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Psychiatric disorders
Published in Anne Lee, Sally Inch, David Finnigan, Therapeutics in Pregnancy and Lactation, 2019
The use of depot antipsychotic preparations in pregnancy is not encouraged. There are no published data on the effects of zuclopenthixol, flupenthixol, pipothiazine and fluphenazine depot preparations in pregnancy. These agents cannot, if necessary, be withdrawn rapidly and the dose cannot be reduced towards delivery to limit neonatal withdrawal symptoms. Depot preparations should only be used where compliance is a problem.
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Zuclopenthixol, a thioxanthene derivative used in the treatment of schizophrenia, has high affinity for both D1 and D2 receptors and α1-adrenergic and 5-HT2 receptors (Kumar and Strech 2005). It has weak histamine H1 receptor blocking activity and lower affinity for muscarinic cholinergic and α2-adrenergic receptors. The pharmacokinetics of zuclopenthixol appears linear over the dosage range investigated. The metabolism of zuclopenthixol is mainly by sulfoxidation, side-chain N-dealkylation, and glucuronidation (Figure 3.30). The metabolites are devoid of pharmacological activity. Zuclopenthixol sulfoxidation and N-dealkylation are mainly metabolized by CYP2D6 and other enzymes (Dahl et al. 1991a). The clearance of zuclopenthixol cosegregates with debrisoquine hydroxylation in humans (Bertilsson et al. 1993; Dahl et al. 1991a), indicating the involvement of CYP2D6 in the metabolism of zuclopenthixol.
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’.
Hyperprolactinemia in psychotic patients treated in monotherapy with long-acting injectable antipsychotics
Published in International Journal of Psychiatry in Clinical Practice, 2019
José María Bonete Llácer, Alicia Martínez Hortelano, Begoña Richart Albelda
We found an overall prevalence of HPRL of 52.41% (87 out of 166 patients). The highest rates of HPRL were detected in patients treated with LAI paliperidone (95.65%) and risperidone (60.61%) (Table 2). Patients treated with zuclopenthixol and fluphenazine presented rates of HPRL of 17.14% and 46.15%, respectively. In all cases we observed higher rates in women than in men, especially in patients treated with zuclopenthixol (33.34% of women versus 8.69% of men). No cases of HPRL were found in patients treated with aripiprazole (Table 2). The levels of PRL observed in the patients varied considerably with each prescribed antipsychotic (Fig. 1). The highest mean values were observed in patients on paliperidone (62.43 ng/ml, CI95 = 53.12–72.09) and risperidone (40.17ng/ml, CI95 = 30.92–52.06), which would be considered as moderate and mild HPRL, respectively (Serri et al., 2003). Patients medicated with fluphenazine and zuclopenthixol presented low mean values of PRL (23.88 ng/ml, CI95 = 19.87–27.89, and 19.32 ng/ml, CI95 = 16.89–21.94, respectively); patients on aripiprazole presented the lowest mean values of PRL (10.34 ng/ml, CI95 = 8.00–12.79).
Safety and tolerability of antipsychotic agents in neurodevelopmental disorders: a systematic review
Published in Expert Opinion on Drug Safety, 2020
Felice Iasevoli, Annarita Barone, Elisabetta Filomena Buonaguro, Licia Vellucci, Andrea de Bartolomeis
Overall, available data indicate that risperidone may be considered as the first-line agent in both child/adolescent and adult ID patients, relatively to safety and tolerability. Second-line agents should be aripiprazole in child/adolescent and olanzapine in adult patients. In child/adolescent patients, olanzapine may be prescribed in the case of failure with first and second-line agents. In adult patients, clozapine may represent a third-line strategy. Zuclopenthixol has been used in a small sample, but data on safety/tolerability should be considered inconclusive, although encouraging. Data on the other agents are extremely sparse and did not allow to formulate reliable practical recommendations.