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Respiratory Pharmacology
PHAR340
26
Pharmacology
Undergraduate 3
12/06/2012

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Term
Histamine
Effector cells found where?
Definition
Bound in granules of mast cells and basophils
Mast cells in potential sites of injury
Enterochromaffin-like cells to activate parietal cells to release acid
Neurons to acts as a neurotransmitter
Term
Histamine?
H1 vs. H2 vs. H3 vs. H4
Definition
GPCRs in brain (H1,H3), bronchioles (H1), stomach (H2), heart (H2), blood (H4)
Smooth muscle and endothelium (H1), specifically
Term
Epinephrine
Relevance to respiratory pharmacology?
Definition
Physiological antagonist
Bronchiodilation and vasoconstriction
Term
Sodium cromolyn
Definition
Release inhibitor
Inhibits mast cell degranulation
Term
Antihistamines
Definition
Receptor antagonists
Treatment for hay fever, hives and bronchoconstriction
Term
Diphenhydramine
Definition
Benadryl
H1 antagonist – 1st generation
Anticholinergic properties, e.g. dry mouth
Term
Chlorpheniramine
Definition
H1 antagonist – 1st generation
Term
Phenothiazine
Definition
H1 antagonist – 1st generation
Block adrenoreceptors and serotonin receptors
Term
Loratadine
Definition
Claritin
H1 antagonists – 2nd generation
Less sedating because they do not reach the CNS
Term
Fexofenadine
Definition
H1 antagonists – 2nd generation
Less sedating because they do not reach the CNS
Term
Cetirizine
Definition
H1 antagonists – 2nd generation
Less sedating because they do not reach the CNS
Term
Sodium cromolyn
Definition
Inhibits mast cell degranulation in airways
Administration: inhalation
Prophylactic
Term
Epinephrine
Respiratory pharmacology relevance?
Definition
Rapid action on ɑβ receptors
IV injection, acute
Term
Salbutamol
Definition
SABA (3-4 hours)
Inhaled, acute
Term
Salmeterol
Definition
LABA (12 hours)
Inhaled, acute
Term
Indacaterol
Definition
uLABA (24+ hours)
Longer acting = not necessarily better
Increase bioavailability, take once a day
Inhaled, acute
Term
Carmoterol
Definition
uLABA (24+ hours)
Longer acting = not necessarily better
Increase bioavailability, take once a day
Term
Glucocorticoids
Respiratory action?
Definition
Anti-inflammatory via decrease of eicosanoid synthesis
Activation of anti-inflammatory genes, repression of pro-inflammatory
Also, stimulation of β receptors
Inhalation, prophylactic
Many adverse effect, minimize long-term use
Term
Combination medication for asthmatics?
Definition
Corticosteroids (reduce inflammation) + LABA (bronchodilation)
Term
Ipratropium
Definition
Anti-cholinergic
Quaternary analog of atropine
Block cholinergic bronchoconstriction and secretions
Inhalation to decrease systemic effects
Acute
Term
Theophylline
Definition
Methylxanthine
Bronchodilation with no Ach/adrenergic receptor activity
Block of adenosine receptors (cause bronchospasms)
Inhibition of PDE4 to increase cAMP
Administration: oral
Metabolized by cytochrome P450
Term
Theophylline
Adverse effects?
Definition
Narrow therapeutic range
Heart: stimulates heart rate and force of contraction → arrhythmias
CNS: stimulation → convulsions
GI tract: acid and pepsin secretion
Term
Zileuton
Definition
Leukotriene pathway inhibitor
5-lipoxygenase inhibitor
Inhibit synthesis of leukotrienes
Term
Montelukast
Definition
Leukotriene pathway inhibitors
CysLT1 receptor antagonist
Block leukotriene action
Oral, prophylactic
Term
Zafirlukast
Definition
CysLT1 receptor antagonist
Block leukotriene action
Oral, prophylactic
Term
Omalizumab
Definition
Anti-IgE antibody
Blocks binding of IgE to mast cells, basophils
Binds to epitope on IgE (Fc region)
Subcutaneous, prophylactic
Potentially severe anaphylactic reactions
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