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Prednisolone

Pronouncation: (pred-NIS-oh-lone)
Class: Corticosteroid, Glucocorticoid Prednisolone

Trade Names:
Prednisolone
- Tablets 5 mg

ratio-Prednisolone (Canada)
Sandoz Prednisolone (Canada)
Prednisolone Acetate

Trade Names:
Econopred Plus
- Ophthalmic suspension 1%

Trade Names:
Flo-Pred
- Oral suspension 5 mg per 5 mL
- Oral suspension 15 mg per 5 mL

Trade Names:
Pred Forte
- Ophthalmic suspension 1%

Trade Names:
Pred Mild
- Ophthalmic suspension 0.12%

Trade Names:
Prelone
- Syrup 15 mg per 5 mL

Prednisolone Sodium Phosphate

Trade Names:
Orapred
- Oral solution 15 mg per 5 mL
- Orally disintegrating tablets 10 mg
- Orally disintegrating tablets 15 mg
- Orally disintegrating tablets 30 mg

Trade Names:
Pediapred
- Oral liquid 5 mg per 5 mL

Trade Names:
Prednisol
- Ophthalmic suspension 1%

Pharmacology

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Intermediate-acting glucocorticoid that depresses formation, release, and activity of endogenous mediators of inflammation, including prostaglandins, kinins, histamine, liposomal enzymes, and complement system. Also modifies body's immune response.

Pharmacokinetics

Absorption

Oral

Rapidly absorbed, reaching C _max in 1 to 2 h. C _max is approximately 336.8 ng•h/mL and AUC _0-t is approximately 1,946.8 ng•h/mL (15 mg).

Distribution

Plasma protein binding 70% to 90%. Vd is 0.22 to 0.7 L/kg.

Metabolism

Primarily hepatic.

Elimination

Excreted in the urine as sulfate and glucuronide conjugates. t _½ is 2 to 4 h.

Special Populations

Elderly

Mean unbound fraction of prednisolone was higher and V _ss unbound prednisolone was reduced in elderly patients.

Indications and Usage

Oral

Allergic conditions; collagen diseases (eg, systemic lupus erythematous, acute rheumatic carditis); dermatologic diseases; edematous states; endocrine conditions; GI diseases; hematologic diseases; neoplastic conditions; neoplastic diseases; nervous system conditions (eg, acute exacerbations of multiple sclerosis); ophthalmic conditions; conditions related to organ transplantation; pulmonary disease (eg, asthma); renal condition (eg, nephrotic syndrome); rheumatologic conditions; specific infectious diseases including trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used concomitantly with appropriate antituberculous chemotherapy; tuberculosis with pleural or pericardial effusion.

Ophthalmic Econopred Plus, Prednisol, Pred Forte

Treatment of steroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe.

Econopred Plus, Prednisol

Treatment of corneal injury from chemical, radiation, or thermal burns, or penetration of foreign bodies.

Pred Mild

Treatment of mild to moderate noninfectious allergic and inflammatory disorders of the lid, conjunctiva, cornea, and sclera (including chemical and thermal burns).

Contraindications

Oral

Hypersensitivity to corticosteroids or any component of the product; systemic fungal infections; administration of live, or live, attenuated vaccines in patients receiving immunosuppressive doses.

Ophthalmic

Most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella; mycobacterial infection of the eye and fungal diseases of the ocular structure; acute untreated purulent ocular infections; hypersensitivity to other corticosteroids or any component of the product.

Dosage and Administration

Adults

PO 5 to 60 mg/day. Oral disintegrating tablet: 10 to 60 mg/day.

Children

PO Range of initial dose is 0.14 to 2 mg/kg/day in 3 or 4 divided doses (4 to 60 mg/m ² /day).

Adults

Ophthalmic Econopred , Prednisol : 2 drops in affected eye(s) 4 times daily. In cases of bacterial infections, concomitant use of anti-infective agents is mandatory. Pred Forte , Pred Mild : Instill 1 to 2 drops into conjunctival sac 2 to 4 times daily. The dose frequency may be increased if necessary during the first 24 to 48 h.

Multiple Sclerosis
Adults

PO 200 mg/day for 1 wk, then 80 mg every other day for 1 mo.

Nephrotic Syndrome
Children

PO 60 mg/m ² /day in 3 or 4 divided doses for 4 wk, followed by 4 wk of single dose alternate-day therapy at 40 mg/m ² /day.

Asthma
Children

PO 1 to 2 m/kg/day in single or divided doses. A short course, or burst therapy, should be continued until children achieve a peak expiratory flow rate of 80% of their personal best or symptoms resolve, which usually requires 3 to 10 days of treatment, although it can take longer.

General Advice

Alternate-day therapy, a corticosteroid dosing regimen in which twice the usual daily dose is administered every other day, is used to provide patients requiring long-term pharmacologic dose treatment with the beneficial effects of prednisolone while minimizing certain adverse reactions (eg, pituitary-adrenal suppression, Cushingoid state, growth suppression in children).
Do not break or use partial orally disintegrating tablets.
Ophthalmic suspensions: Shake well before using.
Ophthalmic use: If signs and symptoms do not improve after 2 days, re-evaluate the patient.
Ophthalmic use: Care should be taken not to discontinue prematurely.

Storage/Stability

Oral tablets

Store at 68° to 77°F. Protect oral disintegrating tablets from moisture.

Orapred

Store at 36° to 46°F.

Prelone

Store at 59° to 86°F.

Pediapred

Store at 39° to 77°F. May be refrigerated.

Ophthalmic suspension Econopred , Prednisol

Store at 46° to 75°F in an upright position.

Flo-Pred

Store at 68° to 77°F.

Pred Forte

Store at temperatures up to 75°F in an upright position. Protect from freezing.

Pred Mild

Store at 59° to 86°F in an upright position. Protect from freezing.

Drug Interactions

Aminoglutethimide

May lead to loss of prednisolone-induced adrenal suppression.

Amphotericin B

Coadministration may be followed by cardiac enlargement and CHF.

Anticholinesterase agents

Coadministration may produce severe weakness in patients with myasthenia gravis. If possible, withdraw anticholinesterase agent 24 h prior to starting prednisolone.

Antidiabetic agents

Because prednisolone may increase blood glucose concentrations, dose adjustments of antidiabetic agents may be required.

Aspirin and other salicylates, NSAIDs

Risk of GI bleeding may be increased. Salicylate clearance may be increased.

CYP3A4 inducers (eg, barbiturates, carbamazepine, phenytoin, rifampin)

Prednisolone metabolism may be increased, reducing prednisolone plasma levels and necessitating an increase in dosage.

CYP3A4 inhibitors (eg, estrogens [eg, hormonal contraceptives], ketoconazole, macrolide antibiotics [eg, erythromycin])

Prednisolone metabolism may be decreased, increasing prednisolone plasma levels and increasing the risk of adverse reactions.

Cholestyramine

Prednisolone clearance may be increased, reducing plasma levels and decreasing the efficacy.

Cyclosporine

Increased activity of cyclosporine and prednisolone may occur. Convulsions have been reported with coadministration of corticosteroids and cyclosporine.

Digitalis glycosides

Because of possible hypokalemia, the risk of arrhythmias may be increased.

Isoniazid

Isoniazid serum levels may be reduced, decreasing the efficacy.

Potassium-depleting agents (eg, amphotericin B, diuretics)

Risk of hypokalemia may be increased.

Toxoids and live or inactivated vaccines

Because of inhibition of antibody response, patients on prolonged prednisolone therapy may exhibit a diminished response to toxoids and live or inactivated vaccines. Replication of some organisms contained in live attenuated vaccines may be potentiated.

Warfarin

Because data are conflicting, monitor coagulation indices frequently.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Bradycardia; cardiac arrest; cardiac arrhythmias; cardiac enlargement; CHF; circulatory collapse; elevated BP; fat embolism; hypertension; hypertrophic cardiomyopathy in premature infants; myocardial rupture following recent MI; pulmonary edema; syncope; tachycardia; thromboembolism; thrombophlebitis; vasculitis.

CNS

Arachnoiditis; behavioral and mood changes; convulsions; depression; emotional instability; euphoria; headache; increased appetite; increased intracranial pressure with papilledema (pseudotumor cerebri) usually following discontinuation of therapy; insomnia; malaise; meningitis; mood swings; neuritis; neuropathy; paraparesis/paraplegia; paresthesia; personality changes; sensory disturbances; vertigo.

Dermatologic

Acne; allergic dermatitis; cutaneous and subcutaneous atrophy; dry scalp; edema; facial erythema; hyper- or hypopigmentation; impaired wound healing; increased sweating; petechiae and ecchymosis; rash; sterile abscess; striae; suppressed reactions to skin tests; thin fragile skin; thinning scalp hair; urticaria.

EENT

Exophthalmos; glaucoma; increased IOP; posterior subcapsular cataracts.

Ophthalmic use

Acute anterior uveitis; conjunctival hyperemia; conjunctivitis; corneal ulcers; delayed wound healing; glaucoma; increased IOP; keratitis; loss of accommodation; mydriasis; optic nerve damage; perforation of the globe; posterior subcapsular cataract formation; ptosis; secondary ocular infection (eg, bacterial, viral).

GI

Abdominal distention; elevation in serum liver enzymes levels; hepatomegaly; hiccups; nausea; pancreatitis; peptic ulcer with possible perforation and hemorrhage; ulcerative esophagitis.

Endocrine

Abnormal fat deposits; decreased carbohydrate tolerance; development of Cushingoid state; hirsutism; manifestations of latent diabetes mellitus and increased requirement for insulin and oral hypoglycemic agents in diabetes; menstrual irregularities; moon facies; secondary adrenocortical and pituitary unresponsiveness (particularly during stress, as in trauma, surgery, or illness); suppression of growth in children.

Genitourinary

Alteration in motility and number of spermatozoa.

Hypersensitivity

Anaphylactoid reaction; anaphylaxis; angioedema.

Metabolic-Nutritional

Alterations in blood glucose; fluid retention; hypokalemic alkalosis; negative nitrogen balance due to catabolism; potassium loss; sodium retention; weight gain.

Musculoskeletal

Aseptic necrosis of femoral and humeral heads; charcot-like arthropathy; loss of muscle mass; muscle weakness; osteoporosis; pathologic fracture of long bones; steroid myopathy; tendon rupture; vertebral compression fractures.

Precautions

Monitor

Body weight, BP, routine laboratory studies, including 2-hour postprandial blood glucose and serum potassium, and a chest x-ray, should be obtained at regular intervals during prolonged therapy. Monitor linear growth of infants and children on prolonged therapy. Upper GI x-rays are desirable in patients with known or suspected peptic ulcer disease. If ophthalmic product is used for more than 10 days or oral product more than 6 wk, routinely monitor IOP.

Pregnancy

Category C .

Flo-Pred

Category D .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established (ophthalmic).

Elderly

Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Hypersensitivity

Reactions may occur, including anaphylaxis.

Renal Function

Use drug with caution.

Adrenal suppression

Prolonged therapy may lead to hypothalamic-pituitary-adrenal suppression.

Bone density

Bone formation may be decreased and bone resorption may be increased. Long-term use in children can have negative effects on growth and development.

Cardiovascular effects

Use drug with great caution in patient who has suffered recent MI.

Cardiovascular/renal function

Prednisolone may cause elevation of BP, salt and water retention, and increased excretion of calcium and potassium.

Cerebral malaria

Do not use.

Fetal effects

Can cause fetal harm when administered to pregnant women. Use during the first trimester of pregnancy has been associated with an increased risk of orofacial clefts, intrauterine growth restriction, and decreased birth weight.

GI disorders

Risk of GI perforation in patients with certain GI disorders may be increased (eg, active or latent peptic ulcers).

Infections

Signs of infection may be masked. Host-defense mechanisms may be decreased, allowing dissemination of infection. Risk of reactivation or exacerbation of latent infection may be increased.

Kaposis sarcoma

Has been reported in patients receiving corticosteroid therapy, usually for chronic conditions.

Long-term ophthalmic local use

Fungal infections of the cornea are particularly prone to develop with chronic use of corticosteroids, and fungal infections should be suspected in any persistent corneal ulceration.

Mood and behavior disturbances

Use may be associated with CNS effects ranging from euphoria, insomnia, mood swings, personality changes, and severe depression to frank psychotic manifestations. Existing emotional instability or psychotic tendencies may be aggravated.

Ocular effects

Use systemic drug with caution in ocular herpes simplex because of possible corneal perforation.

Ophthalmic effects

Prolonged use may produce posterior subcapsular cataracts and glaucoma with possible damage to the optic nerve, and may enhance the establishment of secondary ocular infections due to fungi or viruses. Use with caution in patients with glaucoma. Do not use in the treatment of optic neuritis.

Stress

Increased dosage of rapidly acting corticosteroid may be needed before, during, and after stressful situations.

Surgery

Use after cataract surgery may delay healing and increase the incidence of bleb formation.

Threadworm infestation

Use with great care.

Thyroid status

Changes in thyroid status may necessitate adjustments in prednisolone dosage.

Tuberculosis

Restrict use to those cases of fulminating or disseminated tuberculosis in which prednisolone is used for management of the disease in conjunction with an appropriate antituberculous regimen.

Withdrawal

Abrupt discontinuation may result in adrenal insufficiency.

Overdosage

Symptoms

The effects of ingestion of large quantities over a short period of time have not been reported.

Patient Information

Advise patient to take single daily or alternate-day doses in morning before 9 am and to take multiple doses at evenly-spaced intervals throughout day.
Instruct patient to take medication with meals or snacks to avoid GI irritation.
Caution patient not to take drug with aspirin or other OTC medications containing salicylates unless directed by health care provider.
Instruct patient to check weight at home daily at same time of day.
Advise patient on chronic steroid therapy to wear medical identification (eg, card, bracelet) indicating condition and drug regimen.
Remind patient to wash hands before and after ophthalmic instillation.
Teach patient correct method for instilling eye drops.
Instruct patient not to rub eyes or touch dropper into eye.
Inform patient of increased appetite and counsel patient on appropriate diet management (ie, diet high in protein, calcium, and potassium but low in sodium and carbohydrates).
Advise family that medication may slow growth in children.
Inform patient of the possible adverse reactions of moonface, mood swings, and increased emotions.
Teach patient to monitor for infection, eye burning, or increased bruising.
Instruct patient not to drive soon after using eye drops because vision may be blurred initially.
Inform patient that ophthalmic preparation may cause sensitivity to bright light and recommend use of sunglasses to minimize this effect.
Instruct patient to report the following symptoms to health care provider: black, tarry stools; menstrual irregularities; muscle weakness; prolonged sore throat, fever, cold, or infection; puffing of face; swelling of lower extremities; unusual weight gain; vomiting of blood.
Tell patient to notify health care provider if the following symptoms occur after dosage reduction or withdrawal of therapy: anorexia, diarrhea, dizziness, fatigue, low blood sugar, nausea, vomiting, weakness, weight loss.