Chlorprotixen, 15 mg 30 pcs

Chlorprotixene is a neuroleptic derivative of thioxanthene. It has antipsychotic, marked sedative and moderate antidepressant effect.

Antipsychotic effect of neuroleptics is associated with blockade of dopamine receptors, and possibly also blockade of 5-NT

(5-hydroxytryptamine) receptors. In vivo, chlorprotixene has a high affinity for dopamine receptors type D1 and D2. Chlorprotixene also has high affinity for 5-HT2 receptors, a1-adrenoceptors, histamine (H1) and cholinergic muscarinic receptors. The receptor binding profile of chlorprotixen is very similar to that of clozapine, but it has approximately 10 times higher affinity for dopamine receptors.

Chlorprotixen reduces or eliminates anxiety, obsessions, psychomotor agitation, anxiety, insomnia, as well as hallucinations, delusions and other psychotic symptoms. The very low incidence of extrapyramidal effects (about 1%) and tardive dyskinesia (about 0.05%) indicate that chlorprotixen can be successfully used for maintenance therapy of patients with psychotic disorders.

Low doses of chlorprotixen have an antidepressant effect, which makes the drug useful in mental disorders characterized by anxiety, depression and anxiety. Chlorprotixene therapy also reduces the severity of associated psychosomatic symptoms. Chlorprotixene is not addictive, addictive, or tolerant. In addition, chlorprotixene potentiates the effect of analgesics, has its own analgesic effect as well as antipruritic and antiemetic…

Pharmacokinetics
Absorption

When taken orally the maximum concentration in plasma is reached after about 2 hours (range 0.5-6 hours). The average bioavailability of Chlorprotixen when ingested is approximately 12% (range 5-32%).

Distribution

The apparent volume of distribution (Vd)β is approximately 15.5 L/kg. Binding to plasma proteins is over 99%.

Chlorprotixene penetrates the placental barrier.

Biotransformation

Metabolism of chlorprotixene is primarily by sulfoxidation and N-demethylation of the side chain. The hydroxylation of the ring and N-oxidation are expressed to a lesser extent. Chlorprotixene is determined in bile, indicating the presence of intestinal-hepatic circulation of the drug. Chlorprotixene metabolites lack neuroleptic activity.

Excretion

The elimination half-life is approximately 16 hours (range 4 – 33 hours). Mean systemic clearance (Cls) corresponds to approximately 1.2 L/min. Chlorprotixene is excreted with feces and urine.

In women who are breastfeeding, chlorprotixene is excreted in small amounts with milk. The maternal milk to plasma drug concentration ratio ranges from 1.2 to 2.6.

No differences in plasma concentrations or excretion rates were found between the control group and the alcohol dependent patient group, regardless of whether the latter were sober or acutely intoxicated during the study.

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Similarities