Rociverine

BACKGROUND: Prolonged labour can lead to increased maternal and neonatal mortality and morbidity due to increased risks of maternal exhaustion, postpartum haemorrhage and sepsis, fetal distress and asphyxia and requires early detection and appropriate clinical response. The risks for complications of prolonged labour are much greater in poor resource settings. Active management of labour versus physiological, expectant management, has shown to decrease the occurrence of prolonged labour...

BACKGROUND: Prolonged labour can lead to increased maternal and neonatal mortality and morbidity due to increased risks of maternal exhaustion, postpartum haemorrhage and sepsis, fetal distress and asphyxia and requires early detection and appropriate clinical response. The risks for complications of prolonged labour are much greater in poor resource settings. Active management of labour versus physiological, expectant management, has shown to decrease the occurrence of prolonged labour...

OBJECTIVE: To determine the effectiveness of rociverine, an antispasmodic drug, for reducing the duration of labor among nulliparous women managed according to a standard intrapartum protocol. DESIGN: Randomized controlled trial. SETTING: An academic tertiary care hospital. POPULATION: Nulliparae in spontaneous active labor, with cervical dilatation between 3 and 5 cm. METHODS: Participants were randomly assigned to receive either an intramuscular injection of 20mg rociverine (n=55) or the same volume of saline (n=56)...

The aim of this work was to develop and validate a method to assess the dissolution behaviour of rociverine sugar-coated tablets. In our laboratories, an HPLC-MS in reverse phase method of analysis was developed for the dosage of unknown rociverine solution. This analytical method was applied to determine the dissolution rate of rociverine tablets produced by the industrial procedure, because there is no official method description. Dissolution tests were carried out in sink conditions as follows: dissolution medium HCl 0...

The chemical structure corresponding to 1-hydroxy[1,1'-bicyclohexyl]-2-carboxylic acid 2-(diethylamino)-1-methylethyl ester has the classical profile of ester-type antimuscarinic drugs. The presence of three chiral carbons leads to eight stereoisomers and the substitutions on the cyclohexyl ring generate cis-isomers (1, named rociverine) and trans-isomers (2). The aim of this study was to determine the binding pattern of the eight stereoisomers and two derived compounds, (1S,2S)-1-hydroxy[1,1'-bicyclohexyl]-2-carboxylic acid 2-(dimethylamino)-1-ethyl ester (3) (1S,2S)-1-hydroxy[1,1'-bicyclohexyl]-2-carboxylic acid (S)-2-(diethylamino)-1-methylethyl ester methyl iodide (4), at the five cloned muscarinic receptors stably expressed in chinese hamster ovary cells, in order to define how stereochemical modifications could affect the affinity...

Rociverine [2-(diethylamino)-1-methylethyl cis-1-hydroxy [bicyclohexyl]-2-carboxylate] citrate (ROC) is an antispasmodic agent therapeutically active in humans at doses of 0.5-1 mg/kg. This study investigated the effect of acute administration of the drug on hepatic microsomal cytochrome P450 (P450)-catalysed drug metabolism. Only high doses (> or = 100 mg/kg) of ROC were able to induce in rats the hepatic microsomal pentoxyresorufin O-depenthylase (PROD) and 16 beta-testosterone hydroxylase activities both associated with P4502B1/2 and the erythromycin N-dimethylase (ErD) and 2 beta-testosterone hydroxylase activities both dependent on P4503A1/2...

Forty outpatients of both sexes suffering from irritable colon syndrome were treated for four weeks with rociverine, an antispastic agent with anti-muscarinic and direct miolytic activities, at a dose of 20 mg x 3. The aim of the study was to assess the efficacy and tolerability of this dose since the drug is normally administered at a dose of 30-40 mg a day. The efficacy of treatment was assessed on the basis of the evolution of clinical symptoms, whereas its tolerability was evaluated in both clinical and biohumoral terms...

No abstract text is available yet for this article.

The musculotropic action of dicyclomine hydrochloride in bladder muscle has been attributed to its local anesthetic activity. In this study rabbit detrusor strips were depleted of calcium by incubation in Ca2+-free solution containing ethylene glycol bis(beta-aminoethyl ether)-N,N'-tetraacetic acid (EGTA). Contractions elicited by replacement of Ca2+ during depolarization with 80 mM K+ were only slightly affected by atropine or scopolamine but were antagonized in a noncompetitive manner by dicyclomine and rociverine (pD2' = 4...

No abstract text is available yet for this article.

Thirty-seven subjects without eye diseases were treated with rociverine, a new direct myolytic and parasympatholytic antispasmodic: 15 by intravenous injection (20 mg) and 22 by oral administration (20 mg three times daily for four days). Intraocular pressure, pupil size, iridocorneal angle, blood pressure, and heart rate were checked before and during treatment. No clinically significant variations were observed in the parameters tested.

No abstract text is available yet for this article.

No abstract text is available yet for this article.

No abstract text is available yet for this article.

Caerulein (C)-induced delay in gastric emptying (GE), due to pylorospasm, was used as an experimental model for a quantitative test of the activity of some spasmolytic drugs in conscious rats. Rociverine at doses of 10 and 15 mg kg-1 i.p., though not at higher doses, considerably reduced this delay. Of the other drugs tested only papaverine had this effect and to a lesser degree. Atropine, N-butylscopolammonium bromide and dicyclomine proved to be inactive or further reduced GE. The effect of spasmolytics on C pylorospasm seems to be the outcome of two actions possessed by the drugs in varying degree: on the one hand a pyloric sphincter relaxant action, which increases GE, and on the other a relaxant action on the smooth musculature of the stomach, which tends to reduce GE...

105 patients with either biliary colics (54) or ureteral colics (51) were treated with rociverine, a new antispastic drug, at a dose of 20 mg iv. The drug showed a rapid and effective spasmolytic activity (total disappearance of painful symptoms in 89% of patients with biliary colic and in 92% of patients with ureteral colic).

Gallbladder emptying was induced in female albino mice by single oral administrations of 30% lyophylized egg yolk suspension. Mice were killed 15 min later, their gallbladders removed and then weighed. Gallbladder emptying was assessed by comparing weights from control and egg yolk administered mice. The ability of the antispasmodic drugs atropine, N-butylscopolamine, papaverine, trimebutine, dicyclomine, and rociverine to delay gallbladder emptying was determined by administering them either intraperitoneally or orally 7...

No abstract text is available yet for this article.

In a double-blind factorial clinical trial in 300 patients (150 primiparae and 150 multiparae), the effects of amniotomy, rociverine, and butylscopolamine bromide administration on the course of labor were investigated. Rociverine significantly reduced the dilatation time and had no effect on the delivery time. Butylscopolamine bromide had no appreciable effect on the dilatation and expulsion times. Amniotomy resulted in a lengthening of the dilatation time and no significant change in the expulsion time.

The effect of rociverine (10 or 20 mg given intravenously) as premedication in upper gastro-intestinal tract endoscopy was examined and compared to that of hyoscine butylbromide (20 or 40 mg given i.v.) in a double-blind study involving 121 patients. The drugs' effects were assessed on the degree of opening of the pyloric sphincter and the endoscopist's rating of drug performance. The study showed that rociverine did not differ statistically from the reference drug on either count. No adverse effects were noted...