Formulary
Methylprednisolone: Indications, Dosing, Side Effects and Interactions
Methylprednisolone exerts predominantly glucocorticoid effects with minimal mineralcorticoid effects.
MedNext Academy | 8 min read
Methylprednisolone: Indications, Dosing, Side Effects and Interactions
Methylprednisolone exerts predominantly glucocorticoid effects with minimal mineralcorticoid effects.
Drug action
Methylprednisolone exerts predominantly glucocorticoid effects with minimal mineralcorticoid effects.
Indications and dose
**Suppression of inflammatory and allergic disorders,Cerebral oedema associated with malignancy**
- **Adult** (By Mouth): Initially 2-40 mg daily.
- **Adult** (By Intramuscular Injection, Or By Slow Intravenous Injection, Or By Intravenous Infusion): Initially 10-500 mg.
**Treatment of graft rejection reactions**
- **Adult** (By Intravenous Infusion): Up to 1 g daily for up to 3 days.
**Treatment of relapse in multiple sclerosis**
- **Adult** (By Mouth): 500 mg once daily for 5 days.
**Treatment of relapse in multiple sclerosis (when oral steroids have failed or have not been tolerated, or in those who require hospital admission)**
- **Adult** (By Intravenous Infusion): 1 g once daily for 3-5 days.
**Suppression of inflammatory and allergic disorders**
- **Adult** (By Deep Intramuscular Injection): 40-120 mg, then 40-120 mg after 2-3 weeks if required, to be injected into the gluteal muscle.
**Inflammatory and allergic disorders for methylprednisolone**
- **Child** (By mouth, or by slow intravenous injection, or by intravenous infusion): 0.5-1.7 mg/kg daily in 2-4 divided doses, divide doses depending on condition and response.
**Treatment of graft rejection reactions for methylprednisolone**
- **Child** (By intravenous injection): 10-20 mg/kg once daily for 3 days, alternatively 400-600 mg/m2 once daily (max. per dose 1 g) for 3 days.
**Severe erythema multiforme, Lupus nephritis, Systemic onset juvenile idiopathic arthritis for methylprednisolone**
- **Child** (By intravenous injection): 10-30 mg/kg once daily or on alternate days (max. per dose 1 g) for up to 3 doses.
**Local inflammation of joints and soft tissues for Depo-Medrone**
- **Child** (By intra-articular injection): (consult product literature).
**Suppression of inflammatory and allergic disorders for Depo-Medrone**
- **Child** (By deep intramuscular injection): Seek specialist advice, to be injected into the gluteal muscle.
Cautions
For all corticosteroids (systemic) Congestive heart failure; diabetes mellitus (including a family history of); diverticular disease (increased risk of diverticular perforation); diverticulitis; epilepsy; glaucoma (including a family history of or susceptibility to); history of steroid myopathy; history of tuberculosis or X-ray changes (frequent monitoring required); hypertension; hypothyroidism; infection (particularly untreated); long-term use; myasthenia gravis; ocular herpes simplex (risk of corneal perforation); osteoporosis (postmenopausal women and the elderly at risk); peptic ulcer; psychiatric reactions; recent intestinal anastomoses; recent myocardial infarction (rupture reported); severe affective disorders (particularly if history of steroid-induced psychosis); thromboembolic disorders; ulcerative colitis Cautions, further information With intra-articular use or intradermal use or intralesional use: For further information on cautions associated with intra-articular, intradermal, and intralesional preparations, consult product literature. Elderly Screening Tool of Older Persons' potentially inappropriate Prescriptions (STOPP) criteria to aid medication reviews (see Prescribing in the elderly for information). Potentially inappropriate: if used instead of inhaled corticosteroids for maintenance therapy in moderate to severe COPD (unnecessary exposure to long-term side-effects) as long-term (longer than 3 months) monotherapy for rheumatoid arthritis (risk of side-effects) for treatment of osteoarthritis other than for periodic intra-articular injections for monoarticular pain (risk of side-effects) with concurrent NSAIDs without proton pump inhibitor prophylaxis (increased risk of peptic ulcer disease) Cautions For methylprednisolone With intravenous use Rapid intravenous administration of large doses associated with cardiovascular collapse With systemic use Systemic sclerosis (increased incidence of scleroderma renal crisis)
Contraindications
For all corticosteroids (systemic) Avoid live virus vaccines in those receiving immunosuppressive doses (serum antibody response diminished); systemic infection (unless specific therapy given) Contra-indications, further information With intra-articular use or intradermal use or intralesional use: For further information on contra-indications associated with intra-articular, intradermal and intralesional preparations, consult product literature.
Side effects
For all corticosteroids (systemic) Common or very common Anxiety; appetite increased; behaviour abnormal; cataract subcapsular; cognitive impairment; Cushing's syndrome; electrolyte imbalance; fluid retention; gastrointestinal discomfort; headache; healing impaired; hirsutism; hypertension; increased risk of infection; menstrual cycle irregularities; mood altered; nausea; osteoporosis; peptic ulcer; psychotic disorder; skin reactions; sleep disorder; vision blurred; weight increased Uncommon Adrenal suppression; alkalosis hypokalaemic; bone fractures; diabetic control impaired; glaucoma; haemorrhage; heart failure; hyperhidrosis; leucocytosis; myopathy; osteonecrosis; pancreatitis; papilloedema; seizure; thromboembolism; tuberculosis reactivation; vertigo Rare or very rare Tendon rupture Frequency not known Chorioretinopathy; eye disorders; growth retardation; intracranial pressure increased with papilloedema (usually after withdrawal) Side-effects, further information Adrenal suppression During prolonged therapy with corticosteroids, particularly with systemic use, adrenal atrophy develops and can persist for years after stopping. Abrupt withdrawal after a prolonged period can lead to acute adrenal insufficiency, hypotension, or death. To compensate for a diminished adrenocortical response caused by prolonged corticosteroid treatment, any significant intercurrent illness, trauma, or surgical procedure requires a temporary increase in corticosteroid dose, or if already stopped, a temporary reintroduction of corticosteroid treatment. For vamorolone, there is no evidence on the effects of increasing the dose, and temporary supplementation with hydrocortisone is advised. Infections Prolonged courses of corticosteroids increase susceptibility to infections and severity of infections; clinical presentation of infections may also be atypical. Serious infections e.g. septicaemia and tuberculosis may reach an advanced stage before being recognised, and amoebiasis or strongyloidiasis may be activated or exacerbated (exclude before initiating a corticosteroid in those at risk or with suggestive symptoms). Fungal or viral ocular infections may also be exacerbated. Chickenpox Unless they have had chickenpox, patients receiving oral or parenteral corticosteroids for purposes other than replacement should be regarded as being at risk of severe chickenpox. Manifestations of fulminant illness include pneumonia, hepatitis and disseminated intravascular coagulation; rash is not necessarily a prominent feature. Passive immunisation with varicella-zoster immunoglobulin is needed for exposed non-immune patients receiving systemic corticosteroids or for those who have used them within the previous 3 months. Confirmed chickenpox warrants specialist care and urgent treatment. Corticosteroids should not be stopped and dosage may need to be increased. Measles Patients taking corticosteroids should be advised to take particular care to avoid exposure to measles and to seek immediate medical advice if exposure occurs. Prophylaxis with intramuscular normal immunoglobulin may be needed. Psychiatric reactions Systemic corticosteroids, particularly in high doses, are linked to psychiatric reactions including euphoria, insomnia, irritability, mood lability, suicidal thoughts, psychotic reactions, and behavioural disturbances. These reactions frequently subside on reducing the dose or discontinuing the corticosteroid but they may also require specific management. Patients should be advised to seek medical advice if psychiatric symptoms (especially depression and suicidal thoughts) occur and they should also be alert to the rare possibility of such reactions during withdrawal of corticosteroid treatment. Systemic corticosteroids should be prescribed with care in those predisposed to psychiatric reactions, including those who have previously suffered corticosteroid-induced psychosis, or who have a personal or family history of psychiatric disorders. When used by eye (topical) Vision disorders can occur with use of topical (eye) corticosteroids. Consider seeking specialist advice to evaluate cause if vision blurred or other vision disorder occurs. Side-effects For methylprednisolone Common or very common With oral use Depressed mood Frequency not known With intra-articular use Angioedema; cataract; confusion; delusions; depressed mood; diarrhoea; dizziness; drug dependence; dyslipidaemia; embolism and thrombosis; epidural lipomatosis; fatigue; gastrointestinal disorders; glucose tolerance impaired; hallucination; hepatitis; hiccups; hypopituitarism; hypotension; increased insulin requirement; insomnia; intracranial pressure increased; malaise; memory loss; metabolic acidosis; muscle weakness; myalgia; neuropathic arthropathy; peripheral oedema; psychiatric disorder; schizophrenia exacerbated; sterile abscess; suicidal ideation; vision loss; withdrawal syndrome With oral use Confusion; delusions; diarrhoea; dizziness; dyslipidaemia; fatigue; hallucination; hiccups; hypotension; insomnia; Kaposi's sarcoma; lipomatosis; malaise; myocardial rupture (following recent myocardial infarction); oedema; schizophrenia; suicidal ideation; telangiectasia; withdrawal syndrome With parenteral use Confusion; delusions; depressed mood; diarrhoea; dizziness; dyslipidaemia; fatigue; hallucination; hiccups; hypotension; Kaposi's sarcoma; lipomatosis; malaise; oedema; schizophrenia; suicidal thoughts; telangiectasia; vomiting; withdrawal syndrome
Interactions
**Other interactions (31):**
- Methylprednisolone Methylprednisolone is a cytochrome P450 enzyme (CYP) substrate and is mainly metabolized by the CYP3A enzyme.
- It catalyzes 6-hydroxylation of steroids, the essential Phase I metabolic step for both endogenous and synthetic corticosteroids.
- CYP3A4 INHIBITORS - Drugs that inhibit CYP3A4 activity generally decrease hepatic clearance and increase the plasma concentration of CYP3A4 substrate medications, such as methylprednisolone.
- In the presence of a CYP3A4 inhibitor, the dose of methylprednisolone may need to be titrated to avoid steroid toxicity.
- Co-administration may require an increase in methylprednisolone dosage to achieve the desired result.
- CYP3A4 SUBSTRATES - In the presence of another CYP3A4 substrate, the hepatic clearance of methylprednisolone may be affected, with corresponding dosage adjustments required.
Pregnancy
For all corticosteroids (systemic) The benefit of treatment with corticosteroids during pregnancy outweighs the risk. Corticosteroid cover is required during labour. Following a review of the data on the safety of systemic corticosteroids used in pregnancy and breast-feeding the CSM (May 1998) concluded that corticosteroids vary in their ability to cross the placenta but there is no convincing evidence that systemic corticosteroids increase the incidence of congenital abnormalities such as cleft palate or lip. When administration is prolonged or repeated during pregnancy, systemic corticosteroids increase the risk of intra-uterine growth restriction; there is no evidence of intra-uterine growth restriction following short-term treatment (e.g. prophylactic treatment for neonatal respiratory distress syndrome). Any adrenal suppression in the neonate following prenatal exposure usually resolves spontaneously after birth and is rarely clinically important. Monitoring in pregnancy Pregnant women with pre-eclampsia or fluid retention should be monitored closely when given systemic corticosteroids.
Breast feeding
For all corticosteroids (systemic) The benefit of treatment with corticosteroids during breast-feeding outweighs the risk.
Hepatic impairment
For all corticosteroids (systemic) In general, manufacturers advise caution (risk of increased exposure).
Renal impairment
For all corticosteroids (systemic) In general, manufacturers advise caution.
Medicinal forms
Suspension,Tablet,Solution,Injection
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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