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Questions and Answers
What is the primary role of α2 receptors in the sympathetic nervous system?
What is the primary role of α2 receptors in the sympathetic nervous system?
- To stimulate the release of norepinephrine
- To enhance sympathetic activity
- To bind exclusively to epinephrine
- To inhibit further release of norepinephrine (correct)
Which of the following statements about β1 and β2 receptors is true?
Which of the following statements about β1 and β2 receptors is true?
- β1 receptors have approximately equal affinities for epinephrine and norepinephrine. (correct)
- β2 receptors respond equally to norepinephrine and epinephrine.
- β2 receptors have no role in responding to circulating epinephrine.
- β1 receptors have a higher affinity for epinephrine than norepinephrine.
In which type of tissues are β2 receptors predominantly found?
In which type of tissues are β2 receptors predominantly found?
- Adrenal medulla
- Skeletal muscle vasculature (correct)
- Cardiac tissues
- Parasympathetic innervated tissues
How do α2 receptors on presynaptic parasympathetic neurons function?
How do α2 receptors on presynaptic parasympathetic neurons function?
What mechanism does feedback inhibition serve in the context of sympathetic activity?
What mechanism does feedback inhibition serve in the context of sympathetic activity?
What is the predominant effect of epinephrine on blood glucose levels?
What is the predominant effect of epinephrine on blood glucose levels?
Which route of administration is preferred for epinephrine during anaphylaxis in an outpatient setting?
Which route of administration is preferred for epinephrine during anaphylaxis in an outpatient setting?
Which of the following describes a serious side effect of epinephrine?
Which of the following describes a serious side effect of epinephrine?
How is epinephrine primarily metabolized in the body?
How is epinephrine primarily metabolized in the body?
In which of the following conditions is epinephrine contraindicated?
In which of the following conditions is epinephrine contraindicated?
What is one of the primary uses of norepinephrine?
What is one of the primary uses of norepinephrine?
Which of the following actions is NOT related to epinephrine's effect on blood glucose levels?
Which of the following actions is NOT related to epinephrine's effect on blood glucose levels?
What can occur when epinephrine is used in patients on β-blockers?
What can occur when epinephrine is used in patients on β-blockers?
What is the primary effect of norepinephrine on blood vessels?
What is the primary effect of norepinephrine on blood vessels?
Why is norepinephrine not useful in treating bronchospasm?
Why is norepinephrine not useful in treating bronchospasm?
What occurs as a reflex response when norepinephrine increases blood pressure?
What occurs as a reflex response when norepinephrine increases blood pressure?
Which of the following is a reason for the limited therapeutic use of isoproterenol?
Which of the following is a reason for the limited therapeutic use of isoproterenol?
What is a significant adverse effect of norepinephrine?
What is a significant adverse effect of norepinephrine?
How is norepinephrine typically administered?
How is norepinephrine typically administered?
What metabolic pathway is primarily responsible for the breakdown of isoproterenol?
What metabolic pathway is primarily responsible for the breakdown of isoproterenol?
What effect does isoproterenol have on arterial pressure?
What effect does isoproterenol have on arterial pressure?
What is the primary benefit of using nonselective β-blockers like nadolol and propranolol in patients with portal hypertension?
What is the primary benefit of using nonselective β-blockers like nadolol and propranolol in patients with portal hypertension?
Which of the following β-blockers is NOT considered cardioselective?
Which of the following β-blockers is NOT considered cardioselective?
What unique property does esmolol have compared to other β-blockers?
What unique property does esmolol have compared to other β-blockers?
What is a common therapeutic use for cardioselective β-blockers?
What is a common therapeutic use for cardioselective β-blockers?
What is a significant side effect of labetalol when used for hypertension?
What is a significant side effect of labetalol when used for hypertension?
Which β-blocker has partial agonist activity, impacting both β1 and β2 receptors?
Which β-blocker has partial agonist activity, impacting both β1 and β2 receptors?
What is a consideration when administering cardioselective β-blockers to asthma patients?
What is a consideration when administering cardioselective β-blockers to asthma patients?
For what condition is intravenous labetalol primarily used?
For what condition is intravenous labetalol primarily used?
What effect does phenoxybenzamine have on heart rate?
What effect does phenoxybenzamine have on heart rate?
Which condition is phenoxybenzamine primarily used to treat?
Which condition is phenoxybenzamine primarily used to treat?
What is a characteristic of phentolamine compared to selective α1-blockers?
What is a characteristic of phentolamine compared to selective α1-blockers?
What is the primary adverse effect associated with the first dose of prazosin?
What is the primary adverse effect associated with the first dose of prazosin?
Which of the following is a side effect of both phenoxybenzamine and phentolamine?
Which of the following is a side effect of both phenoxybenzamine and phentolamine?
Why is prazosin suggested to be taken at bedtime?
Why is prazosin suggested to be taken at bedtime?
Which of the following adrenergic agonists is primarily used as a bronchodilator?
Which of the following adrenergic agonists is primarily used as a bronchodilator?
What distinguishes selective α1-blockers from nonselective α-blockers in terms of tolerance?
What distinguishes selective α1-blockers from nonselective α-blockers in terms of tolerance?
What is the primary receptor action of norepinephrine?
What is the primary receptor action of norepinephrine?
What type of receptor does phenoxybenzamine primarily block to achieve its effects?
What type of receptor does phenoxybenzamine primarily block to achieve its effects?
Which adrenergic agonist is used as a nasal decongestant?
Which adrenergic agonist is used as a nasal decongestant?
Which adrenergic agonist is NOT primarily classified for uterine relaxation?
Which adrenergic agonist is NOT primarily classified for uterine relaxation?
What is the therapeutic use of dobutamine?
What is the therapeutic use of dobutamine?
Which of the following is a CNS stimulant?
Which of the following is a CNS stimulant?
Which agent is used to prolong the duration of local anesthesia?
Which agent is used to prolong the duration of local anesthesia?
Which is an example of a mixed-acting adrenergic agonist?
Which is an example of a mixed-acting adrenergic agonist?
What is the main action of phenylephrine?
What is the main action of phenylephrine?
Which adrenergic agonist is primarily used to treat glaucoma?
Which adrenergic agonist is primarily used to treat glaucoma?
Flashcards
What are α2 receptors and their function?
What are α2 receptors and their function?
α2 receptors are located on the presynaptic nerve endings of sympathetic neurons. They control the release of norepinephrine by inhibiting further output when stimulated. This acts as a local mechanism to regulate norepinephrine release.
How do α2 receptors work?
How do α2 receptors work?
When a sympathetic adrenergic nerve is stimulated, a portion of the released norepinephrine binds to α2 receptors on the presynaptic membrane, leading to feedback inhibition, which reduces further release of norepinephrine.
Where else are α2 receptors found?
Where else are α2 receptors found?
α2 receptors are also found on presynaptic parasympathetic neurons, where they play a role in regulating the release of acetylcholine.
How do β-adrenoceptors differ from α-receptors?
How do β-adrenoceptors differ from α-receptors?
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What is the difference in affinity between β1 and β2 receptors?
What is the difference in affinity between β1 and β2 receptors?
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Adrenergic Agonist
Adrenergic Agonist
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Alpha Receptor (α)
Alpha Receptor (α)
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Beta Receptor (β)
Beta Receptor (β)
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Epinephrine (Adrenaline)
Epinephrine (Adrenaline)
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Alpha 1 Receptor (α1)
Alpha 1 Receptor (α1)
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Alpha 2 Receptor (α2)
Alpha 2 Receptor (α2)
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Beta 1 Receptor (β1)
Beta 1 Receptor (β1)
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Beta 2 Receptor (β2)
Beta 2 Receptor (β2)
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Directly Acting Adrenergic Agonists
Directly Acting Adrenergic Agonists
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Indirectly Acting Adrenergic Agonists
Indirectly Acting Adrenergic Agonists
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What is Epinephrine?
What is Epinephrine?
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How does Epinephrine affect blood glucose?
How does Epinephrine affect blood glucose?
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What are the cardiovascular effects of Epinephrine?
What are the cardiovascular effects of Epinephrine?
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How does Epinephrine affect the airways?
How does Epinephrine affect the airways?
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Why are different routes of administration used for Epinephrine?
Why are different routes of administration used for Epinephrine?
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What is Norepinephrine?
What is Norepinephrine?
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What are the main therapeutic uses of Epinephrine?
What are the main therapeutic uses of Epinephrine?
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What are the potential side effects of Epinephrine?
What are the potential side effects of Epinephrine?
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Norepinephrine's effects on the cardiovascular system
Norepinephrine's effects on the cardiovascular system
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Why norepinephrine causes vasoconstriction
Why norepinephrine causes vasoconstriction
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Baroreceptor reflex and norepinephrine
Baroreceptor reflex and norepinephrine
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Limitations of norepinephrine in treating asthma and anaphylaxis
Limitations of norepinephrine in treating asthma and anaphylaxis
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Therapeutic uses of norepinephrine
Therapeutic uses of norepinephrine
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Isoproterenol: A non-selective β-agonist
Isoproterenol: A non-selective β-agonist
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Isoproterenol's effects on the heart and blood vessels
Isoproterenol's effects on the heart and blood vessels
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Isoproterenol's bronchodilator effect
Isoproterenol's bronchodilator effect
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How does phenoxybenzamine affect cardiovascular system?
How does phenoxybenzamine affect cardiovascular system?
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What is phenoxybenzamine used for?
What is phenoxybenzamine used for?
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Describe phentolamine's mechanism of action.
Describe phentolamine's mechanism of action.
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How is phentolamine administered and what are its onset and duration?
How is phentolamine administered and what are its onset and duration?
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What are the potential adverse effects of phentolamine?
What are the potential adverse effects of phentolamine?
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What is prazosin and how does it work?
What is prazosin and how does it work?
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Compare the effects of selective vs. nonselective α-blockers on heart rate.
Compare the effects of selective vs. nonselective α-blockers on heart rate.
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What's the 'first-dose phenomenon' with prazosin?
What's the 'first-dose phenomenon' with prazosin?
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What are nonselective beta-blockers used for in portal hypertension?
What are nonselective beta-blockers used for in portal hypertension?
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What makes cardioselective beta-blockers better for asthma patients?
What makes cardioselective beta-blockers better for asthma patients?
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What are the primary uses of cardioselective beta-blockers?
What are the primary uses of cardioselective beta-blockers?
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What is special about Esmolol in terms of its use and half-life?
What is special about Esmolol in terms of its use and half-life?
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What are the advantages of cardioselective beta-blockers compared to nonselective ones?
What are the advantages of cardioselective beta-blockers compared to nonselective ones?
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What makes Labetalol unique among beta-blockers?
What makes Labetalol unique among beta-blockers?
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What are the uses and safety profile of Labetalol?
What are the uses and safety profile of Labetalol?
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What are the potential side effects of Labetalol?
What are the potential side effects of Labetalol?
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Study Notes
Adrenergic Agents
-
Four classes of drugs (ABCD):
- ACE inhibitors (ARBs)
- Diuretics
- Beta-blockers
- Calcium channel blockers
-
Adrenergic drugs affect receptors stimulated by norepinephrine or epinephrine
-
Drugs that activate adrenergic receptors are called sympathomimetics
-
Drugs that block adrenergic receptors are called sympatholytics
-
Sympathomimetics are adrenergic agonists
Adrenergic Receptors
- Several classes of adrenoceptors can be distinguished pharmacologically.
- Two main families of receptors, designated alpha (α) and beta (β), are classified based on their differential responses to the adrenergic agonists, epinephrine, norepinephrine, and isoproterenol.
- Both alpha and beta receptor types have specific subtypes.
- Alpha-adrenoceptors:
- Respond weakly to isoproterenol
- Respond to epinephrine and norepinephrine
- Divided into subtypes based on affinities for agonists and antagonists.
- Beta-adrenoceptors:
- Beta 1 receptors have similar affinities for epinephrine and norepinephrine.
- Beta 2 receptors have a higher affinity for epinephrine than norepinephrine.
- Adrenergically innervated organs and tissues have a predominant receptor type.
Adrenergic Receptor Subtypes
- a1 receptors: found on postsynaptic effector organs, mediate vascular smooth muscle constriction.
- a2 receptors: found on presynaptic nerve endings, mediate feedback inhibition of norepinephrine release.
- β1 receptors: found in the heart, increase heart rate and contractility.
- β2 receptors: found in smooth muscle of the bronchi, blood vessels, and other organs, mediate relaxation.
- β3 receptors: found in adipose tissue, mediate lipolysis.
Synthesis and Release of Norepinephrine (NE)
- Synthesis of norepinephrine (NE) begins with tyrosine
- NE is stored in vesicles within the presynaptic neuron
- Release of NE involves calcium influx causing vesicle fusion (exocytosis)
- Removal of NE from synaptic space is via reuptake, or by metabolism (MAO, COMT).
Classification of Sympathomimetics
- Based on chemical structure:
- Catecholamines: contain catechol nucleus (e.g., epinephrine, norepinephrine, dopamine, isoproterenol)
- Non-catecholamines: lack catechol nucleus (e.g., tyramine, amphetamine, phenylephrine)
Mechanism of Action of Sympathomimetics
- Direct acting agonists: interact directly with adrenergic receptors (e.g., epinephrine, norepinephrine)
- Indirect acting agonists: enhance the release of norepinephrine or block its reuptake (e.g., cocaine, amphetamine)
Therapeutic Uses of Sympathomimetics
- Based on various therapeutic effects (e.g., shock, bronchodilation, CNS stimulation)
Adverse Effects of Epinephrine
- Often due to extension of pharmacological action (e.g. tachycardia, tremors, hypertension)
- High concentration can cause acute pulmonary oedema, by shifting blood from systemic to pulmonary circulation
- Contraindicated in cardiovascular diseases.
Norepinephrine
- Similar to epinephrine: increase blood pressure by vasoconstriction.
- Not suitable for oral administration.
- Effective treatment for shock
Isoproterenol (Isoprenaline)
- Non-selective beta-receptor agonist.
- Used in treatment of cardiac arrest.
- Not effective orally due to metabolism
Dobutamine
- Primarily a beta-1 receptor agonist with minor beta-2 and alpha-1 effects.
- Increases heart rate and cardiac output.
- Inotropic support in acute heart failure (IV infusion)
Albuterol, Levalbuterol, Metaproterenol, and Terbutaline
- Used to treat acute bronchospasm (i.e. asthma ).
- β2-adrenergic agonists, effective in relaxation of airways.
Salmeterol, Indacaterol, Olodaterol
- Long-acting β2-adrenergic agonists (LABAs).
- Management of respiratory disorders, like asthma and COPD, but not recommended as monotherapy for asthma.
Naphazoline, Oxymetazoline, and Tetrahydrozoline
- Alpha-1 adrenergic agonists.
- Used as nasal decongestants, and ophthalmic drops to improve nasal mucosa or eye redness, respectively.
Mirabegron and Vibegron
- Beta-3 adrenergic agonists.
- They relax detrusor smooth muscle and increase bladder capacity.
- Used in patients with overactive bladders.
Indirect-Acting Adrenergic Agonists
- Potentiation of endogenous norepinephrine or epinephrine, acting indirectly to stimulate norepinephrine increase (e.g. amphetamine).
Cocaine
- Blocks sodium-chloride-dependent norepinephrine transporter.
- Results in increased norepinephrine in the synaptic space, thus increasing sympathetic activity.
- A local anesthetic
Ephedrine and Pseudoephedrine
- Mixed action adrenergic agonists.
- Stimulate both alpha and beta receptors, and enhance release of norepinephrine.
Summary of Important Characteristics of Adrenergic Agonists
- Arrhythmias,
- Headache,
- Hyperactivity,
- Insomnia,
- Nausea,
- Tremors
Adrenergic Antagonists
- These drugs block adrenergic receptors.
- Classified based on selectivity for alpha (α) or beta (β) receptors.
Phenoxybenzamine
- Irreversible, nonselective blocker of alpha-1 and alpha-2 receptors.
Phentolamine
- Competitive, nonselective blocker of alpha-1 and alpha-2 receptors.
Prazosin
- Selective alpha-1 blocker.
- May cause first-dose phenomenon (postural hypotension).
Other Selective alpha-1 Blockers
- Terazosin, Doxazosin, Alfuzosin, and Tamsulosin
- Used for benign prostatic hyperplasia.
Beta-Adrenergic Blockers
- These drugs block beta receptors.
- Classified based on selectivity and other properties
Propranolol
- Nonselective beta-receptor antagonist.
- Useful in hypertension, angina, and arrhythmias.
- High lipophilicity, rapidly crosses the blood-brain barrier.
Nadolol and Timolol
- Non-selective beta-blockers.
- Long duration of action.
- Used topically to treat glaucoma.
Acebutolol, Atenolol, Bisoprolol, Esmolol, Metoprolol
- Selective Beta-1 antagonists.
- Fewer effects compared to non-selective agents
Labetalol
- Competitive beta-1, beta-2, and alpha-1 antagonist.
- Has additional vasodilatory effects.
- Used in hypertensive emergencies and pregnancy.
Carvedilol
- Competitive beta-1, beta-2, and alpha-1 antagonist.
- Additional antioxidant and vasodilatory properties.
- Used in chronic heart failure.
Nebivolol
- Selective beta-1 antagonist.
- Has nitric oxide-releasing vasodilating activity.
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