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General Description:

Tiapride, identified by CAS number 51012-32-9, is a notable compound with significant therapeutic applications. Tiapride is a selective D2 and D3 dopamine receptor blocker in the brain.

Indications:

This drug is primarily indicated for: Tiapride is indicated for the treatment of a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Tiapride undergoes metabolic processing primarily in: Tiapride is minimally metabolized in humans, 70 % of the drug is eliminated in unchanged form in the urine within 24 hours. Only low concentration of N-desethyl tiapride and tiapride N-oxide and no phase II metabolites were detected. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Tiapride are crucial for its therapeutic efficacy: The bioavailability of tiapride is approximately 75 percent. It has a Tmax is 0.4-1.5 hours and Tss is 24-48 hours with 3 time daily dosing. Benzamide and its derivatives are highly water-soluble but known to cross the blood-brain barrier, necessitating carrier-mediated transport. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Tiapride is an important consideration for its dosing schedule: 2.9–3.6 hours. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Tiapride exhibits a strong affinity for binding with plasma proteins: Negligible. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Tiapride from the body primarily occurs through: Urine (70% as unchanged tiapride). Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Tiapride is distributed throughout the body with a volume of distribution of: Tiapride distributes rapidly and exhibits virtually no binding to plasma proteins, giving it a relatively high volume of distribution. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Tiapride is a critical factor in determining its safe and effective dosage: 16.6 l/h. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Tiapride exerts its therapeutic effects through: Tiapride has a high degree of regional selectivity for limbic areas. One study found that tiapride shows over three times as much affinity for limbic areas than striatal areas as opposed to the near equal selectivity for limbic and striatal regions shown by haloperidol. Another study in rats found tiapride's affinity for the septum, a limbic region, to be over thirty times as high as for the striatum. Efficacy at the D2 receptor is moderate, with 80 percent of receptors occupied even in the presence of excess tiapride concentrations. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Tiapride functions by: Tiapride is a selective dopamine D2 and D3 receptor antagonist, offering an advantage over other neuroleptic drugs, such as haloperidol and risperidone, which bind a range of targets including four of the five known dopamine receptor subtypes (D1-4), serotonin (5-HT2A, 2C), α1- and α2-adrenergic, and histamine H1 receptors. Compared to these drugs, tiapride has a relatively moderate affinity for its target receptors, displacing 50 percent of 3H-raclopride binding at a concentration of 320 nM at D2 receptors and a concentration of 180 nM at D3 receptors. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Classification:

Tiapride belongs to the class of organic compounds known as benzenesulfonyl compounds. These are aromatic compounds containing a benzenesulfonyl group, which consists of a monocyclic benzene moiety that carries a sulfonyl group, classified under the direct parent group Benzenesulfonyl compounds. This compound is a part of the Organic compounds, falling under the Benzenoids superclass, and categorized within the Benzene and substituted derivatives class, specifically within the Benzenesulfonyl compounds subclass.

Categories:

Tiapride is categorized under the following therapeutic classes: Acids, Carbocyclic, Amines, Antipsychotic Agents, Benzamides and benzamide derivatives, Benzene Derivatives, Benzoates, Central Nervous System Agents, Central Nervous System Depressants, Dopamine Agents, Dopamine Antagonists, Dopamine D2 Receptor Antagonists, Drugs that are Mainly Renally Excreted, Ethylamines, Nervous System, Neurotoxic agents, Neurotransmitter Agents, Psycholeptics, Psychotropic Drugs, Tranquilizing Agents. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.