Home Drug Guide Belumosudil Mesylate

Drug Guide

Generic Name

Belumosudil Mesylate

Brand Names Rezurock

Classification

Therapeutic: Immunosuppressant

Pharmacological: ROCK2 inhibitor

FDA Approved Indications

  • Prophylaxis of graft-versus-host disease (GVHD) in adult and pediatric patients 12 years and older.

Mechanism of Action

Belumosudil inhibits Rho-associated coiled-coil containing protein kinase 2 (ROCK2), leading to modulation of immune responses and reduction of inflammatory pathways involved in GVHD.

Dosage and Administration

Adult: Starting dose of 200 mg once daily, adjustable based on response and tolerability.

Pediatric: Dose adjustments based on weight and therapeutic response; consult specific pediatric dosing guidelines.

Geriatric: No specific dose adjustment required, but tol erance should be monitored carefully.

Renal Impairment: No specific adjustment recommended; however, renal function should be monitored regularly.

Hepatic Impairment: No specific adjustment recommended.

Pharmacokinetics

Absorption: Orally administered; peak plasma concentration typically reached within 4-6 hours.

Distribution: High protein binding (~98%), primarily to albumin.

Metabolism: Primarily metabolized by CYP3A4 enzyme; minor pathways include CYP2C19.

Excretion: Metabolites are excreted mainly in feces; minor urinary excretion.

Half Life: Approximately 4 days (96 hours).

Contraindications

  • Hypersensitivity to belumosudil or any component of the formulation.

Precautions

  • Use with caution in patients with hepatic impairment.
  • Potential for increased bleeding risk; monitor for signs of bleeding.
  • Increased susceptibility to infections; monitor closely.
  • Pregnancy Category: C; use only if clearly needed.

Adverse Reactions - Common

  • Nausea (Common)
  • Diarrhea (Common)
  • Fatigue (Common)
  • Elevation of liver enzymes (Common)

Adverse Reactions - Serious

  • Infections (e.g., pneumonia, herpes zoster) (Serious)
  • Hepatotoxicity (Serious)
  • Bleeding events (Serious)

Drug-Drug Interactions

  • CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase belumosudil levels.
  • CYP3A4 inducers (e.g., rifampin) may decrease levels.

Drug-Food Interactions

  • No specific food interactions identified.

Drug-Herb Interactions

  • St. John's Wort may reduce efficacy by inducing CYP3A4.

Nursing Implications

Assessment: Monitor liver function tests, complete blood counts, and signs of infection or bleeding.

Diagnoses:

  • Risk for bleeding related to potential thrombocytopenia.
  • Impaired immunity related to immunosuppressive therapy.

Implementation: Administer orally once daily; monitor response and tolerance; educate patient on signs of infection and bleeding.

Evaluation: Assess for reduction in GVHD symptoms and monitor for adverse effects.

Patient/Family Teaching

  • Take the medication exactly as prescribed, at the same time each day.
  • Report signs of infection, unusual bleeding, or bruising promptly.
  • Avoid grapefruit and grapefruit juice, which may increase drug levels.
  • Attend regular follow-up appointments for lab tests and assessment.

Special Considerations

Black Box Warnings:

  • Serious infections and subsequent complications including death.
  • Hepatotoxicity.

Genetic Factors: None specifically identified.

Lab Test Interference: Elevations in liver function tests; may require dose adjustments.

Overdose Management

Signs/Symptoms: Potential toxicity includes severe hepatotoxicity, bleeding, or infections.

Treatment: Supportive care, discontinue drug, and monitor vital signs and laboratory parameters; no specific antidote.

Storage and Handling

Storage: Store at room temperature away from moisture and light.

Stability: Stable for the duration of the shelf life indicated on the label.

🛡️ 5 Critical Medication Safety Tips for Nurses

1

Triple-Check High-Risk Medications

Always have another nurse verify insulin, heparin, warfarin, and chemotherapy drugs. These "high-alert" medications cause the most serious errors. Check concentration, dose calculation, and pump settings twice.

2

Know Look-Alike, Sound-Alike Drugs

Common mix-ups: hydromorphone/morphine, Celebrex/Celexa, Zyprexa/Zyrtec. Always use BOTH generic and brand names, read labels twice, and use barcode scanning when available. One wrong letter can be fatal.

3

Assess Before AND After Giving Meds

Check vitals before cardiac meds, pain levels before analgesics, and blood glucose before insulin. Always reassess within 30 minutes to evaluate effectiveness and watch for adverse reactions.

4

Watch for Drug Interactions

Common dangerous combinations: warfarin + aspirin (bleeding), ACE inhibitors + potassium (hyperkalemia), digoxin + diuretics (toxicity). Always check drug interactions before administering new medications.

5

Educate Your Patients

Teach patients medication names, purposes, major side effects, and what to report. Informed patients catch errors and improve compliance. Always encourage questions - an educated patient is a safer patient.

⚡ Remember: When in doubt, don't give it out! It's always safer to double-check than regret later.

⚠️ Medical Disclaimer

This drug guide is for educational purposes only and is NOT intended for clinical use. Always consult current prescribing information, healthcare providers, and institutional protocols before administering any medication. Do not use this information for patient care decisions.