MSOP1016 Science of Medicines 3 Quiz

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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?

OH Signup and view all the answers

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

Planarity with respect to Ring A is unnecessary. Signup and view all the answers

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

Nordazepam Signup and view all the answers

What is the primary classification criteria used for barbiturates?

'Long' acting for anti-seizure purposes Signup and view all the answers

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

'Basic groups are essential for biological activity' Signup and view all the answers

'Soporific' is best described as:

'A drug inducing drowsiness or sleep' Signup and view all the answers

'Stereochemistry' in relation to benzodiazepines primarily involves:

'Formation of enantiomeric conformations' Signup and view all the answers

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

S-enantiomer 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?

S-enantiomer 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?

Isosteric substitution of isobenzofuran ring with isothiobenzophene ring 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?

To achieve greater efficacy by increasing norepinephrine and serotonin levels Signup and view all the answers

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

Changing the phenyl group to a cyclohexanol group Signup and view all the answers

Which antidepressant has an active metabolite known as desvenlafaxine?

(+)-Venlafaxine Signup and view all the answers

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

10,11-epoxide Signup and view all the answers

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

Eisal Signup and view all the answers

What neurotransmitter deficiency syndromes are discussed in the text?

Serotonin deficiency Signup and view all the answers

What is the mechanism of action of SSRIs like Escitalopram?

Selective inhibition of serotonin reuptake Signup and view all the answers

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

Zimelidine Signup and view all the answers

What is the active enantiomer marketed as Paroxetine?

(3S, 4R) Signup and view all the answers

Which company accidentally developed talopram and talusopram as potent NSRIs?

Lundbeck Signup and view all the answers

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

+5-cyano addition to phthalan ring Signup and view all the answers

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

"Carbamazepine" 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?

Barbiturates 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?

Acute liver failure Signup and view all the answers

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

Barbiturates Signup and view all the answers

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

Poor water solubility 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?

Valproic acid 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?

Valproic acid Signup and view all the answers

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

Agonist of GABAA receptor Signup and view all the answers

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

Clonazepam 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?

Clobazam 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?

Both immediate and extended release options Signup and view all the answers