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At least 19 recordsLinked to original sources
PubMed1975

Effects of 5-hydroxytryptamine on fertility and luteal development following intravaginal administration in the rat.

Intravaginal administration of 5HT was effective in terminating pregnancy when given after implantation in the rat, provided that the tampon was allowed to remain in the vagina for 4 hr or more. Complete antifertility efficacy was associated with a prevention or reversal of the increase in ovarian weight, which occurs in untreated rats between Days 12 and 17 of pregnancy, and correlates with enlargement of the CL. Data from hysterectomized, ovariectomized and progesterone-implanted rats indicated that the effect on CL was not a cause of the antifertility effect. Intravaginal administration of 5HT was found to lead to general systemic effects.

Animals↗
PubMed1987

Intravaginal administration of RU 486 in humans and rats: inadequate absorption in humans.

Vaginal absorption of the antiprogesterone steroid RU 486 was studied in humans and rats. In rats, RU 486 was sufficiently absorbed to terminate early pregnancy following vaginal, oral or intramuscular administration. The quantitation of RU 486 in serum showed that the ratios of the areas under the concentration curves per mg administered were 1:2.8:3.4 for the vaginal, intramuscular and oral routes, respectively. Female volunteers received RU 486 vaginally in polyethylene glycol (PEG) suppositories, in tampons and in oil solution. Following vaginal (PEG-suppository) and oral administration of 100 mg of RU 486, the ratio of the areas under the serum concentration curves was 1:56, respectively. From tampons and oil, RU 486 was absorbed in a similar manner to that of the PEG-suppositories, resulting in nanomolar serum concentrations. In humans no biological effects were noted following vaginal administration of RU 486. These data suggest that vaginal release of RU 486 is not a successful route of administration in humans.

Administration, Intravaginal↗
PubMed1992

[Clinical studies on intravaginal administration of CDDP for dysplasia, carcinoma in situ and microinvasive carcinoma of the uterine cervix].

We attempted CDDP (cis-diaminedichloroplatinum) intravaginal administration by directly exposing the uterine cervix to CDDP in cases of dysplasia of the uterine cervix and cervical intraepithelial and micro-invasive carcinoma. Out of 12 patients, 7 had dysplasia of the uterine cervix (dysplasia was mild in 4, of an intermediate level in 1, 4 with mild dysplasia, 1 with and advanced in 2); 3 had carcinoma in situ, and 2 had microinvasive carcinoma. For CDDP intravaginal administration, a gauze tampon containing CDDP (5mg) was inserted into the vagina. CDDP administration was repeated daily for 10 days. The total dosage of CDDP administered was 50mg (new paragraph). During this period, vaginal cytologic examination was conducted and total plasma Pt content was determined daily for all. Following the completion of CDDP administration, the uterine cervices of those with dysplasia were histologically examined. For those with carcinoma in situ and microinvasive carcinoma, simple total hysterectomy was performed after intravaginal administration of CDDP to determine its therapeutic efficacy and the Pt concentration of the tissue; 1. In the 7 cases of dysplasia, dysplastic cell degeneration was observed 1-2 days after the start of intravaginal CDDP administration and these cells disappeared in all cases after its completion. 2. Sixteen histological sections of the resected cervical specimens from the 3 cases of carcinoma in situ showed complete disappearance of cancerous cells. 3. In the 2 cases of microinvasive carcinoma, no tumor cells were detected in one case; in the other case, tumor cells persisted in part of the resected specimen.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Intravaginal↗
PubMed1982

Midtrimester pregnancy termination by intravaginal administration of prostaglandin E2.

The intravaginal administration of prostaglandin E2 (PGE2) in repeated doses of 20 mg was evaluated for efficacy and safety in 400 midtrimester pregnancy terminations. Patients were assigned to three treatment groups. Group A (232 patients) received PGE2 alone, Group B (106 patients) had prior intracervical laminaria insertion, Group C (62 patients) received both laminaria and continuous intravenous oxytocin infusion. Complete abortion was achieved in 328 cases (82 per cent) and there were 13 failures (3.3 per cent). Mean instillation treatment groups were not statistically significant but outcome was more favorable in pregnancies of 16 to 19 weeks' gestation as compared with those between 13 and 15 weeks. Gastrointestinal symptoms and temperature elevation constituted the most frequent side effects. Excessive blood loss occurred in 11 cases (2.8 per cent) and live births were encountered in 12 cases (3.0 per cent). Vaginal PGE2 is felt to be particularly acceptable for the termination of pregnancies of 16 to 19 weeks' gestation.

Abortion, Induced↗
PubMedDate not supplied

Pharmacokinetics of progesterone in postmenopausal women: 1. Pharmacokinetics following intravaginal administration.

Progesterone was administered to postmenopausal women in a form of vaginal suppositories containing 100 and 200 mg active substance in Butyrum cacao (BC) and Massa estarinum (ME), a base with emulsifying properties. In the case of single doses, blood samples were taken at 2, 4, 6, 24, 48 and 72 h. Another group of patients received vaginal suppositories (100 mg progesterone) once a day for a 6 day period, with blood samples taken 12 h after each administration. The plasma levels of progesterone were evaluated by radioimmunoassay. The time of maximum concentration (tmax) was 4 h in most cases, and 6 h in the others. The plasma levels were not dose-proportional. Peak plasma concentrations were in the range of 10-15 ng/ml with a mean of 10.5 ng/ml for the 100 mg and 12 ng/ml for the 200 mg doses. The ratio of the mean area under the curve (AUC) for 200 mg and the mean AUC for the 100 mg dose was found to be 1.37. Replacing BC with ME resulted in the lowering of cmax and AUC, and an increase in tmax following a reducing in the rate and extent of adsorption. In the case of ME suppositories, the variability in AUC, cmax and tmax was greater compared to that observed with the BC suppositories. Elimination half-time was in the range of 9-10 h for BC and 14 h for ME suppositories. In vitro assessment of the release kinetics from a hydrophobic and an emulsion type base confirmed previous findings: the latter base assured better pharmaceutical availability. The repeated doses did not seem to produce an accumulation of progesterone in the plasma. On the contrary, a small decrease in plasma levels over time appeared during the 6 day period. Numerical analysis revealed an excellent goodness of fit for the in vivo experimental data via biexponential curves, i.e. a pseudomonocompartmental model.

Administration, Intravaginal↗
PubMed1991

[Intravaginal administration of CDDP for adenocarcinoma].

Single vaginal administration of CDDP was done in a case of adenocarcinoma when relapse in the vaginal stump followed surgery for uterine corpus carcinoma. A tumor the size of a large fingertip in the vaginal stump was completely eliminated via 15-time (75 mg) CDDP vaginal administration, suggesting that this treatment was effective against adenocarcinoma. The only side effect over the whole body was slight pain developing in the external genitalia.

Adenocarcinoma↗
PubMed1990

[Intravaginal administration of CDDP in cervical cancer].

An 84-year-old woman was seen on June 19, 1989 with the chief complaint of excessive abnormal genital bleeding of 10 days' duration. The patient was diagnosed as FIGO stage IV b (positive metastasis to lung and Virchow's nodes) and was urgently admitted because of massive bleeding, which was well controlled by whole pelvic irradiation (Lineac 3,000 rad). However, subsequent 3 courses of systemic combination chemotherapy including cisplatin delivered progressing disease (PD) with the evidence of exacerbation of primary and metastatic lesions. In such an intelligible case, authors applied 5 mg of CDDP for 13 consecutive days directly into the vaginal wall and made a pharmaco-dynamic kinetic study by measuring the blood and tissue Pt concentration. Cyto- and pathological analysis of tissue specimen revealed that this topical used of low-dose consecutive CDDP was effective for local tumor control even after failure of systemic chemotherapy.

Administration, Intravaginal↗
PubMed1993

The pharmacokinetics and absorption of recombinant human relaxin in nonpregnant rabbits and rhesus monkeys after intravenous and intravaginal administration.

Recombinant human relaxin (rhRlx) is being developed as a potential cervical ripening agent to be applied intravaginally or intracervically prior to parturition. The pharmacokinetics and absorption of rhRlx were determined in nonpregnant female rabbits and rhesus monkeys after intravenous bolus (iv) and intravaginal administration of 0.1 mg/kg; additionally, rabbits were dosed with 0.5 mg/kg intravaginally. In rabbits (n = 6), mean (+/- SD) peak concentrations following iv bolus administration were 1554 +/- 296 ng/mL. The weight-normalized clearance (CL/W) was 5.9 +/- 0.4 mL/min/kg, initial volume of distribution (V1/W) was 57 +/- 9 mL/kg, and volume of distribution at steady state (Vss/W), assuming central compartment elimination, was 240 +/- 20 mL/kg. Vss/W could be as large as 2000 +/- 400 mL/kg without this assumption. The estimated amounts of rhRlx absorbed in rabbits following intravaginal administration of 0.1 and 0.5 mg/kg (n = 5/dose) were 3.1 +/- 1.4 and 0.7 +/- 0.3%, respectively; peak concentrations were 600 +/- 297 and 1066 +/- 584 pg/mL, respectively. In rhesus monkeys (n = 5) after iv administration, peak concentrations were 971 +/- 277 ng/mL; CL/W was 4.1 +/- 0.6 mL/min/kg, V1/W was 78 +/- 25 mL/kg, and Vss/W, assuming central compartment elimination, was 690 +/- 220 mL/kg. The upper limit for Vss/W was 1600 +/- 200 mL/kg when no assumptions were made regarding site (compartment) of elimination. After intravaginal administration (n = 6), two monkeys had undetectable rhRlx concentrations throughout the 48-hr sampling interval; one monkey had only one sample containing measurable rhRlx (51 pg/mL) at 24 hr; and three monkeys absorbed < 2% of the 0.1 mg/kg dose.(ABSTRACT TRUNCATED AT 250 WORDS)

Absorption↗
PubMed1981

Preliminary results, serum chemistry values before and after the intravaginal administration of 5% nonoxynol-9 cream.

Thirty-two healthy premenopausal women between the ages of 18 and 39 were randomly assigned to three study groups as follows: Group I received daily intravaginal administration of 2.5 gm of 5% nonoxynol-9 vaginal cream (Conceptrol [Ortho Pharmaceutical Corporation, Raritan, N. J.] cream) for 14 days. Group II received daily intravaginal administration of 2.5 gm of the cream base alone, and group III received no treatment. The numbers of subjects completing the study were 12, 11, and 7 groups I, II and III, respectively. Fasting blood samples were obtained from each subject prior to treatment and on days 8 and 15 after treatment. Blood samples were analyzed for 20 constituents, including proteins, lipids, triglycerides, and serum enzymes. There were no differences in any of the measured parameters between the pre- and post-treatment periods in any of the groups. On the basis of these findings it may be concluded that there are no apparent systemic effects following daily intravaginal administration of a 125-mg dose of nonoxynol-9 in a cream base for 2 weeks.

Adolescent↗
PubMed1987

[Labor induction by intravaginal administration of prostaglandin E2 tablets].

Between 1982 and 1984, at Graz University Obstetric and Gynaecological Clinic, labour was induced in 307 women (146 primiparae and 161 multiparae) by intravaginal administration of 3 mg prostaglandin (PG) E2 tablets, because birth was overdue or because labour was irregular. No risk factors were present when PG was administered: signs of deficiency or postmaturity, or twisted cord, were ruled out. The following complications were evaluated: birth rate and induction-birth interval in relation to cervical maturity and parity. The number of complications was low. It was unrelated to cervical maturity and only partially to parity. Birth was induced successfully with a single dose of 3 mg PG E2 in over 80% of the primiparae and over 90% of the multiparae. The majority of the primiparae and all the remaining multiparae were successfully delivered with a second dose; no relationship between birth rate and cervical maturity was established. Among the primiparae with a low degree of cervical maturity the child was born within 12 hours in over 50% of the cases, among primiparae with more mature cervices in almost 90%. Among the multiparae, the child was born within 12 hours in 90% of the cases regardless of the state of cervical maturity. It is concluded from these results that with appropriate monitoring of birth, intravaginal administration of PG E2 tablets is an efficient and easily managed method of inducing birth at term, involving little risk.

Administration, Intravaginal↗
PubMed1992

HPLC method for pharmacokinetic studies on ciclopirox olamine in rabbits after intravenous and intravaginal administrations.

This paper reports a HPLC method to detect unchanged and glucuronide derivatives of ciclopirox olamine (a substituted 2-pyridone antimycotic) and gives pharmacokinetics in rabbits after i.v. and intravaginal administration. The HPLC method utilizes a RP 18 reverse phase column, a mobile phase of water and acetonitrile (60/40), a flux of 1 ml/min and wavelength of 304 nm. For the determination of free ciclopirox the plasma drug is methylated with dimethyl sulphate, extracted with n-exane, purified on Adsorbex CN and injected into the column. For the determination of total (free and glucuronide derivatives) ciclopirox the plasma is previously hydrolized with beta-glucuronidase before the application of the above procedure. In rabbits the drug is administered at 15 mg/kg for both routes; the t1/2 elim is 2.1 hours, the total clearance/F is 0.73 1.h-1 and the distribution volume/F is 2.2 1. Ciclopirox olamine, after intravaginal administration, shows low absorption (about 2%) and is mainly transformed into glucuronide derivatives.

Administration, Intravaginal↗
PubMed1975

Midtrimester abortion induced by serial intravaginal administration of prostaglandin E2 suppositories in conjunction with a contraceptive diaphragm.

Midtrimester abortion was successfully induced in 68 of 69 patients with serial intravaginal administration of prostaglandin E2 suppositories behind a contraceptive diaphragm. The mean abortion time for the successful inductions was 13.07 hours; multiparous patients aborted somewhat faster, mean 12.72 hours, as compared to nulliparous patients, mean 14.22 hours. In 36 patients the PGE2 suppositories were placed behind an intact diaphragm and the mean abortion time was 14.89 hours. In 33 patients the PGE2 suppositories were placed behind a diaphragm modified by having an opening incised in the center, the mean time in these patients was 11.96 hours. Of the 68 successful abortions 59% of the patients aborted in 12 hours or less and 88% aborted within 24 hours. The most frequently encountered side effect was temperature elevation of 2 degrees F or higher which occurred in 68% of the patients. Temperatures returned to normal levels within 4 to 6 hours after the last adminstration of PGE2. Gastrointestinal side effects occurred in 45% of patients, but these side effects were well tolerated and did not require termination of drug administration in any of the patients. Intravaginal administration of PGE2 suppositories is a very effective abortifacient technque during the midtrimester, however the use of PGE2 in conjunction with a diaphragm did not appreciabley improve the technique although the amount of drug administered and the incidence of side effects was somewhat lower than when the PGE2 suppositories are used alone. If a diaphragm is to be used, a modified diaphragm is indicated since it simplifies the clinical management of the abortion, eases administration of the suppositories and permits a more accurate estimation of cervical changes, vaginal bleeding and abortion.

Abortion, Induced↗