BUSULFAN FOR INJECTION SOLUTION

البلد: كندا

اللغة: الإنجليزية

المصدر: Health Canada

العنصر النشط:

BUSULFAN

متاح من:

MARCAN PHARMACEUTICALS INC

ATC رمز:

L01AB01

INN (الاسم الدولي):

BUSULFAN

جرعة:

60MG

الشكل الصيدلاني:

SOLUTION

تركيب:

BUSULFAN 60MG

طريقة التعاطي:

INTRAVENOUS

الوحدات في الحزمة:

10ML

نوع الوصفة الطبية :

Prescription

المجال العلاجي:

ANTINEOPLASTIC AGENTS

ملخص المنتج:

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

الوضع إذن:

APPROVED

تاريخ الترخيص:

2018-04-23

خصائص المنتج

1
PRODUCT MONOGRAPH
PR
BUSULFAN FOR INJECTION
(BUSULFAN)
MANUFACTURER’S STANDARD
6 MG / ML
ANTINEOPLASTIC
Marcan Pharmaceuticals Inc.
Date of Preparation:
77 Auriga Drive, Suite#4,
April 20, 2018
Ottawa, ON, K2E 7Z7
Control # 199906
2
PRODUCT MONOGRAPH
NAME OF DRUG
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
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%)
IV Busulfan had a more consistent pharmacokinetic profile than oral
busulfan among patients.
3
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
metabolized
through
conjugation
with
glutathione,
both
spontaneously