Depo-pred

Approved Indications:

A. Musculoskeletal and Joint Disorders (via intra-articular or intramuscular injection):

• Osteoarthritis
• Rheumatoid arthritis
• Bursitis
• Synovitis of osteoarthritis
• Epicondylitis (e.g., tennis elbow)
• Acute gouty arthritis

B. Dermatologic Diseases:

• Severe seborrheic dermatitis
• Psoriasis
• Contact dermatitis
• Atopic dermatitis
• Keloids

C. Allergic Conditions:

• Bronchial asthma
• Seasonal or perennial allergic rhinitis
• Drug hypersensitivity reactions
• Serum sickness
• Urticaria

D. Respiratory Diseases:

• Chronic obstructive pulmonary disease (COPD) exacerbation
• Pulmonary sarcoidosis
• Aspiration pneumonitis

E. Endocrine Disorders:

• Primary or secondary adrenocortical insufficiency (as adjunct therapy)

F. Hematologic Disorders:

• Idiopathic thrombocytopenic purpura (in adults)
• Secondary thrombocytopenia

G. Gastrointestinal Diseases:

• Ulcerative colitis
• Regional enteritis (Crohn’s disease)

H. Nervous System Disorders:

• Multiple sclerosis exacerbations
• Cerebral edema associated with brain tumors

I. Ophthalmic Conditions:

• Severe inflammatory conditions of the eye (e.g., uveitis, optic neuritis)

Off-label/Clinically Accepted Uses:

• Acute spinal cord injury (early high-dose protocol)
• Postoperative inflammation
• Plantar fasciitis (via local injection)
• Keloid scar reduction (intralesional)

Route: Intramuscular (IM), Intra-articular, Intralesional

Adults:

• IM (Systemic anti-inflammatory):
• Dose: 10 to 80 mg every 1–2 weeks, depending on condition severity and response.
• Duration: Single dose or repeated every 1 to 4 weeks based on clinical need.
• Intra-articular:
• Small joints (e.g., fingers): 4 to 10 mg
• Medium joints (e.g., elbow, wrist): 10 to 40 mg
• Large joints (e.g., knee, shoulder): 20 to 80 mg
• Frequency: Not more than once every 3–4 weeks.
• Intralesional (e.g., for keloids, psoriasis plaques):
• Dose: 20 to 60 mg/mL diluted appropriately; volume varies by lesion size.
• Frequency: Every 1 to 3 weeks

Pediatrics:

• IM Use: 1 to 1.5 mg/kg as a single dose; not to exceed 80 mg per injection. For conditions like asthma or severe allergy.
• Intra-articular and intralesional use is generally reserved for older children under specialist guidance.

Elderly:

• Similar dosing as adults but initiate at the lower end of the dosing range due to increased sensitivity to glucocorticoid side effects.

Renal/Hepatic Impairment:

• No dosage adjustment is provided, but careful monitoring is recommended due to altered metabolism or fluid retention potential.

Administration Notes:

• Do not administer intravenously.
• Shake well before use; suspension should appear uniformly milky.
• Sterile technique is essential for all injection routes.
• Avoid injecting into infected sites or unstable joints.

Methylprednisolone Acetate is a synthetic glucocorticoid prodrug that, once converted to its active form (methylprednisolone), binds to cytoplasmic glucocorticoid receptors. This complex translocates to the nucleus, modulating gene expression to suppress the transcription of pro-inflammatory cytokines and mediators such as interleukins and TNF-α. Simultaneously, it increases the expression of anti-inflammatory proteins like annexin-1. These actions inhibit leukocyte migration, reduce capillary permeability, suppress fibroblast proliferation, and dampen overall immune responses, providing strong anti-inflammatory and immunosuppressive effects.

• Absorption: Slowly absorbed from IM or intra-articular depot injection; onset ranges from 6–48 hours depending on site.
• Bioavailability: Nearly 100% systemically after IM administration.
• Distribution: Widely distributed; crosses the placenta and enters breast milk.
• Metabolism: Primarily in the liver via hepatic enzymes into inactive metabolites.
• Half-life:
• Biologic half-life: 18 to 36 hours
• Plasma half-life: 2 to 4 hours
• Excretion: Mostly renal excretion of inactive metabolites.
• Peak Effect: Within 24–48 hours (IM route)

• Pregnancy: FDA Category C. Animal studies show adverse fetal effects; use only if potential benefit justifies the risk. May increase risk of orofacial clefts in the first trimester.
• Lactation: Excreted in breast milk. While systemic absorption from the infant is minimal with short-term use, high doses or prolonged treatment may suppress infant adrenal function. Monitor infant growth and development if prolonged maternal use occurs.

• Primary Class: Glucocorticoid (Corticosteroid)
• Subclass: Long-acting, intermediate-potency corticosteroid
• Formulation Type: Injectable corticosteroid suspension (depot formulation)

• Known hypersensitivity to methylprednisolone or other corticosteroids
• Systemic fungal infections
• Intravenous administration (not approved for acetate form)
• Administration into infected or unstable joints
• Idiopathic thrombocytopenic purpura (for IM route)
• Herpes simplex infection of the eye (risk of corneal perforation)

• Immunosuppression: Increases risk of infections; latent infections (e.g., TB) may be reactivated.
• Adrenal suppression: Risk of HPA axis suppression with prolonged use or high doses; taper slowly.
• Metabolic disturbances: May cause hyperglycemia, dyslipidemia, and weight gain.
• Musculoskeletal effects: Risk of osteoporosis, myopathy, and tendon rupture with long-term use.
• Ophthalmic effects: May cause increased intraocular pressure, glaucoma, or cataracts.
• Vaccination: Avoid live vaccines during systemic corticosteroid therapy.
• Psychiatric effects: May induce mood changes, psychosis, or insomnia in some individuals.
• Intra-articular use: Risk of joint damage with repeated injections; avoid in septic joints.

Common Side Effects (dose and duration dependent):

• Gastrointestinal: Nausea, dyspepsia, increased appetite
• Neurologic: Headache, insomnia, mood swings
• Endocrine/Metabolic: Hyperglycemia, Cushingoid features, fluid retention
• Dermatologic: Skin thinning, delayed wound healing
• Musculoskeletal: Muscle weakness, osteoporosis with long-term use

Serious/Rare Adverse Effects:

• Cardiovascular: Hypertension, thromboembolism
• Neuropsychiatric: Psychosis, mania, depression
• Infectious: Reactivation of TB, opportunistic infections
• Hematologic: Leukocytosis, immunosuppression
• Ophthalmic: Glaucoma, posterior subcapsular cataracts

Onset: Systemic effects may appear within days of initiation; musculoskeletal and ophthalmic effects more likely with chronic or repeated use.

• CYP3A4 Inhibitors (e.g., Ketoconazole, Clarithromycin): May increase methylprednisolone levels.
• CYP3A4 Inducers (e.g., Rifampin, Phenytoin): May reduce effectiveness by increasing metabolism.
• NSAIDs: Increased risk of GI bleeding and ulceration.
• Diuretics: Enhanced risk of hypokalemia.
• Live Vaccines: May result in vaccine failure or disseminated infection.
• Antidiabetics: May reduce glycemic control and require dose adjustments.
• Enzyme System: Primarily metabolized by CYP3A4.

• FDA Labeling Clarification: Warnings about risk of systemic fungal infections, reactivation of latent TB, and adrenal suppression have been updated.
• Clinical Guidelines: Still recommended as a key treatment in musculoskeletal and inflammatory conditions by rheumatology and orthopedic guidelines for targeted intra-articular therapy.
• Safety Note: Emphasis on avoiding repeated intra-articular injections into the same joint due to cartilage damage risk.

• Temperature: Store at 20°C to 25°C (68°F to 77°F)
• Allowable Excursions: Between 15°C and 30°C
• Light Protection: Protect from light; store in the original carton
• Handling Instructions:
• Do not freeze
• Shake well before use; discard if clumps or discoloration appear
• Reconstitution: Not applicable (ready-to-use suspension)