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Results of treatment of ocular toxoplasmosis with injectable corticosteroids.

Sixty-seven patients with toxoplasmic retinochoroiditis who were treated with periocular injections of depot forms of corticosteroids were studied in an attempt to determine (1) whether patients who did poorly on this regimen could be differentiated predictively from those who responded in a more favorable fashion, and (2) whether a treatment regimen that would allow the safe use of periocular depot corticosteroids in patients with toxoplasmic retinochoroiditis could be delineated. The study did not reveal any reliable way of predicting which patients would be good risks for the use of periocular injections of depot corticosteroids. It does suggest that the concurrent use of antitoxoplasma agents might protect patients in such a way that periocular depot corticosteroids would not worsen their disease. For the reasons outlined, the use of periocular injections of depot corticosteroids in toxoplasmic uveitis must be approached with great caution in the future.

Adult↗
PubMed1977

[Comparison of vaginal cytologic effects and blood elimination curves of different oestrogen drugs (author's transl)].

With different oral oestrogens it was studied, if relations are existing between pharmacokinetic and vaginal effect. By means of Karyopycnotic Index and Dynamic Oestrogenicity Index the cytological effect was quantified from a single dose of oestradiol valerianate, mestranol, ethinyloestradiol and 3 depot oestrogens proved on postmenopause women and compared with adequate pharmacocinetical investigations. The courses of oestrogen levels did not correlate with indices. Both methods of investigation do not compensate, but complete one another. Depotoestrogens and short acting oestrogens are distinguishable with regard to proliferation maxium and steepness of index decline.

Delayed-Action Preparations↗
PubMed1976

Long-term contraception with norethindrone subcutaneous capsules.

Norethindrone (NET) contained in silicone rubber, for slow release, was implanted subcutaneously. The rate of release of NET was 10-12 mug/day/10 mm length of the silicone rubber. The total length of the implants used varied from 100 mm to 200 mm. During the whole observation time 562 women months, 14 a-cidental pregnancies occurred. The pregnancy rate decreased with increasing length of implants. The implants produced a transient ovulation suppression, which subsided in four to five cycles. The plasma levels of NET stabilized at a level which was less than that reached by daily oral administration of 350 mug of NET. The high pregnancy rate and the great number of implants required render the method impractical for contraception. However, the active life-span of implants is three years and because there were few minor side-effects, the method was well accepted.

Contraception↗
PubMed1976

[Depoteffect of benzathine-penicillin (author's transl)].

15 test persons received an injection of 2,400,000 units of benzathine penicillin. Serum levels were subsequently assayed, as well as the excretion of the antibiotic in the urine. The samples were stored in liquid-nitrogen between collection and examination. Each of the speciemens was tested 5 to 10 times and the results were ascertained by empirical evaluation of every single analysis. This assay showed the existence of mean levels above 0.036 I.U./ml in the serum and above 19.75 I.U./ml in the urine for the duration of 26 days. The evaluation of serum levels after the administration of antibiotics is difficult due to several sources of error. Reliable results can, therefore, be obtained only by examination at special institutes which possess experienced technical personnel. The establishment of reference laboratories for this purpose is suggested. The results of the study confirm the efficacy of one-shot treatment of the syphilis by administration of 2,400,000 to units of benzathine penicillin.

Delayed-Action Preparations↗
PubMed1976

Pharmacy, pharmaceutics and modern drug delivery.

Recent developments in the area of drug delivery are reviewed. Controlled delivery of drug substances (including controlled-release oral products, the Folkman-Long silastic device and membrane-medicated delivery systems) are discussed. The prodrug approach is illustrated by discussion of the esterification of epinephrine and the production of the dihydro form of 2-PAM (pro-2-PAM). It is suggested that the pharmacist study the release pattern of drug devices and the pharmaceutics of prodrugs in order to maintain his responsibility as the expert on drugs.

Chemistry, Pharmaceutical↗
PubMed1976

[Comparative characteristics of the serotonin and histamine content in the blood of surgical patients before and after antibiotic administration against a background of droperidol, promedol and atropine premedication].

The effect of intramuscular administration of ceporin and megacillin in single doses of 500 mg and 1000000 Units respectively on serotonin and histamine blood levels in 34 patients against the background of premedication with droperidol, promedol or atropine was studied. The observations showed that after megacillin injection the serotonin blood levels decreased. Ceporin had no effect on serotonin and histamine blood levels.

Adolescent↗
PubMed1976

The use of silastic vaginal device containing (15S)-15 methyl prostaglandin F2 alpha methyl ester for early first trimester pregnancy termination.

(15 S) - 15 methyl prostaglandin F2 alpha methyl ester in a silastic vaginal device was administered to 9 gravid women in the first 7 weeks of gestation for elective termination of pregnancy. Continuous intrauterine pressure recording was carried out in one case. Prompt initiation of uterine activity and vaginal bleeding was seen and expulsion of products of conception occurred in under 24 hours in all cases. There were no serious complications and side effects were considered acceptable. Two patients have required subsequent curettage for removal of retained placental tissue. This incidence of failure to complete expulsion, if confirmed in a larger series, is considered to render this technique without modification unacceptable as a routine method for early pregnancy termination.

Abortion, Induced↗
PubMed1976

First experiences with a (15S)-15-methyl prostaglandin F2alpha vaginal device for termination of early first trimester pregnancy with serial sonographic observations.

A silastic device containing 10 mg (15S)-15-Methyl Prostaglandin F2alpha was administered vaginally in three parous patients under 50 days gestation who requested therapeutic abortion. Painful contractions appeared within one hour and vaginal bleeding within three hours of application. All patients aborted, although in one tissue had to be removed from the uterus. Plasma progesterone concentrations were measured in two patients: they decreased within four hours, then increased slightly and finally decreased 24 hours after administration of the device. Nausea, vomiting, and diarrhea were observed in all three patients. The estimated blood loss was less than 100 ml and no significant hematocrit changes were observed in all patients. In serial sonographic examinations of one patient, the fragmentation and dislodgment of the gestational sac could be observed within six hours after administration of the device. After these albeit limited experiences, it is concluded that the (15S)-15-Methyl PGF2alpha vaginal device is of great potential value for induction of early first trimester abortion.

Abortion, Induced↗
PubMed1976

Induction of abortion by vaginal administration of 15(s)15-methyl prostaglandin F2alpha methyl ester. A comparison of two delivery systems.

15-methyl PGF2alpha methyl ester in a slow releasing vaginal device was administered to 30 women in the first and second trimester of gestation. Ten women were early pregnant (31-49 days following the last menstrual period) and the remaining 20 patients in the 10th to 20th week of gestation. The first group received either a device containing 10 mg 0.5% 15-methyl PGF2alpha methyl ester or a half of that device and the second group either a 0.5% or 1% device. The results were compared with those found following repeated vaginal administration of triglycerides suppositories, containing 15-methyl PGF2alpha methyl ester, to 50 early pregnant patients and 30 patients in the second trimester of gestation. The mean total dose of the compound given to these two groups was 3.9 and 7.8 mg respectively. All the 60 early pregnant patients aborted following treatment judged from clinical course and decreasing HCG values. Bleeding started as a rule three to six hours following the start of treatment and continued for 10 to 14 days. In two patients the abortion was incomplete. The side effects in the patients who received half the 0.5% device was comparable to those following the repeated vaginal suppositories while in the patients who obtained the whole 0.5% device, the frequency of side effects was increased indicating that an unnecessary high dose was given. In all the three groups of patients in the late first and second trimester of pregnancy, treatment resulted in abortion within 24 hours in 90% of the patients. In the 1% device an accumulation of side effects was found during the first hours following the start of treatment probably due to an initial, more rapid absorption of 15-methyl PGF2alpha methyl ester. With the repeated administration and with the 0.5% device, the side effects occurred mainly in the hours prior to abortion. However, in all three groups of patients the side effects were within acceptable levels. These preliminary results indicate that further development on the device may result in an effective one vaginal administration treatment for termination of both first and second trimester pregnancies.

Abortion, Induced↗
PubMed1976

Hormone release and abortifacient effectiveness of a newly developed silastic device containing 15-ME-PGF2alpha methyl ester in concentrations of 0.5% and 1.0%.

Abortion was successfully induced by intravaginal administration of a newly developed silastic device impregnated with 15(S)-15-methyl-prostaglandin F2alpha methyl ester in a concentration of 0.5% in 26 of 35 women in the 12th to the 24th weeks of gestation and by prostaglandin with concomitant oxytocin infusion in an additional 5 patients. A second comparable group of 35 women, with gestational ages from 9 to 23 weeks, received a silastic device with a concentration of 1.0% of the prostaglandin. Twenty-six women in the second group aborted with prostaglandin alone and an additional 6 patients aborted with combined prostaglandin-oxytocin therapy. Seven patients of the 70 included in this study failed to abort with intravaginal administration of 15-ME-PGF2alpha methyl ester even with concomitant oxytocin therapy; this group included 4 patients receiving the 0.5% device and 3 patients with the 1.0% device. The mean abortion time for the 31 successful abortions with 0.5% device was 15.15 hours and multiparous patients aborted in a mean time of 9.69 hours, significantly faster than the nulliparous patients, mean time 18.49 hours. The mean abortion time for the 32 successful abortions with the 1.0% device was 15.61 hours and there was no significant difference in the mean abortion times between nulliparous and multiparous patients in this group. No significant difference could be demonstrated between the mean abortion times of patients receiving an 0.5% concentrations of prostaglandin and patients receiving a 1.0% concentration of the drug. In both groups more than 40% of the patients had aborted within 12 hours of the insertion of the prostaglandin device and more than 80% had aborted within 24 hours. The intravaginal device appeared to be effective in inducing abortion throughout the gestational ages tested in this series. Peripheral plasma levels of 15-ME-PGF2alpha were analyzed in 15 patients with the 0.5% device and 8 patients with the 1.0% device. In patients with the 0.5% device the mean plasma concentration of prostaglandin peaked 2 hours after insertion, while in patients with the 1.0% device the peak was achieved within 15 minutes of insertion followed by a rapid decline in plasma prostaglandin levels. Diarrhea was the most frequent side effect related to the intravaginal administration of the prostaglandin, and in this series the severity of this gastro-intestinal disturbance appeared to be significantly higher in patients receiving the 1.0% device.

Abortion, Induced↗