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At least 163 records · Page 9Linked to original sources
PubMed1988

Induction characteristics of propofol in children: comparison with thiopentone.

The induction characteristics of propofol were studied and compared with thiopentone in children aged 3-14 years who received either no premedication or pethidine-atropine or trimeprazine. Anaesthesia was maintained with nitrous oxide in oxygen, and isoflurane. The induction doses of propofol and thiopentone were 2.9 mg/kg and 6.5-7.1 mg/kg respectively; premedication had no significant effect on the induction doses of either agent. Spontaneous movement and hypertonus occurred in about 20% of children with both agents. The use of propofol was associated with a high incidence of pain on injection (injections were mostly in veins on the dorsum of the hand), but this was reduced by mixing lignocaine with propofol. Cardiovascular effects were not clinically significant with either agent. Apnoea occurred in 35% of patients given propofol and in 50% of those given thiopentone. Children anaesthetised with propofol awoke significantly earlier after cessation of all anaesthesia. It is concluded that the use of propofol is safe in children and may have advantages where early recovery from anaesthesia is desirable, but offers no advantage over thiopentone for routine induction of anaesthesia.

Adolescent↗
PubMed1982

Value of computerised tomography in children with non-specific mental subnormally.

Seventy-six children had computerized tomography scans as part of an investigation of mental subnormality; most of them are severely retarded and all those over age 5 years attend special schools. Seventy-two per cent of the children had normal scans. Twenty per cent showed cerebral atrophy and in only 8% was there a specific abnormality (agenesis of corpus callosum, arachnoid cyst, communicating hydrocephalus). None of these findings had any positive prognostic implication. Sedation or general anaesthesia was required for all except one child. Injection pethidine compound was used for children under age 5 years or less than 30 kg in weight, and trimeprazine orally was used for older children. The radiation exposure was high--5.6 rad per scan, which is 100 times greater than that from a posteroanterior and lateral chest x-ray film. For these reasons computerised tomography scans cannot be recommended as a routine part of the investigation of children with non-specific mental subnormality.

Adolescent↗
PubMed1991

Preanaesthetic medication: a survey of current usage.

A survey has been carried out amongst the UK based members of the Association of Anaesthetists of Great Britain and Ireland regarding their practice of premedication. Ninety-three per cent of respondents (reply rate 51.7%) used sedative-hypnotic premedication routinely in adults and 84% in children. However, anticholinergic premedication was used by only 36% in adults and 56% in children. Temazepam was the most frequently used sedative premedicant in adults and trimeprazine in children. Atropine and hyoscine were the most frequently used anticholinergic drugs. The main reasons for using sedative-hypnotic premedication were allaying anxiety and providing sedation. The main reasons for using anticholinergic drugs were drying of secretions and protection against vagal overactivity. This survey concludes that while sedative-hypnotic premedication continues to be used in the majority of patients with oral benzodiazepines the most frequently used drugs, the use of anti-cholinergic premedication continues to decline.

Ambulatory Surgical Procedures↗
PubMed1991

Hypertensive crisis from chronic intoxication with nasal decongestant and cough medications.

Cardiac hypertensive structural changes, catecholamine-related cardiomyopathy, and congestive heart failure (CHF) have been encountered in pheochromocytoma, as a result of prolonged exposure to high concentrations of endogenous catecholamines. A 34-year-old man presented with severe hypertension, cardiomegaly, and CHF, presumably as a result of continuous alpha-adrenergic intoxication with oxymetazoline hydrochloride, phenylephrine hydrochloride, and ephedrine hydrochloride, consumed in massive doses by an overuse of nasal decongestants and cough syrup (daily doses of 20, 100, and 300 mg, respectively). Coadministered chlorpromazine hydrochloride and trimeprazine tartrate may have also contributed to the clinical presentation through their anticholinergic and antihistaminic properties. The possibility of an overuse of these over-the-counter drugs should be considered in the differential diagnosis of hypertensive emergencies, especially with the simultaneous use of anticholinergic and antihistamine medications, beta-blocking agents, or monoamine oxidase inhibitors.

Adult↗
PubMed2002

Insomnia in children: when are hypnotics indicated?

Insomnia in children is a nonspecific impairing symptom that may be the result of normal developmental changes, psychosocial duress, a sleep disorder, a psychiatric disorder, other medical disorders, substance misuse, or an adverse effect of medication. Careful clinical assessment of insomnia in children may include the use of symptom rating scales, laboratory testing, or other medical assessment. Short- and long-term treatment of insomnia in children involves management of etiological factors and associated syndromes. Controlled treatment studies of pediatric insomnia are limited to <10 published studies of psychosocial and/or psychopharmacological treatment in young children. Directive parent education and behavior modification techniques have been effective in short-term treatment of insomnia in young children, and may be the preferred treatment of extrinsic insomnia, as well as an important adjunctive treatment of any insomnia symptoms. Two benzodiazepines [flurazepam and delorazepam (chlordesmethyldiazepam)], one antihistamine (niaprazine) and one phenothiazine [alimemazine (trimeprazine)] have been shown to be effective in the short-term treatment of insomnia in young children, although none of these agents have US Food and Drug Administration approval for pediatric insomnia. Short-acting benzodiazepines may have a role in the brief treatment of pediatric insomnia associated with an anxiety or mood disorder, psychosis, aggression, medication- induced activation, or anticipatory anxiety associated with a medical procedure. However, tachyphylaxis and risk of misuse preclude the long-term use of benzodiazepines for the treatment of insomnia in children. Newer hypnotics, which appear better tolerated than the benzodiazepines in studies of adults, may have a role when combined with psychosocial treatments of pediatric insomnia. Treatment of intrinsic pediatric insomnia may additionally involve chronotherapy or medical management.

Adolescent↗
PubMed2006

Trypanosoma cruzi dihydrolipoamide dehydrogenase as target for phenothiazine cationic radicals. Effect of antioxidants.

Myeloperoxidase (MPO), myoglobin (Mb) and horseradish peroxidase (HRP), catalyzed the generation of radical-cations by one-electron oxidation of phenothiazines (PTZ). The transient formation of these radicals (PTZ+.) was confirmed by ESR and optical spectroscopy. These species are reactive towards Trypanosoma cruzi LADH (T. cruzi LADH), T. cruzi trypanothione reductase (T. cruzi TR) and possibly other macromolecule targets. Both T. cruzi enzymes were irreversibly inactivated. T. cruzi LADH inactivation depended on: a) PTZ structure, peroxidase nature and the rate production of PTZ+. radical cations; b) incubation time; c) the presence of an antioxidant that intercepts free radicals. The production of PTZ+. radical cations, which is essential for T. cruzi LADH inactivation, is correlated with the electron donor ability of the substrates, as qualified by the Hammett sigmapara constant for the subtituent in the 2-position of the PTZ. Promazine (PZ), trimeprazine (TMPZ) and thioridazine (TRDZ) were the most effective inactivating agents, whereas trifluophenothiazines with CF3 group at 2-position (Trifluoperazine (TFP), fluphenazine (FFZ) and trifluopromazine (TFPZ)), and propericyazine (PCYZ) with CN group at 2-position, were much less active or inactive, all in close agreement with their higher or lowest electron donor ability, respectively. Comparison of inactivation values for T. cruzi LADH and mammalian heart LADH demonstrated a greater sensitivity of T. cruzi LADH to various PTZ studied. Thiol compounds, tyrosine, dopa, tryptophan, NADH, ascorbate and trolox prevented T. cruzi LADH inactivation by the peroxidase/H2O2 systems in agreement with their ability to suppress PTZ+. radical cations. The role of these radicals as enzyme inhibitors, or as generators of secondary free radicals and metabolite depletors may contribute to explain the trypanocidal effect as well as other chemotherapeutic actions of PTZ.

Amino Acid Sequence↗
PubMedDate not supplied

Tuning of the selectivity in capillary electrophoresis by cyclodextrins illustrated by the separation of some structurally related phenothiazines.

Cyclodextrins were used to affect the selectivity of the capillary electrophoresis system in the separation of 10 widely used phenothiazines. It was shown that the addition of cyclodextrins substantially improved the selectivity. The effect of temperature and cyclodextrin concentration was studied on the resolution between the screened phenothiazines. The best results were obtained with 8 mM hydroxypropyl-beta-cyclodextrin at 15.5 degrees C. Under these conditions, a resolution of at least 1.5 between all phenothiazines could be obtained. In addition, the chiral separation of the enantiomers of trimeprazine could be accomplished. Structure separability relations between the phenothiazines showed that a change in the side chain at the R10 position had the greatest effect on the migration.

Cyclodextrins↗
PubMed1999

N-demethylation of phenothiazines by lipoxygenase from soybean and human term placenta in the presence of hydrogen peroxide.

Several phenothiazine derivatives have been shown to cause reproductive toxicity. The biochemical mechanisms responsible for these effects are not fully understood at present. In this study, we investigated hydrogen peroxide-dependent oxidation of six phenothiazines by purified lipoxygenase from soybean (SLO) and human term placenta (HTPLO). Chlorpromazine was employed as the prototype phenothiazine drug. Chlorpromazine was easily demethylated releasing formaldehyde when incubated at pH 7.0 and 6.5 with SLO or HTPLO, respectively, in the presence of hydrogen peroxide. The reaction was linear with respect to time, exhibited dependence on the amount of enzyme, and the concentration of chlorpromazine and hydrogen peroxide. Under the optimal assay conditions, the estimated Vmax values for chlorpromazine N-demethylation were 139 and 7.2 nmoles/min/mg of SLO and HTPLO, respectively. Collectively, the results suggest an enzymatic nature of the reaction. In the presence of gossypol and NDGA, the classical inhibitors of different lipoxygenases, the formaldehyde production was significantly decreased, as expected. Similar to SLO, the generation of chlorpromazine cation radical, an initial oxidation product with an absorption maximum at 525 nm, was also observed with HTPLO. The radical generation was detectable only under acidic conditions (pH 3.5-4.5). The formaldehyde production was also decreased by BHT and BHA, suggesting a radical nature of the SLO-mediated chlorpromazine N-demethylation. Reduced glutathione, ascorbate, and dithiothreitol suppressed the rate of SLO-dependent formaldehyde generation, presumably due to the reduction of the cation radical back to chlorpromazine in a concentration-dependent manner. Besides chlorpromazine, SLO also oxidized promazine, triflupromazine, trifluperazine, trimeprazine, and perphenazine, albeit at different rates, in the presence of hydrogen peroxide. The evidence gathered in this in vitro study suggests that phenothiazines can undergo peroxidative N-demethylation via lipoxygenase pathway. The role of this biochemical mechanism in the in vivo developmental toxicity of phenothiazines remains to be established.

Chlorpromazine↗
PubMed1999

Postoperative vomiting (POV) in the paediatric outpatient general surgical population.

AIM: To determine the incidence of postoperative vomiting (POV) in the paediatric outpatient general surgical population, the factors affecting POV and the incidence of unplanned admissions contributed by POV. METHOD: One hundred and ninety-nine children below 13 yeas of age undergoing elective outpatient general surgical procedures were enrolled into this prospective study. Anaesthesia was induced either intravenously or via the inhalational route. It was then maintained with nitrous oxide, oxygen and isoflurane or halothane. The age, sex, body weight, duration of fasting, administration of trimeprazine, type of general surgical procedure, maintenance technique for general anaesthesia, duration of general anaesthesia, the administration of opiods or local anaesthetics and the incidence of POV were noted. The results were analysed initially with chi-squared test and subsequently subjected to multivariate logistic regression analysis and stepwise variable selection method. RESULTS: The incidence of POV was 8.5%. Duration of general anaesthesia greater than one hour was associated with a significantly higher incidence of POV. Postoperative emesis did not contribute to unplanned admissions in these day surgical patients.

Adolescent↗
PubMedDate not supplied

[Inactivation of Trypanosoma cruzi trypanothione reductase by phenothiazine cationic free radicals].

Peroxidase/H2O2/phenothiazine systems produced irreversible inhibition (inactivation) of Trypanosoma cruzi trypanothione reductase (TR). The enzyme inactivation depended on (a) the incubation time of TR with the peroxidase/H2O2/phenothiazine system; (b) the peroxidase nature and (c) the phenothiazine structure. With the more effective peroxidase/H2O2/phenothiazine systems, TR inactivation kinetics presented a relatively fast initial phase, lasting for about 10 min, in which most of the enzyme activity disappeared. This phase was followed by a slower one and, after 30 min incubation, TR was totally inactivated. Three peroxidases were assayed as catalysts of TR inactivation: the horseradish peroxidase (HRP), leukocyte myeloperoxidase (MPO) and modified myoglobin (Mb). Under comparable experimental conditions, the peroxidase system activity decreased in the given order. With HRP systems, 10 microM Thioridazine (TRDZ), Promazine (PZ), Trimeprazine (TMPZ), Prochlorperazine (PCZ), Propionylpromazine (PPZ), Chlorpromazine (CPZ) and Perphenazine (PFZ), produced 95-100% inactivation of TR. With the MPO/H2O2 systems, PZ. TRDZ and TMPZ were the most effective. Under similar experimental condition, the Mb/H2O2/PZ,/TMPZ, /TRDZ and CPZ systems effectively inactivated TR. The presence of alkylamino, piperazinyl, or piperidinyl groups in PTZ N atom (position 10) and -Cl, -CF3, -SCH3, COCH2CH3 and -CN in position C2 exerted significant influence on phenothiazine activity. Glutathione (GSH) prevented TR inactivation by the HRP/H2O2/PZ and MPO/H2O2/PZ systems. The HRP/H2O2 and MPO/H2O2/phenothiazines systems generated the corresponding cationic radicals (FTZ.+) the stability of which was limited by their conversion into phenothiazine-sulfoxides (PTZ-SO). The latter ones were inactive on TR. GSH rapidly reacted with PTZ+.; thus producing cation radical detoxication. These reactions fit in well with GSH protection of TR against the peroxidase/H2O2/phenothiazine system, as well as with the FTZ.+ role in phenothiazine cytotoxicity.

Animals↗
PubMedDate not supplied

Myeloperoxidase-generated phenothiazine cation radicals inactivate Trypanosoma cruzi dihydrolipoamide dehydrogenase.

Peroxidase/H2O2/phenothiazine systems irreversibly inhibit Trypanosoma cruzi dihydrolipoamide dehydrogenase (LADH). Inactivation of the parasite enzyme depended on (a) phenothiazine structure; (b) peroxidase nature; (c) incubation time and (d) the presence of a cation radical scavenger. With the myeloperoxidase/H2O2/system, promazine, trimeprazine, thioridazine, promethiazine, prochlorperazine, chlorpromazine and perphenazine were the most effective derivatives out of twelve phenothiazines studied. An electronegative substituent at position 2 of the phenothiazine ring such as Cl, or trifluoromethyl, propionyl and nitrile groups decreased or nullified phenothiazine activity. Myeloperoxidase/H2O2/, horseradish peroxidase/H2O2/, and myoglobin/H2O2/systems activated phenothiazines producing the corresponding cation radicals, myeloperoxidase being the most selective one with respect to phenothiazine structure. The myoglobin/H2O2/system activated phenothiazines that were scarcely active or inactivate with the MPO/H2O2/system, such as the trifluoromethyl derivatives. Production of phenothiazine cation radicals was demonstrated by optical spectroscopy. Phenothiazine cation radical stability depended on their structure as illustrated by promazine and thioridazine. Thiol compounds (GSH, N-acetyl-cysteine and penicillamine), aromatic aminoacids (L-tyrosine, L-tryptophan, and the corresponding peptides) and ascorbate scavenged phenothiazine cation radicals, thus preventing LADH inactivation. Comparison of the summarized phenothiazine effects with those of phenothiazines on T. cruzi suggest the role of cation radicals in phenothiazines chemotherapeutic actions.

Amino Acids, Aromatic↗
PubMedDate not supplied

The potentiation of narcotic analgesics with phenothiazines.

Potentiation of narcotic analgesics with phenothiazines have been used for preoperative and postoperative analgesia for a number of years by the podiatric community. The agents most frequently cited in studies are the combination of meperidine with either the phenothiazines chlorpromazine, trimeprazine, or promethazine. Due to the fact that the double-blind clinical studies of pain are mainly subjective, and difficult to quantify, the usefulness of phenothiazines for the sole purpose of potentiation of analgesia is questionable, especially in view of the many side effects of this group of drugs.

Analgesics, Opioid↗
PubMedDate not supplied

Preliminary studies on phenothiazine-mediated reversal of multidrug resistance in mouse lymphoma and COLO 320 cells.

The ability of phenothiazine derivatives to inhibit the transport activity of P-glycoprotein in resistant mouse lymphoma and MDR/COLO 320 cells was studied. A rhodamine 123 efflux from the above-mentioned neoplastic cells in the presence of tested compounds was examined by flow cytometry. Two of the phenothiazine derivatives, namely perphenazine and prochlorperazine dimaleate, proved to be effective inhibitors of the rhodamine efflux. Other tested phenothiazine derivatives (promethazine hydrochloride, oxomemazine, methotrimeprazine maleate, trifluoropromazine hydrochloride, trimeprazine) also modulated the intracellular drug accumulation in both resistant cell lines, however, they exerted additional cytotoxic effects. The differences observed between the effects of the test compounds on intracellular drug accumulation could be the outcome of differences in phenothiazine's chemical structure, which is crucial for drug-cell membrane interactions. The results of this study provide information about a new group of compounds that offer promise in multidrug resistance reversal in tumor cells.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1987

Prevention of post-tonsillectomy pain with analgesic doses of ketamine.

The prevention of postoperative pain in children who had undergone tonsillectomy was investigated in a double-blind trial. Ketamine (Ketalar; Parke-Davis) 0.5 mg/kg was given intravenously before the operation to 20 children and saline to a control group of 20 children. Premedication consisted of oral trimeprazine 4 mg/kg given 2 hours pre-operatively. The anaesthetic technique was standardised. There were no significant differences between the groups pre-or intra-operatively. Postoperatively there were significant differences in the measurement of pain but not in that of sedation. No hallucinations were encountered in those receiving ketamine. It is concluded that analgesic doses of ketamine are safe and effective.

Child↗
PubMed1979

Elimination of F'lac plasmid by different psychotropic drugs and some related compounds.

Desipramine, trimipramine, protriptyline, noxiptyline, promazine, trimeprazine, triflupromazine and chlorprothixene methoiodide eliminated the F'lac plasmid of Escherichia coli, while thiazinanum, toluidine blue, lidocaine and procaine were ineffective in this respect. The plasmid eliminating action of the drug ceased in the presence of 0.05 M magnesium sulphate. Methylene blue did not inhibit plasmid elimination by the psychotropic drugs, and in presence of the dye even lidocaine and procaine became effective. Based on plasmid elimination in the presence of methylene blue and on the selective effects of the lon- mutant, the plasmid eliminating mechanism of psychotropic drugs seems to differ from that of acridine orange.

Animals↗
PubMed1997

Oxidation of phenothiazines by human term placental peroxidase in non-smokers.

Several phenothiazine derivatives have been shown to cause reproductive toxicity. The biochemical mechanisms responsible for these effects are not fully understood at present. In this study, we investigated hydrogen peroxide-dependent oxidation of seven phenothiazines by purified human term placental peroxidase. Promazine was employed as the prototype phenothiazine drug. Promazine was easily oxidized to a cation radical (absorption maximum at 513 nm) when incubated under acidic conditions with human term placental peroxidase in the presence of hydrogen peroxide. The rate of the radical formation was 350 +/- 30 nmol/min/mg protein when 30 micrograms of the purified peroxidase was incubated with 10 mM promazine and 1.0 mM hydrogen peroxide in acetate buffer pH 3.5. The reaction was linear with respect to time, exhibited dependence on the amount of enzyme, and the concentration of promazine and hydrogen peroxide. Collectively, the results suggest an enzymatic nature of the reaction. Reduced glutathione, ascorbate, and NADH suppressed the rate of promazine radical formation presumably by its reduction back to promazine in a concentration-dependent manner. Concomitantly, NADH was co-oxidized. The cation radical formation and NADH oxidation declined significantly by potassium cyanide and sodium azide, the known peroxidase inhibitors. The enzyme also oxidized chlorpromazine, triflupromazine, trifluoperazine, trimeprazine, fluphenazine, and perphenazine in the presence of hydrogen peroxide. The evidence gathered in this study suggests that peroxidative bioactivation of phenothiazines to their corresponding cation radical species by the human placental peroxidase may represent one of the biochemical mechanisms responsible for the reported developmental toxicity of these chemicals.

Antipsychotic Agents↗
PubMed1997

Clinician's Photo Guide To Recognizing and Treating Skin Diseases in Women: Part 2. Pregnancy-Related Dermatoses.

This report identifies 4 pregnancy-induced dermatoses: (1) pemphigoid gestationis, (2) polymorphic eruption of pregnancy, (3) prurigo of pregnancy, and (4) pruritic folliculitis of pregnancy. According to 1 study of 3192 pregnancies, 0.06% of the women had pemphigoid gestationis (PG), 0.5% had polymorphic eruption of pregnancy (PEP), 0.2% had prurigo of pregnancy (PP), and 0.03% had pruritic folliculitis of pregnancy (PFP). Some reports have suggested an increased risk of fetal morbidity and mortality, as well as an increased risk of premature births, among women with PG. The incidence of fetal morbidity and mortality for the other dermatoses of pregnancy appears to be similar to that in normal pregnancies. Among the drugs used in dermatology, isotretinoin and antineoplastic agents, such as methotrexate, are 2 types that present high risk during pregnancy. Antipruritic medications, such as trimeprazine and doxepin, and some nonsteroidal anti-inflammatory agents, such as indomethacin, also should be avoided during pregnancy and lactation. Analgesics, including acetaminophen, are associated with minimal risk to the fetus or infant. Use of topical corticosteroids is associated with a low risk during pregnancy. Fortunately, many dermatologic disorders allow deferral of treatment or alternate therapeutic methods during pregnancy.

Journal Article↗