◉ Summary of Use during Lactation:Limited information on the use of rocuronium during breastfeeding indicates that no adverse infant effects occur. Because it is short acting, highly polar and poorly absorbed orally, it is not likely to reach the breastmilk in high concentration or to reach the bloodstream of the infant. When a combination of anesthetic agents is used for a procedure, follow the recommendations for the most problematic medication used during the procedure. General anesthesia for cesarean section using rocuronium as a component may delay the onset of lactation.
◉ Effects in Breastfed Infants:Four mothers who were breastfeeding 3- to 5-month-old infants underwent general anesthesia were given intravenous propofol and remifentanil as induction agents and rocuronium 0.5 mg/kg for intubation. After induction, propofol was stopped and xenon inhalation was used to maintain anesthesia for between 57 and 70 minutes. Infants resumed breastfeeding from 1.5 to 5 hours after the end of surgery. None of the infants had noticeable symptoms of dizziness or drowsiness. All infants fared well at home after their mothers were discharged with no adverse events noticed at home.
◉ Effects on Lactation and Breastmilk:A randomized study compared the effects of cesarean section using general anesthesia, spinal anesthesia, or epidural anesthesia, to normal vaginal delivery on serum prolactin and oxytocin as well as time to initiation of lactation. General anesthesia was performed using propofol 2 mg/kg and rocuronium 0.6 mg/kg for induction, followed by sevoflurane and rocuronium 0.15 mg/kg as needed. After delivery, patients in all groups received an infusion of oxytocin 30 international units in 1 L of saline, and 0.2 mg of methylergonovine if they were not hypertensive. Fentanyl 1 to 1.5 mcg/kg was administered after delivery to the general anesthesia group. Patients in the general anesthesia group (n = 21) had higher post-procedure prolactin levels and a longer mean time to lactation initiation (25 hours) than in the other groups (10.8 to 11.8 hours). Postpartum oxytocin levels in the nonmedicated vaginal delivery group were higher than in the general and spinal anesthesia groups.
[EN] PHARMACEUTICAL COMPOSITIONS OF POLYANIONIC AND NON-IONIC CYCLODEXTRIN-BASED DENDRIMERS AND USES THEREOF<br/>[FR] COMPOSITIONS PHARMACEUTIQUES DE DENDRIMÈRES À BASE DE CYCLODEXTRINE POLYANIONIQUE ET NON-IONIQUE ET UTILISATIONS ASSOCIÉES
申请人:LING CHANG-CHUN
公开号:WO2016161501A1
公开(公告)日:2016-10-13
The present application provides pharmaceutical compositions comprising polyanionic and polynon-ionic cyclodextrin-based dendrimers. The compositions can be used as excipients, or to bind to compounds such as in the use as a rescue medicine to remove undesired drugs and metabolites from a subject. Methods of use in treating a subject are also provided.
METHODS AND SYSTEMS FOR DESIGNING AND/OR CHARACTERIZING SOLUBLE LIPIDATED LIGAND AGENTS
申请人:TUFTS MEDICAL CENTER
公开号:US20160052982A1
公开(公告)日:2016-02-25
The present application provides methods for preparing soluble lipidated ligand agents comprising a ligand entity and a lipid entity, and in some embodiments, provides relevant parameters of each of these components, thereby enabling appropriate selection of components to assemble active agents for any given target of interest.
[EN] TRIAZOLOBENZAZEPINES AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS<br/>[FR] TRIAZOLOBENZAZÉPINES UTILISÉES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE V1A
申请人:RICHTER GEDEON NYRT
公开号:WO2019116324A1
公开(公告)日:2019-06-20
The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.
[EN] POLYMERIC HYPERBRANCHED CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS POLYMÉRIQUES HYPERBRANCHÉS
申请人:ASCENDIS PHARMA AS
公开号:WO2013024048A1
公开(公告)日:2013-02-21
The present invention relates to water-soluble carrier-linked prodrugs of formula (I),wherein POL is a polymeric moiety,each Hyp is independently a hyperbranched moiety,each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water- soluble carrier-linked prodrugs and methods of treatment.
A prodrug composition is provided which includes a pharmaceutical species and an amino acid having a covalent bond to the pharmaceutical species. The pharmaceutical species is characterized by bioavailability of 30% or less and a molecular weight in the range of 100-1000 Daltons. The composition is characterized further in that the pharmaceutical species is not acyclovir, ganciclovir, BRL44385, or penciclovir. Also described is an inventive method of delivering a pharmaceutical species to an individual including the step of orally administering an inventive prodrug to an individual. In one embodiment the prodrug includes a pharmaceutical species characterized by bioavailability of 30% or less, wherein the pharmaceutical species has a molecular weight in the range of 100-1000 Daltons. The inventive prodrug is transported from the gastrointestinal lumen by a specific transporter and is enzymatically cleaved to yield the pharmaceutical species, such that the pharmaceutical species is delivered to the individual.