Cladribine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Chronic lymphocytic leukaemia
Adult: 120 mcg/kg (4.8 mg/m2) daily by continuous infusion over 2 hr for 5 consecutive days of a 28-day cycle, w/ response determined every 2 cycles. Once Max response has occurred, 2 cycles of treatment are further recommended. Max: 6 cycles. Non-responders (lymphocyte reduction of <50% after 2 cycles) should not receive further therapy.

Intravenous
Hairy cell leukaemia
Adult: Single course of 90 mcg/kg (3.6 mg/m2) daily for 7 days by continuous infusion. Non-responders to initial course are unlikely to respond to additional courses.

Subcutaneous
Hairy cell leukaemia
Adult: 140 mcg/kg (5.6 mg/m2) daily for 5 consecutive days.

Subcutaneous
Chronic lymphocytic leukaemia, Non-Hodgkin's lymphoma, Waldenstrom's macroglobulinaemia
Adult: 100 mcg/kg (4 mg/m2) daily for 5 consecutive days.
Renal Impairment
Subcutaneous
Hairy cell leukaemia: Moderate to severe (CrCl ≤50 mL/min): Contraindicated.
Hepatic Impairment
Subcutaneous
Moderate to severe (Child-Pugh score >6): Contraindicated.
Hướng dẫn pha thuốc
For IV infusion, the calculated dose to a polyvinyl Cl infusion bag containing 100-500 mL of 0.9% NaCl inj.
Tương kỵ
Incompatible w/ dextrose 5%.
Chống chỉ định
For treatment of hairy cell leukaemia by SC inj: Moderate to severe renal and hepatic impairment; pregnancy and lactation.
Thận trọng
Patient w/ pre-existing haematologic or immunologic abnormalities, active infection, high tumour burden or at risk for development of hyperuricaemia. Hepatic and renal impairment. Pregnancy and lactation.
Phản ứng phụ
Myelosuppression (e.g. neutropenia, anaemia, thrombocytopenia), prolonged CD4 lymphopenia and bone-marrow hypocellularity, haemolytic anaemia; fever, chills, diaphoresis, fatigue, malaise, nausea, abdominal pain, GI disturbance, rash, pruritus, urticaria, purpura, headache, anxiety, dizziness, abnormal breath/chest sounds, cough, dyspnoea, oedema, tachycardia, hypotension, arthralgia, myalgia; reversible increase in bilirubin and hepatic transaminases; conjunctivitis; lung infiltration, interstitial lung disease, pneumonitis, pulmonary fibrosis; confusion, neuropathy, ataxia, insomnia, somnolence, peripheral sensory and motor (e.g. paralysis) neuropathies, polyneuropathy. Rarely, myelodysplastic syndrome, hepatic, renal, and cardiac failures, atrial fibrillation, hypereosinophilia, severe neurotoxicity.
Potentially Fatal: Serious infections (e.g. pneumonia, septicaemia, septic shock). Rarely, tumour lysis syndrome.
IV/Parenteral/SC: D
Thông tin tư vấn bệnh nhân
May impair ability to drive or operate machinery.
Monitoring Parameters
Perform peripheral blood counts regularly during the 1st 4-8 wk post-treatment. Closely monitor for fever, infection, and neurotoxicity. Monitor cardiac, hepatic, and renal function regularly.
Quá liều
Symptoms: Neurotoxicity (e.g. irreversible paraparesis/quadraparesis), acute nephrotoxicity, severe myelosuppession (e.g. neutropenia, anaemia, thrombocytopenia, leukopenia, agranulocytosis), nausea, vomiting, diarrhoea, Guillain Barre and Brown Sequard syndromes. Management: Supportive treatment.
Tương tác
Reduced effect w/ antiviral agents (e.g. lamivudine). May enhance immunosuppression w/ other myelosuppressive agents. May increase risk of infection w/ live attenuated vaccines. May cause cross-resistance w/ other nucleoside analogues (e.g. fludarabine).
Tác dụng
Description: Cladribine is a chlorinated purine nucleoside analogue that is cell-cycle nonspecific. It inhibits ribonucleotide reductase causing an imbalance in triphosphorylated deoxynucleotide (dNTP). This leads to breakage of DNA strands and inhibition of DNA synthesis and repair, particularly of resting and proliferating lymphocytes and monocytes. Additionally, it also results in nicotinamide adenine dinucleotide (NAD) and adenosine triphosphate (ATP) depletion.
Pharmacokinetics:
Distribution: Extensively distributed and penetrates into the CNS. Volume of distribution: Approx 9 L/kg. Plasma protein binding: Approx 20%.
Metabolism: Phosphorylated w/in cells into 2-chlorodeoxyadenosine-5’-triphosphate (CdATP) by deoxycytidine kinase.
Excretion: Via urine (18%). Elimination half-life: 5.4 hr.
Đặc tính

Chemical Structure Image
Cladribine

Source: National Center for Biotechnology Information. PubChem Database. Cladribine, CID=20279, https://pubchem.ncbi.nlm.nih.gov/compound/Cladribine (accessed on Jan. 21, 2020)

Bảo quản
Store between 2-8°C. Protect from light.
Phân loại MIMS
Phân loại ATC
L01BB04 - cladribine ; Belongs to the class of antimetabolites, purine analogues. Used in the treatment of cancer.
References
Anon. Cladribine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 29/07/2016.

Buckingham R (ed). Cladribine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 29/07/2016.

Cladribine Injection (Fresenius Kabi USA, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 29/07/2016.

Joint Formulary Committee. Cladribine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 29/07/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Cladribine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 29/07/2016.

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