Pulmonary Pharmacology

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Questions and Answers

In managing chronic obstructive pulmonary disease (COPD), which pharmacological approach is considered the mainstay treatment, reflecting the disease's primary pathophysiology?

  • Employing mucolytic agents to enhance airway clearance and reduce hyperinflation.
  • Utilizing inhaled corticosteroids to directly reverse alveolar wall destruction.
  • Administering bronchodilators to alleviate airflow limitations via smooth muscle relaxation. (correct)
  • Prescribing leukotriene receptor antagonists to counteract the inflammatory response.

A patient with a history of cardiac arrhythmias is prescribed albuterol for acute bronchospasm. Which of the following would be the MOST appropriate modification to their treatment regimen?

  • Administer a higher dose of albuterol via nebulization to ensure optimal bronchodilation.
  • Pre-treat with a beta-blocker to mitigate potential cardiac stimulation from albuterol.
  • Add an anticholinergic agent, such as ipratropium bromide, to counteract the cardiac effects of albuterol.
  • Switch to levalbuterol to potentially minimize the risk of cardiac side effects. (correct)

A patient with asthma requires frequent use of a short-acting beta-2 agonist (SABA) for symptom control. According to current asthma management guidelines, what adjustment is required to improve their treatment?

  • Initiate combination therapy with an inhaled corticosteroid (ICS) and long-acting beta-2 agonist (LABA). (correct)
  • Add an oral corticosteroid to the regimen for persistent symptom relief.
  • Prescribe a leukotriene receptor antagonist as an alternative to the short-acting beta-2 agonist.
  • Increase the dose of the short-acting beta-2 agonist to maximize bronchodilation.

For a patient experiencing an acute asthma exacerbation despite consistent use of inhaled corticosteroids and long-acting beta-2 agonists, which rescue bronchodilator strategy is now MOST recommended?

<p>Utilizing a combination of inhaled corticosteroid and formoterol as needed. (A)</p> Signup and view all the answers

The concurrent use of long-acting beta-2 agonists (LABAs) with inhaled corticosteroids in asthma management aims to exploit what synergistic therapeutic effect?

<p>Corticosteroids reduce the risk of asthma-related deaths associated with LABA monotherapy. (B)</p> Signup and view all the answers

Tolerance to the bronchoprotective effects of beta-2 agonists can be minimized through which concurrent medication?

<p>Continuous use of inhaled corticosteroids. (D)</p> Signup and view all the answers

A researcher is investigating the role of histamine receptors in modulating airway function. Activation of which histamine receptor subtype would MOST directly stimulate smooth muscle contraction within the bronchioles?

<p>H1 receptors. (D)</p> Signup and view all the answers

A patient is prescribed a first-generation H1 antihistamine for allergic rhinitis. What significant physiological effect, mediated by muscarinic acetylcholine receptors, might be inadvertently inhibited by this medication?

<p>Increased mucus production in the respiratory tract. (A)</p> Signup and view all the answers

A researcher aims to develop a novel therapeutic agent targeting histamine receptors to selectively promote wakefulness. Which histamine receptor subtype should be targeted as an antagonist to achieve this effect?

<p>H3 receptors. (D)</p> Signup and view all the answers

In a patient experiencing anaphylaxis, why are H1 receptor antagonists considered adjunctive and not primary therapy for managing bronchoconstriction?

<p>H1 antagonists are ineffective in blocking bronchoconstriction due to redundant autacoid pathways. (B)</p> Signup and view all the answers

A patient presents with allergic conjunctivitis. Which second-generation H1 antagonist possesses mast cell-stabilizing properties, potentially offering enhanced efficacy in this condition?

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

Montelukast can be used in acute prevention of exercise-induced bronchoconstriction (EIB). At what age is this therapy approved?

<p>≥ 6 years (D)</p> Signup and view all the answers

A patient with mild persistent asthma is prescribed montelukast. What is the mechanism of action of Montelukast?

<p>Binds with high affinity and selectivity to the CysLT1 receptor (B)</p> Signup and view all the answers

A patient presents with asthma symptoms poorly controlled by inhaled corticosteroids. Recognizing the role of leukotrienes in inflammation, what distinguishing characteristic suggests adding a leukotriene receptor antagonist (LTRA) to their treatment?

<p>Concurrent allergic rhinitis contributing to asthma exacerbations. (A)</p> Signup and view all the answers

A patient with COPD experiences persistent air trapping and exercise intolerance. Which bronchodilator, demonstrating a distinct mechanism of action, would be MOST effective in addressing these specific symptoms?

<p>Tiotropium bromide, a long-acting muscarinic antagonist. (C)</p> Signup and view all the answers

A patient with severe COPD is prescribed tiotropium bromide. What can be expected with such an administration?

<p>Bronchodilation by competitively inhibiting acetylcholine at muscarinic receptors in the airways (C)</p> Signup and view all the answers

While assessing a patient recently started on tiotropium for COPD, which finding would prompt the MOST immediate reassessment of their medication regimen?

<p>New-onset narrow-angle glaucoma. (B)</p> Signup and view all the answers

A patient with asthma and COPD demonstrates suboptimal bronchodilation with inhaled beta-2 agonists and anticholinergics. What rationale supports adding theophylline to their treatment regimen?

<p>Theophylline promotes adenosine receptor antagonism, counteracting bronchoconstriction. (A)</p> Signup and view all the answers

A patient with severe, refractory COPD exacerbations despite maximal bronchodilator therapy is considered for roflumilast. What fundamental risk assessment is essential prior to initiating this medication?

<p>Assessment for pre-existing psychiatric conditions. (D)</p> Signup and view all the answers

A patient with severe persistent asthma exhibits elevated IgE levels and allergy symptoms despite consistent inhaled corticosteroid use. What pharmacological actions will anti-IgE receptor therapy exert in this patient?

<p>Block IgE binding on mast cells and basophils, attenuating mediator release. (B)</p> Signup and view all the answers

A researcher investigates the potential of benzonatate in alleviating cough. Through what primary mechanism does benzonatate reduce the urge to cough?

<p>Anesthetizing stretch receptors in respiratory passages. (B)</p> Signup and view all the answers

What is a major mechanistic distinction between first- and second-generation H1 receptor antagonists relevant to their clinical use and noted side effect profiles?

<p>First-generation agents readily cross the blood-brain barrier, causing sedation. (C)</p> Signup and view all the answers

A patient with allergic rhinitis seeks long-term symptom relief. What would be an appropriate initial treatment approach?

<p>Initiating nasal steroids gradually to reduce inflammation (C)</p> Signup and view all the answers

A patient previously managed on inhaled corticosteroids for asthma develops oral candidiasis. What adjustment would minimize future occurrences while maintaining therapeutic benefit?

<p>Using a spacer device with the inhaled corticosteroid. (D)</p> Signup and view all the answers

For managing allergic rhinitis with concomitant nasal congestion, what is the rationale to initially selecting a combination therapy over nasal antihistamines and nasal steroids?

<p>Combination treatments have demonstrated superior effects in the topical treatment of allergic conjunctivitis. (C)</p> Signup and view all the answers

A patient with severe asthma and documented aspirin sensitivity requires chronic anti-inflammatory management. Why are leukotriene-modifying agents sometimes favored over NSAIDs in these cases?

<p>Leukotriene modifiers do not inhibit COX enzymes. (D)</p> Signup and view all the answers

While treating mild intermittent asthma with albuterol, what is the potential negative feedback effect in this treatment?

<p>Leading to tolerance toward the medication with long-term use. (C)</p> Signup and view all the answers

A hematologist administers erythropoietin to a patient with anemia secondary to chronic kidney disease. What monitoring parameter is most critical to minimize detrimental cardiovascular outcomes?

<p>Continuous tracking of hematocrit increases. (D)</p> Signup and view all the answers

A dialysis patient treated with erythropoiesis stimulating agents (ESAs) is not achieving the expected hemoglobin response. What treatment is key to improving this scenario?

<p>Administering erythropoietin in conjunction with iron. (D)</p> Signup and view all the answers

In cancer patients receiving erythropoietin-stimulating agents (ESAs) to manage chemotherapy-induced anemia, what black box warning should guide the course of action?

<p>ESAs shorten survival and pose tumor progression risks. (B)</p> Signup and view all the answers

The cardiovascular adverse effects linked to selective COX-2 inhibitors are believed to relate to the disturbance they cause to levels of what?

<p>Suppression of cardioprotective COX-2-derived prostacyclin PGI2. (D)</p> Signup and view all the answers

In a patient with a history of myocardial infarction taking low-dose aspirin, what drug is more likely to interfere with the antiplatelet effect?

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

A patient receiving long-term NSAIDs are more likely to exhibit what physiological characteristic?

<p>Sodium and water retention. (B)</p> Signup and view all the answers

Considering ethical practice with the drug Misoprostol (arthrotec) what should be considered prior to the treatment?

<p>Pregnancy Status. (D)</p> Signup and view all the answers

When using glucocorticoids and PLA-2 there is:

<p>Synthesize a certain protein called Annexin. (B)</p> Signup and view all the answers

Which drug is used for long-term once daily maintenance of COPD?

<p>LAMA-Long Acting Muscarinic Agonist. (D)</p> Signup and view all the answers

What common drug is similar to Theophylline (Theodur)?

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

When the patient reports muscle pain after taking STATINS, which vitamin may cause the same risk to their patient?

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

The clinical effect of 5HT3 is a reduction in the effects to:

<p>GI contractility. (A)</p> Signup and view all the answers

Which of these drugs is most indicated for anti-inflammatory treatment and has shown some anti-ulcer properties?

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

Why should we not give Folic Acid to patients with B12 deficiency before proper diagnosis and treatment?

<p>B12 can prevent some B12 problems from showing. (C)</p> Signup and view all the answers

What side effect is mainly related to aluminum?

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

In the context of bronchodilator usage for managing respiratory conditions, what elucidates the rationale behind prioritizing direct inhalation over oral administration, considering both local and systemic effects?

<p>Inhalation maximizes local drug concentration in the airways while minimizing systemic exposure and side effects. (C)</p> Signup and view all the answers

When managing a patient with asthma who requires both a long-acting beta-2 agonist (LABA) and an inhaled corticosteroid (ICS), what critical consideration directs the prescribing strategy to ensure patient safety and therapeutic efficacy?

<p>Prescribing a combination inhaler containing both LABA and ICS to improve adherence and ensure anti-inflammatory effects. (D)</p> Signup and view all the answers

How do H1 and H2 receptors have opposing effects on smooth muscle cells in the respiratory tract?

<p>H1 receptors stimulate contraction by mobilizing intracellular calcium, whereas H2 receptors promote relaxation via cyclic AMP accumulation. (B)</p> Signup and view all the answers

What characteristic of theophylline is the MOST important limitation to consider when determining its clinical usefulness?

<p>The large interindividual variations in clearance and the potential for significant side effects related to plasma concentration. (B)</p> Signup and view all the answers

A patient with severe COPD and chronic bronchitis is being considered for roflumilast therapy. What is the MOST critical pathophysiological rationale guiding the use of roflumilast in this specific patient population?

<p>Roflumilast reduces exacerbations by inhibiting PDE4, which is the predominant PDE isoform in inflammatory and structural cells involved in COPD. (B)</p> Signup and view all the answers

What are the implications of omalizumab's mechanism of action in treating severe asthma for allergic conditions?

<p>Reduction in the frequency and severity of asthma attacks through decreased lymphocytic and eosinophilic inflammation. (C)</p> Signup and view all the answers

Regarding the mechanism through which benzonatate reduces coughing, what distinguishes its action from centrally acting antitussives?

<p>Benzonatate anesthetizes stretch receptors in the respiratory passages, thereby dampening their activity and reducing the cough reflex. (B)</p> Signup and view all the answers

When counseling a patient on the concurrent use of codeine-based antitussives, what potential physiological outcome creates the MOST concern?

<p>Depression of central respiratory drive. (C)</p> Signup and view all the answers

In what scenarios diclofenac is effective, but carries a range of safety considerations?

<p>Analgesic and antipyretic, limited effect on inflammatory reactions if not topical; may lead to impaired liver function; monitor for renal impairment. (A)</p> Signup and view all the answers

What is an advantage of treating a pt. on aspirin with an NSAID and why should this always be part of ethical practice?

<p>Ibuprofen, if taken 2 hours before aspirin, can block the antiplatelet effect and increase negative cardiac risks. (C)</p> Signup and view all the answers

Why do providers have such a high inclination to inform and not approve steroidal use of an injury unless completely specified first?

<p>If high doses may lead to cardiac risks and affect every organ. (C)</p> Signup and view all the answers

If a male client has limited iron in blood and the provider is suggesting iron supplements, what education is necessary for the patient to retain and what negative affects will the patient show initially if they are improving?

<p>The patients stools will be dark. Monitor reticulocyte, dose, and increase intake. (A)</p> Signup and view all the answers

When a provider needs to put a patient on a diuretic, specifically a Thiazide, what is the rationale to then prescribe vitamin D (cholecalciferol)?

<p>To assist absorption for calcium in the bones. (A)</p> Signup and view all the answers

If the patient is placed on hydrocortisone and then proceeds to ingest multiple antibiotics, what is the potential reasoning for this? (Select all that apply)

<p>There are multiple disease states that are being addressed at once. (A)</p> Signup and view all the answers

Which of the following statements BEST represents an integration with the data: What causes most issues with duodenal and peptic ulcers?

<p>An imbalance between mucosal defenses and factors, caused usually by NSAID and H. Pylori usage. (C)</p> Signup and view all the answers

Flashcards

Bronchodilators Mechanism

Relax airway smooth muscle, preventing bronchoconstriction.

Asthma Treatment

Involve bronchodilators and anti-inflammatory drugs.

COPD Treatment

Mainstay bronchodilators, inflammation corticosteroid-resistant.

MOA of Beta-2 Agonists

B2-selective agonists cause relaxation.

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SABA Use

Rapid-acting relief as needed.

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LABA Use

β2 agonists for long-term control with ICS.

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B2 Agonist Side Effects

Muscle tremor, tachycardia, hypokalemia.

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H1 Antagonist MOA

Constriction of respiratory smooth muscle.

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H3 Histamine Receptors

Mainly in CNS; wakefullness.

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H1 Antagonist Uses

Treat allergic reactions.

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Action of H1 Antagonists

Inhibit histamine effects.

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5-Lipoxygenase Inhibitor drug

Zileuton (Zyflo).

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Action

Muscarinic ACh

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Characteristics of LAMAs

Once daily.

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Side Effects of Muscarinic Antagonists

Dry mouth, urinary retention.

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Theophylline Class

Inhibits phosphodiesterases, adenosine effect, lower inflam.

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Side Effects of Theohylline

Range from headache and nausea to cardiac arrhythmias

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Action of Roflumilast

Reduces exacerbations in severe COPD.

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Omalizumab

High risk of anaphylaxis at any time, very expensive

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use with inhaled corticosteroids

Suppresses coughs in asthma.

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Action of Benzonatate/Tessalon

Anesthetizes stretch of respiratory tissue, thus cough reduction.

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Tessalon (Benzonatate)

Anesthetizes the sensors and relieves cough.

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Benefits of Nasal Steroid

Reducing mediator release

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Drug Class: Analgesic, antipyretic.

Aspirin

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Benzonatate action

Anesthetizes stretch receptors in respiratory tract, reducing cough source.

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Strauss Syndrome (rare vasculitis)

Can use to help in rare vasculitis.

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Steroid action in asthma

Anti-inflammatory

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Aspirin

Low-dose reduces risk of cardiac. Irreversible

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Acute phase - GOUT

Symptomatic for GOUT, NSAIDs or colchicine

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Iron Defiiency

May need more vitamin c 150-200-mg to help.

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Iron Defiinency

Avoid pregnancy and lactation.

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Diarrhea

Bismouth use Pepto

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Diahhrea?

Allerigic? Test done..Avoid if used with other medications

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Study Notes

  • Asthma as an inflammatory condition causes airway constriction. COPD induces respiratory inflammation, resulting in air trapping.
  • Asthma treatment utilizes bronchodilators, which relax airway smooth muscle, along with anti-inflammatory agents. Conversely, COPD primarily uses bronchodilators.

Pulmonary Pharmacology

  • Directly acting on the airways via inhalation is the preferred method, reducing systemic effects. Oral administration needs higher doses, and parenteral methods are reserved for critical cases.
  • β2 adrenergic agonists, theophylline, and anticholinergic agents are the primary classes of bronchodilators. Asthma presents a challenge due to structural changes and persistent inflammation. Corticosteroids are vital, although not a cure. COPD is made complex by progressive blockage of airflow and comorbidities.
  • Effective drug administration involves pressurized inhalers, dry powder inhalers, and nebulizers to deliver meds effectively. For meds through inhalers, spacers are important.
  • β2-selective agonists provide selectivity through structural modifications, leading to bronchial smooth muscle relaxation via the Gs-adenylyl cyclase-cAMP-protein kinase A pathway.
  • Inflammatory cell mediators are indirectly inhibited by the release of bronchoconstrictors, which lead to reduced mucosal edema.
  • Additional effects of β2 agonists include neurotransmission reduction, mucus production and the prevention of microvascular leakage.
  • Submucosal glands see an increase in mucus production and ion transport. The enhanced mucociliary clearance addresses defects found with COPD and Asthma.
  • Short-acting B2 agonists (SABAs) act as rescue drugs, and long-acting B2 agonists (LABAs) act as control drugs.

SABAs

  • Inhaled SABAs are rapid-acting bronchodilators used for immediate symptom relief and acute therapy. If SABAs are needed too often, the therapy requires stepping up.
  • Common SABAs are albuterol (ProAir, Ventolin, Proventil ®) and levalbuterol (Xopenex ®), with cardiac activity reduced compared to albuterol. Metaproterenol (Alupent ®) is a liquid or nebulizer.

LABAs

Provide longer-lasting bronchodilation as control medications. This is often combined with inhaled corticosteroids (ICSs) for improved benefits and adherence.

  • Elevated lipid solubility results in a duration of 12+ hours as a result of smooth muscle cell membranes. Combination drugs offer synergy.
  • Inflammation is not addressed by them, they should only be used in conjunction with ICS in Asthma to prevent death. Combined ICS is always essential.
  • Combining formoterol with ICS is recommended as a rescue bronchodilator for asthma for effectiveness and avoiding the use of short-acting β2 agonists due to potential risks of overuse.
  • Compared to salmeterol, formoterol is faster relative to salmeterol due to its intermediate lipid solubility.

B2 Agonists

  • Muscle tremor, tachycardia, hypokalemia, restlessness and ventilation-perfusion mismatch are all dose-related AEs.
  • Corticosteroids help in tolerance prevention, while smooth muscle tolerance is rare.

HI Antihistamines

Have differing sedation levels, uses and a side-effect profile when compared First-vs-Second-Generation H1-antihistamines. Histamine, Bradykinin, and Their Antagonists are also of concern.

  • Stimulation of eNOS production in vascular endothelium caused by histamine release leading to vasodilation.
  • Contractile effects to smooth muscle receptors, whereas activation of H2 receptors causes relaxation. Both receptors are found in the periphery and CNS.
  • Located in specialized parts of the brain such as the basal ganglia, hippocampus, and cortex and promoting wakefulness.
  • Four histamine receptors (H1-H4) are located throughout the body and have different physiological roles.
  • Antagonists block histamine receptors and offer therapy with allergies, gastric acid production and urticaria.
  • The histamine processes and effects can play a central role in allergic responses, immediate hypersensitivity responses and the modulation of smooth muscle.

H1 receptor antagonists

  • Reduce capillary permeability and action on smooth muscle along nerve endings and should be antagonized by H1 receptors.
  • Allergic reactions, skin conditions and motions sickness can be treated.
  • First-generation drugs often have adverse effects of sedation, while second-generation have fewer side effects. Those in geriatrics are preferred due to reduced sedation.
  • The first-generation antihistamines can cause significant learning and cognitive issues and are not indicated. Benadryl is the most widely used.
  • Olopatadine, loratadine, and cetirizine cause fewer sedative impacts, allergic rhinitis and conjunctivitis are indicated for treatment.
  • Stabilization of mast cells is induced with anti-inflammatory properties - 1st gens include benadryl. This is key in reducing allergic episodes.
  • First-generation tend to inhibit mucosic secretions - causes less or dry mouth. H1 antagonist uses:
  • Anaphylaxis, urticaria, motion sickness and sedation caused by allergies.
  • Smooth muscle, endothelium and nerve ending activity,
  • Inhibit increased capillary permeability and formation of edema. Flare, itch, and reduces secretions. Effects of long term use aren't known, but can be used for topical treatment. and inflammation,
  • Dizziness and fatigue are common side effects. Antihistamine are good for long term effects.
  • The potential for falls and CNS stimulation, should be approached cautioned in geriatrics.

Leukotriene Receptor Antagonists (LTRAS)

Inhibits 5-lipoxygenase and leukotrienes. Typically given orally and treats chronic asthma.

  • Prevents mucus secretion, release of histamine, bronchoconstriction and chemotaxis.
  • Inhibits airway inflammation and leukocyte activation.
  • Not intended to provide benefits for asthma flare-ups (e.g., used as control medications and not rescue ones). Montelukast is an indication.

Muscarinic Antagonists

Short-acting/Long acting muscarinic antagonists:

  • SAMA - Ipratropium
  • LAMA - Tiotropium.
  • The short/ long-acting muscs act on the nicotinic receptors. Act on <3 muscarinic receptors from acetylcholine blocking for bronchodilation. SAMAs/LAMAs:
  • Can produce some relief from bronchoconstriction, and reduce mucus secretion.
  • These often effective to help with asthma in severe forms (add-on therapy).
  • SE dry mouth, urinary retentions seen esp in elderly.
  • Less effective on asthmatics.

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