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Pronunciation |
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(pred
NIS oh
lone) |
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U.S. Brand
Names |
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AK-Pred® Ophthalmic;
Articulose-50® Injection; Delta-Cortef® Oral;
Econopred® Ophthalmic; Econopred® Plus Ophthalmic;
Inflamase® Forte Ophthalmic; Inflamase® Mild Ophthalmic;
Key-Pred® Injection; Key-Pred-SP® Injection;
Pediapred® Oral; Predcor-TBA® Injection; Pred Forte®
Ophthalmic; Pred Mild® Ophthalmic; Prednisol® TBA Injection;
Prelone®
Oral |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Novo-Prednisolone |
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Synonyms |
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Deltahydrocortisone; Metacortandralone; Prednisolone Acetate; Prednisolone
Acetate, Ophthalmic; Prednisolone Sodium Phosphate; Prednisolone Sodium
Phosphate, Ophthalmic; Prednisolone Tebutate |
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Pharmacological Index |
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Corticosteroid, Ophthalmic; Corticosteroid, Parenteral |
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Use |
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Treatment of palpebral and bulbar conjunctivitis; corneal injury from
chemical, radiation, thermal burns, or foreign body penetration; endocrine
disorders, rheumatic disorders, collagen diseases, dermatologic diseases,
allergic states, ophthalmic diseases, respiratory diseases, hematologic
disorders, neoplastic diseases, edematous states, and gastrointestinal diseases;
useful in patients with inability to activate prednisone (liver
disease) |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Acute superficial herpes simplex keratitis; systemic fungal infections;
varicella; hypersensitivity to prednisolone or any
component |
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Warnings/Precautions |
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Use with caution in patients with hyperthyroidism, cirrhosis, nonspecific
ulcerative colitis, hypertension, osteoporosis, thromboembolic tendencies, CHF,
convulsive disorders, myasthenia gravis, thrombophlebitis, peptic ulcer,
diabetes; acute adrenal insufficiency may occur with abrupt withdrawal after
long-term therapy or with stress; young pediatric patients may be more
susceptible to adrenal axis suppression from topical therapy. Because of the
risk of adverse effects, systemic corticosteroids should be used cautiously in
the elderly, in the smallest possible dose, and for the shortest possible
time. |
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Adverse
Reactions |
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>10%:
Central nervous system: Insomnia, nervousness
Gastrointestinal: Increased appetite, indigestion
1% to 10%:
Dermatologic: Hirsutism
Endocrine & metabolic: Diabetes mellitus
Neuromuscular & skeletal: Arthralgia
Ocular: Cataracts, glaucoma
Respiratory: Epistaxis
<1%: Edema, hypertension, vertigo, seizures, psychoses, pseudotumor
cerebri, headache, mood swings, delirium, hallucinations, euphoria, acne, skin
atrophy, bruising, hyperpigmentation, Cushing's syndrome, pituitary-adrenal axis
suppression, growth suppression, glucose intolerance, hypokalemia, alkalosis,
amenorrhea, sodium and water retention, hyperglycemia, peptic ulcer, nausea,
vomiting, abdominal distention, ulcerative esophagitis, pancreatitis, muscle
weakness, osteoporosis, fractures, muscle wasting, hypersensitivity reactions
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Overdosage/Toxicology |
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When consumed in excessive quantities for prolonged periods, systemic
hypercorticism and adrenal suppression may occur, in those cases discontinuation
and withdrawal of the corticosteroid should be done
judiciously. |
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Drug
Interactions |
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CYP3A enzyme substrate; inducer of cytochrome P-450 enzymes
Barbiturates, phenytoin, rifampin decrease corticosteroid effectiveness
Decreases salicylates
Decreases vaccines
Decreases toxoids effectiveness |
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Mechanism of
Action |
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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 |
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Pharmacodynamics/Kinetics |
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Duration: 18-36 hours
Protein binding: 65% to 91% (concentration dependent)
Metabolism: Primarily in the liver, but also metabolized in most tissues, to
inactive compounds
Half-life: 3.6 hours; Biological: 18-36 hours; End-stage renal disease: 3-5
hours
Elimination: In urine principally as glucuronides, sulfates, and unconjugated
metabolites |
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Usual Dosage |
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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. Consider alternate day therapy for long-term therapy.
Discontinuation of long-term therapy requires gradual withdrawal by tapering the
dose.
Acute asthma:
Oral: 1-2 mg/kg/day in divided doses 1-2 times/day for 3-5 days
I.V. (sodium phosphate salt): 2-4 mg/kg/day divided 3-4 times/day
Anti-inflammatory or immunosuppressive dose: Oral, I.V., I.M. (sodium
phosphate salt): 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 (long-term maintenance dose for frequent relapses): 0.5-1
mg/kg/dose given every other day for 3-6 months
Adults:
Oral, I.V., I.M. (sodium phosphate salt): 5-60 mg/day
Multiple sclerosis (sodium phosphate): Oral: 200 mg/day for 1 week followed
by 80 mg every other day for 1 month
Rheumatoid arthritis: Oral: Initial: 5-7.5 mg/day; adjust dose as necessary
Elderly: Use lowest effective dose
Dosing adjustment in hyperthyroidism: Prednisolone dose may need to
be increased to achieve adequate therapeutic effects
Hemodialysis: Slightly dialyzable (5% to 20%); administer dose
posthemodialysis
Peritoneal dialysis: Supplemental dose is not necessary
Intra-articular, intralesional, soft-tissue administration:
Tebutate salt: 4-40 mg/dose
Sodium phosphate salt: 2-30 mg/dose
Ophthalmic suspension/solution: Children and Adults: Instill 1-2 drops into
conjunctival sac every hour during day, every 2 hours at night until favorable
response is obtained, then use 1 drop every 4 hours |
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Dietary
Considerations |
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Should be taken after meals or with food or milk to decrease GI effects;
limit caffeine; increase dietary intake of pyridoxine, vitamin C, vitamin D,
folate, calcium, and phosphorus |
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Monitoring
Parameters |
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Blood pressure, blood glucose, electrolytes |
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Test
Interactions |
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Response to skin tests |
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Mental Health: Effects
on Mental Status |
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Nervousness and insomnia are common; may rarely cause delirium, mood swings,
euphoria, and hallucinations |
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Mental Health:
Effects on Psychiatric
Treatment |
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Barbiturates and carbamazepine may decrease corticosteroid
effectiveness |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take exactly as directed; do not increase dose or discontinue abruptly
without consulting prescriber. Take oral medication with or after meals. Limit
intake of caffeine or stimulants. Prescriber may recommend increased dietary
vitamins, minerals, or iron. Diabetics should monitor glucose levels closely
(antidiabetic medication may need to be adjusted). Inform prescriber if you are
experiencing greater than normal levels of stress (medication may need
adjustment). Some forms of this medication may cause GI upset (oral medication
may be taken with meals to reduce GI upset; small frequent meals and frequent
mouth care may reduce GI upset). You may be more susceptible to infection (avoid
crowds and persons with contagious or infective conditions). Report promptly
excessive nervousness or sleep disturbances; any signs of infection (sore
throat, unhealed injuries); excessive growth of body hair or loss of skin color;
changes in vision; excessive or sudden weight gain (>3 lb/week); swelling of
face or extremities; difficulty breathing; muscle weakness; change in color of
stools (black or tarry) or persistent abdominal pain; or worsening of condition
or failure to improve. Pregnancy precautions: Inform prescriber if you
are or intend to be pregnant. |
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Nursing
Implications |
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Do not administer acetate or tebutate salt I.V. |
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Dosage Forms |
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Injection:
As acetate (for I.M., intralesional, intra-articular, or soft tissue
administration only): 25 mg/mL (10 mL, 30 mL); 50 mg/mL (30 mL)
As sodium phosphate (for I.M., I.V., intra-articular, intralesional, or soft
tissue administration): 20 mg/mL (2 mL, 5 mL, 10 mL)
As tebutate (for intra-articular, intralesional, soft tissue administration
only): 20 mg/mL (1 mL, 5 mL, 10 mL)
Liquid, oral, as sodium phosphate: 5 mg/5 mL (120 mL)
Solution, ophthalmic, as sodium phosphate: 0.125% (5 mL, 10 mL, 15 mL); 1% (5
mL, 10 mL, 15 mL)
Suspension, ophthalmic, as acetate: 0.12% (5 mL, 10 mL); 0.125% (5 mL, 10 mL,
15 mL); 1% (1 mL, 5 mL, 10 mL, 15 mL)
Syrup: 15 mg/5 mL (240 mL)
Tablet: 5 mg |
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References |
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Report of a Workshop by the British Association for Paediatric Nephrology and
Research Unit, Royal College of Physicians,
"Consensus Statement on Management and Audit Potential for Steroid Responsive Nephrotic Syndrome,"
Arch Dis Child, 1994, 70(2):151-7. |
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