Country: Kanada
Bahasa: Inggeris
Sumber: Health Canada
BUSULFAN
EUGIA PHARMA INC.
L01AB01
BUSULFAN
60MG
SOLUTION
BUSULFAN 60MG
INTRAVENOUS
100
Prescription
Active ingredient group (AIG) number: 0103273002; AHFS:
APPROVED
2023-04-04
Page 1 of 31 PRODUCT MONOGRAPH PR BUSULFAN FOR INJECTION SOLUTION, 60 MG / 10 ML (6 MG / ML) MUST BE DILUTED PRIOR TO USE. Intravenous ANTINEOPLASTIC Eugia Pharma Inc. DATE OF PREPARATION: 3700 Steeles Avenue West, Suite 402 April 04, 2023 Woodbridge, Ontario, L4L 8K8 Canada CONTROL NUMBER: 271846 Page 2 of 31 PRODUCT MONOGRAPH NAME OF DRUG PR BUSULFAN FOR INJECTION 60 mg / 10 mL (6 mg / mL) BUSULFAN FOR INJECTION IS A POTENT CYTOTOXIC DRUG THAT RESULTS IN PROFOUND MYELOSUPPRESSION AT THE RECOMMENDED DOSAGE. IT SHOULD BE ADMINISTERED UNDER THE SUPERVISION OF A QUALIFIED PHYSICIAN WHO IS EXPERIENCED IN THE USE OF CANCER CHEMOTHERAPEUTIC AGENTS AND IN THE MANAGEMENT OF PATIENTS WITH SEVERE PANCYTOPENIA. APPROPRIATE MANAGEMENT OF THERAPY AND COMPLICATIONS IS ONLY POSSIBLE WHEN ADEQUATE DIAGNOSTIC AND TREATMENT FACILITIES ARE READILY AVAILABLE. ACTIONS AND CLINICAL PHARMACOLOGY Busulfan is a potent cytotoxic agent and a bifunctional alkylating agent. In aqueous media, release of the methanesulfonate group produces carbonium ions, which can alkylate DNA, thought to be an important biological mechanism for its cytotoxic effect. Current literature suggests that high AUC values (>1,500 mcMol•min) may be associated with an increased risk of developing hepatic veno-occlusive disease and/or seizures. Mean C max , AUC, T 1/2 and plasma clearance are provided below for oral busulfan and IV busulfan (See PHARMACOLOGY). PARAMETER ORAL BUSULFAN BUSULFAN IV C max (ng/mL) (range) (CV%) 870 (30%) 1,167 (12%) AUC (mcMol•min) (CV%) 1,396 (24%) 1,156 (14%) T 1/2 (hr) (CV%) 3.55 (33%) 3.11 (10%) Plasma Clearance (mL/min) (CV%) 195 (27%) 182 (16%) Intravenous busulfan had a more consistent pharmacokinetic profile than oral busulfan among patients. Busulfan achieves concentrations in the cerebrospinal fluid approximately equal to those in plasma. Irreversible binding to plasma elements, primarily albumin, has been estimated to be 32.4 + 2.2%, which is consistent with the reactive electrophilic properties of this alkylator. Page 3 of Baca dokumen lengkap