BUSULFAN FOR INJECTION SOLUTION

País: Canadá

Idioma: inglés

Fuente: Health Canada

Ingredientes activos:

BUSULFAN

Disponible desde:

STERIMAX INC

Código ATC:

L01AB01

Designación común internacional (DCI):

BUSULFAN

Dosis:

60MG

formulario farmacéutico:

SOLUTION

Composición:

BUSULFAN 60MG

Vía de administración:

INTRAVENOUS

Unidades en paquete:

10ML

tipo de receta:

Prescription

Área terapéutica:

ANTINEOPLASTIC AGENTS

Resumen del producto:

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

Estado de Autorización:

APPROVED

Fecha de autorización:

2017-05-05

Ficha técnica

_ _
_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