Yes

Corticosteroid, Parenteral

Dental: Treatment of a variety of oral diseases of allergic, inflammatory or autoimmune origin

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

C

Serious infections, except septic shock or tuberculous meningitis; known hypersensitivity to methylprednisolone; viral, fungal, or tubercular skin lesions; administration of live virus vaccines. Methylprednisolone formulations containing benzyl alcohol preservative are contraindicated in infants.

Use with caution in patients with hyperthyroidism, cirrhosis, nonspecific ulcerative colitis, hypertension, osteoporosis, thromboembolic tendencies, CHF, convulsive disorders, myasthenia gravis, thrombophlebitis, peptic ulcer, diabetes; because of the risk of adverse effects, systemic corticosteroids should be used cautiously in the elderly, in the smallest possible dose, and for the shortest possible time

>10%:

Central nervous system: Insomnia, nervousness

Gastrointestinal: Increased appetite, indigestion

1% to 10%:

Dermatologic: Hirsutism

Endocrine & metabolic: Diabetes mellitus, adrenal suppression, hyperlipidemia

Hematologic: Transient leukocytosis

Neuromuscular & skeletal: Arthralgia

Ocular: Cataracts, glaucoma

Miscellaneous: Infections

<1%: Edema, hypertension, vertigo, seizures, psychoses, pseudotumor cerebri, headache, mood swings, delirium, hallucinations, euphoria, acne, skin atrophy, bruising, hyperpigmentation, Cushing's syndrome, pituitary-adrenal axis suppression, growth suppression, glucose intolerance, hypokalemia, alkalosis, amenorrhea, sodium and water retention, hyperglycemia, peptic ulcer, nausea, vomiting, abdominal distention, ulcerative esophagitis, pancreatitis, muscle weakness, osteoporosis, fractures, hypersensitivity reactions, arrhythmias, avascular necrosis, secondary malignancy, intractable hiccups

Arrhythmias and cardiovascular collapse are possible with rapid intravenous infusion of high dose methylprednisolone. Symptoms of overdose include cushingoid appearance (systemic), muscle weakness (systemic), osteoporosis (systemic) all with long-term use only. When consumed in excessive quantities for prolonged periods, systemic hypercorticism and adrenal suppression may occur; in those cases, discontinuation and withdrawal of the corticosteroid should be done judiciously.

CYP3A enzyme inducer

Phenytoin, phenobarbital, rifampin increase clearance of methylprednisolone

Potassium depleting diuretics enhance potassium depletion

Increased toxicity:

Skin test antigens, immunizations decrease response and increase potential infections

Methylprednisolone may increase circulating glucose levels and may need adjustments of insulin or oral hypoglycemics

Intact vials of methylprednisolone sodium succinate should be stored at controlled room temperature

Reconstituted solutions of methylprednisolone sodium succinate should be stored at room temperature (15°C to 30°C) and used within 48 hours

Stability of parenteral admixture at room temperature (25°C) and at refrigeration temperature (4°C): 48 hours

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

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

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.

Time to obtain peak effect and the duration of these effects is dependent upon the route of administration

Peak Effect:

Oral: 1-2 hours

I.M.: 4-8 days

Intra-articular: 1 week

Duration:

Oral: 30-36 hours

I.M.: 1-4 weeks

Intra-articular: 1-5 weeks

Distribution: V_d: 0.7-1.5 L/kg

Half-life: 3-3.5 hours, clearance is reduced obese patients

Methylprednisolone sodium succinate is highly soluble and has a rapid effect by I.M. and I.V. routes; methylprednisolone acetate has a low solubility and has a sustained I.M. effect

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

Children:

Anti-inflammatory or immunosuppressive: Oral, I.M., I.V. (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 greater than or equal to 30 minutes given once daily for 3 days

Status asthmaticus: I.V. (sodium succinate): Loading dose: 2 mg/kg/dose, then 0.5-1 mg/kg/dose every 6 hours for up to 5 days

Acute spinal cord injury: I.V. (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

Lupus nephritis: I.V. (sodium succinate): 30 mg/kg over greater than or equal to 30 minutes every other day for 6 doses

High-dose therapy for acute spinal cord injury: I.V. bolus: 30 mg/kg over 15 minutes, followed 45 minutes later by an infusion of 5.4 mg/kg/hour for 23 hours

Adults:

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

I.M. (sodium succinate): 10-80 mg/day once daily

I.M. (acetate): 10-80 mg every 1-2 weeks

I.V. (sodium succinate): 10-40 mg over a period of several minutes and repeated I.V. or I.M. at intervals depending on clinical response; when high dosages are needed, administer 30 mg/kg over a period of greater than or equal to 30 minutes and may be repeated every 4-6 hours for 48 hours

Status asthmaticus: I.V. (sodium succinate): Loading dose: 2 mg/kg/dose, then 0.5-1 mg/kg/dose every 6 hours for up to 5 days

High-dose therapy for acute spinal cord injury: I.V. bolus: 30 mg/kg over 15 minutes, followed 45 minutes later by an infusion of 5.4 mg/kg/hour for 23 hours

Lupus nephritis: High-dose "pulse" therapy: I.V. (sodium succinate): 1 g/day for 3 days

Aplastic anemia: I.V. (sodium succinate): 1 mg/kg/day or 40 mg/day (whichever dose is higher), for 4 days. After 4 days, change to oral and continue until day 10 or until symptoms of serum sickness resolve, then rapidly reduce over approximately 2 weeks.

Hemodialysis: Slightly dialyzable (5% to 20%); administer dose posthemodialysis

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

Large joints: 20-80 mg

Small joints: 4-10 mg

Intralesional (acetate): 20-60 mg every 1-5 weeks

Should be taken after meals or with food or milk; limit caffeine; need diet rich in pyridoxine, vitamin C, vitamin D, folate, calcium, phosphorus, and protein

Blood pressure, blood glucose, electrolytes

Interferes with skin tests

Nervousness and insomnia are common; may rarely cause delirium, mood swings, euphoria, or hallucinations

Barbiturates may increase the clearance of methylprednisolone

No information available to require special precautions

No effects or complications reported

Maintain adequate nutritional intake; consult prescriber for possibility of special dietary instructions. If diabetic, monitor serum glucose closely and notify prescriber of any changes; this medication can alter hypoglycemic requirements. Inform prescriber if you are experiencing unusual stress; dosage may need to be adjusted. You will be susceptible to infection; avoid crowds or infected persons or persons with contagious diseases. You may experience insomnia or nervousness; use caution when driving or engaging in tasks requiring alertness until response to drug is known. Report increased pain, swelling, or redness in area being treated; excessive or sudden weight gain; swelling of extremities; difficulty breathing; muscle pain or weakness; change in menstrual pattern; vision changes; signs of hyperglycemia; signs of infection (eg, fever, chills, mouth sores, perianal itching, vaginal discharge); blackened stool; other persistent side effects; or worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Intra-articular: Refrain from excessive use of joint following therapy, even if pain is gone.

Acetate salt should not be given I.V.

Injection, as acetate: 20 mg/mL (5 mL, 10 mL); 40 mg/mL (1 mL, 5 mL, 10 mL); 80 mg/mL (1 mL, 5 mL)

Injection, as sodium succinate: 40 mg (1 mL, 3 mL); 125 mg (2 mL, 5 mL); 500 mg (1 mL, 4 mL, 8 mL, 20 mL); 1000 mg (1 mL, 8 mL, 50 mL); 2000 mg (30.6 mL)

Tablet: 2 mg, 4 mg, 8 mg, 16 mg, 24 mg, 32 mg

Tablet, dose pack: 4 mg (21s)

Tornatore KM, Logue G, Venuto RC, et al, "Pharmacokinetics of Methylprednisolone in Elderly and Young Healthy Males," J Am Geriatr Soc, 1994, 42(10):1118-22.