Antipsychotics Overview and Mechanisms

Questions and Answers

Which statement best describes the activity of carbamates?

They possess both b1 and b2 activity. (correct)

They show degradation by monoamine oxidase (MAO).

They are equivalent to esters of dopamine.

They have no effect on CNS activity.

What is a primary effect of the ethyl substitution at R2 in carbamates?

Decreased oral activity.

Increased degradation through MAO.

Enhanced a activity.

Increased CNS activity. (correct)

What role does physostigmine play in the activity of carbamates?

It functions solely as a CNS depressant.

It enhances acetylcholine esters.

It primarily affects dopamine receptors.

It inhibits the enzyme degradation pathways. (correct)

In regards to the carbamate structure, what is the significance of the methyl substitution?

It enhances a activity. Signup and view all the answers

What is the primary source of physostigmine?

Calabar bean (Physostigma venenosum). Signup and view all the answers

Which of the following drugs is classified as having an ultrashort action?

Thiopental Signup and view all the answers

Which of the following antidepressants does NOT end with 'triptyline'?

Desipramine Signup and view all the answers

What is a common ending for long-acting benzodiazepines?

zepoxide Signup and view all the answers

Which of the following is an example of a drug classified as a secondary amine antidepressant?

Desipramine Signup and view all the answers

Which drug belongs to the short-acting category?

Secobarbital Signup and view all the answers

Which classification of drugs ends with 'zepate'?

Benzodiazepines Signup and view all the answers

Which of the following is NOT a long-acting barbiturate?

Methohexital Signup and view all the answers

Which of the following endings indicates a primary amine antidepressant?

triptyline Signup and view all the answers

Which of the following drugs is not a tertiary amine ending with 'pramine'?

Amitriptyline Signup and view all the answers

What is essential for antipsychotic activity of a tertiary amine?

Minimum of three carbon atoms separating the ring and side chain nitrogen Signup and view all the answers

Which generation of antipsychotics is characterized by low or no extrapyramidal side effects?

2nd Generation Signup and view all the answers

Which of the following is NOT a characteristic of 1st Generation antipsychotics?

Highly effective against negative symptoms Signup and view all the answers

What structural feature is considered part of the pharmacophore in antipsychotic drugs?

Tertiary amine Signup and view all the answers

Which of the following antipsychotic classes does NOT belong to the 1st Generation?

Atypicals Signup and view all the answers

Among the following, which is a primary characteristic of 1st Generation antipsychotics?

High risk of sedation Signup and view all the answers

What type of side chains are important for the activity of antipsychotic drugs?

N-containing side chain substituents Signup and view all the answers

Which statement about Famotidine is true?

It is a thiazole derivative. Signup and view all the answers

What is a characteristic of Nizatidine in relation to cimetidine?

It has a thiazole structure. Signup and view all the answers

What distinguishes proton pump inhibitors from other medications discussed?

They are prodrugs converted to sulfenamide in acid media. Signup and view all the answers

What is the primary function of sulfonylureas listed in the content?

To stimulate insulin secretion. Signup and view all the answers

Which of the following is a feature of 2nd Generation sulfonylureas?

They typically have 'Gli' or 'Gly' as a suffix. Signup and view all the answers

What is the prototype drug for proton pump inhibitors?

Omeprazole Signup and view all the answers

Which medication class includes agents referred to as 'OHAs'?

Sulfonylureas Signup and view all the answers

What class of drugs includes agents that are mainly characterized as 'rapid-acting' and 'long-acting'?

Insulins Signup and view all the answers

What is the primary function of biguanides in diabetes management?

Increasing insulin sensitivity Signup and view all the answers

Which of the following are examples of long-acting insulins?

Glargine and Detemir Signup and view all the answers

Which category includes both Sulfonylureas and Meglitinides?

Insulin Secretagogues Signup and view all the answers

Which of the following drugs is a Dipeptidyl – Peptidase – 4 Inhibitor?

Linagliptin Signup and view all the answers

What type of diuretic is Manitol classified as?

Osmotic Diuretic Signup and view all the answers

Which of the following is not a biguanide?

Thiazolidinedione Signup and view all the answers

Which of the following insulin types is classified as short-acting?

Regular insulin Signup and view all the answers

Which of the following is considered a Thiazolidinedione?

Troglitazone Signup and view all the answers

Study Notes

Tertiary Amine

Ends with “pramine” except Amitriptyline and Doxepin.
Examples include Amitriptyline, Doxepin, Imipramine, Clomipramine, and Trimipramine.
Essential for antipsychotic activity.
Substitution at position X (at 2) with electron-withdrawing groups (ENG) enhances activity.
Halogens are good for electron withdrawal.
Requires a nitrogen-containing side chain for effective antipsychotic activity.
The ring nitrogen and side chain nitrogen must be separated by at least three carbon atoms to maintain antipsychotic effects; two carbon separation leads to antihistaminic/anticholinergic effects.

Generations of Antipsychotics

1st Generation (Typical)
- Common ADRs: Sedation, Extrapyramidal symptoms (EPS).
- Includes phenothiazines (Aliphatic like Promazine, Piperazine like Perazine, Piperidine like Ridazine), Thioxanthenes (Thixene), and Butyrophenones (Peridol).
2nd Generation (Atypical)
- Diverse classes with low to no EPS.
- Example: Aripiprazole.

Opioid Design and SAR

Classification based on duration of action:
- Ultrashort: Thiopental, Thiamylal, Methohexital.
- Short: Pentobarbital, Secobarbital.
- Intermediate: Amobarbital, Butabarbital.
- Long: Phenobarbital, Mephobarbital, Methabarbital.

Antidepressant Classification

Secondary Amines
- Ends with “triptyline” except Desipramine and Amoxapine.
- Examples: Desipramine, Nortriptyline, Protriptyline, Amoxapine.
Carbamates
- Active against acetylcholinesterase.
- Physostigmine derived from Calabar bean.
- Intermediate acting; influences MAO degradation.

H2 Blockers

Used for anti-ulcer treatment, ending with "-tidine".
Examples: Nizatidine (5-18x more potent than cimetidine).

Proton Pump Inhibitors

Substituted benzimidazole compounds.
All prodrugs, converted to sulfenamide in acid media.
Omeprazole serves as the prototype drug.

Hypoglycemic Agents

Insulin classifications:
- Rapid-acting (Lispro, Aspart, Glulisine).
- Short-acting (Regular insulin).
- Intermediate-acting (NPH, Insulin Zn Suspension).
- Long-acting (Glargine, Detemir).
Oral Hypoglycemic Agents (OHAs) include Insulin Secretagogues (Sulfonylureas) and Insulin Sensitizers (Biguanides, Thiazolidinediones).

Cardiovascular Drugs

Carbonic Anhydrase Inhibitor
- Example: Acetazolamide (contains unsubstituted sulfonamide structure).

Osmotic Diuretics

Mannitol is an intravenous osmotic diuretic, chemically composed of hydroxyl groups.

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Description

This quiz covers the details of tertiary amines and their significance in antipsychotic medication. It explores the generations of antipsychotics, their common side effects, and mechanisms of action. Test your knowledge on the pharmacology of these crucial psychiatric treatments!