What are phenothiazine derivatives?

What are phenothiazine derivatives?

Examples of phenothiazines include: chlorpromazine (brand name: Thorazine), fluphenazine (Duraclon), mesoridazine (Serentil), perphenazine (Etrafon and Trilafon), prochlorperazine (Compazine), promazine (Robinul and Anectine), thioridazine (Mellaril), trifluoperazine (Stelazine) and triflupromazine (Robinul).

What do neuroleptic drugs do?

Neuroleptics, also known as antipsychotic medications, are used to treat and manage symptoms of many psychiatric disorders. They fall into two classes: first-generation or “typical” antipsychotics and second-generation or “atypical” antipsychotics.” Neuroleptic drugs block dopamine receptors in the nervous system.

What is a butyrophenone used for?

A butyrophenone derivative and dopamine antagonist used to prevent and treat postoperative nausea and vomiting. An antipsychotic agent used to treat schizophrenia and other psychoses, as well as symptoms of agitation, irritability, and delirium.

Which of the following is a butyrophenone?

Examples of butyrophenone-derived pharmaceuticals include: Haloperidol, the most widely used classical antipsychotic drug in this class. Benperidol, the most potent commonly used antipsychotic (200 times more potent than chlorpromazine) Droperidol, Antiemetic for postoperative nausea and vomiting.

What does derivative mean in drugs?

A derivative is a drug that is made from another drug.

How will you prepare phenothiazine?

In preparing phenothiazine by the present method sulphur is heated together with an excess of diphenylamine to a temperature at which the mixture reacts to evolve hydrogen sulphide.

Is Lithium a neuroleptic?

There are some cases of NMS associated with the use of non-neuroleptic drugs, like carbamazepine6 and metoclopramide,7 or drugs without known antidopaminergic activity, such as lithium. Lithium is a first-line mood stabilizer used in the treatment and prophylaxis of bipolar disorder.

Is haloperidol a Butyrophenone?

Butyrophenones. Haloperidol and droperidol are butyrophenones with antipsychotic effects used in the treatment of psychosis and agitation associated with schizophrenia and mania. They have antiemetic properties as dopamine-2 receptor antagonist (Table 25.1).

What is the most powerful antipsychotic?

Clozapine, which has the strongest antipsychotic effect, can cause neutropenia. A problem in the treatment of schizophrenia is poor patient compliance leading to the recurrence of psychotic symptoms.

Why are derivatives prepared?

Chemical derivatives may be used to facilitate analysis. A crystalline derivative may be prepared, such as a semicarbazone or 2,4-dinitrophenylhydrazone (derived from aldehydes or ketones), as a simple way of verifying the identity of the original compound, assuming that a table of derivative MP values is available.

What is derivatives in pharmaceutical industry?

Cellulose derivatives are extensively used for thickening of pharmaceutical solutions and disperse systems such as emulsions and suspensions (Adibkia et al., 2007a, 2007b). Furthermore, these polymers can increase viscosity of non-aqueous pharmaceutical solution likes organic-based coating solutions.

How do thioxanthenes work?

Thioxanthenes work primarily by blocking postsynaptic dopamine-mediated neurotransmission by binding to dopamine (DA-1 and DA-2) receptors.

What is the bioavailability of thioxanthenes?

Thioxanthenes are readily but incompletely absorbed due to first-pass metabolism in the gut wall. Oral bioavailability ranges from 40% to 50%. Peak absorption occurs in 1 or 2 h.

What is the volume of thioxanthenes in urine?

Thioxanthenes are widely distributed throughout the body, including the central nervous system (CNS). They are highly protein bound (>99%), with a volume of distribution ranging from 11 to 23 l kg −1. The main metabolites are excreted in both the urine and feces.

What are the contraindications for thioxanthenes?

Thioxanthenes are contraindicated in conditions such as blood dyscrasias, bone marrow depression, circulatory collapse, central nervous system depression, and comatose states. Douglas J. Borys, in Encyclopedia of Toxicology (Second Edition), 2005