40 Questions
What is the likely mechanism of tolerance development with BZDs?
Down regulation of receptors
What is the primary effect of Flumazenil on the CNS?
Blocks the action of BZDs and BZD-like drugs
What is the consequence of dependence on BZDs?
An altered physiological state that requires continuous administration of the drug to prevent withdrawal symptoms
What is the primary use of Flumazenil in clinical practice?
Prevention of respiratory and cardiac depression
What is the time frame for the development of withdrawal symptoms with long-acting BZDs?
2-3 weeks after stopping the drug
What is the primary consequence of BZD overdose in the presence of alcohol or other CNS depressants?
Life-threatening respiratory depression
Which of the following is a common side effect of BZDs that can affect job performance?
Drowsiness, confusion, and impaired coordination
Why are long-acting BZDs not used as hypnotics to treat sleep disorders?
Due to their 'hangover' effect
What is a major concern when prescribing BZDs to patients with underlying respiratory and cardiovascular diseases?
Worsening of underlying disease conditions
What is the mechanism by which Flumazenil counteracts BZD toxicity?
By antagonizing BZD effects
What is the primary reason why BZDs are highly lipid soluble and accumulate in body fat?
Due to their high protein binding ability
Which of the following BZDs is directly metabolized to an inactive glucouronide conjugate?
Oxazepam
What is the primary advantage of using short-acting BZDs as hypnotics?
They do not cause hangover effects
What is the primary reason why BZDs are relatively safe during acute overdose?
Due to their ability to cross the blood-brain barrier
What is the primary mechanism of tolerance and dependence to BZDs?
As a result of the accumulation of active metabolites
What is the primary mechanism by which BZD acts on GABAA receptors?
By binding to a regulatory site and acting allosterically
What is the consequence of BZD binding to GABAA receptors?
Facilitation of the opening of Cl- channels
Which of the following BZD is classified as ultra-short acting?
Triazolam
What is the purpose of modifying the four main substituent groups in the basic chemical structure of BZD?
To retain activity without loss of pharmacological effect
What is the selectivity of BZD action?
Acting only on GABAA receptors
What is the primary effect of sedative and hypnotic agents on the nervous system?
Depressing the function of the nervous system
Why can one CNS acting drug be used to treat multiple conditions?
Because most signalling pathways in the CNS are interconnected
What is the difference between a sedative and a hypnotic?
A sedative calms the patient and reduces excitement, while a hypnotic produces drowsiness and facilitates the onset and maintenance of sleep
What is a common feature of CNS acting drugs in terms of their clinical use?
They can be used to treat multiple conditions and/or several types of drugs can be used to treat one kind of condition
Why do patients suffering from one CNS condition often suffer from others?
Because most signalling pathways in the CNS are interconnected
Where does GABA bind to trigger chloride channel opening?
Between α and β subunits
What is the effect of binding of BZDs at the site between α and γ subunits?
Facilitated binding of GABA and opening of the chloride ion channel
Which of the following is a clinical use of BZDs for anxiety?
Acute anxiety disorders
What is the mechanism of action of barbiturates on the GABAA receptor?
They facilitate the binding of GABA to the receptor
What is a drawback of BZD use?
Tolerance and dependence
Which BZD has anti-depressant effects?
Alprazolam
What is a major concern with the use of barbiturates as hypnotics?
They have cumulative effects when given repeatedly
What is the primary clinical use of thiopental?
Inducing anesthesia
Why are barbiturates less commonly used clinically compared to BZDs?
They have a lower safety profile
What is the half-life range of barbiturates?
1-5 days
What is a pharmacological effect of barbiturates similar to BZDs?
Enhanced binding of GABA to the receptor
What is the primary advantage of using barbiturates as hypnotics?
They are effective hypnotics for insomnia
How do barbiturates affect the Cl- channel?
They enhance the opening of the Cl- channel
What is a common side effect of barbiturates similar to BZDs?
Respiratory depression
What is the primary clinical use of phenobarbital?
Treating seizure disorders
Learn about the mechanisms of tolerance and dependence on benzodiazepines, including the potential for increased metabolism and receptor down-regulation. Understand the risks of prolonged use and withdrawal symptoms.
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