A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Gynazole Pharmacology, Pharmacokinetics, Studies, Metabolism - Butoconazole
Gynazole Pharmacology, Pharmacokinetics, Studies, Metabolism - Butoconazole
CLINICAL PHARMACOLOGY
Following vaginal administration of butoconazole nitrate vaginal cream, 2%
to 3 women, 1.7% (range 1.3-2.2%) of the dose was absorbed on average. Peak
plasma levels (13.6-18.6 ng radioequivalents/mL of plasma) of the drug and its
metabolites are attained between 12 and 24 hours after vaginal administration.
Microbiology
The exact mechanism of the antifungal action of butoconazole nitrate is unknown;
however, it is presumed to function as other imidazole derivatives via inhibition
of steroid synthesis.
Imidazoles generally inhibit the conversion of lanosterol to ergosterol, resulting
in a change in fungal cell membrane lipid composition. This structural change
alters cell permeability and, ultimately, results in the osmotic disruption
or growth inhibition of the fungal cell.
Butoconazole nitrate is an imidazole derivative that has fungicidal activity in vitro against
Candida spp. and has been demonstrated to be clinically effective against vaginal infections due
to Candida albicans. Candida albicans has been identified as the predominant species
responsible for vulvovaginal candidasis. .
CLINICAL STUDIES
Vulvovaginal Candidiasis: Two studies were conducted that compared 2% butoconazole nitrate
cream with clotrimazole tablets. There were 322 enrolled patients, 161 received 2.0 %
butoconazole vaginal cream and 161 patients inserted the 500-mg clotrimazole vaginal tablet. At
the second follow-up visit (30 days post-therapy), 118 patients in the butoconzole group and 116
in the clotrimazole group were evaluable for efficacy analysis, respectively. All of these patients
had infection caused by Candida albicans.
The efficacy of the study drugs was assessed by evaluating clinical, mycologic and therapeutic
cure rates (see table 1). The therapeutic cure was defined as complete resolution of signs and
symptoms of vaginal candidiasis (clinical cure) along with a negative KOH examination and
negative culture for Candida spp. (microbiologic eradication) at the long term follow-up (30
days). The therapeutic cure rate was 67% in the butoconazole group and 61 % in the clotrimazole
group
Table 1
| |
2% butoconazole nitrate cream |
500-mg clotrimazole vaginal tablet |
| Enrolled |
161 |
161 |
| Evaluable at Late Follow-up |
118 |
116 |
| Clinical Cure |
95/118 (81 %) |
93/116 (80 %) |
| Mycologic Eradication* |
87/118 (74 %) |
77/116 (66 %) |
| Therapeutic Cure |
79/118 (67 %) |
71/116 (61 %) |
| *= C. albicans in the vaginal culture was proven at admission in all of these patients. |
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