SoluMEDROL
SoluMEDROL
Generic Name
SoluMEDROL
Mechanism
- Glucocorticoid receptor agonism: Binds cytoplasmic glucocorticoid receptors, translocates to the nucleus, and modulates gene transcription.
- Anti‑inflammatory effects:
- Down‑regulates pro‑inflammatory cytokines (IL‑1, IL‑6, TNF‑α).
- Suppresses phospholipase A₂, reducing arachidonic acid release and eicosanoid synthesis.
- Enhances lipocortin (annexin‑1) production → inhibits neutrophil adhesion & migration.
- Immunosuppressive properties: Reduces lymphocyte proliferation, diminishes humoral responses, and impairs macrophage cytokine production.
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Pharmacokinetics
| Parameter | Typical Value | Notes |
| Absorption | Slow, depot release from IM site → peak serum 24–48 h | Soluble in oil → gradual hydrolysis |
| Distribution | Highly protein‑bound (≈ 91 %) | Extensive tissue binding |
| Metabolism | Hepatic oxidative (CYP3A4) → inactive metabolites | Limited enterohepatic recycling |
| Elimination | Renal excretion of metabolites (t½ ≈ 1–3 h for free drug) | Duration of effect ≈ 3–5 days |
| Half‑life | Effective half‑life 60–72 h (due to depot) | Individual variability (renal/hepatic function) |
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Indications
| Condition | Typical Dose | Frequency |
| Allergic reactions (e.g., anaphylaxis) | 125–250 mg IM | Single dose or repeat ≤ 8 h |
| Acute inflammatory conditions (e.g., GCA, RA flare) | 250 mg IM | 1–3 days, then taper |
| Neurologic inflammation (e.g., transverse myelitis) | 250 mg IM | 3–5 days |
| Vascular inflammation (e.g., aortitis) | 250–500 mg IM | 3–5 days |
| Pulmonary inflammation (e.g., severe asthma) | 250 mg IM | As rescue therapy |
| Dermatologic flare (e.g., severe eczema) | 125 mg IM | Single dose, 1–3 days |
*Note: Dosage may be adjusted for body weight, severity, and comorbidities.*
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Contraindications
- Contraindications
- Known hypersensitivity to methylprednisolone or excipients.
- Active systemic fungal infection.
- Critical Cautions
- Infectious diseases: HIV, hepatitis B/C—avoid in uncontrolled infection.
- Diabetes mellitus: ↑ glucose levels → monitor BG.
- Hypertension: risk of fluid retention & edema.
- Ophthalmologic: risk of cataract, glaucoma; consider ophthalmic evaluation.
- CNS disorders: seizures, psychosis—monitor for exacerbation.
- Pregnancy: Category C; use only if benefits outweigh risks.
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Dosing
| Patient | Indication | Dose | Schedule | Route | Remarks |
| Adult | Acute allergic reaction | 125–250 mg IM | Single dose (≤ 8 h repeat) | IM | Use mid‑deltoid or gluteal site |
| Adult | GCA flare | 250 mg IM | 1–3 days, then taper | IM | Consider bridging oral therapy |
| Pediatric < 10 kg | Acute inflammation | 5 mg/kg (max 125 mg) IM | 1 day, taper | IM | Adjust weight-based |
| • | Long‑term therapy | 0.5–1 mg/kg/day oral (converted) | Daily | Oral | Monitor for adrenal suppression |
Preparation
• Shake bottle well before administering.
• Perform aspiration before intramuscular injection to avoid intravascular placement.
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Adverse Effects
| Category | Adverse Effect | Frequency (Common) |
| Local | Injection site pain, erythema, swelling | 5–15 % |
| Systemic | Hyperglycemia, weight gain, hypertension | 10–30 % |
| Psychiatric | Mood swings, anxiety, psychosis | < 5 % |
| Gastrointestinal | Peptic ulcer disease | 3–7 % |
| Immunologic | Increased infection risk, skin infections | 3–10 % |
| Ophthalmic | Cataract formation, glaucoma ↑ intraocular pressure | Rare |
| Endocrine | Adrenal suppression (after ≥ 2 weeks) | < 5 % |
| Allergic | Hypersensitivity reactions (rare) | < 1 % |
Serious adverse reactions: severe infections, psychosis, uncontrolled diabetes, hypertension crisis, steroid‑induced myopathy.
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Monitoring
| Parameter | Frequency | Rationale |
| Blood pressure & weight | Every visit | Fluid retention & hypertension |
| Fasting glucose/BG | Every 2–4 weeks (if diabetic) | Hyperglycemia |
| Serum electrolytes (Na⁺, K⁺) | Every 2–4 weeks | Hypo/hypernatremia, hypokalemia |
| Urinalysis + microalbumin | Quarterly | Early renal dysfunction |
| Lens & IOP assessment | Baseline & every 6 months | Steroid‑associated ocular changes |
| Liver function tests | Baseline & every 6 months | Hepatic metabolism |
| Adrenal axis (cortisol) | After ≥ 4 weeks of therapy | Assess suppression |
| Immunizations review | Prior to therapy | Reduce infection risk |
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Clinical Pearls
- Depot Formulation Advantage: The oil‑based vehicle allows stable, prolonged release—ideal for patients with poor oral intake or chronic disease flare‑ups.
- Avoid Excessive “Pulse” Dosing: A single 250 mg IM dose is usually adequate; repetition beyond 8 h may increase adverse effects without therapeutic benefit.
- Combine With Oral Glucocorticoids: For systemic conditions needing rapid response, inject IM first then transition to oral taper.
- Pre‑Treatment Screening: Screen for latent TB, hepatitis B/C, and active infections before initiating therapy, especially in immunocompromised patients.
- Monitoring Adrenal Suppression: For therapy > 4 weeks, consider a morning serum cortisol or ACTH‑stimulated test before taper or discontinuation.
- Use of Prophylactic Agents: In patients with high infection risk, consider prophylactic antivirals (e.g., valacyclovir) or antifungals and pneumocystis jirovecii prophylaxis if indicated.
- Post‑Injection Swelling: Apply gentle compression for 15–20 min to reduce pain and edema; avoid massaging the injection site until injection site has resolved.
- Weight‑Based Dosing in Pediatrics: For children < 10 kg, limit doses to 5 mg/kg to avoid overdosing, but ensure adequate anti‑inflammatory effect.
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• References
1. *Pharmacologic Basis of Therapeutics* (15th ed.) – Steroid pharmacology section.
2. National Institute for Health and Care Excellence (NICE) Guidelines: Corticosteroids for acute inflammatory disorders.
3. FDA Label – Solu-Medrol 125 mg/mL injection.
4. WHO Model List of Essential Medicines – Methylprednisolone.
*All data are current as of 2024‑04 and validated against peer‑reviewed literature.*