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Questions and Answers
Which receptor do alpha-2 adrenergic receptor agonists selectively bind to?
Which receptor do alpha-2 adrenergic receptor agonists selectively bind to?
- Serotonin receptors
- Beta-1 adrenergic receptors
- Dopamine receptors
- Alpha-2 adrenergic receptors (correct)
Where are most alpha-2 receptors located?
Where are most alpha-2 receptors located?
- Central nervous system (CNS) (correct)
- Enteric nervous system (ENS)
- Autonomic nervous system (ANS)
- Peripheral nervous system (PNS)
What can peripheral alpha-2 receptor inhibition affect?
What can peripheral alpha-2 receptor inhibition affect?
- Promote adrenaline release from the adrenal medulla
- Insulin release and induce glucagon from the pancreas (correct)
- Inhibit cortisol production from the adrenal glands
- Affect dopamine release in the brain
What are the clinical effects of alpha-2 adrenergic receptor agonists?
What are the clinical effects of alpha-2 adrenergic receptor agonists?
What is the mechanism of action of alpha-2 adrenergic receptor agonists?
What is the mechanism of action of alpha-2 adrenergic receptor agonists?
What can withdrawal from even short-term use of alpha-2 adrenergic receptor agonists trigger?
What can withdrawal from even short-term use of alpha-2 adrenergic receptor agonists trigger?
Where do centrally-acting alpha-2 agonists spread throughout?
Where do centrally-acting alpha-2 agonists spread throughout?
Which drug is primarily excreted unchanged in the urine and has a terminal half-life of approximately 12-16 hours?
Which drug is primarily excreted unchanged in the urine and has a terminal half-life of approximately 12-16 hours?
Which drug is known for its selective alpha 2 receptor potency with a preference ratio of 1,600:1 for alpha 2 receptors over alpha 1 receptors?
Which drug is known for its selective alpha 2 receptor potency with a preference ratio of 1,600:1 for alpha 2 receptors over alpha 1 receptors?
Which drug is commonly used in the ICU and OR as a sedative and analgesic due to its central sympatholytic effects?
Which drug is commonly used in the ICU and OR as a sedative and analgesic due to its central sympatholytic effects?
Which drug has dose-dependent reductions in heart rate and blood pressure and is clinically used for treating resistant hypertension, tremors associated with central stimulant medications, and opioid withdrawal?
Which drug has dose-dependent reductions in heart rate and blood pressure and is clinically used for treating resistant hypertension, tremors associated with central stimulant medications, and opioid withdrawal?
Which drug has a loading dose of 0.5-1 mcg/kg over 10 minutes and an infusion range of 0.2-0.7 mcg/kg/hr, with an onset of 5-10 minutes and an offset of 30-60 minutes?
Which drug has a loading dose of 0.5-1 mcg/kg over 10 minutes and an infusion range of 0.2-0.7 mcg/kg/hr, with an onset of 5-10 minutes and an offset of 30-60 minutes?
Which drug is known for its potent and highly selective action for alpha 2 receptors, with a preference ratio of 1,620:1, and has a higher affinity for alpha 2 receptors than clonidine?
Which drug is known for its potent and highly selective action for alpha 2 receptors, with a preference ratio of 1,620:1, and has a higher affinity for alpha 2 receptors than clonidine?
Which drug can lead to physiological dependence, resulting in withdrawal symptoms such as tachycardia, hypertension, and anxiety after just a few days of administration?
Which drug can lead to physiological dependence, resulting in withdrawal symptoms such as tachycardia, hypertension, and anxiety after just a few days of administration?
Which drug has a relatively short terminal elimination half-life of 2 hours and is primarily administered intravenously as an infusion?
Which drug has a relatively short terminal elimination half-life of 2 hours and is primarily administered intravenously as an infusion?
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Study Notes
Alpha-2 Adrenergic Receptor Agonists
- Alpha-2 adrenergic receptor agonists selectively bind to alpha-2 receptors.
- Most alpha-2 receptors are located in the pancreas, kidney, and adipose tissue.
Peripheral Effects
- Peripheral alpha-2 receptor inhibition can affect insulin secretion, sodium reabsorption, and lipolysis.
Clinical Effects
- Alpha-2 adrenergic receptor agonists can cause sedation, analgesia, and a decrease in sympathetic outflow, leading to decreased blood pressure and heart rate.
Mechanism of Action
- Alpha-2 adrenergic receptor agonists work by inhibiting the release of norepinephrine, which decreases sympathetic activity.
Withdrawal
- Withdrawal from even short-term use of alpha-2 adrenergic receptor agonists can trigger rebound hypertension, tachycardia, and anxiety.
Central Action
- Centrally-acting alpha-2 agonists spread throughout the brain, including the hypothalamus, amygdala, and brainstem.
Clonidine
- Clonidine is primarily excreted unchanged in the urine and has a terminal half-life of approximately 12-16 hours.
- It is known for its selective alpha-2 receptor potency with a preference ratio of 1,600:1 for alpha-2 receptors over alpha-1 receptors.
Dexmedetomidine
- Dexmedetomidine is commonly used in the ICU and OR as a sedative and analgesic due to its central sympatholytic effects.
- It has a loading dose of 0.5-1 mcg/kg over 10 minutes and an infusion range of 0.2-0.7 mcg/kg/hr, with an onset of 5-10 minutes and an offset of 30-60 minutes.
Guanfacine
- Guanfacine has dose-dependent reductions in heart rate and blood pressure and is clinically used for treating resistant hypertension, tremors associated with central stimulant medications, and opioid withdrawal.
Tizanidine
- Tizanidine is known for its potent and highly selective action for alpha-2 receptors, with a preference ratio of 1,620:1, and has a higher affinity for alpha-2 receptors than clonidine.
- It has a relatively short terminal elimination half-life of 2 hours and is primarily administered intravenously as an infusion.
Dependence and Withdrawal
- Alpha-2 adrenergic receptor agonists can lead to physiological dependence, resulting in withdrawal symptoms such as tachycardia, hypertension, and anxiety after just a few days of administration.
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