Methylprednisolone

Registered South African indications:

• Anti-inflammatory
• Immune-modulation

Contraindications

Methylprednisolone Acetate

• Hypersensitivity to the active ingredient or any of its excipients
• Systemic fungal infections
• Systemic therapy is contraindicated in patients with arrested tuberculosis, peptic ulcer, acute psychoses, Cushing's syndrome, herpes simplex keratitis, vaccinia and varicella
• Intrathecal, epidural or intravenous route of administration
• Administration of live or live, attenuated vaccines is contraindicated in patients receiving immunosuppressive doses of methylprednisolone acetate

Methylprednisolone Sodium Succinate

• Hypersensitivity to the active ingredient or any of its excipients
• Systemic fungal infections
• Intrathecal or epidural route of administration
• Administration of live or live, attenuated vaccines is contraindicated in patients receiving immunosuppressive doses of corticosteroids
• Unless considered lifesaving methylprednisolone sodium succinate should not be given to patients with acute psychosis, peptic ulcer, or osteoporosis
• Traumatic brain injury

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Premature infants
• Parasitic infections
• Active tuberculosis
• Abrupt withdrawal
• Cushing's disease
• Hypothyroidism
• Diabetes mellitus
• Psychiatric disorders
• Epilepsy
• Myasthenia gravis
• Ocular herpes simplex
• Glaucoma
• Hypertension
• Dyslipidaemia
• Recent myocardial infarction
• Congestive cardiac failure
• Thromboembolic disorders
• Peptic ulceration
• Ulcerative colitis
• Diverticulitis
• Osteoporosis
• Pheochromocytoma

Forms avail. in SA and covered in this monograph: inj

Allergic reactions - severe, life-threatening

• IV (succinate): 30mg/kg, 4-6hrly as needed for 48hrs

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Doses up to 250mg IV should be given over a period of at least 5 minutes. Doses > 250mg IV should be given over at least 30 minutes

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In the case of severe conditions, initial doses should be given IV and then subsequent doses can be given IM or IV at intervals dictated by the patients response

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Specific doses based on individual indications

Other non-life threatening allergic and immune conditions

• IV/IM (succinate): 10-40mg, repeated at intervals determined by clinical response
• IM (acetate): 40-240mg, repeated at intervals determined by clinical response

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On average, the effect of 80mg acetate injection is expected to last approximately 2 weeks

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Status asthmaticus

• IV (succinate): 40mg, 12-24hrly until peak expiratory flow rate > 70% of predicted personal best

Acute asthma short-course steroid treatment

• IM (acetate): 240mg as a single dose

Flare of multiple sclerosis

• IV (succinate): 1g, dly for 3 days
• IM (acetate): Initial: 160mg, dly for 1 week; Maintenace: 64mg, alternate days for 1 month  

Flare of systemic lupus erythematosus

• IV (succinate): 1g, dly for 3 days

Graft rejection reactions

• IV (succinate): 500-1000mg, dly for 2-3 days

Rheumatoid arthritis
Osteoathritis

• Intra-articular (acetate): Large joint: 20-80mg; Medium joint: 10-40mg; Small joint: 4-10mg; repeat if needed at 1-5 week intervals

Subdeltoid bursitis
Prepatellar bursitis
Olecranon bursitis
Tenosynovitis
Epicondylitis

• Intrabursal, periarticular, into tendon sheath (acetate): 4-30mg, repeat as needed

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For tenosynovitis and epicondylitis, injections should be made into the affected tendon's sheath rather than the tendon itself

Due to the absence of tendon sheath, the Achilles tendon should not be injected

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Keloids
Localised lichen planus
Localized lichen simplex
Granuloma annulare
Alopecia areata
Discoid lupus erythematosus

• Intralesional (acetate): 20-60mg directly into lesion; Repeat up to 4 times at appropriate intervals

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Avoid injecting volumes that cause blanching as this may result in sloughing of the lesion

Paed. forms avail. in SA and covered in this monograph: inj

Allergic reactions - severe, life-threatening

• IV/IM (succinate): 30mg/kg/day, daily or alternate day dosing; Max: 1g/24hrs; Max duration: Total 3 doses

Specific doses based on individual indications

Other non-life threatening allergic and immune conditions

• IM (acetate): 4-80mg, repeated every 1-2 weeks

Status asthmaticus

Younger than 12 years

• IV (succinate): 1-2mg/kg/day, in 2 divided doses; Treatment duration: Until peak expiratory flow rate > 70% of expected; Max: 60mg/24hrs

Older than 12 years

• IV (succinate): 40-80mg, 12-24hrly; Treatment duration: Until peak expiratory flow rate > 70% of expected

Acute asthma short-course steroid treatment

Younger than 5 years

• IM (acetate): 7.5mg/kg, as a single dose; Max: 240mg

Older than 5 years

• See adult dosage

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Specialist recommendation: oral and IV routes preferred over IM admin. for this indication

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Graft rejection reactions

• IV (succinate): 10-20mg/kg, dly; Max: 1g/24hrs; Max duration: 3 days

Pregnancy

• Caution
• The ability of corticosteroids to cross the placenta varies between individual medicines, however, methylprednisolone does cross the placenta. One retrospective study found an increased incidence of low birth weights in infants born of mothers receiving corticosteroids. In humans, the risk of low birth weight appears to be dose-related and may be minimized by administering lower corticosteroid doses
• However, corticosteroids do not appear to cause congenital anomalies when given to pregnant women. Administration of corticosteroids to pregnant animals can cause abnormalities of foetal development including cleft palate, intra-uterine growth retardation and affects brain growth and development. There is no evidence that corticosteroids result in an increased incidence of congenital abnormalities, such as cleft palate in man, however, when administered for long periods or repeatedly during pregnancy, corticosteroids may increase the risk of intra-uterine growth retardation
• Hypoadrenalism may, in theory, occur in the neonate following prenatal exposure to corticosteroids but usually resolves spontaneously following birth and is rarely clinically important. Although neonatal adrenal insufficiency appears to be rare in infants who were exposed in utero to corticosteroids, those exposed to substantial doses of corticosteroids must be carefully observed and evaluated for signs of adrenal insufficiency. As with all medicines, corticosteroids should only be prescribed when the benefits to the mother and child outweigh the risks. When corticosteroids are essential, however, patients with normal pregnancies may be treated as though they were in the non-gravid state
• Since adequate human reproductive studies have not been done with methylprednisolone acetate, it should be used during pregnancy only after a careful assessment of the benefit-risk ratio to the mother and foetus. Cataracts have been observed in infants born to mothers treated with long-term corticosteroids during pregnancy

Breastfeeding

• Caution
• Corticosteroids are excreted in small amounts in breast milk, however, doses of up to 40 mg daily of methylprednisolone are unlikely to cause systemic effects in the infant. Infants of mothers taking higher doses than this may have a degree of adrenal suppression, but the benefits of breastfeeding are likely to outweigh any theoretical risk
• Corticosteroids distributed into breast milk may interfere with endogenous glucocorticoid production in nursing infants. Methylprednisolone should be used during breastfeeding only after a careful assessment of the benefit-risk ratio to the mother and infant

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Possibly porphyrinogenic (PSP)

Drugs in Sport

• Prohibited - In competition

Central Nervous System Disorders

• Affective disorders
• Psychotic disorders
• Personality change
• Mood swings
• Confusion
• Anxiety
• Insomnia
• Irritability
• Convulsions
• Raised intracranial pressure
• Amnesia
• Cognitive disorder
• Dizziness
• Headache
• Epidural lipomatosis

Cardiovascular Disorders

• Cardiac arrest
• Congestive cardiac failure
• Myocardial rupture post-myocardial infarction
• Hypertension
• Hypotension
• Thromboembolic events
• Cardiac arrhythmias

Respiratory Disorders

• Pulmonary embolism
• Hiccups
• Bronchospasm

Gastrointestinal Disorders

• Peptic ulcer
• Intestinal perforation
• Gastrointestinal haemorrhage
• Pancreatitis
• Ulcerative oesophagitis
• Abdominal distention
• Abdominal pain
• Diarrhoea
• Nausea

Hepatobiliary Disorders

• Increased hepatic enzymes
• Hepatitis

Endocrine and Metabolic Disorders

• Cushingoid
• Hypopituitarism
• Steroid withdrawal syndrome
• Sodium retention
• Fluid retention
• Hypokalaemic alkalosis
• Impaired glucose tolerance
• Hypokalaemia
• Menstrual irregularity
• Dyslipidaemia
• Increased appetite

Musculoskeletal Disorders

• Muscular weakness
• Myopathy
• Myalgia
• Growth retardation
• Pathological fracture
• Osteoporosis
• Osteonecrosis
• Neuropathic arthropathy
• Arthralgia
• Tendon rupture
• Spinal compression fracture

Skin and Subcutaneous Tissue Disorders

• Skin atrophy
• Acne
• Erythema
• Angioedema
• Pruritus
• Urticaria
• Ecchymosis
• Petechiae
• Rash
• Hirsutism
• Hyperhidrosis
• Skin striae
• Telangiectasia
• Impaired wound healing

Immune, Blood and Lymphatic System Disorders

• Anaphylactic reactions with or without circulatory collapse
• Susceptibility to infection
• Increased severity of infections
• Recurrence of dormant tuberculosis
• Opportunistic infections
• Kaposi's sarcoma
• Leukocytosis

Sensory Disorders

• Subcapsular cataract
• Glaucoma
• Exophthalmos
• Corneal thinning
• Scleral thinning
• Chorioretinopathy
• Vertigo
• Optic nerve damage

• CYP450 inhibitors
• CYP450 inducers
• Non-steroidal anti-inflammatory drugs
• Neuromuscular blockers
• Anticholinesterases
• Antidiabetic agents
• Anticoagulants
• Potassium-depleting agents
• Diuretics
• Aminoglutethimide
• Live/ live, attenuated vaccination
• Antihypertensives
• Sympathomimetics
• Antacids
• Cyclophosphamide 
• Tacrolimus

None routine. Specific cases may require

• Height (children)

Injection 40mg/ml, Injection 125mg/2ml, Injection 500mg/8ml, Injection 1000mg/16m - EML (Hospital)

Methylprednisolone is a synthetic glucocorticoid that is a methyl derivative of prednisolone. It acts by binding to intracellular glucocorticoid receptors that result in changes to gene expression. It also exerts effects independently of its ability to alter gene expression. The net effect is a diverse range of alterations to multiple physiological and organ systems primarily causing a decrease in inflammation and maintaining function under stress.

Injection (per ml) 40mg

• Depo-medrol (Pfizer) originator
• Mylan methylprednisolone (Xixia)
• Solu-medrol (Pfizer) originator

Injection (per 2ml) 40mg

• Mylan methylprednisolone (Xixia)

Injection (per 2ml) 125mg

• Solu-medrol (Pfizer) originator

Injection (per 8ml) 500mg

• AP methylpred (Pharmacare)
• Mylan methylprednisolone (Xixia)
• Solu-medrol (Pfizer) originator

Injection (per 16ml) 1000mg

• Mylan methylprednisolone (Xixia)
• Solu-medrol (Pfizer) originator

Also available in the following form: Tablet.

COMBINATION PREPARATIONS

Lidocaine/ Methylprednisolone 

Injection (per ml) 10mg/40mg

• Depo-medrol with lidocaine (Pfizer) originator (Discontinued: 20/12/2019)