RESUMO
This work describes a novel methodology to analyze four tricyclic antidepressants (amitriptyline, doxepin, imipramine and, nortriptyline) in urine samples by combining supramolecular microextraction and paper spray ionization mass spectrometry (PS-MS). The proposed method uses a supramolecular solvent in which reverse micelles of 1-decanol are dispersed in tetrahydrofuran (THF)/water. The extraction of the tricyclic antidepressants at pH 9.0 requires a sample volume of 10.0 mL, short extraction time (1.0 min of extraction and 5 min of centrifugation), low amounts of organic solvent (50 µL of 1-decanol and 200 µL of THF), and provides high preconcentration factors: 96.9 to amitriptyline, 93.6 to doxepin, 71.3 to imipramine, and 146.9 to nortriptyline. The quantification by PS-MS is fast and straightforward because chromatographic separation is not required and all analytes were determined simultaneously. The limits of detection (LOD), quantification (LOQ), and the precision (RSD, %) of the developed method ranged between 5.2 and 8.6 µg L-1, 17.4-28.7 µg L-1 and 1.3-12.9%, respectively. Urine samples of five individuals (three males and two females) were used for accuracy evaluation. The accuracy obtained in these spiked urine samples at µg L-1 levels varied from 95.3 to 112.0%. The method also provided clean mass spectra with a high signal-to-noise ratio, which demonstrates the analytical appeal combination of supramolecular microextraction with determination by paper spray mass spectrometry.
Assuntos
Antidepressivos Tricíclicos/urina , Microextração em Fase Líquida , Papel , Amitriptilina/urina , Doxepina/urina , Humanos , Imipramina/urina , Substâncias Macromoleculares/química , Espectrometria de Massas , Estrutura Molecular , Nortriptilina/urinaRESUMO
Few studies have described therapeutic options in brachioradial pruritus. We describe a cross-sectional study of brachioradial pruritus patients treated in an outpatient unit. We reviewed medical records and interviewed brachioradial pruritus patients without indication for decompressive surgery, in order to access the perceptions of intensity of pruritus prior to treatment and response to therapy. We found that antidepressants and anticonvulsants were the most frequently prescribed drugs. Best reductions in pruritus were associated with its highest intensities prior to treatment, and with longer periods of therapy.
Assuntos
Aminas/uso terapêutico , Amitriptilina/uso terapêutico , Antidepressivos Tricíclicos/uso terapêutico , Ácidos Cicloexanocarboxílicos/uso terapêutico , Doxepina/uso terapêutico , Prurido/tratamento farmacológico , Ácido gama-Aminobutírico/uso terapêutico , Antidepressivos Tricíclicos/classificação , Antipsicóticos/uso terapêutico , Estudos Transversais , Quimioterapia Combinada , Feminino , Gabapentina , Humanos , Masculino , Pessoa de Meia-IdadeRESUMO
Abstract: Few studies have described therapeutic options in brachioradial pruritus. We describe a cross-sectional study of brachioradial pruritus patients treated in an outpatient unit. We reviewed medical records and interviewed brachioradial pruritus patients without indication for decompressive surgery, in order to access the perceptions of intensity of pruritus prior to treatment and response to therapy. We found that antidepressants and anticonvulsants were the most frequently prescribed drugs. Best reductions in pruritus were associated with its highest intensities prior to treatment, and with longer periods of therapy.
Assuntos
Humanos , Masculino , Feminino , Pessoa de Meia-Idade , Prurido/tratamento farmacológico , Ácidos Cicloexanocarboxílicos/uso terapêutico , Doxepina/uso terapêutico , Aminas/uso terapêutico , Amitriptilina/uso terapêutico , Antidepressivos Tricíclicos/uso terapêutico , Antipsicóticos/uso terapêutico , Estudos Transversais , Quimioterapia Combinada , Antidepressivos Tricíclicos/classificaçãoRESUMO
Trichotillomania is a psychodermatologic disorder characterized by uncontrollable urge to pull one's own hair. Differential diagnoses include the most common forms of alopecia such as alopecia areata. It is usually associated with depression and obsessive-compulsive disorder. Trichotillomania treatment standardization is a gap in the medical literature. Recent studies demonstrated the efficacy of N-acetylcysteine (a glutamate modulator) for the treatment of the disease. We report the clinical case of a 12-year-old female patient who received the initial diagnosis of alopecia areata, but presented with clinical and dermoscopic features of trichotillomania. She was treated with the combination of psychotropic drugs and N-acetylcysteine with good clinical response. Due to the chronic and recurring nature of trichotillomania, more studies need to be conducted for the establishment of a formal treatment algorithm.
Assuntos
Alopecia em Áreas/diagnóstico , Psicotrópicos/uso terapêutico , Tricotilomania/diagnóstico , Acetilcisteína/uso terapêutico , Criança , Diagnóstico Diferencial , Doxepina/uso terapêutico , Feminino , Fluoxetina/uso terapêutico , Humanos , Pimozida/uso terapêutico , Tricotilomania/tratamento farmacológicoRESUMO
ABSTRACT Trichotillomania is a psychodermatologic disorder characterized by uncontrollable urge to pull one's own hair. Differential diagnoses include the most common forms of alopecia such as alopecia areata. It is usually associated with depression and obsessive-compulsive disorder. Trichotillomania treatment standardization is a gap in the medical literature. Recent studies demonstrated the efficacy of N-acetylcysteine (a glutamate modulator) for the treatment of the disease. We report the clinical case of a 12-year-old female patient who received the initial diagnosis of alopecia areata, but presented with clinical and dermoscopic features of trichotillomania. She was treated with the combination of psychotropic drugs and N-acetylcysteine with good clinical response. Due to the chronic and recurring nature of trichotillomania, more studies need to be conducted for the establishment of a formal treatment algorithm.
Assuntos
Humanos , Feminino , Criança , Psicotrópicos/uso terapêutico , Tricotilomania/diagnóstico , Alopecia em Áreas/diagnóstico , Pimozida/uso terapêutico , Acetilcisteína/uso terapêutico , Tricotilomania/tratamento farmacológico , Fluoxetina/uso terapêutico , Diagnóstico Diferencial , Doxepina/uso terapêuticoRESUMO
Abstract Among the wide range of symptoms neglected or resistant to conventional treatments in clinical practice, itch is emerging gradually as a theme to be studied. Itch complaints and the negative effects in the quality of life are observed in several medical fields. Although the partially obscure pathophysiology, some researchers decided to check and test the use of psychotropic drugs in resistant itch to conventional topical treatments and antihistamines. The objective of this study was to evaluate scientific evidence in psychotropic use in the treatment of itch of various causes. This is a systematic review of scientific literature. The following databases were used: PubMed, Web of Science, Scopus and Scielo. Randomized controlled trials that should focus on treatment with psychotropic drugs of pruritus of various causes were the inclusion criteria. All articles were analyzed by the authors, and the consensus was reached in cases of disagreement. Fifteen articles were included after analysis and selection in databases, with the majority of clinical trials focusing on psychopharmacological treatment of itch on account of chronic kidney disease. Clinical trials with psychotropic drugs mostly indicated significant improvement in the itching. In most trials of chronic kidney disease as basal disease for itch, greater effectiveness was observed with the use of psychotropic drugs compared with placebo or other antipruritic. However, the small amount of controlled trials conducted precludes the generalization that psychiatric drugs are effective for itch of various causes.
Assuntos
Humanos , Prurido/tratamento farmacológico , Psicotrópicos/uso terapêutico , Prurido/etiologia , Ensaios Clínicos Controlados Aleatórios como Assunto , Reprodutibilidade dos Testes , Resultado do Tratamento , Ácidos Cicloexanocarboxílicos/uso terapêutico , Doxepina/uso terapêutico , Ácido gama-Aminobutírico/uso terapêutico , Aminas/uso terapêutico , Nefropatias/complicações , Antipruriginosos/uso terapêuticoRESUMO
Among the wide range of symptoms neglected or resistant to conventional treatments in clinical practice, itch is emerging gradually as a theme to be studied. Itch complaints and the negative effects in the quality of life are observed in several medical fields. Although the partially obscure pathophysiology, some researchers decided to check and test the use of psychotropic drugs in resistant itch to conventional topical treatments and antihistamines. The objective of this study was to evaluate scientific evidence in psychotropic use in the treatment of itch of various causes. This is a systematic review of scientific literature. The following databases were used: PubMed, Web of Science, Scopus and Scielo. Randomized controlled trials that should focus on treatment with psychotropic drugs of pruritus of various causes were the inclusion criteria. All articles were analyzed by the authors, and the consensus was reached in cases of disagreement. Fifteen articles were included after analysis and selection in databases, with the majority of clinical trials focusing on psychopharmacological treatment of itch on account of chronic kidney disease. Clinical trials with psychotropic drugs mostly indicated significant improvement in the itching. In most trials of chronic kidney disease as basal disease for itch, greater effectiveness was observed with the use of psychotropic drugs compared with placebo or other antipruritic. However, the small amount of controlled trials conducted precludes the generalization that psychiatric drugs are effective for itch of various causes.
Assuntos
Prurido/tratamento farmacológico , Psicotrópicos/uso terapêutico , Aminas/uso terapêutico , Antipruriginosos/uso terapêutico , Ácidos Cicloexanocarboxílicos/uso terapêutico , Doxepina/uso terapêutico , Gabapentina , Humanos , Nefropatias/complicações , Prurido/etiologia , Ensaios Clínicos Controlados Aleatórios como Assunto , Reprodutibilidade dos Testes , Resultado do Tratamento , Ácido gama-Aminobutírico/uso terapêuticoRESUMO
Tricyclic antidepressants not only inhibit monoamine reuptake but also modulate Cys-loop receptors. However, it is not understood how this modulation is involved in their therapeutic effects. We analyzed the mechanisms of inhibition of homomeric 5-HT(3A) and alpha7-5HT(3A) receptors by tricyclic antidepressants at the single-channel and macroscopic current levels. These drugs reduce agonist-evoked currents in a noncompetitive and concentration-dependent manner. When they act on the open state, the reduction is similar for both receptors and it is voltage-dependent, thus suggesting an open-channel block process in which the blocked channel can either close or remain stabilized. By acting on the resting state, tricyclic antidepressants reduce the peak current in a voltage-independent manner, with a potency 6-fold higher for 5-HT(3A) than for alpha7-5HT(3A) (IC(50): 6 microM and 1 microM for alpha7-5HT(3A) and 5-HT(3A), respectively). Thus, tricyclic antidepressants may act on closed channels at the unshared extracellular domain from where they inhibit channel opening. Single alpha7-5HT(3A) channels in the continued presence of tricyclic antidepressants show: i) reduced open durations, compatible with open-channel block; ii) reduced burst durations, compatible with closing of blocked channels; and iii) reduced frequency of opening events, compatible with both impaired opening and stabilization of a closed state. In summary, our study reveals that tricyclic antidepressants inhibit homomeric Cys-loop receptors by acting through different mechanisms at open and closed conformational states and probably at two different domains, namely, the pore in the open state and the extracellular domain in the closed state.
Assuntos
Antidepressivos Tricíclicos/farmacologia , Antagonistas Nicotínicos/farmacologia , Receptores Nicotínicos/efeitos dos fármacos , Antagonistas do Receptor 5-HT3 de Serotonina , Antagonistas da Serotonina/farmacologia , Acetilcolina/metabolismo , Amitriptilina/farmacologia , Animais , Linhagem Celular , Cisteína/química , Relação Dose-Resposta a Droga , Doxepina/farmacologia , Humanos , Imipramina/farmacologia , Potenciais da Membrana , Camundongos , Mutação , Conformação Proteica , Estrutura Terciária de Proteína , Receptores Nicotínicos/química , Receptores Nicotínicos/genética , Receptores Nicotínicos/metabolismo , Receptores 5-HT3 de Serotonina/química , Receptores 5-HT3 de Serotonina/genética , Receptores 5-HT3 de Serotonina/metabolismo , Proteínas Recombinantes de Fusão/antagonistas & inibidores , Serotonina/metabolismo , Transfecção , Receptor Nicotínico de Acetilcolina alfa7RESUMO
O termo cefaléia do tipo tensional (CTT) define as cefaléias primárias anteriormente denominadas de cefaléias tensionais, cefaléias de contração muscular, psicogênicas, psicomiogênicas, de estresse, essencial e de tensão. Essas denominações revelavam-se ambíguas e controversas incluindo simultaneamente aspectos clínicos e propostas de fisiopatologia, não sendo universalmente aceitas e dificultando a realização de estudos aceitos pela comunidade científica. Com a classificação internacional de cefaléias de 1988, as cefaléias do tipo tensional puderam ser melhor definidas e hoje, com a classificação de 2003, seus critérios diagnósticos estão mais claros e próximos da realidade observada na apresentação desses pacientes. As CTTs constituem-se no tipo mais prevalente de cefaléias primárias. Os seus mecanismos são controversos e sua fisiopatologia complexa e pouco esclarecida parecendo envolver processos centrais de disfunção antinocieptiva e periféricos de comprometimento muscular. Apresenta-se nas formas episódicas freqüentes e infrequentes, crônica e provável. O seu tratamento divide-se em preventivo e agudo. O tratamento preventivo inclui o uso de antidepressivos tricíclicos associados ou não ao uso de relaxantes musculares de ação central. O tratamento das crises utiliza analgésicos e/ ou antiinflamatórios não esteróides e/ ou cafeína e/ ou relaxantes musculares e deve ser limitado a duas vezes por semana uma vez que essa dor pode transformar-se em cefaléia crônica diária. Abordagens acessórias como terapia cognitivo-comportamental, técnicas de relaxamento, biofeedback e a melhora geral das condições de vida também são preconizadas. Há importante associação, na forma crônica, com distúrbios emocionais e do sono e o prognóstico é bom quando o paciente é corretamente tratado
Assuntos
Humanos , Terapia Cognitivo-Comportamental , Diagnóstico Diferencial , Relaxamento , Cefaleia do Tipo Tensional , Amitriptilina , Carisoprodol , Clomipramina , Doxepina , Fluoxetina , Classificação Internacional de Doenças , NortriptilinaRESUMO
In addition to their well known actions on monoamine reuptake, tricyclic antidepressants have been shown to modulate ligand-gated ion channels (LGICs). Since the muscle nicotinic acetylcholine receptor (AChR) has been the model for studying structure-function relationships of LGICs, we analyzed the action of tricyclic antidepressants on this type of AChR at both single-channel and macroscopic current levels. We also determined their effects on ACh equilibrium binding and their interactions with the different conformational states of the AChR. Antidepressants produce a significant concentration-dependent decrease in the duration of clusters of single-channels (eight fold at 20 muM). They also decrease the peak amplitude and increase the decay rate of currents elicited by rapid perfusion of ACh to outside-out patches. In equilibrium binding assays, antidepressants promote the typical high-affinity desensitized state and inhibit binding of [piperidyl-3,4-(3)H (N)]-(N-(1-(2-thienyl)cyclohexyl)-3,4-piperidine ([(3)H]TCP) to its locus in resting and desensitized AChRs. The results indicate that tricyclic antidepressants: (i) interact with resting (closed), open, and desensitized channels; (ii) do not affect significantly channel opening and closing rates; (iii) do not act as fast open-channel blockers; (iv) inhibit activation of resting channels; and (v) may increase the rate of long-lived desensitization from the open state.
Assuntos
Antidepressivos Tricíclicos/farmacologia , Antagonistas Nicotínicos/farmacologia , Fenciclidina/análogos & derivados , Receptores Nicotínicos/efeitos dos fármacos , Acetilcolina/metabolismo , Amitriptilina/farmacologia , Animais , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Doxepina/farmacologia , Antagonistas de Aminoácidos Excitatórios/farmacologia , Humanos , Imipramina/farmacologia , Técnicas In Vitro , Rim/citologia , Rim/efeitos dos fármacos , Rim/metabolismo , Cinética , Potenciais da Membrana/efeitos dos fármacos , Camundongos , Técnicas de Patch-Clamp , Fenciclidina/farmacologia , Receptores Nicotínicos/metabolismo , TorpedoAssuntos
Humanos , Masculino , Idoso , Transtornos de Fotossensibilidade , Porfiria Cutânea Tardia/diagnóstico , Doxepina , Antebraço , Mãos , Insuficiência Renal Crônica/complicações , Insuficiência Renal Crônica/terapia , Transtornos de Fotossensibilidade , Porfiria Cutânea Tardia/induzido quimicamente , Porfiria Cutânea Tardia/tratamento farmacológicoRESUMO
Os medicamentos antidepressivos tornaram a depressäo um problema médico com elevado potencial tratavel. Nas últimas décadas houve um grande avanço na pesquisa e novos compostos surgiram. Os antidepressivos de primeira geraçäo tiveram seu uso limitado devido a tolerabilidade e toxicidade. Os novos compostos, embora mais seguros, näo se mostraram superiores aos antidepressivos tradicionais. Neste artigo o autor revisa a farmacologia e as indicaçöes dos antidepressivos, assim como as indicaçöes e a eficácia diferencial entre os compostos clássicos e de nova geraçäo(au)
Assuntos
Humanos , Antidepressivos , Depressão/tratamento farmacológico , Serotoninérgicos/uso terapêutico , Amitriptilina , Monoaminas Biogênicas , Bupropiona , Clomipramina , Desipramina , Doxepina , Imipramina , Inibidores Seletivos de Recaptação de Serotonina/uso terapêutico , MaprotilinaRESUMO
A doxepina é um antidepressivo tricíclico, que devido às suas propriedades também de bloqueador dos receptores histamínicos (H1) é eficaz no tratamento da urticária crônica. Neste trabalho são citadas suas propriedades e outras indicações
Assuntos
Dermatopatias , Doxepina , Hipersensibilidade , Antidepressivos TricíclicosRESUMO
The dissolution and diffussion methods through homogeneous synthetic membrane were studied in different semisolid topical formulations containing metronidazole and doxepin. The results suggest that the rate of release showed a first order kinetic for one of the formulations and the rate of release described by Higuchi for the others.
Assuntos
Antidepressivos Tricíclicos/química , Antiprotozoários/química , Doxepina/química , Metronidazol/química , Antidepressivos Tricíclicos/administração & dosagem , Antiprotozoários/administração & dosagem , Difusão , Doxepina/administração & dosagem , Membranas Artificiais , Metronidazol/administração & dosagem , SolubilidadeAssuntos
Humanos , Feminino , Antidepressivos Tricíclicos/uso terapêutico , Antagonistas Adrenérgicos beta/uso terapêutico , Doxepina/uso terapêutico , Efedrina/uso terapêutico , Estrogênios/uso terapêutico , Imipramina/uso terapêutico , Incontinência Urinária por Estresse/terapia , Fenilpropanolamina/uso terapêutico , Propranolol/uso terapêutico , Antidepressivos Tricíclicos , Antidepressivos Tricíclicos/efeitos adversos , Terapia por Estimulação Elétrica , Incontinência Urinária por Estresse/classificação , Incontinência Urinária por Estresse/diagnósticoRESUMO
O objetivo deste artigo é rever a literatura no que se refere à eficácia, efeitos colaterais e uso de antidepressivos tricíclicos e de segunda geraçäo em geriatria. Os vários ensaios clínicos duplo-cegos com esses psicofármacos aplicados a idosos, relatados na literatura de língua inglesa até 1989, foram resenhados
Assuntos
Idoso , Humanos , Masculino , Feminino , Antidepressivos Tricíclicos/uso terapêutico , Transtorno Depressivo/tratamento farmacológico , Amitriptilina/uso terapêutico , Antidepressivos Tricíclicos/efeitos adversos , Método Duplo-Cego , Doxepina/uso terapêutico , Imipramina/efeitos adversos , Mianserina/uso terapêutico , Nortriptilina/uso terapêutico , Psicotrópicos/administração & dosagemRESUMO
Neste artigo é exposto sucintamente aspectos do metabolismo dos antidepressivos tricíclicos (desmetilaçao e hipdroxilaçao) que devem ser levados em conta na interpretaçao das dosagens plasmáticas e efeitos clínicos destes medicamentos