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Which type of adrenergic drug decreases sympathetic nervous activity?
Nicotinic receptors are primarily found at postganglionic nerve endings.
False
Name one natural catecholamine.
Dopamine
The primary receptor type affected by beta-blockers is the ______ receptor.
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Match the adrenergic drug classifications with their descriptions:
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What is the primary cardiovascular effect associated with the administration of Ritodrine?
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Cyclopentamine is primarily used as an oral medication for chronic pain management.
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What type of agents are aliphatic amines mainly categorized as?
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The presence of bulky lipophilic groups at ortho and/or para positions enhances selectivity to ______ receptors.
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Match each adrenergic receptor type with its primary effect:
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Which of the following is NOT considered a pharmacological effect of alpha-blockers?
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The chemical synthesis of cyclopentamide involves ______ with perchloric acid.
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Imidazoline derivatives are primarily α2 receptor agonists and have low selectivity.
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Which of the following statements is true about pseudoephedrine?
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Pseudoephedrine has a direct agonist activity.
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What is the pKa value of pseudoephedrine?
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Midodrine is used to treat symptomatic __________ hypotension.
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Match the following drugs with their primary use:
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What property of pseudoephedrine allows it to cross the blood-brain barrier (BBB)?
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Ritodrine causes significant cardiovascular effects compared to nonselective β-agonists.
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Identify one precaution that should be taken when using pseudoephedrine.
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Study Notes
Ritodrine
- Is a selective β2-agonist
- Is developed as a uterine relaxant
- Has more sustained uterine inhibitory effects than its effects on the cardiovascular system
- Causes minimal cardiovascular effects compared with nonselective β-agonists
Cyclopentamine
- Is a non-selective α agonist
- Was used as a nasal decongestant
- 1-Cyclopentyl-N-methylpropan-2-amine is the chemical name
Imidazoline derivatives
- Are α agonists
- Have one carbon bridge between C2 of imidazoline and aryl group
- Have bulky group at ortho position
- Have aryl group
- Essential structural features include:
- Imidazoline
- Aryl group
- One carbon bridge between C2 of imidazoline and aryl group
- Bulky group at ortho position
Imidazoline derivatives (α agonists)
- Naphazoline
- Tetrahydrozoline
- Xylometazoline
- Oxymetazoline
- Bulky lipophilic groups at ortho and/or para positions give selectivity to α1 receptors and diminish the affinity to α2 receptors
Adrenergic drugs
- Exert their principal pharmacological and therapeutic effects by enhancing or reducing the activity of the various components of the sympathetic division of the autonomic nervous system.
- Sympathomimetics or adrenergic stimulants are substances that produce effects similar to stimulation of sympathetic nervous activity
- Sympatholytics, antiadrenergics, or adrenergic-blocking agents decrease sympathetic activity
Sympathomimetics
- Can be classified into three major categories according to their chemical structures:
- Phenylethylamines
- Aliphatic amines
- Imidazolines
Phenylethylamines
- Can be subdivided to catecholamines and non-catecholamines
- Catecholamines contain a catechol ring and an amine and are classified to natural and synthetic catecholamines
- Natural catecholamines include dopamine, epinephrine, and norepinephrine
- Dopamine, Epinephrine, and Norepinephrine are non-selective α and β agonists
Pseudoephedrine
- Is not metabolized by either COMT or MAO
- Is active orally
- Exists as two enantiomers:
- L-(+)-Pseudoephedrine
- D-(-)Pseudoephedrine
- L-(+)-Pseudoephedrine is mainly indirect acting
- D-(-) Pseudoephedrine is a diastereoisomer of ephedrine
- Pseudoephedrine is less polar (log P = 1.05, pKa = 9.38) than Ephedrine
- Has fewer CNS effects than ephedrine and is found in many OTC nasal decongestant and cold medications
- Should be used with caution in hypertensive individuals
- Should not be used in combination with MAO inhibitors
Midodrine
- N-Glycyl prodrug
- Is used in the treatment of symptomatic orthostatic hypotension
- Is hydrolyzed by amidase, giving free amino group that gives α agonist activity with potent vasopressor effect
- Does not have phenolic groups, or a β-OH group
Cholinergic receptors
- Are subdivided to muscarinic and nicotinic receptors
- Muscarinic receptors exist at the postganglionic parasympathetic nerve endings
- Nicotinic receptors are present in the autonomic ganglia, motor end plate, and suprarenal medulla
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Description
This quiz covers various adrenergic drugs including Ritodrine, Cyclopentamine, and Imidazoline derivatives. It focuses on their classifications, structural features, and pharmacological effects. Test your knowledge on selective β2-agonists and non-selective α agonists.
