Benzodiazepines Overview

<p>Ramelteon (A)</p> Signup and view all the answers

<p>Zolpidem (B)</p> Signup and view all the answers

<p>CF3 (B)</p> Signup and view all the answers

<p>Di-ortho (D)</p> Signup and view all the answers

<p>Replacement of the 4,5 double bond with a single bond (B)</p> Signup and view all the answers

<p>Hydroxyl substitution at the 3 position does not affect potency. (B)</p> Signup and view all the answers

<p>Increases potency (A)</p> Signup and view all the answers

<p>Benzyl (A)</p> Signup and view all the answers

<p>They are rapidly metabolized by oxidation of the CH3 group to an alcohol followed by glucuronide formation. (D)</p> Signup and view all the answers

<p>Benzodiazepines with shorter half-lives are less likely to accumulate on multiple dosing. (A)</p> Signup and view all the answers

<p>Promotion of GABA binding (B)</p> Signup and view all the answers

<p>Sedation/hypnosis (D)</p> Signup and view all the answers

<p>Sedation and muscle relaxation (B)</p> Signup and view all the answers

<p>Management of anxiety disorders (D)</p> Signup and view all the answers

<p>They allow rapid entry into the CNS. (A)</p> Signup and view all the answers

<p>Alpha-3 (A)</p> Signup and view all the answers

<p>Zolpidem (B)</p> Signup and view all the answers

<p>Modulation of receptor affinity (C)</p> Signup and view all the answers

<p>It decreases activity. (D)</p> Signup and view all the answers

<p>An aromatic ring at the 5 position. (D)</p> Signup and view all the answers

<p>They exhibit antagonist activity. (B)</p> Signup and view all the answers

<p>Reduction of the 4,5 double bond. (B)</p> Signup and view all the answers

<p>They act as pro-drugs. (B)</p> Signup and view all the answers

<p>Small substitutions at N1 do not affect potency. (C)</p> Signup and view all the answers

<p>It will enhance the potency of the benzodiazepine. (B)</p> Signup and view all the answers

<p>It decreases potency. (D)</p> Signup and view all the answers

<p>Utilization of fused triazole and imidazole compounds. (B)</p> Signup and view all the answers

<p>It provides optimum activity. (B)</p> Signup and view all the answers

<p>Headache (D)</p> Signup and view all the answers

<p>Zaleplon (A), Zolpidem (B), Ramelteon (C), Eszopiclone (D)</p> Signup and view all the answers

<p>30% (B)</p> Signup and view all the answers

<p>6-8 hours (B)</p> Signup and view all the answers

<p>Ramelteon (B)</p> Signup and view all the answers

<p>Zaleplon (A), Eszopiclone (B), Zolpidem (C)</p> Signup and view all the answers

<p>Eszopiclone (A)</p> Signup and view all the answers

<p>CYP3A4 (D)</p> Signup and view all the answers

<p>Ramelteon (A)</p> Signup and view all the answers

<p>Amnesia (A)</p> Signup and view all the answers

<p>Anxiolytic activity (C)</p> Signup and view all the answers

<p>Diazepam (C)</p> Signup and view all the answers

<p>Promoting the binding of GABA to the GABAA receptor (B)</p> Signup and view all the answers

<p>Alpha-3 (B)</p> Signup and view all the answers

<p>Zolpidem (B)</p> Signup and view all the answers

<p>Sedation/hypnosis (C)</p> Signup and view all the answers

<p>Long half-lives are less effective for sleep disorders (C)</p> Signup and view all the answers

<p>None of the above (D)</p> Signup and view all the answers

<p>The ability to modulate chloride ion channels (C)</p> Signup and view all the answers

<p>Ro15-4513 (C)</p> Signup and view all the answers

A non-benzodiazepine sleep aid with a half-life of 2.5 hours and 6-8 hours of duration.

A non-benzodiazepine sleep medication, low bioavailability at 30%, with a half-life of 1 hour.

A non-benzodiazepine with a half-life of 6 hours, rapid absorption but delayed by food.

Melatonin receptor agonist used for sleep onset with an onset of 30 mins and bioavailability of 1.8%.

The time it takes for the concentration of a drug in the bloodstream to reduce to half its initial value.

Drugs that enhance GABA binding to GABAA receptors, leading to sedation and anxiety reduction.

A ligand-gated ion channel that allows chloride ions to enter neurons, inhibited by benzodiazepines.

The duration it takes for half of the drug to be eliminated from the body, affecting therapeutic use.

Produce sedation, decreased anxiety, anterograde amnesia, anticonvulsant effects, and muscle relaxation.

Different versions of GABAA receptors (a1, a2, a3, a5) which determine the effects of benzodiazepines.

Alpha 1 subtypes of GABAA receptors are linked to sedation and hypnosis effects of benzodiazepines.

Alpha 2 and 5 subtypes are associated with anxiety reduction from benzodiazepines.

Alpha 1, 2, and 3 subtypes may be responsible for anticonvulsant activity of benzodiazepines.

General structure for benzodiazepine compounds, essential for their function.

An electron withdrawing group is required at the 7 position to enhance potency.

An aromatic ring at the 5 position is necessary for benzodiazepine activity.

Substitution at the 6, 8, or 9 position decreases the activity of benzodiazepines.

Alkyl substitution at the 3 position decreases potency, while hydroxyl has minimal impact.

3-carboxylic acids are pro-drugs and convert to 3-H compounds in the stomach.

A 2-carbonyl structure provides optimum activity; others like 2-thione are less potent.

Midazolam, triazolam, and alprazolam show selectivity for hypnosis and anxiolytic activity, with short half-lives.

A group at the 7 position of benzodiazepines that enhances potency.

Altering the 6, 8, or 9 positions decreases the activity of benzodiazepines.

Decreasing or shifting this double bond reduces benzodiazepine potency.

This substitution has minimal effect on potency but shortens half-life.

These are pro-drugs that convert to 3-H compounds in the stomach.

A 2-carbonyl structure provides the best potency in benzodiazepines.

Small groups like H, methyl, or ethyl at N1 enhance activity whereas larger groups diminish it.

Esters are converted to less potent intermediate compounds when hydrolyzed.

A non-benzodiazepine with a half-life of 2.5 hours and a duration of 6-8 hours.

A non-benzodiazepine with 30% bioavailability and a half-life of 1 hour.

A non-benzodiazepine sleep aid with a 6-hour half-life and rapid absorption.

Melatonin receptor agonist, with an onset of 30 minutes and bioavailability of 1.8%.

The percentage of a drug bound to proteins in the blood, affecting its action.

The process by which the body breaks down substances, often to inactive metabolites.

Food can delay the absorption of several sleep medications.

Unwanted effects from medications, such as headache or amnesia.

Receptors that help regulate sleep-wake cycles and circadian rhythms.

The proportion of a drug that enters circulation and is available for action.

They enhance GABA binding to GABAA receptors, affecting neurotransmission.

The effectiveness of benzodiazepines varies with their half-lives related to specific conditions.

A ligand-gated ion channel that permits chloride ions to enter neurons.

Different alpha subtypes (a1, a2, a3, a5) influence specific benzodiazepine effects.

Sedative and hypnotic effects are primarily linked to the a1 subtype.

Alpha 2 and 5 subtypes are associated with anxiety relief effects.

a1, a2, and a3 subtypes are linked to anticonvulsant effects of benzodiazepines.

Benzodiazepines enhance chloride influx, increasing neuron inhibition.

Benzodiazepines with short half-lives are preferred for sleep disturbances.

Anticonvulsant benzodiazepines typically have long half-lives to maintain effects.