Adrenergic Direct Agonist
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Questions and Answers

Which enzyme is responsible for the conversion of tyrosine to DOPA in adrenergic neurotransmission?

  • Decarboxylase
  • Tyrosine Hydroxylase (correct)
  • COMT
  • Dopamine hydroxylase

    • Which of the following is a direct-acting sympathomimetic drug that acts directly on adrenergic receptors?

  • Drugs that block the transport of NE into sympathetic neurons
  • Drugs that release or displace NE from sympathetic terminals
  • Mixed acting sympathomimetic drugs that indirectly release NE and directly activate receptors (correct)
  • Drugs that block the metabolizing enzymes MAO or COMT

    • Which receptor is responsible for bronchodilation in the respiratory tract?

  • b1
  • b2 (correct)
  • COMT
  • a1

    • Which receptor subtype is responsible for vasoconstriction in the smooth muscle of blood vessels?

    <p>a1 receptor (D)</p> Signup and view all the answers

    What is the primary effect of sympathomimetics on the smooth muscle in the wall of the gut?

    <p>Constriction (D)</p> Signup and view all the answers

    Which receptor subtype is responsible for inducing lipolysis in adipocytes?

    <p>b3 receptor (D)</p> Signup and view all the answers

    Which receptor subtype is responsible for increasing heart rate and force of contraction?

    <p>b1 receptor (A)</p> Signup and view all the answers

    Which of the following is an adverse effect of β2 agonists?

    <p>Tachycardia (D)</p> Signup and view all the answers

    Which of the following is an adverse effect of β3-selective agonists?

    <p>Urinary tract infection (C)</p> Signup and view all the answers

    In patients with lung disease, how can adverse effects of β2 agonists be minimized?

    <p>Inhalation administration (A)</p> Signup and view all the answers

    Which of the following is a therapeutic application of dopamine?

    <p>Treatment of shock accompanied by compromised renal function and/or severe congestive heart failure (B)</p> Signup and view all the answers

    Which of the following is a clinical effect of α1-selective adrenergic agonists?

    <p>Increased peripheral vascular resistance (C)</p> Signup and view all the answers

    Which of the following is a therapeutic application of metaraminol?

    <p>Treatment of hypotensive states specially in spinal anesthesia and surgical procedures (B)</p> Signup and view all the answers

    Which of the following is an adverse effect of α2-selective adrenergic agonists?

    <p>Xerostomia (A)</p> Signup and view all the answers

    Which one of the following is a therapeutic application of epinephrine?

    <p>Reversal of serious hypersensitivity reactions (D)</p> Signup and view all the answers

    Which one of the following is an adverse effect of epinephrine?

    <p>Cerebral hemorrhage (C)</p> Signup and view all the answers

    Which one of the following is a characteristic of norepinephrine?

    <p>Has metabolic effects similar to epinephrine (D)</p> Signup and view all the answers

    Which one of the following is a dose-dependent effect of dopamine?

    <p>Increased heart rate and cardiac contractility (A)</p> Signup and view all the answers

    Which of the following is the correct statement about the therapeutic applications of b2-ADRENERGIC RECEPTOR AGONISTS?

    <p>They are primarily used for the treatment of bronchoconstriction in asthma or COPD. (B)</p> Signup and view all the answers

    What is the main effect of b2-SELECTIVE AGONISTS?

    <p>Relaxation of bronchial smooth muscle and decreased airway resistance. (C)</p> Signup and view all the answers

    What is the approximate percentage of b2 receptors in the human heart?

    <p>40% (C)</p> Signup and view all the answers

    What is the recommended use of Salmeterol and Formoterol for nocturnal asthma?

    <p>They are the agents of choice for nocturnal asthma in patients who remain symptomatic despite anti-inflammatory agents. (A)</p> Signup and view all the answers

    Which one of these drugs is a centrally acting α2 agonist used for sedation under intensive care and during anesthesia?

    <p>Dexmedetomidine (A)</p> Signup and view all the answers

    Which one of these drugs is an α2 selective adrenergic agonist that is contraindicated in active hepatic disease and can be associated with autoimmune hemolytic anemia?

    <p>Methyldopa (A)</p> Signup and view all the answers

    Which one of these drugs is a mixed-acting sympathomimetic that stimulates heart rate and cardiac output, causes bronchodilation, and has been extensively promoted for weight control and boosting sports performance and energy?

    <p>Ephedrine (A)</p> Signup and view all the answers

    Which one of these drugs is a synthetic catecholamine that potently stimulates both β1- and β2-adrenergic receptors and is used for emergency stimulation of the heart and the rapid alleviation of an acute asthma attack when inhaled?

    <p>Isoproterenol (A)</p> Signup and view all the answers

    Which enzyme is responsible for the conversion of dopamine to norepinephrine in adrenergic neurotransmission?

    <p>Dopamine Hydroxylase (C)</p> Signup and view all the answers

    Which receptor subtype is responsible for vasodilation in the vascular smooth muscle?

    <p>b2 (A)</p> Signup and view all the answers

    What is the primary effect of sympathomimetics on the smooth muscle in the wall of the gut?

    <p>Decreased GI motility (B)</p> Signup and view all the answers

    Which one of the following is a therapeutic use of droxidopa?

    <p>Treatment of orthostatic hypotension (C)</p> Signup and view all the answers

    Which one of the following is an adverse effect of norepinephrine?

    <p>Impaired circulation (D)</p> Signup and view all the answers

    Which one of the following is a characteristic of dopamine?

    <p>Activates D1-D5 dopamine receptors (B)</p> Signup and view all the answers

    Which one of the following is a therapeutic application of fenoldopam?

    <p>Control of severe hypertension (A)</p> Signup and view all the answers

    Which receptor subtype is responsible for vasoconstriction in the smooth muscle of blood vessels?

    <p>α1 (A)</p> Signup and view all the answers

    What is the primary effect of sympathomimetics on the smooth muscle in the wall of the gut?

    <p>Constriction (D)</p> Signup and view all the answers

    Which of the following is an adverse effect of α2-selective adrenergic agonists?

    <p>Hypotension (B)</p> Signup and view all the answers

    Which of the following is a therapeutic application of metaraminol?

    <p>Hypotensive emergency (C)</p> Signup and view all the answers

    Which drug is a centrally acting α2 agonist used for sedation under intensive care and during anesthesia?

    <p>Dexmedetomidine (B)</p> Signup and view all the answers

    Which drug is more selective for α2 receptors than clonidine and has a sustained-release form approved for the treatment of ADHD in children?

    <p>Guanfacine (D)</p> Signup and view all the answers

    Which drug is contraindicated in active hepatic disease and is the drug of choice for the treatment of hypertension during pregnancy?

    <p>Methyldopa (C)</p> Signup and view all the answers

    Which drug is a mixed-acting sympathomimetic that stimulates heart rate and cardiac output, causes bronchodilation, and has been extensively promoted for weight control and boosting sports performance and energy?

    <p>Ephedrine (D)</p> Signup and view all the answers

    Which of the following is a true statement about Salmeterol?

    <p>Salmeterol is more selective for b2 receptors than albuterol. (A)</p> Signup and view all the answers

    What is the FDA-approved use of Arformoterol?

    <p>Bronchoconstriction in patients with COPD. (A)</p> Signup and view all the answers

    Which of the following is a true statement about Indacaterol?

    <p>Indacaterol has a shorter duration of action than salmeterol. (A)</p> Signup and view all the answers

    What is the approved use of Mirabegron and Vibegron?

    <p>Treatment of incontinence. (A)</p> Signup and view all the answers

    Which one of the following drugs is a short-acting β2-selective agonist that is resistant to methylation by COMT and is used for the long-term treatment of COPD, asthma, and acute bronchospasm?

    <p>Metaproterenol (D)</p> Signup and view all the answers

    Which one of the following drugs is an α2 selective adrenergic agonist that is contraindicated in active hepatic disease and can be associated with autoimmune hemolytic anemia?

    <p>Isoproterenol (A)</p> Signup and view all the answers

    Which one of the following drugs is a mixed-acting sympathomimetic that stimulates heart rate and cardiac output, causes bronchodilation, and has been extensively promoted for weight control and boosting sports performance and energy?

    <p>Ephedrine (A)</p> Signup and view all the answers

    Which one of the following drugs is a synthetic catecholamine that potently stimulates both β1- and β2-adrenergic receptors and is used for emergency stimulation of the heart and the rapid alleviation of an acute asthma attack when inhaled?

    <p>Norepinephrine (D)</p> Signup and view all the answers

    Epinephrine is an agonist at both alpha and beta adrenoceptors.

    <p>True (A)</p> Signup and view all the answers

    Epinephrine has a low concentration predominantly activating beta1 and beta2 receptors.

    <p>True (A)</p> Signup and view all the answers

    Epinephrine causes vasoconstriction in the smooth muscle of blood vessels.

    <p>True (A)</p> Signup and view all the answers

    Epinephrine is primarily used for the treatment of cardiac arrest.

    <p>True (A)</p> Signup and view all the answers

    True or false: Dopamine is converted to norepinephrine by the enzyme dopamine hydroxylase.

    <p>True (A)</p> Signup and view all the answers

    True or false: Indirect-acting sympathomimetic drugs increase the availability of norepinephrine or epinephrine to stimulate adrenergic receptors.

    <p>True (A)</p> Signup and view all the answers

    True or false: Sympathomimetics have an inhibitory action on certain types of smooth muscle, such as the wall of the gut and the bronchial tree.

    <p>True (A)</p> Signup and view all the answers

    True or false: Activation of postsynaptic α2 receptors in blood vessels results in vasodilation.

    <p>False (B)</p> Signup and view all the answers

    True or false: Clonidine is more effective than apraclonidine for the treatment of glaucoma.

    <p>False (B)</p> Signup and view all the answers

    True or false: Guanfacine has a higher incidence of withdrawal syndrome compared to clonidine.

    <p>False (B)</p> Signup and view all the answers

    True or false: Methyldopa is the drug of choice for the treatment of hypertension during pregnancy.

    <p>True (A)</p> Signup and view all the answers

    Long-acting β2-selective agonists are suitable for monotherapy and acute attacks.

    <p>False (B)</p> Signup and view all the answers

    Salmeterol has a longer duration of action than formoterol.

    <p>True (A)</p> Signup and view all the answers

    Indacaterol has a faster onset of action than salmeterol.

    <p>True (A)</p> Signup and view all the answers

    Vilanterol is available in combination with umeclidinium in Europe.

    <p>True (A)</p> Signup and view all the answers

    True or false: Ephedrine, phenylpropanolamine, and pseudoephedrine can be used as precursors in the illicit manufacture of amphetamine and methamphetamine.

    <p>True (A)</p> Signup and view all the answers

    True or false: Isoproterenol has a selective affinity for both α receptors and β receptors.

    <p>False (B)</p> Signup and view all the answers

    True or false: Short-acting β2-selective agonists are resistant to methylation by COMT.

    <p>True (A)</p> Signup and view all the answers

    True or false: Levalbuterol is the R-enantiomer of albuterol.

    <p>True (A)</p> Signup and view all the answers

    True or false: Epinephrine can cause a fall in plasma K+ due to stimulation of K+ uptake into skeletal muscle (b2).

    <p>True (A)</p> Signup and view all the answers

    True or false: Norepinephrine can cause vasodilation and lower blood pressure.

    <p>False (B)</p> Signup and view all the answers

    True or false: Dopamine primarily acts on D1 dopaminergic receptors to induce vasodilation of renal, mesenteric, and coronary vasculature.

    <p>True (A)</p> Signup and view all the answers

    True or false: α1-selective adrenergic agonists cause peripheral vascular resistance and bradycardia.

    <p>True (A)</p> Signup and view all the answers

    Match the following enzymes with their function in adrenergic neurotransmission:

    <p>Tyrosine Hydroxylase = Converts Tyrosine to DOPA Decarboxylase = Converts DOPA to Dopamine Dopamine Hydroxylase = Converts Dopamine to Norepinephrine COMT and MAO = Metabolizes Norepinephrine</p> Signup and view all the answers

    Match the following systems with their response to sympathomimetic drugs:

    <p>Cardiovascular System = Positive chronotropic and inotropic effects Respiratory Tract = Bronchodilation Urinary Tract = Relaxes bladder and constricts sphincter GI Tract = Decreases GI motility and constricts sphincter</p> Signup and view all the answers

    Match the following actions with their effects due to sympathomimetics:

    <p>Excitatory action = Increases heart rate and force of contraction Inhibitory action = Relaxes the wall of the gut, the bronchial tree and in blood vessels supplying skeletal muscle Metabolic actions = Increases rate of glycogenolysis in liver and muscle and liberation of free fatty acids from adipose tissue</p> Signup and view all the answers

    Match the following long acting β2-selective agonists with their characteristics:

    <p>Salmeterol = Slow onset of action, not suitable for acute attacks, provides symptomatic relief and improves lung function in patients with COPD Formoterol = Rapid bronchodilation, lasts 12 hrs, FDA-approved for asthma, bronchospasm, prophylaxis of exercise-induced bronchospasm, and COPD Arformoterol = The (R,R) enantiomer of formoterol, has twice the potency of racemic formoterol, FDA-approved for the long-term treatment of bronchoconstriction in patients with COPD Indacaterol = Once daily dosing with a fast onset (5 min) and longer duration of action than salmeterol (24 hrs)</p> Signup and view all the answers

    Match the following β2 agonists with their administration method to minimize adverse effects in patients with lung disease:

    <p>Salmeterol = Inhalation Formoterol = Inhalation Arformoterol = Inhalation Indacaterol = Inhalation</p> Signup and view all the answers

    Match the following β3-selective agonists with their approved use and side effects:

    <p>Mirabegron = Approved for use against incontinence, side effects include increased blood pressure, increased incidence of urinary tract infection, and headache Vibegron = Approved for use against incontinence, side effects include increased blood pressure, increased incidence of urinary tract infection, and headache</p> Signup and view all the answers

    Match the following β2-selective agonists with their approved combinations:

    <p>Olodaterol = Used alone or in combination with tiotropium bromide Vilanterol = Approved for use in combination with fluticasone, available in Europe in combination with umeclidinium</p> Signup and view all the answers

    Match the following drugs with their primary usage:

    <p>Isoproterenol = Intense stimulation of the heart and alleviation of acute asthma attack when inhaled Dobutamine = Short-term treatment of cardiac decompensation after cardiac surgery, in congestive heart failure or acute myocardial infarction Metaproterenol = Long-term treatment of COPD, asthma, and acute bronchospasm Albuterol = Management of status asthmaticus and prevention of exercise-induced bronchospasm</p> Signup and view all the answers

    Match the following drugs with their characteristics:

    <p>Isoproterenol = Synthetic catecholamine potent stimulation of both b1- and b2-adrenergic receptors Dobutamine = The observed clinical effect is that of a selective b1-agonist Metaproterenol = Resistant to methylation by COMT Albuterol = Has the potential to delay preterm labor</p> Signup and view all the answers

    Match the following drugs with their effects:

    <p>Isoproterenol = Lowers peripheral vascular resistance and increases blood sugar and lipolysis Dobutamine = May increase the size of a myocardial infarct Metaproterenol = Fast acting within minutes of inhalation and persist for several hours Albuterol = Produces bronchodilation within 15 minutes and persist for 3-4 hours</p> Signup and view all the answers

    Match the following drugs with their administration methods:

    <p>Isoproterenol = Inhalation for acute asthma attack Dobutamine = Intravenous for short-term treatment of cardiac decompensation Metaproterenol = Aerosol for inhalation, nebulizer, oral Albuterol = Inhalation or oral administration</p> Signup and view all the answers

    Match the following drugs with their primary usage or characteristic:

    <p>Clonidine = Used as a vasoconstricting nasal decongestant and found to cause hypotension, sedation, and bradycardia during clinical trials Apraclonidine = Used topically to decrease intraocular pressure with minimal effects on cardiovascular parameters Brimonidine = Crosses the blood-brain barrier and can produce hypotension and sedation but has lower central nervous system effects than clonidine Tizanidine = Decreases muscle tone and frequency of muscle spasms without reducing strength</p> Signup and view all the answers

    Match the following adverse effects with the corresponding drug:

    <p>Liver damage and sedation = Tizanidine Xerostomia, bradycardia and sedation = Clonidine Contact dermatitis = Transdermal Clonidine Autoimmune hemolytic anemia = Methyldopa</p> Signup and view all the answers

    Match the following drugs with their treatment applications:

    <p>Methyldopa = Treatment of hypertension during pregnancy Dexmedetomidine = Used for sedation under intensive care and during anesthesia Ephedrine = Stimulates heart rate and cardiac output and causes bronchodilation Guanfacine = Treatment of ADHD in children aged 6-17 years</p> Signup and view all the answers

    Match the following drugs with their primary effects on the body:

    <p>Methyldopa = Centrally acting antihypertensive agent Guanfacine = More selective for α2 than clonidine Dexmedetomidine = Decreases sympathetic response to surgery and opioid requirement for pain control Ephedrine = Agonist at both a and b receptors; in addition, increases release of NE from sympathetic neurons</p> Signup and view all the answers

    Match the following receptors with their primary effects:

    <p>α1 (Gq) = Vasoconstriction and Constriction of GI and bladder sphincters α2 (Gi) = Suppression of release of norepinephrine by negative feedback and Inhibition of insulin b1 = Increase in heart rate and force of contraction and Increase in renin secretion b2 = Vasodilation, Bronchodilation and Induction of glucagon</p> Signup and view all the answers

    Match the following receptors with their affinities for catecholamines:

    <p>α receptors = Epinephrine ≥ Norepinephrine &gt;&gt; Isoproterenol β receptors = Isoproterenol &gt; Epinephrine &gt; Norepinephrine b2 and a1 receptors in s.muscle of blood vessels = b2 causes vasodilation, a1 causes vasoconstriction Both α- and β-adrenoceptors = Agonists are Dopamine, Epinephrine and Norepinephrine</p> Signup and view all the answers

    Match the following properties of Catecholamines:

    <p>Catecholamines = High potency, Rapid inactivation, Poor CNS penetration Compounds lacking the catechol hydroxyl groups = Longer half-lives, as they are not inactivated by COMT Endogenous catecholamines = Dopamine, Epinephrine and Norepinephrine Epinephrine = Potent vasopressor drug, Very potent vasoconstrictor and cardiac stimulant</p> Signup and view all the answers

    Match the following effects of Epinephrine with their respective actions:

    <p>Cardiovascular = + inotropic (b1), + chronotropic (b1), ↑ cardiac oxygen consumption Respiratory = Powerful bronchodilation, Direct action on bronchial s.muscle (b2) Metabolic Processes = Hyperglycemia: ↑ glycogenolysis (b2; liver and muscle), ↑ release of glucagon (b2), ↓ release of insulin (α2), initiates lipolysis (b3) Eye = Mydriasis (a1), Lowers intraocular pressure, ↓ production of aqueous humor (vasoconstriction)</p> Signup and view all the answers

    Match the following adrenergic agonists with their primary effects:

    <p>Epinephrine = Causes a fall in plasma K+, may lead to severe hypertension and cerebral hemorrhage Norepinephrine = Systemic administration increases blood pressure, can cause severe hypertension Dopamine = Activates D1-D5 Dopamine receptors and α- and β-adrenergic receptors, effects are dose dependent α 1-Selective Adrenergic Agonists = Increase peripheral vascular resistance, cause bradycardia through activation of reflex vagal responses</p> Signup and view all the answers

    Match the following drugs with their primary therapeutic uses:

    <p>Norepinephrine = Emergency treatment of shock, IV in hypotensive crisis and cardiac arrest Droxidopa = Treatment of orthostatic hypotension Dopamine = Treatment of shock, low cardiac output accompanied by compromised renal function and/or severe congestive heart failure Phenylephrine = IV treatment of hypotension, vasoconstrictor in regional analgesia, mydriatic in ophthalmic procedures and treatment of open-angle glaucoma</p> Signup and view all the answers

    Match the following adverse effects with the corresponding adrenergic agonists:

    <p>Epinephrine = Hemorrhage, Ventricular arrhythmias, Angina Norepinephrine = Decreased blood flow to organs such as kidney and intestines, can cause necrosis at the site of injection Dopamine = Increased risk of arrhythmias α 1-Selective Adrenergic Agonists = A complication is supine hypertension</p> Signup and view all the answers

    Match the following adrenergic agonists with their receptor affinity:

    <p>Epinephrine = Agonist at α1, α2, β1, β2, β3 receptors Norepinephrine = Agonist at α1 and β1; little effect at β2 Dopamine = Activates D1-D5 Dopamine receptors and α- and β-adrenergic receptors α 1-Selective Adrenergic Agonists = Selective agonist at α1 receptors</p> Signup and view all the answers

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