18 Questions
What is one of the reasons for a long half-life of a drug in the body?
Low degree of protein binding
Why does diazepam have a long elimination half-life?
Low extraction ratio
What is the main cause for the longer elimination half-life of diazepam in some subjects?
Genetic polymorphism affecting drug clearance
Which factor contributes to the variations in diazepam metabolism among individuals?
Genetic polymorphism
In subjects who are fast metabolizers, what still contributes to the long elimination half-lives of diazepam?
Small volume of distribution
What is the impact of drug protein binding on the clearance and half-life of diazepam?
Protein binding prolongs clearance and half-life
How does a decrease in protein binding affect drug distribution?
Increases availability of drug to interact at receptor sites
What impact does an increased free drug concentration have on drug distribution?
Enhances drug crossing cell membranes
Which equation is used to relate VD, Cl, and half-life of drugs?
$\ln 2 \times \frac{D}{Cl}$
What does an increase in free drug concentration lead to in terms of pharmacologic effects?
Intensified pharmacologic effect
How does a decrease in protein binding affect the metabolism of a drug?
Increases the rate of metabolism
In pharmacokinetics, how would a lower total steady-state drug concentration but similar steady-state free drug concentration be explained?
Increased metabolism rate
What is the primary factor contributing to the loss of drug from the receptor site?
Dose rate
How can rapid IV injection affect the intensity of action of highly protein-bound drugs?
Increase the intensity of action
What was the observed effect on the hypotensive effect of diazoxide when injected rapidly IV compared to a slower injection?
Increased hypotensive effect
What was the free diazoxide serum level when the serum levels were 100 mg/mL?
20.6%
How did the slow injection of diazoxide affect its free serum level?
Decreased the free serum level
What factor contributed to the transient high free diazoxide concentration after a rapid IV injection?
Initial saturation of protein-binding sites
Test your knowledge on drug half-life and protein binding with this quiz. Learn about factors that contribute to a drug having a long half-life in the body, such as high protein binding and drug molecular properties. Explore clinical examples like diazepam to understand these concepts better.
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