Alkeran

Alkeran Uses, Dosage, Side Effects, Food Interaction and all others data.

An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - melphalan, the racemic mixture - merphalan, and the dextro isomer - medphalan; toxic to bone marrow, but little vesicant action; potential carcinogen.

Alkeran is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.

Alkeran
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Alkeran
Availability	Prescription only
Generic	Melphalan
Melphalan Other Names	L-PAM, L-Phenylalanine mustard, L-Sarcolysine, Melfalano, Melphalan, Melphalanum, p-L-Sarcolysin, Phenylalanine mustard, Phenylalanine nitrogen mustard
Related Drugs	carboplatin, doxorubicin, cisplatin, paclitaxel, Revlimid, Avastin, Lynparza, Velcade, Darzalex, Pomalyst
Weight	2mg, 5mg, , 50mg
Type	Tablet, Injection, Oral, Intravenous Powder For Injection, Oral Tablet, Oral/injection
Formula	C₁₃H₁₈Cl₂N₂O₂
Weight	Average: 305.2 Monoisotopic: 304.074533244
Protein binding	Moderate to high (60 to 90%), primarily to albumin and, to a lesser extent, alpha 1-acid glycoprotein. 30% is irreversibly bound.
Groups	Approved
Therapeutic Class
Manufacturer	Glaxosmithkline
Available Country	Canada, India, United States, Netherlands, Switzerland,
Last Updated:	September 19, 2023 at 7:00 am

Uses

Alkeran is an alkylating antineoplastic agent used to treat multiple myeloma and ovarian carcinoma.

For the palliative treatment of multiple myeloma and for the palliation of non-resectable epithelial carcinoma of the ovary. Has also been used alone or as part of various chemotherapeutic regimens as an adjunct to surgery in the treatment of breast cancer, alone or in combination regimens for palliative treatment of locally recurrent or unresectable in-transit metastatic melanoma of the extremities, as well as for the treatment of amyloidosis with prednisone.

Alkeran is also used to associated treatment for these conditions: Amyloidosis, Multiple Myeloma (MM), Ovarian Epithelial Cancer, Severe Hodgkin Lymphoma, Conditioning regimens for allogeneic stem cell transplantation therapy

How Alkeran works

Alkeran attaches alkyl groups to the N-7 position of guanine and N-3 position of adenine, leading to the formation of monoadducts, and DNA fragmenting when repair enzymes attempt to correct the error. It can also cause DNA cross-linking from the N-7 position of one guanine to the N-7 position of another, preventing DNA strands from separating for synthesis or transcription. Finally, melphalan can induce a number of different mutations.

Toxicity

Vomiting, ulceration of the mouth, diarrhea, and hemorrhage of the gastrointestinal tract; The principal toxic effect is bone marrow suppression. LD₅₀=11.2 mg/kg (orally in rat)

Food Interaction

Drink plenty of fluids.
Take on an empty stomach. Food decreases absorption and decreases bioavailabilty by approximately 30%.

Alkeran Drug Interaction

Moderate: filgrastim, filgrastimMinor: levofloxacin, levofloxacin, bortezomib, bortezomibUnknown: lorazepam, lorazepam, glucose, glucose, diltiazem, diltiazem, metoprolol, metoprolol, metoprolol, metoprolol, acetaminophen, acetaminophen, zoledronic acid, zoledronic acid

Alkeran Disease Interaction

Major: infections, myelosuppressionModerate: pulmonary pneumonitis/fibrosis, renal dysfunction

Volume of Distribution

0.5 L/kg

Elimination Route

Incomplete, variable, 25-89% post oral dose

Half Life

1.5 (±0.83) hours

Elimination Route

The 24-hour urinary excretion of parent drug in these patients was 10% ± 4.5%, suggesting that renal clearance is not a major route of elimination of parent drug.