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PubMed1994

[The effectiveness of intravaginal administration of estrumate for cows in silent heat in relation to the progesterone concentration in the blood].

In 22 silent heat cows with functional corpus luteum the blood progesterone concentrations and appearance of oestrus after administration of Estrumate were examined. 2 ml Estrumate (500 micrograms cloprostenol) were given intravaginally to 12 cows and intramuscularly to 10 cows respectively. Progesterone concentrations declined 32 hrs after application to levels below 3, 18 nmol/l in all animals. Within 10 days 66.6% of the cows after intravaginal administration of Estrumate and 70% after intramuscular administration came into oestrus. The results indicate that intravaginal application of Estrumate in silent cows with functional corpus luteum induced luteolysis and oestrus identical with intramuscular application.

Administration, Intravaginal↗

PubMed1995

[Effect of intravaginal administration of cisplatin (CDDP) suppositories to uterine cervical cancer--blood and tissue concentrations and the therapeutic effects].

Four patients with cervical cancer (squamous cell carcinoma: two cases of stage Ib, one of stage IIa, adenocarcinoma: one of stage Ib), were treated preoperatively by intravaginal administration of CDDP (20 mg) suppositories with pessary 7 times every other day. The uptake, distribution and antitumor effect of CDDP were investigated. Results were as follows. 1) Serum total platinum (Pt) concentration varied between individual patients. Cmax profile (0.17-0.57 micrograms/ml) of Pt was observed at 12 hours after the total dose of 140 mg administration in all patients. 2) The tissue Pt concentration showed high values in the cervix (average 55.4 micrograms/g), followed by the vagina (13.13), endometrium (3.17), uterine wall (0.64), ovary (0.57), lymph node group: parametrial (1.14), obturator (0.34), inguinal (0.28), external iliac (0.51), internal iliac (0.42) and common iliac (0.54). Para-aortic node value was too low to detect. 3) Colposcopic findings were disappearance of bleeding and reduction of tumor outgrowth. Microscopic findings were degeneration and necrosis of cancer nest from the surface to about 2 mm depth of the cervix. In conclusion, it may be necessary to improve CDDP penetration from the tumor surface for effective local chemotherapy.

Adenocarcinoma↗

PubMed2002

Subchronic (13-week) toxicity studies of intravaginal administration of spermicidal vanadocene acetylacetonato monotriflate in mice.

Bis-cyclopentadienyl complexes of vanadium(IV) or vanadocenes are rapid and potent inhibitors of human sperm motility with potential as a new class of contraceptive agents. In this study, groups of 10 B(6)C(3)F(1) and 20 CD-1 female mice were exposed intravaginally to a gel-microemulsion containing 0, 0.06, 0.12, or 0.25% of a representative vanadocene, vanadocene acetylacetonato monotriflate (VDACAC), five days per week for 13 consecutive weeks. The doses of VDACAC used were nearly 300- to 1250-fold higher than its in vitro spermicidal EC(50) value. After 13 weeks of intravaginal treatment, B(6)C(3)F(1) mice were evaluated for survival, body weight gain, absolute and relative organ weights, and systemic toxicity. Blood was analyzed for hematological and clinical chemistry profiles. Microscopic examination was performed on hematoxylin- and eosin-stained tissue sections from each study animal. Vanadium content in tissues was determined by atomic absorption spectroscopy. Gel-microemulsion (placebo) control and VDACAC dosed female CD-1 mice were mated with untreated males in order to evaluate if VDACAC has any adverse effects on the reproductive outcome. There were no treatment-related mortalities in either study. Mean body weight gain during the dosing period was not reduced by VDACAC treatment. Hemograms or clinical chemistry profiles did not reveal any toxicologically significant changes attributed to VDACAC treatment. No clinically significant dose-dependent changes in absolute and relative organ weights were noted in VDACAC dose groups. Extensive histopathological examination of tissues revealed no treatment-related abnormalities in any of the three VDACAC dose groups. Vanadium was not incorporated in mouse tissues at levels above 1 microg/g. Repeated intravaginal exposure of CD-1 mice to increasing concentrations of VDACAC for 13 weeks had no adverse effect on their subsequent reproductive capability (100% fertile), neonatal survival (>96%) or pup development. Collectively, these findings demonstrate that repetitive intravaginal administration of VDACAC to yield effective spermicidal concentrations (<0.1%) in the vagina was not associated with systemic toxicity and did not adversely affect the reproductive performance in mice. The spermicidal vanadocene-chelated complex, VDACAC, may be useful as a safe vaginal contraceptive.

Administration, Intravaginal↗

PubMed1999

Systemic absorption of clindamycin after intravaginal administration of clindamycin phosphate ovule or cream.

The absolute bioavailability of clindamycin phosphate vaginal ovule with comparison to a reference treatment of clindamycin phosphate sterile solution, as well as the relative bioavailability of the ovule compared to clindamycin phosphate vaginal cream, was evaluated in 12 healthy adult female volunteers. Subjects were randomly assigned to receive either the ovule or cream formulation intravaginally for 3 consecutive days during the two-way crossover portion of the study. During a third treatment period, all subjects received 100 mg of clindamycin as a 4-minute intravenous infusion of clindamycin phosphate sterile solution (10 mg/mL). Clindamycin concentrations in serum were assayed by a high-performance liquid chromatography method with detection by mass spectrometry. Pharmacokinetic analyses of the serum data indicated low systemic absorption of clindamycin from the vaginal cream (about 4%), consistent with results of previous bioavailability studies. Following intravaginal administration of the clindamycin phosphate ovule, systemic absorption averaged 30%, which was approximately sevenfold greater than after dosing with the vaginal cream. The higher drug absorption for the ovule may be related to differences in formulation effects on the vaginal membrane. Nevertheless, systemic exposure to clindamycin from the ovule is still considerably lower than from a therapeutic oral dose.

Absorption↗

PubMed2001

Subchronic (13-week) toxicity studies of intravaginal administration of spermicidal vanadocene dithiocarbamate in mice.

Spermicidal organometallic complexes of vanadium(IV) with bis(cyclopentadienyl) rings or vanadocenes are a new class of experimental contraceptive agents. In a systematic search for vanadocenes with selective spermicidal activity, we identified vanadocene dithiocarbamate (VDDTC) as the most potent and stable spermicidal compound. In this study, groups of 10 B(6)C(3)F(1) and 20 female CD-1 mice were exposed intravaginally to a gel-microemulsion containing 0, 0.06, 0.12, and 0.25% VDDTC 5 days per week for 13 consecutive weeks. The doses of VDDTC used were nearly 1250- to 5000-fold higher than its in vitro spermicidal EC(50) value. After 13 weeks of intravaginal treatment, B(6)C(3)F(1) mice were evaluated for survival, body weight gain, absolute and relative organ weights, and systemic toxicity. Blood was analyzed for hematologic and clinical chemistry parameters. Microscopic examination was performed on hematoxylin and eosin-stained tissue sections from each study animal. Vanadium content in tissues was determined by atomic absorption spectroscopy. Placebo control and VDDTC-dosed female CD-1 mice were mated with untreated males to evaluate whether VDDTC has any deleterious effects on the reproductive performance. There were no treatment-related effects on survival and mean body weight and mean body weight gain during the dosing period. The blood chemistry or hemogram profiles did not reveal any toxicologically significant changes that could be attributed to VDDTC treatment. No clinically significant changes in absolute and relative organ weights were noted in VDDTC dose groups. Extensive histopathological examination of tissues revealed no treatment-related abnormalities in any of the three VDDTC dose groups. The vanadium content of all mouse tissue analyzed was <1 microg/g. Repeated intravaginal exposure of CD-1 mice to increasing concentrations of VDDTC for 13 weeks had no adverse effect on their subsequent reproductive capability (100% fertile), neonatal survival (>90%), or pup development. Collectively, these findings demonstrate that repetitive intravaginal administration of VDDTC to yield effective spermicidal concentrations (<0.1%) in the vagina was not associated with systemic toxicity and did not adversely affect the reproductive performance in mice. VDDTC may have clinical utility as an active ingredient of non-detergent type, safe, vaginal spermicidal contraceptives.

Administration, Intravaginal↗

PubMed1998

Induction of labor with intravaginal administration of misoprostol.

OBJECTIVE: The purpose of this study was to evaluate the efficacy and safety of intravaginal misoprostol for labor induction. METHODS: 110 singleton term pregnancies with or without rupture of membranes were enrolled. Fractionated doses of misoprostol were applied (50-100 microg), every 6 h until a maximum of three doses or beginning of labor. RESULTS: The average interval (+/- S.D.) from vaginal application to the beginning of active labor and to delivery were, respectively, 9.5 +/- 5.7 h and 14.8 +/- 9.5 h. Failed labor induction was observed in two cases (2%). Cesarean section rate was 14%. The incidence of tachysystole was 18% and hypersystole 4%, but these situations were associated with abnormal fetal heart rate pattern (hyperstimulation) in only 3%. No maternal side effects and neonatal adverse effects were noted. CONCLUSIONS: Intravaginal misoprostol administration with low doses is an effective and safe method for labor induction in term pregnancies, with or without rupture of membranes.

Administration, Intravaginal↗

PubMed1975

Induction of midtrimester abortion by serial intravaginal administration of 15(S)-15-methyl-prostaglandin F2alpha (THAM) suppositories.

Midtrimester abortion was successfully induced in 13 of 22 patients by serial intravaginal administration of 15(S)-15-methyl-prostaglandin F2alpha (THAM) suppositories. Nine patients, 4 nulliparas and 5 multiparas, failed to abort after 24 hours of prostaglandin administration and a concomitant infusion of oxytocin was initiated. Seven of the nine patients aborted within 7 hours of the combined therapy and one patient on methadone maintainence aborted after 17.5 hours of combined therapy, 41.5 hours after the first dose of prostaglandin. A single patient failed to abort, despite the concomitant prostaglandin-oxytocin administration and underwent surgical evacuation. The mean abortion time for the 21 successful abortions was 22.56 hours. Nulliparous patients aborted somewhat faster, mean 21.79 hours, than multiparous patients, mean 23.80 hours, but this difference was not statistically significant. In this study, one patient aborted in less than 12 hours, and 62% of the successful cases aborted within 24 hours. The plasma levels of 15-ME-PGF2alpha were analyzed by radioimmunoassay in 10 patients. Plasma prostaglandin levels rose significantly 30 minutes after the insertion of the first suppository, but there was a wide variation in levels from patient to patient. It was observed that the 2 patients with the highest levels had the fastest abortion times and episodes of gastro-intestinal side effects appeared related to a rise in prostaglandin levels. Sixty-four percent of the patients in this study had no gastro-intestinal side effect related to prostaglandin administration.

Abortion, Induced↗

PubMed1998

Absorption and excretion of radioactivity after intravaginal administration of an advanced delivery system of 14C-flutrimazole vaginal cream to postmenopausal women.

In order to improve the effectiveness of treatment of vaginal yeast infections, flutrimazole, (CAS 119006-77-8), a broad spectrum local imidazolic fungicide, has been formulated in an advanced delivery system (Site Release, here in after briefly referred to as SR) designed to improve vaginal retention of the drug. To determine the extent of absorption of 14C-flutrimazole from this formulation, the absorption and excretion of total radioactivity have been studied in healthy postmenopausal female volunteers after intravaginal administration of approximately 5 g of SR Vaginal Cream containing 2% 14C-flutrimazole. Concentrations of unchanged flutrimazole have also been measured in plasma and urine, using a validated gas chromatography-mass spectrometry method. The rate of absorption was slow, with a mean peak plasma radioactivity concentration, Cmax, of 56 ng equivalents/ml, achieved at a mean Tmax of 28 h. Corresponding parameters for flutrimazole were 1.94 ng/ml at 24 h. At 24 h post-dose, unchanged flutrimazole represented only 3% of plasma total radioactivity which indicates that flutrimazole is extensively metabolised in man. Total radioactivity and unchanged flutrimazole were eliminated from plasma with terminal half-lives of 37 and 22 h, respectively. From the proportion of the radioactive dose excreted in urine and faeces, the maximal extent of absorption indicated for the intravaginal dose was about 8%, which is similar to that observed with other imidazolic compounds administered by this route. Thus, the formulation achieves the aim of prolonged drug action through the maintenance of therapeutic concentrations of the drug at the site of infection without notably increased absorption.

Absorption↗

PubMed1975

Mid-trimester abortion induced by intravaginal administration of prostaglandin E2 suppositories.

Mid-trimester abortion was successfully induced in 70 of 71 patients by administration of vaginal PGE2 suppositories. The one patient who failed to abort with this method was pregnant in the blind horn of a duplex uterus. The mean abortion time for the successful inductions was 11.88 hours. Multiparous patients aborted somewhat faster than nulliparous patients, but the difference was not significant. Among the 70 successful inductions 42 patients aborted in 12 hours or less and only one patient had an abortion time of more than 24 hours. The drug appeared effective throughout the stages of gestation included in this series--from 8 to 27 weeks. Eight patients were monitored throughout the abortion procedure and uterine activity was calculated and analyzed. The development of uterine activity was gradual without the sudden rise in frequency of contractions and intrauterine baseline tonus that characterized prostaglandin administered by other methods. The most frequently encountered side effect of vaginal PGE2 suppositories was a temperature elevation, which returned to normal within a few hours of the last dose of the drug. Gastrointestinal disturbances--vomiting and diarrhea--were also common, despite a low initial dose of PGE2 and premedication with antiemetic and antidiarrheal agents. These side effects were in general well tolerated by the patients and never required termination of therapy. The cardiovascular effects of PGE2 in this series could be considered minimal. In a single patient surgical intervention was required to remove the placenta. In seven patients the placenta was removed by sponge forceps and in five patients the placenta was removed manually. There was an estimated blood loss exceeding 250 ml. in 10 patients, but transfusion was not required. Although white blood cell count rose significantly during the abortion period there were no significant changes in hematocrit or platelet count. Mid-trimester abortion with intravaginal administration of PGE2 suppositories appears to offer a valid alternative to the presently available techniques, with a rapid abortion time, high success rate, and low incidence of complications.

Abortion, Induced↗

PubMed1999

[Ultrasound imaging of the lower urinary tract in post-menopausal women with urinary stress or combined type of incontinence before and after intravaginal administration of estriol].

The finding that climacteric symptoms are caused mainly by a decline of the oestrogen level and that their development can practically always be prevented by long-term local or general oestrogen treatment was a great asset to the treatment of this problem. Oestriol, a less effective natural oestrogen, has a favourable effect on urogenital tissues without stimulating the endometrium [2]. The objective of the present investigation was to analyze ultrasonographic parameters of the lower urinary tract in women after the menopause with the stress or mixed type of urinary incontinence before and after two-month local oestriol treatment (Ovestin). The trial comprised 40 women with confirmed stress (GSI) or the mixed type of urinary incontinence. The group with GSI comprised 124 patients and the group suffering from the mixed type of incontinence comprised 26 women. The type of incontinence was assessed by urogynaecological examination. This was followed by transperineal and introital ultrasound examination of patients in a supine position by means of an Acuson 128 XP10 apparatus using a convex probe with a frequency of 5 MHz and a vaginal probe with a frequency of 7.0 MHz. Assessment of the position and mobility of the urethrovesical junction was implemented by the transperineal route using a convex probe and filling the bladder with 300 ml. After urination followed assessment of the urethral sphincter by the introital route in a vertical plane whereby the authors followed the anterior and posterior surface of the rhabdosphincter, and in a horizontal plane its left and right surface (10). The authors assessed also in both planes the maximal thickness of the sphincter. In the vertical plane and in a proximal position in relation to the urethra they evaluated the vascular supply qunatitatively (minimal-1 to very abundant-4) and also the arterial flow-the pulsatile index PI was investigated as well as the resistance index RI. In the vertical plane 1 cm from the urethrovesical junction the authors assessed the thickness of the urethral mucosa; at the same level they evaluated the thickness of the urinary bladder wall; the anterior wall, the vertex and the area of the trigone. They assessed also the thickness of pelvic floor muscles. The assessments were made before and after two-month intravaginal oestriol administration (Ovestin crm)-two weeks 0.5 mg/day and then 0.5 mg twice a week. After treatment no statistically significant differences in thickness and areas of the urethral sphincter were found nor in the thickness of the pelvic floor muscles before and after oestriol administration. Statistically significant differences were recorded in the mobility of the urethrovesical junction and there was a significant increase in the thickness of the urethral mucosa and a more abundant vascularization was recorded during the quantitative evaluation and evaluation of PI. In women with the mixed type of incontinence after oestrogen treatment a decline in the thickness of the urinary bladder was found. Ultrasound examination of the lower urinary tract before and after oestriol treatment (Ovestin crm) is a useful supplement of common examination methods and it confirms its favourable therapeutic effect when administered by the intravaginal route.

Administration, Intravaginal↗

PubMed1980

Pharmacokinetics and metabolic disposition of 14C-metronidazole-derived radioactivity in rat after intravenous and intravaginal administration.

Urinary metabolites and the pharmacokinetics of radioactivity derived from 14C-metronidazole (14C-MTZ) were determined after intravenous (iv) or intravaginal (ivg) administration of 10 mg/kg to adult rats. Following iv or ivg administration, the disappearance of 14C from blood followed the kinetics of a two-compartment open-system model. The blood half-lives of 14C during the beta-phase were 10.9 +/- 1.6 and 13.6 +/- 4.2 hr, after iv and ivg administration, respectively. After ivg application, the MTZ-derived radioactivity was detected in tail blood at 5 min, peaked at 1 hr, declined rapidly to 6 hr and more slowly thereafter. The vaginal absorption half-life of 14C-MTZ was 0.28 +/- 0.09 hr. About 12% of the administered dose remained in the vagina after 1 hr and 1.5% after 24 hr. At 24 hr, the tissue distribution and concentration of 14C were similar in iv and ivg dosed rats, the highest 14C concentration being present in the kidneys and lowest in the fat. The percentages of the dose excreted in 24 hr in the urine and feces were 58 and 15 after iv administration, compared to 37 and 40 after the ivg route, respectively. Unchanged 14C-MTZ and five of its metabolites were detected in the urine irrespective of the route of administration. The results show that metronidazole is rapidly absorbed through the vaginal mucosa of the rat and the metabolism and excretion of this chemotherapeutic agent are influenced by the route of administration.

Animals↗

PubMed1987

[Labor induction at term: amniotomy versus intravaginal administration of prostaglandin E2 tablets].

This study compares the conventional method for induction of labour, amniotomy (A) with or without oxytocin infusion, with induction by means of intravaginal prostaglandin (PG)-E2 tablets. We reviewed the records of 266 women (A group: 155 women, PG group: 111 women), who had no risk factors at the time of induction. Both methods were effective. However, induction by PGE2 tablets presented less risk and was more comfortable than early amniotomy. We conclude that A should no longer be the method of choice for the induction of labour at term; the application of intravaginal PGE2 tablets is an efficacious, easy, and low-risk alternative.

Administration, Intravaginal↗

PubMed1989

[The "other induction"--experiences and consequences in 281 deliveries following intravaginal administration of PGE2 tablets].

186 patients have been included prospectively in a study, aimed at analysing the course of birth after induction with 3 mg PGE2-tablets given intravaginally. These data are compared with those gained from a retrospective analysis of 95 patients using a dose of 2 mg. The total of the births within our clinic in 1986/87 functions as controls. Although in every case there has been an urgent need for the termination of pregnancy and there have been also unfavourable cervix findings in the 3 mg group, no differences could be observed in comparison to the control group concerning duration of cervical dilatation and expulsion, as well as foetal outcome parameters. When comparing the 2 mg and 3 mg groups, a certain superiority of the 3 mg dosage could be noted, leading to the opinion, that trial dosages of less than 3 mg should be abandoned. C-section rate was lowest and spontaneous birth rate was highest in the 3 mg group as compared to the 2 mg and the control groups. Permanent CTG-monitoring was not necessary. CTG-controls after 2 and 6 hours proved to be sufficient. Uterine hyperstimulation occurred in 2.1% of cases in both groups. In every case, prompt antagonization by means of high dose betamimetic therapy could be achieved. Due to reducing maternal and foetal side effects, the maximal mobility of the mother after tablet application, as well as, for the smooth congruence of cervical ripening and labour induction, the clinical use of the 3 mg tablet is a modern alternative to the classic oxytocin induction.

Administration, Intravaginal↗

PubMedDate not supplied

[Present and future choice of pharmaceutical forms for intravaginal administration. II. Barrier systems and vaginal rings].

In part I of this review, various vaginal products for local and systemic treatment have been described and discussed. Part II is reserved to other intravaginal contraceptive systems. Some devices as diaphragms, sponges, ... have a mechanical contraceptive advantage associated or not with a spermicidal activity and can or cannot protect against venereal diseases. Other devices like intravaginal rings allow a long-acting and controlled release of contraceptive hormones and it is quite possible that they replace orale contraceptive dosage forms. Various approaches in designs, safety, effectiveness, inconvenience and advantages are discussed.

Administration, Intravaginal↗

PubMed2006

Intravaginal administration of an inactivated vaccine prevents lesions induced by caprine herpesvirus-1 in goats.

To evaluate the efficacy of mucosal vaccination with a beta-propiolactone inactivated caprine herpesvirus-1 (CpHV-1) vaccine, goats received vaginal administrations of two 7-day cycles at 2 weeks intervals. Seven days after the end of the second cycle, goats were challenged intravaginally with 4 ml of virulent BA.1 strain of CpHV-1. Vaccinated goats shed challenge virus for 8 days but, in comparison with control unvaccinated-challenged goats, were significantly protected from the classical clinical signs of genital lesions. Even without adjuvants, prolonged mucosal vaccination induced production of secretory IgA and provided significant clinical protection.

Administration, Intravaginal↗

PubMed1981

Intravaginal administration of progesterone: enhanced absorption after estrogen treatment.

A progesterone solution was administered by intravaginal instillation, intramuscular injection, and sublingually to estrogen-deficient women, with or without estradiol (E2) replacement, and serum progesterone (P) concentrations were measured by radioimmunoassay. Intravaginal application to postmenopausal subjects receiving E2 gave the highest values of serum P: 10 times baseline at 15 minutes and 30 to 40 times at 1 to 2 hours, with sustained levels, for 7 hours and decline to 10 times baseline at 24 hours. Intravaginal application to hypoestrogenic women gave similar results, but of much lower magnitude (highest value, 20 times baseline). Intramuscular injection, in contradistinction, showed gradually increasing levels over the study period, up to 30 times basal values at 24 hours. It contrast, sublingual application produced very modest serum increases, to approximately 10 times baseline within 2 hours and return to basal value at 24 hours. Since the most rapid and highest levels were observed by vaginal application to postmenopausal women receiving estrogen, and considering that the vagina has been similarly shown to be very effective for estrogen absorption, it is conceived that full hormone replacement could be accomplished in the deficient states by cyclic vaginal application of both steroids.

Absorption↗

PubMed2006

The systemic absorption of etoposide after intravaginal administration in patients with cervical intraepithelial lesions associated with human papillomavirus infection.

PURPOSE: The purpose of this study was to determine the systemic absorption and the release of etoposide in cervical tissue administered via a vaginal ovule to women diagnosed with cervical intraepithelial lesions associated with human papillomavirus (HPV). METHODS: Fifteen women with low- and high-grade intraepithelial neoplasia confirmed by colposcopic test received a 50-mg intravaginal etoposide dose three times a week for 3 weeks. At the end of the study period, paralleled with the last ovule administered, blood samples were collected over a period of 24 h, and in situ cervical samples were obtained at 3 and 10 h after drug administration. Etoposide concentrations were determined in plasma and in in situ cervical samples using the high-performance liquid chromatography method with electrochemical detection. RESULTS: Pharmacokinetic analyses of plasma data indicated low or lack of systemic exposure of etoposide after the vaginal administration. Nevertheless, high concentrations of etoposide were found in all in situ cervical samples, indicating that etoposide could be released from its pharmaceutical formulation. CONCLUSIONS: The results of the study suggest that the etoposide administered as intravaginal ovule is safe and tolerable and apparently could be a suitable option in patients with cervical intraepithelial neoplasia. Clinical results and the true impact on HPV infection and evolution of dysplasia need to be confirmed.

Absorption↗

PubMedDate not supplied

Intravaginal administration of conjugated estrogens in premenopausal and postmenopausal women.

Daily doses of 0.625 mg of conjugated estrogens were administered intravaginally for 14 days to 12 postmenopausal women (six with highly atrophic and six with slightly atrophic vaginal mucosa), resulting in vaginal mucosae similar to those found in premenopausal women in all 12 subjects. In a second experiment, serum estrogens, follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were determined before and hourly for six hours after a single intravaginal dose of 0.625 mg of conjugated estrogens was given to five postmenopausal women and to five premenopausal women on cycle days 6-8. Serum levels of unconjugated immunoreactive estrogens and total estrone increased rapidly in four of five postmenopausal women. Luteal phase values were found after only two hours, but there were no effects on serum FSH and LH. One of the postmenopausal women who had an unatrophied vaginal mucosa, showed a considerable lower resorption of estrogens. There were no significant changes in the serum estrogen levels of the premenopausal women. Thus, we conclude that daily vaginal administration of 0.625 mg of conjugated estrogens for 14 days is sufficient to restore an atrophic vaginal mucosa to a premenopausal condition. Furthermore, the condition of the vaginal mucosa seems to influence the resorption, thus indicating an inbuilt mechanism of protection against overdosage of intravaginally applied estrogens.

Aged↗