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Flashcards in Respiratory - Pharmacology Deck (18):
1

1st generation H1 blockers

  • Examples
  • Mechanism
  • Clinical use
  • Toxicity

  • Examples
    • Diphenhydramine, dimenhydrinate, chlorpheniramine.
    • Names contain “-en/-ine” or “-en/-ate.”
  • Mechanism
    • Reversible inhibitors of H1 histamine receptors.
  • Clinical use
    • Allergy, motion sickness, sleep aid.
  • Toxicity
    • Sedation, antimuscarinic, anti-α-adrenergic.

2

2nd generation H1 blockers

  • Examples
  • Mechanism
  • Clinical use
  • Toxicity

  • Examples
    • Loratadine, fexofenadine, desloratadine, cetirizine.
    • Names usually end in “-adine.”
  • Mechanism
    • Reversible inhibitors of H1 histamine receptors.
  • Clinical use
    • Allergy.
  • Toxicity
    • Far less sedating than 1st generation because of decreased entry into CNS.

3

Guaifenesin

  • Mechanism

  • Mechanism
    • Expectorant
    • Thins respiratory secretions
    • Does not suppress cough reflex.

4

N-acetylcysteine

  • Mechanism
  • Clinical use

  • Mechanism
    • Expectorant / mucolytic
  • Clinical use
    • Can loosen mucous plugs in CF patients.
    • Also used as an antidote for acetaminophen overdose.

5

Dextromethorphan

  • Mechanism
  • Toxicity

  • Mechanism
    • Antitussive (antagonizes NMDA glutamate receptors).
    • Synthetic codeine analog.
  • Toxicity
    • Has mild opioid effect when used in excess.
    • Naloxone can be given for overdose.
    • Mild abuse potential.

6

Pseudoephedrine, phenylephrine

  • Mechanism
  • Clinical use
  • Toxicity

  • Mechanism
    • Sympathomimetic α-agonistic nonprescription nasal decongestants.
  • Clinical use
    • Reduce hyperemia, edema, and nasal congestion
    • Open obstructed eustachian tubes.
    • Pseudoephedrine also illicitly used to make methamphetamine.
  • Toxicity
    • Hypertension.
    • Can also cause CNS stimulation/anxiety (pseudoephedrine).

7

Asthma drugs (614)

  • Bronchoconstriction is mediated by...
    • (1) inflammatory processes
    • (2) parasympathetic tone
  • Therapy is directed at these 2 pathways.

8

Albuterol (614)

  • Type of drug
  • Mechanism
  • Clinical use

  • Type of drug
    • Asthma drug: β2-agonist
  • Mechanism
    • Relaxes bronchial smooth muscle (β2).
  • Clinical use
    • Use during acute exacerbation.

9

Salmeterol, formoterol (614)

  • Type of drug
  • Mechanism
  • Clinical use
  • Toxicity

  • Type of drug
    • Asthma drugs: β2-agonists
  • Mechanism
    • Long-acting agents
  • Clinical use
    • For prophylaxis
  • Toxicity
    • Adverse effects are tremor and arrhythmia.

10

Theophylline (614)

  • Type of drug
  • Mechanism
  • Clinical use
  • Toxicity

  • Type of drug
    • Asthma drug: Methylxanthine
  • Mechanism
    • Likely causes bronchodilation by inhibiting phosphodiesterase -->Ž increased cAMP levels due to decreased cAMP hydrolysis.
    • Metabolized by cytochrome P-450.
    • Blocks actions of adenosine.
  • Clinical use
    • Usage is limited because of narrow therapeutic index
  • Toxicity
    • Cardiotoxicity, neurotoxicity

11

Ipratropium (614)

  • Type of drug
  • Mechanism
  • Clinical use

  • Type of drug
    • Asthma drug: Muscarinic antagonist
  • Mechanism
    • Competitive block of muscarinic receptors
  • Clinical use
    • Prevents bronchoconstriction
    • Also used for COPD

12

Tiotropium (614)

  • Type of drug
  • Mechanism
  • Clinical use

  • Type of drug
    • Asthma drug: Muscarinic antagonist
  • Mechanism
    • Long-acting
  • Clinical use
    • Used for COPD

13

Beclomethasone, fluticasone (614)

  • Type of drug
  • Mechanism
  • Clinical use

  • Type of drug
    • Asthma drugs: Corticosteroids
  • Mechanism
    • Inhibit the synthesis of virtually all cytokines.
    • Inactivate NF-κB, the transcription factor that induces the production of TNF-α and other inflammatory agents.
  • Clinical use
    • 1st-line therapy for chronic asthma.

14

Montelukast, zafirlukast (614)

  • Type of drug
  • Mechanism
  • Clinical use

  • Type of drug
    • Asthma drugs: Antileukotrienes
  • Mechanism
    • Block leukotriene receptors.
  • Clinical use
    • Especially good for aspirin-induced asthma

15

Zileuton (614)

  • Type of drug
  • Mechanism

  • Type of drug
    • Asthma drug: Antileukotriene
  • Mechanism
    • A 5-lipoxygenase pathway inhibitor
    • Blocks conversion of arachidonic acid to leukotrienes.

16

Omalizumab (614)

  • Type of drug
  • Mechanism
  • Clinical use

  • Type of drug
    • Asthma drug
  • Mechanism
    • Monoclonal anti-IgE antibody.
    • Binds mostly unbound serum IgE and blocks binding to FcεRI.
  • Clinical use
    • Used in allergic asthma resistant to inhaled steroids and long-acting β2-agonists.

17

Methacholine

  • Mechanism
  • Clinical use

  • Mechanism
    • Muscarinic receptor agonist.
  • Clinical use
    • Used in bronchial provocation challenge to help diagnose asthma.

18

Bosentan

  • Mechanism
  • Clinical use

  • Mechanism
    • Competitively antagonizes endothelin-1 receptors
    • Decreases pulmonary vascular resistance.
  • Clinical use
    • Used to treat pulmonary arterial hypertension.

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