphotericin B
- Antibiotics
- Anticholinesterase agents such as donepezil, rivastigmine, and galantamine
- Anticoagulants such as warfarin
- Antidiabetic agents
- anti-tumor necrosis factor agents (e.g., adalimumab, etanercept, infliximab, )
- azathioprine
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- beta-blockers (e.g., carvedilol, metoprolol, propranolol)
- carbamazepine
- clonidine
- clozapine
- corticosteroids (e.g.dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- diltiazem
- imatinib
- Estrogens, including oral contraceptives
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- methotrexate
- methyldopa
- mycophenolate
- phenobarbital
- phenytoin
- rituximab
- tacrolimus
- verapamil
- warfarin
- Prednisone may increase the risk of tendon rupture in patients treated with fluoroquinolone type antibiotics. Examples of fluoroquinolones include ciprofloxacin and levofloxacin(Levaquin).
The above list is not the sufficient drugs interactions list, please always consult your doctor or pharmacist before taking this drug.
Pregnancy and Lactation of Prednisone
FDA pregnancy category: D
Prednisone can cause intrauterine growth retardation and cleft palate, and its use during pregnancy is recommended only in situations where the benefits to the mother outweigh the risks to the fetus. Cases of hypoadrenalism (reduced levels of adrenaline in the blood) in newborns have been reported, but symptoms quickly go away without any complications. Cases of cataracts in newborns whose mothers took this drug during pregnancy have been reported.
Lactation and Breastmilk
Published information on the effects of prednisone on serum prolactin or on lactation in nursing mothers was not found as of the revision date. However, medium to large doses of depot corticosteroids injected into joints has been reported to cause temporary reduction of lactation.
