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PubMed1983

Labor induction with prostaglandins.

Prostaglandins E2 and F2 alpha have been used for labor induction for more than 10 years. Many investigations have shown that these prostaglandins are effective, and within certain dosage schedules, safe oxytocics, even though the systemic administration is accompanied by side effects, mainly from the gastro-intestinal tract. Oral PGF2 appears to be the prostaglandin favored in recent years. It gives few side effects when administered in this manner. It is concluded from the present investigation and a study of the literature that oral PGE2 has certain advantages in comparison with other oxytocics for induction of labor at term, although it cannot entirely replace intravenous oxytocin. This, together with the relatively high cost of oral PGE2, will limit its use in the future for labor induction at term in normal cases.

Dinoprostone↗
PubMed1988

V1-vasopressin receptors in the septum of the rat brain. Electrophysiological evidence.

In slices from the rat brain, extracellular recordings were obtained from single neurones located in the lateral septum, an area known to receive a vasopressinergic innervation. Approximately half of the neurones tested responded to vasopressin by a concentration-dependent increase in firing rate, the lowest effective concentration being in the order of 2 nM. The effect of vasopressin was blocked by a synthetic structural analogue possessing vasopressor and oxytocic antagonistic properties on peripheral vasopressin and oxytocin receptors. Oxytocin had a weak effect in firing septal neurones, whereas a selective oxytocic agonist was totally ineffective. The action of vasopressin on neuronal firing was mimicked by a vasopressor agonist (Phe2-Orn8-VT) but not by a selective antidiuretic agonist (dDAVP). These results indicate that the vasopressin receptors present in rat septum are V1 (vasopressor type) rather than V2 (antidiuretic type) receptors. In addition, we conclude that these receptors, when occupied, lead to increased firing of lateral septal neurones.

Action Potentials↗
PubMed2004

Uterovaginal packing with rolled gauze in postpartum hemorrhage.

Management options for postpartum hemorrhage (PPH) include oxytocics, prostaglandins, genital tract exploration, ligation or angiographic embolization of uterine/internal iliac arteries, and hysterectomy. After excluding uterine rupture, genital tract lacerations, and retained placental tissue, efforts are directed toward contracting the uterus by bimanual compression and oxytocics. If these are not successful, one must resort to surgical techniques. At this stage, an alternative option to remember is uterovaginal packing. Easy and quick to perform, it may be used to control bleeding by tamponade effect and stabilize the patient until a surgical procedure is arranged. Uterovaginal packing may sometimes obviate the need for surgery altogether. Two cases, a primary and a secondary PPH, managed recently with uterovaginal packing are reported. Despite concerns about concealed hemorrhage or the development of infection with this intervention, none of these problems were encountered, and uterine packing was successful even in the case of secondary PPH with documented infection.

Adult↗
PubMed1992

[Antagonistic properties of tetra-substituted analog of vasopressin with selective antidiuretic effects].

Biological properties of a novel vasopressin analogue were investigated. It was found that this analogue has no vasopressor and oxytocic activities but it exhibits a selective antidiuretic effect which is weaker than that of adiuretin (DDAVP). Novel analogue inhibits vasopressor, oxytocic and antidiuretic effects caused by arginine--vasopressin. The usefulness of novel compound as a pharmacological tool--vasopressin antagonist is suggested.

Animals↗
PubMed2006

Phytochemical components of Hunteria umbellata (K. Schum) and its effect on isolated non-pregnant rat uterus in oestrus.

Hunteria umbellate plant is used by West African traditional midwives as phytomedicine in herbal remedies to treat pregnancy related ailment and most especially to augment or induce labour in gravid uterus. The purpose of this study was to investigate this claim with view to validating scientifically the ethno - medicinal usage. The phytochemical analysis of the crude medicinal plant extract revealed the presence of saponin, saponin glycosides, steroid, tannins, volatile oils, phenols and copious amount of alkaloids. The aqueous extract obtained by maceration technique was subjected to pharmacological testing in vitro on a piece of isolated rat uterus previously pretreated with stilbesterol, suspended in De Jalon at 37 degrees C and aerated with 95% Oxygen and 5% CO(2). The oxytocic activity of the aqueous pulp extract of the pulp of Hunteria umbellata was compared with uterine stimulant like oxytocin. The extract affected the contractility of the uterus significantly (P<0.05) in a dose dependent manner. The effect of 10mg/ml extract was blocked by 0.1 ml of 0.1mg/ml atropine. The extract also potentiated the response shown by various doses of oxytocin. This preliminary investigation revealed that Hunteria umbellata has oxytocic effect thus justifying the use by the traditional birth attendants.

Animals↗
PubMed1989

Uterine rupture complicating midtrimester abortion. A report of two cases.

Uterine rupture occurring during a midtrimester abortion is rare. This complication may lead to profound shock and death as well as to interference with the patient's future fertility. Two patients sustained a uterine rupture during midtrimester abortion. This complication seems to be preventable. The risk of uterine rupture due to overstimulation is higher when amnioinfusion with prostaglandin or hypertonic saline is combined with the use of other oxytocic drugs. Grand multiparas undergoing amnioinfusion should not be given oxytocin; in the rare cases in which oxytocin is needed, it should be administered cautiously and monitored continuously. When a supplemental agent, such as an oxytocic, is needed, it should not be started until several hours after the amnioinfusion.

Abortion, Therapeutic↗
PubMed1989

[Cicatricial uteri. Vaginal delivery under peridural analgesia].

The results of 108 attempts to deliver women who had previously had caesarean sections vaginally under epidural analgesia are studied. 94 patients (87%) delivered vaginally taking the usual length of time for dilatation and delivery. These confirm that epidural analgesia does not alter the prognosis for this type of delivery. However, one uterus unfortunately ruptured with the rapid death of the baby. This study makes it possible to define certain rules that should be carried out to lessen or even get rid completely of the risk of these accidents. As far as the anaesthetic is concerned, epidural analgesia should be carried out and watched very carefully. Small doses of anesthetics should be used and those in low concentrations. Symmetry analgesia should be good. Medics should be aware of the cumulative effect of adding dose on dose. Finally, morphine or morphine-like substances should either be used carefully or forbidden altogether. These precautions will limit the quantities of epidural analgesics that are delivered and assure that there is symmetry so that it is easier to recognize the signs before rupture of the uterus. As far as the obstetrical side is concerned, although we did not use oxytocics very often (37%) we did not find that there was any risk attached to it. We recommend, however, that internal monitoring should be carried out very often whether oxytocics are used or not. Routinely, instruments should be used for the delivery to lessen the efforts required to expel the baby. Exploring the cavity of the uterus after the delivery does not seem to us to be necessary unless there are the usual obstetric indications for doing this.

Adult↗
PubMed1989

[Drugs for the mother and infant in the maternity ward. A study of 5 Norwegian university hospitals].

Hospital records were used to record, all drugs prescribed in the maternity ward, delivery characteristics and complications in both mother and infant at five university hospitals. The retrospective survey comprised 970 women and represented 10% of all vaginal deliveries in these hospitals in 1980, and 2% of all annual births in Norway. In total 90% of the women received drugs, excluding laxatives, oxytocics and long-term medication, vitamins and iron. Large variations were found between hospitals in respect of hypnotics (41-86%) and analgesics (65-95%). Of newborns 4-23% were treated with a drug. The large variation was largely due to frequent administration of naloxone at one of the hospitals. Drug utilization post partum was significantly higher in primipareas and in mothers who underwent interventions such as epidural anaesthesia, oxytocin drip, forceps delivery and tears. 98% of the babies were breast-fed on discharge and thus received milk potentially containing drugs. The frequent use of hypnotics indicates that breast-feeding mothers were treated like hospital patients in general. For the majority of the drugs used as a routine in the maternity wards there was no data or insufficient data on excretion in breast milk. The large discrepancy between hospitals as regards prescription of hypnotics and oxytocics to the mother and naloxone to the newborn was considered not to reflect rational prescription criteria and should therefore be reassessed.

Adult↗
PubMed1978

[Effects of peridural analgesia on labor].

A review of the effects during labour of epidural analgesia on dilatation, expulsion and delivery of the placenta. Uncertainties in knowledge of the precise organisation of uterine innervation and of the intrinsic innervation of the organ render the study of changes in uterine contraction and in cervical resistances difficult. At circulating levels higher than those found in clinical practice, local anaesthetics have a definite oxytocic e-fect, local anaesthetics have a definite oxytoci effect, whilst adrenalin is a powerfult tocolytic. By contrast, the indirect effects related to neurolysis in extradural analgesia are negligeable. Cervico-segmentary resistances are decreased. In practice, there is no increase in the period of dilatation in the absence of any haemodynamic disturbances and if mixtures containing adrenalin are avoided. Expulsion is favourised by muscular relaxation but impaired by the lack of voluntary expulsive effort, hence the choice of a local anaesthetic with the lowest possible motor effect. Delivery of the placenta, which involves only uterine contraction, which is not affected, may be accelerated by oxytocics.

Anesthesia, Epidural↗
PubMed1985

[Vasopressin and oxytocin receptors in the central nervous system of the rat].

Synaptic plasma membranes containing binding sites for (3H) oxytocin and (3H) arginine vasopressin were isolated from rat amygdala, olfactory bulb and hippocampus. In the hippocampus, two specific binding sites have been characterized: an "oxytocic" binding site, which has a high affinity for oxytocin, arginine vasopressin and arginine vasotocin, and a "vasopressic" binding site, which has a high affinity for arginine vasopressin, arginine vasotocin and a low affinity for oxytocin. The specificity of these binding sites were tested in competition experiments. The affinity of different antidiuretic and vasopressic analogues for the vasopressic site was similar to that observed for the V1 type of vasopressin receptors present in the hepatocytes and vascular smooth muscle cells. The affinity of several analogues for the oxytocic site shows some similarities with their corresponding relative activities in increasing the firing rate of non pyramidal neurones in hippocampal slices. Arginine vasopressin and oxytocin did not change the activity of adenylate cyclase present in the hippocampal synaptic plasma membranes. The properties of these specific binding sites for the neurohypophyseal hormones are compared with the receptors present on the peripheral targets.

Adenylyl Cyclases↗
PubMed1984

Direct regulation of rat testicular steroidogenesis by neurohypophysial hormones. Divergent effects on androgen and progestin biosynthesis.

The direct regulation of testis androgen and progestin biosynthesis by neurohypophysial hormones was investigated in a primary culture of rat testis cells. Treatment with arginine vasotocin (AVT; 10(-6) M) over a 10-day period inhibited the human chorionic gonadotropin (hCG)-stimulated testosterone accumulation while enhancing hCG-stimulated progesterone accumulation. Furthermore, treatment with increasing doses (10(-11) - 10(-6) M) of AVT by itself led to dose-dependent increases in the accumulation of pregnenolone (ED50: 8.0 +/- 0.2 X 10(-9) M) and progesterone (ED50: 1.6 +/- 0.3 X 10(-8) M) but not testosterone. Under blockade of pregnenolone metabolism using cyanoketone and spironolactone, AVT, like hCG, stimulated pregnenolone accumulation with an ED50 dose of 5.8 +/- 0.3 X 10(-9) M. Similar effects were observed with several related neurohypophysial hormones, but not with nine unrelated peptides. AVT, arginine vasopressin, and lysine vasopressin were about 100-fold more potent than mesotocin, valitocin, and oxytocin. Pressor (but not antidiuretic or oxytocic)-selective agonists of the neurohypophysial hormones also exerted dose-dependent stimulation of pregnenolone accumulation. Potent pressor (but not oxytocic)-selective antagonistic analogs of the neurohypophysial hormones prevented the AVT-stimulated accumulation of pregnenolone. Thus, the neurohypophysial hormones may exert a direct stimulatory effect on testis pregnenolone and progesterone biosynthesis via putative, pressor-selective recognition sites, and this progestin-stimulatory activity may be partly due to stimulation of steroidogenic steps preceding pregnenolone formation. Since the effective doses of neurohypophysial hormones in vitro are higher than the serum hormone levels, the present results suggest an intratesticular paracrine role for these peptides.

Animals↗
PubMed1982

Uterine rupture occurring during midtrimester abortion.

Uterine rupture is an uncommon complication of midtrimester abortion, occurring more frequently in the older multiparous patient and with the use of high doses of oxytocic agents. The clinical presentation may vary from an unexplained drop in the hematocrit or persistent abdominal pain to profound shock and maternal death. There is often considerable delay in diagnosis and subsequent treatment. The clinical presentation of a patient who sustained uterine rupture during midtrimester abortion is described and the possible etiology, clinical presentation, and management of this condition are described. It is recommended that older multiparous patients receiving oxytocic agents be monitored closely to prevent uterine hyperstimulation and that prompt laparotomy be performed when the diagnosis of uterine rupture is made.

Abortion, Induced↗
PubMed1981

[A study of uterine contractility in the onset of labour (author's transl)].

We have studied uterine contractility in 100 inductions of labour at term. We have been able to compare the effects of oxytocic infusions with rupture of the membranes on contractility. Oxytocic infusions and rupture of the membranes seem to have similar effects on the amplitude as well as on the contractile surface and these effects are quantitatively reinforced by one another.

Extraembryonic Membranes↗
PubMed1977

[Neurohypophyseal hormones in the cerebrospinal fluid with different degrees of hydration].

Antidiuretic and oxytocic activities of venous blood plasma and liquor of ambient cistern of the cerebrum were studied in chronic experiments on alert dogs at different levels of hydration. Liquor was found to have oxytocic activity and practically no antidiuretic activity at ordinary hydration and after two days of thirst. After three days of thirst, dog's liquor caused antidiuretic reaction in rats anesthetized with alcohol, the reaction being lesser than those caused by simultaneously received plasma samples. Liquor displayed an obvious antidiuretic reaction similar to that of vasopressin after prolonged i.v. administration of hypotonic NaCl solution, while plasma samples only had the diuretic effect.

Animals↗
PubMed2006

Position 4 analogues of [deamino-Cys(1)] arginine vasopressin exhibit striking species differences for human and rat V(2)/V(1b) receptor selectivity.

Arginine vasopressin (AVP) mediates a wide variety of biological actions by acting on three distinct G-protein coupled receptors, termed V(1a) (vascular), V(1b) (pituitary) and V(2) (renal). It also binds to the oxytocin (OT) receptor. As part of a program aimed at the design of selective agonists for the human V(1b) receptor, we recently reported the human V(1b), V(1a), V(2) and OT receptor affinities of the following position 4 substituted analogues of [deamino-Cys(1)] arginine vasopressin (dAVP)-(1) d[Leu(4)]AVP, (2) d[Orn(4)]AVP, (3) d[Lys(4)]AVP, (4) d[Har(4)]AVP, (5) d[Arg(4)]AVP, (6) d[Val(4)]AVP, (7) d[Ala(4)]AVP, (8) d[Abu(4)]AVP, (9) d[Nva(4)]AVP, (10) d[Nle(4)]AVP, (11) d[Ile(4)]AVP, (12) d[Phe(4)]AVP, (13) d[Asn(4)]AVP, (14) d[Thr(4)]AVP: (15) d[Dap(4)]AVP. With the exception of Nos. 7 and 12, all peptides exhibit very high affinities for the human V(1b) receptor. Furthermore, peptides 1-4 exhibit high selectivities for the human V(1b) receptor with respect to the V(1a), V(2) and OT receptors and, with d[Cha(4)]AVP, in functional tests, are the first high affinity selective agonists for the human V(1b) receptor (Cheng LL et al., J. Med. Chem. 47: 2375-2388, 2004). We report here the pharmacological properties of peptides 1-4, 5 (from a resynthesis), 7, 9-13, 15 in rat bioassays (antidiuretic, vasopressor and oxytocic) (in vitro: no Mg(++)) with those previously reported for peptides 5, 6, 8, 14. We also report the rat V(1b), V(1a), V(2) and OT receptor affinities of peptides 1-5 and the rat V(2) receptor affinities for peptides: 7-15.The antidiuretic activities in units/mg of peptides 1-15, are: 1=378; 2=260; 3=35; 4=505; 5=748; 6=1150; 7=841; 8=1020; 9=877; 10=1141; 11=819, 12=110; 13=996; 14=758; 15=1053. Peptides 1-4 exhibit respectively the following rat and human (in brackets) V(2) receptor affinities: 1=3.1 nm (245 nm); 2=3.4 nm (1125 nm); 3=24.6 nm (11,170 nm); 4=0.6 nm (1386 nm). Their rat V(1b) receptor affinities are 1=0.02 nm; 2=0.45 nm; 3=9.8 nm; 4=0.32 nm. Their rat V(1a) receptor affinities are 1=1252 nm; 2=900 nm; 3=1478 nm; 4=32 nm. Their rat oxytocin (OT) receptor affinities are 1=481 nm; 2=997 nm; 3=5042 nm; 4=2996 nm. All four peptides have high affinities and selectivities for the rat V(1b) receptor with respect to the rat V(1a) and OT receptors. However, in contrast to their high selectivity for the human V(1b) receptor with respect to the human V(2) receptor, they are not selective for the V(1b) receptor with respect to the V(2) receptor in the rat. These findings confirm previous observations of profound species differences between the rat and human V(2) receptors. Peptides 1-4 are promising leads to the design of the first high affinity selective agonists for the rat V(1b) receptor.

Animals↗
PubMed1999

Studies on the spasmolytic and uterine relaxant actions of n -ethyl and n -benzyl-1,2-diphenyl ethanolamines: elucidation of the mechanisms of action.

The influence of N -ethyl- and N -benzyl-1,2-diphenyl ethanolamines (compounds E and B, respectively) was examined on the spontaneously contracting rabbit jejunum and the rat uterus together with their influence on the contractions induced by some spasmogens in the guinea-pig ileum and oxytocics and CaCl2in the pregnant rat uterus. Both E and B inhibited the spontaneous contractions of the rabbit jejunum with ID50values of 0.13 and 0.03 micromol ml-1. Their inhibitory activities were not antagonized by alpha- or beta-adrenoceptor blockers but significantly reversed by CaCl2(0.015 micromol ml-1). The compounds also antagonized nicotine, ACh-, histamine-, 5-HT- and CaCl2-induced contractions by 44-100%. Compound E seemed to be several times more potent than B in inhibiting the spontaneous uterine contractions with an ID50of (7 nmol ml-1). Their inhibitory effects were not antagonized by beta2-adrenoceptor or H2-receptor blocking drugs. Both compounds (40 nmol ml-1) antagonized in a competitive manner CaCl2-induced contractions in the K+-depolarised uterus and PGE2and oxytocin-induced uterine contractions. The ID50values were in the range of 1.6-10.7 nmol ml-1. The results suggest that E and B compounds may be considered as putative L-Ca2+channel blockers with certain selectivities. The E compound seemed to be more selective against uterine L-Ca2+channels and the B compound against intestinal smooth muscles. Thus, the compounds may be of potential value in treatment of some colics, the irritant bowel syndrome, dysmenorrhoea and premature deliveries.

Adrenergic alpha-Antagonists↗
PubMed1990

Birth asphyxia and obstetric care in Curaçao Netherlands Antilles.

Out of the 223 fetal and neonatal deaths that occurred on the island of Curaçao in a 2-year period (1984-1985), 35 were due to birth asphyxia (15.7%). In order to evaluate the quality of obstetric care, the circumstances surrounding each asphyxiated death were scrutinized. On the whole, patients' compliance with antenatal care was satisfactory. However, when the woman presented in labor the attending physician or midwife often lacked information on maternal antecedents and the course of pregnancy. Inadequate intrapartum surveillance together with failure to respond appropriately to abnormalities in labor constituted the principle factors which were associated with asphyxiated deaths. In addition, asphyxial conditions during labor were often preceded by inappropriate administration of oxytocic agents.

Adolescent↗
PubMed1991

Recommendations for the management of low risk obstetric patients.

Specific interventional procedures have enjoyed widespread popularity in the United States in the routine management of low risk obstetric patients without the benefit of clinical studies attesting to their utility. A review of the literature was conducted to survey obstetric practice with regard to amniotomy, intravenous fluids, third stage administration of oxytocics, episiotomy and continuous fetal monitoring.

Amnion↗