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Pharmacology: Respiratory

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
Created by: amichael87



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