Chlorprothixene (?Truxal?) compared to chlorpromazine

Remvig, J; Sonne, Lass Mahler

doi:10.1007/bf00407980

Cited by 16 publications

(5 citation statements)

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“…Chlorprothixene (a thioxanthene analogue), chlordiazepoxide and amitriptyline have properties that do not fit easily into any of the above groups, although they do exert a psychic calming effect. Chlorprothixene and amitriptyline appear to produce psychic stimulation or "anti-depression" but there is also an element of hypnotic depression (Darling, 1961;Remvig and Sonne, 1961;Pare, Rees and Sainsbury, 1962;Sulser, Watts and Brodie, 1962). For the anaesthetist, it would probably serve best to use the simple term "psychotropic drugs" to apply to any drug which either depresses or stimulates the central nervous system, as recommended by Gerard (1957).…”

Section: Discussionmentioning

confidence: 99%

“…The main side effects are drowsiness, dizziness, dryness of the mouth, orthostatic hypotension, nausea and faintness. All side effects except the drowsiness can be accounted for by hypotension which is undoubtedly a frequent occurrence with chlorprothixene therapy in ambulant patients (Darling, 1961;Karn, Mead and Fishman, 1961;Remvig and Sonne, 1961). Hougs (1960) has studied the pharmacology of chlorprothixene to determine its efficacy in anaesthesia and has pointed out that its anti-acetylcholine, anti-adrenaline and anti-serotonin activities (which are greater than those of chlorpromazine) are desirable properties.…”

Section: Chlorprothixenementioning

confidence: 99%

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CHLORPROTHIXENE AND AMTTRIPTYLINEt: INTERACTION WITH THIOPENTONE, CIRCULATORY EFFECT AND ANTISIALOGOGUE EFFECT

Dobkin

Israel

Byles

et al. 1963

British Journal of Anaesthesia

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Evaluation of the interaction of chlorprothixene and amitriptyline with thiopentone, in dogs, showed that both of these have pharmacological properties which cause delayed recovery from anaesthesia. This effect is particularly strong with chlorprothixene. The effect on the circulatory response to tilt was measured with these two drugs in young healthy male subjects, and both caused orthostatic hypotension, which was rather severe in the case of chlorprothixene, and mild with amitriptyline. Tests of antisialogogue activity with chlorprothixene, on the same subjects, showed that this drug was inactive in this respect, although it is reported to exert very strong anticholinergic effects on other organ systems. Chlorprothixene and amitriptyline have some pharmacological properties that led to the suggestion that they might be of value in pre-anaesthetic medication. Chlorprothixene is the transisomer of 2-chloro-9-(3-dimethylaminopropylidene thioxanthene, which is closely related to the phenothiazine derivative chlorpromazine-the main difference being the substitution of carbon for nitrogen in the central ring. Their pharmacological properties are quite similar (Pellmont et al., 1960). Amitriptyline is a cyclic dibenzyl compound which resembles imipramine (Tofranil) in chemical structure, the difference being the same as in the above comparison. The latter two also have similar properties (fig. 1) (Vernier, 1961; Scheckel, 1963). Prior to considering clinical evaluation of these two for pre-anaesthetic medication, we wished to define clearly a few of their pharmacological properties, as reported here.

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Section: Discussionmentioning

confidence: 99%

Section: Chlorprothixenementioning

confidence: 99%

CHLORPROTHIXENE AND AMTTRIPTYLINEt: INTERACTION WITH THIOPENTONE, CIRCULATORY EFFECT AND ANTISIALOGOGUE EFFECT

Dobkin

Israel

Byles

et al. 1963

British Journal of Anaesthesia

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“…Table 2 includes a comparative summary of these three classes of neuroleptics, listing some of the common risks of antipsychotic medications [ 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 ].…”

Section: Therapeutic Usage Of Thioxanthenesmentioning

confidence: 99%

A Double-Edged Sword: Thioxanthenes Act on Both the Mind and the Microbiome

Poulsen

Dastidar²,

Roy³

et al. 2021

Molecules

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The rising tide of antibacterial drug resistance has given rise to the virtual elimination of numerous erstwhile antibiotics, intensifying the urgent demand for novel agents. A number of drugs have been found to possess potent antimicrobial action during the past several years and have the potential to supplement or even replace the antibiotics. Many of these ‘non-antibiotics’, as they are referred to, belong to the widely used class of neuroleptics, the phenothiazines. Another chemically and pharmacologically related class is the thioxanthenes, differing in that the aromatic N of the central phenothiazine ring has been replaced by a C atom. Such “carbon-analogues” were primarily synthesized with the hope that these would be devoid of some of the toxic effects of phenothiazines. Intensive studies on syntheses, as well as chemical and pharmacological properties of thioxanthenes, were initiated in the late 1950s. Although a rather close parallelism with respect to structure activity relationships could be observed between phenothiazines and thioxanthenes; several thioxanthenes were synthesized in pharmaceutical industries and applied for human use as neuroleptics. Antibacterial activities of thioxanthenes came to be recognized in the early 1980s in Europe. During the following years, many of these drugs were found not only to be antibacterial agents but also to possess anti-mycobacterial, antiviral (including anti-HIV and anti-SARS-CoV-2) and anti-parasitic properties. Thus, this group of drugs, which has an inhibitory effect on the growth of a wide variety of microorganisms, needs to be explored for syntheses of novel antimicrobial agents. The purpose of this review is to summarize the neuroleptic and antimicrobial properties of this exciting group of bioactive molecules with a goal of identifying potential structures worthy of future exploration.

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“…Chlorprothixene was first approved in the late 1950s, and clinical studies did not focus on metabolic adverse events at the time but rather on adverse effects like extrapyramidal symptoms. 1 , 14 …”

Section: Introductionmentioning

confidence: 99%

“…12,13 Chlorprothixene was first approved in the late 1950s, and clinical studies did not focus on metabolic adverse events at the time but rather on adverse effects like extrapyramidal symptoms. 1,14 1.1 | Aims of the study Given the potential for cardiometabolic adverse events with chlorprothixene due to its pharmacological properties, further studies on the cardiometabolic safety of chlorprothixene are warranted. Our aim was therefore to assess the risk of diabetes, major cardiovascular events and mortality with off-label, low-dose use of chlorprothixene, by using Danish nationwide registers and comparing with off-label, low-dose use of the commonly used second-generation antipsychotic quetiapine.…”

Section: Introductionmentioning

confidence: 99%

Use of chlorprothixene and the risk of diabetes and major adverse cardiovascular events: A nationwide cohort study

Wagner

Wesselhoeft

Andersen

et al. 2022

Basic Clin Pharma Tox

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Chlorprothixene is commonly used off-label in low doses for sedative-hypnotic purposes although it might carry a risk of cardiometabolic adverse events due to its pharmacodynamic profile. We investigated the risk of diabetes and major adverse cardiovascular events (MACE) with use of low-dose chlorprothixene, compared with use of low-dose quetiapine in a nationwide cohort study, including all new users of low-dose chlorprothixene (n = 81 328) and low-dose quetiapine (n = 91 163) in Denmark 2000-2017. Main outcomes were diabetes and MACE (myocardial infarction, stroke and death from cardiovascular causes). The association between cumulative dose of chlorprothixene and the outcomes was tested in a case-control analysis. Low-dose chlorprothixene use was associated with increased risk of diabetes (intention-to-treat [ITT]-hazard ratio [HR]: 1.16; 95% CI: 1.08-1.25), compared with low-dose quetiapine use. This association strengthened when follow-up was restricted to time on treatment (as-treated [AT]-HR: 1.34; 95% CI: 1.14-1.56). Low-dose chlorprothixene use was also associated with increased risk of MACE (ITT-HR: 1.12; 95% CI: 1.04-1.21) and stroke (ITT-HR: 1.21; 95% CI: 1.06-1.37) but not with myocardial infarction (ITT-HR: 1.11; 95% CI: 0.95-1.30) nor death from cardiovascular causes (ITT-HR: 1.07; 95% CI: 0.96-1.20). Cumulative dose of chlorprothixene ≥6000 mg was associated with increased risk of diabetes (OR:1.15-1.63; test for trend: p < 0.001), whereas cumulative dose of chlorprothixene ≥1500 mg was associated with increased risk of MACE (OR: 1.10-1.85; test for trend: p < 0.001). In conclusion, low-dose chlorprothixene use is associated with increased risk of cardiometabolic adverse events compared with low-dose quetiapine use.

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Chlorprothixene (?Truxal?) compared to chlorpromazine

Cited by 16 publications

References 1 publication

CHLORPROTHIXENE AND AMTTRIPTYLINEt: INTERACTION WITH THIOPENTONE, CIRCULATORY EFFECT AND ANTISIALOGOGUE EFFECT

CHLORPROTHIXENE AND AMTTRIPTYLINEt: INTERACTION WITH THIOPENTONE, CIRCULATORY EFFECT AND ANTISIALOGOGUE EFFECT

A Double-Edged Sword: Thioxanthenes Act on Both the Mind and the Microbiome

Use of chlorprothixene and the risk of diabetes and major adverse cardiovascular events: A nationwide cohort study

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