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At least 235 records · Page 13Linked to original sources
PubMed1998

Ergot alkaloids. Current status and review of clinical pharmacology and therapeutic use compared with other oxytocics in obstetrics and gynaecology.

Ergot alkaloids are well known preparations. Ergot alkaloids used in obstetrics and gynaecology are ergometrine (ergonovine; EM), methylergometrine (methergine; ME) and bromocriptine. The pharmaceutical properties of ME EM) are critical. To guarantee stability, ME and EM ampoules should be stored in a cool, dark place. ME and EM tablets are unstable in all conditions and they show an unpredictable bioavailability, which prevents oral use of the drugs for any purpose. ME and EM are known for their strong uterotonic effect and, compared with other ergot alkaloids, for their relatively slight vasoconstrictive abilities. ME and EM do have a place in the management of the third stage of labour as they are strong uterotonics. They act differently from oxytocin and prostaglandins, and have different adverse effects. Oxytocin should be used as prophylaxis or a the drug of first choice; next, ME or EM should be used, and if none of these drugs produce the desired effects, prostaglandins should be used to control bleeding. Ergot alkaloid use in gynaecology has been limited and today is discouraged even in essential menorrhagia. It is suggested that EM and ME be used (parenterally) only in first trimester abortion curettage, to reduce blood loss. Bromocriptine has been used for lactation suppression. However, alternatives such as cabergoline, which possess fewer adverse effects, are now available and therefore preferred for this indication. In sum, there is no place for the prophylactic use of ME and EM in obstetrics or gynaecology. They can be used for therapeutic purposes in the third stage of labour. During use, the practitioner must be alert for adverse effects.

Ergonovine↗
PubMed1983

Use of oral oxytocics for stimulation of labor in cases of premature rupture of the membranes at term. A randomized comparative study of prostaglandin E2 tablets and demoxytocin resoriblets.

The efficacy of oral PGE2 tablets and buccal demoxytocin (resoriblets) for the induction of labor in cases of premature rupture of the membranes (PROM) after the 37th week of gestation has been evaluated in a prospective, randomized investigation of 193 women. PGE2 tablets (Prostin) were given to 109 parturients and demoxytocin resoriblets (Sandopart) to 84. The former were given in increasing doses from an initial 0.5 mg to a maximum of 1.5 mg every hour. The demoxytocin was administered at a constant dosage of 50 I.U. every 30 min. The treatment was unsuccessful in 10 of the women treated with PGE2 tablets and in 19 women receiving demoxytocin resoriblets. In addition, the treatment had to be discontinued in 5 women in the PGE2 group due to gastrointestinal side effects. This gives a total success rate of 86.3% for treatment with PGE2 against 77.4% in respect of demoxytocin. This difference is not significant. No difference was observed between the two treatment groups as regards: the stimulation-delivery interval, duration of the various stages of labor, efficacy in primiparae and multiparae, efficacy in patients with a high/low Bishop score. A significantly higher frequency of gastro-intestinal side effects was seen in those treated with PGE2 (21.7%) as compared with demoxytocin (3.6%). The frequency of surgical intervention was 17% in the PGE2 group and 10% in the demoxytocin group. In 4 cases where the stimulation was successful, cesarean section was carried out for reasons unrelated to the drug therapy. Despite the fact that demoxytocin treatment results in fewer side effects than PGE2, the efficacy of the drug is not superior. Based on experience from previous investigations carried out in this department, where intravenous oxytocin was found to be clearly better than oral PGE2 for the induction of labor in cases of PROM, intravenous oxytocin will remain the method of choice due to the shorter period of treatment, which must take priority.

Administration, Oral↗
PubMed2001

[Oxytocic use and duration of labor under peridural ambulatory analgesia].

OBJECTIVE: Extradural analgesia is associated with an increase duration of labor and oxytocin use. MATERIAL AND METHODS: We conducted a study of walking during active labor under extradural analgesia among 41 women. This group, with uncomplicated pregnancies, was similar to associate with a usual-care group according to the following criteria: maternal age, parity, gestational age, Bishop's score at the admission, and labor entrance mode. Analgesia was performed by using combined spinal-epidural analgesia and patient controlled extradural analgesia. Fetal heart and uterine contractions were continuously monitored using Telemetry. Anesthetic and obstetrical parameters were noted every hour. The main criteria were length of labor and oxytocin consumption. Statistical analysis was performed using Student's t-test and Fischer's exact test. RESULTS: Duration of the 1st and 2nd stage of labor, and oxytocin consumption were not statistically different in the two groups, neither was mode of delivery. No neonates had an Apgar score less than 5 at one minute. Parturients walked about 2 h 30 for about 2,000 m. CONCLUSION: Obstetrical parameters and oxytocin consumption are not modified during walking extradural analgesia. No maternal or neonatal adverse effects were noted in our study.

Analgesia, Epidural↗
PubMed1976

An investigation of the natriuretic, antidiuretic and oxytocic actions of neurohypophysial hormones and related peptides: delineation of separate mechanisms of action and assessment of molecular requirements.

The substitution of the 4-glutamine of oxytocin by a lipophilic aliphatic amino acid leucine yields [4-Leu] oxytocin which possesses natriuretic-diuretic anti-arginine-vasopressin (anti-ADH) activities. Alkyl substitutions of the beta-carbon of the 1 half-cystine of oxytocin yield a series of antioxytocin analogs which inhibit the uterotonic response to oxytocin. In this paper, the results of our further investigations on the molecular requirements for natriuretic, anti-ADH and antioxytocic activities of these peptides are reported. A total of 12 analogs of oxytocin and lysine-vasopressin (LVP) with leucine and/or beta-carbon alkyl substitutions were studied. Our findings reveal that the effect of 4-leucine substitution may not be to enhance the natriuretic activity but rather to abolish the antidiuretic activity of oxytocin. The lack of antidiuretic activity of these 4-leucine analogs makes it possible to unmask the intrinsic natriuretic activity of these peptides at the high dose level. Structure-activity correlations suggest that the oxytocin molecule may be the optimal requirement for natriuretic activity of these peptides. Substitution of 4-glutamine by lipophilic aromatic phenylalanine yields [4-Phe] oxytocin which possesses anti-ADH activity with little or no natriuretic activity. The "hybrid" antioxytocin and anti-ADH molecules, beta-carbon alkyl and 4-leucine substituted analogs did not possess enhanced antihormone activity. Although they had antioxytocic and antipressor activities, they were less potent than their respective singly alkyl substituted analogs. Furthermore, they had no demonstrable anti-ADH activity. The single alkyl substituted oxytocin and LVP also had no anti-ADH activity. It therefore appears that beta-carbon alkyl substitution had different effects on activities depending on the morphological features and the functions of the target cell. In target cells of contractile smooth muscles (uterus and vascular), the alkyl substituted analogs had no intrinsic activity but retained a relatively high receptor affinity to become effective antagonists to the natural hormone. On the other hand, in target cells of the renal tubule which are noncontractile epithelial cells, both intrinsic activity and receptor affinity were reduced or abolished. Thus none of these alkyl substituted analogs possessed more than very slight antidiuretic activity, and none had any natriuretic or anti-ADH activity.

Animals↗