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PubMedDate not supplied

[Effect of novocaine incorporation into the structure of a water-soluble polymer on its pharmacological activity].

The topically anesthesizing action and acute toxicity of two polymetric derivatives of novocaine-celnovocaine and polynovocaine No 5 (PN-5) were studied. The polymeric derivatives differ in the orientation of the novocaine molecule with respect to the macro-molecule of the water-soluble polymer-the modified cellulose. In celnovocaine novocaine joins the macromolecule through the intermediary of diethylamino-ethanol nitrogen and in PN-5-through the intermediary of paraaminobenzoic acid nitrogen. The ratio of the polymer-carrier (mol. weight 20 000-26 000) to novocaine is 1:1. The chemical bonding between novacaine and modified cellulose potentiates ad prolongs the infiltrative and terminal anesthesia, without changing (PN-5) or lowering (celnovocaine) the toxicity. The extent to which the action and duration of the effect, as well as changes in the toxicity depend upon the orientation of the novocaine molecule relative to the water-soluble polymer molecule.

Animals↗
PubMed1977

[Long-acting local anesthetics - an enrichment in ophthalmosurgery? (author's transl)].

In 300 cases the effectiveness of the long-acting anesthetic Meaverin-ultra for retrobulbar anesthesia was systematically investigated. The duration of analgesis and immobilisation for the globe as well as for the eyelids runs over hours; they are considerabley more effective than with other common local anesthetics so far. 91% of the patients got free of pains for more than 24 hours after the operation. As to the interruption of pain attacks in cases of haemorrhagic glaucoma painless intervalls of more than 30 hours were reached. Special advantages result in cases of buckling operations for retinal detachment, which have to be followed by photo-(xenon)-coagulation. On the whole, long-acting anesthetics are an extraordinary gain for ophthalmosurgery.

Anesthetics, Local↗
PubMedDate not supplied

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↗