Carmustine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intracavitary
Malignant glioma, Recurrent glioblastoma multiforme
Adult: Implantation of wafers containing 7.7 mg/wafer into the cavity left by removal of the tumour. Max: 8 wafers.

Intravenous
Brain tumour, Hodgkin's disease, Multiple myeloma, Non-Hodgkin's lymphoma
Adult: As a single dose of 150-200 mg/m2 or divided into doses of 75-100 mg/m2 given on 2 successive days. Doses are given via IV infusion over 1-2 hours. Doses may be repeated every 6 weeks provided that blood counts have returned to acceptable levels. Adjust subsequent doses based on haematological toxicity. Used in combination with prednisolone for the treatment of multiple myeloma. Used as secondary therapy (with other approved drugs) in the treatment of Hodgkin's disease and non-Hodgkin's lymphomas.
Hướng dẫn pha thuốc
Initially, reconstitute 100 mg of carmustine with 3 mL of supplied diluent, then further dilute with 27 mL of sterile water for injection, resulting to a 3.3 mg of carmustine in 10% alcohol. Further dilute for infusion with 500 mL 0.9% Na chloride for injection or 5% glucose for injection.
Chống chỉ định
Hypersensitivity. Pregnancy and Lactation.
Thận trọng
Patient with bone marrow suppression (e.g. thrombocytopenia, leucopenia), reduced lung function or pre-existing lung disease. Children.
Phản ứng phụ
Significant: Bone marrow suppression (e.g. thrombocytopenia, leucopenia), hepatotoxicity (reversible increased serum transaminase, alkaline phosphatase and bilirubin), renal failure, progressive azotemia; intracranial hypertension, wound healing impairment (implant); secondary malignancies (long-term IV use).
Cardiac disorders: Hypotension, tachycardia, chest pain.
Eye disorders: Conjunctival flushing, blurred vision, retinal haemorrhage.
Gastrointestinal disorders: Nausea, vomiting, anorexia, constipation, diarrhea, stomatitis.
Nervous system disorders: Dizziness, somnolence, hemiplegia, convulsion, brain oedema.
Psychiatric disorders: Depression, anxiety, abnormal thinking, hallucinations.
Reproductive system and breast disorders: Gynecomastia.
Respiratory, thoracic and mediastinal disorders: Pulmonary embolism.
Skin and subcutaneous tissue disorders: Hyperpigmentation (in skin exposure), rash, alopecia.
Vascular disorders: Phlebitis.
Potentially Fatal: Pulmonary fibrosis, opportunistic infections.
IV/Parenteral/Topical: D
MonitoringParameters
Monitor CBC with differential and platelet count weekly for at least 6 weeks after a dose; pulmonary, renal, and hepatic function periodically. Implant: Monitor for seizures, impaired neurosurgical wound healing; signs and symptoms of meningitis, CNS infection, and obstruction hydrocephalus.
Tương tác
May enhance myelosuppressive effects with cimetidine. Increased risk of pulmonary toxicity with melphalan. Decreased antiepileptic activity of phenytoin. Decreased absorption of digoxin.
Tác dụng
Description: Carmustine, a cell cycle non-specific antineoplastic agent belonging to nitrosourea group, interferes with the normal function of DNA and RNA by alkylation and cross-linking the strands of DNA and RNA, and by possible protein modification. It inhibits enzymatic processes by carbamoylation of amino acids in proteins.
Pharmacokinetics:
Distribution: Readily crosses the blood-brain barrier.
Metabolism: Rapidly metabolised after IV administration.
Excretion: Mainly via urine (approx 60-70%); lungs (approx 10%, as carbon dioxide). Elimination half-life: 15-75 minutes (IV).
Đặc tính

Chemical Structure Image
Carmustine

Source: National Center for Biotechnology Information. PubChem Database. Carmustine, CID=2578, https://pubchem.ncbi.nlm.nih.gov/compound/2578 (accessed on June 25, 2020)

Bảo quản
Reconstituted solution for inj: Store intact vials between 2-8°C. Protect from light. Reconstituted solutions may be stored either between 2-8°C for 24 hours or at 25°C for 8 hours. Protect from light. Implant: Store at -20°C. Unopened foil pouches may be kept at 25°C for not more than 6 hours and may only be refrozen once. Refrozen foil pouches must be used within 30 days.
Phân loại MIMS
Phân loại ATC
L01AD01 - carmustine ; Belongs to the class of alkylating agents, nitrosoureas. Used in the treatment of cancer.
References
Anon. Carmustine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 01/06/2020.

Anon. Carmustine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/06/2020.

Bicnu (Heritage Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/06/2020.

Buckingham R (ed). Carmustine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2020.

Carmustine 100 mg Powder and Solvent for Solution for Infusion (Tillomed Laboratories Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 05/06/2020.

Gliadel 7.7 mg Implant (MGI Pharma Limited). MHRA. https://products.mhra.gov.uk/. Accessed 05/06/2020.

Gliadel Wafer (Arbor Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/06/2020.

Joint Formulary Committee. Carmustine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2020.

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