PubMed Health⌕ Search

SEARCH · PubMed Health

Results for “Prostaglandins, Synthetic”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 19 recordsLinked to original sources
PubMed1986

Treatment of duodenal ulcer with enprostil, a synthetic prostaglandin E2 analogue.

Enprostil is a synthetic prostaglandin E2 analogue developed by Syntex. In a randomized, double-blind trial involving 128 patients with duodenal ulcer disease, four weeks of treatment with enprostil at doses of 70 micrograms twice daily and 35 micrograms twice daily produced healing rates (78 percent and 65 percent, respectively) that were statistically significantly higher than the placebo rate (39 percent; p less than 0.05). In a subgroup of smokers, ulcer healing occurred with statistically significantly greater frequency at both the high dose (70 percent) and the low dose (60 percent) when compared with the rate in the placebo group (32 percent; p less than 0.05). The only clinically important side effect was diarrhea, which was generally mild, self-limited, and of short duration. This study demonstrated that enprostil is highly effective in the treatment of duodenal ulcer and has a favorable safety profile.

Adolescent↗
PubMed1979

The effects of synthetic prostaglandin analogs on canine hepatic bile flow.

The synthetic prostaglandin analogs 16, 16-dimethyl PGF2 alpha and 16, 16-dimethyl PGE2 were administered to dogs with chronic biliary and gastric fistulas. The effects of 16, 16 diMePGF2 alpha and 16, 16 diMePGE2 were evaluated on bile flow and composition and bile adenosine 3', 5' monophosphate (cyclic AMP) secretion. 16, 16 diMePGF2 alpha in doses of 0.125 and 0.25 microgram-kg-min significantly increased hepatic bile flow. The choleresis was characterized by increased chloride and bicarbonate secretion. Measurement by radioimmunoassay of bile cyclic AMP concentration demonstrated no evident increase in bile cyclic AMP secretion associated with the choleresis produced by 16, 16 diMePGF2 alpha. The administration of 16, 16 diMePGE2 in a dose range 0.01 to 1.0 microgram-kg-min did not significantly alter bile flow rates or composition. Bile erythritol-14C clearance, a measure of canalicular bile flow, was significantly increased by PGF2 alpha but not by 16, 16-dimethyl PGF2 alpha, suggesting that the mechanism of action of PGF2 alpha in stimulating hepatic bile flow may be different from that involved in 16, 16-dimethyl PGF2 alpha choleresis. The results of this study indicate that the synthetic PGF2 alpha analog produces a choleretic response not mediated by adenylate cyclase and associated with increased chloride and bicarbonate secretion.

16,16-Dimethylprostaglandin E2↗
PubMed1982

[Action of a new synthetic prostaglandin on gastroesophageal motility of the rat].

A new synthetic prostaglandin, namely the 15 alpha, 16 (R), 16-methyl-16-methoxy PGE1 (compound marked MDL 646), endowed with a potent antiulcer activity, was studied for its effects on gastroesophageal motility of the rat in comparison with natural PGE1. Surprisingly enough, the two compounds were found to differ not only from a quantitative but also from a qualitative point of view. In fact, the natural PGE1 had, as expected, a relaxant effect on all the preparations examined except the rat fundus which is known to be contracted by all the different types of prostaglandins; conversely its synthetic analogue (MDL 646) showed a remarkable stimulatory effect on both "in vitro" and "in vivo" preparations. It is obvious that if these observations will be confirmed in other animal species, they could have a remarkable practical interest.

Alprostadil↗
PubMed1983

Action of MDL 646, a new synthetic prostaglandin, on gastric acid secretion of some experimental animals.

The new synthetic prostaglandin 11,15-dihydroxy-16-methyl-16-methoxy-9-oxo-prost-13-en-1-oic acid,methyl ester (8 alpha,11 alpha,15R,16R) (compound marked MDL 646), belonging to the 16-methyl-16-methoxy series, was tested for its activity on gastric secretion of different animal species and in different experimental conditions. In the dog provided with gastric fistula and Heidenhain pouch, MDL 646 (25 micrograms/kg by intragastric administration) caused a remarkable inhibition of the histamine- and bethanechol-induced acid secretion, an effect which was more evident in the main stomach than on the Heidenhain pouch. In the cat, but not in the dog, the compound inhibited not only the hypersecretion induced by histamine and bethanechol but also that induced by pentagastrin. However, in this case, high doses (50-100 micrograms/kg) had to be used to obtain a significant inhibition. Similar results were obtained with the perfused stomach of the anaesthetized rat in which the natural PGE2 appeared to be from 3 to 5 times less potent. In the conscious rat provided with gastric fistula MDL 646 (15 and 50 micrograms/kg) significantly inhibited spontaneous gastric secretion. Untoward reactions, represented by salivation and vomiting lasting 30 min, were experienced by some dogs following administration of 50-100 micrograms/kg of the synthetic prostaglandin. These data appear of considerable interest in view of the possibility of the use of MDL 646 also in humans.

Alprostadil↗
PubMed1979

The use of synthetic prostaglandin analogue (fluprostenol) to induce foaling.

The synthetic prostaglandin (PG) analogue fluprostenol was used to induce parturition in mares and its mode of action was investigated by measuring endocrine changes before and during the induction period. Progestagens and unconjugated oestrogens showed little change during the induction period, but two different patterns in plasma PGFM levels were observed. The first was seen when foaling occurred within 90 min of injection; PGFM levels rose soon after injection and peaked during the maximum expulsive stage of labour, thus resembling events during natural foaling. The second occurred when foaling took longer than 90 min, and in these mares PGFM levels rose at various times after injection and peaked well before the onset of the expulsive stage of labour. It is suggested that these differences reflect the hormonal readiness of the mares to foal. Other procedures, such as rupture of the allantochorion, and dilatation of the cervix and injection of fluprostenol into the allantois, produced no uterine activity and did not stimulate labour or PGFM release.

Animals↗
PubMed1983

Effect of MDL 646, a new synthetic prostaglandin, on gastroesophageal motility of the rat.

Compound marked MDL 646, a synthetic prostaglandin belonging to the 16-methyl-16-methoxy PGE1 series was tested for its motor effects on some in vitro and in vivo preparations from the rat. The lower esophageal sphincter (LES) was contracted at threshold doses ranging from 10 to 20 ng/ml; the fundus was even more sensitive whereas the pyloric sphincter showed remarkable differences according to the in vitro or in vivo preparation. In all the different tests MDL 646 showed a high degree of tachyphylaxis. PGE1 tested for comparison, exerted a constant relaxant effect in all the preparations excepting the gastric fundus. The present data emphasize the importance of the substitutions in positions 15 and 16 in the synthetic prostaglandin for determining the peculiar biological activity: in fact both MDL 646 and the parent PGE1 inhibit gastric secretion but they have almost opposite effects on gastroesophageal motility.

Alprostadil↗
PubMedDate not supplied

Cellular effects induced by some synthetic prostaglandins obtained at ICCF-Bucharest.

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.

Animals↗
PubMed1987

Antigastrolesive, gastric antisecretory, diarrheagenic and mucus-stimulating effects in rats following topically applied rioprostil, a synthetic prostaglandin E1 analog.

Prostaglandins may have many biological actions including hypotensive and antipeptic ulcer activity. The purpose of this investigation was to determine if the primary alcohol prostaglandin E1 analog rioprostil1 prevents ethanol-induced gastric lesions (antigastrolesive activity), inhibits gastric acid secretion (antisecretory activity), or causes diarrhea in rats when administered topically, and to compare these responses to the effect of rioprostil following enteral (oral or intraduodenal) administration. Rioprostil exhibited antigastrolesive activity in rats when administered either orally or when applied topically. The topical antigastrolesive potency of rioprostil against ethanol-induced lesions [ED50 = 3.7 (0.5-12) micrograms/kg] was similar to its oral potency [ED50 = 1.9 (1.7-2.2) micrograms/kg]. In 4 hr pylorus-ligated rats, topically administered rioprostil inhibited total gastric acid output with a potency [ED50 = 5.1 (2.6-24) mg/kg] similar to intraduodenal administration [ED50 = 3.7 (2.8-5.3) mg/kg]. In addition, in these rats rioprostil increased mucin levels and did not cause dermal irritation. Finally, the incidence of diarrhea was lower when rioprostil was applied topically than when given orally with a 16-fold difference in potency between these two routes of administration. These data show that when rioprostil is applied via the skin it has antigastrolesive, gastric antisecretory and mucus stimulatory effects in rats equal to enteral administration, and a diarrheagenic potency lower than following oral administration. This profile suggests that topical administration of rioprostil may be a useful means of delivery for clinical treatment of peptic ulcer disease.

Administration, Topical↗
PubMed1980

Manipulation of duration of action of a synthetic prostaglandin analogue (TPT) assessed in the pregnant beagle bitch.

Beagle bitches were treated on days 20-22 of pregnancy with TPT as an aqueous solution administered subcutaneously via a minipump at a rate of 10 micrograms per hour for either 24 (I) or 48 hours (II). Additional animals received a single subcutaneous injection of 200 micrograms of TPT as an aqueous solution (III) or dissolved in polyethylene glycol 400 (IV) or the methyl ester of TPT dissolved in polyethylene glycol 400 (V). The duration of action was assessed by the nadir in circulating progesterone levels. By this criterion the duration of action in the different groups ranked I=III<II=IV<V, the nadir occurring at 2, 3 and 3-4 days post treatment, respectively. Duration of action correlated with the incidence of abortion. Salivation, emesis and diarrhea or hypothermia side effects, previously noted for this agent, were not affected by the manipulations of duration of action.

Abortifacient Agents↗
PubMedDate not supplied

The use of a synthetic prostaglandin E1 analog as a gastric protectant against aspirin-induced hemorrhage in the dog.

Misoprostol prevented gastric hemorrhage in dogs, each of which received aspirin (35 mg/kg body weight, orally q 8 hrs for 10 days). All dogs receiving aspirin alone had gastroscopic and histopathological lesions. No lesions were noted in four of five dogs given aspirin plus misoprostol (15 micrograms/kg body weight, q 8 hrs for five days; then 7.5 micrograms/kg body weight, q 8 hrs for five days). Four of 10 dogs receiving 15 micrograms/kg body weight of misoprostol developed diarrhea. The misoprostol dose was reduced to 7.5 micrograms/kg body weight, and the diarrhea subsided.

Alprostadil↗
PubMed1990

The synthetic prostaglandin E1 analogue rioprostil reduces the nephrotoxic potential of cyclosporine A.

Acute CyA nephrotoxicity involves alteration in the proximal tubule and leads to glomerular lesions. Administration of a vasodilatator agent such as the prostaglandin E1 analogue Rioprostil (Bayer AG, BAY 06893) might prevent preglomerular vasoconstriction and hence reduce cyclosporin nephrotoxicity. As an increased excretion of urinary enzymes as a consequence of CyA-nephrotoxicity is well known we investigated in 40 male Wistar rats the excretion of three urinary enzymes: the brush border enzyme gamma-glutamyltransferase (GGT), the leucine aminopeptidase (LAP), and the lysosomal enzyme N-acetyl-beta-glucosaminidase (NAG). Additionally we determined s-creatinine and CyA plasma level. The kidneys were studied histologically at the end of the study. Wistar rats receiving 20 or 50 mg CyA/kg/d showed a marked deterioration in renal function and an increase of all urinary enzymes determined. In the rats receiving 20 mg CyA/kg/d and Rioprostil (150 micrograms/d) renal function and the enzymes determined remained in the normal range. There was no change in the enzyme excretion and only a minor improvement of renal function in rats receiving 50 mg CyA/kg/d and Rioprostil. Histological findings showed prevention of CyA nephrotoxicity in the 20 mg/kg/d group and diminished renal damage in the 50 mg/kg/d group.

Acetylglucosaminidase↗