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At least 199 records · Page 11Linked to original sources
PubMed2003

Sedative use in the last week of life and the implications for end-of-life decision making.

BACKGROUND: The use of sedation at the end of life has aroused ethical controversy, attracting accusations of hastening death by gradually increasing sedative doses. The doctrine of double effect has been introduced as an ethical defense. This study aimed to determine how sedative doses change at the end of life and how often the doctrine of double effect might be relevant. METHODS: Case note review was performed of 237 consecutive patients who died in a specialist palliative care unit. Sedative dose changes during the last week of life were noted and survival from admission was compared between groups of patients receiving no sedation, sedation for 7 days, or a commencement of sedation in the last 48 hours of life. There was detailed review of notes from patients who received a marked increase in sedative dose to explore the applicability of the doctrine of double effect. RESULTS: Sedation was given to 48% of patients. Of these, 13% received sedatives for 7 days or more, while 56% commenced sedative use only in the last 48 hours of life. The groups receiving no sedation or sedation for less than 48 hours had the shortest survival from admission (mean, 14.3 and 14.2 days), whereas the 7-day sedation group survived for a mean of 36.6 days (P<.001). Sedative use and dose increased toward the end of life, but the detailed case note review disclosed only 2 cases where the doctrine of double effect may have been implicated. CONCLUSION: Sedative dose increases in the last hours of life were not associated with shortened survival overall, suggesting that the doctrine of double effect rarely has to be invoked to excuse sedative prescribing in end-stage care.

Adult↗
PubMedDate not supplied

High performance liquid chromatographic determination of levomepromazine in human breast milk and serum using solid phase extraction.

A high performance liquid chromatographic (HPLC) method has been developed for the determination of levomepromazine in human breast milk and serum. The levomepromazine was extracted by a rapid and simple extraction method using a Sep-Pak C18 cartridge. The extracts were separated by HPLC on a C8 bonded reversed phase column and detected by UV absorbance at 254 nm. There was no interference with endogenous substance in human breast milk and serum. A linear relationship was obtained for the levomepromazine over the concentration range of 10-300 ng/mL. The recoveries of levomepromazine added to human breast milk and serum were 92.5-99.1% and 86.9-103.9%, respectively.

Chromatography, High Pressure Liquid↗
PubMed1982

Gas chromatographic mass spectrometric identification of O-demethylated and mono-hydroxylated metabolites of levomepromazine in blood from psychiatric patients by selected ion recording with high resolution.

An O-demethylated and two mono-hydroxylated metabolites of levomepromazine have previously been identified as conjugates in the urine from psychiatric patients. The three metabolites were identified in hydrolysed and nonhydrolysed plasma and erythrocytes from three patients by selected ion monitoring of the trimethylsilyl derivatives, with a mass spectrometric resolution of 5000. The three metabolites were mainly found as conjugates in the plasma, and smaller amounts were found unconjugated in the plasma and the erythrocytes.

Adult↗
PubMed2003

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↗
PubMed1993

The protective effect of inhaled levomepromazine (Nozinan) on histamine-induced bronchial constriction.

The effect of inhaled levomepromazine (Nozinan, Veractil) on bronchial responsiveness to inhaled histamine was investigated in asthmatics. In a double blind, randomized controlled study, 12 asthmatics (FEV1% pred 52-96%, and PC20 histamine 1.01 mg/ml (geometric mean)) were challenged before and after inhalation of levomepromazine in three different doses. Before and after each inhalation of levomepromazine, PC20, FEV1, the continuous reaction time (CRT) and the subjective sedation score (VAS) were determined. A dose-dependent increase in PC20 was observed after inhalation of levomepromazine. PC20 was increased by up to 4.02 two-fold concentration differences (doubling), i.e. up to a 38-fold increase from the basic values. Inhalation of the two higher doses of levomepromazine had a small sedative effect evaluated from an increase in CRT and the VAS-score and corresponding to the plasma concentrations. We conclude that inhaled levomepromazine has a dose-dependent protective effect on histamine-induced bronchial hyperresponsiveness in asthmatics and that inhalation of levomepromazine was well tolerated. The mechanism by which levomepromazine acts on histamine-induced bronchial hyperresponsiveness is not known but it could be partly explained by the antihistaminic effect. In this respect levomepromazine bears comparison with the most potent second generation antihistamines. The plasma concentrations of levomepromazine measured corresponded to those seen after oral intake of 5-10 mg levomepromazine.

Administration, Inhalation↗
PubMed1987

Anti-apomorphine effects of phenothiazine drug metabolites.

The potencies in producing muscle relaxation, and in antagonizing apomorphine-induced climbing and hypothermia in mice, were examined for chlorpromazine, levomepromazine and their main metabolites, and for fluphenazine and 7-hydroxy fluphenazine. 3-Hydroxy chlorpromazine was more potent than chlorpromazine in antagonizing apomorphine-induced climbing, while levomepromazine and 3-hydroxy levomepromazine were equipotent in this test. The 3-hydroxy metabolites of chlorpromazine and levomepromazine were more potent than the parent compounds in antagonizing hypothermia, and had significantly weaker muscle relaxant effects than the parent compounds. The 7-hydroxy and N-monodesmethyl metabolites were generally less potent that the parent compounds in antagonizing apomorphine-induced effects. N-Monodesmethyl levomepromazine had a pronounced muscle relaxant effect, like levomepromazine itself. The sulphoxide metabolites of chlorpromazine and levomepromazine were inactive in all tests. Their potencies in these tests indicate that among the metabolites 7-hydroxy chlorpromazine, N-monodesmethyl chlorpromazine and 3-hydroxy levomepromazine, which have all been identified in plasma from patients, may contribute to the antipsychotic effects of the drugs, and furthermore that N-monodesmethyl levomepromazine may contribute to the sedative effects of levomepromazine.

Animals↗
PubMed1975

[Plasma levels of imipramine and desmethylimipramine and antidepressant effect during controlled therapy(author's transl)].

24 depressed impatients received a standardized treatment by imipramine, 6 among them receiving also levomepromazine. Plasma concentration of imipramine and DMI were controlled weekly during the study, and standardized assessment of clinical state were made by a psychiatrist who was unware of biochemical findings. Interaction between the antidepressant and neuroleptic metabolism is shown by a significant increase of DMI levels, though the clinical effect of the drug association could not be asserted. The therapeutic effect seems mainly dependant of etiology of depression. Endogeneous depressions improve more than other types. Among endogenous depressions a significant correlation was found between the degree of clinical improvement after three weeks and DMI level, sum of imipramine + DMI level, but not with concentration of imipramine alone.

Adjustment Disorders↗
PubMed1981

Effect of single oral doses of various neuroleptic drugs on salivary secretion rate, pH, and buffer capacity in healthy subjects.

The effects of melperone, thioridazine, levomepromazine, and chlorprotixene on salivary secretion rate, pH, and buffer capacity was studied in eight healthy volunteers given single oral doses of placebo or 10, 25, and 50 mg of the drugs in a single-blind crossover design. Both resting and stimulated saliva samples were collected before and every hour for 6h after administration. All drugs reduced secretion rate and lowered pH and buffer capacity, mostly in a dose-dependent manner. The effects of levomepromazine and chlorprotixene were more pronounced than those of melperone and thioridazine.

Adult↗
PubMed1981

Binding affinity of levomepromazine and two of its major metabolites of central dopamine and alpha-adrenergic receptors in the rat.

N-Monodesmethyl levomepromazine and levomepromazine sulfoxide have previously been found in higher plasma concentrations than the parent drug in patients who received oral doses of levomepromazine. In the present study levomepromazine, N-monodesmethyl levomepromazine and levomepromazine sulfoxide have been assayed for their binding affinity to rat striatal dopamine receptors and to alpha-adrenergic receptors in rat cortex, and compared with the potency of chlorpromazine and some of its metabolites in the same systems. Levomepromazine sulfoxide was relatively inactive in the dopamine receptor binding test but much more active in the alpha-adrenergic receptor binding test, where it had a binding affinity similar to 7-hydroxy chlorpromazine. Levomepromazine and N-monodesmethyl levomepromazine were active in both systems, having a slightly higher potency than chlorpromazine in the alpha-adrenergic binding test, and a somewhat lower potency than chlorpromazine in the dopamine receptor binding test. The results indicate that N-monodesmethyl levomepromazine may significantly contribute to the antipsychotic effects of levomepromazine while the sulfoxide metabolite lacks neuroleptic potency, and that both metabolites may contribute to the autonomic side-effects of the drug.

Adrenergic alpha-Antagonists↗
PubMed1994

Single photon emission computed tomography with 123I-IMP in three cases of the neuroleptic malignant syndrome.

Single photon emission computed tomography (SPECT) perfusion brain scans using 123I-N-isopropyl-p-iodoamphetamine (123I-IMP) were performed in three patients with the neuroleptic malignant syndrome (NMS). In two accumulation was increased in the left basal ganglia and decreased in the right on the early images during the active phase of NMS; this asymmetry was not seen after recovery. In the third patient two examinations were performed during the active phase; on the first, increased accumulation of 123I-IMP in the left basal ganglia was found on the early images, but on the second, increased accumulation of tracer was found in the right basal ganglia on the delayed images. These abnormalities disappeared after improvement of the NMS. These results suggest that a disturbance in the basal ganglia is related to the development of NMS.

Adult↗