Leukeran

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

Leukeran produces its anti-cancer effects by interfering with DNA replication and damaging the DNA in a cell. The DNA damage induces cell cycle arrest and cellular apoptosis via the accumulation of cytosolic p53 and subsequent activation of Bax, an apoptosis promoter.

Leukeran alkylates and cross-links DNA during all phases of the cell cycle, inducing DNA damage via three different methods of covalent adduct generation with double-helical DNA:

Attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA.DNA damage via the formation of cross-links which prevents DNA from being separated for synthesis or transcription.Induction of mispairing of the nucleotides leading to mutations.The precise mechanisms by which Leukeran acts to kill tumor cells are not yet completely understood.

Leukeran is an antineoplastic in the class of alkylating agents that 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.

Trade Name Leukeran
Availability Prescription only
Generic Chlorambucil
Chlorambucil Other Names Ambochlorin, Chlorambucil, Chloraminophen, Clorambucilo
Related Drugs Brukinsa, Leukeran, Venclexta, prednisone, methotrexate, dexamethasone, Keytruda, rituximab, carboplatin, pembrolizumab
Weight 2mg, , 5mg
Type Tablet, Oral Tablet
Formula C14H19Cl2NO2
Weight Average: 304.212
Monoisotopic: 303.079284271
Protein binding

99%

Groups Approved
Therapeutic Class Cytotoxic Chemotherapy
Manufacturer Glaxosmithkline, Excella, Germany, Aspen Pharma Trading Limited (aptl), Glaxowellcome
Available Country India, Bangladesh, Canada, Saudi Arabia, United States, Netherlands, Portugal, Switzerland,
Last Updated: September 19, 2023 at 7:00 am
Leukeran
Leukeran

Uses

Hodgkin's disease, certain forms of non-Hodgkin's lymphoma, chronic lymphocytic leukaemia, Waldenstrom's macroglobulinaemia.

Leukeran is also used to associated treatment for these conditions: Chronic Lymphocytic Leukaemia (CLL), Hodgkins Disease (HD), Nephrotic syndrome with lesion of minimal change glomerulonephritis, Non-Hodgkin's Lymphoma (NHL), Waldenström's Macroglobulinemia (WM), Giant follicular lymphoma

How Leukeran works

Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations.

Dosage

Leukeran dosage

Hodgkin's disease: 200 mcg/kg/day for 4-8 wk.

Non-Hodgkin's lymphoma: 100-200 mcg/kg/day for 4-8 wk. Maintenance: Reduced daily dosage of intermittent courses of treatment.

Chronic lymphocytic leukaemia: Initially, 150 mcg/kg/day until the total leukocyte count falls to 10,000 microliter. Treatment may be resumed 4 wk after at a dose of 100 mcg/kg/day.

Waldenstrom's macroglobulinaemia: Starting dose of 6-12 mg daily until leucopenia occurs followed by 2-8 mg daily.

Should be taken on an empty stomach: Ensure adequate hydration. Swallow whole, do not chew/crush.

Side Effects

Bone marrow suppression, seizures in childn with nephrotic syndrome, nausea, vomiting, diarrhoea, oral ulceration. Rarely, irreversible bone marrow failure, allergic reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis, seizures, movement disorders, interstitial pulmonary fibrosis, interstitial pneumonia, hepatotoxicity, jaundice, sterile cystitis, drug fever

Precaution

Monitor FBC closely. Bone marrow suppression reversible only if withdrawn early enough. Should not be given to patients who have recently undergone radio- or chemotherapy. In lymphocytic infiltration of bone marrow or hypoplastic bone marrow, max daily dose is 0.1 mg/kg. Childn with nephrotic syndrome, patients on high pulse dosing regimens, history of seizure disorders. Renal or hepatic impairment. Ensure adequate contraceptive precautions. Pregnancy.

Food Interaction

  • Avoid echinacea. Echinacea should be used with caution, if at all, in patients receiving therapeutic immunosuppressants. Monitor for reduced efficacy of the immunosuppressant during concomitant use.
  • Drink plenty of fluids.
  • Take on an empty stomach. Co-administration with food decreases bioavailability.

Half Life

1.5 hours

Elimination Route

Leukeran is extensively metabolized in the liver primarily to phenylacetic acid mustard. The pharmacokinetic data suggests that oral chlorambucil undergoes rapid gastrointestinal absorption and plasma clearance and that it is almost completely metabolized, having extremely low urinary excretion.

Pregnancy & Breastfeeding use

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).

Contraindication

Pregnancy (1st trimester) & lactation.

Innovators Monograph

You find simplified version here Leukeran

Leukeran contains Chlorambucil see full prescribing information from innovator Leukeran Monograph, Leukeran MSDS, Leukeran FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
Share