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Active ingredient: Chlorpromazine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Antipsychotics
  • Antiemetics
  • Dopamine Antagonists
  • Phenothiazines

Dosage Forms

  • Drops
  • Liquid
  • Solution
  • Syrup
  • Tablet

Brands / Synonyms

Aminazin; Aminazine; Ampliactil; Chlorderazin; Chlorpromados; Chlorpromanyl-20; Chlorpromanyl-40; Chlorpromazine; Chlorpromazine Hydrochloride Intensol; Contomin; Fenactil; Fenaktyl; Largactil; Largactil Liquid; Largactil Oral Drops; Novo-Chlorpromazine; Thorazine; Thorazine Spansule

Indications

For the treatment of schizophrenia, control nausea and vomiting, For relief of restlessness and apprehension before surgery, adjunct in the treatment of tetanus, control the manifestations of the manic type of manic-depressive illness.

Pharmacology

Chlorpromazine is a psychotropic agent indicated for the treatment of schizophrenia. It also exerts sedative and antiemetic activity. Chlorpromazine has actions at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Chlorpromazine has strong antiadrenergic and weaker peripheral anticholinergic activity; ganglionic blocking action is relatively slight. It also possesses slight antihistaminic and antiserotonin activity.

Mechanism of Action

Chlorpromazine acts as an antagonist (blocking agent) on different postsysnaptic receptors -on dopaminergic-receptors (subtypes D1, D2, D3 and D4 - different antipsychotic properties on productive and unproductive symptoms), on serotonergic-receptors (5-HT1 and 5-HT2, with anxiolytic, antidepressive and antiaggressive properties as well as an attenuation of extrapypramidal side-effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation difficulties), on histaminergic-receptors (H1-receptors, sedation, antiemesis, vertigo, fall in blood pressure and weight gain), alpha1/alpha2-receptors (antisympathomimetic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism - controversial) and finally on muscarinic (cholinergic) M1/M2-receptors (causing anticholinergic symptoms like dry mouth, blurred vision, obstipation, difficulty/inability to urinate, sinus tachycardia, ECG-changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side-effects). Additionally, Chlorpromazine is a weak presynaptic inhibitor of Dopamine reuptake, which may lead to (mild) antidepressive and antiparkinsonian effects. This action could also account for psychomotor agitation and amplification of psychosis (very rarely noted in clinical use).

Absorption

Not Available

Toxicity

Agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, restlessness

Biotrnasformation / Drug Metabolism

Not Available

Contraindications

Do not use in patients with known hypersensitivity to phenothiazines. Do not use in comatose states or in the presence of large amounts of central nervous system depressants (alcohol, barbiturates, narcotics, etc.).

Drug Interactions

The concurrent use of two or more drugs with anticholinergic activity--such as an antipsychotic drug (eg, chlorpromazine), an antiparkinsonian drug (eg, trihexyphenidyl), and/or a tricyclic antidepressant (eg, amitriptyline)--commonly results in excessive anticholinergic effects, including dry mouth and associated dental complications, blurred vision, and, in patients exposed to high temperature and humidity, hyperpyrexia.

Interactions may also occur with the following: anti-depressants/anti-anxiety drugs, drugs used to treat an overactive thyroid, beta-blockers (e.g., propranolol), sparfloxacin, grepafloxacin, guanethidine, guanadrel, metrizamide, cabergoline, lithium, narcotic pain medication (e.g., codeine), drugs used to aid sleep, drowsiness-causing antihistamines (e.g., diphenhydramine), any other drugs that may make you drowsy.

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