Celkeran

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

Celkeran 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.

Celkeran 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 Celkeran acts to kill tumor cells are not yet completely understood.

Celkeran 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.

Celkeran
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	Celkeran
Availability	Prescription only
Generic	Chlorambucil
Chlorambucil Other Names	Ambochlorin, Chlorambucil, Chloraminophen, Clorambucilo
Related Drugs	Brukinsa, Leukeran, Venclexta, prednisone, methotrexate, dexamethasone, Keytruda, rituximab, carboplatin, pembrolizumab
Type	Tablet
Formula	C₁₄H₁₉Cl₂NO₂
Weight	Average: 304.212 Monoisotopic: 303.079284271
Protein binding	99%
Groups	Approved
Therapeutic Class	Cytotoxic Chemotherapy
Manufacturer	Celon Labs
Available Country	India,
Last Updated:	September 19, 2023 at 7:00 am

Uses

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

Celkeran 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 Celkeran 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

Celkeran 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.

Celkeran Disease Interaction

Major: infections, myelosuppressionModerate: hepatic impairment, pneumonitis/fibrosis, seizures

Half Life

1.5 hours

Elimination Route

Celkeran 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).