Pharmacology: Respiratory
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| 1. In which cells is histamine stored? 2. Where are these cells found? | 1. within vesicles or basophils and mast cells 2. basophils are in blood; mast cells are in tissue | ||||
| What GPCR do the following act through? Which tissues are they found in? 1. H1 histamine receptor 2. H2 histamine receptor | 1. Gq; airway smooth muscle, endothelium 2. Gs; gastric parietal cells, cardiac muscle, mast cells | ||||
| What effect does histamine have on: 1. Vasculature 2. Respiratory tract | 1. vasodilation (vessel permeability) 2. bronchoconstriction, mucus & sputum production | ||||
| Mechanism of action of: 1. antihistamines 2. Nasal decongestants 3. expectorants | 1. competitively inhibit H1 receptors 2. alpha-adrenergic agonists 3. ↑ sputum production | ||||
| 1. mechanism of action of Dornase alfa. 2. What is its clinical use? | 1. mucolytic; hydrolyzes extracellular DNA in mucus 2. cystic fibrosis | ||||
| What are the 2 classes of H1 antihistamines? | 1. 1st Gen: "sedating" 2. 2nd Gen: "non-sedating" | ||||
| 1. Why do 1st generation H1 antihistamines cause sedation? 2. How does affinity to H1 receptor change over the generations of antihistamines? | 1. cross the blood-brain barrier and block muscarinic receptors in the CNS 2. 1st gen. have the lower affinity while 2nd gen. have higher affinity | ||||
| Why are some antihistamines effective against motion sickness and not others? | the first generation antihistamines have antimuscarinic action and are effective against motion sickness | ||||
| 1. Dephenhydramine mechanism of action 2. Uses | 1. (trade name Benadryl - 1st gen antihistamine) 2. symptomatic relief of allergic symptoms, sleep aid, treatment of motion sickness | ||||
| Which CNS conditions are H1 antihistamines effective against? | 1. motion sickness 2. vertigo 3. sedation 4. emesis | ||||
| What are the side effects of first generation H1 antihistamines? | 1. sedation 2. anticholinergic effects (blurry vision, dry mouth) 3. long QT/arrhythmias (K+ channel block) | ||||
| 1. What is a decongestant? 2. What is an example? | 1. a drug that reduces nasal or oropharyngeal mucosal swelling by constricting blood vessels in the submucosal tissue 2. phenylephrine | ||||
| 1. Drug of choice for immediate anaphylactic shock. 2. What is the mechanism of action of nasal decongestants? | 1. epinephrine 2. alpha-adrenergic agonists | ||||
| 1. Treatment of allergic conjunctivitis 2. What is the mechanism of action? 3. adverse effect | 1. Naphcon and visine eyedrops 2. H1 antihistamine 3. ↑ intraocular pressure → ↑risk for glaucoma | ||||
| 1. Mechanism of action of central antitussives? 2. Which drugs are in this class? | 1. agonist of opiate receptor in medulla 2. codeine, hydrocodone | ||||
| Mechanism of action 1. Albuterol 2. Salmeterol 3. Theophylline | 1. β2 agonist → bronchodilation 2. β2 agonist → bronchodilation 3. inhibits phosphodiesterae → ↑ cAMP and bronchodilation; also blocks adenosine's bronchoconstrictive action | ||||
| Adverse effects of: 1. salmeterol 2. theophylline | 1. tremor, arrhythmia 2. cardiotoxicity, neurotoxicity | ||||
| Mechanism of action: 1. Ipratropium 2. Cromolyn | 1. muscarinic antagonist, prevents bronchoconstriction 2. prevents release of mediators from mast cells | ||||
| Corticosteroids 1. Mechanism of action 2. examples | 1. inhibit synthesis of cytokines; inactivate NF-kB →↓inflammatory agents 2. Beclomethasone, prednisone | ||||
| Mechanism of action: 1. Zileuton 2. Zafirlukast, montelukast | 1. 5-lipoxygenase pathway inhibitor 2. block leukotriene receptors | ||||
| 1. Expectorant that removes mucus but does not relieve cough 2. Expectorant loosens mucus plugs in CF patients. | 1. Guaifenesin (Robitussin) 2. N-acetylcysteine | ||||
| 1. Treatment for pulmonary hypertension 2. mechanism of action | 1. Bosentan 2. competitively antagonizes endothelin-1 receptors → ↓pulmonary vascular resistance | ||||
| Used for aspirin induced asthma. | Zafirlukast, montelukast | ||||
| 1. β2 agonist used for acute exacerbation of asthma 2. β2 agonist used for long action prophylaxis. | 1. Albuterol 2. Salmeterol | ||||
| 1. Mechanism of action of N-acetylcystein as a decongestant? 2. Mechanism by which N-acetylcystein can decrease cough? | 1. breaks disulfide bond links in mucin oligomers 2. decreases free radical injury and inflammation | ||||
| 1. What are the three major antihistamines that have no CNS entry? 2. What is the only pharmacologic use? 3. Antitussive that blocks stretch receptors in throat. | 1. Cetirizine, Loratadine, Fexofenadine 2. allergic reactions (seasonal rhinitis) 3. Benzonatate | ||||
| 1. How are all antihistamines metabolized? 2. Antihistamine that is highly effective in motion sickness. 3. Mechanism of action of Dextromethorphan | 1. hepatic cytochrome P450 2. meclizine 3. centrally acting antitussive that binds NMDA receptors | ||||
| 1. Treatment for aspirin induced asthma 2. Cetirizine 3. Used to treat bronchospasm caused by β blockers | 1. Zafirlukast, montelukast 2. 2nd generation antihistamine; trade name Zyrtec 3. muscarinic receptor blockers (Ipratropium) | ||||
| Histamine effect on the heart 1. H1 receptors 2. H2 receptors | 1. ↓ AV nodal conduction 2. ↑ SA nodal rate, positive inotropism |
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Created by:
amichael87
on 2011-10-19