Selective and extremely long inhibition of prolactin release in man by 1‐ethyl‐3‐(3′‐dimethylaminopropyl)‐3‐(6′‐allylergoline‐8′‐beta‐ carbonyl)‐urea‐diphosphate (FCE 21336).
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The effects on anterior pituitary function of FCE 21336 (1‐ethyl‐3‐(3′‐ dimethylaminopropyl)‐3‐(6′‐allylergoline‐8′‐beta‐ca rbonyl)‐urea‐ diphosphate), a synthetic ergoline derivative with selective dopamine agonistic properties, were studied. Circulating PRL, GH, TSH, cortisol and LH levels were determined up to 96 h after single oral doses of 50, 100, 200 and 300 micrograms of the compound to eight healthy males, and up to 168 h after single oral doses of 400 and 600 micrograms to six healthy males, according to double‐blind, within subjects, experimental designs vs placebo. Vital signs, ECG, laboratory tests and the appearance of newly observed signs and symptoms were monitored. A dose‐ related decrease of serum PRL in comparison with both basal and post‐ placebo levels was observed after 200 micrograms and greater doses of the compound, with inhibition of spontaneous circadian rhythm. Maximal inhibition (PRL less than 2 ng ml‐1) was observed in one out of five subjects after 200, three out of seven subjects after 300, four out of six after 400 and five out of six subjects after 600 micrograms. The effect was of rapid onset and long duration; the maximum or nearly maximum decrease was observed within 3 h after dosing as well as up to 96 h (200 and 300 micrograms) and up to 168 h (400 and 600 micrograms). No modifications of GH, TSH, LH and cortisol as well as of vital signs, ECG and laboratory tests were apparent.(ABSTRACT TRUNCATED AT 250 WORDS)Keywords:
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Μελέτη της πολυπαραγοντικής αναλγησίας στο μετεγχειρητικό πόνο μετά από λαπαροσκοπική χολοκυστεκτομή
Σκοπός:Ο βασικός σκοπός της μελέτης ήταν να ελεγχθεί αν ο συνδυασμός γκαμπαπεντίνης (600mg 4ώρες προεγχειρητικά, 600mg 24ώρες μετά), κεταμίνης (0.3mg/kg πριν την αναισθησία), λορνοξικάμης (8mg πριν την αναισθησία και 8mg/12ώρες) και τοπικής έγχυσης ροπιβακαΐνης (5ml 7.5% στα σημεία εισόδου των trocar) έχει καλύτερη αναλγητική δράση σε σχέση με το καθένα από αυτά τα φάρμακα ξεχωριστά τις πρώτες 24 ώρες μετά από λαπαροσκοπική χολοκυστεκτομή. Δευτερεύων σκοπός ήταν να εξετασθεί αν αυτός συνδυασμός έχει λιγότερες επιπλοκές σχετιζόμενες με την κατανάλωση οπιοειδών.Μέθοδος:Διεξήχθη μία ελεγχόμενη τυχαιοποιημένη μελέτη σε 2 νοσηλευτικά κέντρα. 148 ασθενείς ηλικίας 18-70 ετών κατανεμήθηκαν τυχαία σε 6 ομάδες (28 σε κάθε ομάδα) με τη χρήση λογισμικού: A (γκαμπαπεντίνη/κεταμίνη/λορνοξικάμη/ροπιβακαΐνη), B (γκαμπαπεντίνη/placebo/placebo/placebo), Γ (placebo/κεταμίνη/placebo/placebo), Δ (placebo/placebo/λορνοξικάμη/placebo), E (placebo/placebo/placebo/ροπιβακαΐνη) και ΣΤ (placebo/placebo/placebo/placebo). Μόνο ο κύριος ερευνητής γνώριζε την ομάδα κάθε ασθενούς και παρείχε τα φάρμακα και τα εικονικά φάρμακα σε καλυμμένες προγεμισμένες σύριγγες. Η κύρια έκβαση της μελέτης ήταν η 24ωρη κατανάλωση μορφίνης. Δευτερεύουσες εκβάσεις ήταν η συχνότητα των σχετιζόμενων με τα οπιοειδή επιπλοκών (ναυτία, έμετος, καταστολή, κνησμός και δυσκολία ούρησης).Αποτελέσματα:Μόνο οι ομάδες Α (6.4mg), B (9.46mg) και Δ (9.36mg) είχαν χαμηλότερη κατανάλωση μορφίνης σε σχέση με την ομάδα ελέγχου (20.29mg) (p<0.001, p=0.01 και p=0.008 αντίστοιχα). Η ομάδα Α δε διέφερε από τις ομάδες Β και Δ (p=0.92, p=0.93). Υπήρξε διαφορά μόνο στα επεισόδια ναυτίας και μόνο μεταξύ των ομάδων Α (n=5) και της ομάδας ελέγχου (n=12) (p=0.018). Συμπεράσματα:Ο συνδυασμός γκαμπαπεντίνης, κεταμίνης, λορνοξικάμης, και τοπικής έγχυσης ροπιβακαΐνης δεν έχει ισχυρότερη αναλγητική δράση σε σχέση με μόνη την γκαμπαπεντίνη ή τη λορνοξικάμη μετά από λαπαροσκοπική χολοκυστεκτομή. Ο συνδυασμός μειώνει μόνο τη συχνότητα της μετεγχειρητικής ναυτίας αλλά απαιτούνται μεγαλύτερες μελέτες για την εξαγωγή ασφαλών συμπερασμάτων.
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Pituitary prolactin has been quantified by radioimmunoassay in whole milk obtained from cattle, goats, sheep and rats. Prolactin concentrations in milk samples obtained following the completion of lactogenesis approximate concentrations of the hormone in blood plasma or serum. However, concentrations of prolactin in prepartum mammary secretions were much higher than plasma prolactin in prepartum dairy cows. This observation was consistent with the hypothesis that during mammary lactogenesis, endogenous milk prolactin in the alveolar lumen may be an additional source of biologically active prolactin. The value of milk prolactin to neonatal animals remains unknown. Experiments with milk-fed calves and suckling rats failed to demonstrate absorption of the intact molecule into the neonate's blood. Further research is needed to determine the role, if any, that maternal prolactin consumed in milk plays in neonatal physiology. Measurements of milk prolactin seem to be highly predictive of the average blood prolactin concentration. Milk prolactin can probably be used in lactating females to predict average plasma prolactin in a manner that is relatively independent of stress- or milking-induced increases in pituitary release of the hormone.
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Basal serum prolactin concentrations have been measured in 50 normal prepubertal children. There was no significant difference in prolactin levels between males and females and all concentrations were within the normal range for adult females (3-15 mug/l). Prolactin concentrations before and during insulin hypoglycaemia and intravenous thyrotrophin releasing hormone (TRH) have been measured in normal children of short stature, in children with isolated growth hormone (GH) deficiency and in those with hypothalamo-pituitary disease. There was no difference in either basal or stimulated prolactin levels in the normal group compared with the isolated GH-deficient group. In most of the children with hypothalamo-pituitary disease basal prolactin concentrations were within the normal range but there was an impaired response to both hypoglycaemia and TRH. Basal and stimulated levels of prolactin are compared in the same subjects with those of GH, thyroid stimulating hormone and the gonadotrophins and the clinical value of the dynamic tests described is discussed.
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Prolactin has been separated from growth hormone (GH) in extracts from sheep and cattle pituitaries, but not when human pituitaries were used. The prolactin activity found in most human growth hormone (HGH) preparations (Li & Liu, 1964; Forsyth, Folley & Chadwick, 1965) supports the hypothesis that HGH and human prolactin (H-Pr) are biologically and immunologically related and suggests that both activities reside in the same molecule (Irie & Barrett, 1962). However, Chen & Wilhelmi (1964) have reported that prolactin activity can be separated from that of GH by chromatography. Moreover, Pasteels, Brauman & Brauman (1963), using tissue cultures of human pituitary cells, found a rapid decrease of GH activity in the medium but an increase in prolactin activity. The present report describes the immunological properties of a human prolactin preparation (Apostolakis, 1965) more potent than any previous preparation. The activities of batches XVI-R8 and XVII-R8 of human prolactin
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Abstract Prolactin response to suckling was studied in a group of fully breast feeding women ( N = 58) between 4–6 weeks postpartum. Basal, suckling stimulated and the increment of prolactin showed wide individual variations. Basal prolactin concentrations varied from 140 to 4,600 mlU/ l , suckling stimulated prolactin from 400 to 5,600 mlU/ l and the increment of prolactin from 40 to 4,160 mlU/ l . Basal (p = 0.0395) and suckling stimulated (p = 0.0423) prolactin concentrations significantly increased as the number of night breast feeds increased and the suckling stimulated (p = 0.0218) prolactin concentrations significantly increased as the number of breast feeds/24 h increased. However, the magnitude of the rise in prolactin in response to suckling was not dependent on basal prolactin concentration. Basal, suckling stimulated or the increment of prolactin were not significantly different between subjects having different breast feeding frequencies, when the subjects were grouped according to the number of breast feeds. These differences may be due to the large individual variation in prolactin concentrations seen in women having similar breast feeding frequencies which may arise from individual variations in hypotha‐lamic — pituitary response to suckling.
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Prolactin is a human peptide hormone synthesized in the anterior pituitary by the lactotrophs. Prolactin is responsible for breast epithelial cell proliferation and milk production during pregnancy and after delivery. This chapter discusses the physiology, laboratory tests, indications, screening, and evaluation of prolactin. During pregnancy, the prolactin level is normally elevated to support those functions in pregnant and lactating females; the prolactin level can become 10 times the normal level in pre-pregnancy. Otherwise, the prolactin level is low in males and nonpregnant or lactating females. Prolactin can be measured from a serum sample that should be drawn after fasting. Prolactin may be used to evaluate signs/symptoms suspicious for hypo- or hyperprolactinemia.
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