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PubMed1978

Cholestatic effects of cis-chlorprothixene on the perfused rat liver.

The cis-isomer of chlorprothixene (CPX) inhibited the excretory function of the isolated perfused rat liver. It decreased the biliary clearance and transport maximum of sulfobromophthalein (BSP). Calculation of the BSP 'clearance constants' suggested that the primary effect of the drug was on excretion and not uptake. The ability of the drug to inhibit the excretion of indocyanine green suggested that the effects of CPX were not the result of inhibition of hepatic conjugative enzymes. Measurement of 14C-erythritol clearance indicated that the deleterious effects of CPX on bile formation were at the canalicular level and that they were mainly on the bile acid-independent fraction of bile. The data indicated that the adverse effects of CPX were at the excretory level of the hepatocyte.

Animals↗
PubMed1975

[Chlorprothixene for premedication in children: oral versus intramuscular route (author's transl)].

The effect of chlorprothixene (Taractan), a neuroleptic agent, administered either intramuscularly (1 mg/kg) or orally as a 4% solution (1,5-2 mg/kg), was compared in a double-blind study in 200 children between 11 months and 10 years of age. In addition, intramuscular 1-hyoscyamine (Bellafolin) was given to all patients 30 minutes before the induction of anaesthesia (0.005-0.01 mg/kg). With regard to antisalivary action, suppression of reflex irritability, frequency of post-anaesthetic vomiting, postoperative sedation and requirement of postoperative analgesics, there was no significant difference between the two methods. Preoperative sedation was slightly more pronounced with the intramuscular technique. An undesirable side-effect, hypotension, was observed more often after intramuscular than oral premedication. To obtain optimum effect, an interval of 2 hours between the oral premedication and induction of anaesthesia is recommended.

Anesthesia↗
PubMedDate not supplied

Phenolic metabolites of chlorprothixene in man and dog.

From urine and feces of dogs and urine of patients given chlorprothixene (CPT) per os, metabolites were extracted without or with enzymatic deconjugation and separated by repeated TLC. Purified compounds were characterized by UV, NMR, and mass spectrometry, by color reactions, and by chemical interconversions. Both species excreted 6- and 7-hydroxy-CPT besides the sulfoxide and demethylated analogues. In urine, the phenols were largely present as conjugates. The major metabolites in dog feces were 5-hydroxy-CPT and its demethylated derivative, whereas 5-hydroxylation was not detected in man. Dog excrete also contained 6-hydroxy-7-methoxy (or 7-hydroxy-6-methoxy)-CPT; further, a 5-hydroxy compound was detected in which the exocyclic double bond was hydrated. In the other metabolites, the Z-configuration of CPT had been retained, but small quantities of E-isomers were formed during isolation. According to preliminary quantitative data, phenols accounted for a small part of extractable metabolites in human urine, whereas they predominated in dog feces.

Animals↗
PubMedDate not supplied

Action of antidepressant neuroleptics, chlorprothixene and levomepromazine, on the central noradrenergic system: comparison with other antidepressants.

In contrast to imipramine, chlorprothixene (CPX) and levomepromazine (LMZ) given chronically did not affect clonidine-induced hypothermia and depression of noradrenaline synthesis rate, while similarly to imipramine and citalopram depressed the density of cortical 3H-clonidine binding sites and increased their affinity. Two week treatment with the antidepressants did not affect the parameters of 3H-dihydroalprenolol binding sites, while spiroperidol administration increased their density, without changing KD values. The data suggest that changes in alpha 2 adrenoceptor population parameters may be a general characteristics of antidepressant treatment, but not necessarily followed by changes in clonidine effects.

Animals↗
PubMed1975

[Comparison of the endocrine response under 2 kinds of anesthesia: neuroleptanalgesia of the chlorprothixene-dextromoramide type and venous anesthesia of the type alfadione-fentanyl].

In 14 patients anaesthetized before undergoing an orthopedic surgical intervention, the variations induced by anaesthesia in the 17 hydroxycorticosterone rate, catecholamine, somatotropic hormone (STH), insulin, glycemia, free fatty acids and thyrotropin (TSH), all these variations were studied before the surgery. The patients were divided into 2 groups of 7, the first one being anaesthestized by chlorprothixene dextromoramide Neurolept-Analgesia and the second one by Alfadione Fentanyl venous anaesthesia.

Alfaxalone Alfadolone Mixture↗
PubMed1976

[Proceedings: Age and sex specificity of organ distribution and metabolism of chlorprothixene and nortriptyline in the rat (author's transl)].

Chlorprothixene and its N-desmethyl derivative are found to be present in the brain, liver, kidneys and lungs of young animals in larger quantities and for a longer period of time than in older animals. The N-demethylation rate is significantly higher in the brain, liver, kidney and lungs of older animals than of young animals. In general, female animals show higher levels in the organs. The "youth dependent" hyper-content exceeds that of the older animals by the factor of appr. 2. For nortriptyline there is an inverse ratio, with more nortriptyline and desmethylnortriptyline in the older animals than in the young ones. The organ content is also higher in the females than in the males. The "age-dependent" hyper-content exceeds that of the younger animals by the factor of appr. 2. These results correspond roughly with the differences in toxicity.

Aging↗