GGG's Asthma and autocoids review questions

Continuous use of inhaled albuterol can result in which of the following actions? a Increased phospholipase C activity b Activation of alpha 2 adrenergic receptors c Activation of intracellular kinases that decrease receptor function d An increase in the synthesis of beta-adrenergic receptors e Increase in the number of beta-adrenergic at the cell surface

Activation of beta-2 receptors by exposure to agonist can result in the desensitization and downregulation of the receptors. This is a form of cellular tolerance. In the case of desensitization, the activation of beta-adrenergic receptor kinase leads to phosphorylation of the beta-receptor. When phosphorylated by BARK the receptor can no longer couple to Gs.

Which drug is prescribed, "as needed" in mild cases of asthma? a Oral corticosteroid b IgE monoclonal antibodies c Adrenergic beta 2 receptor-agonists d Oral gold e Theophylline

Adrenergic beta-2 receptor-agonists. Drugs used to reduce bronchoconstriction are useful to treat a patient while they are having an asthmatic attack.

A 25-year-old female patient presents with dyspnea and wheezing, which often wakes her up at night. A diagnosis of asthma is established after demonstrating an increase in the FEV1 after two puffs of a beta-2 adrenergic-receptor agonist. Which drug was used? a Albuterol b Omalizumab c Theophylline d Triamcinolone e Zileuton

Albuterol

A 14-year-old female has mild asthmatic attacks that occur once or twice a month would most likely be prescribed which of the following medicines to relieve her bronchoconstriction during an attack? a Albuterol b Epinephrine c Nedocromil d Omalizumab e Theophylline

Albuterol is a beta-2 receptor agonist that is commonly used for intermittent asthma.

Which of the following drugs are now considered appropriate for the treatment of most cases of persistent asthma? a Katanserin b Chlorpheniramine c Ranitidine d Beclomethasone e Salmeterol

Beclomethasone can be used as an inhaled glucocorticoid to reduce the inflammation associated with all types of persistent asthma (mild to sever)

Which of the following anti-asthma drug can cause esophageal candidiasis? a.Zafirlukast b.Ipratropium c.Nedocromil d.Salmeterol e.Beclomethasone

Beclomethasone is a glucocorticoid that is used in the inhaled form to reduce the inflammation associated with the pathophysiology that underlies asthma. A side effect of using this type of immunosuppressant drug is opportunistic infections such as thrush or oral/esophageal candidiases.

A 45-year-old male with mild persistent asthma is prescribed an anti-inflammatory drug that affects DNA transcription via binding to a cytoplasmic protein. Which drug was used? a Ipratropium b Beclomethasone c Zileuton d Salmeterol e Theophylline

Beclomethasone like all glucocorticoid drugs once inside cell bind to and activate DNA transcription factors.

The most widely used, safe and effective drugs used to decrease bronchoconstriction during an asthmatic attack is which of the following? a.Methylxanthine b. Beta-2-selective sympathomimetics c.Corticosteroids d. Leukotriene-pathway inhibitors e.Potassium-sparing agents

Beta-2-selective sympathomimetics (e.g. albuterol). Methylxanthine, like theophylline, are phosphodiesterase inhibitors with many systemic side effects. Corticosteroids and leukotriene pathway inhibitors are used to reduce inflammation.

Which of the following would be an expected affect following histamine H1 receptor activation? a Bronchoconstriction b Increased gastric acid secretion c Increased intracellular cAMP production d Increased Sedation e Vasoconstriction

Bronchoconstriction is produced via H1 receptor activation of Gq, intracellular IP3 production and an increase in intracellular calcium. Gastric acid secretion is an H2 effect. Histamine produces vasodilation via the release of NO.

A 48-year-old man with mild seasonal allergic rhinoconjunctivitis is directed to take an oral medication to treat his symptoms. He is a truck driver and spends most of his days behind driving a semi-trailer. Which medication was he most likely directed to take? a Beclomethasone b Cetirizine c Diphenhydramine d Prednisolone e Theophylline

Cetirizine, fexofenadine, and loratadine are all second generation antihistamines with reduced CNS penetration.

A 48-year-old man with seasonal allergic rhinitis uses a nasal spray to treat his mild symptoms. The intranasal spray contains a drug that when used prophylactically prevents mast cell degranulation. Which drug is being used by this patient? a Cromolyn b Diphenhydramine c Fexofenadine d Phenylephrine e Salmetero

Cromolyn

Which of the following is a prophylactic agent that appears to stabilize mast cells and inhibits the release of mediators? a Cromolyn b Ergonovine c Famotidine d Metoprolol e Salmeterol

Cromolyn inhibits the degranulation of mast cells. Cromolyn and nedocromil alter chloride conductance in mast cells reducing degranulation (histamine release). Based on this mechanism of action it is used ONLY prophylactically. It can be used for allergic rhinitis and as a before treatment for things like exercise induced asthma.

A 44-year-old male has trouble falling asleep. His doctor informs him of an over-the-counter- medication that might help. Which of the following was most likely suggested by this patient's doctor? a Astemizole b Cetirizine c Diphenhydramine d Fexofenadine e Loratadine

Diphenhydramine, first generation antihistamine with good CNS penetration. The other drugs are second generation antihistamines with less CNS penetration and less sedation.

A 45-year-old male suffers from seasonal nasal allergies and motion sickness. He is told to take on of the following medication because it has efficacy against both problems. Which drug did the clinician tell the patient to buy? a Astemizole b Cetirizine c Diphenhydramine d Fexofenadine e Loratadine

Diphenhydramine: Diphenhydramine is a first generation anti-histamine. This class in general has antagonistic effects on other receptors like, muscarinic, alpha, and serotonin receptors. The non-specific effects on muscarinic receptors can be used to treat other disease states like motion sickness.

Motion sickness can be treated with a Diphenhydramine b Dorzolamide c Famotidine d Pergolide e Sumatriptan

Diphenhydramine: Diphenhydramine is a first generation anti-histamine. This class in general has antagonistic effects on other receptors like, muscarinic, alpha, and serotonin receptors. The non-specific effects on muscarinic receptors can be used to treat other disease states like motion sickness.

A 47-year-old man is having trouble sleeping because his seasonal allergies are keeping him awake. Which drug listed below can be used to decrease the effect of histamine and has relatively pronounced sedative side effects? a Cetirizine b Doxylamine c Fexofenadine d Loratadine e Triamcinolone

Doxylamine is a first generation antihistamine and the rest are second generation. Second generation drugs are associated with less CNS effects as compared to first generation drugs.

Which drug is the most likely to cause arrhythmias? a Albuterol b Epinephrine c Formoterol d Ipratropium bromide e Terbutaline

Epinephrine is a non-selective adrenergic receptor agonist. It has high affinity for beta-1 receptors, which can result in tachycardia and arrhythmias.

A 43-year-old man will begin treatment with oral albuterol to control his symptoms of asthma. Which of the following adverse effects is most likely to occur with this form of therapy? a Diarrhea b Diuresis c Peptic ulcer disease d Severe itching e Tachycardia

Even though albuterol is selective for beta-2 receptors it can still activate beta-1 receptors on the heart at higher doses to produce tachycardia.

A 48-year-old truck driver is suffering from nasopharyngeal and ocular itching, sneezing, and watery rhinorrhea. He is prescribed a medication that blocks H1 receptors and has poor lipid solubility. Which drug was used on this patient? a Cromolyn b Diphenhydramine c Fexofenadine d Phenylephrine e Salmeterol

Fexofenadine is a second generation antihistamine with less CNS penetration.

Which statement is true regarding histamine receptor (H1) blockers? a Are safe to use during pregnancy b Are used to reduce gastric acid secretion c Drugs in this class are not associated with any adverse cardiac effects d First generation drugs have more CNS (central nervous system) effects e Second generation drugs are used for motion sickness

First generation drugs have more CNS (central nervous system) effects

A 15-year-old male with moderate asthma is told to gargle and spit after inhaling a Albuterol b Omalizumab c Theophylline d Flunisolide e Zileuton

Flunisolide is a glucocorticoid with potent immunosuppressant effects, which may allow opportunistic organism to produce infections in the mouth and throat.

Which of the following inhalant drugs has the most prolonged bronchodilation effects? a Albuterol b Epinephrine c Isoproterenol d Formoterol e Terbutaline

Formoterol and salmeterol are long acting beta-2 agonist.

Albuterol-induced activation of beta-adrenergic receptors produces which sequence of events to increase in heart rate? a Gi (activation) ==> inhibition of potassium channels b Gq (activation) ==> phospholipase C (activation) ==> Ip3 production ==> intracellular Ca++ increase ==> Calcium-calmodulin-kinase (activation) c Gs (activation) ==> adenylyl cyclase (activation) ==> cAMP production ==> PKA (activation) d Gq (activation) ==> stimulation of nitric oxide synthase ==> nitric oxide release e Guanylyl cyclase activation ==> cGMP production ==> phosphatase (activation)

Gs (activation) ==> adenylyl cyclase (activation) ==> cAMP production ==> PKA (activation)

What class of drugs are the first choice for the treatment of hay fever and urticaria? a Beta 2 adrenoceptor agonists b Doxycycline c H1 histamine receptor antagonists d H2 histamine receptor antagonists e 5HT1 serotonin receptor agonists

H1 histamine receptor antagonists

Blockade of which receptor listed below would be most useful to treat allergic rhinoconjunctivitis? a Alpha-1 adrenergic receptors b Beta-1 adrenergic receptors c Beta-2 adrenergic receptors d H1- histamine receptors e H2 -histamine receptors

H1- histamine receptors

Regarding its effects on smooth muscle, which of the following is a physiological antagonist of histamine? a Epinephrine b Fexofenadine c Nedocromil d Salmeterol e Serotonin

Histamine activates H1 receptors on the vasculature to produce vasodilation (indirectly via NO production and release) and bronchoconstriction (directly through Gq mediated Ip3 production). Epinephrine can produce vasoconstriction via activation of alpha-1 receptors and an increase in cardiac output (beta-1 receptor activation). The activation of beta-2 receptors on the lung produces relaxation. These opposing changes on the CV and respiratory systems are examples of physiologic antagonism to the hypotensive and bronchoconstrictive effects of histamine.

A 45-year-old male with chronic-obstructive-pulmonary-disease is treated with an inhaled-quaternary-amine-muscarinic-antagonist... a Ipratropium b Beclomethasone c Zileuton d Salmeterol e Theophylline

Ipratropium

A 50-year-old patient with chronic obstructive pulmonary disease is treated with an inhaled drug that has poor oral bioavailability and CNS penetration a Atropine b Ipratropium c Pilocarpine d Neostigmine e Mecamylamine

Ipratropium

Ipratropium bromide is beneficial in asthma, because it a.Inhibits adrenergic effects on bronchi b.Stimulates vagal effects on bronchi c.Inhibits the effects of acetylcholine in the bronchi d.Inhibits cytokine production e.Inhibits mast cell degranulation

Ipratropium and the longer acting tiotropium are quaternary amine (doesn't pass readily through lipid bilayers) that block muscarinic receptors. In this case the M3 receptors on the lungs are antagonized preventing acetylcholine from activating these receptors. This blocks vagal induced bronchoconstriction and mucous secretion. Note. These drugs are reserved for acute asthmatic attacks in combination with beta 2 drugs and glucocorticoids. They are the primary drugs to treat COPD.

A patient with allergic rhinoconjunctivitis produced by allergen-induced histamine release would most likely be treated with which one of the following? a Bromocriptine b Dinoprostone c Epinephrine d Loratadine e Methysergide

Loratadine

A 72-year-old patient has trouble urinating because of his benign prostatic hyperplasia (BPH). He is suffering from seasonal allergies (allergic rhinitis) and his physician prescribes to him a drug to treat his allergies with the least amount of antimuscarinic side effects. Which drug was used? a Carbinoxamine b Diphenhydramine c Loratadine d Promethazine e Theophylline

Loratadine: loratadine, a second generation antihistamine, has less effects on other receptors as compared to first generation antihistamines like diphenhydramine, carbinoxamine and promethazine. First generation antihistamines, in general, have antagonistic effects on other receptors like, muscarinic, alpha, and serotonin receptors. The non-specific effects on muscarinic receptors can be an unwanted side effect. In this case prevention of sphincter relaxation can exacerbate his symptoms of urinary hesitancy.

A 48-year-old suffers from motion sickness decides to take a medication that contains in part a histamine antagonist that also has antimuscarinic properties. Which drug listed below was in this medication? a Cetirizine b Meclizine c Fexofenadine d Loratadine e Terfenadine

Meclizine. First generation antihistamines have more CNS penetration and more non-specific receptor effects.

Activation of beta 2-adrenergic receptors by norepinephrine produces smooth muscle relaxation via an intracellular cascade that results in the phosphorylation and inhibition of function of which protein? a Beta-adrenergic receptor kinase b Myosin light chain kinase c Voltage gated sodium channels d Voltage gated potassium channels e Voltage gated calcium channels

Myosin light chain kinase is required for contraction in smooth muscle cells. When it is phosphorylated by PKA it becomes inhibited.

Nedocromil is used for the prophylactic treatment of asthma. It has as its major action a Block of calcium channels b Block of mediator release from mast cells c Sedation d Stimulation of cortisol release by the adrenals e Stimulation of beta2-adrenoceptors

Nedocromil inhibits the degranulation of mast cells. Cromolyn and nedocromil alter chloride conductance in mast cells reducing degranulation (histamine release). Based on this mechanism of action it is used ONLY prophylactically. It can be used for allergic rhinitis and as a before treatment for things like exercise induced asthma.

A 15-year-old male with persistent severe asthma is treated with a drug that is used in combination with other drugs because of its ability to lowers IgE to undetectable levels by inhibiting the binding of IgE to mast cells a Albuterol b Omalizumab c Theophylline d Triamcinolone e Zileuton

Omalizumab

A 14-year-old boy with severe persistent asthma is treated with a beta-2 agonist inhaler as well as a glucocorticoid inhaler. Unfortunately, he still suffers from frequent asthmatic attacks. His physician prescribes an additional drug that lowers IgE levels when injected every month. Which drug was added to his regimen? a Albuterol b Ipratropium c Montelukast d Nedocromil e Omalizumab

Omalizumab is a monoclonal antibody against IgE. Once or twice a month injections are administered to reduce IgE levels.

A 48-year-old man with seasonal allergic rhinitis uses a nasal spray to treat his mild symptoms. The intranasal spray contains a drug that activates alpha-1 adrenergic receptors. Which drug was used? a Cromolyn b Diphenhydramine c Fexofenadine d Phenylephrine e Salmeterol

Phenylephrine

Which statement regarding cromolyn is CORRECT? a.Relaxes the bronchial smooth muscle directly b.Prevents bronchoconstriction caused by exercise c.Inhibits muscarinic action on smooth muscle d. Is used for the treatment for acute asthmatic attacks e.Stimulates the degranulation of mast cells

Prevents bronchoconstriction caused by exercise. Cromolyn and nedocromil alter chloride conductance in mast cells reducing degranulation (Histamine release). Based on this mechanism of action it is used ONLY prophylactically. It can be used for allergic rhinitis and as a before treatment for things like exercise induced asthma.

A 45-year-old male with severe persistent asthma in addition to the drugs he is currently using is prescribed a long-duration beta-2 agonist. Which drug was prescribed? a Ipratropium b Beclomethasone c Zileuton d Salmeterol e Theophylline

Salmeterol

A long-acting beta-2-adrenegic receptor agonist that is used in combinations with glucocorticoids for the treatment of poorly controlled moderate persistent asthma is which of the following a Albuterol b Budesonide c Epinephrine d Nedocromil e Salmeterol

Salmeterol

Which of the following is a very long acting beta 2-adrenoceptor selective agonist that is used for asthma prophylaxis? a Cromolyn b Omalizumab c Prednisone d Salmeterol e Zileuton

Salmeterol and formoterol are long-acting beta 2 adrenoceptor agonists that are used in combination with glucocorticoids for moderate to severe asthma.

Beta-2 receptor agonists are used chiefly to produce a Bronchoconstriction b Increase cardiac output c Smooth muscle relaxation d Reduce intraocular pressure e Uterine contraction

Smooth muscle relaxation. Beta-2 receptors located on smooth muscle (lungs, vasculature, uterus, and gut walls) activate intracellular cascades that inhibit myosin light chain kinase.

Inhaled ipratropium bromide has the following properties, EXCEPT a Competitively inhibits the effects of acetylcholine b Bronchial effects are similar to those of atropine c Inhibits bronchoconstriction d Inhibits mucus secretion e Systemic toxicities are similar to those of atropine

Systemic toxicities are similar to those of atropine: The principle difference between atropine and ipratropium is that atropine is a tertiary amine that can cross the gut and blood brain barrier depending on the pH. Therefore, inhaled atropine can be absorbed across the gut and into the brain to produce more systemic toxicities as compared to the lipid insoluble quaternary amine, Ipratropium.

Which of the following is a methylxanthine drug? a Beclomethasone b Nedocromil c Montelukast d Terbutaline e Theophylline

Theophylline along with Caffeine and Theobromine are methylxanthine. These drugs have a molecular shape similar to adenosine and can alter the activity of enzymes like phosphodiesterases and receptors involved in adenosine signaling.

Because of its narrow therapeutic window, the plasma concentration of one of the following drugs should be determined in patients. Which drug is it? a Theophylline b Nedocromil c Albuterol d Zafirlukast e Budesonide

Theophylline: Theophylline is a phosphodiesterase inhibitor. Phosphodiesterases are a family of enzyme is responsible for breaking down cyclic nucleotides like cGMP and cAMP into the open monophosphate forms. Theophylline is a relatively non-specific phosphodiesterase inhibitor so it will increase cAMP in the lung to produce smooth muscle relaxation. It will also increase cAMP in the heart that can result in tachycardia and in the vasculature that will result in vasodilation. These later two effects can lead to arrhythmias or severe hypotension. Therefore, it is important to measure plasma levels of theophylline because of its narrow therapeutic window.

A 65-year-old patient with chronic obstructive pulmonary disease is prescribed a drug that produces bronchodilation by blocking muscarinic receptors. a Albuterol b Tiotropium c Montelukast d Nedocromil e Omalizumab

Tiotropium Tiotropium and ipratropium are both quaternary amine muscarinic antagonists used to treat COPD. Tiotropium is the long-acting-drug with the half-life of days while ipratropium has a half life of hours.

The mechanism of action of zileuton is similar to that of a. Beclomethasone b.Ipratropium bromide c. Terbutaline d. Cromolyn e. Zafirlukast

Zileuton inhibits the enzyme, 5' lipoxygenase, responsible for the production of leukotrienes associated with inflammation and bronchoconstriction. The other drug that affects leukotriene function is zafirlukast (leukotriene receptor antagonist--notice the ast ending which looks like an abbreviation for antagonist).

Which of the following anti-asthma drugs inhibits the 5-lipoxygenase-- an enzyme involved in the synthesis of leukotrienes? a Aminophylline b Nedocromil c Salmeterol d Terbutaline e Zileuton

Zileuton inhibits the enzyme, 5' lipoxygenase, responsible for the production of leukotrienes associated with inflammation and bronchoconstriction. The other drug that affects leukotriene function is zafirlukast and montelukast (leukotriene receptor antagonist--notice the ast ending which looks like an abbreviation for antagonist).

Which of the following drug reduces aspirin-induced asthma by inhibiting the shift of arachidonic acid metabolism from the prostaglandin pathway to the leukotriene pathway? a Budesonide b Formoterol c Nedocromil d Theophylline e Zileuton

Zileuton inhibits the enzyme, 5' lipoxygenase, responsible for the production of leukotrienes associated with inflammation and bronchoconstriction. Arachidonic acid is the precursor for both cyclooxygenase and lipoxygenase pathways. When cyclooxygenase is inhibit the arachidonic acid can be fed into the lipoxygenase pathway.

A14-year-old boy with mild intermittent asthma is prescribed a drug to be used when he is experiencing an episode of asthmatic symptoms. The drugs principal mechanism of action is to stimulate the intracellular production of cAMP in bronchiolar smooth muscle cells. a Albuterol b Ipratropium c Montelukast d Nedocromil e Omalizumab

albuterol This drug is a beta-2 specific agonist. Beta 2 receptors when activated produce the following cascade: Gs (activation) ==> adenylyl cyclase (activation) ==> cAMP production ==> PKA (activation)==> PKA phosphorylation and inhibition of Myosin light chain kinase.

A 14-year-old female with moderate persistent asthma is currently uses a beta-2 adrenergic receptor agonist on an as needed basis. Which drug would you most likely prescribe below to reduce airway inflammation and reduce lung fibrosis associated with untreated asthma? a Albuterol b Budesonide c Epinephrine d Nedocromil e Theophylline

budesonide

Histamine binding to the histamine receptor (subtype 1) produces which of the following responses? a bronchodilation b Central nervous system depression c gastric acid secretion d production of cAMP (intracellular messenger) e vasodilation

vasodilation--via the stimulation of NO production , diffusion into smooth muscle cells of the vasculature and subsequent activation of cGMP in SM cells.