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1.
Psychiatr Danub ; 34(2): 245-252, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35772134

RESUMO

BACKGROUND: To assess potential benefits of quetiapine for persistent sleep disturbances in patients with posttraumatic stress disorder (PTSD) on stable combined SSRI and benzodiazepine therapy, who previously failed to respond to various benzodiazepine and non-benzodiazepine hypnotic adjuvant treatment as well as to first-generation antipsychotic add-on treatment. SUBJECTS AND METHODS: Fifty-two male PTSD outpatients on stable combination treatment with SSRI and benzodiazepines, with persistent sleep disturbances not responding to prescription of zolpidem, flurazepam, nitrazepam, promazine, and levopromazine, were assessed for sleep disturbances improvements after prescription of quetiapine in the evening. Each patient met both ICD-10 and DSM-IV criteria for PTSD. Psychiatric comorbidity and premorbidity were excluded using the Mini-International Neuropsychiatric Interview (MINI). Improvement on the CAPS recurrent distressing dream item, reduction in the amount of time needed to fall asleep, prolongation of sleep duration, and reduction in average number of arousals per night in the last 7 days before the assessment period were used as efficacy measures. RESULTS: All sleep-related parameters improved significantly at the end of a five-week follow-up: sleep duration increased by one hour (p<0.001), sleep latency decreased by 52.5 minutes (p<0.001), median number of arousals per night decreased from two to one (p<0.001), CAPS recurrent distressing dream item median decreased from five to four (p<0.001), and the number of patients dissatisfied with their sleep quality and quantity decreased from 45 to two (p<0.001). CONCLUSION: Quetiapine prescribed in the evening may be successful therapy for persistent sleep disturbances in patients with PTSD and generally good response to an SSRI and benzodiazepine combination, who previously failed to respond to some of the usual hypnotic medication or addition of first-generation antipsychotics: zolpidem, flurazepam, nitrazepam, promazine, and levopromazine.


Assuntos
Antipsicóticos , Transtornos do Sono-Vigília , Transtornos de Estresse Pós-Traumáticos , Antipsicóticos/farmacologia , Antipsicóticos/uso terapêutico , Benzodiazepinas/uso terapêutico , Flurazepam/farmacologia , Flurazepam/uso terapêutico , Humanos , Hipnóticos e Sedativos/uso terapêutico , Masculino , Metotrimeprazina/farmacologia , Metotrimeprazina/uso terapêutico , Nitrazepam/farmacologia , Nitrazepam/uso terapêutico , Promazina/farmacologia , Promazina/uso terapêutico , Fumarato de Quetiapina/farmacologia , Fumarato de Quetiapina/uso terapêutico , Sono/fisiologia , Transtornos do Sono-Vigília/tratamento farmacológico , Transtornos do Sono-Vigília/etiologia , Transtornos de Estresse Pós-Traumáticos/complicações , Transtornos de Estresse Pós-Traumáticos/tratamento farmacológico , Transtornos de Estresse Pós-Traumáticos/psicologia , Zolpidem/farmacologia , Zolpidem/uso terapêutico
2.
Rev. psiquiatr. Urug ; 85(1): 28-42, oct. 2021. graf, tab
Artigo em Espanhol | LILACS, BNUY, UY-BNMED | ID: biblio-1343130

RESUMO

El tratamiento farmacológico de demostrada eficacia en la esquizofrenia es el antipsicótico. Sin embargo, en muchas ocasiones se requiere medicación concomitante que depende de comorbilidades y efectos adversos. Se realizó un estudio cuantitativo, longitudinal, retrospectivo, considerando el año 2006 y 2016, en una población de usuarios con esquizofrenia de la Policlínica del Hospital Vilardebó, analizando los tratamientos con psicofármacos. Se diferenciaron los tratamientos según monoterapia antipsicótica y polifarmacia con 2 antipsicóticos, y polifarmacia con más de 2 antipsicóticos, antidepresivos, estabilizantes del humor, benzodiacepinas y anticolinérgicos. La población inicial en 2006 fue de 621 pacientes y 398 pacientes continuaban en tratamiento en 2016. Mantuvieron el trata-miento con antipsicóticos 377 pacientes; 184 mantuvieron benzodiacepinas; 59 se mantuvieron con anticolinérgicos; 49, con estabilizantes del humor y 47, con antidepresivos. La monoterapia antipsicótica se presentó en torno al 50 % de la población estudiada. Se deberían revisar aquellas prácticas que se infieren a partir de este estudio, como el uso prolongado de anticolinérgicos, benzodiacepinas, y polifarmacia con más de 2 antipsicóticos, que está extendida en los usuarios con esquizofrenia. El tratamiento con clozapina fue el más estable y no parece aumentar la mortalidad en estos pacientes


Antipsychotics are the proved effective therapy for schizophrenia. However, on many occasions, associated drugs are required depending on comorbidities and side effects. A retrospective longitudinal quantitative study of drug prescription for 2006 and 2016 in patients with schizophrenia diagnosis was carried out in an outpatient clinic at Hospital Vilardebó. Treatments were classified as antipsychotic monotherapy, two antipsychotic drugs polypharmacy and polypharmacy with two antipsychotic drugs, antidepressants, mood stabilizers, benzodiazepines and anticholinergic drugs. Initial population in 2006 included 621 patients, 398 were still being treated in 2016. Antipsychotic drugs were still being received in 377 patients, benzodiazepines in 184, anticholinergic drugs in 59, mood stabilizers in 49, and anti-depressants in 47. Antipsychotic monotherapy was 50% of the population. Those practices that can be inferred from this study, with lengthy use of anticholinergic drugs, benzodiazepines, and the use of more than 2 antipsychotic drugs in patients with schizophrenia diagnosis should be revised. Clozapine therapy was the most stable and does not seem to increase mortality.


Assuntos
Humanos , Masculino , Feminino , Adulto , Pessoa de Meia-Idade , Idoso , Esquizofrenia/tratamento farmacológico , Antipsicóticos/uso terapêutico , Tratamento Farmacológico/estatística & dados numéricos , Fenotiazinas/uso terapêutico , Clorpromazina/uso terapêutico , Epidemiologia Descritiva , Estudos Retrospectivos , Estudos de Coortes , Clozapina/uso terapêutico , Risperidona/uso terapêutico , Polimedicação , Distribuição por Idade e Sexo , Cloridrato de Tiaprida/uso terapêutico , Fumarato de Quetiapina/uso terapêutico , Aripiprazol/uso terapêutico , Olanzapina/uso terapêutico , Haloperidol/uso terapêutico , Metotrimeprazina/uso terapêutico
3.
Biol Pharm Bull ; 44(8): 1140-1150, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34334499

RESUMO

The clinical applications of antipsychotics for symptoms unrelated to schizophrenia, such as behavioral and psychological symptoms, in patients with Alzheimer's disease, and the likelihood of doctors prescribing antipsychotics for elderly people are increasing. In elderly people, drug-induced and aging-associated urinary disorders are likely to occur. The most significant factor causing drug-induced urinary disorders is a decrease in urinary bladder smooth muscle (UBSM) contraction induced by the anticholinergic action of therapeutics. However, the anticholinergic action-associated inhibitory effects of antipsychotics on UBSM contraction have not been sufficiently assessed. In this study, we examined 26 clinically available antipsychotics to determine the extent to which they inhibit acetylcholine (ACh)-induced contraction in rat UBSM to predict the drugs that should not be used by elderly people to avoid urinary disorders. Of the 26 antipsychotics, six (chlorpromazine, levomepromazine (phenothiazines), zotepine (a thiepine), olanzapine, quetiapine, clozapine (multi-acting receptor targeted antipsychotics (MARTAs))) competitively inhibited ACh-induced contractions at concentrations corresponding to clinically significant doses. Further, 11 antipsychotics (perphenazine, fluphenazine, prochlorperazine (phenothiazines), haloperidol, bromperidol, timiperone, spiperone (butyrophenones), pimozide (a diphenylbutylpiperidine), perospirone, blonanserin (serotonin-dopamine antagonists; SDAs), and asenapine (a MARTA)) significantly suppressed ACh-induced contraction; however, suppression occurred at concentrations substantially exceeding clinically achievable blood levels. The remaining nine antipsychotics (pipamperone (a butyrophenone), sulpiride, sultopride, tiapride, nemonapride (benzamides), risperidone, paliperidone (SDAs), aripiprazole, and brexpiprazole (dopamine partial agonists)) did not inhibit ACh-induced contractions at concentrations up to 10-5 M. These findings suggest that chlorpromazine, levomepromazine, zotepine, olanzapine, quetiapine, and clozapine should be avoided by elderly people with urinary disorders.


Assuntos
Acetilcolina/metabolismo , Antipsicóticos/efeitos adversos , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Bexiga Urinária/efeitos dos fármacos , Acetilcolina/farmacologia , Envelhecimento , Animais , Antipsicóticos/uso terapêutico , Clorpromazina/efeitos adversos , Antagonistas Colinérgicos/efeitos adversos , Clozapina/efeitos adversos , Dibenzotiepinas/efeitos adversos , Masculino , Transtornos Mentais/complicações , Transtornos Mentais/tratamento farmacológico , Metotrimeprazina/efeitos adversos , Olanzapina/efeitos adversos , Fumarato de Quetiapina/efeitos adversos , Ratos Wistar , Doenças Urológicas/complicações
4.
Pharmacol Rep ; 73(1): 303-308, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32888176

RESUMO

BACKGROUND: Cytochrome P450 (CYP) enzymes are involved in the metabolism of many important endogenous substrates (steroids, melatonin), drugs and toxic xenobiotics. Their induction accelerates drug metabolism and elimination. The present study aimed at examining the inducing abilities of two antipsychotic drugs levomepromazine and clozapine for the main CYPs. METHODS: The experiments were performed using cryopreserved human hepatocytes. The hepatotoxicity of levomepromazine and clozapine was assessed after exposure to the neuroleptics (LDH test). CYP activities were measured in the incubation medium using the CYP-specific reactions: caffeine 3-N-demethylation (CYP1A1/2), diclofenac 4'-hydroxylation (CYP2C9), perazine N-demethylation (CYP2C19) and testosterone 6ß-hydroxylation (CYP3A4). In parallel, CYP mRNA levels were measured in neuroleptic-treated hepatocytes. RESULTS: The results indicate that levomepromazine and clozapine induce the expression of main CYP enzyme CYP3A4 in human hepatocytes. Levomepromazine and clozapine at concentrations of 2.5 and 10 µM, respectively, caused a significant increase in the mRNA level and activity of CYP3A4. Both neuroleptics did not produce any changes in CYP1A1/2, CYP2C9 and CYP2C19. CONCLUSION: Levomepromazine and clozapine induce CYP3A4 in human hepatocytes in vitro. Further in vivo studies are advisable to confirm the CYP3A4 induction by levomepromazine and clozapine in the liver, and to assess the effect of these drugs on their own metabolism and on the biotransformation of other co-administered drugs which are the CYP3A4 substrates.


Assuntos
Antipsicóticos/farmacologia , Clozapina/farmacologia , Citocromo P-450 CYP3A/biossíntese , Indução Enzimática/efeitos dos fármacos , Metotrimeprazina/farmacologia , Células Cultivadas , Inibidores das Enzimas do Citocromo P-450 , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Humanos , Fígado , RNA Mensageiro/biossíntese
5.
BMJ Support Palliat Care ; 10(3): 343-349, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32546559

RESUMO

BACKGROUND: Anticipatory prescribing (AP) of injectable medications in advance of clinical need is established practice in community end-of-life care. Changes to prescribing guidelines and practice have been reported during the COVID-19 pandemic. AIMS AND OBJECTIVES: To investigate UK and Ireland clinicians' experiences concerning changes in AP during the COVID-19 pandemic and their recommendations for change. METHODS: Online survey of participants at previous AP national workshops, members of the Association for Palliative Medicine of Great Britain and Ireland and other professional organisations, with snowball sampling. RESULTS: Two hundred and sixty-one replies were received between 9 and 19 April 2020 from clinicians in community, hospice and hospital settings across all areas of the UK and Ireland. Changes to AP local guidance and practice were reported: route of administration (47%), drugs prescribed (38%), total quantities prescribed (35%), doses and ranges (29%). Concerns over shortages of nurses and doctors to administer subcutaneous injections led 37% to consider drug administration by family or social caregivers, often by buccal, sublingual and transdermal routes. Clinical contact and patient assessment were more often remote via telephone or video (63%). Recommendations for regulatory changes to permit drug repurposing and easier community access were made. CONCLUSIONS: The challenges of the COVID-19 pandemic for UK community palliative care has stimulated rapid innovation in AP. The extent to which these are implemented and their clinical efficacy need further examination.


Assuntos
Cuidadores , Vias de Administração de Medicamentos , Cuidados Paliativos/métodos , Padrões de Prática Médica/estatística & dados numéricos , Assistência Terminal/métodos , Administração Bucal , Administração Sublingual , Analgésicos não Narcóticos/administração & dosagem , Analgésicos Opioides/administração & dosagem , Betacoronavirus , COVID-19 , Infecções por Coronavirus/epidemiologia , Fentanila/administração & dosagem , Clínicos Gerais , Cuidados Paliativos na Terminalidade da Vida/métodos , Hospitais para Doentes Terminais , Humanos , Hipnóticos e Sedativos/administração & dosagem , Irlanda/epidemiologia , Lorazepam/administração & dosagem , Metotrimeprazina/administração & dosagem , Antagonistas Muscarínicos/administração & dosagem , Enfermeiras Especialistas , Medicina Paliativa , Pandemias , Médicos , Pneumonia Viral/epidemiologia , Guias de Prática Clínica como Assunto , SARS-CoV-2 , Inquéritos e Questionários , Telemedicina/métodos , Adesivo Transdérmico , Reino Unido/epidemiologia
6.
J Chromatogr A ; 1624: 461232, 2020 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-32540073

RESUMO

The separation of the enantiomers of mepromazine, promethazine, thioridazine and alimemazine was studied by nonaqueous capillary electrophoresis in the presence of cyclodextrins using 1 M acetic acid and 50 mM ammonium acetate in methanol as background electrolyte. Heptakis(2,3-di-O-acetyl-6-O-sulfo)-ß-cyclodextrin, heptakis(2,3-di-O-methyl-6-O-sulfo)-ß-cyclodextrin (HDMS-ß-CD) and octakis(2,3-di-O-methyl-6-O-sulfo)-γ-cyclodextrin were the most effective chiral selectors for mepromazine, promethazine and alimemazine. Subsequently, a method for the determination of dextromepromazine as chiral impurity of levomepromazine was developed employing quality by design principles. Using HDMS-ß-CD as selector, a fractional factorial resolution V+ design was employed for evaluating the knowledge space, while a central composite face centered design provided further method optimization and the basis for the computation of the design space by Monte Carlo simulations. The final experimental conditions included a 30/40.2 cm fused-silica capillary with 75 µm inner diameter and a background electrolyte composed of 0.75 M acetic acid and 55 mM ammonium acetate in methanol containing 27.5 mg/mL HDMS-ß-CD. The applied voltage was 22 kV and the capillary temperature was 15°C. Following method robustness testing via a Plackett-Burman design, the method was validated for dextromepromazine in the range of 0.01 to 3.0 % relative to a concentration of 0.74 mg/mL levomepromazine and applied to the analysis of reference standards of the European Pharmacopoeia and commercial tablets. The assay also allowed the detection of levomepromazine sulfoxide although the quantitation of the compound was hampered by the poor peak shape of the late migrating diastereomer.


Assuntos
Eletroforese Capilar/métodos , Metotrimeprazina/análise , Fenotiazinas/química , Fenotiazinas/isolamento & purificação , Metotrimeprazina/análogos & derivados , Metotrimeprazina/química , Metotrimeprazina/isolamento & purificação , Probabilidade , Padrões de Referência , Reprodutibilidade dos Testes , Estereoisomerismo
7.
Soud Lek ; 65(4): 76-78, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33736437

RESUMO

We present here a fatal case of heatstroke, involving olanzapine and levomepromazine medications. A male in his sixties was found dead in his storage room in the middle of August, with a high rectal temperature. Autopsy revealed congestion of the lungs without any specific findings. Quantitative toxicological analysis demonstrated concentrations of olanzapine, levomepromazine, 7-aminonitrazepam, and 7-aminoflunitrazepam in a femoral blood sample of 0.433 µg/mL, 0.177 µg/mL, 0.604 µg/mL, and 0.041 µg/mL, respectively. The concentration of olanzapine exceeded toxic levels; however, levomepromazine level was within the therapeutic range. Due to the blocking mechanism of both olanzapine and levomepromazine against muscarinic receptors, they might depress sweating and impair heat dissipation. Based on autopsy findings, results of toxicological examination, and investigation by the authorities, we concluded that the cause of death was heatstroke under the influence of olanzapine and levomepromazine.


Assuntos
Golpe de Calor/mortalidade , Metotrimeprazina/sangue , Olanzapina/sangue , Psicotrópicos/sangue , Autopsia , Evolução Fatal , Golpe de Calor/etiologia , Humanos , Masculino , Metotrimeprazina/efeitos adversos , Pessoa de Meia-Idade , Olanzapina/efeitos adversos , Psicotrópicos/efeitos adversos
8.
Aust J Gen Pract ; 48(12): 838-845, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31774984

RESUMO

BACKGROUND: Evidence exists for the use of palliative sedation for people approaching the last days of life with refractory and intolerable symptoms. It is a third-line intervention that deliberately lowers the conscious state to relieve intolerable and refractory symptoms. This level of intervention is not routinely used in primary care, and there is a lack of guidelines for palliative sedation in this context. OBJECTIVE: This article provides some key information about palliative sedation and global issues faced by all individuals involved. A tertiary centre case study is used to illustrate the key points. Given this form of therapy may be required for palliative patients in the community, another aim of this article is to provide an overview for primary care practitioners to raise their awareness of such therapy and the issues related to it. DISCUSSION: While palliative sedation has been regarded as 'controversial' in early palliative care literature, there has been an increased effort to formulate standardised guidelines to define and ethically justify this procedure.


Assuntos
Analgésicos/uso terapêutico , Sedação Consciente/métodos , Dispneia/tratamento farmacológico , Hipnóticos e Sedativos/uso terapêutico , Dor/tratamento farmacológico , Cuidados Paliativos/métodos , Agitação Psicomotora/tratamento farmacológico , Assistência Terminal/métodos , Idoso , Desidratação , Humanos , Hidromorfona/uso terapêutico , Masculino , Metotrimeprazina/uso terapêutico , Midazolam/uso terapêutico , Mieloma Múltiplo , Insuficiência de Múltiplos Órgãos , Fenobarbital/uso terapêutico , Propofol/uso terapêutico , Sepse
9.
BMJ Open ; 9(9): e029942, 2019 09 12.
Artigo em Inglês | MEDLINE | ID: mdl-31515428

RESUMO

OBJECTIVES: Methotrimeprazine is commonly used for the management of nausea but never tested formally against other drugs used in this setting. The aim was to demonstrate superior antiemetic efficacy. DESIGN: Double-blind, randomised, controlled trial of methotrimeprazine versus haloperidol. SETTING: 11 palliative care sites in Australia. PARTICIPANTS: Participants were >18 years, had cancer, an average nausea score of ≥3/10 and able to tolerate oral medications. Ineligible patients had acute nausea related to treatment, nausea for which a specific antiemetic was indicated, were about to undergo a procedure or had received either of the study drugs or a change in glucocorticoid dose within the previous 48 hours. INTERVENTIONS: Based on previous studies, haloperidol was used as the control. Participants were randomised to encapsulated methotrimeprazine 6·25 mg or haloperidol 1·5 mg one time or two times per day and assessed every 24 hours for 72 hours. MAIN OUTCOME MEASURES: A ≥two-point reduction in nausea score at 72 hours from baseline. Secondary outcome measures were as follows: complete response at 72 hours (end nausea score less than 3), response at 24 and 48 hours, vomiting episodes, use of rescue antiemetics, harms and global impression of change. RESULTS: Response to treatment at 72 hours was 75% (44/59) in the haloperidol (H) arm and 63% (36/57) in the methotrimeprazine (M) arm with no difference between groups (intention-to-treat analysis). Complete response rates were 56% (H) and 51% (M). In the per protocol analysis, there was no difference in response rates: (85% (44/52) (H) and 74% (36/49) (M). Complete per protocol response rates were 64% (H) and 59% (M). Toxicity worse than baseline was minimal with a trend towards greater sedation in the methotrimeprazine arm. CONCLUSION: This study did not demonstrate any difference in response rate between methotrimeprazine and haloperidol in the control of nausea. TRIAL REGISTRATION NUMBER: ACTRN 12615000177550.


Assuntos
Glucocorticoides , Haloperidol , Metotrimeprazina , Náusea , Neoplasias/complicações , Cuidados Paliativos/métodos , Antieméticos/administração & dosagem , Antieméticos/efeitos adversos , Relação Dose-Resposta a Droga , Método Duplo-Cego , Esquema de Medicação , Monitoramento de Medicamentos , Quimioterapia Combinada/métodos , Feminino , Glucocorticoides/administração & dosagem , Glucocorticoides/efeitos adversos , Haloperidol/administração & dosagem , Haloperidol/efeitos adversos , Humanos , Masculino , Metotrimeprazina/administração & dosagem , Metotrimeprazina/efeitos adversos , Pessoa de Meia-Idade , Náusea/tratamento farmacológico , Náusea/etiologia , Resultado do Tratamento
10.
J Pharmacol Sci ; 140(2): 197-200, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31178327

RESUMO

Antipsychotics are often the first-line treatment for behavioral and psychological symptoms of dementia. However, the potential anticholinergic effects of antipsychotics could counteract the therapeutic effects of cholinesterase inhibitors used to treat dementia. We investigated the inhibitory effects of 26 antipsychotics on [N-Methyl-3H]scopolamine specific binding in mouse cerebral cortex. At 10-5 M, chlorpromazine, levomepromazine, prochlorperazine, timiperone, zotepine, pimozide, blonanserin, olanzapine, quetiapine, and clozapine inhibited [N-Methyl-3H]scopolamine binding by > 45%. Furthermore, the pKi values of chlorpromazine, levomepromazine, zotepine, olanzapine, and clozapine overlapped with their clinically achievable blood concentrations. Therefore, the anticholinergic properties of these antipsychotics could attenuate the effects of cholinesterase inhibitors.


Assuntos
Antipsicóticos/metabolismo , Antipsicóticos/farmacologia , Córtex Cerebral/metabolismo , Antagonistas Colinérgicos/metabolismo , Inibidores da Colinesterase/metabolismo , Receptores Muscarínicos/metabolismo , Escopolamina/metabolismo , Animais , Clorpromazina/farmacologia , Depressão Química , Interações Medicamentosas , Masculino , Metotrimeprazina/farmacologia , Camundongos Endogâmicos , Proclorperazina/farmacologia , Ligação Proteica
11.
Early Interv Psychiatry ; 13(3): 589-597, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-29498481

RESUMO

AIM: Early clinical response predicts symptomatic remission and recovery in the maintenance treatment phase of first-episode schizophrenia (FES). However, little is known about predictors of symptomatic remission during acute treatment of severely ill patients with FES. Here, we conducted a secondary analysis of our retrospective observational study, which examined response, remission and treatment-resistance rates in seriously ill patients with FES spectrum disorders involuntarily hospitalized and treated with algorithm-based pharmacotherapy. METHODS: We performed a retrospective chart review of 131 involuntarily admitted patients with schizophrenia or schizoaffective disorder. Our algorithm aimed to delay olanzapine treatment, standardize medications and suggest initiation of clozapine after failure of third-line antipsychotic treatment. The duration of each adequate antipsychotic treatment at an optimal dosage was 4 weeks or more. Remission was defined using the symptom-severity component of consensus remission criteria. A logistic regression model was applied to identify significant predictors of remission at discharge. RESULTS: Overall, 74 patients (56%) were in remission at discharge. Non-remitters were hampered from becoming remitters mainly by the presence of negative symptoms. There were no differences in first-line antipsychotics, dosage of antipsychotics at time of response and adherence rates to algorithm-based pharmacotherapy between remitters and non-remitters. Shorter duration of untreated psychosis, favourable early response and less negative symptoms at baseline were identified as independent predictors of remission at discharge. CONCLUSIONS: The importance of early intervention and specific and adequate treatments of negative symptoms is highlighted.


Assuntos
Algoritmos , Antipsicóticos/uso terapêutico , Internação Compulsória de Doente Mental , Transtornos Psicóticos/tratamento farmacológico , Esquizofrenia/tratamento farmacológico , Psicologia do Esquizofrênico , Administração Oral , Adulto , Antipsicóticos/efeitos adversos , Clozapina/efeitos adversos , Clozapina/uso terapêutico , Quimioterapia Combinada , Feminino , Haloperidol/efeitos adversos , Haloperidol/uso terapêutico , Humanos , Injeções Intramusculares , Masculino , Metotrimeprazina/efeitos adversos , Metotrimeprazina/uso terapêutico , Olanzapina/efeitos adversos , Olanzapina/uso terapêutico , Transtornos Psicóticos/diagnóstico , Transtornos Psicóticos/psicologia , Fumarato de Quetiapina/efeitos adversos , Fumarato de Quetiapina/uso terapêutico , Estudos Retrospectivos , Risperidona/efeitos adversos , Risperidona/uso terapêutico , Esquizofrenia/diagnóstico , Falha de Tratamento , Resultado do Tratamento
12.
Palliat Med ; 33(1): 109-113, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30404581

RESUMO

BACKGROUND:: This case report describes a patient with known idiopathic Parkinson's disease, being managed with transdermal rotigotine, whose refractory nausea and vomiting was successfully controlled with subcutaneous levomepromazine. No drug-induced extrapyramidal side effects emerged. CASE PRESENTATION:: A patient was found to have a locally advanced serous carcinoma, causing secondary bowel obstruction. Furthermore, due to compromised oral access, the patient's oral antiparkinsonian medications for motor control were converted to transdermal rotigotine. Unfortunately, the patient's nausea and vomiting was refractory to a number of recommended antiemetic options. CASE MANAGEMENT:: Low dose levomepromazine was administered on a, 'when required' basis, via subcutaneous injection. CASE OUTCOME:: After the first dose of levomepromazine, the patient's nausea and vomiting completely subsided and no extrapyramidal side effects were observed. This was confirmed by daily assessments, revealing no worsening of the motor symptoms associated with idiopathic Parkinson's disease. CONCLUSIONS:: The pharmacology of rotigotine and levomepromazine appear complementary and may allow for the simultaneous use of both drugs, with favourable outcomes. This case report highlights that rotigotine may afford protection against antipsychotic induced extrapyramidal side effects, while preserving antiemetic effects. Such combinations may have a role in the end-of-life management of idiopathic Parkinson's disease.


Assuntos
Antipsicóticos/uso terapêutico , Metotrimeprazina/uso terapêutico , Náusea/tratamento farmacológico , Náusea/etiologia , Doença de Parkinson/complicações , Tetra-Hidronaftalenos/uso terapêutico , Tiofenos/uso terapêutico , Vômito/tratamento farmacológico , Vômito/etiologia , Administração Cutânea , Idoso , Antiparkinsonianos/administração & dosagem , Antiparkinsonianos/uso terapêutico , Antipsicóticos/administração & dosagem , Agonistas de Dopamina/administração & dosagem , Agonistas de Dopamina/uso terapêutico , Feminino , Humanos , Metotrimeprazina/administração & dosagem , Tetra-Hidronaftalenos/administração & dosagem , Tiofenos/administração & dosagem , Adesivo Transdérmico , Resultado do Tratamento
13.
Eur J Mass Spectrom (Chichester) ; 24(6): 420-436, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30400754

RESUMO

The results of research on selected drugs used in palliative care are presented, including fentanyl, tramadol, metoclopramide, hyoscine butylbromide, midazolam, haloperidol, levomepromazine and clonazepam. Interpretation of their ESI mass spectra obtained by the use of a triple quadrupole linear ion trap mass spectrometer is given. As a result, fragmentation pathways described in the literature are complemented and presented with more details. On their basis, transitions for quantitative analysis are selected and chromatographic conditions for the determination of the palliative care drugs are proposed as well. These results enable future studies on palliative care drugs in elderly patients including both their quantitation in body fluids and easier identification of their metabolites.


Assuntos
Preparações Farmacêuticas/química , Espectrometria de Massas por Ionização por Electrospray/métodos , Adjuvantes Anestésicos/química , Analgésicos Opioides/química , Anticonvulsivantes/química , Antieméticos/química , Antipsicóticos/química , Clonazepam/química , Fentanila/química , Haloperidol/química , Humanos , Metotrimeprazina/química , Metoclopramida/química , Midazolam/química , Cuidados Paliativos , Espectrometria de Massas em Tandem/métodos , Tramadol/química
14.
J Pharm Biomed Anal ; 158: 294-299, 2018 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-29906685

RESUMO

A high-performance liquid chromatography method for the determination of dextromepromazine, levomepromazine sulfoxide and 2-methoxyphenothiazine in levomepromazine samples was developed. The separation of the analytes was achieved within 10 min on a stationary phase containing cellulose tris(4-methylbenzoate) as chiral selector. The mobile phase consisted of 0.1% diethylamine in methanol with a flow rate of 1.0 mL/min. The method was validated according to the International Council for Harmonization guideline Q2(R1). The detection limits based on a signal-to-noise ratio of 3 were in the range of 0.002 to 0.005 µg/mL. The method proved to be precise and accurate in the concentration range of 0.025-1.0 % for levomepromazine sulfoxide and 2-methoxyphenothiazine and 0.025% to 3.0% for dextromepromazine relative to a concentration of 0.1 mg/mL of levomepromazine, with the exception of levomepromazine sulfoxide at the 0.1% level. The method was subsequently applied to the analysis of finished pharmaceutical products as well as of reference substances of the European Pharmacopoeia.


Assuntos
Fracionamento Químico/métodos , Antagonistas de Dopamina/análise , Metotrimeprazina/análise , Benzoatos/química , Celulose/análogos & derivados , Celulose/química , Fracionamento Químico/instrumentação , Cromatografia Líquida de Alta Pressão/instrumentação , Cromatografia Líquida de Alta Pressão/métodos , Antagonistas de Dopamina/química , Limite de Detecção , Metotrimeprazina/química , Padrões de Referência , Estereoisomerismo
15.
Cienc. Serv. Salud Nutr ; 9(1): 36-45, abr. 2018.
Artigo em Espanhol | LILACS | ID: biblio-981835

RESUMO

La esquizofrenia es un trastorno mental severo que afecta el área cognitivo, social y afectivo de quienes lo padecen. El subtipo paranoide es el más frecuente, en el que predominan las ideas de persecución. La presentación de este caso clínico permite orientar a los profesionales de la salud en el reconocimiento temprano de la esquizofrenia paranoide y diferenciarlo de otros trastornos mentales. El presente caso trata de una mujer de 59 años de edad diagnosticada con esquizofrenia paranoide en el Centro Psiquiátrico Sagrado Corazón de Jesús de la Ciudad de Ambato, Ecuador por medio de una anamnesis detallada, basada en criterios diagnósticos de esquizofrenia y los ejes del DSM IV. Actualmente en el Ecuador la esquizofrenia, tiene una prevalencia del 38% del total de los egresos en hospitales psiquiátricos, y un 21,7% de las atenciones en consulta externa. A pesar de estas cifras significativas, existen escasos estudios sobre el tema en Ecuador, por lo cual consideramos prudente la presentación de este caso, para despertar el interés en nuestra comunidad de salud y consolidar conocimientos útiles para la vida laboral del médico, enfocados en mejorar las intervenciones médicas basados en diagnósticos certeros que se enmarquen en el Plan Estratégico Nacional de Salud Mental 2015­2017, acorde con el Ministerio de Salud Pública, enfocados en el objetivo 3 del Buen Vivir que busca mejorar el bienestar y la calidad de vida de la población.


Schizophrenia is a severe mental disorder that affects cognition, social and emotional life of the persons. Paranoid schizophrenia is the most common subtype in which dominates the perception of persecution. The purpose of the present case report is to orientate health professionals to recognize paranoid schizophrenia in early stages and to distinguish this kind of pathology from another mental disorders. The present article reports the clinical case of a 59 year old woman with paranoid schizophrenia from the Psychiatric Center "Sacred Heart of Jesus" of the City of Ambato, Ecuador who has been diagnosed with paranoid schizophrenia by a detailed anamnesis, based in diagnostic criteria for paranoid schizophrenia and the DSM­IV classification. Currently schizophrenia has a prevalence of 38% of the total of psychiatric hospitalizations in Ecuador and a prevalence of 21,7% in ambulatory consultation. Despite these significant numbers there are only a few reports about the paranoid schizophrenia in Ecuador, reason why we consider it from mayor importance to present the following case report, with the intention to awake interest in our health community and strengthen knowledge for the daily work of physicians, focused in medical interventions based in adequate diagnostic procedures and framed in the National Strategic Plan of Mental Health 2015­2017 in accordance with the Ministry of Public Health, guarantying criteria 3 of the "Buen vivir" to improve the well­being and quality of life of the population.


Assuntos
Humanos , Feminino , Pessoa de Meia-Idade , Esquizofrenia Paranoide , Saúde Pública , Manual Diagnóstico e Estatístico de Transtornos Mentais , Transtornos Mentais , Diagnóstico , Equador , Anamnese , Metotrimeprazina
16.
Palliat Med ; 32(7): 1189-1197, 2018 07.
Artigo em Inglês | MEDLINE | ID: mdl-29557260

RESUMO

BACKGROUND: Sedatives are frequently used towards the end of life. However, there is scarce information when their use is labelled as 'palliative sedation'. AIM: To assess the use and labelling of 'continuous administration of sedatives within the last 7 days of life', based on objective operational criteria, on a palliative care unit. DESIGN: Retrospective cohort study, using medical records. Explorative statistical analysis (SPSS 23). SETTING/PARTICIPANTS: Patients who died on a palliative care unit from August 2014 to July 2015. Sedatives recorded were benzodiazepines, levomepromazine, haloperidol ⩾5 mg/day and propofol. RESULTS: Of the 192 patients, 149 (78%) patients received continuous sedatives within the last week of life. The prevalence of delirium/agitation was significantly higher in patients with continuous sedatives compared to those without continuous sedatives at admission to the unit (35% vs 16%, p = 0.02) and on the day before death (58% vs 40%, p = 0.04). The term '(palliative) sedation' was used in the records for 22 of 149 (15%) patients with continuous sedatives. These patients had significantly higher total daily midazolam doses 2 days before death (median (range), 15.0 (6.0-185.0) mg vs 11.5 (1.0-70.0) mg, p = 0.04) and on the day of death (median (range), 19.5 (7.5-240.0) mg vs 12.5 (2.0-65.0) mg, p = 0.01). The dose range was large in both groups. CONCLUSION: The prevalence of delirium/agitation was associated with the administration of continuous sedatives. There was no consistent pattern regarding labelling the use of continuous sedatives as '(palliative) sedation'. Multicentre mixed-methods research is needed for a better characterization of sedation practices in palliative care.


Assuntos
Antipsicóticos/uso terapêutico , Benzodiazepinas/uso terapêutico , Sedação Consciente/métodos , Delírio/tratamento farmacológico , Haloperidol/uso terapêutico , Hipnóticos e Sedativos/uso terapêutico , Metotrimeprazina/uso terapêutico , Cuidados Paliativos/métodos , Agitação Psicomotora/tratamento farmacológico , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Delírio/epidemiologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Prevalência , Agitação Psicomotora/epidemiologia , Estudos Retrospectivos , Assistência Terminal/métodos , Adulto Jovem
17.
J Pharm Biomed Anal ; 146: 402-409, 2017 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-28926734

RESUMO

Using a quality by design approach, a capillary electrophoresis method for the simultaneous determination of dextromepromazine and the oxidation product levomepromazine sulfoxide in levomepromazine was developed. The analytical target profile was defined that the method should be able to quantify 0.1% of both impurities with a precision of ≤10%. Hydroxypropyl-γ-cyclodextrin was used as chiral selector. The critical process parameters cyclodextrin concentration, buffer pH and concentration as well as temperature and applied voltage were studied using a fractional factorial resolution V+ design for defining the knowledge space. A central composite face centered design was used as response surface methodology for deriving the design space by Monte Carlo simulations. The selected working point was a 100mM citric acid buffer, pH 2.85, containing 3.6mg/mL hydroxypropyl-γ-cyclodextrin, a temperature of 15°C and a voltage of 25kV. Robustness was estimated using a Plackett-Burman design. The method was subsequently validated in the relative concentration range of 0.1%-1.0% of the impurities for a solution containing 0.25mg/mL levomepromazine. The method was applied to the determination of the purity of the reference substance of the European Pharmacopoeia and of the drug in a commercial injection solution.


Assuntos
Metotrimeprazina/análogos & derivados , Metotrimeprazina/química , Sulfóxidos/química , Bioensaio/métodos , Cromatografia Capilar Eletrocinética Micelar/métodos , Contaminação de Medicamentos , Concentração de Íons de Hidrogênio , Método de Monte Carlo , Reprodutibilidade dos Testes , gama-Ciclodextrinas/química
18.
Rev. Rol enferm ; 40(2): 111-118, feb. 2017. tab
Artigo em Espanhol | IBECS | ID: ibc-160177

RESUMO

Objetivo. Para el control de los síntomas físicos en situación de últimos días el manejo farmacológico supone la intervención principal. El objetivo de este artículo es revisar las cuestiones relevantes en el manejo enfermero de las situación clínicas y los fármacos comúnmente usados en sedación paliativa en la agonía. Metodología. Se seleccionan las intervenciones sobre manejo enfermero de fármacos en sedación paliativa recomendadas por la literatura científica mediante búsqueda realizada en Scopus, CINAHL, Medline-PubMed y Google Académico con las palabras clave «sedación paliativa», «farmacología», «cuidados de enfermería» y «cuidados paliativos». Resultados. El objetivo de la sedación paliativa (SP) es disminuir el nivel de conciencia como única forma de aliviar un sufrimiento intenso en pacientes en situación terminal, tal como delirium, dolor o disnea refractarias, hemorragia masiva, estado convulsivo, estertores premortem o sufrimiento psicológico refractario. La vía de elección en SP es la vía subcutánea (sc). Son fármacos de 1.ª línea en sedación el midazolam y la levomepromazina. Los opioides deben mantenerse en dosis equianalgésicas, siendo el cloruro mórfico el de uso más extendido. El papel fundamental de enfermería en SP es la monitorización del nivel de sedación según la escala de Ramsay (o similar) y el reconocimiento de los signos indicativos de malestar para la administración de rescate de medicación sedante o analgésica o despistaje de proceso intercurrente tratable (globo vesical, fecaloma, obstrucción de vía, efecto final de dosis, etc.) (AU)


Objetive. To control the physical symptoms in end-of-life pharmacological management involves major intervention. The aim of this article is to review the relevant issues in the management of clinical nursing situation and drugs commonly used in palliative sedation in agony. Methodology. Nursing management in Palliative Sedation recommended by scientific literature search in Scopus, CINAHL, Medline-PubMed and Google Scholar, with key words: «palliative sedation», «pharmacology», «nursing care» and «palliative care» are selected. Results. The goal of palliative sedation (PS) is to reduce the level of consciousness as the only way to relieve intense suffering in terminally ill patients, such as refractory delirium or dyspnea, massive bleeding, convulsive status, crackles premortem or refractory psychological suffering. The route of choice in PS is subcutaneous injection (sc). First line drugs in sedation are midazolam and levomepromazina. Opioids should be kept at equi-analgesic doses, morphine chloride being the most widely used. The fundamental role of nursing in SP is monitoring the level of sedation based on the Ramsay scale (or similar) and recognition of the indicative signs of discomfort for administration rescue sedative or analgesic medication and/or screening treatable intercurrent process (distended bladder, constipation, obstruction way, final dose effect, etc.) (AU)


Assuntos
Humanos , Masculino , Feminino , Cuidados Paliativos , Cuidados Paliativos na Terminalidade da Vida , Cuidados Paliativos na Terminalidade da Vida/métodos , Enfermagem de Cuidados Paliativos na Terminalidade da Vida/métodos , Papel do Profissional de Enfermagem , Sedação Consciente/enfermagem , Midazolam/farmacologia , Midazolam/uso terapêutico , Farmacologia Clínica/métodos , Metotrimeprazina/uso terapêutico
19.
Vertex ; 28(136): 411-415, 2017 Nov.
Artigo em Espanhol | MEDLINE | ID: mdl-29522601

RESUMO

INTRODUCTION: Sedation of patients in pediatric ICU extubated and in weaning of mechanic ventilation is diffcult under regular sedation, because of the tolerance and/or abstinence generated by its sustained use. The objective of this study is to describe the use of Levomepromazine as sedative coadjuvant in these patients. POPULATION AND METHODS: Observational and longitudinal study in intensive care from Juan P. Garrahan Pediatric Hospital. Patients older than 2 years were included, extubated and in weaning of mechanic ventilation with requirements of additional sedation. The level of basal sedation and post-intervention (levomepromazine 0.5 mg/kg every 8 hours) were evaluated with Ramsay and Khalil scales. Doses of regular sedatives were compared before and after the indication. It was considered positive an increase of 1 in the scales, or a decrease of 20% in the regular sedatives doses. RESULTS: 36 patients, medium age of 8,5 years, average doses of levomepromazine 0.38 mg/kg. 97% showed positive result. The regular sedative doses were reduced more than 20% after the intervention. No adverse effects or deceased were registered.


Assuntos
Hipnóticos e Sedativos/uso terapêutico , Metotrimeprazina/uso terapêutico , Adolescente , Criança , Pré-Escolar , Quimioterapia Combinada , Humanos , Unidades de Terapia Intensiva Pediátrica
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