Respiratory - Pharmacology

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Author:
jknell
ID:
210725
Filename:
Respiratory - Pharmacology
Updated:
2013-04-01 14:05:04
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Respiratory pharmacology
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  1. First Generation H1 Blockers
    "-en/-ine" or "-en/-ate"
    • Diphenhydramine
    • Dimenhydrinate
    • Chlorpheniramine

    • Mechanism:
    • -reversible inhibitors of H1 receptors

    • Clinical Use:
    • -allergy
    • -motion sickness
    • -sleep aid

    • Toxicity:
    • -sedation
    • -antimuscarinic
    • -anti-α-adrenergic
  2. Second Generation H1 Blockers
    "-adine"
    • Loratadine
    • Fexofenadine
    • Desloratadine
    • Cetirizine

    • Mechanism:
    • -reversible inhibition of H1 receptors
    • -decreased entry into CNS

    • Clinical Use:
    • -allergy

    • Toxicity:
    • -far less sedating than first generation (↓ entry into CNS)
  3. Asthma drugs
    • Bronchoconstriction is mediated by:
    • 1. inflammatory processes
    • 2. Parasympathetic tone
    • Therapy is directed at these 2 pathways
  4. β2 Agonists
    • Albuterol:
    • -relaxes bronchial smooht muscle
    • -use during acute exacerbation

    • Salmeterol, Formoterol:
    • -long-acting agents for prophylaxis
    • -toxicity: tremor, arrhythmia
  5. Methylxanthines
    • Theopylline
    • Mechanism:
    • -inhibits phosphodiesterase → decrease cAMP hydrolysis → bronchodilation

    • Clinical Use:
    • -asthma
    • -limited due to narrow therapeutic index 

    • Toxicity:
    • -cardiotoxicity
    • -neurotoxicity
    • -blocks actions of adenosine
  6. Corticosteroids
    • Beclomethasone
    • Fluticasone

    • Mechanism:
    • -inhibit the synthesis of virtually all cytokines
    • -inactivate NF-κB (decrease TNFa transcription)

    • Clinical Use:
    • -first line therapy for chronic asthma
  7. Antileukotrienes
    • Montelukast, Zafirlukast:
    • -MOA: block LT receptors
    • -Clinical Use: esp good for ASA-induced asthma

    • Zileuton:
    • -MOA: 5-lipoxygenase pathway inhibitor, blocks conversion of AA to LTs
  8. Omalizumab
    • Mechanism:
    • -monoclonal anti-IgE antibody
    • -binds mostly unbound serum IgE

    • Clinical Use:
    • -allergic asthma resistant to inhaled steroids and long-acting β2-agonists
  9. Guaifenesin
    • Mechanism:
    • -expectorant
    • -thins respiratory secretions
    • -does not suppress cough reflex
  10. N-acetylcysteine
    • Mechanism:
    • -mucolytic

    • Clinical Use:
    • -can loosen mucus plugs in CF patients
    • -antidote for acetaminophen OD
  11. Bosentan
    • Mechanism:
    • -competitive antagonist of endothelin-1 receptors
    • -decreases PVR

    • Clinical Use:
    • -Pulmonary arterial HTN
  12. Dextromethorphan
    • Mechanism:
    • -antitussive (antagonizes NMDA glutamate Rs)
    • -synthetic codeine analog
    • -mild opioid effect when used in excess

    • Clinical Use:
    • -cough suppressant?

    • Toxicity:
    • -naloxone can be given for OD
    • -mild abuse potential
  13. Pseudoephedrine
    Phenylephrine
    • Mechanism:
    • -sympathomimetic alpha agonist

    • Clinical Use:
    • -reduce hyperemia, edema and nasal congestion
    • -open obstructed eustachian tubes

    • Toxicity:
    • -hypertension
    • -can also cause CNS stimulation/anxiety
  14. Methacholine
    • Muscarinic receptor agonist
    • Used in asthma challenge testing

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