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PubMed1994

Alternatives to oral estrogen replacement. Transdermal patches, percutaneous gels, vaginal creams and rings, implants, other methods of delivery.

Alternatives to oral estrogen replacement, including the transdermal patch, deliver estradiol in a constant manner, produce more physiologic estrone and estradiol levels than oral therapy, and avoid the first-pass effect on hepatic protein synthesis. Transdermal patches and estradiol implants have been demonstrated to produce favorable lipid profiles, prevent bone loss, relieve vasomotor symptoms, and improve urogenital atrophy. Vaginal estrogen is an effective treatment for vaginal atrophy. The advantages and disadvantages of each of the hormonal alternatives to oral estrogen replacement are discussed.

Administration, Cutaneous↗
PubMed1994

Initial management of recurrent vulvovaginal candidiasis with oral ketoconazole and topical clotrimazole.

In a randomized study, 151 women with a history of recurrent vulvovaginal candidiasis and suffering from an acute episode of candidal vaginitis were assigned to receive either oral ketoconazole, 400 mg daily for 14 days, or clotrimazole vaginal suppositories, 100 mg daily for 7 days. One week after completion of therapy, evaluation revealed a clinical cure or improvement in 86.4% of ketoconazole- and 81.7% of clotrimazole-treated patients (P > .5), with a mycologic response in 80.3% and 81.7%, respectively. In the absence of maintenance suppressive antimycotic therapy, further follow-up for two months revealed an extremely high rate of clinical and mycologic failure in both groups, reaching 52.5% after ketoconazole and 62.6% after clotrimazole (NS). Adverse effects were significantly more common with systemic ketoconazole than accompanying topical clotrimazole therapy. Although both forms of antifungal therapy were highly successful in inducing clinical and mycologic remission in patients with recurrent vulvovaginal candidiasis, this study emphasized the need for immediate initiation of maintenance therapy following an initial clinical improvement.

Acute Disease↗
PubMed1995

[Recurrent vulvovaginal mycoses].

The treatment of recurrent vulvovaginal fungal infections is difficult. Pathogenic mechanisms are discussed. Available pharmacologic treatments and their mechanisms of action are reviewed. Patients clearly prefer oral treatment. Ketoconazole is toxic. Only topical or nonabsorbed oral agents can be used during pregnancy. Agents absorbed via the digestive tract can be used in women who use effective contraceptive methods. Published data demonstrate that trifluconazole (which has not yet been granted a license in France) is potent and less toxic than ketoconazole, and that recurrences at discontinuation of this drug are less common. A few hypotheses for future research are presented.

Administration, Intravaginal↗
PubMed1997

[Urogenital complaints: value of systemic estrogen therapy].

Local and systemic therapies with estrogens lead to a fast alleviation of urogenital symptoms, which occur frequently in the postmenopausal women. Especially atrophical changes in vulva and vagina, but also complaints about incontinence are improved by estrogen therapy. Even though there is no objective evidence of an improvement of stress incontinence, there are less infections of the lower urinary tract as well as a diminution of urge incontinence. Moreover, systemic estrogen therapy helps to prevent postmenopausal osteoporosis and cardiovascular diseases. Urogenital complaints may motivate patients easily for a long lasting systemic estrogen therapy, because symptoms are bothering and annoying.

Administration, Cutaneous↗
PubMedDate not supplied

[Luteal phase support after vaginal progesterone: comparative study with micronized oral progesterone].

Two progesterone presentations, a vaginal application of 90 mg progesterone per day (Crinone) or 300 mg progesterone orally administered (Utrogestan) were compared for luteal phase support of patients undergoing an in vitro fertilisation (IVF) procedure. 283 patients were randomly allocated to either treatment. The treatment started within 24 hours after the embryo transfer procedure and continued until day 30 in cases of implantation. Efficacy was assessed using the pregnancy and delivery rates. Safety was assessed through specific symptoms and usual safety monitoring. The pregnancy rate per transfer was not significantly different in the Crinone and Utrogestan groups at day 12 (Crinone: 35.3%, Utrogestan: 29.9%, p = 0.55), at day 30 (Crinone: 28.8%, Utrogestan: 25%, p = 0.61), at day 90 (Crinone: 25.9%, Utrogestan: 22.9%, p = 0.69). No difference in spontaneous abortion rates were seen thereafter. The delivery rate was not significantly different (proportion delivery per patients included, Crinone: 23.0%, Utrogestan: 22.2%, p = 1), as well as the ratio new-born per transferred embryo (Crinone: 11.7%; Utrogestan: 11.1%, p = 0.91). Safety parameters were similar in both groups except for drowsiness, which was more significantly frequent in the oral P group than in the Crinone group at all time points. No serious adverse events were recorded in this study. The fact that Crinone matches the efficacy of the larger doses of progesterone used orally reflects an advantage of the transvaginal route of administration which avoids metabolic inactivation of progesterone during its first liver pass.

Administration, Intravaginal↗
PubMed1976

The efficacy of intravaginal 15 methyl prostaglandin F2alpha methyl ester in first and second trimester abortion.

Fifteen methyl prostaglandin F2alpha methyl ester prepared within a silastic device for intravaginal administration appears to be advantageous. This study describes the technique carried out and the results observed in 50 patients. The analogue is prepared in 1.0% and 0.5% delivery systems. Twenty-four patients received the 1.0% dosage schedule and all twenty-four patients aborted. Twenty-six patients received 0.5% and twenty-three patients aborted. The coagulation millieu and other parameters were similar to that reported for other prostaglandins.

Abortion, Induced↗
PubMed1999

[Cervical ripening and labor induction].

To induce labour successfully, a good cervical status and favorable obstetrical conditions are necessary. If these conditions are not present, cervical ripening must take place before induction of labour. Cervical ripening is only justified when a pathology (maternal or foetal) indicates termination of pregnancy. Intracervical or intravaginal administration of prostaglandin E2 is actually the standard for cervical ripening.

Cervical Ripening↗
PubMed1991

[The effectiveness of intravaginal estriol tablet administration in women with urge incontinence].

In postmenopausal patients, stress and urge incontinence often occur as a consequence of oestrogen deficiency. We performed a comparative study in a prospectively randomised and placebo controlled group of women with urge incontinence to investigate different dosages of intravaginally applied oestriol. Clinical and urodynamic parameters were also compared. 15 women (Group I) received 1 mg oestriol applied daily intravaginally over 3 weeks; 15 women (Group II) received a daily dosage of 3 mg and 10 women received a placebo. A complete clinical and urodynamic evaluation was carried out twice at a 4-week interval. The women receiving a daily dose of 3 mg oestriol applied intravaginally demonstrated a significant improvement of the parameters strong desire to void, pollakisuria, and nycturia. No improvement was seen in patients with motoric urge incontinence.

Administration, Intravaginal↗
PubMed1989

A comparison of single-dose oral fluconazole with 3-day intravaginal clotrimazole in the treatment of vaginal candidiasis. Report of an international multicentre trial.

A total of 369 women with clinical and mycological evidence of vaginal candidiasis received treatment, after random allocation, with either a single oral 150-mg dose of fluconazole (188 women) or 200 mg of intravaginal clotrimazole given daily for 3 consecutive days (181 women). They were assessed at 5-16 days and again at 27-62 days after treatment. Candida species were completely eradicated from the vagina in 72% of the fluconazole group and in 62% of the clotrimazole group at the long-term assessment (P = 0.07). Favourable clinical responses were obtained in 99% of the fluconazole group and in 97% of the clotrimazole group at the short-term assessment and in 93% and 84% respectively at the long-term assessment when there was a significant advantage for fluconazole treatment (P = 0.02). Symptoms in patients receiving fluconazole were relieved more rapidly (P less than 0.001). Treatment-related side-effects were few and minor in both groups. It is concluded that treatment of vaginal candidiasis with fluconazole, as a single oral dose, was more effective in the long term, relieved symptoms more rapidly, and was as safe as treatment with intravaginal clotrimazole.

Administration, Intravaginal↗
PubMed1975

Gonadotropin-releasing activity of two highly active and long-acting analogs of luteinizing hormone-releasing hormone after subcutaneous, intravaginal, and oral administration.

The gonadotropin-releasing activities of two synthetic analogs of luteinizing hormone-releasing hormone (LH-RH), D-Ala6-des-Gly10-LH-RH ethylamide and D-Leu6-des-Gly10-LH-RH ethylamide were evaluated in immature female rats after subcutaneous, intravaginal, and oral administration. Maximal peaks of serum LH and follicle-stimulating hormone (FSH) levels after administration of both analogs by any of the three routes were obtained at 2 hours. Therefore, serum gonadotropin levels declined slowly, so that at 6 hours LH levels had returned to base line values, whereas FSH levels remained elevated for up to 10 hours. The integrated serum gaondotropin levels after LH-RH and both analogs over a 10-hour period indicated that D-Leu6-des-Gly10-LH-RH EA and D-Ala6-des-Gly10-LH-RH EA released more LH and FSH than did the LH-RH decapeptide. The intense and long-acting properties of these analogs in releasing LH and FSH suggest the possibility that they may be more useful therapeutically than LH-RH.

Administration, Oral↗
PubMed1982

Fate of metronidazole following intravaginal and intravenous administration to rabbits.

The rate and extent of transvaginal absorption and the disposition of [14C]-metronidazole ([14C]MTZ) were compared during the first 6 h after intravaginal (ivg) and intravenous (iv) administration of 10 mg/kg to adult female rabbits. Upon ivg administration, peak blood 14C levels were reached at 20 min, remained steady up to 1 h, and thereafter followed a decline similar to that of the iv injected group. Following ivg application, both the area under the blood 14C concentration versus time curve (AUC) and the elimination half-life (t1/2) of 14C from blood during the beta-phase were similar to those of iv injected females. Less than 1% of the administered radioactivity was recovered from the vagina after 5 h. Urine was the main channel of 14C excretion, and only 5--8% of the administered dose was recovered in bile during 6 h in either treatment group. The combined excretions of 14C in the urine, bile, and feces were similar (ivg = 72.2 +/- 4.5 and iv = 66.6 +/- 1.9% of dose) in both groups. At the end of 6 h, the levels of 14C were highest in the urinary bladder, liver, and kidney, followed by those in the duodenum, cecum, and uterus, but lowest in fat after both iv and ivg treatments. Unchanged [14C]MTZ and five of its metabolites were detected in the urines of both groups; however, the amount of unchanged [14C]MTZ was significantly greater in 0--1 and 1--2 h urines of ivg treated rabbits than their iv dosed counterparts. The results show that MTZ is quickly absorbed through rabbit vagina and the metabolism of this chemotherapeutic agent is influenced by the route of administration.

Absorption↗
PubMedDate not supplied

Efficacy of low-dose intravaginal estriol on urogenital aging in postmenopausal women.

OBJECTIVE: To assess the efficacy and safety of intravaginal estriol administration on urinary incontinence, urogenital atrophy, and recurrent urinary tract infections in postmenopausal women. DESIGN: Eighty-eight postmenopausal women with urogenital aging symptoms were enrolled in this prospective, randomized, placebo-controlled study. Participants were randomly divided into two groups, with each group consisting of 44 women. Women in the treatment group received intravaginal estriol ovules: 1 ovule (1 mg) once daily for 2 weeks and then 2 ovules once weekly for a total of 6 months as maintenance therapy. Women in the control group received inert placebo vaginal suppositories in a similar regimen. We evaluated urogenital symptomatology, urine cultures, colposcopic findings, urethral cytologic findings, urethral pressure profiles, and urethrocystometry before as well as after 6 months of treatment. RESULTS: After therapy, the symptoms and signs of urogenital atrophy significantly improved in the treatment group in comparison with the control group. Thirty (68%) of the treated participants, and only seven (16%) of the control participants registered a subjective improvement of their incontinence. In the treated participants, we observed significant improvements of colposcopic findings, and there were statistically significant increases in mean maximum urethral pressure, in mean urethral closure pressure as well as in the abdominal pressure transmission ratio to the proximal urethra. Urethrocystometry showed positive but not statistically significant modifications. CONCLUSIONS: Our results show that intravaginal administration of estriol may represent a satisfactory therapeutic choice for those postmenopausal women with urogenital tract disturbances who have contraindications or refuse to undergo standard hormone therapy.

Administration, Intravaginal↗
PubMed1977

Stimulation of luteinizing hormone (LH) and follicle-stimulating hormone by (D-Leu6, des-Gly10-NH2)-LH-releasing hormone ethylamide after subcutaneous, intravaginal, and intrarectal administration to women.

Women, most of whom had regular menstrual cycles, were administered D-Leu6,des-Gly10-NH2)-luteinizing hormone-releasing hormone (LH-RH) ethylamide (D-Leu6-LH-RH-EA)via different routes during the early or midfollicular phase of the cycle. Plasma LH, follicle-stimulating hormone (FSH), and estrogen levels were determined by radioimmunoassay before and after administration of D-Leu6-LH-RH-EA. plasma LH and FSH increased and reached peak levels 3 to 4 hours and 3 to 6 hours, respectively, after subcutaneous injection of 25 mug of the analog of LH-RH. Intravaginal or intrarectal application of 2 mg of D-Leu6-LH-RH-EA also increased plasma LH and FSH levels in most of the women, but the magnitude of the rise, the time of initiation of response, and the peak level varied among the women. The plasma estrogen level also rose after administration via either route.

Adult↗