BUSULFEX SOLUTION

국가: 캐나다

언어: 영어

출처: Health Canada

유효 성분:

BUSULFAN

제공처:

OTSUKA PHARMACEUTICAL CO LTD

ATC 코드:

L01AB01

INN (International Name):

BUSULFAN

복용량:

60MG

약제 형태:

SOLUTION

구성:

BUSULFAN 60MG

관리 경로:

INTRAVENOUS

패키지 단위:

8X10ML

처방전 유형:

Prescription

치료 영역:

ANTINEOPLASTIC AGENTS

제품 요약:

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

승인 상태:

CANCELLED POST MARKET

승인 날짜:

2020-09-01

제품 특성 요약

PRODUCT MONOGRAPH
PR
BUSULFEX
®
(BUSULFAN)
6 MG/ML
INJECTION
ANTINEOPLASTIC
Otsuka Pharmaceutical Co., Ltd.
DATE OF REVISION:
Tokyo, 101-8535 Japan
March 10, 2017
Distributed and Marketed by:
CONTROL # 200963
Otsuka Canada Pharmaceutical Inc.
Saint-Laurent, Quebec H4S 2C9
2
PRODUCT
MONOGRAPH
NAME OF DRUG
Pr
BUSULFEX


(Busulfan) Injection 6
mg/mL
BUSULFEX
(BUSULFAN)
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 PHARMACOL
OGY
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 IV
BUSULFEX (busulfan) (See PHARMACOLOGY).
PARAMETER
ORAL BUSULFAN
BUSULFEX IV
C
max
(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%)
3
Intravenous BUSULFEX 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
me