methylprednisolone

Absorption: Well absorbed after oral administration. Succinate salt is rapidly absorbed after IM administration. Acetate salt is slowly but completely absorbed after IM administration. Absorption from local sites (intra-articular, intralesional) is slow but complete. IV administration results in complete bioavailability.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Metabolized mostly by the liver. Primarily excreted in urine as metabolites.

Half-Life: Oral: 2.5 hr; IV: 15 min.

Time/Action Profile ⬆ ⬇

(anti-inflammatory activity)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1–2 hr	1.25–1.5 days
IM (acetate)	6–48 hr	4–8 days	1–4 wk
IM, IV (succinate)	rapid	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Active untreated infections (may be used in patients being treated for tuberculous meningitis);
Epidural use (may result in serious neurological injury or death);
Known alcohol, bisulfite, cow's milk, or tartrazine hypersensitivity or intolerance (some products contain these and should be avoided in susceptible patients);
Lactation: Lactation.

Use Cautiously in:

Chronic treatment (will lead to adrenal suppression; use lowest possible dose for shortest period of time);
Stress (surgery, infections—supplemental doses may be needed);
Potential infections may mask signs (fever, inflammation);
Systemic sclerosis (↑ risk of scleroderma renal crisis);
Tumors that have a high proliferative rate, high tumor burden, and high sensitivity to cytotoxic agents (↑ risk of tumor lysis syndrome);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Chronic use will result in growth; use lowest possible dose for shortest period of time;
Pedi: Neonates (avoid use of benzyl alcohol containing injectable preparations; use preservative-free formulations).

Adv. Reactions/Side Effects ⬆ ⬇

Adverse reactions/side effects are much more common with high-dose/long-term therapy

CV: hypertension, edema, THROMBOEMBOLISM

Derm: ↓wound healing, acne, ecchymoses, fragility, hirsutism, petechiae

EENT: ↑intraocular pressure, cataracts

Endo: adrenal suppression, hyperglycemia

F and E: hypokalemia, hypokalemic alkalosis

GI: anorexia, nausea, PEPTIC ULCERATION, vomiting

Hemat: leukocytosis, thrombophlebitis

Metab: weight gain, weight loss

MS: muscle wasting, osteoporosis, avascular necrosis of joints, muscle pain

Neuro: depression, euphoria, ↑intracranial pressure (children only), headache, personality changes, psychoses, restlessness

Misc: cushingoid appearance (moon face, buffalo hump), INFECTION, KAPOSI'S SARCOMA, tumor lysis syndrome

Interactions ⬆ ⬇

Drug-drug:

Additive hypokalemia with thiazide and loop diuretics, amphotericin B, or piperacillin/tazobactam.
Hypokalemia may ↑ the risk of digoxin toxicity.
May ↑ requirement for insulins or oral hypoglycemic agents.
Phenytoin,phenobarbital, and rifampin stimulate metabolism; may ↓ levels and effectiveness.
Oral contraceptives may ↑ levels and risk of toxicity.
↑risk of adverse GI effects with NSAIDs (including aspirin).
At chronic doses that suppress adrenal function, may ↓ the antibody response to and ↑ the risk of adverse reactions from live-virus vaccines.
May ↑ levels and risk of toxicity of cyclosporine and tacrolimus.
May ↑ risk of tendon rupture from fluoroquinolones.

Route/Dosage ⬆ ⬇

PO (Adults ): Multiple sclerosis: 160 mg/day for 7 days; then 64 mg every other day for 1 mo. Other uses: 2–60 mg/day as a single dose or in 2–4 divided doses. Asthma exacerbations: 120–180 mg/day in divided doses 3–4 times/day for 48 hr; then 60–80 mg/day divided twice daily.
PO (Children ): Anti-inflammatory/Immunosuppressive: 0.5–1.7 mg/kg/day or 5–25 mg/m²/day in divided doses every 6–12 hr. Asthma exacerbations: 1 mg/kg every 6 hr for 48 hr; then 1–2 mg/kg/day (maximum: 60 mg/day) divided twice daily.
IM IV (Adults ): Most uses: methylprednisolone sodium succinate: 40–250 mg every 4–6 hr. High-dose “pulse” therapy: Methylprednisolone sodium succinate: 30 mg/kg IV every 4–6 hr for up to 72 hr. Multiple sclerosis: Methylprednisolone sodium succinate: 160 mg/day for 7 days; then 64 mg every other day for 1 mo.Adjunctive therapy of Pneumocystis jirovecii pneumonia in patients with AIDS:Methylprednisolone sodium succinate: 30 mg twice daily for 5 days; then 30 mg once daily for 5 days; then 15 mg once daily for 10 days. Acute spinal cord injury: Methylprednisolone sodium succinate: 30 mg/kg over 15 min initially, followed 45 min later with 5.4 mg/kg/hr for 23 hr (unlabeled).
IM IV (Children ): Anti-inflammatory/Immunosuppressive: 0.5–1.7 mg/kg/day or 5–25 mg/m²/day in divided doses every 6–12 hr Acute spinal cord injury: Methylprednisolone sodium succinate: 30 mg/kg over 15 min initially; then 45 min later, initiate continuous infusion of 5.4 mg/kg/hr for 23 hr (unlabeled). Status asthmaticus: 2 mg/kg/dose; then 0.5–1 mg/kg/dose every 6 hr. Lupus nephritis: 30 mg/kg IV every other day for 6 doses.
IM (Adults ): Methylprednisolone acetate: 40–120 mg daily, weekly, or every 2 wk.

Availability ⬆ ⬇

(Generic available)

Tablets: 2 mg; 4 mg; 8 mg; 16 mg; 32 mg
Powder for injection (sodium succinate): 40 mg/vial; 125 mg/vial; 500 mg/vial; 1 g/vial; 2 g/vial
Suspension for injection (acetate): 20 mg/mL; 40 mg/mL; 80 mg/mL

Assessment ⬆ ⬇

Indicated for many conditions. Assess involved systems before and periodically during therapy.
Monitor for signs and symptoms of adrenal insufficiency (fatigue, weakness, nausea and vomiting, low BP); corticosteroid should be tapered slowly.
Monitor for signs and symptoms of hypercorticism (moon face, buffalo hump, stretch marks, obesity, bruising, hyperglycemia, elevated BP) every 6 mo; pediatric patients under one yr of age may require more frequent monitoring (every 3–4 mo); temporary discontinuation, dose reduction, or slowed taper may be needed.
Assess for signs of infection (fever, chills, sore throat, wound that will not heal).
Assess for signs and symptoms of Kaposi's sarcoma (purple, red, or brown skin blotches on skin or inside the mouth) with long term use.
Monitor intake and output ratios and daily weights. Observe patient for peripheral edema, steady weight gain, rales/crackles, or dyspnea. Notify health care professional should these occur.
Pedi: Evaluate growth of children periodically during therapy. Monitor linear growth and weight gain. Adjust doses accordingly

Lab Test Considerations:

Monitor CBC, electrolytes, serum and urine glucose, and lipid panel routinely during therapy. May cause hyperglycemia, especially in persons with diabetes. May cause hypokalemia, hypocalcemia, hypernatremia. May ↓ WBC counts. May ↑ lipid values.
- May suppress reactions to allergy skin tests.
- Guaiac test stools. Promptly report presence of guaiac-positive stools.
- May ↓ uptake of thyroid ¹²³I or ¹³¹I.
- Periodic adrenal function tests may be ordered to assess degree of hypothalamic-pituitary-adrenal axis suppression in systemic and chronic topical therapy.

Implementation ⬆ ⬇

Do not confuse Depo-Medrol with Solu-Medrol. Do not confuse Solu-Medrol with Solu-Cortef. Do not confuse methylprednisolone with medroxyprogesterone or methyltestosterone.
If dose is ordered daily or every other day, administer in the morning to coincide with the body's normal secretion of cortisol.
Periods of stress, such as surgery, may require supplemental systemic corticosteroids.
PO: Administer with meals to minimize GI irritation; do not administer with grapefruit juice.
- Tablets may be crushed and administered with food or fluids for patients with difficulty swallowing.
IM: Shake suspension well before drawing up. IM doses should not be administered when rapid effect is desirable. Do not dilute with other solution or admix. Do not administer acetate suspensions IV.

IV Administration:

Reconstitute with provided solution (Act-O-Vials, Univials, ADD-Vantage vials) or 2 mL of bacteriostatic water (with benzyl alcohol) for injection. Use preservative-free diluent for use in neonates. Concentration: Maximum of 125 mg/mL.
Rate: Low dose (≤1.8 mg/kg or ≤125 mg/dose): May be administered IV push over 3–15 min.
Intermittent/Continuous Infusion: Diluent: May be diluted further in D5W (infuse within 8 hr), 0.9% NaCl, or D5/0.9% NaCl. Concentration: 2.5–20 mg/mL.

Patient/Family Teaching ⬆ ⬇

Educate patient on reason for methylprednisoloneand side effects. Instruct them to take medication as directed. Take missed doses as soon as remembered unless almost time for next dose. Do not double doses. Do not share medication with others, even if they have similar symptoms; may be harmful. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
- Explain need for continued medical follow-up to assess effectiveness and possible side effects of medication. Periodic lab tests and eye exams may be needed.
- Stopping the medication suddenly may result in adrenal insufficiency (anorexia, nausea, weakness, fatigue, dyspnea, hypotension, hypoglycemia). If these signs appear, notify health care professional immediately. This can be life-threatening. Medical ID should be worn in case of emergencies.
- Advise patient to avoid grapefruit juice during therapy; may ↑methylprednisolonelevels.
- Advise patient to notify health care professional of signs and symptoms of hypercorticism (acne; thicker or more hair on body and face; bruising easily; fatty pad or hump between shoulders [buffalo hump]; rounding of face [moon face]; pink or purple stretch marks on skin of abdomen, thighs, breasts, and arms; ankle swelling), adrenal suppression (tiredness, weakness, nausea and vomiting, low blood pressure), worsening of allergies (eczema, rhinitis), or infection (fever, chills, pain, feeling tired, aches, nausea and vomiting).
- May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
- Instruct patient to inform health care professional promptly if severe abdominal pain or tarry stools occur.
- Corticosteroids cause immunosuppression and may mask symptoms of infection. May worsen existing tuberculosis; fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex. Notify health care professional immediately if exposed to chicken pox or measles.
- Caution patient to avoid vaccinations without first consulting health care professional.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications, especially St. John's wort.
- Advise parents that use may cause shortened stature.
- Instruct patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Hypoadrenalism may occur in infants born to mothers receiving corticosteroids during pregnancy. Observe infant for signs of hypoadrenalism (poor feeding, irritability, weakness, vomiting).
Long-term Therapy: Encourage patient to eat a diet high in protein, calcium, and potassium, and low in sodium and carbohydrates (see Food Sources for Specific Nutrients). Alcohol should be avoided during therapy.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇