Chlorprothixene

ATC CodeN05AF03
CAS number113-59-7
PUB number667467
Drugbank IDDB01239
Empirical formulaC18H18ClNS
Molar mass (g·mol−1)315,86
Physical statesolid
Melting point (°C)97,5

Basics

Chlorprothixene is a typical antipsychotic from the group of thioxanthenes. The main indications of chlorprothixene are the treatment of psychotic disorders (e.g. schizophrenia) and acute mania in the context of bipolar disorders. Other indications include pre- and postoperative states of anxiety and insomnia, severe nausea/vomiting (in hospitalized patients), improvement of anxiety and agitation due to the use of selective serotonin reuptake inhibitors in depression, and, off-label, for the improvement of alcohol and opioid withdrawal.

Pharmacology

Pharmacodynamics

Chlorprothixene blocks postsynaptic dopaminergic D1 and D2 receptors and, with weaker affinity, serotonin histamine and adrenergic receptors, in the brain. Thus it has sedative, antipsychotic and antidepressant effects. Furthermore, it suppresses the release of hypothalamic and pituitary hormones and is thought to suppress the reticular activating system, thereby affecting basal metabolic rate, body temperature, wakefulness, vasomotor tone, and vomiting.

Pharmacokinetics

The half-life is approximately 8 hours.

Drug Interactions

  • Chlorprothixene may increase plasma levels of concomitantly administered lithium.
  • When chlorprothixene is administered concomitantly with opioids, the opioid dose should be reduced (by approximately 50%) because chlorprothixene significantly potentiates the therapeutic effects and side effects of opioids.
  • The concomitant use of chlorprothixene and tramadol should be avoided. Seizures may occur with this combination.
  • Additive sedative effects and confusional states are to be expected when chlorprothixene is given together with benzodiazepines or barbiturates.
  • Particular caution should be exercised when chlorprothixene is combined with other anticholinergic drugs (tricyclic antidepressants and antiparkinsonian agents): delirium, high fever, severe constipation up to ileus and glaucoma may occur, especially in the elderly.

Toxicity

Side effects

Chlorprothixene has a strong sedative effect with a high incidence of anticholinergic side effects.

Possible side effects:

  • Dry mouth
  • massive hypotension
  • tachycardia
  • hyperhidrosis
  • significant weight gain
  • severe constipation
  • difficulty urinating
  • confusion
  • constipation

Toxicological data

LD50 (rat, oral): 200 mg-kg-1

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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