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Intestinal Pharmacomanometry
Published in Fuad Lechin, Bertha van der Dijs, Neurochemistry and Clinical Disorders: Circuitry of Some Psychiatric and Psychosomatic Syndromes, 2020
Fuad Lechin, Bertha van der Dijs, Francisco Gomez, Marcel Lechin, Luis Arocha, Simon Villa
The cholinergic-serotonergic (ACh-5HT), noradrenergic (NE), and dopaminergic (DA) systems are known to influence distal colon motility (DCM) in humans. The administration in usual therapeutic doses of drugs, agonistic or antagonistic to these systems, can enhance or reduce that motor activity.14 Up to the present, we have investigated the effect of drugs such as D-amphetamine (releases catecholamines and inhibits their reuptake by terminals); fenfluramine (releases serotonin); mianserin, chlorprothixene (α2-blocking agents, which induce NE release from terminals); prazosin (α1-blocking agent, which antagonizes NE effect at postsynaptic level); phentolamine and dihydroergotamine (α + α2-blocking agents); clonidine (α2- agonist which inhibits NE release from terminals); propranolol (β, + β2-blocking agent); haloperidol, sulpiride, pimozide, thioproperazine, trifluoperazine, chlorproperazine, and other dopaminergic blocking agents; thioridazine (DA + NE antagonist); domperidone (peripheral DA blocking agent); nomifensine and methylphenidate (inhibitors of DA uptake); metergoline (5HT2-blocking agent); methysergide (peripheral 5HT antagonist); clonazepam (inhibits DA release by acting at presynaptic level); bromocriptine (presynaptic DA agonist); lorazepam, prazepam and other benzodiazepines; biperiden (central acting anti-ACh agent); hioscine (peripheral anti-ACh agent); baclofen (Gabamimetic agent); and other drugs such as diphenyl-hydantoin and cholecystokinin.5,11
‘In and Out of the Hole’
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Management of MXE toxicity depends on the clinical scenario and other drugs taken (Adamowicz & Zuba, 2015; Hydzik, Gomółka, Sulka, & Cudzich-Czop, 2012; Rosenbaum et al., 2012). Low doses of benzodiazepines are recommended along with keeping the patient under observation during recovery (Wood et al., 2012). Benzodiazepines were used intravenously for treatment of agitation and aggression induced by MXE. The benzodiazepine derivatives used were diazepam, clonazepam, chlorprothixene, and midazolam. Antiemetics can be used for nausea and vomiting. Prevention of rhabdomyolysis can be undertaken by administering body fluids. Moreover, malignant hypertension can be treated using BZDs, sodium nitroprusside, or phentolamines (Craig & Loeffler, 2014). If needed, respiratory support should be offered to the patient.
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
The first-generation antipsychotics are known as “typical antipsychotics,” including chlorpromazine, chlorprothixene, haloperidol, flupentixol, fluphenazine, mesoridazine, perphen-azine, promazine, promethazine, thioridazine, trifluproma-zinc, and zuclopenthixol (Lieberman et al. 2008). Most of the drugs in the second generation, known as “atypical anti-psychotics,” have been developed. The second-generation antipsychotics include amisulpride, aripiprazole, clozapine, olanzapine, paliperidone, quetiapine, risperidone, sertindole, ziprasidone, and zotepine (Lieberman et al. 2008; Vohora 2007; Worrel et al. 2000). Newer antipsychotic agents, such as asenapine, bifeprunox, norclozapine, and iloperidone, are being developed (Bishara and Taylor 2008). Antipsychotics are generally highly lipid soluble, subject to high clearance, and eliminated by metabolic rather than renal pathways. CYP2D6 is involved in the metabolism of a variety of anti-psychotics, including clozapine, thioridazine, perphenazine, chlorpromazine, fluphenazine, haloperidol, zuclopenthixol, risperidone, iloperidone, and sertindole (Gardiner and Begg 2006; Ingelman-Sundberg 2005; Zhou et al. 2008). CYP1A2 and 3A are also involved in the metabolism of antipsychotic drugs including clozapine, olanzapine, pimozide, and haloperidol (Gardiner and Begg 2006; Ingelman-Sundberg 2005; Zhou et al. 2008). There is preliminary evidence that CYP2D6 phenotype status may affect the clearance of this group and thus alter the clinical response to them.
Engineered PLGA microspheres for extended release of brexpiprazole: in vitro and in vivo studies
Published in Drug Development and Industrial Pharmacy, 2021
Bangqing Wu, Lijun Wu, Yingju He, Zongning Yin, Li Deng
Schizophrenia refers to a chronic and disabling mental disease [1,2], characterized by high morbidity and mortality rates, recurrent episodes, and a lack of treatment options leading to great psychological and economic burden to the patient and the society [3,4]. Current anti-schizophrenia therapeutics on the market were divided into three categories, including the first generation anti-schizophrenia drugs such as chlorpromazine, chlorprothixene, and haloperidol, the second generation drugs such as olanzapine, clozapine, risperidone, and paliperidone, and the third generation drugs including aripiprazole, brexpiprazole, and cariprazine [5,6]. The first generation drugs showed numerous adverse reactions due to a lack of selectivity on receptors [7]. For example, the most severe and frequent adverse reaction is extra pyramidal syndrome [8]. The second and the third generation drugs are proven effective to most symptoms of schizophrenia with less systemic adverse effects [9,10].
Severe drug-induced liver injury in patients under treatment with antipsychotic drugs: Data from the AMSP study
Published in The World Journal of Biological Psychiatry, 2021
Katrin Druschky, Sermin Toto, Stefan Bleich, Jessica Baumgärtner, Rolf R. Engel, Renate Grohmann, Hannah B. Maier, Alexandra Neyazi, Yannick J. Rudolph, Eckart Rüther, Harald Schwörer, Johanna Seifert, Susanne Stübner, Detlef Degner
The group of patients with severe DILI was further differentiated into two categories, namely, ‘all events’, in which either the individual drug or the drug in combination with others was assessed to be causative for severe DILI, or ‘imputed alone’, in which only the individual drug was considered responsible. The three APDs most often related to severe DILI were olanzapine, clozapine and perazine (Table 3). The median dosages of the APDs applied were within the recommended levels for each substance. For the following 7 out of 17 substances, the APD median dosages were considerably (i.e. more than 1.5 times) higher in the DILI cases: amisulpride, chlorprothixene, haloperidol, perazine, promethazine, quetiapine and zuclopenthixol/clopenthixol. The largest differences were found with chlorprothixene and zuclopenthixol/clopenthixol (‘drug imputed alone’). In these cases, chlorprothixene was applied at a median dosage that was more than three times higher, and zuclopenthixol/clopenthixol was applied at a median dosage that was 4.6 times higher than that for all treated patients. For perazine, promethazine and zuclopenthixol/clopenthixol, the described higher dosages were related to both categories (‘all events’ and ‘drug imputed alone’), and for amisulpride, chlorprothixene, haloperidol and quetiapine, the described higher dosages were only related to ‘drug imputed alone’.
Antipsychotics as a method of suicide: population based follow-up study of suicide in Northern Finland
Published in Nordic Journal of Psychiatry, 2021
Arja Mainio, Liisa Kuusisto, Helinä Hakko, Pirkko Riipinen
There are contradictory findings regarding the fatal toxicity of quetiapine [28,29]. While comparing toxicity of quetiapine with the reference drug chlorpromazine, quetiapine was not found to be more toxic than reference [28]. However, other studies have found toxicity of quetiapine to be relatively high. Ojanperä et al. [29] found that, among antipsychotics, the most toxic drug was levomepromazine, followed by chlorprothixene and then quetiapine. They also highlighted that, when fatal poisoning occurs, there are often several drugs involved rather than one single medication. Methling et al. [30] also reported that, among antipsychotics, quetiapine was the most toxic drug compared to both FGAs and SGAs among suicide autopsies. In large poison center study Nelson and Spyker [31] noted that, among depressed patients using atypical antipsychotics, the major fatal index represented quetiapine. Quetiapine had relatively high rates of coma and respiratory depression compared to other medications, and these problems may be responsible of suicide death.