KETOCONAZOLE TABLET

מדינה: קנדה

שפה: אנגלית

מקור: Health Canada

מרכיב פעיל:

KETOCONAZOLE

זמין מ:

APOTEX INC

קוד ATC:

J02AB02

INN (שם בינלאומי):

KETOCONAZOLE

כמות:

200MG

טופס פרצבטיות:

TABLET

הרכב:

KETOCONAZOLE 200MG

מסלול נתינה (של תרופות):

ORAL

יחידות באריזה:

100

סוג מרשם:

Prescription

איזור תרפויטי:

AZOLES

leaflet_short:

Active ingredient group (AIG) number: 0116793001; AHFS:

מצב אישור:

APPROVED

תאריך אישור:

2021-04-07

מאפייני מוצר

PRODUCT MONOGRAPH
Pr
KETOCONAZOLE
Ketoconazole Tablets USP
200 mg
Antifungal Agent
APOTEX INC.
150 Signet Drive
Weston,
Ontario
M9L 1T9
DATE OF
PREPARATION:
April 6, 2021
CONTROL NO.: 245850
1
2
PRODUCT MONOGRAPH
KETOCONAZOLE
Ketoconazole Tablets USP
200 mg
THERAPEUTIC CLASSIFICATION
Antifungal Agent
ACTION AND CLINICAL PHARMACOLOGY
_In vitro _studies suggest that the antifungal properties of
ketoconazole may be related to
its ability to impair the synthesis of ergosterol, a component of
fungal and yeast cell
membranes. Without the availability of this essential sterol, there
are morphological
alterations of the fungal and yeast cell membranes manifested as
abnormal membranous
inclusions between the cell wall and the plasma membrane. The
inhibition of ergosterol
synthesis has been attributed to interference with the reactions
involved in the removal
of the 14-α-methyl group of the precursor of ergosterol, lanosterol.
Comparative Bioavailability
A double-blind, two way, randomized, cross-over bioavailability study
was conducted
in 18 adult, healthy, male volunteers to evaluate the relative
bioavailability of single oral
doses (200 mg) of Ketoconazole 200. mg tablets manufactured by Apotex
Inc. and
Nizoral
®
200 mg tablets manufactured by Janssen Pharmaceutica Inc.
The mean pharmacokinetic data obtained from the 17 evaluable subjects
were as follows:
Table 1: Pharmacokinetic Indices for Ketoconazole
Parameter
Geometric Mean
Arithmetic Mean (C.V.)
Ratio of Geometric
Means (%) *
Ketoconazole
Nizoral
®
†
AUC
T
(ng.hr/mL)
AUC
I
(ng.hr/mL)
C
max
(ng/mL)
T
max
**
(hr)
t
1/2
**
(hr)
15246.7
17667.8 (51)
15679.2
18036.4 (51)
3756.6
4218.7 (38)
2.32 (35)
1.75 (50)
16668.8
18600.0 (42)
17041.7
18941.6 (42)
4030.7
4355.7 (33)
2.44 (34)
1.59 (18)
91.5
92.0
93.2
--
--
† Nizoral
®
(Janssen Pharmaceutica Inc.) was purchased at a Canadian retail
pharmacy.
*
Based on the least squares estimate of the geometric means.
**
The T
max
and t
1/2
parameters are expressed as the arithmetic means (CV).
3
INDICATIONS
KETOCONAZOLE (ke