logo image

Melphalan information from DrugsUpdate  

See Available Brands of Melphalan in India

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

Melphalan, also known as L-phenylalanine mustard, phenylalanine mustard, L-PAM, or L-sarcolysin, is a phenylalanine derivative of nitrogen mustard. Melphalan is a bifunctional alkylating agent that is active against selected human neoplastic diseases.

Pharmacodynamics

Pharmacokinetics

Melphalan, a mechlorethamine derivative, is an alkylating antineoplastic agent. It forms carbonium ions, resulting in DNA and RNA synthesis inhibition. It cross-links DNA strands and acts on both resting and rapidly dividing tumour cells.

Absorption

Variable absorption from the GI tract; absorption reduced by food (oral).

Distribution

Rapid throughout body water. Protein-binding: 50-60%, mainly to albumin.

Metabolism
Inactivated by hydrolysis.

Excretion
Via urine (10%, as unchanged drug); 30-150 minutes (terminal half-life).

Melphalan Indications / Melphalan Uses

Information Not Available

Melphalan Adverse Reactions / Melphalan Side Effects

Diarrhoea, stomatitis, vomiting; haemolytic anaemia, vasculitis, pulmonary fibrosis, hepatic disorders, suppression of ovarian function in premenopausal women, temporary or permanent sterility in male patients. Allergic reactions.

Potentially Fatal: Bone marrow suppression. Secondary malignancy, cardiac arrest. Anaphylaxis.

Precautions

Warnings
Administer under supervision of a qualified health care provider experienced in the use of cancer chemotherapy. Severe bone marrow suppression with resulting infection or bleeding may occur. Hypersensitivity reactions, including anaphylaxis, have occurred in 2% of patients who received IV melphalan. Melphalan is leukemogenic in humans. This has been demonstrated in vitro and in vivo; therefore, consider melphalan to be potentially mutagenic.

Monitor
Monitor platelet count, hemoglobin, whole blood cell count, and differential at the start of therapy and prior to each subsequent course of therapy. Obtain at least 1 CBC determination prior to each treatment course. Observe patients closely for consequences of bone marrow suppression, including severe infections, bleeding, and symptomatic anemia.

Overdosage
Symptoms: Hypocalcaemia, hyponatraemia, pulmonary fibrosis, severe nausea and vomiting, diarrhoea, GI haemorrhage, mucositis, stomatitis, bone marrow suppression. Deaths have been reported (IV). Management: Symptomatic and supportive. Closely monitor haematologic function for 3-6 wk. Growth factor support, transfusions and antibiotics may be considered. Not removed by haemodialysis.

Special Precautions

Renal impairment. Lactation. Prior bone marrow suppression, prior chemotherapy or irradiation. May mask signs of infection e.g. fever and increased WBC. Elderly.

Other Drug Interactions

Information Not Available

Other Interactions

Food Interaction
Food significantly reduces oral absorption. Avoid excessive alcohol intake.

Dosage

Oral
Multiple myeloma
Adult: 150 mcg/kg daily in divided doses for 4-7 days or 250 mcg/kg daily for 4 days or 6 mg daily for 2-3 weeks. Usually combined with corticosteroids. Follow treatment course by a rest period of up to 6 weeks to allow haematologic recovery. Then repeat the course or start maintenance treatment with 1-3 mg or up to 50 mcg/kg daily. For optimal effect, adjust therapy to produce moderate leucopenia (WBC counts of 3,000-3,500 cells/mm3).
Renal impairment: Dose reduction may be required.

Oral
Breast cancer
Adult: 150 mcg/kg daily or 6 mg/m2 daily for 5 days, repeated every 6 weeks.
Renal impairment: Dose reduction may be required.

Oral

Ovarian carcinoma
Adult: 200 mcg/kg daily for 5 days every 4-8 weeks.
Renal impairment: Dose reduction may be required.

Oral
Polycythemia vera
Adult: 6-10 mg daily for 5-7 days; 2-4 mg daily for remission induction. Maintenance dose: 2-6 mg weekly.
Renal impairment: Dose reduction may be required.

Intravenous

Ovarian adenocarcinoma
Adult: 1 mg/kg as a single dose repeated in 4 weeks if platelet and neutrophil counts permit. May be infused in sodium chloride 0.9% or injection
into the tubing of a fast-running drip.
Renal impairment: Reduce dose by 50%.

Intravenous
Multiple myeloma
Adult: 400 mcg/kg or 16 mg/m2 infused over 15-20 minutes. First 4 doses may be given every 2 weeks and further doses given every 4 weeks depending on toxicity. High-dose regimen: 100-200 mg/m2 followed by autologous stem cell rescue which is essential if doses exceed 140 mg/m2, to be given through a central venous catheter.
Renal impairment: Conventional dose: Reduce dose by 50%. High-dose regimen: Not recommended in moderate to severe impairment.

Intravenous
Neuroblastoma
Adult: High-dose regimen: 100-240 mg/m2 followed by autologous stem cell rescue which is essential if doses are >140 mg/m2. Give through a central venous catheter.
Renal impairment: High-dose regimen: Not recommended in moderate to severe impairment.

Intra-arterial
Melanoma
Adult: Upper extremity perfusions: 0.6-1 mg/kg. Lower extremity perfusions: 0.8-1.5 mg/kg (in melanoma) or 1-1.4 mg/kg (in sarcoma).
Renal impairment: Reduce dose by 50%.

Intra-arterial

Soft tissue sarcoma
Adult: Upper extremity perfusions: 0.6-1 mg/kg. Lower extremity perfusions: 0.8-1.5 mg/kg (in melanoma) or 1-1.4 mg/kg (in sarcoma).
Renal impairment: Reduce dose by 50%.

Reconstitution

Injection must be prepared fresh. Keep to a minimum (<60 minutes) the time between reconstitution/dilution and admin. Dissolve powder initially with diluent 10 ml to a concentration of 5 mg/ml. Shake vigorously to dissolve. Immediately dilute in 250-500 ml normal saline to a concentration of 0.1-0.45 mg/ml.

Incompatibility

Dextrose 5% in water, Lactated Ringer's; variable stability in normal saline.

Food(before/after)

Should be taken on an empty stomach. (Take on an empty stomach 1 hour before or 2 hours after meals.)

List of Contraindications

Melphalan and Pregnancy

Contraindicated in pregnancy

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Melphalan and Lactation

Caution when used during lactation

Melphalan and Children

Safety and efficacy in children have not been established.

Melphalan and Geriatic

Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Melphalan and Other Contraindications

Hypersensitivity. Severe bone marrow suppression. Pregnancy.

Storage

Intravenous
Store at room temperature (15-30°C).
Protect from light.

Oral

Store in a refrigerator at 2-8°C (36-46°F).
Protect from light.

Lab interference

Intravenous
Store at room temperature (15-30°C).
Protect from light.

Oral

Store in a refrigerator at 2-8°C (36-46°F).
Protect from light.

Melphalan brands in India:

Alkacel Alkeran Alphalan

© 2011-2020 DrugsUpdate.com from UPilot INC. Disclaimer | Site Map

Feedback
  • Companies that own platforms will own the market
  • Trusted and recognized by all Doctors
  • Access to Millions of Visitors instantly.
  • Companies that own platforms will own the market
  • Trusted and recognized by all Doctors
  • Access to Millions of Visitors instantly.