BUSULFAN FOR INJECTION SOLUTION

국가: 캐나다

언어: 영어

출처: Health Canada

유효 성분:

BUSULFAN

제공처:

STERIMAX INC

ATC 코드:

L01AB01

INN (International Name):

BUSULFAN

복용량:

60MG

약제 형태:

SOLUTION

구성:

BUSULFAN 60MG

관리 경로:

INTRAVENOUS

패키지 단위:

10ML

처방전 유형:

Prescription

치료 영역:

ANTINEOPLASTIC AGENTS

제품 요약:

Active ingredient group (AIG) number: 0103273002; AHFS:

승인 상태:

APPROVED

승인 날짜:

2017-05-05

제품 특성 요약

_ _
_Busulfan for Injection _
_Page 1 of 31 _
PRODUCT MONOGRAPH
PR
BUSULFAN FOR INJECTION
6 mg/mL
Sterile solution for injection
Antineoplastic
SteriMax Inc.
2770 Portland Drive
Oakville, ON L6H 6R4
Date of Preparation:
May 4, 2017
Submission Control No: 193322
_ _
_Busulfan for Injection _
_Page 2 of 31 _
PRODUCT MONOGRAPH
PR
BUSULFAN FOR INJECTION
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 μMol•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 intravenous (IV) busulfan (See PHARMACOLOGY).
PARAMETER
ORAL BUSULFAN
IV BUSULFAN
Cmax (ng/mL) (range) (CV%)
870 (30%)
1,167 (12%)
AUC (μMol•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. Busulfan is
predominately meta