PMS-BUSULFAN SOLUTION

Pays: Canada

Langue: anglais

Source: Health Canada

Ingrédients actifs:

BUSULFAN

Disponible depuis:

PHARMASCIENCE INC

Code ATC:

L01AB01

DCI (Dénomination commune internationale):

BUSULFAN

Dosage:

6MG

forme pharmaceutique:

SOLUTION

Composition:

BUSULFAN 6MG

Mode d'administration:

INTRAVENOUS

Unités en paquet:

8X10ML

Type d'ordonnance:

Prescription

Domaine thérapeutique:

ANTINEOPLASTIC AGENTS

Descriptif du produit:

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

Statut de autorisation:

APPROVED

Date de l'autorisation:

2018-06-15

Résumé des caractéristiques du produit

PRODUCT MONOGRAPH
Pr
PMS-BUSULFAN
Busulfan for injection
6 mg / mL
Sterile concentrated solution
ANTINEOPLASTIC
PHARMASCIENCE INC.
6111 Royalmount Ave., Suite 100
Montréal, Canada
H4P 2T4
www.pharmascience.com
Date of Preparation:
June 14, 2018
Submission Control No: 198231
_pms-BUSULFAN Product Monograph _
_Page 2 of 30 _
PRODUCT MONOGRAPH
Pr
PMS-BUSULFAN
Busulfan for injection
6 mg / mL
Sterile concentrated solution
PMS-BUSULFAN (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 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
IV BUSULFAN
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 electrophi