Podcast
Questions and Answers
What is the main difference between barbiturates and benzodiazepines?
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?
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?
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?
In the SAR of Benzodiazepines, what substituent at position 3 is considered unfavorable for activity?
What is the role of Ring C in the SAR of Benzodiazepines?
What is the role of Ring C in the SAR of Benzodiazepines?
Which active metabolite has the longest half-life among Temazepam, Diazepam, and Nordazepam?
Which active metabolite has the longest half-life among Temazepam, Diazepam, and Nordazepam?
What is the primary classification criteria used for barbiturates?
What is the primary classification criteria used for barbiturates?
How did Sternbach's approach differ from other benzodiazepine developers in the 1950s?
How did Sternbach's approach differ from other benzodiazepine developers in the 1950s?
'Soporific' is best described as:
'Soporific' is best described as:
'Stereochemistry' in relation to benzodiazepines primarily involves:
'Stereochemistry' in relation to benzodiazepines primarily involves:
Which enantiomer of escitalopram inhibits the serotonin transporter (SERT) twice as much as (±)-citalopram?
Which enantiomer of escitalopram inhibits the serotonin transporter (SERT) twice as much as (±)-citalopram?
Which enantiomer is reported to be 27 times more potent than the other in the context of serotonin reuptake?
Which enantiomer is reported to be 27 times more potent than the other in the context of serotonin reuptake?
What type of substitution was made in derivatives of Talopram to convert it into a selective serotonin reuptake transporter (SERT) inhibitor?
What type of substitution was made in derivatives of Talopram to convert it into a selective serotonin reuptake transporter (SERT) inhibitor?
What was the aim of designing a drug with combined SSRI & SNRI properties that only blocked SERTs & NETs without side effects?
What was the aim of designing a drug with combined SSRI & SNRI properties that only blocked SERTs & NETs without side effects?
What structural modification was made in venlafaxine compared to tricyclic antidepressants (TCAs) to reduce side effects?
What structural modification was made in venlafaxine compared to tricyclic antidepressants (TCAs) to reduce side effects?
Which antidepressant has an active metabolite known as desvenlafaxine?
Which antidepressant has an active metabolite known as desvenlafaxine?
What is the metabolite of carbamazepine that is active but more toxic?
What is the metabolite of carbamazepine that is active but more toxic?
Which company produces a pro-drug of carbamazepine that avoids the toxic epoxide metabolite?
Which company produces a pro-drug of carbamazepine that avoids the toxic epoxide metabolite?
What neurotransmitter deficiency syndromes are discussed in the text?
What neurotransmitter deficiency syndromes are discussed in the text?
What is the mechanism of action of SSRIs like Escitalopram?
What is the mechanism of action of SSRIs like Escitalopram?
Which SSRI led to the development of second-generation drugs like Citalopram and Fluoxetine?
Which SSRI led to the development of second-generation drugs like Citalopram and Fluoxetine?
What is the active enantiomer marketed as Paroxetine?
What is the active enantiomer marketed as Paroxetine?
Which company accidentally developed talopram and talusopram as potent NSRIs?
Which company accidentally developed talopram and talusopram as potent NSRIs?
What modification was made to Z-Zimelidene to obtain Citalopram?
What modification was made to Z-Zimelidene to obtain Citalopram?
"Phenobarbital" and "Phenytoin" share structural features with which other drug mentioned in the text?
"Phenobarbital" and "Phenytoin" share structural features with which other drug mentioned in the text?
Which group of drugs was replaced by benzodiazepines due to safety concerns such as tolerance, dependence, and potential for abuse?
Which group of drugs was replaced by benzodiazepines due to safety concerns such as tolerance, dependence, and potential for abuse?
What was the most common adverse drug reaction associated with anti-seizure drugs that led to the discontinuation of its clinical use?
What was the most common adverse drug reaction associated with anti-seizure drugs that led to the discontinuation of its clinical use?
Which drug family is no longer used for absence seizures as it was found to worsen the condition?
Which drug family is no longer used for absence seizures as it was found to worsen the condition?
What property of Phenytoin makes its absorption erratic when administered intramuscularly?
What property of Phenytoin makes its absorption erratic when administered intramuscularly?
Which anti-seizure drug is administered orally and is completely ionized at physiological pH, with its anion being the active form?
Which anti-seizure drug is administered orally and is completely ionized at physiological pH, with its anion being the active form?
In anti-seizure drugs, which compound was discovered to have anti-seizure properties serendipitously while being used as a solvent in drug testing?
In anti-seizure drugs, which compound was discovered to have anti-seizure properties serendipitously while being used as a solvent in drug testing?
What is the primary mechanism of action of Clonazepam among anti-seizure drugs?
What is the primary mechanism of action of Clonazepam among anti-seizure drugs?
Which anti-seizure drug has the highest affinity among benzodiazepines for the GABAA receptor?
Which anti-seizure drug has the highest affinity among benzodiazepines for the GABAA receptor?
Which anti-seizure drug is considered the 'underdog' due to a surprising lack of promotion by manufacturers despite its effectiveness in specialist clinics?
Which anti-seizure drug is considered the 'underdog' due to a surprising lack of promotion by manufacturers despite its effectiveness in specialist clinics?
What type of release does Levetiracetam have for anti-seizure treatment, specifically for partial onset, myoclonic, or tonic-clonic seizures?
What type of release does Levetiracetam have for anti-seizure treatment, specifically for partial onset, myoclonic, or tonic-clonic seizures?
Which class of drugs is known for their efficacy in treating anxiety disorders?
Which class of drugs is known for their efficacy in treating anxiety disorders?
When was the first benzodiazepine developed?
When was the first benzodiazepine developed?
Which drug class has much less side effects compared to barbiturates?
Which drug class has much less side effects compared to barbiturates?
Which drug is classified as an anxiolytic and hypnotic?
Which drug is classified as an anxiolytic and hypnotic?
What is the mechanism of action of benzodiazepines?
What is the mechanism of action of benzodiazepines?
Which substance was first marketed and clinically used in the 1960s?
Which substance was first marketed and clinically used in the 1960s?