Loxapine

The early and correct assessment of psychomotor agitation (PMA) is essential to ensure prompt intervention by healthcare professionals to improve the patient's condition, protect healthcare staff, and facilitate future management. Proper training for recognizing and managing agitation in all care settings is desirable to improve patient outcomes. The best approach is one that is ethical, non-invasive, and respectful of the patient's dignity. When deemed necessary, pharmacological interventions must be administered rapidly and avoid producing an excessive state of sedation, except in cases of severe and imminent danger to the patient or others...

Psychotropic medication treatment can cause elevated serum prolactin levels and hyperprolactinaemia (HPRL). Reports have suggested that aripiprazole may decrease elevated prolactin. The aim of this review was to assess evidence for the efficacy of adjunct aripiprazole in the treatment of psychotropic-induced HPRL. PubMed and Google Scholar were searched to identify randomised placebo-controlled trials (RCTs) of adjunct aripiprazole in patients with HPRL attributed to primary psychotropic medications. Data for individual patients from case studies, chart reviews and open-label studies were also identified and assessed...

This case series highlights the importance of loxapine in psychiatric disorders when clozapine is unable to control agitation and psychotic symptoms due to medication noncompliance, intolerable side effects, or inadequate clinical outcomes. Loxapine is classified as a first-generation typical antipsychotic but displays atypical antipsychotic-like characteristics with structural similarity to clozapine. However, since the inception of second-generation antipsychotic medications, the role of loxapine in modern psychiatric practice has become limited...

BACKGROUND/AIM: We investigated drugs that could sensitize P-glycoprotein (P-gp)-overexpressing drug-resistant cancer cells to vincristine (VIC) or eribulin treatment and assessed their associated mechanisms of action. MATERIALS AND METHODS: We investigated 15 bipolar drugs (quetiapine, risperidone, clozapine, asenapine, iloperidone, paliperidone, ziprasidone, trifluoperazine, loxapine succinate, pilocarpine, valproic acid, carbamazepine, levetiracetam, topiramate, and felbamate) to identify drugs with a sensitizing effect on VIC-resistant KBV20C cells at relatively low doses...

OBJECTIVE: In this paper, we aimed at reviewing evidence-based treatment options for bipolar mania and proposed tentative evidence-based clinical suggestions regarding the management of a manic episode, especially regarding the choice of the proper mood stabilizer and antipsychotic medication. METHOD: A narrative review was undertaken addressing 'treatment of bipolar mania'. Findings have been synthesized and incorporated with clinical experience into a model to support different treatment choices...

Patients with substance use disorders (SUD) are at high risk to die by suicide. So far, the neurobiology of the suicide-SUD association has not been elucidated. This study aimed to identify potential pharmacological targets among hub genes from brain gene co-expression networks of individuals with SUD in a suicidal and non-suicidal context. Post-mortem samples from the prefrontal cortex of 79 individuals were analyzed. Individuals were classified into the following groups: suicides with SUD (n = 28), suicides without SUD (n = 23), nonsuicides with SUD (n = 9), nonsuicides without SUD (n = 19)...

PURPOSE OF REVIEW: Agitation associated with schizophrenia remains an important clinical concern and if not managed effectively, can escalate into aggressive behavior. This is a review of the recent biomedical literature on agitation in individuals with schizophrenia. RECENT FINDINGS: Themes in the recent literature include consideration of comorbidities such as cigarette smoking and cannabis use. Surveys reveal that pharmacological approaches to manage agitation have changed little, with haloperidol remaining in common use and intramuscular administration of antipsychotics and/or benzodiazepines being frequently administered to more severely agitated/aggressive individuals...

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Background: Acute agitation in the pediatric emergency department (ED) has the potential to escalate into aggression and result in harm. Rapid and effective management may be warranted. Use of pro re nata (prn) oral immediate-release (IR) quetiapine, haloperidol, loxapine, and chlorpromazine has been observed in the pediatric ED at Surrey Memorial Hospital to manage this condition; however, evidence for oral prn antipsychotic use is limited in the pediatric population. Objectives: The primary objective is to characterize the dose of prn oral IR quetiapine used to manage acute agitation or aggression in a pediatric ED...

Cases of foreign body ingestion in the forensic literature are mainly described in children or psychiatric patients. Postmortem imaging can detect most foreign bodies, but its sensitivity depends, among other things, on the type of item and its location. In some cases, the ingestion of foreign bodies can remain unnoticed and have serious consequences for the patient. We describe the case of a patient who died in a psychiatric seclusion room with no obvious cause and for whom a forensic autopsy was requested...

Two-pore domain K+ channels (K2Ps) regulate the resting membrane potential in excitable cells and determine ease of depolarization. Gain-of-function (gf) mutations in one of these channels (unc-58) in C. elegans switch it to a Na+ conductance channel and cause tremors, paralysis and other defects. We hypothesized that it should be possible to identify drugs that corrected these defects in unc-58(gf) mutant animals by blocking or modulating the over-active channels. We examined dispersal of animals on food because the absence of effective forward locomotion is the most obvious defect...

Introduction There are several new and emerging antipsychotic medication strategies recently marketed or under clinical development for the treatment of several mental disorders. There is the need to provide an up-to-date overview on the safety of this new generation of antipsychotic medications, which includes also the third-generation antipsychotics (TGA). Areas covered The authors aimed at providing a synthesis of the most current evidence about the safety profile of the recently developed and/or marketed antipsychotics...

BACKGROUND: Clozapine is mainly used in patients with treatment-resistant schizophrenia and may lead to potentially severe haematologic adverse events, such as agranulocytosis. Whether clozapine might be associated with haematologic malignancies is unknown. We aimed to assess the association between haematologic malignancies and clozapine using Vigibase®, the WHO pharmacovigilance database. METHODS: We performed a disproportionality analysis to compute reporting odds-ratio adjusted for age, sex and concurrent reporting of antineoplastic/immunomodulating agents (aROR) for clozapine and structurally related drugs (loxapine, olanzapine and quetiapine) compared with other antipsychotic drugs...

Angioedema is characterized by marked swelling of the subcutaneous or submucosal tissue and may affect various parts of the body, including the face, mouth, and extremities. Angioedema has specifically been associated with the use of several antipsychotic agents, including clozapine, olanzapine, iloperidone, haloperidol, quetiapine, paliperidone, ziprasidone, risperidone, and chlorpromazine. A 67-year-old African American male with a past medical history significant for hypertension, coronary artery disease requiring stent placement, mitral insufficiency, hyperlipidemia, tobacco use disorder, and schizophrenia presented with altered mental status and disorientation in the setting of clozapine nonadherence, which prompted acute hospitalization for clozapine reinitiation...

Agitation is a common and serious symptom of bipolar mania and schizophrenia, and can be defined as excessive motor and verbal activity. If left unrecognized and untreated, agitation can evolve into aggression, resulting in potential patient and staff injury. An ideal treatment for agitation would have a rapid onset, cause calmness without sedation, and be tolerable, efficacious, and non-coercive, while managing the underlying condition. A novel approach for the treatment of agitation is inhaled loxapine. Inhaled loxapine is rapidly absorbed into the systemic circulation through the alveoli, resulting in a near immediate onset of action...

Neuropathic pain is a debilitating and commonly treatment-refractory condition requiring novel therapeutic options. Accumulating preclinical studies indicate that the potassium channel Slack (KNa 1.1) contributes to the processing of neuropathic pain, and that Slack activators, when injected into mice, ameliorate pain-related hypersensitivity. However, whether Slack activation might reduce neuropathic pain in humans remains elusive. Here, we evaluated the tolerability and analgesic efficacy of loxapine, a first-generation antipsychotic drug and Slack activator, in neuropathic pain patients...

BACKGROUND: The emergence of multiple-antibiotic-resistant (MAR) Salmonella has been a serious threat worldwide. Salmonella can invade into host cells and evade the attacks of host humoral defenses and antibiotics. Thus, a new antibacterial agent capable of inhibiting intracellular Salmonella is highly needed. METHODS: The anti-intracellular activity and cytotoxicity of drugs on intracellular bacteria and macrophages were assayed using intracellular CFU assay and MTT cell viability assay, respectively...

Autosomal dominant polycystic kidney disease (ADPKD) is caused mostly by mutations in polycystin-1 or polycystin-2. Fluid flow leads to polycystin-dependent calcium influx and nuclear export of histone deacetylase 5 (HDAC5), which facilitates the maintenance of renal epithelial architecture by de-repression of MEF2C target genes. Here, we screened a small-molecule library to find drugs that promotes nuclear export of HDAC5. We found that dopamine receptor antagonists, domperidone and loxapine succinate, stimulate export of HDAC5, even in Pkd1-/-cells...

Migraine is a disabling primary headache disorder that requires effective treatments. Inhalation is currently being explored for the delivery of drugs for migraine. Pulmonary-route delivery of drugs shows potential advantages for its use as a treatment, particularly compared the oral route. Areas covered: The authors highlight the current state of the literature and review multiple therapies for migraine-utilizing inhalation as the route of administration. The following therapeutics are discussed: inhaled ergotamine, inhaled dihydroergotamine mesylate (MAP0004), inhaled prochlorperazine, and inhaled loxapine...

OBJECTIVES: Our objective was to compare outcomes of discharge disposition, need for additional medications, and restraint use for patients who received inhaled loxapine compared with patients receiving traditional antipsychotic drugs in the emergency department (ED). METHODS: A retrospective chart review was conducted on all patients who presented to the ED with agitation and received antipsychotic therapy, including loxapine, ziprasidone, or haloperidol from December 1, 2014, through October 31, 2016...