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At least 19 recordsLinked to original sources
PubMed1990

Oral premedication in children. A comparison of trimeprazine with a trimeprazine, droperidol and methadone mixture.

One hundred children who presented for minor general surgical procedures were randomly assigned to receive one of two oral premedications. Those in group A (n = 50) were given 3 mg/kg of trimeprazine and those in group B (n = 50) a mixture of trimeprazine 1.0 mg/kg, droperidol 0.15 mg/kg and methadone 0.08 mg/kg. Patients in group B were more likely to be asleep on arrival in the anaesthetic room (p less than 0.02) and were less likely to be distressed at induction of anaesthesia (p less than 0.02). Thiopentone requirements were less in group B (p less than 0.001). The incidence of side effects was similar in the two groups. It is concluded that the mixture produces more satisfactory sedation than trimeprazine.

Administration, Oral↗
PubMed1997

Oral midazolam compared with diazepam-droperidol and trimeprazine as premedicants in children.

Ninety children were assigned randomly to one of three groups for premedication with oral midazolam 0.5 mg.kg-1, diazepam 0.25 mg.kg-1 with droperidol 0.25 mg.kg-1, or trimeprazine 2 mg.kg-1. On arrival at the anaesthetic room, anxiolysis was satisfactory in 26 out of 29 (90%) children who received midazolam compared with 23 out of 29 (79%) who received diazepam-droperidol and 18 out of 29 (62%) who received trimeprazine (P < 0.05); at induction of anaesthesia these proportions were 24 out of 29 (83%), 16 out of 29 (55%) and 11 out of 29 (40%) respectively (P < 0.001). When individual groups were compared, anxiolysis was significantly greater in the midazolam group compared with the trimeprazine group on arrival in the anaesthetic room (P < 0.05) and significantly greater in the midazolam group than in either the diazepam-droperidol or the trimeprazine groups at induction of anaesthesia (P < 0.05 and P < 0.001 respectively). There were no significant differences in times to early recovery between the groups (25.4, 24.4 and 28.5 min). Analysis of behavioural questionnaires completed two weeks after hospitalization showed a trend towards fewer postoperative behavioural disturbances in children who received midazolam or diazepam-droperidol compared with trimeprazine (47 and 44% vs 75%); when the results for the benzodiazepine-containing premedicants were combined, the difference between these groups and trimeprazine was statistically significant (P < 0.05).

Adjuvants, Anesthesia↗
PubMed1997

Studies on antimicrobial effect of the antihistaminic phenothiazine trimeprazine tartrate.

The antibacterial and bactericidal activities of the antihistamine trimeprazine were studied against 243 strains of bacteria which included both Gram positive and Gram negative types. The susceptibility of these bacterial strains to trimeprazine was assessed by determining their minimum inhibitory concentration (MIC) which was found to be between 10 and 100 micrograms/ml. Nineteen strains of Staphylococcus spp. and Salmonella spp. were trimeprazine. Most of the strains belonging to Bacillus spp. and Salmonella spp. were inhibited by less than 100 micrograms/ml. Trimeprazine could also inhibit strains of Shigella spp. Vibrio cholerae and V. parahaemolyticus at 10-100 micrograms/ml. Strains of klebsiella, proteus, pseudomonas and citrobacter were moderately sensitive to trimeprazine. In in vivo studies it was seen that when trimeprazine was used at a concentration of 0.75 and 0.4 micrograms/gm body weight of the mouse both levels offered significant protection to Swiss mice challenged with 50LD50 of virulent strain of S. typhimurium 74. Statistical analysis of the data was found to be significant, p < 0.001 according to chi 2 test.

Animals↗
PubMed1984

Radioimmunoassay for trimeprazine in human plasma.

Antisera to trimeprazine were raised in New Zealand white rabbits to an immunogen synthesized by covalent linkage of bovine serum albumin to N-(2-carboxyethyl)desmethyltrimeprazine. By use of an antiserum, a radioimmunoassay for trimeprazine was developed that is able to quantitate 0.38 ng/ml-1 in a 200 microliter plasma sample with a coefficient of variation of approximately 12%. The antiserum did not cross-react with the supposedly pharmacologically inactive metabolite trimeprazine sulfoxide; however, the cross-reactivity with the supposedly active metabolite N-desmethyltrimeprazine is significant (49%). The radioimmunoassay was able to measure the drug and/or N-desalkyl metabolites in plasma samples obtained as late as 24 hr following administration of a single oral dose (10mg) of trimeprazine tartrate. Analysis of the same plasma samples by a published high-performance liquid chromatographic procedure gave values much lower than those obtained by the radioimmunoassay, indicating the N-desalkyl metabolites are produced significantly after trimeprazine oral administration.

Antibody Affinity↗
PubMed1986

Temazepam and trimeprazine compared with placebo as premedication in children. An investigation extended into the first 2 weeks at home.

Temazepam, trimeprazine and placebo were compared as premedication in 85 children undergoing routine otolaryngological operations. Premedication with trimeprazine caused significantly more sedation than temazepam or placebo in patients on arrival in the anaesthetic room (P less than 0.02). Recovery time was significantly longer after trimeprazine than temazepam or placebo (P less than 0.012). Significantly more children (P less than 0.05) failed to recall a picture shown immediately before induction after trimeprazine and temazepam than with placebo. Fewer patients vomited after operation with trimeprazine than with temazepam or placebo (P less than 0.01). The majority of children exhibited some behavioural problem during the first 2 weeks at home, although this rarely lasted for more than a few days. More children exhibited apathetic/withdrawn behaviour after receiving placebo (P less than 0.05), although the significance of this should be interpreted with caution.

Anesthesia Recovery Period↗
PubMedDate not supplied

Determination of trimeprazine-facilitated sedation in children by hair analysis.

Trimeprazine or alimemazine is largely used as an antipruritic agent, but it is also used for insomnia, cough, and oral premedication in pediatric day surgery. The first cases involving repetitive sedation linked to the use of trimeprazine as a drug-facilitated crime and subsequent impairment of two children are reported. Because of the long delay between the alleged crime and clinical examination, collection of blood or urine was of little value. This is the reason why the laboratory developed an original approach based on hair testing by liquid chromatography-tandem mass spectrometry. A strand of hair from each child was sampled about 2 months after the first suspicion of administration and was cut into small segments. After cutting into small pieces, 20 mg of hair was incubated overnight in a phosphate buffer (pH 8.4). The aqueous phase was extracted by 5 mL of a mixture of diethyl ether/methylene chloride (80:20) in presence of diazepam-d(5) used as the internal standard (IS). Hair extract was separated on a XTerra MS C18 column using a gradient of acetonitrile and formate buffer. Detection was based on two daughter ions: transitions m/z 299.3 to 299.0 and 100.0 and m/z 289.9 to 154.0 for trimeprazine and the IS, respectively. In the hair of the two subjects, trimeprazine was detected at concentrations in the range 23 to 339 pg/mg. The stepmother, who was the perpetrator in both cases, did not challenge the use of trimeprazine as a sedative drug.

Adolescent↗
PubMed1999

In vitro and in vivo study of the antithyroid side effects of trimeprazine.

Trimeprazine (TMP), a phenothiazine used as antipsychotic drug, was previously shown to induce a decrease in thyroid hormone serum levels in rats. Different mechanisms might be involved, mainly (i) a central mechanism, involving a reduction of thyroid-stimulating hormone (TSH) secretion; (ii) a peripheral mechanism, acting upon the synthesis of thyroid hormones, by inhibition of thyroperoxidase (TPO) or trapping of molecular iodine present in the thyroid gland. These different hypotheses were investigated in the present study, using in vitro and in vivo experiments. In vitro studies concerned TMP and its three main metabolites: trimeprazine sulphoxide (TSO), N-desmethyl trimeprazine (NDT), and 3-hydroxy-trimeprazine (3-OHT). TMP and TSO expressed a high affinity for iodine in vitro, contrary to NDT, which did not complex iodine. Only 3-OHT inhibited TPO in vitro. Administration of 5 mg/kg TMP ip twice daily for 11 days to Wistar rats induced a decrease of free triiodothyronine and free thyroxine (fT(3) and fT(4)) and a trend toward an increase of TSH serum levels. Thyroid concentrations of TMP, NDT, and TSO were significantly higher than serum levels, while 3-OHT was never detected. An iodine-supplemented diet administered to a group of rats treated with TMP significantly increased the thyroid concentration of TMP and TSO, but not that of NDT, while it did not affect the concentrations observed in serum and other organs. The increase in plasma TSH is not consistent with the central mechanism hypothesis, and the absence of TPO inhibition by TMP, TSO, and NDT contradicts the TPO inhibition hypothesis. On the contrary, three findings support the hypothesis of iodine trapping through formation of a complex with TMP and TSO: these molecules complex iodine in vitro, they accumulate in the thyroid, and their thyroid concentration is increased when the rats are fed an iodine-supplemented diet.

Animals↗
PubMed2005

A comparative study on the effects of oral amiodarone and trimeprazine, two in vitro retinyl ester hydrolase inhibitors, on the metabolic availability of vitamin A in rats.

Amiodarone, an antiarrhythmic drug, and trimeprazine, an antipsychotic drug, are both in vitro inhibitors of retinyl ester hydrolase. To determine whether these agents have deleterious effects on aspects of vitamin A metabolism, Brown Norway rats (n 18) were treated at clinically equivalent doses once daily for 26 d with either oral drug. On day 27, a tolerance test was used to determine whether these agents interfered with vitamin absorption. During the first 8 d, the plasma retinol level declined in all animals. Between days 12 and 27, it rose to near pre-treatment concentrations in the control and trimeprazine groups and remained relatively constant at low levels (P<0.001) in the amiodarone group. The intestinal absorption of vitamin A was reduced (P<0.05) in the amiodarone group compared with the placebo and trimeprazine groups, which did not differ significantly from each other. At the end of the 4-week treatment period, hepatic retinyl ester hydrolase activity was lower in the drug-dosed rats (P=0.06 for amiodarone) than in the controls. With regard to effects on liver reserves, drug treatment resulted in vitamin A depletion (P<0.019), and distinctive patterns of retinol and its esters were seen in response to dosing. In conclusion, amiodarone and trimeprazine have been shown to influence different aspects of retinoid metabolism, namely absorption, storage and transport. In clinical practice, the routine unmonitored use of these drugs and the suggestion that these agents be taken with meals are not recommended.

Absorption↗
PubMed1990

Pharmacokinetics of trimeprazine in children.

The pharmacokinetics of trimeprazine (alimemazine) were studied over 24 hr in six children after a recommended preanaesthetic oral dose of 3 mg.kg-1. The degree of sedation before anaesthesia was evaluated. Median maximal venous blood drug concentration was 0.357 mumols.1(-1), 1-2 hr after oral ingestion, half-life 6.8 hr and AUC0-infinity h 2.758 mumols.1(-1) hr. Assuming 100 per cent bioavailability, blood clearance was estimated to median 3.7 1.kg-1.hr-1. Trimeprazine concentrations in cerebrospinal fluid (CSF) and in venous blood were compared in three other children, measured by gas chromatography. No trimeprazine was detected in the cerebrospinal fluid. We found a rough correlation between preanaesthetic sedation and blood trimeprazine concentrations. The kinetic parameters showed substantial interindividual differences, and accordingly, major interindividual variations in drug response might be anticipated even on standardized dosage regimens.

Administration, Oral↗
PubMed1986

Relative bioavailability of trimeprazine tablets investigated in man using HPLC with electrochemical detection.

The stability, partition coefficient, plasma protein binding, red blood cell distribution, and whole blood concentrations of trimeprazine were investigated. Trimeprazine solution was stable for 6 months at -20 degrees C and 3.5 months at 40 degrees C. In whole blood trimeprazine was stable for 5 weeks at -20 degrees C, 24 h at 4 degrees C, 4 h at 25 degrees C and 1 h at 37 degrees C. The apparent hexane-water partition coefficient varied from 1.50 (at pH 4.83) to over 100 (at pH 10.54). The fraction bound to plasma protein exceeded 0.9 as estimated by equilibrium dialysis with correction for volume shift. The mean plasma/red blood cell concentration ratio was 1.17 and the mean red blood cell/plasma distribution coefficient was 8.65. Six healthy adult males received single 5 mg doses of trimeprazine in a syrup (5 mg in 10 ml) and tablets with at least two weeks between doses. Blood was collected for 48 h. The mean (+/- s.e.m.) times for peak blood concentrations were 3.5 +/- 0.22 h for the syrup and 4.5 +/- 0.43 h for the tablets. There were no significant differences in Cmax values. The overall mean (+/- s.e.m.) terminal phase half-life was 4.78 +/- 0.59 h. Mean (+/- s.e.m.) areas under the concentration time curves from 0 to infinity (AUC infinity) were 11.0 +/- 1.99 ng h-1 ml-1 and 7.67 +/- 1.05 ng h-1 ml-1 for syrup and tablets, respectively. The mean relative bioavailability for the tablets was approximately 70% with respect to the syrup.

Adult↗
PubMed1992

Identification of new urinary metabolites of trimeprazine in rats by gas chromatography-mass spectrometry.

The metabolites of trimeprazine were identified in urine of rats by gas chromatography-mass spectrometry. After the oral administration of trimeprazine, the urinary metabolites were extracted with diethyl ether before or after hydrolysis with beta-glucuronidase. The identified metabolites were N-demethyltrimeprazine,3-hydroxytrimeprazine,N-demethyl-3-++ +hydroxytrimeprazine and trimeprazine sulphoxide.

Animals↗
PubMed1984

Premedication for children with oral trimeprazine and droperidol.

In 60 children aged 1-9 years, weighing under 33 kg, oral trimeprazine and oral trimeprazine plus droperidol were compared as premedicants in a controlled, double-blind clinical trial. The addition of droperidol to the trimeprazine syrup produces greater uniformity in pre-operative sedation, a low incidence of postoperative vomiting, and a reduced requirement for postoperative analgesia.

Administration, Oral↗
PubMed1997

A comparison of midazolam with trimeprazine as an oral premedicant for children.

The effect of oral premedication was investigated in a double-blind, randomised trial in 85 children undergoing tonsillectomy and/or adenoidectomy. Orally administered midazolam 0.5 mg.kg-1 given 30 min pre-operatively was compared with trimeprazine 2 mg.kg-1 given 90 min pre-operatively and a placebo preparation. Compliance, sedation and ease of induction were assessed as were the duration and quality of recovery. Following premedication with midazolam none of the patients was anxious, crying or distressed on leaving the ward, compared with 2/28 in the trimeprazine group and 5/28 in the placebo group (p = 0.0007). More patients were calm and quiet on arrival in the anaesthetic room following midazolam than following trimeprazine, with both premedicant agents comparing favourably with placebo. There was no significant difference between the three groups in the time to recovery or the sedation score on discharge to the ward. Midazolam is a safe and effective oral premedicant for children.

Adenoidectomy↗
PubMed1987

Controlled trial of trimeprazine tartrate for night waking.

Mild hypnotics are often recommended for young children with sleep problems. This study assesses the efficacy of trimeprazine tartrate in 1 to 3 year old children with persistent and severe night waking in a double blind crossover trial with placebo. Children on treatment with trimeprazine had significantly fewer wakings, less time awake at night, and more night time sleep compared with those on treatment with placebo. There were no differences in these sleep variables when the first and last (fourth) week of treatment with drugs were compared. Follow up observations showed no significant difference in any sleep variables from baseline measures. The results are consistent with the idea that trimeprazine tartrate may be a useful short term treatment for night waking in young children.

Child, Preschool↗
PubMed1990

Trimeprazine as oral premedication in children.

The effect of oral trimeprazine alone or in combination with either atropine or glycopyrrolate or pethidine as oral premedication in children was studied. The effects of different drug combinations were evaluated in respect of pre-operative sedation, salivary secretion, induction characteristic, postoperative sedation and postoperative vomiting. The study concludes that trimeprazine in combination with either atropine or glycopyrrolate is mostly effective, safe and satisfactory as oral premedication in children. Trimeprazine along with pethidine can be recommended for all purpose oral medication both in pre- and post-operative period.

Administration, Oral↗
PubMed1990

On-line recovery of trimeprazine enantiomers following chiral separation by reversed-phase high-performance liquid chromatography using a beta-cyclodextrin-containing mobile phase.

A procedure is described which allows the on-line recovery of enantiomers following semi-preparative chiral separation by RP-HPLC using beta-cyclodextrin in the mobile phase. By this method, the phenothiazine antihistamine trimeprazine (I) was resolved into its antipodes at greater than 95% optical purity at a throughput of more than 1 mg of each enantiomer per hour, using 4 mm i.d. columns. The recovered trimeprazine was found to be free from cyclodextrin.

Chromatography, High Pressure Liquid↗
PubMed1999

A multiple-baseline, double-blind evaluation of the effects of trimeprazine tartrate on infant sleep disturbance.

Infant sleep disturbance involving chronic night waking and resistance to settling to sleep or returning to sleep is a common problem for families with children 6-27 months old. Prescription and nonprescription sedatives are frequently administered without clear evidence that they are effective as either long-term or short-term palliatives. Trimeprazine tartrate, administered either 15 mg/5 mL or 30 mg/5 mL, was compared with both baseline and placebo in a multiple-baseline-across participants, double-blind study. No clinically significant effects of the low dose were detected, whereas the effects of the high dose were not consistently replicated across nor within participants. During active drug treatment, only 2 of 12 children achieved Sleep Behaviour Scale scores indicative of nonproblem sleep. Trimeprazine tartrate is not recommended as a pharmacological treatment for infant sleep disturbance unless as an adjunct to a behavioral therapy program.

Child, Preschool↗
PubMed1981

Premedication of children with trimeprazine tartrate.

A double-blind trial was undertaken to compare the effects of trimeprazine tartrate (2 mg kg-1 or 4 mg kg-1) plus atropine 0.03 mg kg-1 for oral premedication of 192 children undergoing tonsillectomy. Demeanour before operation, side-effects after operation, recovery times and fluid balance were studied. Behaviour in the anaesthetic room and restlessness after operation were unaffected by the dose given. There was less vomiting associated with 4 mg kg-1 compared with 2 mg kg-1. Prolonged recovery times occurred frequently in the two groups, 14% in the small- and 17% in the large-dose groups taking more than 10 h to recover full mental faculties. Fluid balance was unaffected by the dose and prolonged recovery did not result in a reduction of urine output. Trimeprazine tartrate is not recommended for routine premedication when early recovery is required.

Administration, Oral↗