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«Presentation APO-PREDNISONE 1mg tablets are round, white, biconvex, 5.5mm in diameter and identified P over 1 on one side. Each tablet contains 1mg ...»

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New Zealand Data Sheet

APO-PREDNISONE

Prednisone 1mg, 2.5mg, 5mg and 20mg Tablets

Presentation

APO-PREDNISONE 1mg tablets are round, white, biconvex, 5.5mm in diameter and identified P over 1 on one

side. Each tablet contains 1mg prednisone and typically weighs 80mg.

APO-PREDNISONE 2.5mg tablets are round, white, biconvex, 6.0mm in diameter and identified P over 2.5 on

one side. Each tablet contains 2.5mg prednisone and typically weighs 87mg.

APO-PREDNISONE 5mg tablets are round, white, flat-faced with bevelled edges, 6.5mm in diameter and identified P over 5 on one side. Each tablet contains 5mg prednisone and typically weighs 94mg.

APO-PREDNISONE 20mg tablets are round, pink, biconvex, 6.5mm in diameter and identified P over 20 with a breakline on one side. Each tablet contains 20mg prednisone and typically weighs 97mg.

Uses Actions Prednisone is a biologically inert glucocorticosteroid which is rapidly converted in the liver to its active metabolite prednisolone. Glucocorticosteroids chief pharmacological effects are upon gluconeogenesis, glycogen deposition and protein and calcium metabolism. Glucocorticoids possess marked anti-inflammatory, anti-allergic and anti- rheumatic properties where they decrease the vascular and cellular component of the inflammatory response.

Immunosuppressant properties are also exhibited especially with pharmacological doses.

Prednisone is a potent therapeutic agent influencing the biochemical behaviour of most tissues in the body.

When prednisone is compared with the naturally occurring glucocorticoids, cortisone and cortisol (hydrocortisone), its anti-inflammatory effects are 5 times more potent whilst its mineralocorticoid properties are less pronounced. The onset of action of prednisone varies considerably depending on the dose and condition for which it is used. Its duration of action is approximately 18 to 36 hours.

Pharmacokinetics Prednisone is readily absorbed from the gastro-intestinal tract and has a preconversion biological half-life of about 60 minutes before hydroxylation in the liver to its active metabolite prednisolone. Prednisolone has a plasma half-life of 2 to 3 hours and is extensively bound to plasma proteins. There are wide inter-individual differences in the rate of metabolism of prednisolone. Prednisolone is metabolised primarily in the liver to biologically inactive metabolites (primarily the gluconoride and sulphate). Prednisone is excreted in the urine as free and conjugated metabolites together with an appreciable amount of unchanged prednisolone. The conversion of prednisone is probably not diminished by liver disease.

Indications

Glucocorticoids are used to suppress the clinical manifestations of disease in a wide range of disorders such as:

bronchial asthma, emphysema, pulmonary fibrosis, allergic skin reactions, blood disorders including auto-immune haemolytic anaemia and idiopathic thrombocytopenic purpura, selected collagen and rheumatic disorders (but rarely rheumatoid arthritis), connective tissue disorders such as arteritis and systemic lupus erythematosus, inflammatory bowel disease such as ulcerative colitis and Crohn's disease, some hepatic disorders such as chronic active hepatitis, nephritic syndrome and other renal disorders, selected inflammatory ocular diseases, acute exacerbations of eczema, exfoliate dermatitis and pemphigus, and some neurological disorders such as infantile seizures (epilepsy) and sub-acute demyelinating polyneuropathy.

Miscellaneous uses include raised intracranial pressure, sarcoidosis, the neonatal respiratory distress syndrome, the gastric acid aspiration syndrome, acute rheumatic fever with carditis and occasionally hypercalcaemia.

Glucocorticoids may be used in conjunction with antineoplastic agents in regimens for the management of

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malignant disease such as leukaemia. They are also used to suppress the rejection phenomenon in tissue transplants.

Dosage and Administration The smallest dose which is effective or produces adequate control should be used since inhibition of corticotrophin secretion is related to dose and the duration of glucocorticoid therapy. Alternate day early-morning dosage regimens produce less suppression of the HPA (Hypothalmic-pituitary-adrenal) axis but may not always provide adequate control - this regimen is not recommended for treatment of haematological disorders, malignancies, ulcerative colitis or severe conditions.

It may be necessary to increase dosage temporarily during maintenance therapy or during a steroid withdrawal programme for flare-ups of the underlying disease or for major stress such as infection or trauma. When pharmacological doses of glucocorticoids are to be reduced or withdrawn the dosage must be tapered gradually;

this will be limited by the underlying disease process and the recovery of the HPA axis. Sudden cessation can be dangerous.

Take with food and a full glass of water.

Adults:

The initial dose of prednisone is 10mg - 100mg daily in divided doses, as a single daily dose at 8.00am or as a double dose on alternate days.

The maintenance dose is usually 5mg to 20mg daily. The dose should be individualised according to the severity of the disease and the patient’s response rather than by age or body weight.





The usual adult prescribing limit is up to 250mg daily.

Short Term Therapy:

20mg to 40mg daily with dosage reductions of 2.5mg or 5mg every 2 to 4 days depending on response.

Children:

For infants and children the dosage should be governed by the severity and expected duration of the disease and reaction to medication rather than a strict adherence to the ratio indicated by age or bodyweight. For the treatment of adrenocortical insufficiency the USPDI recommends that doses be based on body surface area.

Typically, for children over 18 months of age, initial dosage is 0.5mg/kg daily. This dosage can be doubled or trebled until definitive remission occurs. Maintenance dose is 0.125 - 0.25mg/kg daily.

Contraindications Hypersensitivity to any ingredient Systemic infections unless specific anti-infective therapy is given.

Live virus immunisation Pancreatitis (except pancreatitis caused by sarcoidosis) Warnings and Precautions Ideally corticosteroid therapy should not be instituted until a definite diagnosis has been made since the clinical signs and symptoms of disease can be masked or inhibited.

Abrupt withdrawal of prednisone after chronic use may precipitate acute adrenal insufficiency as a result of the suppression of corticotrophin at the anterior pituitary. Symptoms of adrenal insufficiency include malaise, muscle weakness, mental changes, muscle and joint pain, desquamation of the skin, dyspnoea, anorexia, nausea and vomiting, fever, hypoglycaemia, hypotension and dehydration.

The withdrawal symptoms may simulate a clinical relapse of the disease for which the patient is undergoing treatment. Withdrawal of prednisone should always be gradual, the rate depending on the individual patient’s response, the dose and duration of therapy.

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A degree of inhibition of hypothalmo-pituitary-adrenocortical function may persist for 6 to 12 months after prolonged high-dose treatment is withdrawn; steroid therapy may need be re-instituted during periods of stress.

General Precautions Caution is necessary when oral corticosteroids are used in patients with the following conditions and frequent

monitoring is necessary:

 Hypertension  Hypothyroidism  Congestive Heart failure or recent myocardial infarction  Liver failure  Renal insufficiency  Diabetes mellitus or in those with a family history of diabetes  Osteoporosis  Glaucoma  Patients with a history of severe affective disorders particularly of steroid induced psychoses  Epilepsy and/or seizure disorder  Peptic ulceration  Previous steroid myopathy  Tuberculosis  Patients with myasthenia gravis receiving anticholinesterase therapy since prednisone may decrease plasma anticholinesterase activity  Patients with thromboembolic disorders  Patients with Duchenne’s muscular dystrophy since transient rhabdomyolysis and myoblobinuria have been reported following strenuous physical activity  Patients with Cushing’s disease Adrenocortical Insufficiency Pharmacologic doses of corticosteroids administered for prolonged periods may result in hypothalamicpituitary-adrenal (HPA) suppression (secondary adrenocortical insufficiency). The degree and duration of adrenocortical insufficiency produced is variable among patients and depends on the dose, frequency, time of administration and duration of therapy.

Symptoms of adrenal insufficiency include: malaise, muscle weakness, mental changes, muscle and joint pain, desquamation of the skin, dyspnoea, anorexia, nausea and vomiting, fever, hypoglycaemia, hypotension and dehydration.

During prolonged courses of corticosteroid therapy sodium intake may need to be reduced and calcium and potassium supplements may be necessary. Monitoring of fluid intake and output and daily weight records may give an early warning of fluid retention.

Acute adrenal insufficiency leading to a fatal outcome may occur if glucocorticoids are withdrawn abruptly, therefore withdrawal of prednisone should always be gradual. A degree of adrenal insufficiency may persist for 6 to 12 months; therefore in any situation of stress occurring during that period steroid therapy may need to be reinstituted. Since mineralocorticoid secretion may be impaired treatment with salt and/or a mineralocorticoid may also be needed.

During prolonged therapy, any intercurrent illness, trauma or surgical procedure will require a temporary increase in dosage.

Anti-inflammatory/ Immunosuppressive effects and Infection Suppression of the inflammatory response and immune function increases susceptibility to infections and their severity. The clinical presentation may often be atypical and serious infections such as septicaemia and tuberculosis may be masked and may reach an advanced stage before being recognized when corticosteroids including prednisone are used. The immunosuppressive effects of glucocorticoids may result in activation of latent infection or exacerbation of intercurrent infections.

Chickenpox is of particular concern since this may be fatal in immunosuppressed patients. Patients without a definite history of chickenpox should be advised to avoid close personal contact with chickenpox or herpes Please refer to Medsafe website (www.medsafe.govt.nz) for the most recent datasheet Page 3 APO-PREDNISONE

Prednisone 1mg, 2.5mg, 5mg and 20mg Tablets

zoster and if exposed they should seek urgent medical attention. Passive immunization is recommended for non-immune patients who do come into contact with chickenpox. If a diagnosis of chickenpox is confirmed the illness warrants specialist care and urgent treatment.

Live vaccines are contraindicated in individuals on high doses of corticosteroids and should be postponed until at least 3 months after stopping corticosteroid therapy.

Ocular Effects Prolonged use of corticosteroids may produce subcapsular cataracts and nuclear cataracts (particularly in children), exophthalmos or increased intraocular pressure, which may result in glaucoma with possible damage to the optic nerves.

Corticosteroids should only be initiated in patients with ocular herpes simplex with appropriate viral cover by ophthalmologists because of the risk of corneal scaring loss of vision and corneal perforation.

Psychiatric effects Patients and/or careers should be warned that potentially severe psychiatric reactions may occur. Symptoms typically emerge within a few days or weeks of starting treatment. Most reactions recover after either dose reduction or withdrawal, although specific treatment may be necessary. Patients and/or carers should be encouraged to seek medical advice is worrying psychological symptoms develop, especially if depressed mood or suicidal ideation is suspected.

Particular care is required when considering the use of prednisone in patients with existing or previous history of severe affective disorders.

Psychic derangements range from euphoria, insomnia, mood swings, personality changes and severe depression to frank psychotic manifestations.

Use in Pregnancy and Lactation Category A Prednisone crosses the placenta and although there have been reports of foetal abnormalities in animal studies these findings do not seem to be relevant to humans. Use in pregnancy requires that the possible benefit to the mother be weighed against the potential hazards to the foetus.

Corticosteroids appear in breast milk but physiologic doses of 5mg or less of Prednisone per day are not considered likely to affect the infant adversely. However, the use of higher doses could suppress growth, interfere with endogenous corticosteroid production or cause other unwanted effects and is therefore not recommended.

Use in Children Corticosteroids cause growth retardation in infancy, childhood and adolescence, which may be irreversible and therefore long-term administration of pharmacological doses should be avoided. If prolonged therapy is necessary, treatment should be limited to the minimum suppression of the hypothalamo-pituitary adrenal axis and growth retardation, the growth and development of infants and children should be closely monitored.

Treatment should be administered where possible as a single dose on alternate days.

Children are at special risk from raised intracranial pressure.

Use in the Elderly Long-term use in the elderly should be planned bearing in mind the more serious consequences of the common side-effects of prednisone in old age, especially osteoporosis, diabetes, hypertension, hypokalaemia, susceptibility to infection and thinning of the skin. Close medical supervision is required to avoid life threatening reactions.

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Adverse Effects Adverse effects are generally related to dose and duration of treatment. Their incidence increases steeply if dosage exceeds 7.5mg prednisone daily.



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