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At least 469 records · Page 26Linked to original sources
PubMed1990

[Treatment with low-dose vaginal estradiol in post-menopausal women. A double-blind controlled trial].

Twenty-three postmenopausal women with recurrent cystitis were allorted at random to treatment for five months with local oestrogen in the vagina or placebo treatment with the object of assessing the local effect on the vaginal epithelium and on the tendency to recurrent cystitis. The therapeutic group and the placebo group were entirely comparable prior to treatment. In the therapeutic group, the oestrogen index in vaginal scrapings was significantly higher after treatment than in the placebo group (p less than 0.01). The number of positive urine cultures and the patients/satisfaction with treatment wee not significantly different in the two groups.

Administration, Intravaginal↗
PubMed1990

Persistent vaginitis caused by metronidazole-resistant trichomonas.

Persistent trichomonal vaginitis is usually considered the result of either patient noncompliance with therapy or reinfection. Drug-resistant trichomoniasis may also cause continued infection despite repeated courses of conventional metronidazole therapy. We report two cases of exceptionally persistent and prolonged infection despite repetitive and varied treatments, including parenteral metronidazole. An unconventional approach combining oral and topical therapy resulted in clinical and microbiologic cure in both cases.

Administration, Intravaginal↗
PubMed1989

[Evaluation of the use of prostaglandins E2 in cervical maturation].

This is a prospective study in order to know the efficacy of prostaglandin E2 gel in the induction of labor by intravaginal administration at the Instituto Nacional de Perinatología. All pregnancies had between 16 and 34 weeks of gestation. There were two groups: Group A (n = 40) patients in whom the induction was made with prostaglandin plus oxitocin, and Group B (n = 40) when just oxitocin was employed. In the first group it was shown a shortening in the length of time of induction, hospitalization days and resolution of the pregnancy by vaginal route in the 100% of the cases. We did not observed side effects in relation to the use of the prostaglandin.

Abortion, Induced↗
PubMed1989

"Body burden" of phosphonoformic acid after topical and vaginal administration to rabbits and beagle dogs.

Trisodium phosphonoformate (PFA), an antiviral compound, was studied in two animal species, dogs and rabbits, for systemic absorption after vaginal and topical application. Antiviral agents to be possibly used against genital and skin herpes should penetrate deeply into the skin and, hopefully, should remain there as long as possible with no or little systemic uptake. In the rabbit the absolute bioavailability after vaginal and topical administration is 14% and 12%, respectively, and in the dog 34% and 3%, respectively. Because PFA has a low toxicity the body burden may be acceptable if the compound is found to be high clinical benefit.

Administration, Intravaginal↗
PubMedDate not supplied

[Action of drugs in relation to the administration route].

The factors capable of modifying the activity of a given drug may be divided into two categories: those related to the patient (age, sex, weight, state of health, genetic factors, etc.) and those related to the drug (pharmaceutical formulation, dose, dose frequency, interaction with other drugs taken more or less simultaneously and administration mode). One example of a drug whose action varies according to the mode of administration adopted is offered by the estrogens which may be given orally (estradiol valerianate, estriol, conjugated estrogens, etc.) or parenterally (estradiol valerianate intramuscularly; conjugated estrogens and estriol vaginally, estradiol as a skin gel, by subcutaneous implant or transdermally). Blood concentrations of estradiol and estrogen after the same dose vary considerably according to the administration mode adopted so that doses may have to be adjusted in order to achieve the same levels of the circulating hormone. Having no first pass effect on the liver, parenteral administrations have less influence than oral ones on the synthesis of certain proteins by the liver (increased SHBG, CBG, TBG, transferrin, ceruloplasmin, angiotensinogen, clotting factors VII, IX, X and X complex; decreased antithrombin III and anti Xa) and on lipid metabolism (increased biliary cholesterol, triglycerides and HDL, especially HDL2; reduced LDL). In particular, it has been found that estradiol (differently from other estrogens) when administered transdermically is able to relieve menopausal symptoms at doses which do not influence the liver synthesis of proteins.

Administration, Cutaneous↗
PubMed1989

Urodynamic changes following hormonal replacement therapy in women with premature ovarian failure.

The mechanism by which estrogen supplementation improves the symptom of stress incontinence in postmenopausal women is unclear. Six women with proved premature ovarian failure were studied urodynamically before and after administration of oral and vaginal estrogen to study estradiol's effects on lower urinary tract function. Regardless of the mode of administration, estrogen supplementation did not produce any significant change in urethral pressure, functional length, or cystometric parameters. However, a significant increase in pressure transmission ratio (P less than .05) to the proximal and mid-urethra was noted after the administration of vaginal estrogen cream. We conclude that estrogen alone, in the absence of aging and other known precipitating factors for stress incontinence, is of minimal significance in maintaining normal urinary tract physiology.

Administration, Intravaginal↗
PubMedDate not supplied

Progesterone administration in patients with absent ovaries.

Forty-four women with absent ovaries who were referred to our centre for oocyte donation were treated with oestradiol valerate and natural progesterone. Serum concentrations and endometrial changes were evaluated on day 21 of stimulated luteal phases after the daily administration of 100 mg of natural progesterone in oil injected intramuscularly or after the ingestion of 300 mg of micronized progesterone or after vaginal administration of 300 mg or 600 mg micronized progesterone, respectively. Endometrial tissue did not show evidence of an adequate secretory pattern after orally administered progesterone. However, after intramuscular injection of 100 mg of natural progesterone and after the vaginal administration of 300 to 600 mg of micronized progesterone, the histologic and electron microscopic pictures were similar in all treatment groups and were close to the expected day 21 of the cycle. Serum levels of progesterone after intramuscular injection were five times higher than after vaginal administration.

Administration, Intravaginal↗
PubMedDate not supplied

[Paralytic ileus secondary to podophyllin poisoning].

The authors report a case of general and local poisoning after erroneous intravaginal administration of podophyllin for warts. The clinical course mainly showed a 10 day paralytic ileus, vaginal and urethral lesions and a severe peripheral neurological illness: paresthesia, dysesthesia and ataxia. The authors stress the potential toxicity of podophyllin and recommend great caution in using this product.

Adult↗
PubMed1988

Vaginal bromocriptine: pharmacology and effect on serum prolactin in normal women.

Oral bromocriptine treatment of hyperprolactinemia is frequently associated with gastrointestinal side effects. To assess the efficacy and safety of an alternate route of treatment, we randomly administered 2.5, 5.0, and 7.5 mg of bromocriptine vaginally to five normal women at 1-week intervals. Plasma bromocriptine and prolactin (PRL) levels were measured hourly for 12 hours, then every 2 hours for 12 hours after each dose. At the end of each study, the vagina was flushed with saline for measurement of residual drug. For comparison of serum PRL levels, six additional women were given 2.5 mg bromocriptine orally. After administration of 2.5, 5.0, and 7.5 mg vaginally, plasma bromocriptine was initially detectable at 5.4 +/- 0.4, 4.4 +/- 0.7, and 3.5 +/- 0.6 hours, respectively. For the same vaginal doses, the mean (+/- SEM) peak plasma levels were 555 +/- 164 pg/mL at 12 +/- 0.6 hours, 702 +/- 252 pg/mL at 11.2 +/- 0.9 hours, and 1055 +/- 220 pg/mL at 10.7 +/- 1.7 hours, respectively. After each dose, there was a slow decline in plasma bromocriptine levels, remaining above 50% of peak values at 24 hours. Less than 1% of the administered drug was recovered from the vagina at 24 hours. The pattern of PRL inhibition with all three doses was similar. The mean plasma PRL level decreased by 7 hours, the maximum PRL decrease (64 +/- 3, 75 +/- 1, and 66 +/- 4% after 2.5, 5.0, and 7.5 mg, respectively) occurring at 11 hours, and the plasma PRL levels changed little during the remaining 13 hours.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Intravaginal↗
PubMed1988

Dissolution of metronidazole from oral and vaginal dosage forms in sink and non-sink conditions.

The pharmaceutical availability of metronidazole from several commercial oral and vaginal dosage forms in sink and non-sink conditions has been examined by measuring the rate of drug dissolution. The results were interpreted by means of reversible and irreversible dissolution models. For non-sink conditions the reversible model was found to better interpret the data. The values of the relative dissolution rate constant, theoretical dissolution time and dissolution efficiency were obtained and discussed.

Administration, Intravaginal↗
PubMed1987

Nonoral routes of estrogen administration.

Thus, the effects that a specific estrogen has on the liver is the summation of several mechanisms, including the first pass mechanism and the enhanced delivery of circulating estrogens to this organ. For example, the major estrogen in conjugated estrogen is estrone sulfate. Based on the present data, very little circulating estrone sulfate is available to the brain or uterus (Fig. 25). Since most of the hypothalamus is behind the blood-brain barrier, it is unlikely estrone sulfate exerts a direct action on gonadotropin-releasing hormone (GnRH) neurons to reduce its secretion and, subsequently, gonadotropin levels. Estrone sulfate also does not interact with the estrogen receptor. It is possible the small amount of estrone sulfate that crosses the blood-brain barrier is converted to unconjugated estrogens locally and these could have function. More likely, the major mechanism by which estrone sulfate suppresses GnRH release is through conversion to unconjugated estrogens, principally estrone, in the liver. The large extraction of estrone sulfate by the liver allows accessibility of the hepatocyte for this conversion. Based on this concept, conjugated estrogen must enter the liver to be converted to its active forms. The route of administration then should have little impact on changing the relative potency of this preparation on hepatic and nonhepatic markers of estrogen action. For ethinyl estradiol, the preparation is orally active because it is rapidly and almost completely absorbed from the stomach and undergoes limited hepatic metabolism before entry into the general circulation (Fig. 26). This limited hepatic metabolism reduces the impact of the first pass mechanism on ethinyl estradiol. Thus, the enhanced hepatic action of ethinyl estradiol is principally related to the greater entry of this estrogen into the liver than other organs (Fig. 27). Consequently, the route of administration should have little impact on the exaggerated hepatic actions of this estrogen. Orally administered estradiol undergoes substantial hepatic metabolism to less active forms, principally estrogen conjugates. The amount of estradiol leaving the liver following oral administration is substantially less than that which enters it through the portal vein. The systemic administration of estradiol avoids this initial hepatic metabolism. Furthermore, only 25 per cent of nonorally administered estrogen will go to the liver at each pass, and nonhepatic tissues would be exposed to a greater extent than after oral administration. Thus, peripheral administration of estradiol reduces the exaggerated hepatic responses in comparison to nonhepatic actions.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Cutaneous↗