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Product Name
:
PREDLONE (amp)
Chemical Name
:
Prednisolone
Therapeutic Category
:
Anti-inflammatory drugs
Pharmacologic Category
:
Corticosteroid, Systemic
Pharmaceutical Form
:
Ampoule
Composition
:
Prednisolone 25mg/2ml
Dosing
 
Dosing: Adult
Dose depends upon condition being treated and response of patient. Oral dosage expressed in terms of prednisolone base. Consider alternate day therapy for long-term therapy. Discontinuation of long-term therapy requires gradual withdrawal by tapering the dose. Patients undergoing unusual stress while receiving corticosteroids, should receive increased doses prior to, during, and after the stressful situation.
Usual dose (range): Oral: 5-60 mg/day
Rheumatoid arthritis: Oral: Initial: 5-7.5 mg/day, adjust dose as necessary
Multiple sclerosis: Oral: 200 mg/day for 1 week followed by 80 mg every other day for 1 month
Dosing adjustment in hyperthyroidism: Prednisolone dose may need to be increased to achieve adequate therapeutic effects.

Dosing: Pediatric

Dose depends upon condition being treated and response of patient; dosage for infants and children should be based on severity of the disease and response of the patient rather than on strict adherence to dosage indicated by age, weight, or body surface area. Oral dosage expressed in terms of prednisolone base. Consider alternate day therapy for long-term therapy. Discontinuation of long-term therapy requires gradual withdrawal by tapering the dose. Patients undergoing unusual stress while receiving corticosteroids, should receive increased doses prior to, during, and after the stressful situation.
Acute asthma: Oral: 1-2 mg/kg/day in divided doses 1-2 times/day for 3-5 days
Anti-inflammatory or immunosuppressive dose: Oral: 0.1-2 mg/kg/day in divided doses 1-4 times/day
Nephrotic syndrome: Oral:
Initial (first 3 episodes): 2 mg/kg/day or 60 mg/m2/day (maximum: 80 mg/day) in divided doses 3-4 times/day until urine is protein free for 3 consecutive days (maximum: 28 days); followed by 1-1.5 mg/kg/dose or 40 mg/m2/dose given every other day for 4 weeks
Maintenance (for frequent relapses): 0.5-1 mg/kg/dose given every other day for 3-6 months
Dosing adjustment in hyperthyroidism: Refer to adult dosing.

Dosing: Geriatric

Use lowest effective adult dose. Dose depends upon condition being treated and response of patient; alternate day dosing may be attempted in some disease states.

Dosing: Renal Impairment

Hemodialysis: Slightly dialyzable (5% to 20%); administer dose posthemodialysis
Peritoneal dialysis: Supplemental dose is not necessary
Use
 
Treatment of endocrine disorders, rheumatic disorders, collagen diseases, allergic states, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, and gastrointestinal diseases; resolution of acute exacerbations of multiple sclerosis; management of fulminating or disseminated tuberculosis and trichinosis; acute or chronic solid organ rejection
Adverse Reactions
 
Frequency not defined.
Cardiovascular: Cardiomyopathy, CHF, edema, facial edema, hypertension
Central nervous system: Headache, insomnia, malaise, nervousness, pseudotumor cerebri, psychic disorders, seizure, vertigo
Dermatologic: Bruising, facial erythema, hirsutism, petechiae, skin test reaction suppression, thin fragile skin, urticaria
Endocrine & metabolic: Carbohydrate tolerance decreased, Cushing's syndrome, diabetes mellitus, growth suppression, hyperglycemia, hypernatremia, hypokalemia, hypokalemic alkalosis, menstrual irregularities, negative nitrogen balance, pituitary adrenal axis suppression
Gastrointestinal: Abdominal distention, increased appetite, indigestion, nausea, pancreatitis, peptic ulcer, ulcerative esophagitis, weight gain
Hepatic: LFTs increased (usually reversible)
Neuromuscular & skeletal: Arthralgia, aseptic necrosis (humeral/femoral heads), fractures, muscle mass decreased, muscle weakness, osteoporosis, steroid myopathy, tendon rupture, weakness
Ocular: Cataracts, exophthalmus, eyelid edema, glaucoma, intraocular pressure increased, irritation
Respiratory: Epistaxis
Miscellaneous: Diaphoresis increased, impaired wound healing
Contraindications
 
Hypersensitivity to prednisolone or any component of the formulation; acute superficial herpes simplex keratitis; live or attenuated virus vaccines (with immunosuppressive doses of corticosteroids); systemic fungal infections; varicella
Warnings / Precautions Drug
 
Concerns related to adverse effects:
• Adrenal suppression: May cause hypercorticism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in younger children or in patients receiving high doses for prolonged periods. HPA axis suppression may lead to adrenal crisis. Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully. Particular care is required when patients are transferred from systemic corticosteroids to inhaled products due to possible adrenal insufficiency or withdrawal from steroids, including an increase in allergic symptoms. Patients receiving >20 mg per day of prednisone (or equivalent) may be most susceptible. Fatalities have occurred due to adrenal insufficiency in asthmatic patients during and after transfer from systemic corticosteroids to aerosol steroids; aerosol steroids do not provide the systemic steroid needed to treat patients having trauma, surgery, or infections.
• Cataracts: Prolonged use of corticosteroids may result in posterior subcapsular cataract formation.
• Glaucoma: Prolonged use of corticosteroids may result in elevated intraocular pressure (IOP) and glaucoma. Monitor IOP in any patient receiving treatment for ≥10 days.
• Immunosuppression: Prolonged use of corticosteroids may also increase the incidence of secondary infection, mask acute infection (including fungal infections) or prolong or exacerbate viral infections. Exposure to chickenpox should be avoided; corticosteroids should not be used to treat ocular herpes simplex. Corticosteroids should not be used for cerebral malaria or viral hepatitis. Use with caution in patients with tuberculosis.
• Kaposi's sarcoma: Prolonged treatment with corticosteroids has been associated with the development of Kaposi's sarcoma (case reports); if noted, discontinuation of therapy should be considered.
• Myopathy: Acute myopathy has been reported with high dose corticosteroids, usually in patients with neuromuscular transmission disorders; may involve ocular and/or respiratory muscles; monitor creatine kinase; recovery may be delayed.
• Psychiatric disturbances: Corticosteroid use may cause psychiatric disturbances, including depression, euphoria, insomnia, mood swings, and personality changes. Pre-existing psychiatric conditions may be exacerbated by corticosteroid use.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with HF; long-term use has been associated with fluid retention and hypertension.
• Diabetes: Use with caution in patients with diabetes mellitus; may alter glucose production/regulation leading to hyperglycemia.
• Gastrointestinal disease: Use with caution in patients with GI diseases (diverticulitis, peptic ulcer, ulcerative colitis) due to perforation risk.
• Hepatic impairment: Use with caution in patients with hepatic impairment, including cirrhosis; long-term use has been associated with fluid retention.
• Myasthenia gravis: Use with caution in patients with myasthenia gravis; exacerbation of symptoms has occurred especially during initial treatment with corticosteroids.
• Myocardial infarction (MI): Use with caution following acute MI; corticosteroids have been associated with myocardial rupture.
• Osteoporosis: Use with caution in patients with osteoporosis; high doses and/or long-term use of corticosteroids have been associated with increased bone loss and osteoporotic fractures.
• Renal impairment: Use with caution in patients with renal impairment; fluid retention may occur.
• Seizure disorders: Use with caution in patients with a history of seizure disorder; seizures have been reported with adrenal crisis.
• Thyroid disease: Changes in thyroid status may necessitate dosage adjustments; metabolic clearance of corticosteroids increases in hyperthyroid patients and decreases in hypothyroid ones.
Special populations:
• Elderly: Because of the risk of adverse effects, systemic corticosteroids should be used cautiously in the elderly in the smallest possible effective dose for the shortest duration.
• Pediatrics: May affect growth velocity; growth should be routinely monitored in pediatric patients.
Other warnings/precautions:
• Discontinuation of therapy: Withdraw therapy with gradual tapering of dose.
Metabolism/Transport Effects
Substrate of CYP3A4 (minor); Inhibits CYP3A4 (weak)
Interactions
 
Acetylcholinesterase Inhibitors: Corticosteroids (Systemic) may enhance the adverse/toxic effect of Acetylcholinesterase Inhibitors. Increased muscular weakness may occur. Risk C: Monitor therapy
Aldesleukin: Corticosteroids may diminish the antineoplastic effect of Aldesleukin. Risk X: Avoid combination
Aminoglutethimide: May increase the metabolism of Corticosteroids (Systemic). Risk C: Monitor therapy
Amphotericin B: Corticosteroids (Systemic) may enhance the hypokalemic effect of Amphotericin B. Risk C: Monitor therapy
Antacids: May decrease the bioavailability of Corticosteroids (Oral). Risk D: Consider therapy modification
Antidiabetic Agents: Corticosteroids (Systemic) may diminish the hypoglycemic effect of Antidiabetic Agents. In some instances, corticosteroid-mediated HPA axis suppression has led to episodes of acute adrenal crisis, which may manifest as enhanced hypoglycemia, particularly in the setting of insulin or other antidiabetic agent use. Risk C: Monitor therapy
Antifungal Agents (Azole Derivatives, Systemic): May decrease the metabolism of Corticosteroids (Systemic). Risk C: Monitor therapy
Aprepitant: May increase the serum concentration of Corticosteroids (Systemic). Risk D: Consider therapy modification
Barbiturates: May decrease the serum concentration of Corticosteroids (Systemic). Risk C: Monitor therapy
BCG: Immunosuppressants may diminish the therapeutic effect of BCG. Risk X: Avoid combination
Bile Acid Sequestrants: May decrease the absorption of Corticosteroids (Oral). Risk C: Monitor therapy
Calcitriol: Corticosteroids (Systemic) may diminish the therapeutic effect of Calcitriol. Risk C: Monitor therapy
Calcium Channel Blockers (Nondihydropyridine): May decrease the metabolism of Corticosteroids (Systemic). Exceptions: Bepridil [Off Market]. Risk C: Monitor therapy
Coccidioidin Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioidin Skin Test. Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (Low risk). Risk C: Monitor therapy
Corticorelin: Corticosteroids may diminish the therapeutic effect of Corticorelin. Specifically, the plasma ACTH response to corticorelin may be blunted by recent or current corticosteroid therapy. Risk C: Monitor therapy
CycloSPORINE: PrednisoLONE (Systemic) may increase the serum concentration of CycloSPORINE. PrednisoLONE (Systemic) may decrease the serum concentration of CycloSPORINE. CycloSPORINE may increase the serum concentration of PrednisoLONE (Systemic). Risk C: Monitor therapy
CycloSPORINE (Systemic): PrednisoLONE (Systemic) may decrease the serum concentration of CycloSPORINE (Systemic). PrednisoLONE (Systemic) may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of PrednisoLONE (Systemic). Risk C: Monitor therapy
Deferasirox: Corticosteroids (Systemic) may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Risk C: Monitor therapy
Deferasirox: Corticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Risk C: Monitor therapy
Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. Risk C: Monitor therapy
Echinacea: May diminish the therapeutic effect of Immunosuppressants. Risk D: Consider therapy modification
Estrogen Derivatives: May increase the serum concentration of Corticosteroids (Systemic). Risk C: Monitor therapy
Fluconazole: May decrease the metabolism of Corticosteroids (Systemic). Risk C: Monitor therapy
Fosaprepitant: May increase the serum concentration of Corticosteroids (Systemic). The active metabolite aprepitant is likely responsible for this effect. Risk D: Consider therapy modification
Isoniazid: Corticosteroids (Systemic) may decrease the serum concentration of Isoniazid. Risk C: Monitor therapy
Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Risk D: Consider therapy modification
Loop Diuretics: Corticosteroids (Systemic) may enhance the hypokalemic effect of Loop Diuretics. Risk C: Monitor therapy
Macrolide Antibiotics: May decrease the metabolism of Corticosteroids (Systemic). Exceptions: Azithromycin; Azithromycin (Systemic); Fidaxomicin (Systemic); Spiramycin. Risk D: Consider therapy modification
Mitotane: May decrease the serum concentration of Corticosteroids (Systemic). Risk D: Consider therapy modification
Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Risk X: Avoid combination
Neuromuscular-Blocking Agents (Nondepolarizing): May enhance the adverse neuromuscular effect of Corticosteroids (Systemic). Increased muscle weakness, possibly progressing to polyneuropathies and myopathies, may occur. Risk D: Consider therapy modification
NSAID (COX-2 Inhibitor): Corticosteroids (Systemic) may enhance the adverse/toxic effect of NSAID (COX-2 Inhibitor). Risk C: Monitor therapy
NSAID (Nonselective): Corticosteroids (Systemic) may enhance the adverse/toxic effect of NSAID (Nonselective). Risk C: Monitor therapy
Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Risk X: Avoid combination
Primidone: May decrease the serum concentration of Corticosteroids (Systemic). Risk C: Monitor therapy
Quinolone Antibiotics: May enhance the adverse/toxic effect of Corticosteroids (Systemic). Risk of tendon-related side effects, including tendonitis and rupture, may be enhanced. Risk C: Monitor therapy
Rifamycin Derivatives: May increase the metabolism of Corticosteroids (Systemic). Risk C: Monitor therapy
Roflumilast: May enhance the immunosuppressive effect of Immunosuppressants. Risk D: Consider therapy modification
Salicylates: May enhance the adverse/toxic effect of Corticosteroids (Systemic). These specifically include gastrointestinal ulceration and bleeding. Corticosteroids (Systemic) may decrease the serum concentration of Salicylates. Withdrawal of corticosteroids may result in salicylate toxicity. Risk C: Monitor therapy
Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Risk C: Monitor therapy
Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Risk X: Avoid combination
Telaprevir: Corticosteroids (Systemic) may decrease the serum concentration of Telaprevir. Telaprevir may increase the serum concentration of Corticosteroids (Systemic). Management: Concurrent use of telaprevir and systemic corticosteroids is not recommended. When possible, consider alternatives. If used together, employ extra caution and monitor closely for excessive corticosteroid effects and diminished telaprevir effects. Risk D: Consider therapy modification
Telaprevir: May increase the serum concentration of Corticosteroids. Corticosteroids may decrease the serum concentration of Telaprevir. Management: Concurrent use of telaprevir and systemic corticosteroids is not recommended. When possible, consider alternatives. If used together, employ extra caution and monitor closely for excessive corticosteroid effects and diminished telaprevir effects. Risk D: Consider therapy modification
Thiazide Diuretics: Corticosteroids (Systemic) may enhance the hypokalemic effect of Thiazide Diuretics. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Risk C: Monitor therapy
Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Risk C: Monitor therapy
Vaccines (Live): Corticosteroids (Systemic) may enhance the adverse/toxic effect of Vaccines (Live). Risk D: Consider therapy modification
Warfarin: Corticosteroids (Systemic) may enhance the anticoagulant effect of Warfarin. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may increase gastric mucosal irritation).
Food: Prednisolone interferes with calcium absorption. Limit caffeine.
Herb/Nutraceutical: St John's wort may decrease prednisolone levels. Avoid cat's claw, echinacea (have immunostimulant properties).
Pregnancy
 
C/D
Pregnancy Implications
Adverse events have been observed with corticosteroids in animal reproduction studies. Prednisolone crosses the placenta; prior to reaching the fetus, prednisolone is converted by placental enzymes to prednisone. As a result, the amount of prednisolone reaching the fetus is ~8-10 times lower than the maternal serum concentration (healthy women at term; similar results observed with preterm pregnancies complicated by HELLP syndrome). Human studies have shown an association between first trimester corticosteroid use and oral clefts. Additional adverse events in the fetus/neonate, including low birth weight, have been noted in case reports following large doses of systemic corticosteroids during pregnancy. Women exposed to prednisolone during pregnancy for the treatment of an autoimmune disease may contact the OTIS Autoimmune Diseases Study at 877-311-8972.
Lactation
 
Enters breast milk/use caution (AAP rates “compatible”; AAP 2001 update pending)
Breast-Feeding Considerations
Prednisolone is excreted into breast milk with peak concentrations occurring ~1 hour after the maternal dose. The milk/plasma ratio was found to be 0.2 with doses ≥30 mg/day and 0.1 with doses <30 mg/day. Following a maternal dose of prednisolone 80 mg/day, a breast-feeding infant would ingest <0.1% of the dose.
Monitoring Parameters
 
Blood pressure; blood glucose, electrolytes; intraocular pressure (use >6 weeks); bone mineral density; growth in children
Mechanism of Action
 
Decreases inflammation by suppression of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability; suppresses the immune system by reducing activity and volume of the lymphatic system
Pharmacodynamics / Kinetics
 
Duration: 18-36 hours
Protein binding (concentration dependent): 65% to 91%; decreased in elderly
Metabolism: Primarily hepatic, but also metabolized in most tissues, to inactive compounds
Half-life elimination: 3.6 hours; End-stage renal disease: 3-5 hours
Excretion: Primarily urine (as glucuronides, sulfates, and unconjugated metabolites)
 
   
 
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