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PubMed1977

Controlled clinical investigation of trimeprazine as a sleep-inducer in normal subjects.

The effects of acute introduction and withdrawal of trimeprazine (Vallergan), an antihistaminic phenothiazine derivative with known sedative effects, were investigated by a single blind polygraphic study in 8 healthy volunteers. A baseline placebo was given on Nights 1-3, followed either by 10 mg or 20 mg of the drug on Nights 4-6, and then withdrawal effects were recorded on Nights 7-9. The subjective effects of the drug and EEG sleep variables were determined on these nights. The results showed that the drug might have had dose related effects. REM-sleep was increased by 10 mg doses, which also caused an increase in SW sleep. There was no significant change after the 20 mg dose. Significant REM rebound was not observed after withdrawal of either dose. These characteristics may be of value in the treatment of certain aspects of sleep disturbances.

Adult↗
PubMed1982

Comparative study of lorazepam and trimeprazine for oral premedication in paediatric anaesthesia.

One hundred and ninety-nine children received lorazepam 0.05 mg kg-1 or trimeprazine 3 mg kg-1 as oral premedication in a double-blind trial. Lorazepam proved more palatable and produced a cheerful demeanour, but possessed no significant advantages on overall assessment before surgery. Following operation, restlessness with vomiting, and evidence of retrograde amnesia occurred more frequently with lorazepam.

Administration, Oral↗
PubMed1983

Lorazepam in children. A double-blind trial comparing lorazepam, diazepam, trimeprazine and placebo.

One hundred patients aged 5-13 yr were randomly allocated to four groups in a double-blind study of premedication. Drugs studied were lorazepam, diazepam and trimeprazine. A placebo group was included. All the drugs appeared satisfactory as premedicants. Lorazepam induced the most sedation immediately after surgery, but by 4 h lorazepam and diazepam appeared similar. Lorazepam produced better amnesia than the other drugs. There were no untoward side-effects and no cardiorespiratory depression in any group. Lorazepam appears a suitable premedicant for children.

Adolescent↗
PubMed1987

Comparison of temazepam elixir and trimeprazine syrup as oral premedication in children undergoing tonsillectomy and associated procedures.

Temazepam 0.5, 1.0 and 1.5 mg kg-1 in an elixir formulation (Euhypnos Elixir), was compared with trimeprazine tartrate 3 mg kg-1 in a syrup (Vallergan Forte Syrup), as premedication in 220 children (ASA grade I) undergoing tonsillectomy and associated procedures. Each patient was randomly allocated to one of the four treatments. The administration was blind to the observers in theatre, recovery room and postoperative ward, who assessed each patient according to a total of 14 criteria. A modelling technique allowed account to be taken of the effects of concomitant variables (e.g. age and duration of anaesthesia) where appropriate. No statistically significant difference was found between the efficacy of the treatments. The only statistically significant differences were that temazepam was associated with more ectopic beats under anaesthesia (P = 0.03 or 0.002, depending on the test applied), more postoperative vomiting (P = 0.04) and more postoperative restlessness (P less than 0.0001).

Adolescent↗
PubMed1990

Oral ketamine premedication for paediatric cardiac surgery--a comparison with intramuscular morphine (both after oral trimeprazine).

In a single-blind controlled study, forty children with congenital heart disease were premedicated with oral trimeprazine 3 mg/kg and either intramuscular morphine 0.1 mg/kg or oral ketamine 10 mg/kg. Cardiovascular and respiratory effects of premedication and degree of sedation induced were similar in the two groups of patients. Oral ketamine is a safe and effective premedicant in this group of patients.

Administration, Oral↗
PubMed2000

A new powerful antibacterial synergistic combination of trimethoprim and trimeprazine.

The antihistaminic phenothiazine trimeprazine (Tz) was found to exhibit significant antibacterial activity on the basis of in vitro and in vivo tests. For the study of synergism due to a combination between Tz and trimethoprim (Tm), drug soaked filter paper discs were placed on young culture lawns of sensitive bacteria on nutrient agar plates. Calculation of the area of inhibition zones for determining the degree of synergism between Tz and Tm showed the increase to be statistically significant (p<0.01) when compared with their individual effects. By the checkerboard assessment procedure, the fractional inhibitory concentration (FIC) index was found to be 0.18, confirming synergism. The protective capacity of this combination was then assessed in Swiss white mice using S. typhimurium as the challenge bacterium, and the level of bacterial load was determined from infected autopsied animals. Statistical analysis of the data by students 't' test finally proved that a combination of Tz+Tm was highly synergistic.

Animals↗
PubMedDate not supplied

Interaction of trimeprazine with cyclodextrins in aqueous solution.

The synergistic effect of pH and complexation with cyclodextrins on some properties of phenothiazine derivative--trimeprazine (TM) was investigated. Inclusion complexes of TM with beta-cyclodextrin (beta-CD) and its substituted derivatives (DM-beta-CD, HP-beta-CD, beta-CDsulf) were obtained in phosphate buffer solution of different pH (6.8; 5.9; 5.0) using spectral and phase solubility methods Irrespective of the method of determination the apparent stability constant of TM-beta-CD system was the greatest and, in the case of the spectral method, its value increased with decreasing pH. The results obtained by the method of solubility diagrams indicate that increase in solubility of the basic form of TM, following decrease of pH, resulted rather from its transformation to a better soluble, protonated form than its inclusion into CD cavity. The thermodynamic parameters estimated from linear Van't Hoff plot suggest that the van der Waals forces were operating in the TM-beta-CD system. The effect of pH and the presence of cyclodextrins on photostability of TM was also investigated. The photochemical decomposition of TM in the absence and in the presence of CD proceeds according to the first order reaction. The charged form of TM was more stable than free base of this drug and hence the stability of TM increases first of all as result of a decrease in pH and then owing to the presence of CD. The data of 13C NMR analysis indicate that the aromatic portion of TM molecule tends to the interior of CD.

Antipruritics↗
PubMedDate not supplied

[Value of trimeprazine among hypnotics in a psychiatric facility].

Trimeprazine (TPZ) has been marketed in France since 1959, as tablets and solution containing respectively 5 mg and 40 mg/ml. TPZ is a phenothiazine derivative with known antihistaminic and sedative effects. The first approved indication for TPZ is in the treatment of allergy. However, its frequent sedative effects are undesirable in this indication. The second approved indication is in the treatment of insomnia (5-20 mg/day) and TPZ is an alternative to conventional hypnotics as diazepam, flunitrazepam, zolpidem, butobarbital... Due to the prescription frequency of this medicine in our hospital, we analyzed the naturalistic prescriptions mode and the clinical end point in patients hospitalized for mental illness. On the one hand, using the hospital prescription software, we analyzed: prescriptions frequency, dose regimen and drug associations with hypnotics, anxiolytics and sedative antipsychotics. On the other hand, we came into contact with physicians in order to know their opinion on TPZ and the whole point of that indication. The results showed a very high prescription frequency (139/400 patients; 35%), a marked increase in dose compared to those approved by the French Drug Administration (5-20 mg/day: 5%; 20-200 mg/day: 95%) and main drug association with hypnotics, tranquilizers or antipsychotics, respectively 38%, 65% and 91%. Clinical end points are: non addictive properties and an easily adequation of posology for the drinkable drop form in contrast with tablets. Thus, TPZ appears as a first-line hypnotic in spite of its adverse effects common to phenothiazine (atropinic and antidopaminergic effects) and is a usefull medicine for the treatment of insomnia in psychotic patients.

Adult↗
PubMed1991

Treatment of infant sleep disturbance by trimeprazine in combination with extinction.

Chronic sleep disturbance is a common problem in preschool children. Prescription and non-prescription sedatives provide short-term palliative relief. Behavioral extinction by withdrawal of parental attention is enduringly effective but may be distressing short-term because of postextinction bursts of intense activity by the child. This study evaluated the effects of combining extinction and sedative medication (trimeprazine tartrate), prescribed in a reducing dose over the first 10 days of extinction. Control groups received either extinction alone or a placebo administered double-blind. After baseline, all subjects reduced their sleep disturbance to low levels, the extinction and placebo groups declining slowly, the medication group abruptly. These gains were maintained at follow-up. Measures of infant security and maternal anxiety showed improvements with treatment.

Arousal↗
PubMed1988

Cardiovascular and respiratory effects of oral premedication with trimeprazine and droperidol in children.

The systolic blood pressure, pulse rate and respiratory rate were assessed in 112 children before and after receiving premedication consisting of trimeprazine (3 mg/kg) and droperidol (0.2 mg/kg) by mouth. A mild (10%) drop in blood pressure was shown, but no statistical difference was found in the other parameters measured. The premedication is highly efficacious, 70% of patients being asleep in the preanaesthetic room; 27% were calm and only 3% were distressed or crying.

Administration, Oral↗
PubMed1979

Effects of trimeprazine and trimipramine on nocturnal scratching in patients with atopic eczema.

Twelve men with severe and long-standing atopic eczema were admitted to a double-blind trial to establish the effects of trimeprazine tartrate, trimipramine maleate, and placebo on nocturnal scratching. Neither of the drugs altered the likelihood of a scratching bout beginning in wakefulness or in any stage of sleep. However, both drugs, especially trimipramine, made sleep less broken, and the reduced time spent in stage 1 of sleep accounted for a modest reduction in the overall amount of scratching during the night.

Adult↗
PubMed1998

A double blind randomized comparison of oral trimeprazine-methadone and ketamine-midazolam for sedation of pediatric dental patients for oral surgical procedures.

The safety and efficacy of an oral sedation technique for children having minor oral surgical procedures under local anesthesia were studied. One hundred healthy children between the ages of 2 and 7 yr received either a combination of midazolam (0.35 mg/kg) and ketamine (5 mg/kg) (Group A), or a combination of trimeprazine (3 mg/kg) and methadone (0.2 mg/kg) (Group B) 30 min preoperatively. Hemodynamic parameters, adverse reactions, postoperative recovery, and behavior were evaluated. More children were asleep, but rousable to verbal commands, 30 min after drug administration in Group A (40%) than in Group B (8%). Immediately before the dental procedure, 46% of children in Group A were asleep in contrast to 8% of children in group B. Significantly more children in Group A were awake, coughing, crying, and moving purposefully 30 and 60 min after admission to the recovery room. Two children (4%) in Group A vomited. Ten (20%) children in Group A hallucinated compared to none in Group B. The surgeon rated the procedure as good or very good in 94% of children in Group A compared to 78% in Group B. Our results show that the combination of midazolam and ketamine, administered orally, is a safe, effective, and practical approach to managing children for minor oral surgical procedures under local anesthesia.

Administration, Oral↗