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Metabolism of Chemical Carcinogens by Intestinal Tissue
Published in Herman Autrup, Gary M. Williams, Experimental Colon Carcinogenesis, 2019
Several N-nitrosamines were also metabolized by human colon into metabolites which associate with DNA (Table 1, Figure 1). The highest level of modification occurred with dimethylnitrosamine (DMNA).50 Only the tissues that exhibit a high level of binding of DMNA also bound detectable amounts of diethylnitrosamine or N-nitro-sopyrrolidine.50 However, these N-nitrosamines were metabolized as indicated by binding to cellular proteins and formation of CO2. Two other nitrosamines, N-nitrosopi-perazine and N-nitrosopiperidine, were also metabolized in colon as measured by the same criteria.50 A positive correlation between the amount of 14COz formed after incubation with DMNA for 24 hr and the level of radioactivity associated with DNA was observed in human colon. Most of the alkylation of DNA with DMNA occurred at the phosphate groups, but some alkylation was also observed at the O6 and 7 positions of guanine50 (Figure 2).
Migraine: diagnosis and treatment
Published in Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby, Headache in Clinical Practice, 2018
Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby
Nausea and vomiting can be as disabling as the headache itself. Gastric stasis and delayed gastric emptying decrease the effectiveness of oral medication.7 We use metoclo–pramide or domperidone as an antiemetic and a prokinetic to enhance the absorption of oral medications. Promethazine intravenously (0.15 mgftg diluted in 50 ml of 5% dextrose or normal saline) or ondansetron (a selective 5-HT3–receptor antagonist) orally (8-mg tablet) or intravenously (4–8 mg) can be used by patients who cannot tolerate metoclopramide because of side-effects. We use the neuroleptics, chlorpromazine, droperidol, and prochlor–perazine, intravenously, intramuscularly, and by suppository, for nausea, vomiting, and pain. Prochlorperazine suppositories (25 mg) are used as a primary treatment for headache and nausea and also as a rescue medication.
Intracytoplasmic sperm injection Technical aspects
Published in David K. Gardner, Ariel Weissman, Colin M. Howles, Zeev Shoham, Textbook of Assisted Reproductive Techniques, 2017
Queenie V. Neri, Nigel Pereira, Tyler Cozzubbo, Zev Rosenwaks, Gianpiero D. Palermo
Semen samples are collected by masturbation after 3-5 days of abstinence and allowed to liquefy for at least 20 minutes at 37°C before analysis. When the semen has high viscosity, this can be reduced within three to five minutes usually by adding it to 2-3 mL of 4-(2 hydroxyethyl)-1-pi- perazine-ethanesulfonic acid (HEPES)-buffered human tubal fluid (HTF) containing 200-300 IU of chymotrypsin (Sigma Chemical Co., St Louis, MO). The use of limited proteolytic enzyme with chymotrypsin was shown to effectively disperse hyperviscous samples for semen preparation (21, 22). Electroejaculation is applied in cases of spinal cord injury or psychogenic anejaculation (23).
Psychiatric and non-psychiatric drugs causing false-positive amphetamines urine test in psychiatric patients: a pharmacovigilance analysis using FAERS
Published in Expert Review of Clinical Pharmacology, 2023
Vera Battini, Giovanna Cirnigliaro, Luca Giacovelli, Maria Boscacci, Silvia Massara Manzo, Giulia Mosini, Greta Guarnieri, Michele Gringeri, Beatrice Benatti, Emilio Clementi, Bernardo Dell’Osso, Carla Carnovale
Many psychoactive drugs, ranging from antidepressants to antipsychotics, were listed as a cause for false-positive results, such as bupropion [52], trazodone [43], atomoxetine [29], promethazine [51] and selegiline [61,75]. Most of the detected drugs were first-generation antipsychotics, such as promethazine, perazine, chlorpromazine, and promazine; these agents work on dopaminergic neurotransmission, but are less selective, with noradrenergic, cholinergic, and histaminergic blocking actions [76]. Many of these drugs are today rarely used but remain a good choice for their sedative effects and for the treatment of more resistant and acute psychiatric patients [77]. All of them showed similarities with the structure of amphetamine [51]. Of note, some studies included in the review reported also false-positive results associated with the use of newer antipsychotics, such as Aripiprazole [18,33], a third-generation drug known for their partial agonism of dopamine receptor, suggesting that further evaluation on recently introduced new drugs of this class (Brexpiprazole, Cariprazine) may lead to similar issues or, conversely, the changes apported in the chemical structures may be sufficient to avoid the mis-interpretation of the drug. At the same time, many drugs involved in false-positive UDS emerged in our literature review are commonly used in the clinical practice of general medicine, for example beta blockers, fenofibrate, and ranitidine.
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’.
Seizure rates under treatment with antipsychotic drugs: Data from the AMSP project
Published in The World Journal of Biological Psychiatry, 2019
Katrin Druschky, Stefan Bleich, Renate Grohmann, Rolf R. Engel, Alexandra Neyazi, Susanne Stübner, Sermin Toto
The median APD dosages in patients experiencing a seizure in terms of an ADR and in all the patients treated are given in Table 1b. The seizure group was further differentiated into two categories, namely, ‘all cases’, in which either the individual drug or the drug in combination with others was causative of a seizure, or to the category ‘imputed alone’, in which the individual drug is considered responsible. The median dosages of the APDs administered were within the recommended range for each substance. In 11 out of 19 instances, the APD median dosages lay somewhat higher in the seizure cases, with the largest differences found with perazine and quetiapine in the patients of the category ‘drug imputed alone’. In this category, perazine was administered at a median dosage that was three times higher, and quetiapine at a median dosage twice as high as that in all the treated patients. In the group of schizophrenic disorders, the median daily APD dosages were somewhat higher for most substances, with the largest difference seen with clozapine-treated schizophrenic patients (300 mg/day) compared to the other diagnostic groups (137.5–150 mg/day).