MSOP1016 Science of Medicines 3 Quiz
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Questions and Answers

What is the main difference between barbiturates and benzodiazepines?

  • Benzodiazepines have a wider range of structural variations than barbiturates. (correct)
  • Benzodiazepines have longer half-lives than barbiturates.
  • Barbiturates have faster absorption rates than benzodiazepines.
  • Barbiturates are more effective as anti-anxiety drugs compared to benzodiazepines.

What was the unexpected rearrangement observed during the development of Chlorodiazepoxide?

  • Formation of a 7-ring structure instead of the intended 6-ring structure. (correct)
  • Introduction of a basic nitrogen despite Sternbach's advice.
  • Conversion of an aromatic ring to a non-aromatic ring.
  • Loss of tranquilizer activity after modification.

Which modification made Diazepam more potent than Chlorodiazepoxide?

  • Introduction of an active metabolite.
  • Removal of the basic nitrogen. (correct)
  • Change from 6-ring to 7-ring structure.
  • Addition of basic nitrogen as suggested by Sternbach.

In the SAR of Benzodiazepines, what substituent at position 3 is considered unfavorable for activity?

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

What is the role of Ring C in the SAR of Benzodiazepines?

<p>Planarity with respect to Ring A is unnecessary. (C)</p> Signup and view all the answers

Which active metabolite has the longest half-life among Temazepam, Diazepam, and Nordazepam?

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

What is the primary classification criteria used for barbiturates?

<p>'Long' acting for anti-seizure purposes (A)</p> Signup and view all the answers

How did Sternbach's approach differ from other benzodiazepine developers in the 1950s?

<p>'Basic groups are essential for biological activity' (A)</p> Signup and view all the answers

'Soporific' is best described as:

<p>'A drug inducing drowsiness or sleep' (A)</p> Signup and view all the answers

'Stereochemistry' in relation to benzodiazepines primarily involves:

<p>'Formation of enantiomeric conformations' (B)</p> Signup and view all the answers

Which enantiomer of escitalopram inhibits the serotonin transporter (SERT) twice as much as (±)-citalopram?

<p>S-enantiomer (D)</p> Signup and view all the answers

Which enantiomer is reported to be 27 times more potent than the other in the context of serotonin reuptake?

<p>S-enantiomer (D)</p> Signup and view all the answers

What type of substitution was made in derivatives of Talopram to convert it into a selective serotonin reuptake transporter (SERT) inhibitor?

<p>Isosteric substitution of isobenzofuran ring with isothiobenzophene ring (D)</p> Signup and view all the answers

What was the aim of designing a drug with combined SSRI & SNRI properties that only blocked SERTs & NETs without side effects?

<p>To achieve greater efficacy by increasing norepinephrine and serotonin levels (C)</p> Signup and view all the answers

What structural modification was made in venlafaxine compared to tricyclic antidepressants (TCAs) to reduce side effects?

<p>Changing the phenyl group to a cyclohexanol group (C)</p> Signup and view all the answers

Which antidepressant has an active metabolite known as desvenlafaxine?

<p>(+)-Venlafaxine (A)</p> Signup and view all the answers

What is the metabolite of carbamazepine that is active but more toxic?

<p>10,11-epoxide (B)</p> Signup and view all the answers

Which company produces a pro-drug of carbamazepine that avoids the toxic epoxide metabolite?

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

What neurotransmitter deficiency syndromes are discussed in the text?

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

What is the mechanism of action of SSRIs like Escitalopram?

<p>Selective inhibition of serotonin reuptake (C)</p> Signup and view all the answers

Which SSRI led to the development of second-generation drugs like Citalopram and Fluoxetine?

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

What is the active enantiomer marketed as Paroxetine?

<p>(3S, 4R) (A), (3S, 4R) (C)</p> Signup and view all the answers

Which company accidentally developed talopram and talusopram as potent NSRIs?

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

What modification was made to Z-Zimelidene to obtain Citalopram?

<p>+5-cyano addition to phthalan ring (A)</p> Signup and view all the answers

"Phenobarbital" and "Phenytoin" share structural features with which other drug mentioned in the text?

<p>&quot;Carbamazepine&quot; (A)</p> Signup and view all the answers

Which group of drugs was replaced by benzodiazepines due to safety concerns such as tolerance, dependence, and potential for abuse?

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

What was the most common adverse drug reaction associated with anti-seizure drugs that led to the discontinuation of its clinical use?

<p>Acute liver failure (B)</p> Signup and view all the answers

Which drug family is no longer used for absence seizures as it was found to worsen the condition?

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

What property of Phenytoin makes its absorption erratic when administered intramuscularly?

<p>Poor water solubility (D)</p> Signup and view all the answers

Which anti-seizure drug is administered orally and is completely ionized at physiological pH, with its anion being the active form?

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

In anti-seizure drugs, which compound was discovered to have anti-seizure properties serendipitously while being used as a solvent in drug testing?

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

What is the primary mechanism of action of Clonazepam among anti-seizure drugs?

<p>Agonist of GABAA receptor (A)</p> Signup and view all the answers

Which anti-seizure drug has the highest affinity among benzodiazepines for the GABAA receptor?

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

Which anti-seizure drug is considered the 'underdog' due to a surprising lack of promotion by manufacturers despite its effectiveness in specialist clinics?

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

What type of release does Levetiracetam have for anti-seizure treatment, specifically for partial onset, myoclonic, or tonic-clonic seizures?

<p>Both immediate and extended release options (A)</p> Signup and view all the answers

Which class of drugs is known for their efficacy in treating anxiety disorders?

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

When was the first benzodiazepine developed?

<p>1960s (A)</p> Signup and view all the answers

Which drug class has much less side effects compared to barbiturates?

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

Which drug is classified as an anxiolytic and hypnotic?

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

What is the mechanism of action of benzodiazepines?

<p>Act as allosteric modulators (C)</p> Signup and view all the answers

Which substance was first marketed and clinically used in the 1960s?

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

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