Melphalan

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Dosage 4 Pharmacokinetics 5 Adverse-effects 6 Drug-interactions 7 Test-interactions 8 Mechanism-of-action 9 More General Terms 10 Internet Database 11 References

Introduction

• Tradename: Alkeran.

Indications

• palliative treatment of multiple myeloma
• palliative treatment of non-resectable epithelial ovarian carcinoma
• neuroblastoma
• rhabdomyosarcoma
• thyroid carcinoma
• testicular carcinoma
• breast cancer

Dosage

• 0.25 mg/kg/day PO for 4 days every 6 weeks
• maximum: 6 mg/day

• Tabs: 2 mg (preferred route of administration is oral)
• Powder for injection: 50 mg (10 mL)
• Do:

• protect from light
• do not refrigerate reconstituted solution
• complete administration within 1 hour of reconstitution

Pharmacokinetics

• erratic oral absorption (25-90%)
• 90% protein bound
• metabolized spontaneously in blood
• cleared mostly by non-renal routes
• 1/2life 1.5-4 hours
  

• elimination via plasma
• 1/2life = 1.5-4 hours

Adverse-effects

• common (> 10%)

• myelosuppression

• onset 7 days
• nadir 8-10 days & 27-32 days
• recovery 6-7 weeks

• secondary malignancies
• SIADH
• pulmonary fibrosis
• interstitial pneumonitis
• hemolytic anemia
• pruritis & rash
• sterility (permanent) & amenorrhea
• hypersensitivity
• alopecia

• less common (1-10%)

• vasculitis, alopecia, rash, pruritis, leukopenia, thrombocytopenia, anemia, agranulocytosis, hemolytic anemia, vesiculation of skin, bladder irritation, hemorrhagic cystitis, pulmonary fibrosis, nausea/vomiting, stomatitis, diarrhea

• other [2]:

• mild to moderate nausea
• anaphylaxis
  
• drug adverse effects of alkylating agents

Drug-interactions

• cyclosporine increases the risk of nephrotoxicity
• cimetidine decreases oral absorption of melphalan

Test-interactions

• false positive Coomb's test (direct)

Mechanism-of-action

• alkylating agent
• interferes with DNA & RNA synthesis

More General Terms

• alkylating agent
• antineoplastic agent (chemotherapeutic agent)

Internet Database

PubChem: 4053
PubChem: 460612

References

1. Kaiser Permanente Northern California Regional Drug Formulary, 1998
2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
3. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529

melphalan (Alkeran, L-PAM, L-sarcolysin phenylalanine mustard)