ABSTRACT
The synthetic analogous of the prostaglandins are utilized in the obstetrical and gynecological therapy for multiple purposes. 4 lots with 12 nonpregnant female rats were use: the Ist received 25 g/kg/day isopropyl ester PGF2; the IInd lot received 50 g/kg/day isopropyl ester PGF2; the IIIrd lot received 50 g/kg/day optic active cloprostenol; the IVth lot was the witness lot. The medication was intraperitoneally (i.p.) administrated in a unique daily dose. Prostaglandin F2 analogous at small doses (25 micrograms/kg/day) induce vasodilating effects on the ovary blood vessels and functional luteolysis rather than structural luteolysis. Both of the prostaglandins analogous at doses of 50 micrograms/kg/day present obvious vasodilating and luteolytic effects, although the intensity of the phenomenon is not the same, cloprostenol is more active, inducing a more obvious vasodilatation and luteolysis.
Subject(s)
Cloprostenol/pharmacology , Dinoprost/analogs & derivatives , Fallopian Tubes/drug effects , Ovary/drug effects , Animals , Dinoprost/pharmacology , Dose-Response Relationship, Drug , Epithelium/drug effects , Epithelium/pathology , Fallopian Tubes/pathology , Female , Ovary/blood supply , Ovary/pathology , Rats , Statistics, Nonparametric , Time Factors , Vasodilation/drug effectsABSTRACT
Four prostaglandin compounds synthetized at ICCF [chloprostenol triacetate (a), the isopropylic ester of the chloprostenol analogue (b), a PGA2 sulprostone analogue (c) and a PGE2 analogue (d)] were tested with respect to the cytotoxic effect, by successive studies on chicken embryo fibroblasts (CEF) and on human cells (HeLa). It was established that (b) and (d) display a high cytotoxicity, while (a) and (c) were relatively well tolerated by the cell layer. The spectrofluorometric determinations showed that these drugs did not induce modifications at the cell membrane level. The treatment with 4 micrograms/ml PGs (a) and (c) of HeLa cells inoculated with Sendai virus produced a significant decrease of TCID50/ml 24 hrs after drug introduction into the culture medium, from 10(6.5) to 10(4.5) and to 10(3.25), respectively.
Subject(s)
Antiviral Agents/pharmacology , Prostaglandins/pharmacology , Respirovirus/drug effects , Animals , Antiviral Agents/chemical synthesis , Cell Membrane/drug effects , Chick Embryo , HeLa Cells , Humans , Molecular Structure , Prostaglandins/chemical synthesis , Respirovirus/growth & developmentABSTRACT
The theoretical part of this paper presents the mechanism of the IOP lowering effect using these drugs, the indications of treatment and the main side effects. The second part consist of the experimental study made on rabbits, using the izopropilic ester of (+)Cloprostenol as an hypotensive agent. We have registered the IOP values and the main side effect--conjunctival hyperemia. The third part consist of the clinical study, made on a test lot of 23 patients. We have used the same substance and in the experimental study, as a unique treatment or in association with a beta-blocker or a pilocarpine derivative. The following-up has implied: the IOP, the ophthalmoscopic appearance of the optic disc, the visual field, the visual acuity and the main side effects. In the end, we have formulated the conclusions of these studies.
Subject(s)
Glaucoma/drug therapy , Prostaglandins, Synthetic/therapeutic use , Adrenergic beta-Antagonists/therapeutic use , Adult , Aged , Animals , Cloprostenol/adverse effects , Cloprostenol/therapeutic use , Drug Evaluation , Drug Evaluation, Preclinical , Drug Therapy, Combination , Female , Glaucoma/physiopathology , Humans , Intraocular Pressure/drug effects , Male , Middle Aged , Pilocarpine/therapeutic use , Prostaglandins, Synthetic/adverse effects , RabbitsABSTRACT
We tested the influence of 30 mg/kg/per os BN 52021, 300 micrograms/kg Cloprostenol (CIPG) and of 5 mg/kg per os LY 171883B in stress restrain and indomethacin induced ulcers in rats. The data obtained show that CIPG and LY 171883 have a significant gastroprotective action in both ulcer models. BN 52021 has a significant protective activity in stress ulcer and less in indomethacin-induced ulcers.
Subject(s)
Acetophenones/pharmacology , Cloprostenol/pharmacology , Diterpenes , Lactones/pharmacology , Stomach Ulcer/prevention & control , Tetrazoles/pharmacology , Animals , Dinoprost/analogs & derivatives , Ginkgolides , Indomethacin , Leukotrienes/pharmacology , Male , Platelet Activating Factor/antagonists & inhibitors , Rats , Rats, Wistar , Restraint, Physical , Stomach Ulcer/chemically induced , Stomach Ulcer/etiology , Stress, Physiological/complicationsABSTRACT
We studied the influence of cloprostenol (CIPG) 200 micrograms/Kg i.p. (a synthetic analogue of PGF2-alpha) and of imidazol 70 mg/Kg i.p. (a selective inhibitor of thromboxane synthetase) on fasting glycemia and on hypoglycemia induced by Actrapid insulin 0.5 UI/Kg i.p. to rats (male adults). The determinations of glycemia were made 60 minutes and 3 hours after the administration of the substances. The tests were made in groups of 20 animals which were not fed 14 hours before the experiment, but were not deprived of water. The results were interpreted statistically by means of the "t" test. The data obtained show that CIPG 200 micrograms/Kg i.p. is a significant hyperglycemic icosanoid (statistically p less than 0.01) both in the case of fasting glycemia and in the case of insulin hypoglycemia. The hyperglycemic effect was stronger at 60 min. Imidazol does not modify significantly either glycemia or insulin hypoglycemia, which pleads for a more reduced implication of thromboxanes in the regulation of glycemia in comparison to the prostaglandins.
Subject(s)
Blood Glucose/metabolism , Cloprostenol/pharmacology , Hypoglycemia/chemically induced , Imidazoles/pharmacology , Insulin/pharmacology , Prostaglandins F, Synthetic/pharmacology , Animals , Hypoglycemia/blood , Hypoglycemia/metabolism , Insulin, Regular, Pork , Male , Rats , Thromboxane-A Synthase/antagonists & inhibitorsSubject(s)
Blood Glucose/metabolism , Thromboxanes/metabolism , Animals , Fasting , Glucose/administration & dosage , Hyperglycemia/etiology , Hyperglycemia/metabolism , Imidazoles/pharmacology , Male , Prostanoic Acids/pharmacology , Rats , Receptors, Prostaglandin/drug effects , Receptors, Prostaglandin/metabolism , Receptors, Thromboxane , Thromboxane A2/antagonists & inhibitors , Thromboxane-A Synthase/antagonists & inhibitors , Thromboxanes/antagonists & inhibitors , Time FactorsABSTRACT
Alkyl-1-biguanides are determined by titration with copper(II), or excess of copper(II) is added and the surplus determined by titration with EDTA, a liquid-state copper-sensitive electrode being used in both cases for potentiometric detection of the end-point.
