methylprednisolone (redirected from methylprednisolone-21-dimethylaminoacetate)

methylprednisolone /meth·yl·pred·nis·o·lone/ (-pred-nis´ah-lon) a synthetic glucocorticoid derived from progesterone, used in replacement therapy for adrenocortical insufficiency and as an antiinflammatory and immunosuppressant; also used as m. acetate and m. sodium succinate.

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meth·yl·pred·nis·o·lone (mthl-prd-ns-ln)

n.

An anti-inflammatory steroid administered to children and adolescents to relieve the pain induced by sickle cell anemia.

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methylprednisolone

a glucocorticoid with anti-inflammatory action similar to that of prednisolone. The acetate is often prepared in long-acting forms while the water-soluble, rapid-acting succinate is suitable for intravenous administration and is used in the treatment of shock.

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methylprednisolone-21-dimethylaminoacetate

a long-acting glucocorticoid, used in the treatment of dermatoses and allergic conditions.

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methylprednisolone

Medrol, Medrone (UK)

Pharmacologic class: Glucocorticoid

Therapeutic class: Antiasthmatic, anti-inflammatory (steroidal), immunosuppressant

Pregnancy risk category C

Action

Unclear. Reduces inflammation and prevents edema by stabilizing membranes and reducing permeability of leukocytic cells. Suppresses immune system by interfering with antigen-antibody interactions of macrophages and T cells.

Availability

Solution for injection: 40 mg, 125 mg, 500 mg, 1 g, 2 g

Suspension for injection: 20 mg/ml, 40 mg/ml, 80 mg/ml

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

⊘Indications and dosages

➣ Diseases and disorders of endocrine system, collagen, skin, eye, GI tract, respiratory system, or hematologic system; neoplastic diseases; allergies; edema; multiple sclerosis; tuberculous meningitis; trichinosis; rheumatic disorders; osteoarthritis; bursitis; localized inflammatory lesions

Adults: Methylprednisolone - 4 to 160 mg P.O. daily in four divided doses, depending on disease or disorder. Acetate - 40 to 120 mg I.M., or 4 to 80 mg by intra-articular or soft-tissue injection, or 20 to 60 mg by intralesional injection (depending on type, size, and location of inflammation); may be repeated at 1 to 5 weeks. Sodium succinate high-dose therapy - 30 mg/kg I.V. over at least 30 minutes. May be repeated q 4 to 6 hours for 48 hours.

Off-label uses

• Lupus nephritis
• Pneumocystis jiroveci pneumonia in AIDS patients

Contraindications

• Hypersensitivity to drug or its component
• Systemic fungal infections
• Use in premature infants (with sodium succinate form, which contains benzyl alcohol)

Precautions

Use cautiously in:
• cardiovascular, hepatic, renal, or GI disease; active untreated infections; thromboembolitic tendency; idiopathic thrombocytopenic purpura; osteoporosis; myasthenia gravis; hypothyroidism; glaucoma; ocular herpes simplex; vaccinia or varicella; seizure disorders; metastatic cancer
• pregnant or breastfeeding patients
• children.

Administration

• As needed and prescribed, give prophylactic antacids to prevent peptic ulcers in patients receiving high doses.
• When methylprednisolone acetate is substituted for oral form, know that I.M. dosage should equal oral dosage and should be given once daily.
• Know that methylprednisolone acetate is not for I.V. use. It may be given I.M. or by intra-articular, intralesional, or soft-tissue injection.
• Be aware that methylprednisolone sodium succinate may be given I.M. or I.V. Reconstitute with bacteriostatic water for injection containing 0.9% benzyl alcohol, per manufacturer's instructions.
• In long-term methylprednisolone therapy, alternate-day therapy should be considered.
• For direct I.V. injection, inject each 500-mg dose over 2 to 3 minutes or more. For I.V. infusion, further dilute in compatible I.V. solution (such as 5% dextrose, 0.9% sodium chloride, or 5% dextrose in 0.9% sodium chloride injection) and give over 10 to 20 minutes.
• Maintain patient on lowest effective dosage, to minimize adverse effects.

Route	Onset	Peak	Duration
P.O.	Rapid	2-3 hr	30-36 hr
I.M., I.V. (succinate)	Rapid	Unknown	Unknown
I.M. (acetate)	6-48 hr	4-8 days	1-4 wk

Adverse reactions

CNS: headache, restlessness, nervousness, depression, euphoria, personality changes, psychoses, vertigo, paresthesias, insomnia, adhesive arachnoiditis, conus medullaris syndrome, increased intracranial pressure, seizures, meningitis

CV: hypotension, hypertension, arrhythmias, heart failure, shock, fat embolism, thrombophlebitis, thromboembolism

EENT: cataracts, glaucoma, increased intraocular pressure, nasal irritation, nasal septum perforation, sneezing, epistaxis, nasopharyngeal or oropharyngeal fungal infection, dysphonia, hoarseness, throat irritation

GI: nausea, vomiting, abdominal distention, rectal bleeding, dry mouth, anorexia, esophageal candidiasis, esophageal ulcer, peptic ulcer, pancreatitis

GU: amenorrhea, irregular menses

Respiratory: cough, wheezing, bronchospasm

Metabolic: decreased growth (in children), reduced carbohydrate tolerance, diabetes mellitus, hyperglycemia, sodium and fluid retention, hypokalemia, hypocalcemia, cushingoid state (with long-term use), hypothalamic-pituitary-adrenal suppression (with systemic use beyond 5 days), adrenal suppression (with long-term, high-dose use), acute adrenal insufficiency (with abrupt withdrawal)

Musculoskeletal: muscle wasting, osteoporosis, osteonecrosis, tendon rupture, aseptic joint necrosis, muscle pain and weakness, steroid myopathy, spontaneous fractures (with long-term use)

Skin: facial edema, rash, pruritus, urticaria, contact dermatitis, acne, decreased wound healing, bruising, hirsutism, thin and fragile skin, petechiae, purpura, striae, subcutaneous fat atrophy, skin atrophy, acneiform lesions, angioedema

Other: anosmia, bad taste, increased appetite, weight gain (with long-term use), Churg-Strauss syndrome, increased susceptibility to infection, aggravation or masking of infections, impaired wound healing, atrophy at injection site, local pain and burning, irritation, hypersensitivity reaction

Interactions

Drug-drug. Amphotericin B, mezlocillin, piperacillin, thiazide and loop diuretics, ticarcillin: additive hypokalemia

Fluoroquinolones: increased risk of tendon rupture

Isoniazid, phenobarbital, phenytoin, rifampin: decreased methylprednisolone efficacy

Ketoconazole: decreased methylprednisolone clearance

Live-virus vaccines: decreased antibody response to vaccine, increased risk of adverse reactions

Nonsteroidal anti-inflammatory drugs: increased risk of adverse GI effects

Oral anticoagulants: altered anticoagulant requirement

Drug-diagnostic tests. Calcium, potassium, thyroxine, triiodothyronine: decreased levels

Cholesterol, glucose: increased levels

Nitroblue tetrazolium test for bacterial infection: false-negative result

Drug-herbs. Echinacea: increased immune stimulation

Ginseng: immunomodulation

Drug-behaviors. Alcohol use: increased risk of gastric irritation and ulcers

Patient monitoring

• Monitor fluid and electrolyte balance, weight, and blood pressure.
• With long-term or high-dose use, assess for cushingoid effects, such as moon face, central obesity, acne, abdominal striae, hypertension, osteoporosis, myopathy, hyperglycemia, fluid and electrolyte imbalances, and increased susceptibility to infection.
☞ Check for signs and symptoms of steroid-induced psychosis (delirium, euphoria, insomnia, mood swings, personality changes, and depression).
• Monitor growth and development in children on prolonged therapy.
• Know that therapy beyond 6 months increases risk of osteoporosis. Obtain baseline bone density mass, and provide teaching about lifestyle factors (such as weight-bearing exercise, proper diet, moderation of alcohol intake, and smoking cessation) and possible need for calcium, vitamin D, or bisphosphonate therapy.
• With long-term use, withdraw drug gradually.
☞ After dosage reduction or drug withdrawal, monitor patient for signs and symptoms of adrenal insufficiency.

Patient teaching

• Tell patient to take with food to minimize GI upset.
• Advise patient on chronic therapy to have periodic eye exams and to carry medical identification that states he's taking drug.
• Inform patient that drug increases risk for infection. Urge him to avoid exposure to people with infections such as measles and chickenpox. Tell him to contact prescriber if exposure occurs.
• Advise patient to report unusual weight gain, swelling, muscle weakness, black tarry stools, vomiting of blood, menstrual irregularities, sore throat, fever, or infection.
☞ Tell patient to immediately report signs or symptoms of adrenal insufficiency (including fatigue, appetite loss, nausea, vomiting, diarrhea, weight loss, weakness, and dizziness) after dosage reduction or drug withdrawal.
• Advise diabetic patient to monitor blood glucose level carefully.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.