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13 Cards in this Set

  • Front
  • Back
h1 blockers: 1st generation

diphenhydramine, dimenhydrinate, chlorpheniramine
reversible inhibitors of h1 histamine receptors

use: allergy, motion sickness, sleep aid.

toxicity: sedation, antimuscarinic, anti-a-adrenergic
h1 blockers: 2nd generation

loratadine, fexofenadine, desloratadine, cetirizine
reversible inhibitors of h1 histamine receptors.

use: allergy.

toxicity: far less sedating than 1st generation b/c of decreased entry into CNS.
asthma drug therapy goal
bronchoconstriction is mediated by:

1. inflammatory processes
2. sympathetic tone

therapy directed at these 2 pathways.
asthma drug
nonspecific b-agonist

isoproterenol
relaxes bronchial smooth muscle (b2). adverse effect is tachycardia (b1).
asthma drug
b2 agonist


albuterol, metaproterenol, salmeterol
albuterol/metaproterenol - relaxes bronchial SM (b2). used during acute exacerbations.

salmeterol - long acting agent for prophylaxis (b2). AE are tremor and arrhythmias.
asthma drug
methylxanthines

theophylline
likely causes bronchodilation by inhibiting phosphodiesterase, decreasing cAMP hydrolysis (increase overall cAMP levels in cell). usage is limted b/c of narrow therapeutic index (cardiotoxicity, neurotoxicity); metabolized by p450. blocks actions of adenosine.

treat poisoning with b-blockers.
asthma drug
muscarinic antagonist

ipratropium
competitive block of muscarinic receptors, preventing bronchoconstriction. also used for COPD.
asthma drugs
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.

histamine causes bronchoconstriction.
asthma drugs
corticosteroids

beclomethasone, prednisone
inhibts the synthesis of virtually all cytokines. inactivate NF-kB, the TF that induces the production of TNF-a among other inflammatory agents. 1st line therapy for chronic asthma.

use associated with development of candidiasis in asthmatic patients.
asthma drugs
antileukotrienes

zileuton
zafirlukast, montelukast
zileuton: a 5-lipoxygenase pathway inhibitor. blocks conversion of arachidonic acid to leukotrienes.

zafirlukast, montelukast: block leukotriene receptors. especially good for aspirin-induced asthma.
Expectorants

guaifenesin (robitussin, mucinex)
removes excess sputum but large doses necessary; does not suppress cough reflex
expectorants

N-acetylcysteine
mucolytic: can loosen mucous plugs in CF patients. also used as an antidote for acetaminophen OD
Bosentan
used to treat pulmonary hypertension. competively antagonizes endothelin-a receptors, decreasing pulmonary vascular resistance.