Pharmacology: H1RAs vs H2RAs
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Questions and Answers

Under what circumstances should cough suppression be used?

  • For productive cough to enhance secretion clearance
  • For any type of cough to promote rest
  • Whenever a patient experiences severe coughing fits
  • Only for nonproductive cough or at night when needed (correct)

What distinguishes antitussives from expectorants?

  • Expectorants suppress the cough reflex.
  • Antitussives are cough suppressants for nonproductive coughs. (correct)
  • Antitussives are typically used for productive coughs.
  • Expectorants are used primarily for dry throat relief.

What is the primary role of intranasal corticosteroids?

  • To relieve acute symptoms by blocking histamine
  • To directly treat cough caused by infections
  • To enhance mucus production for easier cough clearance
  • To prevent and decrease symptoms by lowering inflammatory mediators (correct)

What is a significant benefit of nasal antihistamines?

<p>They have a rapid onset and reduce airway hyperreactivity. (C)</p> Signup and view all the answers

How do leukotriene modifiers work in allergy treatment?

<p>By decreasing smooth muscle contraction and inflammatory response (C)</p> Signup and view all the answers

What is the Black Box Warning associated with Montelukast (Singulair)?

<p>Risk of mood changes and suicidal ideation (C)</p> Signup and view all the answers

Which class of drugs is typically not appropriate for young children under 2 years old?

<p>Opioids for cough suppression (B)</p> Signup and view all the answers

What is the role of 2nd generation oral antihistamines?

<p>To relieve acute allergy symptoms by blocking histamine action (C)</p> Signup and view all the answers

Which intranasal corticosteroid is categorized as safe during pregnancy?

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

What is the main concern regarding chlorpheniramine when used in large doses during breastfeeding?

<p>Infant sedation and reduced milk supply (C)</p> Signup and view all the answers

Doxylamine is known for its safety in which context?

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

What precaution should be taken when administering codeine to breastfeeding mothers?

<p>Monitor for sedation and respiratory difficulties (A)</p> Signup and view all the answers

Which decongestant is associated with an increased risk of gastroschisis when used in the first trimester?

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

Which of the following medications should be avoided during lactation due to safety concerns?

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

What is the recommended first-line antihistamine for breastfeeding mothers?

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

What is a potential adverse effect of using Oxymetazoline for more than three days?

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

Which antitussive medication has questionable effectiveness and potential risks in the first trimester?

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

What should be considered first when treating acute congestive episodes in pregnancy?

<p>Intranasal saline sprays (C)</p> Signup and view all the answers

What are the potential side effects associated with the prolonged use of inhaled corticosteroids?

<p>Risk of bone loss (D)</p> Signup and view all the answers

Why is it important to taper off glucocorticoids gradually?

<p>To prevent adrenal crisis (A)</p> Signup and view all the answers

What is a major concern regarding the use of inhaled corticosteroids in children?

<p>Reduction in growth velocity (D)</p> Signup and view all the answers

How do mast cell stabilizers function in asthma treatment?

<p>They block the release of certain inflammatory mediators (D)</p> Signup and view all the answers

Which of the following statements correctly describes the role of SABAs in asthma treatment?

<p>They provide quick relief from symptoms (B)</p> Signup and view all the answers

What does a narrow therapeutic index indicate regarding medication use?

<p>Higher risk for toxicity (C)</p> Signup and view all the answers

What caution should be taken when using inhaled corticosteroids in patients with a history of eye diseases?

<p>Routine eye exams are advised, but they are safe (C)</p> Signup and view all the answers

What is a common adverse effect of monoclonal antibodies in asthma treatment?

<p>Risk of anaphylaxis (C)</p> Signup and view all the answers

What is a primary use of oral corticosteroids in COPD management during acute exacerbations?

<p>To reduce treatment failure and improve lung function (A)</p> Signup and view all the answers

Which of the following is a potential side effect of Phosphodiesterase-4 (PDE4) inhibitors?

<p>Hepatotoxicity and neuropsychiatric effects (B)</p> Signup and view all the answers

What role do antibiotics play in the management of COPD according to recent studies?

<p>They may decrease exacerbation rates due to their anti-inflammatory properties. (B)</p> Signup and view all the answers

What is a necessary consideration when prescribing mucolytics to COPD patients?

<p>They may not be effective in patients already on ICS treatment. (B)</p> Signup and view all the answers

Which patients are recommended to consider the use of Phosphodiesterase-4 (PDE4) inhibitors?

<p>Patients with chronic bronchitis on maximal inhaled therapy. (C)</p> Signup and view all the answers

What is a significant disadvantage of using metered-dose inhalers (MDIs)?

<p>Deliver only about 10% of the drug to the lungs (A)</p> Signup and view all the answers

What is the primary reason why long-acting beta2 agonists (LABAs) are used in combination with inhaled corticosteroids?

<p>They pose an increased risk of asthma-related deaths if used alone (B)</p> Signup and view all the answers

Which medication type is classified as a controller in asthma management?

<p>Inhaled corticosteroids (ICS) (D)</p> Signup and view all the answers

Why might patients with diabetes mellitus need to be cautious with beta2 agonists?

<p>They can potentially increase serum glucose levels (B)</p> Signup and view all the answers

What is a notable advantage of using dry powder inhalers (DPIs) compared to metered-dose inhalers (MDIs)?

<p>They deliver approximately 20% of the drug to the lungs (B)</p> Signup and view all the answers

In what way are oral glucocorticoids typically administered during asthma exacerbations?

<p>In short bursts to provide immediate coverage (B)</p> Signup and view all the answers

What are the main roles of inhaled corticosteroids in asthma treatment?

<p>They decrease inflammation and control symptoms (B)</p> Signup and view all the answers

Which type of device does not require hand-breath coordination for administration?

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

What is one of the potential serious adverse effects of Varenicline?

<p>Increased risk for neuropsychiatric effects (B)</p> Signup and view all the answers

What is the primary mechanism of action of Bupropion SR (Zyban) in smoking cessation?

<p>Inhibits neuronal uptake of norepinephrine and dopamine (C)</p> Signup and view all the answers

Which statement regarding the use of Bupropion during pregnancy is correct?

<p>Bupropion and its metabolites cross the placenta. (B)</p> Signup and view all the answers

What is a notable side effect of Varenicline related to alcohol?

<p>Enhancement of alcohol's sedative effects (D)</p> Signup and view all the answers

Which of the following is a Black Box Warning associated with Bupropion SR (Zyban)?

<p>Suicidal thoughts and behavior in young individuals (B)</p> Signup and view all the answers

Flashcards

Drug therapy for cough (indications)

Use cough suppressants (antitussives) for non-productive coughs or nighttime rest. Avoid opioids in those with substance abuse history or COPD, and avoid OTC cough and cold meds in those under age 2.

Antitussive vs. Expectorant

Antitussives suppress coughing (nonproductive coughs), while expectorants thin secretions to help clear a productive cough.

Allergy Controllers

Prevent allergy symptoms. Examples: intranasal corticosteroids (e.g., Flonase) and leukotriene modifiers (e.g., Singulair).

Allergy Relievers

Relieve allergy symptoms quickly by blocking histamine. Examples: oral antihistamines (e.g., Claritin), intranasal or ocular antihistamines.

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Nasal Antihistamine Benefits

Quick symptom relief and reduced airway hyperreactivity.

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Leukotriene Modifiers (Mechanism)

Decrease smooth muscle contraction, vessel permeability and inflammation, reducing allergy symptoms, most effective at bedtime.

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Leukotriene Modifier Black Box Warning

Potential for serious mental health adverse effects (agitation, aggression, suicidal thoughts, etc.).

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Allergy Treatments during Pregnancy/Lactation

Limited information provided, consider other treatments.

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1st line treatment for allergic rhinitis in pregnancy

Intranasal corticosteroids are the most effective treatment for allergic rhinitis, and are a first-line medication choice during pregnancy.

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Intranasal corticosteroid example (pregnancy category B)

Budesonide (Rhinocort) is a corticosteroid considered safe during pregnancy (category B).

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Category C intranasal corticosteroids

Beclomethasone, Flunisolide, and others fall into category C intranasal corticosteroids. Safety during lactation is uncertain.

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Decongestant use limitation (pregnancy)

Decongestants like pseudoephedrine are NOT a first-line rhinitis treatment during pregnancy.

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First-line antihistamine (breastfeeding)

Chlorpheniramine is often the first-line antihistamine due to its safety profile. Cetirizine is an alternative non-sedating option.

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Antihistamine caution (breastfeeding)

Large doses or prolonged use of some antihistamines can reduce breast milk supply.

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Codeine classification (pregnancy)

Codeine is a category C antitussive, which raises some caution and concerns about possible fetal effects during pregnancy.

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Guaifenesin classification (pregnancy)

Guaifenesin, a category C antitussive, may be associated with birth defects in the first trimester, although infant exposure is generally lower.

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Dextromethorphan classification (pregnancy)

Dextromethorphan is a category C antitussive with limited studies on infant effects. Limited data on usage during pregnancy and breastfeeding.

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Decongestant delivery preference (pregnancy)

Prefer nasal over oral decongestants for rhinitis treatment in pregnancy to limit potential systemic effects.

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MDIs

Handheld devices delivering measured drug doses with each actuation. Require hand-breath coordination. Only ~10% reaches the lungs.

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DPIs

Deliver dry, micronized powder directly to the lungs. No hand-breath coordination needed. ~20% reaches the lungs.

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Nebulizers

Convert drug solution into a fine mist. Greater drug deposition in lungs, less in oropharynx. No hand-breath coordination needed.

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Asthma Controllers

Prevent and control symptoms by reducing inflammation, controlling symptoms, and reducing future risks. Includes ICS, leukotriene modifiers, and ICS combined with LABAs

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Asthma Relievers

Provide quick relief from acute asthma symptoms and exacerbations. Includes SABAs, SAMAs, and oral corticosteroids.

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Steroids in Asthma

Oral steroids are used in short bursts for exacerbations. Inhaled steroids are the mainstay of maintenance therapy. They decrease inflammation, provide bronchodilation, and decrease airway mucus production.

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Long-acting Beta2 Agonists (LABAs) in Asthma

Not used as monotherapy in asthma due to increased risk of death. Used in combination with inhaled corticosteroids for sustained bronchodilation. Do not provide quick relief.

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Albuterol and QT Prolongation

Albuterol (a beta2 agonist) can prolong the QT interval.

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Hypothalamic-Pituitary-Adrenal (HPA) Axis Suppression

A condition where the body's stress response system is weakened due to prolonged use of corticosteroids, causing various side effects.

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Adrenal Crisis

A life-threatening condition that can occur when the body is suddenly deprived of cortisol, often due to abrupt withdrawal of corticosteroids.

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Inhaled Corticosteroids: Bone Loss

Prolonged use of high-dose inhaled corticosteroids can increase the risk of bone loss.

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Inhaled Corticosteroids: Eye Concerns

Inhaled corticosteroids can increase intraocular pressure, which can worsen conditions like cataracts and glaucoma.

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Inhaled Corticosteroids: Tapering Off

Gradually reducing the dose of inhaled corticosteroids is essential to prevent withdrawal symptoms.

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Mast Cell Stabilizers: Role in Asthma

Mast cell stabilizers prevent the release of inflammatory chemicals from mast cells, reducing bronchoconstriction.

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Narrow Therapeutic Index

A medication with a narrow therapeutic index has a small difference between the effective dose and the toxic dose.

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Monoclonal Antibodies: Asthma Treatment

Monoclonal antibodies target specific proteins involved in the inflammatory process, reducing asthma symptoms.

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Varenicline: Dopamine Impact

Varenicline works by blocking nicotine from stimulating the dopamine system in the brain, which is associated with addiction.

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Varenicline: Side Effects

Varenicline can cause serious side effects, including increased risk of suicidal thoughts, depression, hostility, and worsening of alcohol-related problems.

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Bupropion SR: Mechanism

Bupropion SR works by inhibiting the reuptake of dopamine and norepinephrine, chemicals that regulate mood and motivation.

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Bupropion SR: Side Effects

Bupropion SR can lead to severe side effects, such as suicidal thoughts and behavior, especially in children, adolescents, and young adults.

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Smoking Cessation in Pregnancy

Bupropion is not recommended for smoking cessation during pregnancy due to limited safety data and potential risks.

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PDE4 Inhibitors for COPD

PDE4 inhibitors can be used in COPD patients with chronic bronchitis or those on maximal inhaled therapy. They may reduce inflammation, especially in patients with high eosinophilia counts or an asthma component.

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PDE4 Inhibitor Adverse Effects

PDE4 inhibitors can cause side effects like diarrhea, nausea, weight loss, sleep disturbances, and potential liver problems. They may also have neuropsychiatric effects, including anxiety, depression, and insomnia.

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Antibiotics for COPD

Regular use of antibiotics in COPD patients may help reduce exacerbation rates, likely due to their anti-inflammatory properties.

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Mucolytics for COPD

Mucolytics can help thin mucus in COPD patients, especially those not receiving inhaled corticosteroids, potentially reducing exacerbations and improving overall health.

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When to Use Oral Corticosteroids in COPD?

Oral corticosteroids are used for treating acute COPD exacerbations in hospitalized patients or during emergencies, as they can reduce treatment failures, relapse rates, and improve lung function and breathing difficulties.

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Study Notes

H1RAs vs H2RAs

  • H1RAs bind selectively to H1 receptors, blocking histamine actions at these sites
  • H1RAs have low receptor specificity, interacting with both peripheral and central histamine receptors
  • H1RAs readily cross the blood-brain barrier
  • H2RAs selectively block H2 receptor sites, reducing gastric acid secretion
  • H2RAs are useful for treating gastric ulcers and GERD (e.g., cimetidine, famotidine)

Histamine Receptor Antagonist Generations

  • First-generation H1 receptor antagonists cross the blood-brain barrier, causing sedation
  • Second-generation H1 receptor antagonists do not significantly cross the blood-brain barrier, avoiding sedation (except for cetirizine/Zyrtec)

Anticholinergic Side Effects

  • Sinus tachycardia, dry skin, dry mucous membranes, dilated pupils, constipation, ileus, urinary retention, and agitated delirium
  • Elderly, glaucoma, and BPH patients should avoid anticholinergic drugs

Anticholinergic Drugs

  • Oral decongestants (e.g., pseudoephedrine)
  • First-generation antihistamines (e.g., diphenhydramine)
  • Second-generation antihistamines (e.g., cetirizine, fexofenadine)

Cough and Cold Medicine Combination

  • Choose single-agent products to reduce overdose risk
  • Avoid unnecessary medications
  • Easier to identify allergens

Nasal Decongestants

  • Potential side effects: sneezing, nasal dryness, rebound nasal congestion
  • Not recommended for more than 3 days consecutively due to rebound congestion risk
  • Patients with hypertension, arrhythmias, and sleep problems should avoid oral decongestants

Drug Therapy for Cough

  • Use cough suppression for non-productive coughs or nighttime use
  • Avoid opioids in patients with substance abuse or COPD history
  • OTC cough medications should not be used in those under 2

Antitussives vs Expectorants

  • Antitussives suppress cough (nonproductive)
  • Expectorants thin secretions (productive cough)

Asthma Controllers and Relievers

  • Controllers: Prevent symptoms (intranasal corticosteroids, leukotriene modifiers)
  • Relievers: Relieve acute symptoms (2nd generation oral antihistamines, intranasal antihistamines, ocular antihistamines)

Nasal Antihistamines

  • Benefits: rapid onset, reduce airway hyperreactivity
  • Potential Side effects: sedation (less than oral), bitter taste

Leukotriene Modifiers

  • Decrease smooth muscle contraction, blood vessel permeability, and inflammatory response
  • Most effective when taken at bedtime

Black Box Warning for Leukotriene Modifiers

  • Montelukast carries a warning for agitation, aggression, anxiety, dream abnormalities, hallucinations, depression, insomnia, irritability, restlessness, suicidal ideation, behavior (including suicide), and tremor.

Asthma Treatment During Pregnancy and Lactation

  • First-line treatments: rest, hydration, a diet high in fruits and vegetables, saline nasal spray
  • Intranasal corticosteroids (e.g., Budesonide) are most effective and deemed safe in pregnancy
  • Antihistamines and some other medications (e.g., Chlorpheniramine, Diphenhydramine) are considered safe in most breastfeeding cases

Inhaled Medication Delivery Methods

  • Metered-dose inhalers (MDIs): Small hand-held devices; require hand-breath coordination; ~10% of drug reaches lungs
  • Dry-powder inhalers (DPIs): Deliver drugs as a dry powder to the lungs; do not require hand-breath coordination; ~20% of drug reaches lungs
  • Nebulizers: Machines that convert drug solution into a fine mist; less drug deposition in the mouth, increased delivery to the lungs; hand-breath coordination is not necessary

Inhaled Corticosteroids

  • Effective in controlling asthma and suppressing inflammation
  • Potential side effects: bone loss (avoid with calcium, vitamin D, and exercise), increased intraocular pressure (routine eye exams), oral fungal infections (rinse mouth), and slowed growth

Mast Cell Stabilizers

  • Prevent bronchoconstriction by blocking histamine and SRS-A release from sensitized mast cells
  • Anti-inflammatory agents

SABA, LABA, SAMA, and LAMA Role in Asthma Management

  • SABAs: quick-relief (short-acting beta-agonists)
  • LABAs: long-acting bronchodilators (maintenance)
  • SAMAs: quick-relief (short-acting muscarinic antagonists)
  • LAMAs: long-acting bronchodilators (maintenance)

Narrow Therapeutic Index

  • Risk of toxicity is high because the therapeutic range is very narrow.

Monoclonal Antibodies in Asthma Treatment

  • Anti-IgE antibodies (e.g., omalizumab) limit allergen-induced histamine, leukotriene, and other mediator release.
  • Interleukin-5 receptor antagonists reduce eosinophil production
  • Associated risks: anaphylaxis, malignancy, neoplasms, immunogenicity,

COPD Treatment Considerations

  • Anticholinergics (i.e., SAMAs and LAMAs): Long-acting bronchodilators are beneficial for moderate-severe COPD patients

Oral & Inhaled Corticosteroids in COPD

  • Inhaled corticosteroids decrease inflammation
  • Oral corticosteroids are used for exacerbations
  • Both reduce exacerbations and improve lung function

NRT (Nicotine Replacement Therapy)

  • Gum, Lozenge, Patch: Advantages: Serves as a tobacco alternative, may delay weight gain, easy titration
  • Gum, Lozenge, Patch: Disadvantages: frequent dosing, may cause mouth/tooth issues (gum) and/or swallowing issues, inconsistent nicotine delivery (lozenge), potential for skin reaction (patch), and need to adhere to use schedule

Varenicline Mechanism of Action

  • Blocks nicotine binding to dopaminergic receptors, reducing cravings and withdrawal symptoms

Varenicline Potential Side Effects

  • Potential for increased risk of suicidal thoughts, depression, and other psychiatric events

Bupropion (Zyban) Mechanism of Action

  • Inhibits dopamine/norepinephrine uptake

Bupropion Potential Side Effects

  • Increased risk of suicidal thoughts, mood changes, hallucinations, panic, depression, restlessness, insomnia, and anxiety

Smoking Cessation During Pregnancy

  • Bupropion and metabolites cross the placenta.
  • Limited data on long-term effects

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Description

This quiz covers the key differences between H1 receptor antagonists (H1RAs) and H2 receptor antagonists (H2RAs) in pharmacology. You will explore their mechanisms, uses, and side effects, including the impact of anticholinergic drugs on patients. Test your understanding of these important drug classes to enhance your knowledge of pharmacological treatments.

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