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Antipsychotic Drugs - Dr. M Casely-Hayford Objectives 1

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22 Questions

What is the primary neurotransmitter implicated in psychotic behaviors such as schizophrenia?

Dopamine

What is the primary function of dopamine in the synapse?

Inhibits neuronal firing

Which class of antipsychotic drugs is associated with less extrapyramidal side effects?

Atypical

What is the neurotransmitter primarily targeted by many antipsychotic drugs?

Dopamine

Which neurotransmitter system, other than dopamine, is mentioned to be involved in the action of antipsychotic agents?

Serotonin

What is the term used to refer to side effects like tremors and anxiety that are less common with atypical antipsychotic drugs?

Extrapyramidal side effects (EPS)

What is the Chlorpromazine Index (CI) used for in the context of the text?

To determine the optimal position of X on the phenyl ring

Why do phenothiazines need to have a 3-carbon chain between position 10 and the amino nitrogen for antipsychotic activity?

To promote proper receptor attachment

Which substitution on the ring in phenothiazines lacks antipsychotic efficacy?

-H at position 2

How does the Z isomer differ from the E isomer in thioxanthene compounds?

The Z isomer has a better 3-D structure to fit the receptor site

What does maintaining an effective size of the tertiary amino group on the side sidechain help achieve?

Activity enhancement by chain extension

Why do thiothexene compounds display properties similar to piperazine sub-group of phenothiazines?

As they share similar pharmacological properties with phenothiazines

What is the main mechanism of action for phenothiazines as antipsychotic drugs?

Acting as dopamine D2 receptor antagonists

How does the two carbon distance between the anionic site and the ring site in receptor binding of phenothiazines occur?

Through molecular bending of the side chain

What is the function of X, the electron withdrawing group in ring 'A' of phenothiazines?

Enhances binding to an electron rich area on the receptor

What does the Chlorpromazine Index (CI) indicate in terms of potency?

CI greater than 1 indicates more potency than chlorpromazine

Why does substitution at C1 have a deleterious effect on antipsychotic activity?

It prevents molecular bending

Which pharmacophoric group of norepinephrine interacts with the receptor similarly to phenothiazines?

$CO_2^-$ group

In receptor binding, what is the role of the sulfur atom at position 5 in phenothiazines?

Enhances receptor binding similar to a hydroxyl group in dopamine

How do electron withdrawing groups affect phenothiazine activity?

$\delta+$ charge on 'A' ring increases binding to electron-rich areas on receptors

Why is more than one substitution on the ring system detrimental to phenothiazine potency?

$\pi$-electron cloud gets disrupted

'The side chain in phenothiazines creates a two carbon distance between which sites in receptor binding?'

'A' ring and nitrogen site

Learn about the drugs used to treat schizophrenia, how antipsychotic drugs are classified, and gain detailed knowledge of antipsychotic drugs and their structural activity relationships. Explore neuroleptics and their role in treating psychotic behaviors like delusions, hallucinations, and aggressive behavior.

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