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At least 19 recordsLinked to original sources
PubMed1979

Absorption and penetration of dinoprost (prostaglandin F2 alpha) and dinoprost methyl ester into perfused mesenteric circulation in rats.

The absorption of dinoprost (prostaglandin F2 alpha) and its methyl ester in rat jejunum was studied. A 22-cm segment of rat jejunum was cannulated at both ends and connected to an oscillating perfusion pump system. The mesenteric vasculature supplying this isolated segment also was cannulated and perfused with Kreb's bicarbonate buffer with dextran. Solutions of 3H-dinoprost or its methyl ester were introduced into the lumen and oscillated through the segment. The disappearance of radioactivity from the lumen and the appearance of radioactivity in the vascular perfusate were monitored. The metabolite patterns in the vascular perfusate were analyzed by TLC. A lag between the time the drug disappeared from the lumen and the time it appeared in the mesenteric circulation was detected. This lag was longer for the methyl ester than for the free acid, even though the ester disappears from the lumen faster than does the free acid. Upon removal of dinoprost from the gut lumen, a gradual decrease in the amount of drug appearing in the mesenteric circulation could be detected. However, with the ester, a slight increase could be observed for approximately 0.5 hr, followed by a decrease. Metabolism by the gut wall appears to be greater for the ester than for the acid. The results suggest that, although the ester disappears from the lumen more quickly than does the acid, it actually penetrates to the blood at a slower rate and undergoes greater metabolism.

Absorption↗
PubMed1993

Termination of early pregnancy in sheep with dinoprost or cloprostenol: comparison of two commercial preparations.

The response of the ovine corpus luteum of pregnancy to the luteolytic effect of prostaglandin F2 alpha (dinoprost) and its analogue, cloprostenol, was tested in both superovulated and untreated ewes by monitoring plasma progesterone concentrations at the time of 'material recognition' and beyond (days 13 to 30). On days 13, 16 and 28, the majority of the superovulated ewes were refractory to 10 mg of dinoprost. The luteolytic efficacy of 250 micrograms of cloprostenol was compared with 10 mg of dinoprost on day 20 of pregnancy in superovulated and untreated animals and the two prostaglandins were also compared on days 26 and 30 in animals previously unresponsive to dinoprost. Generally, cloprostenol was more effective than dinoprost because there was less refractoriness on day 20 and no refractoriness on days 26 and 30 to this prostaglandin. No difference in the sensitivity to this drug was found between the superovulated and untreated groups on days 20 and 26.

Abortion, Induced↗
PubMed1979

Prostaglandin prodrugs III: Synthesis and biological properties of C9- and C15-monoesters of dinoprost (prostaglandin F2 alpha).

Methods are described for the synthesis of dinoprost C9- and C15-monoesters using protective groups. Esters at C9 were synthesized by acylation of dinoprost 11,15-bis(tetrahydropyran-2-yl)ether followed by acid-catalyzed protective group removal. Esters at C15 were synthesized by initial formation of the protected intermediate, dinoprost 9,11-n-butylboronate, followed by acylation and hydrolytic protective group removal. Many esters were active in vivo in the hamster antifertility screen. Plasma hydrolysis studies showed that the C15-esters were more readily cleaved than the C9-esters. In vivo studies in the rat showed that both the C9- and C15-esters resulted in urinary excretion of 5 alpha, 7 alpha-dihydroxy-11-ketotetranorprosta-1,16-dioic acid in amounts comparable to those obtained after dosing with dinoprost, indicating that ester hydrolysis occurred in vivo.

Animals↗
PubMed1981

Evaluation of single and double artificial insemination regimes as methods of shortening calving intervals in dairy cows treated with dinoprost.

Conception rates in 535 commercial lactating Friesian dairy cows on two farms were compared between treated animals after two injections of dinoprost at an 11-day interval, and untreated contemporary controls bred by conventional artificial insemination. The conception rate for a single insemination 75 to 80 hours after the second dinoprost injection was 46 per cent, for two inseminations 72 and 96 hours after the second injection was 47 per cent, and for untreated controls was 50 per cent. The differences are not statistically significant. Both dinoprost treated groups had a mean calving interval of 366 days compared with 378 for controls. The time advantage of 12 days in calving interval was principally due to the shorter calving-to-first-service interval of treated cows. This 10-day advantage in calving-to-first-service was increased to a 12-day advantage in calving-to-conception in treated cows, and applied also to cows which failed to conceive to the induced oestrus. The accuracy of pregnancy diagnosis was confirmed by calving data; pregnancy diagnosis by rectal palpation was 94 per cent and by milk progesterone assay 81 per cent accurate, overall. Oestrus occurred in 3.8 per cent of pregnant cows, on the basis of stockmen's observations. The relevance of the information to herd sterility control is discussed.

Animals↗
PubMed1987

Inhibition of constriction of cerebral arterioles in vivo by naftidrofuryl. Action against serotonin and dinoprost.

The effect of 2-(diethylamino) ethyl-tetrahydro-alpha-(1-naphthyl-methyl)-2-furanpropionate (naftidrofuryl, Praxilene) on an in vivo preparation of mouse cerebral blood vessels was investigated. Naftidrofuryl significantly reduced the arteriolar constriction produced by topical application of serotonin or dinoprost (prostaglandin F2 alpha). Local application of 10(-5) mol/l naftidrofuryl reduced both the constrictions to serotonin or dinoprost, when applied simultaneously with either constrictor. However, 10(-7) mol/l naftidrofuryl only inhibited serotonin. Moreover, 30 min after intraperitoneal injection, 160 mg/kg naftidrofuryl inhibited constrictions by either serotonin or dinoprost but 40 mg/kg only inhibited serotonin. 10 mg/kg also inhibited serotonin. The results are compatible with reports of a relatively selective action of naftidrofuryl on the serotonin S2 receptor. Moreover, while naftidrofuryl has long been suggested as a drug which could enhance cerebral blood flow or improve cerebral ischemia, the present observations suggest an antispasmodic effect on cerebral vessels in vivo.

Animals↗
PubMed1994

Reproductive performance of dairy cows following treatment with fenprostalene, dinoprost, or cloprostenol between 24 and 31 Days post partum: a field trial.

Three hundred and one Holstein cows (n=301), calving at a commercial free-stall dairy farm, were randomly assigned to 1 of 3 prostaglandin treatment groups or a placebo group. The placebos were packaged 3 ways to mimic the 3 commercial prostaglandin preparations. Group 1 received 1 mg fenprostalene and 1.6 mg oxytetracycline; Group 2 received the fenprostalene placebo (2 ml polyethylene glycol and 1.6 mg oxytetracycline); while Group 3 was given 25 mg dinoprost. Group 4, the dinoprost placebo received 5 ml saline; Group 5 received 500 microg cloprostenol; and Group 6 the cloprostenol placebo received 2 ml saline. The treatments were administered between Days 24 and 31 post partum. Double blind techniques were used in administering treatments and in assessing the response to treatment. There were no significant differences among treatment groups with respect to incidence of retained fetal membranes, endometritis, pyometra, anestrus, number of services per pregnancy, calving-to-first estrus interval, services per conception, number of prostaglandin treatments other than those administered between Days 24 and 31 post partum, the percentage culled for reproductive reasons and all factors combined. Cows receiving fenprostalene, dinoprost or cloprostenol had a decreased calving-to-conception interval compared with that of the controls (P = 0.05). It is concluded that, in the herd studied, treatment with any of the 3 commercially available prostaglandin products between Days 24 and 31 post partum was beneficial for reproductive performance.

Journal Article↗
PubMed1984

Physical model approach to gastrointestinal absorption of prostaglandins II: In situ rat intestinal absorption of dinoprost.

In situ absorption studies with dinoprost in the rat jejunum were carried out using a modified Doluisio technique. The absorption rate was first order. There was a sigmoidal decrease in the rate with increasing buffer pH (from 3.5 to 9.5), which strongly indicated the partitioning of weak acid species into the lipoidal membrane. An asymptotic minimum rate was attained from buffer pH 7.5 to 9.5, operationally indicative of transport of anions across aqueous pores. The importance of the aqueous diffusion layer on the mucosal side of the membrane was evident; rates at pH 3.5 and 4.5 were faster at high agitation hydrodynamics in the lumen solution. Preliminary studies showed that there was no metabolism in the lumenal solution and that metabolism occurred within the membrane. The transport mechanism involved simultaneous passive diffusion and bioconversion in the membrane because (a) a 1.5 X 10(4)-fold range in dinoprost concentration (0.014-210 microM) showed no saturable carrier-mediated tendency on the rate, (b) iodoacetic acid and indomethacin did not inhibit the absorption rate, and (c) the shape of the absorption-pH profiles was suggestive of passive diffusion. The prostaglandin did not have apparent adverse membrane and vascular effects under the conditions employed. The quantification and factorization of the physically meaningful transport parameters were accomplished using the physical model previously described. The permeability coefficients of the aqueous diffusion layer for the oscillation and static hydrodynamic situations were 0.8 X 10(-4) and 1.7 X 10(-4) cm/s, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed2002

Synchronization of estrus in virgin beef heifers using melengestrol acetate and PGF2alpha: an efficacy comparison of cloprostenol and dinoprost tromethamine.

This study compared the efficacy of two sources of PGF2alpha on the reproductive performance of virgin beef heifers, after synchronization of estrus using melengestrol acetate (MGA) and PGF2alpha. Angus-based heifers (n = 1002) in five herds were fed 0.5 mg per head per day of MGA for 14 days. Nineteen days after the last day of MGA feeding, heifers were randomly assigned to receive (i.m.) either 0.5 mg cloprostenol (n = 504; Estrumate, E) or 25 mg dinoprost tromethamine (n = 498; Lutalyse, L) as a source of exogenous PGF2alpha. Heifers were observed twice daily for 5 days for signs of estrus and artificially inseminated 8-12 h later, except in herd A, wherein animals not detected in estrus by 80 h after PGF2alpha were mass-mated and no longer monitored for signs of estrus. Estrumate and Lutalyse were equally (P > 0.1) effective among all response variables evaluated, including estrus response (E, 89% and L, 86%), conception rate (E, 67% and L, 67%), and synchronized pregnancy rate (E, 61% and L, 57%). Synchrony of estrus was not affected (P > 0.1) by PGF2alpha source, and peak estrus response occurred 60 h post-PGF for both treatments. Conception rate to timed insemination was not different (P > 0.1) among Estrumate- and Lutalyse-treated heifers within herd A (14%, 4/28 and 7%, 2/29, respectively). Herd had a significant (P < 0.05) effect on all indicators of reproductive performance. Conception rates within herds A and D were influenced by technician (P < 0.05), however, this effect was balanced across treatments and no treatment by technician interaction was detected. In conclusion, when administered 19 days after a 14-day MGA feeding period, cloprostenol and dinoprost tromethamine are equally efficacious for synchronous induction of a fertile estrus in virgin beef heifers.

Animals↗
PubMed1989

Dinoprost 14-day oestrus synchronisation schedule for dairy cows.

Oestrus and ovulation were synchronised in 82 lactating Friesian dairy cows with two injections of dinoprost, and the cows were inseminated 72 and 96 hours after the second injection. Twenty-one of the 41 cows (51 per cent) which had a 14-day interval between the dinoprost injections conceived to the inseminations, compared with 18 of the 41 cows (44 per cent) which had an 11-day interval between the injections.

Animals↗
PubMed1976

High-pressure liquid chromatographic determination of the 15-epimer of dinoprost in bulk drug.

The p-nitrophenacyl esters of dinoprost and its 15-epimer are well resolved using high-pressure liquid chromatography. Quantitation was achieved using the internal standard technique. The specially synthesized diphenylurea ester of cholic acid was found to be a model internal standard. Graphs of peak height ratios of the prostaglandin to the internal standard were linear with respect to the amount of prostaglandin injected, with the lower detection limit of the 15-epimer being about 0.5%. Data are presented that demonstrate the usefulness of this analytical technique in determining the concentration of the 15-epimer present during studies on the kinetics of decomposition of dinoprost.

Chromatography, High Pressure Liquid↗
PubMed1979

Plasma progesterone and luteinising hormone levels in cattle after synchronisation of oestrus with dinoprost.

The plasma levels of progesterone and luteinising hormone (LH) were monitored in a group of cattle after pretreatment with two injections of 25 mg dinoprost. Close groupings of preovulatory LH peaks were observed and the possible significance of this is discussed. Based on the findings of this study, supporting evidence is provided for the timing of insemination after injection of cattle which have been synchronised for oestrus with dinoprost.

Animals↗
PubMed1980

Effect of gonadotrophin releasing hormone on levels of luteinising hormone in cattle synchronised with dinoprost.

Synchronisation of oestrus was achieved in a group of three cows and two heifers with dinoprost. Sixty-six hours after the second injection of dinoprost, 0.125 mg synthetic gonadotrophin releasing hormone (GnRH) was given intramuscularly. Concentrations of luteinising hormone (LH) were monitored in peripheral blood and close grouping of preovulatory LH peaks was seen around 2.5 hours after injection of GnRH.

Animals↗
PubMed1981

Binding of prostaglandins E1 (alprostadil), E2 (dinoprostone), F1 alpha, and F2 alpha (dinoprost) to human serum proteins.

Prostaglandins E1 (alprostadil), E2 (dinoprostone), F1 alpha, and F2 alpha (dinoprost) were characterized in terms of binding to human serum, albumin, gamma-globulin II, beta-globulin III, alpha-globulin IV-1, and alpha-globulin IV-4. By using equilibrium dialysis and tritium-labeled ligands, the percent binding for all four ligands was found to decrease in the following order: human serum, albumin, and alpha-globulin IV-4. For the other three proteins, the order was not consistent with the four ligands, and less than 10% binding was observed. In general, prostaglandins E1 and E2 showed a higher percent binding for all fractions than prostaglandins F1 alpha and F2 alpha. All four ligands can be characterized as showing significant binding to human serum, albumin, and alpha-globulin IV-4.

Alprostadil↗
PubMed1992

The effect of dinoprost on transport of water and imipramine through rat small intestinal membranes.

The relation between transmucosal fluid movement and its effect on absorption and exsorption of imipramine was studied with the in-situ single-pass perfusion technique in rats. Dinoprost (prostaglandin F2 alpha, PGF2 alpha) caused a dose-related inhibition of both absorption and secretion of water across the intestinal membrane. When PGF2 alpha was infused at a rate of 5 mumols kg-1 h-1, the absorption rate of water decreased from 51.7 to 21.5 mL h-1 and the secretion rate decreased from 48.9 to 26.8 mL h-1. Net water flux changed from net water absorption (0.9 mL h-1) to net water secretion (5.33 mL h-1) by infusion of PGF2 alpha. However, absorption and exsorption of imipramine were little affected by infusion of PGF2 alpha. The absorption rates of imipramine were 3.03 and 2.36 mg h-1 in the absence and presence of PGF2 alpha, respectively. Furthermore, the average amounts of imipramine exsorbed into the intestinal lumen in 2 h were 7.82 and 8.10% in the absence and presence of PGF2 alpha, respectively. Infusion of PGF2 alpha also enhanced motility of the small intestine compared with the control. From these results, it appears that PGF2 alpha has no effect on the absorption and exsorption of imipramine across the intestinal membrane although it is reasonable to use PGF2 alpha in the case of patients with overdoses of drugs which decrease gastrointestinal motility.

Animals↗
PubMed1984

Routine induction of farrowing with dinoprost in a commercial sow breeding unit over a year.

Details were recorded on a commercial sow breeding unit where dinoprost was used to induce farrowing in groups of sows every second week. Criteria considered were the interval from injection to start of farrowing, called the induction interval, the time required for farrowing to be completed, called the duration of farrowing, litter size and percentage of piglets born dead. Data were analysed to look for the effect on these of the day of gestation on which the injection was given, the parity status of the sow and the litter size.

Age Factors↗
PubMed2001

Luteal and clinical response following administration of dinoprost tromethamine or cloprostenol at standard intramuscular sites or at the lumbosacral acupuncture point in mares.

OBJECTIVE: To determine whether administration of a microdose of prostaglandin at the BAI HUI acupuncture point offers any advantage over IM injections for luteolysis, ovulatory interval, or systemic response in mares. ANIMALS: 17 mature cycling mares, 3 to 20 years of age and weighing 400 to 500 kg. PROCEDURE: Conventional and microdoses of the prostaglandin dinoprost tromethamine (PGF2alpha), the analogue cloprostenol, or sterile water (control) were administered to mares in 7 treatment groups. Treatments were assigned by dose, administration site (semimembranosus, semitendinosus, or lumbosacral region), and treatment type (PGF2alpha, analogue, or sterile water). Mares were observed for ovulatory interval and systemic response to treatment, including heart, and respiratory rates, rectal temperature, and sweat score. Plasma progesterone concentrations were also determined at the time of treatment and at 24-hour intervals for 96 hours following treatment. RESULTS: Ovulatory interval was shortened and progesterone concentrations decreased in prostaglandin-treated mares, compared with control mares, regardless of dose or treatment site. However, no differences in ovulatory interval were observed among prostaglandin-treated mares. Mares treated with conventional doses of PGF2alpha had greater systemic responses than mares treated with microdoses of PGF2alpha or sterile water. CONCLUSIONS AND CLINICAL RELEVANCE: Administration of prostaglandins at the BAI HUI acupuncture point does not appear to offer any advantage over administration at standard IM injection sites for induction of luteolysis or to shorten the ovulatory interval. However, administration of a microdose of the analogue cloprostenol was effective at inducing luteolysis and shortening ovulatory interval regardless of administration site.

Abortifacient Agents, Nonsteroidal↗
PubMed1977

Prostaglandin monolayers II: monomolecular film behavior of dinoprost C-15 alkyl esters.

Monomolecular film compression-relaxation behavior was examined for select dinoprost C-15 alkyl esters. Higher homologs of the series such as palmitate and decanoate esters yielded stable expanded monolayers that exhibited minimal relaxation of surface pressure during noncompression. Their limiting molecular areas were consistent with a Hirschfelder model projection in which the prostaglandin moiety assumes a horizontal orientation at the interface with its alkyl ester chain oriented vertical to the surface plane. Shorter chain homologs such as hexanoate, valerate, butyrate, propionate, and acetate also formed expanded monolayers but exhibited increased instability with decreased alkyl chain length, as reflected in their lower surface pressure development during compression and significant relaxation of pressure during noncompression. Such instability can be tied to their increased solubility in the subphase solution and higher desorption rate from the interface.

Chemical Phenomena↗
PubMed1986

Improved reproductive performance from dairy cows treated with dinoprost tromethamine soon after calving.

The first-service conception rate for 74 commercial dairy cows that were given a single injection of dinoprost tromethamine (prostaglandin F(2)alpha THAM) between 14 and 28 d after calving was 56%. For 74 untreated control herdmates the rate was 47%. The average interval from calving to first oestrus was 57 d for treated cows and 70 d for the control group. The difference is significant at the P = 0.017 level. The advantage in the conception rate of treated over control group cows occurred mostly in cows with a blood progesterone concentration of less than 0.5 ng/ml at the time of treatment; this numbered about two-thirds of the cows in the trial. The results support the findings of a previous study.

Journal Article↗