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7 Cards in this Set
- Front
- Back
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H1 blockers
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Reversible inhibitors of H1 histamine receptors
-1st generation: diphenhydramine, dimenhydrinate, chlorpheniramine -clinical uses: allergy, motion sickness, sleep aid -toxicity: sedation, antimuscarinic, anti-alpha-adrenergic -Second generation: loratadine, fexofenadine, desloratadine, cetirizine -uses: allergy -toxicity: far less sedating than 1st generation because of decrease entry into CNS |
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drugs that can be used to treat asthma
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Bronchoconstriction is mediated by 1. inflammatory processes and 2. sympathetic tone; therapy is directed at these 2 pathways
nonspecific B agonists B2 agonists methylxanthines muscarinic antagonists cromolyn corticosteroids antileukotrienes |
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B agonists used in asthma
methylxanthines |
Nonspecific B-agonists: Isoproterenol - relaxes bronchial smooth muscle (B2); AE: tachycardia (B1)
B2-agonists: Albuterol: relaxes bronchial smooth muscle (B2); use during acute exacerbation; Slameterol: long-acting agent for prophylaxis; AE: tremor and arrhythmia Methylxanthines: Theophylline: likely causes bronchodilation by inhibiting phosphodiesterase, thereby decreasing cAMP hydrolysis. Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity); metabolized by P-450. Blocks actions of adenosine. |
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Asthma agents:
muscarinic antagonists cromolyn corticosteroids |
Ipratropium - competitive block of muscarinic receptors, preventing bronchoconstriction. Also used in COPD
Cromolyn: prevents release of mediators from mast cells. Effective only for the prophylaxis of asthma. Not effective during an acute asthmatic attack. Toxicity is rare. Beclomethasone, predinsone - inhibit the synthesis of virtually all cytokines. Inactivate NF-kB, the transcription factor that induces production of TNF-alpha, among other inflammatory agents. 1st line therapy for chronic asthma |
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Asthma agents:
antileukotrienes |
Zileuton - a 5-lipoxygenase pathway inhibitor. Blocks conversion of arachidonic acid to leukotrienes
Zafirlukast, montelukast - block leukotriene receptors. Especially good for asprin-induced asthma |
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expectorants
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Guaifenesin (Robitussin): Removes excess sputum but large doses necessary; does not suppress the cough reflex
N-acetylcysteine: mucolytic -> can loosen mucous plugs in CF patients. Also used as an antidote in acetominophen overdose |
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bosentan
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used to treat pulmonary hypertension. Competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance
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