Chlorambucil


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Chronic lymphocytic leukaemia
Adult: Initially, 0.15 mg/kg daily until the total leucocyte count falls to 10,000 cells/mm3. Daily dose should not exceed 0.1 mg/kg if bone marrow presents lymphocytic infiltration or is hypoplastic. Maintenance: 0.03-0.1 mg/kg daily (once remission is established). Alternatively, initiate at 0.4 mg/kg as a single dose, then increase by 0.1 mg/kg at each 2- or 4-week dose interval until lymphocytosis is controlled or toxicity occurs. Dosing recommendations may vary among countries and individual products (refer to detailed product or local treatment guidelines).
Elderly: Initiate at the lower end of the dosing range.

Oral
Non-Hodgkin's lymphoma
Adult: As a single agent: Initially, 0.1-0.2 mg/kg daily for 4-8 weeks. Daily dose should not exceed 0.1 mg/kg if bone marrow presents lymphocytic infiltration or is hypoplastic. Maintenance: 0.03-0.1 mg/kg daily (once remission is established). Dosing recommendations may vary among countries and individual products (refer to detailed product or local treatment guidelines).
Elderly: Initiate at the lower end of the dosing range.

Oral
Hodgkin's disease
Adult: As a single agent in the palliative treatment of advanced disease: 0.2 mg/kg daily for 4-8 weeks. Daily dose should not exceed 0.1 mg/kg if bone marrow presents lymphocytic infiltration or is hypoplastic. Maintenance: 0.03-0.1 mg/kg daily (once remission is established). Dosing recommendations may vary among countries and individual products (refer to detailed product or local treatment guidelines).
Elderly: Initiate at the lower end of the dosing range.

Oral
Waldenstrom's macroglobulinaemia
Adult: Initially, 6-12 mg daily until leucopenia occurs. Maintenance: 2-8 mg daily indefinitely. Treatment and dosing recommendations may vary among countries and individual products (refer to detailed product or local treatment guidelines).
Elderly: Initiate at the lower end of the dosing range.
Suy gan
Severe: Dosage reduction may be required.
Cách dùng
Should be taken on an empty stomach. Ensure adequate hydration. Swallow whole, do not chew/crush.
Chống chỉ định
Lactation.
Thận trọng
Patient with history of seizure disorder or head trauma; nephrotic syndrome; receiving high pulse dosing regimens. Patients who have recently undergone radiotherapy or received other cytotoxic agents. Patients who may undergo autologous stem cell transplantation should not receive long-term chlorambucil therapy. Avoid the administration of live vaccines. Severe hepatic impairment. Elderly. Pregnancy.
Tác dụng không mong muốn
Significant: Severe bone marrow suppression; infertility, seizures; secondary malignancy (e.g. acute myelocytic leukaemia), particularly after long-term treatment. Rarely, severe skin reactions (e.g. erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis).
Blood and lymphatic system disorders: Leucopenia, neutropenia, thrombocytopenia, pancytopenia, anaemia.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, mouth ulceration.
Chỉ số theo dõi
Monitor LFTs and CBC with differential. Assess for signs of skin reactions, infections, bruising or bleeding.
Quá liều
Symptoms: Agitated behaviour, ataxia, multiple grand mal seizures and reversible pancytopenia. Management: Supportive treatment with appropriate blood transfusion if needed.
Tương tác
Increased cytotoxicity with purine nucleoside analogues (e.g. cladribine, fludarabine, pentostatin). Increased risk of vaccine-associated infection with live vaccines.
Tương tác với thức ăn
Decreased absorption with food.
Tác dụng
Description:
Mechanism of Action: Chlorambucil, an aromatic nitrogen mustard derivative, is a bifunctional alkylating agent. It interferes with DNA replication and RNA transcription by alkylation and cross-linking the DNA strands, thus inducing cellular apoptosis via the accumulation of cytosolic p53 and subsequent activation of an apoptosis promoter (Bax).
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract. Decreased absorption with food. Time to peak plasma concentration: Within 1 hour.
Distribution: Volume of distribution: Approx 0.31 L/kg. Plasma protein binding: Approx 99%, mainly to albumin.
Metabolism: Extensively metabolised in the liver via monodichloroethylation and β-oxidation, mainly into phenylacetic acid mustard (major metabolite). Chlorambucil and phenylacetic acid mustard undergo oxidative degradation to monohydroxy and dihydroxy derivatives.
Excretion: Via urine (approx 20-60%, mainly as inactive metabolites, <1% as unchanged drug or phenylacetic acid mustard). Terminal elimination half-life: Approx 1.5 hours.
Đặc tính

Chemical Structure Image
Chlorambucil

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2708, Chlorambucil. https://pubchem.ncbi.nlm.nih.gov/compound/Chlorambucil. Accessed Jan. 25, 2024.

Bảo quản
Store between 2-8°C. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
Phân loại MIMS
Hóa trị gây độc tế bào
Phân loại ATC
L01AA02 - chlorambucil ; Belongs to the class of alkylating agents, nitrogen mustard analogues. Used in the treatment of cancer.
Tài liệu tham khảo
Anon. Chlorambucil. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 14/09/2023.

Anon. Chlorambucil. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/09/2023.

Buckingham R (ed). Chlorambucil. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/09/2023.

Chlorambucil 2 mg Tablets (Aspen Pharma Trading Limited). MHRA. https://products.mhra.gov.uk. Accessed 14/09/2023.

Joint Formulary Committee. Chlorambucil. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/09/2023.

Leukeran Tablet, Film Coated (Waylis Therapeutics LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 14/09/2023.

Leukeran Tablets 2 mg (Aspen Medical Products Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 14/09/2023.

Pharmacy Retailing (NZ) Ltd t/a Healthcare Logistics. Leukeran Tablet data sheet April 2019. Medsafe. http://www.medsafe.govt.nz. Accessed 14/09/2023.

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