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Pulmonary
FA complete review part 4 Pharmacology
| Question | Answer |
|---|---|
| What is the mechanism of action of Histamine-1 blockers? | Reversible inhibitors of H1 histamine receptors. |
| What are some First generation H1-blockers? | Diphenhydramine, dimenhydrinate, and chlorpheniramine. |
| What are the clinical uses for H1-blockers? | Allergy, motion sickness, and sleep aid |
| What are common side effects of H1-blockers? | Sedation, antimuscarinic, anti-alpha-adrenergic. |
| What are some examples of Second generation H1-blockers? | Loratadine, fexofenadine, desloratadine, cetirizine. |
| What is the main use for H1-blockers of second generation? | Allergy |
| Why are second generation far less sedating than 1st generation H1-blockers? | Less entry into CNS |
| Common expectorant? | Guaifenesin |
| What is N-acetylcysteine? | Mucolytic- liquifies mucus in chronic bronchopulmonary diseases by disrupting disulfide bonds. |
| N-acetylcysteine is used for antidote for ____________________ overdose. | Acetaminophen |
| What is Dextromethorphan mechanism of action? | Antitussive; antagonizes NMDA glutamate receptors; Synthetic codeine analog. |
| How can Dextromethorphan overdose treated? | Naloxone |
| What is a significant adverse effect of Dextromethorphan? | Serotonin syndrome if combined with other serotonergic agents. |
| What is the mechanism of action of Pseudoephedrine and Phenylphrine? | a-adrenergic agonists, used as nasal decongestants |
| What are the clinical uses for Pseudoephedrine and phenylephrine? | 1. Reduce hyperemia, edema, and nasal congestion 2. Open obstructed eustachian tubes |
| What are the most significant adverse effects of Pseudoephedrine and phenylephrine? | 1. Hypertension 2. Rebound congestion if used more than 4-6 days 3 CNS stimulation/anxiety (pseudoephedrine) |
| What drug categories are used in the treatment of Pulmonary hypertension? | 1. Endothelin receptor antagonists 2. PDE-5 inhibitors 3. Prostacyclin analogs |
| What is the MOA of Endothelin receptor antagonists? | Competitively antagonizes endothelin-1 receptors --> decrease in pulmonary vascular resistance |
| Which endothelin receptor is blocked by Endothelin-receptor blockers? | Endothelin-1 |
| What is the most common example of an Endothelin-receptor antagonist? | Bosentan |
| Bosentan is an _______________________________. | Endothelin-receptor antagonists |
| What is the associated adverse effect of Bosentan? | Hepatotoxic (monitor LFTs) |
| What is the MOA of PDE-2 inhibitors? | Inhibits PDE-5 --> Increase in cGMP, which as result causes prolonged vasodilatory effect of NO (nitric monoxide). |
| Besides management of Pulmonary HTN, another common use for PDE-5 inhibitors is _____________________. | Erectile dysfunction |
| What drugs/compounds are contraindicated in a patient on PDE-5 inhibitors? | Nitroglycerin or other nitrates |
| What is the most common example of PDE-5 inhibitor? | Sildenafil |
| What are the examples of Prostacyclin analogs? | Epoprostenol, iloprost |
| MOA of Prostacyclin analogs | -PGI2 (prostacyclin) with direct vasodilatory effects on pulmonary and systemic arterial vascular beds - Inhibits platelet aggregation. |
| What are the most common side effects of Prostacyclin analogues? | Flushing and jaw pain |
| Asthma therapy is directed to counteract which two processes of Bronchoconstriction? | 1. Inflammatory processes 2. Parasympathetic tone |
| Short acting B2 agonist | Albuterol |
| What are 3 common B2-agonists used in Asthma treatment? | Albuterol (short acting), Salmeterol, and formoterol |
| What is the common B2-agonist used in acute exacerbation of asthma? | Albuterol |
| What is MOA of Albuterol? | Relaxes bronchial smooth muscle in acute setting. |
| Which B-2 agonists are commonly used a prophylaxis of Asthma? | Salmeterol and Formoterol |
| What are common adverse effects of Salmeterol? | Tremor and arrhythmias |
| Examples of common inhaled corticosteroids? | Fluticasone and Budesonide |
| What Asthma drugs are known to inhibit the synthesis of virtually all cytokines? | Inhaled corticosteroids (fluticasone, budesonide) |
| What drug(s) are the first line of treatment for chronic asthma ? | Inhaled corticosteroids (fluticasone, budesonide) |
| What is the mode action of Fluticasone? | Inactivate NF-KB |
| What is the function of NF-KB? | Transcription factor that induces production of TNF-alpha and other inflammatory agents |
| What transcription factor is inactivated by inhaled corticosteroids, such as Fluticasone? | NF-KB |
| What actions must be taken in order to prevent oral thrush formation from the use of Fluticasone and other inhaled corticosteroids? | Use a spacer or rinse mouth after use |
| Which are two common Muscarinic antagonists? | Tiotropium and Ipratropium |
| What is the MOA of Muscarinic antagonist? | Competitively block muscarinic receptor, preventing bronchoconstriction. |
| Tiotropium and Ipratropium are ______________ _______________. | Muscarinic antagonists |
| Which muscarinic antagonist is used in treatment of asthma and is known to be long-acting? | Tiotropium. |
| 3 common antileukotrienes: | Montelukast, Zafirlukast, and ZIleuton |
| Which antileukotrienes block leukotriene receptors CysLT1? | Montelukast and Zafirlukast |
| What are the recommended asthma drugs for Aspirin-induced asthma and Exercise-induced asthma? | Montelukast and Zafirlukast |
| Montelukast and Zafirlukast are _______________________-. | Antileukotrienes |
| 5-lipoxygenase pathway inhibitor. | Zileuton |
| What is blocked by the use of Zileuton? | Conversion of arachidonic acid to leukotrienes |
| Which antileukotriene is known to be hepatotoxic? | Zileuton |
| What is Omalizumab? | Anti-IgE monoclonal antibody in the treatment of asthma |
| What is the mode of action of Omalizumab? | Binds unbound serum IgE and blocks binding to FcERI |
| What type of asthma is the one that most commonly uses Omalizumab as part of drug therapy? | Allergic asthma with elevated IgE levels resistant to inhaled steroids and long-acting B2-agonist |
| Patient's asthma proven ineffective treatment with inhaled steroids and Salmeterol, may be given _______________ as therapy for asthma. | Omalizumab |
| Theophylline is a __________________________. | Methylxanthine |
| How does Theophylline causes bronchodilation? | By inhibiting phosphodiesterase --> elevated cAMP levels due to decreased cAMP hydrolysis |
| Why is the use of Theophylline limited? | Due cardiotoxicity and neurotoxicity |
| Theophylline blocks actions of _______________. | Adenosine |
| Theophylline is metabolized by the ________________________. | CYP450 system. |
| What are common examples of Mast cell stabilizers? | Cromolyn and nedocromil |
| Mechanism of action of Mast cell stabilizers | Prevent release of inflammatory mediators from mast cells |
| What is the main use for mast cell stabilizers? | Prevention of bronchospasm |
| Which Asthma drugs are used to prevent/treat symptoms? | 1. B-agonists 2. Theophylline 3. Muscarinic antagonists |
| Which Anti-asthmatic drugs are used for prevention or treatment of bronchial hyperreactivity? | Studies and Antileukotrienes |
| What is the early response of asthma process? | Bronchoconstriction --> symptoms |
| What is the late response of asthma? | Inflammation --> bronchial hyperreactivity. |