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Methylprednisolone information from DrugsUpdate  

See Available Brands of Methylprednisolone in India

P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *
LI - Lab *

Methylprednisolone is a synthetic glucocorticoid drug. It is sold in the USA and Canada under the brand names Medrol, Solu-Medrol and Cadista. It is also available as a generic drug.

It is a variant of prednisolone, methylated at carbon 6 of the B ring.

Pharmacodynamics

Pharmacokinetics

Methylprednisolone is a synthetic corticosteroid with mainly glucocorticoid activity and minimal mineralocorticoid properties. It decreases inflammation by suppression of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability.

Onset
Peak effect: Oral: 1-2 hours; IM: 4-8 days; Intra-articular: 1 week.

Duration
Oral: 30-36 hours; IM: 1-4 weeks; Intra-articular: 1-5 weeks; As acetate, has a low solubility and has sustained IM effect.

Absorption

Methylprednisolone is fairly rapidly distributed after oral doses; plasma half-life:≥3.5 hours; tissue half-life: 18-36 hours. As acetate, it is absorbed from joints over a wk but is more slowly absorbed following deep IM injection. As sodium succinate ester, it is rapidly absorbed after IM doses, with peak plasma concentrations in 2 hours.

Distribution
Volume of distribution: 0.7-1.5 L/kg ; crosses the placenta.

Excretion
Half-life elimination: 3-3.5 hours; clearance reduced in obese.

Methylprednisolone Indications / Methylprednisolone Uses

Information Not Available

Methylprednisolone Adverse Reactions / Methylprednisolone Side Effects

Oedema, hypertension, arrhythmia; CNS, endocrine, metabolic and GI effects; hirsutism, acne, skin atrophy, bruising, hyperpigmentation; transient leukocytosis; arthralgia, muscle weakness, osteoporosis, fractures, cataracts, glaucoma; infections, hypersensitivity reactions, avascular necrosis, secondary malignancy, intractable hiccups.

Precautions

Information Not Available

Special Precautions

Children and adolescents (possible irreversible growth retardation), elderly (monitoring required on long-term treatment). Frequent monitoring if history of tuberculosis (or X-ray changes), hypertension, recent MI (rupture reported), CHF, liver and renal failure (associated with fluid retention), DM including family history (glucose regulation altered), osteoporosis especially post-menopausal women (associated with increased bone loss and osteoporotic fractures), glaucoma including family history (risk of increased intraocular pressure), corneal perforation, severe affective disorders (particularly if history of steroid-induced psychosis), epilepsy, GI disease (perforation risk), thyroid disease (changes in thyroid status may necessitate dosage adjustments ), history of steroid myopathy. Pregnancy and lactation. Avoid abrupt withdrawal after a prolonged period of use. When applied topically to large areas, broken skin, or under occlusive dressings, may cause systemic effects.

Other Drug Interactions

Decreases effect of anticholinesterases in myasthenia gravis. May decrease the hypoglycaemic effects of antidiabetic agents. Decreases serum concentrations of salicylates. Increased hypokalemic effects of potassium-depleting diuretics (thiazides or furosemide), amphotericin B, bronchodilator therapy with xanthines or β2 agonists. Increase incidence of GI bleeding and ulceration with NSAIDs. May increase the anticoagulant effects of warfarin. Decreased levels/effects with CYP3A4 inducers (aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins). Increased levels/effects with CYP3A4 inhibitors (azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, and verapamil). May decrease the effects of vaccines (dead organism) or increase the risk of vaccinal infection (live organism). Antacids and bile sequestrants may decrease the absorption of corticosteroids, separate admin by 2 hr. Increased risk of myopathy with neuromuscular-blocking agents, tendinopathies with fluoroquinolones.

Other Interactions

Food Interaction
Interferes with calcium absorption. Limit caffeine.

Dosage

Oral
Anti-inflammatory or immunosuppressive
Adult: Initially, 2-60 mg/day in 1-4 divided doses, followed by gradual reduction in dosage to the lowest possible level consistent with maintaining an adequate clinical response.
Child: As 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.

Intravenous
Anti-inflammatory or immunosuppressive
Adult: As sodium succinate: 10-40 mg over a period of several min and repeated I.V. or I.M. 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.
Child: As 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.

Intravenous

Status asthmaticus
Adult: As sodium succinate: Loading dose: 2 mg/kg/dose, then 0.5-1 mg/kg/dose every 6 hours for up to 5 days.
Child: Children: As sodium succinate: Loading dose: 2 mg/kg/dose, then 0.5-1 mg/kg/dose every 6 hours for up to 5 days.

Intravenous
Acute spinal cord injury
Adult: As sodium succinate: 30 mg/kg over 15 minutes, followed in 45 minutes by a continuous infusion of 5.4 mg/kg/hr for 23 hours.
Child: As sodium succinate: 30 mg/kg over 15 minutes, followed in 45 minutes by a continuous infusion of 5.4 mg/kg/hr for 23 hours.

Intravenous
Lupus nephritis
Adult: As sodium succinate: High-dose "pulse" therapy: 1 g/day for 3 days.
Child: Children: As sodium succinate: 30 mg/kg over ≥30 minutes every other day for 6 doses.

Intravenous
Aplastic anaemia
Adult: As 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 approx 2 weeks.

Intravenous
Pneumocystis carinii pneumonia in patients with acquired immunodeficiency syndrome (AIDS)
Adult: As sodium succinate: 30 mg bid for 5 days, then 30 mg once daily for 5 days, then 15 mg once daily for 11 days.

Intravenous
Life-threatening shock
Adult: As sodium succinate: 30 mg/kg initially and repeated every 4-6 hours if needed or 100-250 mg initially and repeated at 2- 6-hours intervals as required by direct IV injection over a period of 3-15 minutes. Alternatively, following the initial dose by direct IV injection, 30 mg/kg by slow continuous IV infusion every 12 hours for 24-48 hours.

Intravenous
Croup
Child: 1-2 mg/kg followed by 0.5 mg/kg every 6-8 hours.

Intramuscular
Anti-inflammatory or immunosuppressive
Adult: As sodium succinate: 10-80 mg/day once daily; As acetate: 10-80 mg every 1-2 weeks.
Child: As 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.

Topical/Cutaneous
Corticosteroid-responsive dermatoses
Adult: As 0.1% aceponate ointment, fatty ointment or cream or lotion: Apply a thin coating once daily to the affected area. Duration: <12 weeks.
Child: >4 months: As 0.1% aceponate ointment, fatty ointment or cream: Apply a thin coating once daily to the affected area; Lotion: Apply sparingly once daily to the affected area and rub gently. Duration: <4 weeks.

Intralesional

Anti-inflammatory or immunosuppressive
Adult: As acetate: 20-60 mg every 1-5 weeks.

Intra-articular
Anti-inflammatory or immunosuppressive
Adult: As acetate: Large joints: 20-80 mg every 1-5 weeks; Small joints: 4-10 mg every 1-5 weeks.

Reconstitution
Standard diluent: 40 mg/50 ml D5W; 125 mg/50 ml D5W. Min volume: 50 ml D5W.

Incompatibility
Y-site incompatibility: Allopurinol, amsacrine, ciprofloxacin, propofol, sargramostim, vinorelbine, docetaxel, etoposide phosphate, filgrastim, gemcitabine, ondansetron, paclitaxel. Syringe incompatibility: Doxapram. Admixture incompatibility: Calcium gluconate, glycopyrrolate, regular insulin, penicillin G sodium, metaraminol, nafcillin.

Food(before/after)

Should be taken with food

List of Contraindications

Methylprednisolone and Pregnancy

Caution when used during pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Methylprednisolone and Lactation

Caution when used during lactation

Methylprednisolone and Children

May be more susceptible to adverse effects from topical use. Benzyl alcohol/gasping syndrome may occur with use of methylprednisolone sodium succinate.

Methylprednisolone and Geriatic

May require lower doses

Methylprednisolone and Other Contraindications

Serious infections except septic shock or tuberculous meningitis; viral, fungal and tubercular skin lesions; admin of live virus vaccines. Preparations containing benzyl alcohol preservative are contraindicated in infants.

Storage

Intra-articular
Store at a temperature <40°C, preferably between 15-30 °C. As acetate: freezing of sterile solution suspension should be avoided; store at controlled room temperature of 20-25°C.

Intralesional

Store at a temperature <40°C, preferably between 15-30 °C. As acetate: freezing of sterile solution suspension should be avoided; store at controlled room temperature of 20-25°C.

Intramuscular
Store at a temperature <40°C, preferably between 15-30 °C. As acetate: Freezing of sterile solution suspension should be avoided; store at controlled room temperature of 20-25°C. As sodium succinate: Store unreconstituted sterile powder and reconstituted solutions at a controlled room temperature of 20-25°C. Reconstituted solutions should not be used unless they are clear, and unused solutions should be discarded after 48 hours.

Intravenous

Store at a temperature <40°C, preferably between 15-30 °C. As acetate: freezing of sterile solution suspension should be avoided; store at controlled room temperature of 20-25°C. As sodium succinate: Store unreconstituted sterile powder and reconstituted solutions at a controlled room temperature of 20-25°C. Reconstituted solutions should not be used unless they are clear, and unused solutions should be discarded after 48 hours.

Oral
Store at a temperature <40°C, preferably between 15-30 °C.


Topical/Cutaneous
Ointment or cream: <25°C, stable for 3 years from date of manufacture; Fatty ointment or lotion: <30°C, stable for 5 years from date of manufacture.

Lab interference

Intra-articular
Store at a temperature <40°C, preferably between 15-30 °C. As acetate: freezing of sterile solution suspension should be avoided; store at controlled room temperature of 20-25°C.

Intralesional

Store at a temperature <40°C, preferably between 15-30 °C. As acetate: freezing of sterile solution suspension should be avoided; store at controlled room temperature of 20-25°C.

Intramuscular
Store at a temperature <40°C, preferably between 15-30 °C. As acetate: Freezing of sterile solution suspension should be avoided; store at controlled room temperature of 20-25°C. As sodium succinate: Store unreconstituted sterile powder and reconstituted solutions at a controlled room temperature of 20-25°C. Reconstituted solutions should not be used unless they are clear, and unused solutions should be discarded after 48 hours.

Intravenous

Store at a temperature <40°C, preferably between 15-30 °C. As acetate: freezing of sterile solution suspension should be avoided; store at controlled room temperature of 20-25°C. As sodium succinate: Store unreconstituted sterile powder and reconstituted solutions at a controlled room temperature of 20-25°C. Reconstituted solutions should not be used unless they are clear, and unused solutions should be discarded after 48 hours.

Oral
Store at a temperature <40°C, preferably between 15-30 °C.


Topical/Cutaneous
Ointment or cream: <25°C, stable for 3 years from date of manufacture; Fatty ointment or lotion: <30°C, stable for 5 years from date of manufacture.

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