Lomustine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Brain tumour
Adult: As palliative treatment of primary and metastatic cases in combination with appropriate surgical and/or radiotherapeutic procedures or as part of multiple chemotherapeutic regimens: Recommended dose: 120-130 mg/m2 as a single dose once every 6-8 weeks, when given as a single agent. Patients with compromised bone marrow function: 100 mg/m2 as a single dose once every 6 weeks. Dose reduction may be necessary when given as part of combination chemotherapy regimens. Dosing adjustment or discontinuation may be required according to individual platelet and leukocyte counts (refer to detailed product guideline).
Child: Same as adult dose. Dosing adjustment or discontinuation may be required according to individual platelet and leukocyte counts (refer to detailed product guideline).

Oral
Metastatic malignant melanoma, Lung cancer
Adult: As palliative treatment in combination with appropriate surgical and/or radiotherapeutic procedures or as part of multiple chemotherapeutic regimens: Recommended dose: 120-130 mg/m2 as a single dose once every 6-8 weeks, when given as a single agent. Patients with compromised bone marrow function: 100 mg/m2 as a single dose once every 6 weeks. Dose reduction may be necessary when given as part of combination chemotherapy regimens. Dosing adjustment or discontinuation may be required according to individual platelet and leukocyte counts (refer to detailed product guideline).
Child: Same as adult dose. Dosing adjustment or discontinuation may be required according to individual platelet and leukocyte counts (refer to detailed product guideline).

Oral
Hodgkin's lymphoma
Adult: In combination with other chemotherapy agents following disease progression with initial chemotherapy: Recommended dose: 120-130 mg/m2 as a single dose once every 6-8 weeks, when given as a single agent. Patients with compromised bone marrow function: 100 mg/m2 as a single dose once every 6 weeks. Dose reduction may be necessary when given as part of combination chemotherapy regimens. Dosing adjustment or discontinuation may be required according to individual platelet and leukocyte counts (refer to detailed product guideline).
Child: Same as adult dose. Dosing adjustment or discontinuation may be required according to individual platelet and leukocyte counts (refer to detailed product guideline).
Renal Impairment
Brain tumour:
Dose reduction may be required.
Cách dùng
Should be taken on an empty stomach. May be taken at bedtime to reduce occurrence of nausea.
Chống chỉ định
Previous failure of tumour response to other nitrosoureas; severe bone marrow depression, coeliac disease or wheat allergy. Severe renal impairment. Pregnancy and lactation. Concomitant use with yellow fever vaccine or other live vaccines in immunosuppressed patients.
Thận trọng
Patient with baseline <70% of carbon monoxide diffusing capacity or predicted forced vital capacity (FVC). Renal and hepatic impairment.
Phản ứng phụ
Significant: Gastrointestinal toxicity (e.g. moderate emesis, stomatitis), hepatotoxicity (e.g. increased transaminases, alkaline phosphatase, and bilirubin), pulmonary toxicity (e.g. infiltrates, fibrosis), nephrotoxicity (e.g. progressive renal failure with decreased kidney size); secondary malignancies, including leukaemia and myelodysplasia (prolonged use).
Blood and lymphatic system disorders: Anaemia.
Eye disorders: Blindness, optic atrophy, visual disturbances.
Gastrointestinal disorders: Nausea, diarrhoea.
General disorders and administration site conditions:
Ataxia, lethargy.
Metabolism and nutrition disorders: Anorexia.
Nervous system disorders: Abnormal coordination.
Psychiatric disorders: Disorientation, dysarthria, confusion.
Renal and urinary disorders: Azotaemia.
Skin and subcutaneous tissue disorders: Alopecia.
Potentially Fatal: Delayed bone marrow suppression.
Monitoring Parameters
Monitor CBC with differential and platelet count every week for at least 6 weeks after a dose; liver, renal, and pulmonary function tests at baseline and periodically thereafter. Assess for signs and symptoms of abnormal bleeding and infection.
Quá liều
Symptoms: Bone marrow or haematological toxicity, nausea, vomiting, diarrhoea, abdominal pain, anorexia, cough, shortness of breath, dizziness, lethargy, and abnormal hepatic function. Management: Symptomatic and supportive treatment. May perform gastric lavage immediately after an overdose. Administer appropriate blood product replacement as clinically required.
Tương tác
May potentiate bone marrow toxicity with theophylline and cimetidine. May reduce the anti-tumour effects with phenobarbital.
Potentially Fatal: Increased risk of systemic vaccinal disease with live vaccines (e.g. yellow fever vaccine).
Tác dụng
Description: Lomustine, a lipid soluble nitrosourea, blocks the deoxyribonucleic acid (DNA), ribonucleic acid (RNA), and protein synthesis via alkylation and carbamylation of DNA and RNA.
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 3 hours.
Distribution: Crosses the blood-brain barrier; highly concentrated in the CNS. Enters breast milk.
Metabolism: Rapidly metabolised in the liver to active metabolites.
Excretion: Mainly via urine (approx 50% as metabolites). Elimination half-life: 16-48 hours (as metabolites).
Đặc tính

Chemical Structure Image
Lomustine_01

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3950, Lomustine. https://pubchem.ncbi.nlm.nih.gov/compound/Lomustine. Accessed July 29, 2020.

Bảo quản
Store at 25°C. Protect from light and moisture. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
Phân loại MIMS
Phân loại ATC
L01AD02 - lomustine ; Belongs to the class of alkylating agents, nitrosoureas. Used in the treatment of cancer.
References
Anon. Lomustine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/06/2020.

Buckingham R (ed). Lomustine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/06/2020.

Gleostine Capsule, Gelatin Coated (NextSource Biotechnology, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 02/06/2020.

Joint Formulary Committee. Lomustine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/06/2020.

Lomustine “Medac” 40 mg Capsule (Medac). MHRA. https://products.mhra.gov.uk/. Accessed 02/06/2020.

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