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MethylPREDNISolone

Pronunciation

Pronunciation

(meth il pred NIS oh lone)

Index Terms

  • 6-α-Methylprednisolone
  • A-Methapred
  • Medrol Dose Pack
  • Methylprednisolone Acetate
  • Methylprednisolone Sodium Succinate
  • Solumedrol

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution Reconstituted, Injection, as sodium succinate [strength expressed as base]:

A-Methapred: 40 mg (1 ea); 125 mg (1 ea) [contains benzyl alcohol]

Solu-MEDROL: 500 mg (1 ea); 1000 mg (1 ea)

Solu-MEDROL: 2 g (1 ea) [contains benzyl alcohol]

Generic: 40 mg (1 ea); 125 mg (1 ea); 500 mg (1 ea [DSC]); 1000 mg (1 ea); 1 g (1 ea [DSC])

Solution Reconstituted, Injection, as sodium succinate [strength expressed as base, preservative free]:

Solu-MEDROL: 40 mg (1 ea); 125 mg (1 ea); 500 mg (1 ea); 1000 mg (1 ea)

Suspension, Injection, as acetate:

Depo-Medrol: 20 mg/mL (5 mL); 40 mg/mL (5 mL, 10 mL) [contains benzyl alcohol, polyethylene glycol, polysorbate 80]

Depo-Medrol: 40 mg/mL (1 mL) [contains polyethylene glycol]

Depo-Medrol: 80 mg/mL (1 mL)

Depo-Medrol: 80 mg/mL (5 mL) [contains benzyl alcohol, polyethylene glycol, polysorbate 80]

Depo-Medrol: 80 mg/mL (1 mL) [contains polyethylene glycol]

Generic: 40 mg/mL (1 mL, 5 mL, 10 mL); 80 mg/mL (1 mL, 5 mL)

Suspension, Injection, as acetate [preservative free]:

Generic: 80 mg/mL (1 mL [DSC])

Tablet, Oral:

Medrol: 2 mg, 4 mg, 8 mg, 16 mg, 32 mg [scored]

Medrol (Pak): 4 mg [scored]

Generic: 4 mg, 8 mg, 16 mg, 32 mg

Brand Names: U.S.

  • A-Methapred
  • Depo-Medrol
  • Medrol
  • Medrol (Pak)
  • Solu-MEDROL

Pharmacologic Category

  • Corticosteroid, Systemic

Pharmacology

In a tissue-specific manner, corticosteroids regulate gene expression subsequent to binding specific intracellular receptors and translocation into the nucleus. Corticosteroids exert a wide array of physiologic effects including modulation of carbohydrate, protein, and lipid metabolism and maintenance of fluid and electrolyte homeostasis. Moreover cardiovascular, immunologic, musculoskeletal, endocrine, and neurologic physiology are influenced by corticosteroids. Decreases inflammation by suppression of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability.

Distribution

Vd: 0.7 to 1.5 L/kg

Excretion

Clearance: Reduced in obese

Onset of Action

Peak effect (route dependent): Oral: 1 to 2 hours; IM: 4 to 8 days; Intra-articular: 1 week; methylprednisolone sodium succinate is highly soluble and has a rapid effect by IM and IV routes

Duration of Action

Route dependent: Oral: 30 to 36 hours; IM: 1 to 4 weeks; Intra-articular: 1 to 5 weeks; methylprednisolone acetate has a low solubility and has a sustained IM effect

Half-Life Elimination

3 to 3.5 hours; reduced in obese

Use: Labeled Indications

Primarily as an anti-inflammatory or immunosuppressant agent in the treatment of a variety of diseases including those of dermatologic, endocrine, GI, hematologic, allergic, inflammatory, neoplastic, neurologic, ophthalmic, renal, respiratory, and autoimmune origin. Prevention and treatment of graft-versus-host disease following allogeneic bone marrow transplantation.

Use: Unlabeled

Acute spinal cord injury; COPD exacerbation

Contraindications

Hypersensitivity to methylprednisolone or any component of the formulation; systemic fungal infection; administration of live virus vaccines; methylprednisolone formulations containing benzyl alcohol preservative are contraindicated in premature infants; IM administration in idiopathic thrombocytopenic purpura; intrathecal administration

Dosage

Dosing should be based on the lesser of ideal body weight or actual body weight

Children: Only sodium succinate may be given IV; methylprednisolone sodium succinate is highly soluble and has a rapid effect by IM and IV routes. Methylprednisolone acetate has a low solubility and has a sustained IM effect.

Acute spinal cord injury (off-label use): IV (sodium succinate): 30 mg/kg over 15 minutes, followed in 45 minutes by a continuous infusion of 5.4 mg/kg/hour for 23 hours. Note: Due to insufficient evidence of clinical efficacy (ie, preserving or improving spinal cord function), the routine use of methylprednisolone in the treatment of acute spinal cord injury is no longer recommended. If used in this setting, methylprednisolone should not be initiated >8 hours after the injury; not effective in penetrating trauma (eg, gunshot) (Consortium for Spinal Cord Medicine 2008).

Anti-inflammatory or immunosuppressive: Oral, IM, IV (sodium succinate): 0.5-1.7 mg/kg/day or 5-25 mg/m2/day in divided doses every 6-12 hours; “Pulse” therapy: 15-30 mg/kg/dose over ≥30 minutes given once daily for 3 days

Asthma exacerbations, including status asthmaticus (emergency medical care or hospital doses) (NAEPP 2007): Children ≤12 years: Oral, IV: 1-2 mg/kg/day in 2 divided doses (maximum: 60 mg/day) until peak expiratory flow is 70% of predicted or personal best

Lupus nephritis: IV (sodium succinate): 30 mg/kg over ≥30 minutes every other day for 6 doses

Adults: Only sodium succinate may be given IV; methylprednisolone sodium succinate is highly soluble and has a rapid effect by IM and IV routes. Methylprednisolone acetate has a low solubility and has a sustained IM effect.

Acute spinal cord injury (off-label use): IV (sodium succinate): 30 mg/kg over 15 minutes, followed in 45 minutes by a continuous infusion of 5.4 mg/kg/hour for 23 hours. Note: Due to insufficient evidence of clinical efficacy (ie, preserving or improving spinal cord function), the routine use of methylprednisolone in the treatment of acute spinal cord injury is no longer recommended. If used in this setting, methylprednisolone should not be initiated >8 hours after the injury; not effective in penetrating trauma (eg, gunshot) (Consortium for Spinal Cord Medicine 2008).

Allergic conditions: Oral: Tapered-dosage schedule (eg, dose-pack containing 21 x 4 mg tablets):

Day 1: 24 mg on day 1 administered as 8 mg (2 tablets) before breakfast, 4 mg (1 tablet) after lunch, 4 mg (1 tablet) after supper, and 8 mg (2 tablets) at bedtime OR 24 mg (6 tablets) as a single dose or divided into 2 or 3 doses upon initiation (regardless of time of day)

Day 2: 20 mg on day 2 administered as 4 mg (1 tablet) before breakfast, 4 mg (1 tablet) after lunch, 4 mg (1 tablet) after supper, and 8 mg (2 tablets) at bedtime

Day 3: 16 mg on day 3 administered as 4 mg (1 tablet) before breakfast, 4 mg (1 tablet) after lunch, 4 mg (1 tablet) after supper, and 4 mg (1 tablet) at bedtime

Day 4: 12 mg on day 4 administered as 4 mg (1 tablet) before breakfast, 4 mg (1 tablet) after lunch, and 4 mg (1 tablet) at bedtime

Day 5: 8 mg on day 5 administered as 4 mg (1 tablet) before breakfast and 4 mg (1 tablet) at bedtime

Day 6: 4 mg on day 6 administered as 4 mg (1 tablet) before breakfast

Anti-inflammatory or immunosuppressive:

Oral: 2-60 mg/day in 1-4 divided doses to start, followed by gradual reduction in dosage to the lowest possible level consistent with maintaining an adequate clinical response.

IM (sodium succinate): 10-80 mg/day once daily

IM (acetate): 10-80 mg every 1-2 weeks

IV (sodium succinate): 10-40 mg over a period of several minutes and repeated IV or IM at intervals depending on clinical response; when high dosages are needed, give 30 mg/kg over a period ≥30 minutes and may be repeated every 4-6 hours for 48 hours.

Arthritis: Intra-articular (acetate): Administer every 1-5 weeks.

Large joints (eg, knee, ankle): 20-80 mg

Medium joints (eg, elbow, wrist): 10-40 mg

Small joints: 4-10 mg

Asthma exacerbations, including status asthmaticus (emergency medical care or hospital doses): Oral, IV: 40-80 mg/day in 1-2 divided doses until peak expiratory flow is 70% of predicted or personal best (NAEPP 2007)

Asthma, severe persistent, long-term control: Oral: 7.5-60 mg/day (or on alternate days) (NAEPP 2007)

Bronchiolitis obliterans syndrome, prevention (off-label use): IV: 1,000 mg daily for 3 days. Note: Many centers use 10 to 15 mg/kg/day for smaller patients (Meyer 2014).

Cadaveric organ recovery (hormonal resuscitation) (off-label use): IV: 15 mg/kg or 2,000 mg bolus administered to the brain-dead donor who is hemodynamically unstable requiring significant vasopressor support; give concomitantly with vasopressin, levothyroxine or liothyronine (preferred), dextrose (if bolus dose insulin used), and regular insulin (bolus dose or continuous infusion). If continuous infusion insulin is employed, maintain blood glucose 120 to 180 mg/dL (Rosendale 2003a; Rosendale 2003b; Rosengard 2002; Salim 2007; Zaroff 2002).

COPD exacerbation (off-label use): Note: Dose, frequency, and duration of therapy not established. GOLD guidelines recommend the use of oral prednisone; however, methylprednisolone may be used as an alternative (GOLD [Decramer 2014]). No comparative studies exist to examine safety and efficacy between low-, medium-, or high-dose regimens. While several clinical trials have examined the use of methylprednisolone in this setting, these trials included low numbers of patients, employed vastly different regimens, and/or examined different clinical outcomes (Albert 1980; Alía 2011; Niewoehner 1999; Sayiner 2001; Shortall 2002; Vrondracek 2006; Willaert 2002). Current dosing strategies are empiric and have not been established by clinical trials. Based on expert opinion, commonly used regimens ranging from 60 to 125 mg IV administered 1 to 4 times daily followed by oral therapy (eg, prednisone 40 mg once daily) for a total of 5 to 14 days of therapy may be employed; the shorter duration (ie, 5 days) may be preferred (Leuppi 2013); however, comparative prospective data does not exist. IV administration with a higher dose (eg, ≥60 mg) may be preferred for those patients with impending or actual acute respiratory failure; outcome trials not available for this approach.

Dermatitis, acute severe: IM (acetate): 80 to 120 mg as a single dose

Dermatitis, chronic: IM (acetate): 40 to 120 mg every 5 to 10 days

Dermatologic conditions (eg, keloids, lichen planus): Intralesional (acetate): 20 to 60 mg

Dermatomyositis/polymyositis: IV (sodium succinate): 1 g/day for 3 to 5 days for severe muscle weakness, followed by conversion to oral prednisone (Drake 1996)

Gout, acute: IM, IV: Initial: 0.5 to 2 mg/kg; may be repeated as clinically indicated (ACR guidelines [Khanna 2012])

Lupus nephritis: High-dose “pulse” therapy: IV (sodium succinate): 0.5 to 1 g/day for 3 days (Ponticelli 2010)

Pneumocystis pneumonia in AIDS patients: IV: 30 mg twice daily for 5 days, then 30 mg once daily for 5 days, then 15 mg once daily for 11 days

Dosage adjustment in renal impairment: There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

Dosage adjustment in hepatic impairment: There are no dosage adjustments provided in the manufacturer’s labeling.

Reconstitution

Standard diluent (Solu-Medrol): 40 mg/50 mL D5W; 125 mg/50 mL D5W.

Minimum volume (Solu-Medrol): 50 mL D5W.

Administration

Administer with meals to decrease GI upset.

Parenteral: Methylprednisolone sodium succinate may be administered IM or IV; IV administration may be IVP over one to several minutes or IVPB or continuous IV infusion. Acetate salt should not be given IV. Avoid injection into the deltoid muscle due to a high incidence of subcutaneous atrophy. Avoid injection or leakage into the dermis; dermal and/or subdermal skin depression may occur at the site of injection.

IV: Succinate:

Low dose: ≤1.8 mg/kg or ≤125 mg/dose: IV push over 3 to 15 minutes

Moderate dose: ≥2 mg/kg or 250 mg/dose: IV over 15 to 30 minutes

High dose: 15 mg/kg or ≥500 mg/dose: IV over ≥30 minutes

Doses >15 mg/kg or ≥1 g: Administer over 1 hour

Do not administer high-dose IV push; hypotension, cardiac arrhythmia, and sudden death have been reported in patients given high-dose methylprednisolone IV push (>0.5 g over <10 minutes); intermittent infusion over 15 to 60 minutes; maximum concentration: IV push 125 mg/mL

IM: Avoid injection into the deltoid muscle due to a high incidence of subcutaneous atrophy. Avoid injection or leakage into the dermis; dermal and/or subdermal skin depression may occur at the site of injection. Do not inject into areas that have evidence of acute local infection.

Dietary Considerations

Take with meals to decrease GI upset; need diet rich in pyridoxine, vitamin C, vitamin D, folate, calcium, phosphorus, and protein.

Compatibility

Stable in D51/2NS, D5NS, LR, NS.

Y-site administration: Incompatible with allopurinol, amsacrine, caspofungin, ciprofloxacin, docetaxel, etoposide phosphate, fenoldopam, filgrastim, gemcitabine, ondansetron, paclitaxel, palonosetron, propofol, sargramostim, tigecycline, vinorelbine.

Storage

Methylprednisolone acetate; tablets: Store at 20°C to 25°C (68°F to 77°F).

Methylprednisolone sodium succinate: Store intact vials at controlled room temperature of 20°C to 25°C (68°F to 77°F). Protect from light. Reconstituted solutions of methylprednisolone sodium succinate should be stored at room temperature of 20°C to 25°C (68°F to 77°F) and used within 48 hours. Stability of parenteral admixture at room temperature (25°C) and at refrigeration temperature (4°C) is 48 hours.

Drug Interactions

Acetylcholinesterase Inhibitors: Corticosteroids (Systemic) may enhance the adverse/toxic effect of Acetylcholinesterase Inhibitors. Increased muscular weakness may occur. Monitor therapy

Aldesleukin: Corticosteroids may diminish the antineoplastic effect of Aldesleukin. Avoid combination

Amodiaquine: CYP2C8 Inhibitors may increase the serum concentration of Amodiaquine. Avoid combination

Amphotericin B: Corticosteroids (Systemic) may enhance the hypokalemic effect of Amphotericin B. Monitor therapy

Androgens: Corticosteroids (Systemic) may enhance the fluid-retaining effect of Androgens. Monitor therapy

Antacids: May decrease the bioavailability of Corticosteroids (Oral). Management: Consider separating doses by 2 or more hours. Budesonide enteric coated tablets could dissolve prematurely if given with drugs that lower gastric acid, with unknown impact on budesonide therapeutic effects. Consider therapy modification

Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy

Aprepitant: May increase the serum concentration of Corticosteroids (Systemic). Management: No dose adjustment is needed for single 40 mg aprepitant doses. For other regimens, reduce oral dexamethasone or methylprednisolone doses by 50%, and IV methylprednisolone doses by 25%. Antiemetic regimens containing dexamethasone reflect this adjustment. Consider therapy modification

BCG (Intravesical): Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

Bile Acid Sequestrants: May decrease the absorption of Corticosteroids (Oral). Monitor therapy

Calcitriol (Systemic): Corticosteroids (Systemic) may diminish the therapeutic effect of Calcitriol (Systemic). Monitor therapy

Coccidioides immitis Skin Test: Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test. Monitor therapy

Corticorelin: Corticosteroids may diminish the therapeutic effect of Corticorelin. Specifically, the plasma ACTH response to corticorelin may be blunted by recent or current corticosteroid therapy. Monitor therapy

CycloSPORINE (Systemic): May increase the serum concentration of MethylPREDNISolone. MethylPREDNISolone may increase the serum concentration of CycloSPORINE (Systemic). MethylPREDNISolone may decrease the serum concentration of CycloSPORINE (Systemic). Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of MethylPREDNISolone. Management: Consider methylprednisolone dose increases in patients receiving strong CYP3A4 inducers and monitor closely for reduced steroid efficacy. Consider therapy modification

CYP3A4 Inhibitors (Strong): May increase the serum concentration of MethylPREDNISolone. Management: Consider methylprednisolone dose reduction in patients receiving strong CYP3A4 inhibitors and monitor for increased steroid related adverse effects. Consider therapy modification

Deferasirox: Corticosteroids (Systemic) may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Monitor therapy

Deferasirox: Corticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Monitor therapy

Denosumab: May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. Monitor therapy

Echinacea: May diminish the therapeutic effect of Immunosuppressants. Consider therapy modification

Estrogen Derivatives: May increase the serum concentration of Corticosteroids (Systemic). Monitor therapy

Fingolimod: Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections). Consider therapy modification

Fosaprepitant: May increase the serum concentration of Corticosteroids (Systemic). The active metabolite aprepitant is likely responsible for this effect. Consider therapy modification

Hyaluronidase: Corticosteroids may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving corticosteroids (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Consider therapy modification

Indacaterol: May enhance the hypokalemic effect of Corticosteroids (Systemic). Monitor therapy

Indium 111 Capromab Pendetide: Corticosteroids (Systemic) may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Avoid combination

Isoniazid: Corticosteroids (Systemic) may decrease the serum concentration of Isoniazid. Monitor therapy

Leflunomide: Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. Consider therapy modification

Loop Diuretics: Corticosteroids (Systemic) may enhance the hypokalemic effect of Loop Diuretics. Monitor therapy

Mifepristone: May diminish the therapeutic effect of Corticosteroids (Systemic). Mifepristone may increase the serum concentration of Corticosteroids (Systemic). Management: Avoid mifepristone in patients who require long-term corticosteroid treatment of serious illnesses or conditions (e.g., for immunosuppression following transplantation). Corticosteroid effects may be reduced by mifepristone treatment. Avoid combination

Mitotane: May decrease the serum concentration of Corticosteroids (Systemic). Consider therapy modification

Natalizumab: Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Avoid combination

Neuromuscular-Blocking Agents (Nondepolarizing): May enhance the adverse neuromuscular effect of Corticosteroids (Systemic). Increased muscle weakness, possibly progressing to polyneuropathies and myopathies, may occur. Consider therapy modification

Nicorandil: Corticosteroids (Systemic) may enhance the adverse/toxic effect of Nicorandil. Gastrointestinal perforation has been reported in association with this combination. Monitor therapy

NSAID (COX-2 Inhibitor): Corticosteroids (Systemic) may enhance the adverse/toxic effect of NSAID (COX-2 Inhibitor). Monitor therapy

NSAID (Nonselective): Corticosteroids (Systemic) may enhance the adverse/toxic effect of NSAID (Nonselective). Monitor therapy

Pimecrolimus: May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Quinolone Antibiotics: Corticosteroids (Systemic) may enhance the adverse/toxic effect of Quinolone Antibiotics. Specifically, the risk of tendonitis and tendon rupture may be increased. Monitor therapy

Roflumilast: May enhance the immunosuppressive effect of Immunosuppressants. Consider therapy modification

Salicylates: May enhance the adverse/toxic effect of Corticosteroids (Systemic). These specifically include gastrointestinal ulceration and bleeding. Corticosteroids (Systemic) may decrease the serum concentration of Salicylates. Withdrawal of corticosteroids may result in salicylate toxicity. Monitor therapy

Sipuleucel-T: Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Monitor therapy

Tacrolimus (Topical): May enhance the adverse/toxic effect of Immunosuppressants. Avoid combination

Telaprevir: Corticosteroids (Systemic) may decrease the serum concentration of Telaprevir. Telaprevir may increase the serum concentration of Corticosteroids (Systemic). Management: Concurrent use of telaprevir and systemic corticosteroids is not recommended. When possible, consider alternatives. If used together, employ extra caution and monitor closely for excessive corticosteroid effects and diminished telaprevir effects. Consider therapy modification

Thiazide Diuretics: Corticosteroids (Systemic) may enhance the hypokalemic effect of Thiazide Diuretics. Monitor therapy

Tofacitinib: Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants. Avoid combination

Trastuzumab: May enhance the neutropenic effect of Immunosuppressants. Monitor therapy

Urea Cycle Disorder Agents: Corticosteroids (Systemic) may diminish the therapeutic effect of Urea Cycle Disorder Agents. More specifically, Corticosteroids (Systemic) may increase protein catabolism and plasma ammonia concentrations, thereby increasing the doses of Urea Cycle Disorder Agents needed to maintain these concentrations in the target range. Monitor therapy

Vaccines (Inactivated): Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation. Consider therapy modification

Vaccines (Live): Corticosteroids (Systemic) may enhance the adverse/toxic effect of Vaccines (Live). Corticosteroids (Systemic) may diminish the therapeutic effect of Vaccines (Live). Management: Doses equivalent to less than 2 mg/kg or 20 mg per day of prednisone administered for less than 2 weeks are not considered sufficiently immunosuppressive to create vaccine safety concerns. Higher doses and longer durations should be avoided. Consider therapy modification

Warfarin: Corticosteroids (Systemic) may enhance the anticoagulant effect of Warfarin. Monitor therapy

Test Interactions

Interferes with skin tests

Adverse Reactions

Frequency not defined.

Cardiovascular: Arrhythmias, bradycardia, cardiac arrest, cardiomegaly, circulatory collapse, congestive heart failure, edema, fat embolism, hypertension, hypertrophic cardiomyopathy in premature infants, myocardial rupture (post MI), syncope, tachycardia, thromboembolism, vasculitis

Central nervous system: Delirium, depression, emotional instability, euphoria, hallucinations, headache, intracranial pressure increased, insomnia, malaise, mood swings, nervousness, neuritis, personality changes, psychic disorders, pseudotumor cerebri (usually following discontinuation), seizure, vertigo

Dermatologic: Acne, allergic dermatitis, alopecia, dry scaly skin, ecchymoses, edema, erythema, hirsutism, hyper-/hypopigmentation, hypertrichosis, impaired wound healing, petechiae, rash, skin atrophy, sterile abscess, skin test reaction impaired, striae, urticaria

Endocrine & metabolic: Adrenal suppression, amenorrhea, carbohydrate intolerance increased, Cushing's syndrome, diabetes mellitus, fluid retention, glucose intolerance, growth suppression (children), hyperglycemia, hyperlipidemia, hypokalemia, hypokalemic alkalosis, menstrual irregularities, negative nitrogen balance, pituitary-adrenal axis suppression, protein catabolism, sodium and water retention

Gastrointestinal: Abdominal distention, appetite increased, bowel/bladder dysfunction (after intrathecal administration), gastrointestinal hemorrhage, gastrointestinal perforation, nausea, pancreatitis, peptic ulcer, perforation of the small and large intestine, ulcerative esophagitis, vomiting, weight gain

Hematologic: Leukocytosis (transient)

Hepatic: Hepatomegaly, transaminases increased

Local: Postinjection flare (intra-articular use), thrombophlebitis

Neuromuscular & skeletal: Arthralgia, arthropathy, aseptic necrosis (femoral and humoral heads), fractures, muscle mass loss, muscle weakness, myopathy (particularly in conjunction with neuromuscular disease or neuromuscular-blocking agents), neuropathy, osteoporosis, parasthesia, tendon rupture, vertebral compression fractures, weakness

Ocular: Cataracts, exophthalmoses, glaucoma, intraocular pressure increased

Renal: Glycosuria

Respiratory: Pulmonary edema

Miscellaneous: Abnormal fat disposition, anaphylactoid reaction, anaphylaxis, angioedema, avascular necrosis, diaphoresis, hiccups, hypersensitivity reactions, infections, secondary malignancy

<1% (Limited to important or life-threatening): Venous thrombosis (Johannesdottir, 2013)

Warnings/Precautions

Concerns related to adverse effects:

• Adrenal suppression: May cause hypercorticism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in younger children or in patients receiving high doses for prolonged periods. HPA axis suppression may lead to adrenal crisis. Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully. Particular care is required when patients are transferred from systemic corticosteroids to inhaled products due to possible adrenal insufficiency or withdrawal from steroids, including an increase in allergic symptoms. Adult patients receiving >20 mg per day of prednisone (or equivalent) may be most susceptible. Fatalities have occurred due to adrenal insufficiency in asthmatic patients during and after transfer from systemic corticosteroids to aerosol steroids; aerosol steroids do not provide the systemic steroid needed to treat patients having trauma, surgery, or infections.

• Anaphylactoid reactions: Rare cases of anaphylactoid reactions have been observed in patients receiving corticosteroids.

• Dermal changes: Avoid injection or leakage into the dermis; dermal and/or subdermal skin depression may occur at the site of injection. Avoid deltoid muscle injection; subcutaneous atrophy may occur

• Immunosuppression: Prolonged use of corticosteroids may increase the incidence of secondary infection, cause activation of latent infections, mask acute infection (including fungal infections), prolong or exacerbate viral or parasitic infections, or limit response to vaccines. Exposure to chickenpox or measles should be avoided; corticosteroids should not be used to treat ocular herpes simplex. Corticosteroids should not be used for cerebral malaria, fungal infections, or viral hepatitis. Close observation is required in patients with latent tuberculosis and/or TB reactivity; restrict use in active TB (only fulminating or disseminated TB in conjunction with antituberculosis treatment). Amebiasis should be ruled out in any patient with recent travel to tropic climates or unexplained diarrhea prior to initiation of corticosteroids. Use with extreme caution in patients with Strongyloides infections; hyperinfection, dissemination and fatalities have occurred.

• Myopathy: Acute myopathy has been reported with high dose corticosteroids, usually in patients with neuromuscular transmission disorders; may involve ocular and/or respiratory muscles; monitor creatine kinase; recovery may be delayed.

• Kaposi's sarcoma: Prolonged treatment with corticosteroids has been associated with the development of Kaposi's sarcoma (case reports); discontinuation may result in clinical improvement.

• Psychiatric disturbances: Corticosteroid use may cause psychiatric disturbances, including depression, euphoria, insomnia, mood swings, and personality changes. Pre-existing psychiatric conditions may be exacerbated by corticosteroid use.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with HF and/or hypertension; use has been associated with fluid retention, electrolyte disturbances, and hypertension. Cardiomegaly and congestive heart failure have been reported following concurrent use of amphotericin B and hydrocortisone for the management of fungal infections.

• Diabetes: Use with caution in patients with diabetes mellitus; may alter glucose production/regulation leading to hyperglycemia.

• Gastrointestinal disease: Use with caution in patients with GI diseases (diverticulitis, intestinal anastomoses, peptic ulcer, ulcerative colitis) due to perforation risk. Avoid ethanol may enhance gastric mucosal irritation.

• Head injury: Increased mortality was observed in patients receiving high-dose IV methylprednisolone; high-dose corticosteroids should not be used for the management of head injury.

• Hepatic impairment: Use with caution in patients with hepatic impairment, including cirrhosis; long-term use has been associated with fluid retention.

• Multiple sclerosis: Use with caution; studies have not shown that corticosteroids ultimately impact the natural history or outcome of disease; relatively high doses are usually necessary to have a significant effect.

• Myasthenia gravis: Use with caution in patients with myasthenia gravis; exacerbation of symptoms has occurred especially during initial treatment with corticosteroids.

• Myocardial infarction (MI): Use with caution following acute MI; corticosteroids have been associated with myocardial rupture.

• Ocular disease: Use with caution in patients with cataracts and/or glaucoma; increased intraocular pressure, open-angle glaucoma, and cataracts have occurred with prolonged use. Not recommended for the treatment of optic neuritis; may increase frequency of new episodes. Use with caution in patients with a history of ocular herpes simplex; corneal perforation has occurred; do not use in active ocular herpes simplex. Consider routine eye exams in chronic users.

• Osteoporosis: Use with caution in patients with osteoporosis; high doses and/or long-term use of corticosteroids have been associated with increased bone loss and osteoporotic fractures.

• Renal impairment: Use with caution in patients with renal impairment; fluid retention may occur.

• Seizure disorders: Use with caution in patients with a history of seizure disorder; seizures have been reported with adrenal crisis.

• Septic shock or sepsis syndrome: A study has failed to demonstrate efficacy in septic shock or sepsis syndrome treatment; use may increase mortality in some populations (eg, patients with elevated serum creatinine, patients who develop secondary infections after use).

• Thyroid disease: Changes in thyroid status may necessitate dosage adjustments; metabolic clearance of corticosteroids increases in hyperthyroid patients and decreases in hypothyroid ones.

Concurrent drug therapy issues

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Elderly: Because of the risk of adverse effects, systemic corticosteroids should be used cautiously in the elderly in the smallest possible effective dose for the shortest duration.

• Pediatric: May affect growth velocity; growth should be routinely monitored in pediatric patients.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Methylprednisolone acetate I.M. injection (multiple-dose vial) and the diluent for methylprednisolone sodium succinate injection may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer’s labeling.

Other warnings/precautions:

• Discontinuation of therapy: Withdraw therapy with gradual tapering of dose.

• Epidural injection: Corticosteroids are not approved for epidural injection. Serious neurologic events (eg, spinal cord infarction, paraplegia, quadriplegia, cortical blindness, stroke), some resulting in death, have been reported with epidural injection of corticosteroids, with and without use of fluoroscopy.

• Stress: Patients may require higher doses when subject to stress (ie, trauma, surgery, severe infection).

Monitoring Parameters

Blood pressure, blood glucose, electrolytes, growth in children

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been observed with corticosteroids in animal reproduction studies. Methylprednisolone crosses the placenta (Anderson 1981). Some studies have shown an association between first trimester systemic corticosteroid use and oral clefts (Park-Wyllie 2000; Pradat 2003). Systemic corticosteroids may also influence fetal growth (decreased birth weight); however, information is conflicting (Lunghi 2010). Hypoadrenalism may occur in newborns following maternal use of corticosteroids in pregnancy; monitor.

When systemic corticosteroids are needed in pregnancy, it is generally recommended to use the lowest effective dose for the shortest duration of time, avoiding high doses during the first trimester (Leachman 2006; Lunghi 2010; Makol 2011; Østensen 2009). Inhaled corticosteroids are preferred for the treatment of asthma during pregnancy. Systemic corticosteroids such as methylprednisolone may be used for the treatment of severe persistent asthma if needed; the lowest dose administered on alternate days (if possible) should be used (NAEPP 2005).

Pregnant women exposed to methylprednisolone for antirejection therapy following a transplant may contact the National Transplantation Pregnancy Registry (NTPR) at 215-955-4820. Women exposed to methylprednisolone during pregnancy for the treatment of an autoimmune disease may contact the OTIS Autoimmune Diseases Study at 877-311-8972.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea, insomnia, akathisia, or hyperhidrosis. Have patient report immediately to prescriber signs of infection, signs of hyperglycemia, signs of hypokalemia, signs of pancreatitis, severe asthenia, irritability, tremors, tachycardia, confusion, dizziness, dyspnea, excessive weight gain or loss, edema of extremities, skin changes, moon face, buffalo hump, significant headache, angina, menstrual irregularities, osteodynia, arthralgia, vision changes, mood changes, behavioral changes, depression, paresthesia, ecchymosis, hemorrhaging, intolerable dyspepsia, melena, hematemesis, injection site irritation, or blindness (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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