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Questions and Answers
Which adrenergic agonist works by promoting norepinephrine release, blocking norepinephrine reuptake, and inhibiting norepinephrine inactivation?
Which adrenergic agonist works by promoting norepinephrine release, blocking norepinephrine reuptake, and inhibiting norepinephrine inactivation?
- Ephedrine (correct)
- Epinephrine
- Dopamine
- Isoproterenol
Which enzyme is responsible for the metabolism of catecholamines like epinephrine and norepinephrine?
Which enzyme is responsible for the metabolism of catecholamines like epinephrine and norepinephrine?
- Amylase
- Catechol-O-methyltransferase (correct)
- Protease
- Lipase
What is the main reason that catecholamines cannot be used orally?
What is the main reason that catecholamines cannot be used orally?
- They have a brief duration of action
- They contain a catechol group and an amine group
- They cannot cross the blood-brain barrier
- They are quickly metabolized by enzymes (correct)
Which class of adrenergic agonists includes drugs like dopamine, epinephrine, isoproterenol, and ephedrine?
Which class of adrenergic agonists includes drugs like dopamine, epinephrine, isoproterenol, and ephedrine?
What is the defining feature of noncatecholamines that distinguishes them from catecholamines?
What is the defining feature of noncatecholamines that distinguishes them from catecholamines?
What is the common property shared by all catecholamines due to their chemistry?
What is the common property shared by all catecholamines due to their chemistry?
Which adrenergic agonist works on receptor binding and is considered a direct agonist?
Which adrenergic agonist works on receptor binding and is considered a direct agonist?
Why are catecholamines unable to cross the blood-brain barrier?
Why are catecholamines unable to cross the blood-brain barrier?
What differentiates noncatecholamines from catecholamines?
What differentiates noncatecholamines from catecholamines?
What is the defining characteristic of catecholamines?
What is the defining characteristic of catecholamines?
Which enzyme metabolizes catecholamines like epinephrine and norepinephrine?
Which enzyme metabolizes catecholamines like epinephrine and norepinephrine?
What is the reason that catecholamines are ineffective if given orally?
What is the reason that catecholamines are ineffective if given orally?
What causes the pigmentation of catecholamine-containing solutions over time?
What causes the pigmentation of catecholamine-containing solutions over time?
What distinguishes noncatecholamines from catecholamines in terms of metabolism?
What distinguishes noncatecholamines from catecholamines in terms of metabolism?
Which drug is highly selective, acting at B2 receptors only?
Which drug is highly selective, acting at B2 receptors only?
At low doses, which drug acts on B2 receptors only, but at high doses, it also acts on B1 and B2 receptors?
At low doses, which drug acts on B2 receptors only, but at high doses, it also acts on B1 and B2 receptors?
Which response can be elicited by the activation of A1 receptors in blood vessels?
Which response can be elicited by the activation of A1 receptors in blood vessels?
What is the primary adverse effect of alpha-1 receptor activation?
What is the primary adverse effect of alpha-1 receptor activation?
Activation of beta-1 receptors stimulates which organ?
Activation of beta-1 receptors stimulates which organ?
What is the therapeutic application of beta-1 agonists?
What is the therapeutic application of beta-1 agonists?
Where are beta-2 receptors primarily located?
Where are beta-2 receptors primarily located?
What effect does the activation of alpha-2 receptors in the central nervous system produce?
What effect does the activation of alpha-2 receptors in the central nervous system produce?
Which receptor subtype does epinephrine act on?
Which receptor subtype does epinephrine act on?
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Study Notes
Adrenergic Agonists
- Cocaine works by promoting norepinephrine release, blocking norepinephrine reuptake, and inhibiting norepinephrine inactivation.
Catecholamine Metabolism
- Catechol-O-methyltransferase (COMT) is responsible for the metabolism of catecholamines like epinephrine and norepinephrine.
Catecholamine Administration
- Catecholamines cannot be used orally because they are ineffective when given orally.
Classes of Adrenergic Agonists
- The class of adrenergic agonists that includes drugs like dopamine, epinephrine, isoproterenol, and ephedrine is called catecholamines.
Characteristics of Catecholamines
- The defining feature of noncatecholamines is that they are not inactivated by COMT, distinguishing them from catecholamines.
- The common property shared by all catecholamines due to their chemistry is that they are inactivated by COMT.
- The defining characteristic of catecholamines is that they are inactivated by COMT.
Pharmacology of Adrenergic Agonists
- Direct agonists work on receptor binding, and examples include epinephrine and isoproterenol.
- Catecholamines are unable to cross the blood-brain barrier due to their chemical structure.
- Noncatecholamines are differentiated from catecholamines in terms of metabolism, as they are not inactivated by COMT.
Enzymatic Metabolism
- COMT metabolizes catecholamines like epinephrine and norepinephrine.
- The reason catecholamines are ineffective when given orally is that they are metabolized by COMT.
Oxidation of Catecholamines
- The pigmentation of catecholamine-containing solutions over time is caused by oxidation.
Receptor Pharmacology
- Salbutamol is highly selective, acting at B2 receptors only.
- At low doses, salmeterol acts on B2 receptors only, but at high doses, it also acts on B1 and B2 receptors.
- The activation of A1 receptors in blood vessels can elicit vasoconstriction.
- The primary adverse effect of alpha-1 receptor activation is hypertension.
- Activation of beta-1 receptors stimulates the heart.
- The therapeutic application of beta-1 agonists is in the treatment of heart failure.
- Beta-2 receptors are primarily located in the lungs.
- The activation of alpha-2 receptors in the central nervous system produces a decrease in sympathetic tone.
- Epinephrine acts on alpha-1, alpha-2, beta-1, and beta-2 receptors.
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