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January 2, 2023
Prednisone
medicaldialogues.in/generics/prednisone-2722820
Indications, Uses, Dosage, Drugs Interactions, Side effects
Prednisone
Medicine Type :
Allopathy
Prescription Type:
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Pharmacological Class:
Corticosteroid,
Therapy Class:
Anti-inflammatory Agent, Antineoplastic agent, Vasoconstrictor,
Prednisone belongs to the pharmacological class of Corticosteroids. Prednisone appears
to have anti-inflammatory Anti-neoplastic and Vasoconstrictive effects .
Prednisone had been approved for relieving symptoms as well as also for the treatment
and maintenance of episodes of blood problems, arthritis, cancer, immune system
problems, eye conditions, breathing problems, allergies etc.
2/14
Prednisone is completely and rapidly absorbed with oral bioavailability of 70%.
Prednisone achieved a steady state volume of distribution of 29.3 L at a dose of about
0.15mg/kg and 44.2L at 0.30mg/kg dose. Prednisone can be reversibly metabolized to
prednisolone and various other metabolites such as 6βhydroxy-prednisone,6α-hydroxy-
prednisone, 17α,21-dihydroxy-pregnan-1,4,6-trien-3,11,30-trione, etc. Prednisone was
found to be excreted in the form of urine in the form of sulfate and glucuronide
conjugates.
The common side effects associated with Prednisone are irregular nausea, headache,
dizziness, menstrual pain, acne, etc.
Prednisone is available in the form of oral soluble tablets and solutions. Prednisone is
available in the U.S., Canada, E.U., India, Australia, and Japan.
Prednisone belongs to the pharmacological class Corticosteroids. Prednisone appears to
have anti-inflammatory, Anti-neoplastic and Vasoconstrictive effects .
Prednisone binds to the glucocorticoid receptor which mediates changes in gene
expression that might lead to multiple downstream effects over hours to days.
Glucocorticoids inhibit demargination and neutrophil apoptosis.They inhibit
phospholipase A2, which further decreases the formation of arachidonic acid derivatives
which in turn inhibits NF-Kappa B and other inflammatory transcription factors. They
also promote anti-inflammatory genes like interleukin-10.
Lower doses of Prednisone provide an anti-inflammatory effect, while higher doses are
said to be immunosuppressive. The High doses of glucocorticoids for an extended period
binds to the mineralocorticoid receptor which in turn causes raising sodium levels and
decreasing potassium levels
Prednisone had been approved for relieving symptoms as well as also for the treatment
and maintenance of episodes of adrenal insufficiency ,alcoholic
hepatitis,angioedema,asthma, Bell palsy ,Chronic obstructive pulmonary disease
,duchenne muscular dystrophy ,focus sedimental glomerulosclerosis, giant cell arteritis,
gout, hepatitis ,immune thrombocytopenia ,inflammatory bowel disease, minimal change
disease ,multiple myeloma ,myasthenia gravis ,myopathies ,pericarditis ,polymyalgia
rheumatica ,prostate cancer ,takayasu arteritis ,tuberculosis ,urticaria ,warm autoimmune
hemolytic anemia.
The Onset of action of Prednisone is found to be very fast within a few minutes during the
acute condition and 2-20 hours during the chronic condition. and the duration of action is
about 14 to 22 hrs
Prednisone is available in oral tablets and solutions
Prednisone can be used in the treatment of the following conditions:
Adrenal insufficiency
3/14
Alcoholic hepatitis
Angioedema
Asthma
Bell palsy
Chronic obstructive pulmonary disease
Duchenne muscular dystrophy
Focus sedimental glomerulosclerosis
Giant cell arteritis
Gout
Hepatitis
Immune thrombocytopenia
Inflammatory bowel disease
Minimal change disease
Multiple myeloma
Myasthenia gravis
Myopathies
Pericarditis
Polymyalgia rheumatica
Prostate cancer
Takayasu arteritis
Tuberculosis
Urticaria
Warm autoimmune hemolytic anemia
Prednisone can help to relieve symptoms and also for the treatment and maintenance of
respiratory, rheumatoid, infectious, endocrine, neoplastic, allergies, immune system
conditions, dermatologic, gastrointestinal, hematologic, nervous system, and renal
conditions.
Prednisone is approved for use in the following clinical indications/conditions:
Adrenal insufficiency
Alcoholic hepatitis
Angioedema
Asthma
Bell palsy
Chronic obstructive pulmonary disease
Duchenne muscular dystrophy
Focus sedimental glomerulosclerosis
Giant cell arteritis
Gout
Hepatitis
Immune thrombocytopenia
Inflammatory bowel disease
Minimal change disease
4/14
Multiple myeloma
Myasthenia gravis
Myopathies
Pericarditis
Polymyalgia rheumatica
Prostate cancer
Takayasu arteritis
Tuberculosis
Urticaria
Warm autoimmune hemolytic anemia
Oral:
To be swallowed with the water as a whole as per the physician's prescription.
Oral:
Oral prednisone solution: 5 mg per 5 milliliters (mL)
Tablets: 1 mg 2.5 mg, 5 mg, 10 mg, 20 mg, 50 mg.
Delayed-release tablets: 1 mg, 2 mg, 5 mL.
Oral prednisone intensol concentrated solution: 5 mg/1 ml.
Adrenal insufficiency: 2.5 to 7.5 mg once daily
Adrenal insufficiency: Usual dosage range: 2.5 to 7.5 mg once a day.
Alcoholic hepatitis (off-label): 40 mg once a day for 28 days and then the dose is
tapered down.
Angioedema: 20-60 mg once daily and then the dose is tapered down over 5 to 7 days.
Asthma: 40-60 mg once daily divided into 1 or 2 doses.
Bell palsy: (off-label use): 60 mg - 80 mg once a day for 5 days and then tapered
down to 10 mg daily for 10 days.
Chronic obstructive pulmonary disease(off-label use): 40-60 mg for 5 - 14 days.
Duchenne muscular dystrophy(off-label): 0.75mg/kg/day.
Gout, treatment: 30 to 40 mg/day given once daily or in 2 divided doses.
Focal segmental glomerulosclerosis, primary (off-label use): 1 mg once daily or
2 mg every alternative day.
Hepatitis, autoimmune (off-label use): Oral: 40 to 60 mg once daily for one week
followed by the tapering down of the dose to 20 mg and 10 mg.
5/14
Immune thrombocytopenia: 1 mg/kg/day for 1 or 2 weeks and then tapering down.
Inflammatory bowel disease: 40 to 60 mg once daily for seven to fourteen days,
followed by a taper of up to 3 months and further tapering down to 5mg.
Minimal change disease, treatment (off-label use): Initial dose of Oral: 1
mg/kg/day a maximum: 80 mg/day once a day or 2 mg/kg alternative days
Multiple sclerosis, acute exacerbation: Oral: 625 mg to 1.25 g daily for three to
seven days followed by tapering.
Myasthenia gravis, crisis (adjunctive therapy) (off-label use): 1 mg/kg/day.
Myopathies (dermatomyositis/polymyositis), treatment: 1 mg/kg/day a
maximum: 80 mg/day as a single daily dose until improvement.
Pericarditis, acute or recurrent (alternative agent) (off-label use): 0.2 to 0.5
mg/kg/day until the symptoms are resolved for at least twenty-four hours and
normalization of inflammatory biomarkers .
Pneumocystis pneumonia, an adjunctive therapy for moderate to severe
disease (off-label use): 40 mg twice daily on days one to five beginning as early as
possible,followed by tapering down the dose to 2o mg and 10 mg or 5mg.
Polymyalgia rheumatica:Initial: Usual dose of 15 mg/day in a single daily dose or in
an divided doses or consider lower initial doses of about 7.5 to 10 mg/day for smaller
patients having mild symptoms or at high risk for side effects.
Takayasu arteritis (off-label use): Oral: Initial dose of 40 to 60 mg daily in
combination with the appropriate steroid-sparing agent followed by gradually tapering to
the lowest effective dose.
Thyroiditis, subacute (off-label use): Initial dose of 40 mg/day for one to two weeks;
gradually tapered eg, by 5 to 10 mg/day every five to seven days, which is based on clinical
response.
Tuberculosis pulmonary (off-label): 40 mg once a day for fourteen days, followed by
20 mg once daily for fourteen days
Urticaria, chronic spontaneous, acute exacerbation (off-label use): 35 to 40 mg
once a day until symptoms are controlled usually occurs after two to three days of
therapy.
Warm autoimmune hemolytic anemia: Oral dose of 1 to 2 mg/kg/day until a
hemoglobin response had occurred, typically within one to three weeks.
Ophthalmic, Oral.
Dosage Adjustments in Pediatric Patients:
6/14
In infants and children who are less than 12 years of age suffering from asthma, the dose
of 1 to 2 mg/kg/day PO in 2 divided doses until the peak expiratory flow is about 70% of
predicted or personal best. A 3 to 5-day course is usually a sufficient maximum of about
60 mg/day. A dose of 1 mg/kg/day PO had been shown to be just as effective as a dose of
2 mg/kg/day with lesser adverse effects, and this dose might be preferable. Another
source recommends the following Max doses of 20 mg/day of Prednisolone in children
less than two years, 30 mg/day of Prednisolone in children aged 3 to 5 years, and 40
mg/day of Prednisolone in children aged 6 to 11 years.
In the condition of bell palsy, the dosage of 2-4mg/kg/day is to be administered three or
four times a day.
In the condition of Juvenile idiopathic arthritis, 1mg/kg/day is to be administered every
day along with methylprednisolone.
In the condition of Dermatomyositis, juvenile 1-2mg/kg/day is recommended every day.
Smoking cessation and maintaining health is a must.
Caffeine should be avoided or limited to use as it might lead to the risk of nausea,
palpitations, nervousness, rapid heartbeat, etc.
Alcohol should be avoided in the patient, especially with an underlying liver disorder or
liver dysfunction.
A diet containing food with high sugar content and carbohydrates should be restricted.
This includes pies, cakes, honey, cookies, jams, candies, chips, and bread. It is also
advised to reduce or limit the intake of cholesterol and saturated fat and instead chooses
poultry, lean meat, or fish.
The dietary restrictions need to be individualized as per the patient's requirements.
Prednisone may be contraindicated under the following conditions:
Hypersensitivity to the ingredients of the medication. Rare instances of
anaphylactoid reactions have been found to have occurred in patients receiving
corticosteroid therapy.
The treating physician should closely monitor the patients and keep pharmacovigilance as
follows:
Behavioral and Mood Disturbances
Corticosteroid use might be associated with central nervous system effects ranging from
personality changes, euphoria, insomnia, mood swings, and severe depression to frank
psychotic manifestations. Also, existing emotional instability or psychotic tendencies
might be aggravated by corticosteroids.
Decrease in Bone Density
7/14
Corticosteroids decrease bone formation and increase bone resorption both through their
effect on calcium regulation which is decreasing absorption and increasing excretion and
also by the inhibition of osteoblast function. This, together with a decrease in the protein
matrix of the bone secondary to an increase in protein catabolism, as well as reduced sex
hormone production, might lead to the inhibition of bone growth in children and
adolescents and also the development of osteoporosis at any age. Special consideration
should be given to patients who are at an increased risk of osteoporosis such as
postmenopausal women before initiating corticosteroid therapy, bone density should be
monitored in patients who are on long-term corticosteroid therapy.
Ophthalmic Effects
Prolonged use of corticosteroids might produce posterior subcapsular cataracts and
glaucoma with possible damage to the optic nerves and might enhance the establishment
of secondary ocular infections caused due to fungi or viruses. The use of oral Prednisone
is not recommended in the treatment of optic neuritis and might lead to an increased risk
of new episodes. Intraocular pressure might become elevated in some individuals. In case
steroid therapy is continued for more than 6 weeks Herpes Simplex Corticosteroids
should be used with caution in patients with ocular herpes simplex because of possible
corneal perforation. Corticosteroids should not be given or used in active ocular herpes
simplex.
Vaccination
The Administration of live or live attenuated vaccines is found to be contraindicated in
patients receiving immunosuppressive doses of corticosteroids. Killed or inactivated
vaccines might be administered; however, the response to such vaccines can be predicted.
Immunization procedures might be undertaken in patients who are receiving
corticosteroids as replacement therapy such as for Addison's disease. While on
corticosteroid therapy, it is advised that patients should not be vaccinated against
smallpox. Any other immunization procedures should not be undertaken in patients who
are on corticosteroids, especially those on high dose, as it might lead to possible hazards
of neurological complications and a lack of antibody response.
Effect on Growth and Development
Long-term use of corticosteroids might have negative effects on growth and development
in children. Hence it is advised that growth and development of pediatric patients on
prolonged corticosteroid therapy should be carefully monitored.
Alterations in Endocrine Function
Cushing's syndrome, Hypothalamic-pituitary-adrenal (HPA) axis suppression, and
hyperglycemia. It is advised that patients should be monitored for these conditions with
chronic use. Corticosteroids might produce reversible Hypothalamic-pituitary-adrenal
axis suppression with the potential for glucocorticosteroid insufficiency after withdrawal
of treatment. Drug-induced secondary adrenocortical insufficiency might be minimized
8/14
by gradual reduction of dosage. This type of relative insufficiency might persist for many
months after discontinuation of therapy. Therefore, in any situation of stress occurring
during that period, it is advised that hormone therapy should be reinstituted.
Alterations in Cardiovascular/Renal Function
Corticosteroids can cause an increase in salt, blood pressure, and water retention, and
increased excretion of potassium and calcium. These effects are found to be less likely to
occur while using synthetic derivatives except when used in large doses. Dietary salt
restriction and potassium supplementation might be necessary. Such agents should be
used cautiously in patients with renal insufficiency, hypertension, congestive heart
failure.Reports suggest an association between concomitant use of corticosteroids and left
ventricular free wall rupture after a recent myocardial infarction.Therefore, therapy with
corticosteroids should be used cautiously in these patients
Use in Patients with Gastrointestinal Disorders
There is said to be an increased risk of gastrointestinal (GI) perforation in patients
suffering from certain gastrointestinal disorders. Signs of gastrointestinal perforation,
including peritoneal irritation, might be masked in patients receiving corticosteroids.
Corticosteroids should be used cautiously if there is a probability of abscess, impending
perforation, or other fresh intestinal anastomoses; pyogenic infections; diverticulitis;
active or latent peptic ulcer, etc.
Alcohol Warning
Avoid alcohol usage while on Prednisone medication as alcohol can worsen the effects of
any underlying disease condition, including conditions such as dizziness, blurred vision
etc.
Breast Feeding Warning
Prednisone is found to be secreted in human milk. Reports suggest that Prednisone
concentrations in human milk are about 5 to 25% of maternal serum levels, and that total
infant daily doses are as small, about 0.14% of the maternal daily dose. Therefore, caution
should be exercised when Prednisone is administered to a nursing woman. High doses of
corticosteroids for a long period could potentially produce problems in infant
development and growth and interfere with endogenous corticosteroid production. If
Prednisone is to be prescribed to a breastfeeding mother, the very lowest dose should be
prescribed to achieve the desired clinical effect.
Pregnancy Warning
Pregnancy Category D
9/14
Prednisone has not been formally evaluated in clinical or nonclinical studies for its effects
on pregnancy and fetal development. Multiple cohorts and case-controlled studies in
humans suggested that maternal corticosteroid use during the first trimester causes an
increase in the incidence of cleft lip with or without cleft palate from around 1/1000
infants to 3-5/1000 infants. 2 prospective case-control studies had shown that decreased
birth weight in infants when exposed to maternal corticosteroids in the uterus.
Prednisone should be prescribed and used during pregnancy only when the potential
benefits outweigh the potential risks associated with the fetus. Published literature
indicated that Prednisone has been shown to be teratogenic in animal studies such as
hamsters, rats, rabbits, and mice with increased incidence of cleft palate in offspring have
been reported in the clinical data. In teratogenicity studies, cleft palate along with an
elevated fetal lethality and reductions in fetal body weight had been seen in rats at
maternal doses of 30 mg/kg which is equivalent to 290 mg in a 60 kg individual based on
mg/m2 body surface comparison and higher. Cleft palate had been observed in mice at a
maternal dose of 20 mg/kg which is equivalent to 100 mg in a 60 kg individual based on
an mg/m2 comparison. Additionally, constriction of the ductus arteriosus had been
observed in the clinical studies in the fetuses of pregnant rats exposed to Prednisone.
Food Warning
No sufficient scientific evidence traceable regarding the use and safety of Prednisone in
concurrent use with any particular food.
The adverse reactions related to Prednisone can be categorized as:
Common
Muscle pain or weakness
Stomach discomfort, bloating
Changes in your menstrual periods
Headache
Fluid retention
Dizziness
Spinning sensation
Rare
Painful or difficult urination
Skin rash
Sleeplessness
Sweating
Trouble healing
Trouble sleeping
Unexplained weight loss
Unusual tiredness or weakness
Vision changes
10/14
Vomiting
Heartburn and/or indigestion (severe and continuous)
Increased hunger
Increased thirst
Increased urination
Loss of appetite
Loss of sexual desire or ability
Lower back or side pain
Menstrual irregularities
Muscle pain or tenderness
Muscle wasting or weakness
Nausea
Pain in back, ribs, arms, or legs
The clinically relevant drug interactions of Prednisone is briefly summarized here:
• Aminoglutethimide: Aminoglutethimide might lead to a loss of corticosteroid-
induced adrenal suppression.
• Amphotericin B: There had been cases reported in which concomitant use of
Amphotericin B with Prednisone caused cardiac enlargement and congestive heart failure.
• Anticholinesterase agents: Concomitant use of anticholinesterase agents and
corticosteroids might produce severe weakness in patients suffering from myasthenia
gravis. It is advised that anticholinesterase agents should be withdrawn at least 24 hours
before initiating the corticosteroid therapy.
• Anticoagulant agents: Co-administration of corticosteroids with warfarin usually
resulted in inhibition of response to warfarin, although there had been some conflicting
reports. Therefore, it is advised that coagulation indices should be monitored frequently
to maintain the desired anticoagulant effect.
• Antidiabetic Agents: As corticosteroids might increase blood glucose concentrations,
dosage adjustments of antidiabetic agents might be required.
• Antitubercular drugs: Serum concentrations of isoniazid might be decreased with
the concomitant use of corticosteroids.
• CYP 3A4 inducers e.g.carbamazepine, barbiturates, phenytoin, and
rifampin: Drugs such as ephedrine, barbiturates, phenytoin,and rifampin, which
induces hepatic microsomal drug metabolizing enzyme activity might enhance
metabolism of Prednisone and requires that the dosage of Prednisone be increased.
• CYP 3A4 inhibitors, e.g., macrolide antibiotics, ketoconazole: Ketoconazole
had been reported to decrease the metabolism of certain corticosteroids by up to 60%
causing an increased risk of corticosteroid side effects.
11/14
• Cholestyramine: Cholestyramine might cause an increase in the clearance of
corticosteroids.
• Cyclosporine: An Increased activity of both cyclosporine and corticosteroids might
occur when the both are used concurrently. Convulsions had been reported with this
concurrent use with corticosteroids.
• Digitalis: Patients on digitalis glycosides might be at increased risk of arrhythmias due
to condition called as hypokalemia.
• Estrogens, including oral contraceptives: Estrogens might decrease the hepatic
metabolism of certain corticosteroids, thereby causing increase in their effect.
• NSAIDS, including aspirin and salicylates: Coadministration of use of aspirin or
other non-steroidal anti-inflammatory agents with corticosteroids causes an increase in
the risk of gastrointestinal side effects. Aspirin should be used cautiously along with
corticosteroids in hypoprothrombinemia. The clearance of salicylates might be increased
with concurrent use of corticosteroids.
• Potassium-depleting agents such as diuretics, Amphotericin B: When
corticosteroids are administered along with potassium-depleting agents, patients should
be observed closely for development conditions called as of hypokalemia.
• Skin Tests: Corticosteroids might suppress reactions to the skin tests.
• Toxoids as well as live or inactivated Vaccines: Due to inhibition of antibody
response, the patients who are on prolonged corticosteroid therapy might exhibit a
reduced response to toxoids and live or inactivated vaccines. Corticosteroids might also
potentiate the replication of some organisms contained in live attenuated vaccines.
The common side effects of Prednisone include the following:
Nausea
Heartburn
Headache
Dizziness
Menstrual period changes
Trouble sleeping
Increased sweating
Acne
Pregnancy
Pregnancy Category D
Prednisone has not been formally evaluated in clinical or nonclinical studies for effects on
pregnancy and fetal development. Multiple cohort as well as case controlled studies in
humans suggested that maternal corticosteroid use during the first trimester causes
12/14
increase in the incidence of cleft lip with or without cleft palate from around 1/1000
infants to 3-5/1000 infants. 2 prospective case control studies had shown that decreased
birth weight in infants when exposed to maternal corticosteroids in uterus. Prednisone
should be prescribed and used during pregnancy only when the potential benefits
outweigh the potential risks associated with the fetus. Published literature indicated that
Prednisone has been shown to be teratogenic in animal studies such as hamsters, rats,
rabbits, and mice with increased incidence of cleft palate in offspring has been reported in
the clinical data. In teratogenicity studies, the formation of cleft palate along with an
elevated fetal lethality and reductions in fetal body weight had been seen in rats at
maternal doses of 30 mg/kg which is equivalent to 290 mg in a 60 kg individual based on
mg/m2 body surface comparison and higher. Cleft palate had been observed in mice at a
maternal dose of 20 mg/kg which is equivalent to 100 mg in a 60 kg individual based on
an mg/m2 comparison. Additionally, constriction of the ductus arteriosus had been
observed in the clinical studies in the fetuses of pregnant rats exposed to Prednisone.
Nursing Mothers
Prednisone is found to be secreted in human milk. Reports suggest that Prednisone
concentrations in human milk are about 5 to 25% of maternal serum levels as well as that
total infant daily doses are as small, about 0.14% of the maternal daily dose. Therefore,
caution should be exercised when Prednisone is administered to a nursing woman. High
doses of corticosteroids for a long period could potentially produce problems in infant
development and growth and interfere with endogenous corticosteroid production. If
Prednisone is to be prescribed to a breastfeeding mother, the very lowest dose should be
prescribed and used to achieve the desired clinical effect.
Pediatric Use
The safety and efficacy of Prednisone in the pediatric population are based on the well-
established study of the effect of corticosteroids, which is found to be similar in pediatric
and adult populations. Published studies provide evidence of safety and efficacy in
pediatric patients for the treatment of nephrotic syndrome in >2 years of age, and
aggressive lymphomas and leukemias in >1 month of age. The adverse effects of
Prednisone in pediatric patients are found to be similar to those in adults.
Geriatric Use
No overall differences in effectiveness and safety were observed between elderly subjects
as well as younger subjects, and other reported clinical experience with Prednisone had
not identified differences in responses between the elderly and younger patients.
However, the incidence of corticosteroid-induced side effects might be increased in
geriatric patients and also appear to be dose-related. Osteoporosis is found to be the most
frequently encountered complication, which occurs at a higher rate in Prednisone-treated
older patients as compared to younger populations and in age-matched controls. Loss of
bone mineral density appears to be greatest early on in the course of treatment and might
recover over time after steroid withdrawal or use of lower doses which is ≤5 mg/day. The
13/14
doses of 7.5 mg/day of Prednisone or higher, had been associated with an increased
relative risk of both vertebral as well as nonvertebral fractures, even with higher bone
density when compared to patients with involutional osteoporosis.
Physicians should be knowledgeable and vigilant about the treatment pertaining to the
treatment and identification of overdosage of Prednisone.
The adverse effects of accidental ingestion of large quantities of Prednisone in a very short
period of time had not been reported, but prolonged use of the drug can produce thinning
scalp hair, increased blood pressure, tachycardia, thrombophlebitis, hypertrichosis, acne,
striae, ecchymosis, increased sweating, pigmentation, hypokalemia,fluid retention,
excessive appetite,mental symptoms, moon face, abnormal fat deposits, weight gain, dry
scaly skin,and adrenal insufficiency, etc. Hepatomegaly and abdominal distention had
been observed in children.
Treatment of acute overdosage is done by immediate gastric lavage or emesis followed by
a symptomatic and suppporative therapy. For chronic overdosage in the face of severe
disease which requires continuous steroid therapy, the dosage of Prednisone might be
reduced only temporarily, or alternate day treatment might be introduced.
Pharmacodynamics
Corticosteroids are said to bind to the glucocorticoid receptor, inhibiting the pro-
inflammatory signals, and thereby promoting anti-inflammatory signals. Prednisone is
said to have a short duration of action as the half life is about 2.1-3.5 hours.
Corticosteroids are found to have a wide therapeutic window as patients might require
doses that are multiples of what the body can produce naturally. Patients who are taking
corticosteroids should be counseled regarding the risk of hypothalamic-pituitary-adrenal
axis suppression as well as increased susceptibility to infections.
Pharmacokinetics
Absorption
Oral prednisone has been found to have a Tmax of 2 hours.The delayed-release
formulation has been found to have a Tmax of 6-6.5 hours. A 5mg dose of prednisone
achieved an AUC of 572mL/min/1.73m2, while a 20mg dose of prednisone achieved an
AUC of 1034mL/min/1.73m2, and a 50mg dose of prednisone achieved an AUC of
2271mL/min/1.73m2.5 The data reports regarding the Cmax of prednisone is not
available
Distribution
A 0.15mg/kg dose of Prednisone had been found to have achieved a volume of
distribution of 29.3L, while 0.30mg/kg dose of Prednisone had been found to have
achieved a volume of distribution of 44.2L.
Metabolism
14/14
Prednisone has been reported to be metabolized mainly in the liver and is excreted in the
urine as sulfate and glucuronide conjugates. Prednisone is found to be reversibly
metabolized to prednisolone which is then metabolized to 6βhydroxy-prednisone (M-
XII), 6α-hydroxy-prednisone (M-XIII), 17α,21-dihydroxy-pregnan-1,4,6-trien-3,11,30-
trione (M-XVII), 20α-dihydro-prednisone (M-V), or 20β-dihydro-prednisone (M-IV).
Elimination
Prednisone was found to be eliminated in the form of urine as sulfates and glucoronide
conjugates.
1. https://go.drugbank.com/drugs/DB00635
2. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202020s000lbl.pdf
3. https://www.drugs.com/prednisone.html
4. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=10fe5a3b-84dc-4600-
87c2-b80c97ce18cf
5. https://cdn.brief.vet/web-files/PVD/drupal-uploads/files/VMG-Prednisolone-
Prednisone-2019-01-30-1259.pdf
6. https://docs.boehringer-ingelheim.com/Prescribing
Information/PIs/Roxane/Prednisone Reformulated/PredniSONEReform.pdf
7. https://www.singlecare.com/prescription/prednisone/dosage
Dr JUHI SINGLA
Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow
Medical college and done MD pharmacology from SGT UNIVERSITY
Gurgaon. She can be contacted at editorial@medicaldialogues.in.
Contact no. 011-43720751
Sonali R Muralidhar
I am Sonali R Muralidhar currently residing at Madurai.I have
completed my Master’s in Pharmacy with my core subject as
Pharmaceutics. I am interested in Pharmaceutical research , medical
content writing, Biopharmaceutics , regulatory affairs , novel drug
delivery, targeted drug delivery.

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Prednisone: Indications, Uses, Dosage

  • 1. 1/14 January 2, 2023 Prednisone medicaldialogues.in/generics/prednisone-2722820 Indications, Uses, Dosage, Drugs Interactions, Side effects Prednisone Medicine Type : Allopathy Prescription Type: Prescription Required Approval : DCGI (Drugs Controller General of India) Schedule Schedule H Pharmacological Class: Corticosteroid, Therapy Class: Anti-inflammatory Agent, Antineoplastic agent, Vasoconstrictor, Prednisone belongs to the pharmacological class of Corticosteroids. Prednisone appears to have anti-inflammatory Anti-neoplastic and Vasoconstrictive effects . Prednisone had been approved for relieving symptoms as well as also for the treatment and maintenance of episodes of blood problems, arthritis, cancer, immune system problems, eye conditions, breathing problems, allergies etc.
  • 2. 2/14 Prednisone is completely and rapidly absorbed with oral bioavailability of 70%. Prednisone achieved a steady state volume of distribution of 29.3 L at a dose of about 0.15mg/kg and 44.2L at 0.30mg/kg dose. Prednisone can be reversibly metabolized to prednisolone and various other metabolites such as 6βhydroxy-prednisone,6α-hydroxy- prednisone, 17α,21-dihydroxy-pregnan-1,4,6-trien-3,11,30-trione, etc. Prednisone was found to be excreted in the form of urine in the form of sulfate and glucuronide conjugates. The common side effects associated with Prednisone are irregular nausea, headache, dizziness, menstrual pain, acne, etc. Prednisone is available in the form of oral soluble tablets and solutions. Prednisone is available in the U.S., Canada, E.U., India, Australia, and Japan. Prednisone belongs to the pharmacological class Corticosteroids. Prednisone appears to have anti-inflammatory, Anti-neoplastic and Vasoconstrictive effects . Prednisone binds to the glucocorticoid receptor which mediates changes in gene expression that might lead to multiple downstream effects over hours to days. Glucocorticoids inhibit demargination and neutrophil apoptosis.They inhibit phospholipase A2, which further decreases the formation of arachidonic acid derivatives which in turn inhibits NF-Kappa B and other inflammatory transcription factors. They also promote anti-inflammatory genes like interleukin-10. Lower doses of Prednisone provide an anti-inflammatory effect, while higher doses are said to be immunosuppressive. The High doses of glucocorticoids for an extended period binds to the mineralocorticoid receptor which in turn causes raising sodium levels and decreasing potassium levels Prednisone had been approved for relieving symptoms as well as also for the treatment and maintenance of episodes of adrenal insufficiency ,alcoholic hepatitis,angioedema,asthma, Bell palsy ,Chronic obstructive pulmonary disease ,duchenne muscular dystrophy ,focus sedimental glomerulosclerosis, giant cell arteritis, gout, hepatitis ,immune thrombocytopenia ,inflammatory bowel disease, minimal change disease ,multiple myeloma ,myasthenia gravis ,myopathies ,pericarditis ,polymyalgia rheumatica ,prostate cancer ,takayasu arteritis ,tuberculosis ,urticaria ,warm autoimmune hemolytic anemia. The Onset of action of Prednisone is found to be very fast within a few minutes during the acute condition and 2-20 hours during the chronic condition. and the duration of action is about 14 to 22 hrs Prednisone is available in oral tablets and solutions Prednisone can be used in the treatment of the following conditions: Adrenal insufficiency
  • 3. 3/14 Alcoholic hepatitis Angioedema Asthma Bell palsy Chronic obstructive pulmonary disease Duchenne muscular dystrophy Focus sedimental glomerulosclerosis Giant cell arteritis Gout Hepatitis Immune thrombocytopenia Inflammatory bowel disease Minimal change disease Multiple myeloma Myasthenia gravis Myopathies Pericarditis Polymyalgia rheumatica Prostate cancer Takayasu arteritis Tuberculosis Urticaria Warm autoimmune hemolytic anemia Prednisone can help to relieve symptoms and also for the treatment and maintenance of respiratory, rheumatoid, infectious, endocrine, neoplastic, allergies, immune system conditions, dermatologic, gastrointestinal, hematologic, nervous system, and renal conditions. Prednisone is approved for use in the following clinical indications/conditions: Adrenal insufficiency Alcoholic hepatitis Angioedema Asthma Bell palsy Chronic obstructive pulmonary disease Duchenne muscular dystrophy Focus sedimental glomerulosclerosis Giant cell arteritis Gout Hepatitis Immune thrombocytopenia Inflammatory bowel disease Minimal change disease
  • 4. 4/14 Multiple myeloma Myasthenia gravis Myopathies Pericarditis Polymyalgia rheumatica Prostate cancer Takayasu arteritis Tuberculosis Urticaria Warm autoimmune hemolytic anemia Oral: To be swallowed with the water as a whole as per the physician's prescription. Oral: Oral prednisone solution: 5 mg per 5 milliliters (mL) Tablets: 1 mg 2.5 mg, 5 mg, 10 mg, 20 mg, 50 mg. Delayed-release tablets: 1 mg, 2 mg, 5 mL. Oral prednisone intensol concentrated solution: 5 mg/1 ml. Adrenal insufficiency: 2.5 to 7.5 mg once daily Adrenal insufficiency: Usual dosage range: 2.5 to 7.5 mg once a day. Alcoholic hepatitis (off-label): 40 mg once a day for 28 days and then the dose is tapered down. Angioedema: 20-60 mg once daily and then the dose is tapered down over 5 to 7 days. Asthma: 40-60 mg once daily divided into 1 or 2 doses. Bell palsy: (off-label use): 60 mg - 80 mg once a day for 5 days and then tapered down to 10 mg daily for 10 days. Chronic obstructive pulmonary disease(off-label use): 40-60 mg for 5 - 14 days. Duchenne muscular dystrophy(off-label): 0.75mg/kg/day. Gout, treatment: 30 to 40 mg/day given once daily or in 2 divided doses. Focal segmental glomerulosclerosis, primary (off-label use): 1 mg once daily or 2 mg every alternative day. Hepatitis, autoimmune (off-label use): Oral: 40 to 60 mg once daily for one week followed by the tapering down of the dose to 20 mg and 10 mg.
  • 5. 5/14 Immune thrombocytopenia: 1 mg/kg/day for 1 or 2 weeks and then tapering down. Inflammatory bowel disease: 40 to 60 mg once daily for seven to fourteen days, followed by a taper of up to 3 months and further tapering down to 5mg. Minimal change disease, treatment (off-label use): Initial dose of Oral: 1 mg/kg/day a maximum: 80 mg/day once a day or 2 mg/kg alternative days Multiple sclerosis, acute exacerbation: Oral: 625 mg to 1.25 g daily for three to seven days followed by tapering. Myasthenia gravis, crisis (adjunctive therapy) (off-label use): 1 mg/kg/day. Myopathies (dermatomyositis/polymyositis), treatment: 1 mg/kg/day a maximum: 80 mg/day as a single daily dose until improvement. Pericarditis, acute or recurrent (alternative agent) (off-label use): 0.2 to 0.5 mg/kg/day until the symptoms are resolved for at least twenty-four hours and normalization of inflammatory biomarkers . Pneumocystis pneumonia, an adjunctive therapy for moderate to severe disease (off-label use): 40 mg twice daily on days one to five beginning as early as possible,followed by tapering down the dose to 2o mg and 10 mg or 5mg. Polymyalgia rheumatica:Initial: Usual dose of 15 mg/day in a single daily dose or in an divided doses or consider lower initial doses of about 7.5 to 10 mg/day for smaller patients having mild symptoms or at high risk for side effects. Takayasu arteritis (off-label use): Oral: Initial dose of 40 to 60 mg daily in combination with the appropriate steroid-sparing agent followed by gradually tapering to the lowest effective dose. Thyroiditis, subacute (off-label use): Initial dose of 40 mg/day for one to two weeks; gradually tapered eg, by 5 to 10 mg/day every five to seven days, which is based on clinical response. Tuberculosis pulmonary (off-label): 40 mg once a day for fourteen days, followed by 20 mg once daily for fourteen days Urticaria, chronic spontaneous, acute exacerbation (off-label use): 35 to 40 mg once a day until symptoms are controlled usually occurs after two to three days of therapy. Warm autoimmune hemolytic anemia: Oral dose of 1 to 2 mg/kg/day until a hemoglobin response had occurred, typically within one to three weeks. Ophthalmic, Oral. Dosage Adjustments in Pediatric Patients:
  • 6. 6/14 In infants and children who are less than 12 years of age suffering from asthma, the dose of 1 to 2 mg/kg/day PO in 2 divided doses until the peak expiratory flow is about 70% of predicted or personal best. A 3 to 5-day course is usually a sufficient maximum of about 60 mg/day. A dose of 1 mg/kg/day PO had been shown to be just as effective as a dose of 2 mg/kg/day with lesser adverse effects, and this dose might be preferable. Another source recommends the following Max doses of 20 mg/day of Prednisolone in children less than two years, 30 mg/day of Prednisolone in children aged 3 to 5 years, and 40 mg/day of Prednisolone in children aged 6 to 11 years. In the condition of bell palsy, the dosage of 2-4mg/kg/day is to be administered three or four times a day. In the condition of Juvenile idiopathic arthritis, 1mg/kg/day is to be administered every day along with methylprednisolone. In the condition of Dermatomyositis, juvenile 1-2mg/kg/day is recommended every day. Smoking cessation and maintaining health is a must. Caffeine should be avoided or limited to use as it might lead to the risk of nausea, palpitations, nervousness, rapid heartbeat, etc. Alcohol should be avoided in the patient, especially with an underlying liver disorder or liver dysfunction. A diet containing food with high sugar content and carbohydrates should be restricted. This includes pies, cakes, honey, cookies, jams, candies, chips, and bread. It is also advised to reduce or limit the intake of cholesterol and saturated fat and instead chooses poultry, lean meat, or fish. The dietary restrictions need to be individualized as per the patient's requirements. Prednisone may be contraindicated under the following conditions: Hypersensitivity to the ingredients of the medication. Rare instances of anaphylactoid reactions have been found to have occurred in patients receiving corticosteroid therapy. The treating physician should closely monitor the patients and keep pharmacovigilance as follows: Behavioral and Mood Disturbances Corticosteroid use might be associated with central nervous system effects ranging from personality changes, euphoria, insomnia, mood swings, and severe depression to frank psychotic manifestations. Also, existing emotional instability or psychotic tendencies might be aggravated by corticosteroids. Decrease in Bone Density
  • 7. 7/14 Corticosteroids decrease bone formation and increase bone resorption both through their effect on calcium regulation which is decreasing absorption and increasing excretion and also by the inhibition of osteoblast function. This, together with a decrease in the protein matrix of the bone secondary to an increase in protein catabolism, as well as reduced sex hormone production, might lead to the inhibition of bone growth in children and adolescents and also the development of osteoporosis at any age. Special consideration should be given to patients who are at an increased risk of osteoporosis such as postmenopausal women before initiating corticosteroid therapy, bone density should be monitored in patients who are on long-term corticosteroid therapy. Ophthalmic Effects Prolonged use of corticosteroids might produce posterior subcapsular cataracts and glaucoma with possible damage to the optic nerves and might enhance the establishment of secondary ocular infections caused due to fungi or viruses. The use of oral Prednisone is not recommended in the treatment of optic neuritis and might lead to an increased risk of new episodes. Intraocular pressure might become elevated in some individuals. In case steroid therapy is continued for more than 6 weeks Herpes Simplex Corticosteroids should be used with caution in patients with ocular herpes simplex because of possible corneal perforation. Corticosteroids should not be given or used in active ocular herpes simplex. Vaccination The Administration of live or live attenuated vaccines is found to be contraindicated in patients receiving immunosuppressive doses of corticosteroids. Killed or inactivated vaccines might be administered; however, the response to such vaccines can be predicted. Immunization procedures might be undertaken in patients who are receiving corticosteroids as replacement therapy such as for Addison's disease. While on corticosteroid therapy, it is advised that patients should not be vaccinated against smallpox. Any other immunization procedures should not be undertaken in patients who are on corticosteroids, especially those on high dose, as it might lead to possible hazards of neurological complications and a lack of antibody response. Effect on Growth and Development Long-term use of corticosteroids might have negative effects on growth and development in children. Hence it is advised that growth and development of pediatric patients on prolonged corticosteroid therapy should be carefully monitored. Alterations in Endocrine Function Cushing's syndrome, Hypothalamic-pituitary-adrenal (HPA) axis suppression, and hyperglycemia. It is advised that patients should be monitored for these conditions with chronic use. Corticosteroids might produce reversible Hypothalamic-pituitary-adrenal axis suppression with the potential for glucocorticosteroid insufficiency after withdrawal of treatment. Drug-induced secondary adrenocortical insufficiency might be minimized
  • 8. 8/14 by gradual reduction of dosage. This type of relative insufficiency might persist for many months after discontinuation of therapy. Therefore, in any situation of stress occurring during that period, it is advised that hormone therapy should be reinstituted. Alterations in Cardiovascular/Renal Function Corticosteroids can cause an increase in salt, blood pressure, and water retention, and increased excretion of potassium and calcium. These effects are found to be less likely to occur while using synthetic derivatives except when used in large doses. Dietary salt restriction and potassium supplementation might be necessary. Such agents should be used cautiously in patients with renal insufficiency, hypertension, congestive heart failure.Reports suggest an association between concomitant use of corticosteroids and left ventricular free wall rupture after a recent myocardial infarction.Therefore, therapy with corticosteroids should be used cautiously in these patients Use in Patients with Gastrointestinal Disorders There is said to be an increased risk of gastrointestinal (GI) perforation in patients suffering from certain gastrointestinal disorders. Signs of gastrointestinal perforation, including peritoneal irritation, might be masked in patients receiving corticosteroids. Corticosteroids should be used cautiously if there is a probability of abscess, impending perforation, or other fresh intestinal anastomoses; pyogenic infections; diverticulitis; active or latent peptic ulcer, etc. Alcohol Warning Avoid alcohol usage while on Prednisone medication as alcohol can worsen the effects of any underlying disease condition, including conditions such as dizziness, blurred vision etc. Breast Feeding Warning Prednisone is found to be secreted in human milk. Reports suggest that Prednisone concentrations in human milk are about 5 to 25% of maternal serum levels, and that total infant daily doses are as small, about 0.14% of the maternal daily dose. Therefore, caution should be exercised when Prednisone is administered to a nursing woman. High doses of corticosteroids for a long period could potentially produce problems in infant development and growth and interfere with endogenous corticosteroid production. If Prednisone is to be prescribed to a breastfeeding mother, the very lowest dose should be prescribed to achieve the desired clinical effect. Pregnancy Warning Pregnancy Category D
  • 9. 9/14 Prednisone has not been formally evaluated in clinical or nonclinical studies for its effects on pregnancy and fetal development. Multiple cohorts and case-controlled studies in humans suggested that maternal corticosteroid use during the first trimester causes an increase in the incidence of cleft lip with or without cleft palate from around 1/1000 infants to 3-5/1000 infants. 2 prospective case-control studies had shown that decreased birth weight in infants when exposed to maternal corticosteroids in the uterus. Prednisone should be prescribed and used during pregnancy only when the potential benefits outweigh the potential risks associated with the fetus. Published literature indicated that Prednisone has been shown to be teratogenic in animal studies such as hamsters, rats, rabbits, and mice with increased incidence of cleft palate in offspring have been reported in the clinical data. In teratogenicity studies, cleft palate along with an elevated fetal lethality and reductions in fetal body weight had been seen in rats at maternal doses of 30 mg/kg which is equivalent to 290 mg in a 60 kg individual based on mg/m2 body surface comparison and higher. Cleft palate had been observed in mice at a maternal dose of 20 mg/kg which is equivalent to 100 mg in a 60 kg individual based on an mg/m2 comparison. Additionally, constriction of the ductus arteriosus had been observed in the clinical studies in the fetuses of pregnant rats exposed to Prednisone. Food Warning No sufficient scientific evidence traceable regarding the use and safety of Prednisone in concurrent use with any particular food. The adverse reactions related to Prednisone can be categorized as: Common Muscle pain or weakness Stomach discomfort, bloating Changes in your menstrual periods Headache Fluid retention Dizziness Spinning sensation Rare Painful or difficult urination Skin rash Sleeplessness Sweating Trouble healing Trouble sleeping Unexplained weight loss Unusual tiredness or weakness Vision changes
  • 10. 10/14 Vomiting Heartburn and/or indigestion (severe and continuous) Increased hunger Increased thirst Increased urination Loss of appetite Loss of sexual desire or ability Lower back or side pain Menstrual irregularities Muscle pain or tenderness Muscle wasting or weakness Nausea Pain in back, ribs, arms, or legs The clinically relevant drug interactions of Prednisone is briefly summarized here: • Aminoglutethimide: Aminoglutethimide might lead to a loss of corticosteroid- induced adrenal suppression. • Amphotericin B: There had been cases reported in which concomitant use of Amphotericin B with Prednisone caused cardiac enlargement and congestive heart failure. • Anticholinesterase agents: Concomitant use of anticholinesterase agents and corticosteroids might produce severe weakness in patients suffering from myasthenia gravis. It is advised that anticholinesterase agents should be withdrawn at least 24 hours before initiating the corticosteroid therapy. • Anticoagulant agents: Co-administration of corticosteroids with warfarin usually resulted in inhibition of response to warfarin, although there had been some conflicting reports. Therefore, it is advised that coagulation indices should be monitored frequently to maintain the desired anticoagulant effect. • Antidiabetic Agents: As corticosteroids might increase blood glucose concentrations, dosage adjustments of antidiabetic agents might be required. • Antitubercular drugs: Serum concentrations of isoniazid might be decreased with the concomitant use of corticosteroids. • CYP 3A4 inducers e.g.carbamazepine, barbiturates, phenytoin, and rifampin: Drugs such as ephedrine, barbiturates, phenytoin,and rifampin, which induces hepatic microsomal drug metabolizing enzyme activity might enhance metabolism of Prednisone and requires that the dosage of Prednisone be increased. • CYP 3A4 inhibitors, e.g., macrolide antibiotics, ketoconazole: Ketoconazole had been reported to decrease the metabolism of certain corticosteroids by up to 60% causing an increased risk of corticosteroid side effects.
  • 11. 11/14 • Cholestyramine: Cholestyramine might cause an increase in the clearance of corticosteroids. • Cyclosporine: An Increased activity of both cyclosporine and corticosteroids might occur when the both are used concurrently. Convulsions had been reported with this concurrent use with corticosteroids. • Digitalis: Patients on digitalis glycosides might be at increased risk of arrhythmias due to condition called as hypokalemia. • Estrogens, including oral contraceptives: Estrogens might decrease the hepatic metabolism of certain corticosteroids, thereby causing increase in their effect. • NSAIDS, including aspirin and salicylates: Coadministration of use of aspirin or other non-steroidal anti-inflammatory agents with corticosteroids causes an increase in the risk of gastrointestinal side effects. Aspirin should be used cautiously along with corticosteroids in hypoprothrombinemia. The clearance of salicylates might be increased with concurrent use of corticosteroids. • Potassium-depleting agents such as diuretics, Amphotericin B: When corticosteroids are administered along with potassium-depleting agents, patients should be observed closely for development conditions called as of hypokalemia. • Skin Tests: Corticosteroids might suppress reactions to the skin tests. • Toxoids as well as live or inactivated Vaccines: Due to inhibition of antibody response, the patients who are on prolonged corticosteroid therapy might exhibit a reduced response to toxoids and live or inactivated vaccines. Corticosteroids might also potentiate the replication of some organisms contained in live attenuated vaccines. The common side effects of Prednisone include the following: Nausea Heartburn Headache Dizziness Menstrual period changes Trouble sleeping Increased sweating Acne Pregnancy Pregnancy Category D Prednisone has not been formally evaluated in clinical or nonclinical studies for effects on pregnancy and fetal development. Multiple cohort as well as case controlled studies in humans suggested that maternal corticosteroid use during the first trimester causes
  • 12. 12/14 increase in the incidence of cleft lip with or without cleft palate from around 1/1000 infants to 3-5/1000 infants. 2 prospective case control studies had shown that decreased birth weight in infants when exposed to maternal corticosteroids in uterus. Prednisone should be prescribed and used during pregnancy only when the potential benefits outweigh the potential risks associated with the fetus. Published literature indicated that Prednisone has been shown to be teratogenic in animal studies such as hamsters, rats, rabbits, and mice with increased incidence of cleft palate in offspring has been reported in the clinical data. In teratogenicity studies, the formation of cleft palate along with an elevated fetal lethality and reductions in fetal body weight had been seen in rats at maternal doses of 30 mg/kg which is equivalent to 290 mg in a 60 kg individual based on mg/m2 body surface comparison and higher. Cleft palate had been observed in mice at a maternal dose of 20 mg/kg which is equivalent to 100 mg in a 60 kg individual based on an mg/m2 comparison. Additionally, constriction of the ductus arteriosus had been observed in the clinical studies in the fetuses of pregnant rats exposed to Prednisone. Nursing Mothers Prednisone is found to be secreted in human milk. Reports suggest that Prednisone concentrations in human milk are about 5 to 25% of maternal serum levels as well as that total infant daily doses are as small, about 0.14% of the maternal daily dose. Therefore, caution should be exercised when Prednisone is administered to a nursing woman. High doses of corticosteroids for a long period could potentially produce problems in infant development and growth and interfere with endogenous corticosteroid production. If Prednisone is to be prescribed to a breastfeeding mother, the very lowest dose should be prescribed and used to achieve the desired clinical effect. Pediatric Use The safety and efficacy of Prednisone in the pediatric population are based on the well- established study of the effect of corticosteroids, which is found to be similar in pediatric and adult populations. Published studies provide evidence of safety and efficacy in pediatric patients for the treatment of nephrotic syndrome in >2 years of age, and aggressive lymphomas and leukemias in >1 month of age. The adverse effects of Prednisone in pediatric patients are found to be similar to those in adults. Geriatric Use No overall differences in effectiveness and safety were observed between elderly subjects as well as younger subjects, and other reported clinical experience with Prednisone had not identified differences in responses between the elderly and younger patients. However, the incidence of corticosteroid-induced side effects might be increased in geriatric patients and also appear to be dose-related. Osteoporosis is found to be the most frequently encountered complication, which occurs at a higher rate in Prednisone-treated older patients as compared to younger populations and in age-matched controls. Loss of bone mineral density appears to be greatest early on in the course of treatment and might recover over time after steroid withdrawal or use of lower doses which is ≤5 mg/day. The
  • 13. 13/14 doses of 7.5 mg/day of Prednisone or higher, had been associated with an increased relative risk of both vertebral as well as nonvertebral fractures, even with higher bone density when compared to patients with involutional osteoporosis. Physicians should be knowledgeable and vigilant about the treatment pertaining to the treatment and identification of overdosage of Prednisone. The adverse effects of accidental ingestion of large quantities of Prednisone in a very short period of time had not been reported, but prolonged use of the drug can produce thinning scalp hair, increased blood pressure, tachycardia, thrombophlebitis, hypertrichosis, acne, striae, ecchymosis, increased sweating, pigmentation, hypokalemia,fluid retention, excessive appetite,mental symptoms, moon face, abnormal fat deposits, weight gain, dry scaly skin,and adrenal insufficiency, etc. Hepatomegaly and abdominal distention had been observed in children. Treatment of acute overdosage is done by immediate gastric lavage or emesis followed by a symptomatic and suppporative therapy. For chronic overdosage in the face of severe disease which requires continuous steroid therapy, the dosage of Prednisone might be reduced only temporarily, or alternate day treatment might be introduced. Pharmacodynamics Corticosteroids are said to bind to the glucocorticoid receptor, inhibiting the pro- inflammatory signals, and thereby promoting anti-inflammatory signals. Prednisone is said to have a short duration of action as the half life is about 2.1-3.5 hours. Corticosteroids are found to have a wide therapeutic window as patients might require doses that are multiples of what the body can produce naturally. Patients who are taking corticosteroids should be counseled regarding the risk of hypothalamic-pituitary-adrenal axis suppression as well as increased susceptibility to infections. Pharmacokinetics Absorption Oral prednisone has been found to have a Tmax of 2 hours.The delayed-release formulation has been found to have a Tmax of 6-6.5 hours. A 5mg dose of prednisone achieved an AUC of 572mL/min/1.73m2, while a 20mg dose of prednisone achieved an AUC of 1034mL/min/1.73m2, and a 50mg dose of prednisone achieved an AUC of 2271mL/min/1.73m2.5 The data reports regarding the Cmax of prednisone is not available Distribution A 0.15mg/kg dose of Prednisone had been found to have achieved a volume of distribution of 29.3L, while 0.30mg/kg dose of Prednisone had been found to have achieved a volume of distribution of 44.2L. Metabolism
  • 14. 14/14 Prednisone has been reported to be metabolized mainly in the liver and is excreted in the urine as sulfate and glucuronide conjugates. Prednisone is found to be reversibly metabolized to prednisolone which is then metabolized to 6βhydroxy-prednisone (M- XII), 6α-hydroxy-prednisone (M-XIII), 17α,21-dihydroxy-pregnan-1,4,6-trien-3,11,30- trione (M-XVII), 20α-dihydro-prednisone (M-V), or 20β-dihydro-prednisone (M-IV). Elimination Prednisone was found to be eliminated in the form of urine as sulfates and glucoronide conjugates. 1. https://go.drugbank.com/drugs/DB00635 2. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202020s000lbl.pdf 3. https://www.drugs.com/prednisone.html 4. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=10fe5a3b-84dc-4600- 87c2-b80c97ce18cf 5. https://cdn.brief.vet/web-files/PVD/drupal-uploads/files/VMG-Prednisolone- Prednisone-2019-01-30-1259.pdf 6. https://docs.boehringer-ingelheim.com/Prescribing Information/PIs/Roxane/Prednisone Reformulated/PredniSONEReform.pdf 7. https://www.singlecare.com/prescription/prednisone/dosage Dr JUHI SINGLA Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow Medical college and done MD pharmacology from SGT UNIVERSITY Gurgaon. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751 Sonali R Muralidhar I am Sonali R Muralidhar currently residing at Madurai.I have completed my Master’s in Pharmacy with my core subject as Pharmaceutics. I am interested in Pharmaceutical research , medical content writing, Biopharmaceutics , regulatory affairs , novel drug delivery, targeted drug delivery.