Chlorprothixene

(Z ) -3 - ( 2-chloro- 9H- thioxanthen -9- ylidene )-N, N- dimethylpropane - 1-amine

N05AF03

Antipsychotic

97.5 ° C

Risk

• 200 mg · kg -1 ( LD50, rat, oral)
• 56.2 mg · kg -1 ( LD50, mouse, ip)

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Chlorprothixene is a low potent antipsychotic medication from the group of thioxanthenes. It is in the form of tablets, oral solutions or inject used to treat anxiety and agitation with special mental and spiritual diseases and conditions that are characterized by abnormally elevated mood and drive. Since chlorprothixene can alleviate physical stress states it is administered in chronic pain in some cases as a second-line in addition to analgesics. Ultimately, it can be used against nausea.

History

Chlorprothixene was introduced in 1959 on the German market under the name Truxal.

Effect

Chlorprothixene has a very broad spectrum of action. It has a sedative effect primarily antipsychotic in higher doses, anti-emetic, local anesthetic, ganglienblockierend, anticholinergic, antihistaminic and antiadrenerg. The effect is due to the post-synaptic blockade of dopamine D1 - and D2 -, 5 -HT2, alpha -1, H1, and muscarinic receptors. Chlorprothixene also acts as FIASMA ( functional inhibitors of acid sphingomyelinase ).

Indication

Possible indications are agitated or anxious - depressive syndrome usually in the context of psychotic or bipolar disorders. In contrast to Germany chlorprothixene in Switzerland has also a specific and official indication for the treatment of anxiety, agitation and aggression in alcoholics and Toxikomanen and for concomitant medication for chronic pain.

Contraindications

Chlorprothixene may not be used in known hypersensitivity thioxanthenes and in conditions of deep unconsciousness ( coma ). In the presence of morbidly sad upset (endogenous depression) should be used with caution chlorprothixene.

Side effects

The most common side effects are peripheral autonomic effects such as anticholinergic effects through the blockade of muscarinic receptors, such as dry mouth, failure of accommodation and mydriasis with risk of glaucoma attack, constipation, micturition disorders with risk of urinary retention, tachycardia. For prolonged therapy, these effects decrease, however.

Other relevant adverse reactions may be due to the blockade of peripheral α1 -adrenoceptors, ie with orthostatic hypotension or reflex tachycardia, or by direct cardiac effect by chinidinartige properties such as conduction disturbances ( PQ-/QRS-Verbreiterung ).

Central side effects are sedation, drowsiness, delirium ( in elderly patients ), increased appetite, weight gain, sleep disorders and epileptic seizures in predisposed persons. Dyskinesias are also possible.

Poisoning

Symptoms of poisoning are similar to those of atropine poisoning, so at low doses dry mouth, dryness of the skin, easy bradycardia.

At higher doses, there is thirst, tachycardia, dilated pupils, glare sensation, photophobia, with progressive poisoning dysphagia (due to drying up of glandular function ), accommodation is no longer possible, intestinal atony, urinary retention, restlessness, confusion, mirth / crying spells, hallucinations, AV block.

In the final stage, the body temperature rises as a result of inhibition of the sweat and by the failure of the central regulation; the skin is hot, dry and red. Finally, the central excitation may turn into depression, followed by somnolence and respiratory paralysis.

Trade names

Taractan (USA), Truxal (D, CH, AT), and generic (D).