methylprednisolone

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methylprednisolone

 [meth″il-pred-nis´o-lōn]
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.

methylprednisolone

Medrol, Medrone (UK)

methylprednisolone acetate

Depo-Medrol, Depo-Medrone (UK), Unimed (CA)

methylprednisolone sodium succinate

A-Methapred, Solu-Medrol, Solu-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.

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.

methylprednisolone

(mĕth′əl-prĕd-nĭs′ə-lōn′)
n.
A glucocorticoid used therapeutically primarily as an anti-inflammatory agent.

methylprednisolone

A CORTICOSTEROID drug used in a wide range of conditions to control severe inflammation, treat allergies and replace stroid deficiencies. It is commonly used in depot form for long-term action. Brand names are Medrone, Depo-Medrone and Solu-Medrone.
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