Delayed profound respiratory depression after premedication with trimeprazine.
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Humans↗
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Oral premedication in children.
Preoperative and postoperative sedation, postoperative analgesia and vomiting were assessed following four different oral premedications in 143 children aged 1-10 years, weighing 10-30 kg, and undergoing elective adenotonsillectomy or inguinal surgery. Diazepam, diazepam combined with droperidol, trimeprazine and trimeprazine combined with droperidol were compared in a double-blind trial in conjunction with a standardised inhalational anaesthetic technique employing an intraoperative narcotic. Trimeprazine produced significantly more preoperative sedation (P less than 0.001) and was associated with enhanced postoperative analgesia (P less than 0.01). The incidence of postoperative vomiting was significantly less in the group receiving trimeprazine (P less than 0.001). The addition of droperidol to diazepam and trimeprazine only marginally improved the performance of those drugs but significantly prolonged postoperative recovery times. This was more marked when droperidol was combined with trimeprazine.
Child↗
Oral premedications in paediatric day surgery.
The degree of sedation in 191 day-stay children after oral premedication were compared. One hundred and forty-six were 1-5 years old (Group 1) and were randomised to receive either chloral 40 mg/kg, midazolam 0.2 mg/kg, promethazine 1 mg/kg, trimeprazine 3 mg/kg or placebo. Forty-five were 5-12 years old and were randomised to receive either trimeprazine 3 mg/kg, midazolam 0.2 mg/kg or placebo (Group 2). The children were assessed using four categories: asleep or drowsy, awake but calm, crying or anxious and oversedated or obstructed airway. They were assessed on leaving the ward, at separation from the parents, at induction, in the recovery room and one and two hours after returning to the ward. In Group 1, it was found that chloral and trimeprazine gave the best degree of sedation but the sedative effect of trimeprazine lasted longer into the post operative period. In Group 2, it was found that the children did not require deep sedation and the anxiolysis obtained with midazolam was adequate.
Administration, Oral↗
Recent advances in the analysis of phenothiazine drugs and their metabolites using high performance liquid chromatography.
HPLC procedures with electrochemical or ultraviolet detection were developed in order to analyze plasma samples from patients and volunteers who had received antipsychotic drugs. Procedures were described for the determination of chlorpromazine and trimeprazine in human plasma. The described procedures for chlorpromazine and trimeprazine demonstrated sufficient sensitivity for their use in pharmacokinetic studies following low single oral doses of these agents. The HPLC-EC procedures for chlorpromazine and trimeprazine were compared with GC-MS and radioimmunoassay procedures, respectively.
Adult↗
The perioperative effects of oral premedication in children.
The pre- and postoperative effects of oral diazepam (0.5 mg/kg), trimeprazine (4 mg/kg), pentobarbitone (3 mg/kg) and a placebo were compared in a randomized double-blind clinical trial in 149 children, aged one to ten years, undergoing adenotonsillectomy. The anaesthetic was standardised and each patient received intraoperative intramuscular papaveretum (0.3 mg/kg). Preoperative sedation was assessed in the ward before transfer onto the theatre trolley, on leaving the ward, on arrival on the theatre floor, on arrival in the induction room and on induction of anaesthesia. There was no significant difference in sedation between the four drug groups except for the placebo group which had a significantly greater unsatisfactory rating at the stage of induction of anaesthesia (P = 0.001). There were no differences in waking times between the diazepam, pentobarbitone and placebo groups, but the trimeprazine group's waking times were significantly prolonged (P less than 0.001). However, the trimeprazine group exhibited significantly less distress in the recovery unit (P = 0.02) and had half the incidence of vomiting (P less than 0.001) than did the other premedication groups.
Adenoidectomy↗
Antihistamine selection in patients with allergic rhinitis.
Seven hundred eighty-two patients diagnosed as having either seasonal allergic rhinitis or perennial allergic rhinitis in a solo allergy practice were given five different antihistamine products representing each of the five classes of antihistamines. The following products were evaluated for 2 weeks each: tripelennamine, diphenhydramine, chlorpheniramine, hydroxyzine, and trimeprazine. Symptoms and side effects were graded 0 to 4. The more troublesome side effects, graded 3 or 4, were tabulated. The antihistamine products in order of increasing frequency of significant side effects were: trimeprazine, chlorpheniramine, hydroxyzine, diphenhydramine, and tripelennamine. The order of antihistamine preference by the patients was chlorpheniramine (27%), diphenhydramine (22%), tripelennamine (20%), hydroxyzine (16%), and trimeprazine (14%). Only seven of 758 patients (less than 1%) were unable to find an acceptable antihistamine class. Patients remained on their antihistamine class of first choice 78% of the time after 1 year, 71% after 3 years and 51% after 5 years. The antihistamine pack provides a rational approach to antihistamine selection in patients with allergic rhinitis.
Chlorpheniramine↗
Self-Association of Phenothiazine Drugs: Influence of the Counterion on the Mode of Association
The association characteristics of the phenothiazine drug trimeprazine tartrate in water and aqueous electrolyte solution have been examined using static and dynamic light scattering techniques and compared with those reported for the structurally related drug promethazine hydrochloride, to identify differences in association pattern arising from differences in the counterions of the two drugs. The association of trimeprazine tartrate was micellar in water and in the presence of added electrolyte. A progressive increase of aggregation number and micellar radius was observed with increase of sodium chloride concentration over the range 0.05 to 0.60 M NaCl. This behavior is in contrast to that of promethazine hydrochloride which exhibits continuous association above the critical concentration in electrolyte of concentrations >/=0.2 M NaCl. Moreover, static light scattering curves for trimeprazine tartrate showed a single discontinuity corresponding to the onset of micellization, whereas the association behavior of promethazine hydrochloride (and other phenothiazine drugs with chloride counterions), in water and dilute electrolyte (0.05-0.1 M NaCl), is complex, with discontinuities in solution properties at several critical concentrations. The results of this study highlight the influence of the counterion on the association characteristics of this class of amphiphile.
Journal Article↗
Enantioseparation of phenothiazines in capillary zone electrophoresis using cyclodextrins as chiral selectors.
In this study, enantioseparations of five phenothiazines, including promethazine, ethopropazine, trimeprazine, methotrimeprazine, and thioridazine, in cyclodextrin (CD)-modified capillary zone electrophoresis were investigated using a phosphate buffer (40 mM) at pH 3.0. We focussed on the separation of phenothiazines with the use of CDs at low concentrations. Three different CDs, including beta-CD, hydroxypropyl-beta-CD (HP-beta-CD) and gamma-CD, were chosen as chiral selectors. The results indicate that effective enantioseparation of phenothiazines, except for methotrimeprazine, is simultaneously achievable with addition of gamma-CD at a concentration of 2.5-6.0 mM. The enantiomers of ethopropazine and trimeprazine are effectively separated with addition of HP-beta-CD at low concentrations, in the range 0.4-6.0 mM, whereas those of promethazine and trimeprazine are baseline resolved with beta-CD at much lower concentrations (0.02-3.0 mM) than with HP-beta-CD. The results also confirm that the separation window is greatly enlarged at low CD concentrations. Moreover, the drastic variations of the electrophoretic mobility of phenothiazines as a function of CD concentration reveal that phenothiazines interact very strongly with CDs in the order gamma-CD<HP-beta-CD<beta-CD.
Cyclodextrins↗
Sensitive determination of phenothiazines in body fluids by gas chromatography with surface ionization detection.
Fourteen phenothiazine derivatives were tested for their detection by gas chromatography (GC) with surface ionization detection (SID). The sensitivity of GC-SID was highest with trimeprazine and levomepromazine, which contain aliphatic tertiary amino side chains, and lowest with thiethylperazine and thioproperazine, which contain sulphur residues. Chlorpromazine, trimeprazine and promazine showed excellent linearity between the SID response and the drug amount in the range 0.25-3.0 pmol on-column. Their detection limits were as low as ca. 5-10 pg (15-30 fmol) on-column (250-500 pg per ml of body fluid). A detailed procedure for isolation of phenothiazines from human whole blood and urine using Sep-Pak C18 cartridges, before the GC with SID, is also presented. The recoveries of the drugs (100 pmol), which were added to 1 ml of whole blood or urine, were more than 79%. The baselines remained steady as the column temperature was increased.
Chromatography, Gas↗
Effect of premedication on the induction dose of thiopentone in children.
The effective dose of thiopentone in 90% ( ED90 ) of unpremedicated children is 10.5 mg/kg. This is significantly greater (p less than 0.01) than in premedicated children. The ED90 in children premedicated with TDP (a mixture of trimeprazine , droperidol and physeptone with atropine) is 4.2 mg/kg which is significantly less (p less than 0.05) than with trimeprazine and atropine ( ED90 5.2 mg/kg) or papaveretum and hyoscine ( ED90 5.0 mg/kg).
Anesthesia, Intravenous↗
Induction dose of propofol in children.
In a study of 144 children aged 1-12 years, attempts were made to assess the ED50 and ED90 of the intravenous induction agent, propofol. The doses required for loss of eyelash reflex and tolerance of facemask, in 50% of unpremedicated children, were 1.6 mg/kg and 2.5 mg/kg respectively. In children premedicated with oral trimeprazine the corresponding values of ED50 were 1.1 mg/kg and 2.0 mg/kg. Doses of 2.8 mg/kg in unpremedicated and 2.0 mg/kg for those who received trimeprazine were required for loss of eyelash reflex in 90% of children. This probably corresponds to an effective induction dose. Pain and movement on induction were common; the incidence was 27% and 21.5% respectively.
Anesthesia, Intravenous↗
Enantioseparation of phenothiazines in cyclodextrin-modified capillary zone electrophoresis using sulfated cyclodextrins as chiral selectors.
In this study, enantioseparations of five phenothiazines, including promethazine, ethopropazine, trimeprazine, methotrimeprazine, and thioridazine, in CD-modified CZE using dual CD systems consisting of randomly sulfate-substituted CD (MI-S-beta-CD) and a neutral CD as chiral selectors in a citrate buffer (100 mM) at pH 3.0 were investigated. The results indicate that MI-S-beta-CD is an excellent chiral selector for enantioseparation of ethopropazine. The enantiomers of promethazine can also be baseline-resolved with MI-S-beta-CD at concentrations in the range of 0.5-1.0% w/v. On the other hand, thioridazine and trimeprazine interact strongly with neutral CDs. As a result, the enantioselectivity of these two phenothiazines is remarkably and synergistically enhanced with increasing the concentration of neutral CDs in the presence of MI-S-beta-CD and simultaneous enantioseparations of these phenothiazines, except for methotrimeprazine, could favorably be achieved with the use of dual CD systems. Moreover, by varying the concentration of beta-CD or gamma-CD at a fixed concentration of MI-S-beta-CD (0.75% w/v) reversal of the enantiomer migration order of promethazine occurred. This may be attributable to the opposite effects of charged and neutral CDs on the mobility of the enantiomers of promethazine.
Cyclodextrins↗
An animal model for preclinical screening of systemic antipruritic agents.
Reliable antipruritic agents that can be given systemically are not available at present. This may be due to the lack of animal models for screening such compounds. Bombesin, a tetradecapeptide originally isolated from frog skin, induces dose-related excessive scratching when administered intracerebroventricularly (i.c.v.) to rats. With the help of a microcomputer, we monitored the scratching elicited by a standard, submaximal dose of bombesin (0.10 microgram, i.c.v.). This system provides 1) a sensitive and novel way of assessing drug-induced behavioral depression, and 2) a means of quantifying interactions between bombesin and possible antagonists. Thus, bombesin-induced grooming is antagonized by behaviorally nondepressant doses of methdilazine, trimeprazine, and chlorpromazine but not by morphine, haloperidol, diphenhydramine, hydroxyzine, mepyramine, cimetidine, or cyproheptadine. Methdilazine and trimeprazine are used clinically as antipruritic agents. The model therefore offers a means of evaluating new, systemic antipruritic agents, particularly those which may be active in treating histamine-independent pruritus.
Animals↗
Phenothiazine radicals inactivate Trypanosoma cruzi dihydrolipoamide dehydrogenase: enzyme protection by radical scavengers.
Phenothiazine cation radicals (PTZ+*) irreversibly inactivated Trypanosoma cruzi dihydrolipoamide dehydrogenase (LADH). These radicals were obtained by phenothiazine (PTZ) peroxidation with myeloperoxidase (MPO) or horseradish peroxidase (HRP/H2O2) systems. LADH inactivation depended on PTZ structure and incubation time. After 10 min incubation of LADH with the MPO-dependent systems, promazine, trimeprazine and thioridazine were the most effective; after 30 min incubation, chlorpromazine, prochlorperazine and promethazine were similarly effective. HRP-dependent systems were equally or more effective than the corresponding MPO-dependent ones. Chloro, trifluoro, propionyl and nitrile groups at position 2 of the PTZ ring significantly decreased molecular activity, specially with the MPO/H2O2 systems. Comparison of inactivation values for LADH and T. cruzi trypanothione reductase demonstrated a greater sensitivity of LADH to chlorpromazine and perphenazine and a 10-fold lower sensitivity to promazine, thioridazine and trimeprazine. Alkylamino, alkyl-piperidinyl or alkyl-piperazinyl groups at position 10 modulated PTZ activity to a limited degree. Production of PTZ+* radicals was demonstrated by optical and ESR spectroscopy methods. PTZ+* radicals stability depended on their structure as demonstrated by promazine and thioridazine radicals. Thiol compounds such as GSH and N-acetylcysteine, L-tyrosine, L-tryptophan, the corresponding peptides, ascorbate and Trolox, prevented LADH inactivation by the MPO/H2O2/thioridazine system, in close agreement with their action as PTZ+* scavengers. NADH (not NAD+) produced transient protection of LADH against thioridazine and promazine radicals, the protection kinetics being affected by the relatively fast rate of NADH oxidation by these radicals. The role of the observed effects of PTZ radicals for PTZ cytotoxicity is discussed.
Amino Acids↗
The extent of postmortem drug redistribution in a rat model.
The aim of this study was to investigate the postmortem redistribution of several drugs in a rat model and to examine if any of the pharmacological properties was related to the extent of this phenomenon. One of the following drugs: phenobarbital (phenobarbitone), acetaminophen (paracetamol), carbamazepine, codeine, verapamil, amphetamine, mianserin, trimeprazine (alimemazine) or chloroquine was administered together with nortriptyline orally to rats 90 min prior to sacrifice. Heart blood was sampled immediately before sacrifice and after 2 h postmortem, as it has previously been shown that this is sufficient time for postmortem concentration changes to occur in heart blood. Blood was also sampled from the clamped abdominal inferior vena cava (representing peripheral blood) and tissue samples were taken from lungs, myocardium, liver, kidney, thigh muscle, forebrain, and vitreous humor together with a specimen from the minced carcass. Drugs were analyzed by high performance liquid or gas chromatography. For phenobarbital, acetaminophen and carbamazepine the postmortem to antemortem blood drug concentration ratios were close to 1.0 and tissue concentrations were low. The postmortem to antemortem heart blood drug concentration ratio for chloroquine (6.9 +/- 1.5) was higher than for nortriptyline (3.5 +/- 0.3), and the remaining drugs (codeine, verapamil, amphetamine, mianserin, and trimeprazine) showed ratios of the same magnitude as nortriptyline. The postmortem to antemortem blood drug concentration ratios for both heart blood and blood from the vena cava and also the lung to antemortem blood drug concentration ratio were closely related to the apparent volume of distribution for the drugs studied (p < 0.001). Accordingly, an apparent volume of distribution of more than 3-4 L/kg is a good predictor that a drug is liable to undergo postmortem redistribution with significant increments in blood levels. The postmortem drug concentration in blood from vena cava was closely related to the antemortem blood level, confirming that among the postmortem samples, the peripheral blood sample was the most representative for the antemortem blood concentration.
Animals↗
THE EFFECT OF SOME NEW ANTIHISTAMINES ON THE ANAPHYLACTIC MICROSHOCK OF THE GUINEA-PIG.
The dose/response curves for the protective effects of the new antihistamine compounds trimeprazine, 10-(3-diethylamino-2-methylpropyl)phenothiazine 1,1-dioxide hydrochloride (oxomemazine hydrochloride), cyproheptadine, homochlorcyclizine and methotrimeprazine against the anaphylactic microshock of the guinea-pig were similar to that of promethazine. The first three compounds, however, protected at lower doses than promethazine (5 to 10 mug/kg). The protective effect of cyproheptadine lasted longer than 24 hr.
Anaphylaxis↗
Enantioseparation of phenothiazines in cyclodextrin-modified capillary zone electrophoresis: reversal of migration order.
Enantioseparations of phenothiazines with gamma-cyclodextrin (gamma-CD) as a chiral selector were investigated using citrate and phosphate buffer electrolytes at pH 3.0. Reversal of the enantiomer migration order of promethazine, ethopropazine, and trimeprazine was observed by varying gamma-CD concentration in the range of 5-9 mM, 2.5-4.5 mM and 1.5-2.8 mM, respectively, using 100 mM citrate buffer at pH 3.0. As in the case of beta-CD, the (+)-enantiomers of phenothiazines possess greater binding strength to gamma-CD than the (-)-enantiomers. The evaluation of the binding constants and limiting mobility of the complexes formed between the enantiomers of phenothiazines and gamma-CD reveals that the binding strength of phenothiazines to gamma-CD and the differences in the binding constants and limiting mobility of the complexes are responsible for the enantiomer migration reversal. Both the binding constants and limiting mobility of the complexes between the (+)-enantiomers of phenothiazine and gamma-CD are greater than those of the corresponding (-)-enantiomers in a citrate buffer, while the binding constants of the complexes primarily determined the migration order of the enantiomers in a phosphate buffer. Compared with the results obtained using a phosphate buffer, we may conclude that citrate buffer which involves competitive complexation with chiral selector plays a significant role in the enantiomer migration reversal.
Binding, Competitive↗
Response to treatment with antihistamines in a family with myotonia congenita.
In a family in which myotonia congenita was found in five generations, both great-grandparents of the index case were affected. In subsequent generations mild and severely affected cases were clearly segregated down parallel lines of this family. The grandmother of the index case had noted improvement with an antihistamine. When the index case was prescribed trimeprazine, she showed a striking reduction in severity of symptoms. Antihistamines seem to deserve further evaluation as a safe and effective treatment for myotonia congenita.
Adult↗