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55 Cards in this Set
- Front
- Back
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Advantage of inhaled asthma treatment
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Fewer side effects
More rapid relief |
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B2 agonists MOA
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Activates adenylate cyclase, which increases cAMP production
cAMP relaxes bronchial smooth muscle |
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B2 agonists (4)
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Albuterol (Ventolin, Proventil, Accuneb)
Levabuterol (Xopenex) Fluticasone/salmeterol (Advair) Formoterol Fumarate (Foradil) |
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Prototype of B2 agonists
-Effects on B1 receptors |
Albuterol
Not much effect, pretty selective for B2 in airway; so few cardiac side effects |
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A long acting B2 agonist
-Advantages |
Salmeterol
Able to use less frequently; less likely to develop tolerance |
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Advantage of Levabuterol
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An isolated isomer that produces specific effects at receptors, thereby reducing side effects
However, more expensive |
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Serious adverse effects of albuterol
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Urticaria
Arrythmia QT prolongation Angina Hypokalemia Paradoxical bronchospasm |
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Common adverse effects of albuterol
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Nervousness
Tremor Tachycardia Bad taste Throat irritation |
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Vagal stimulation on airways
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Causes bronchoconstriction and mucus secretion
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Anticholinergics (2)
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Ipratroprium bromide (Atrovent)
Tiotroprium bromide (Spiriva Handihaler) |
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Anticholinergics MOA
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Blocks ganglionic vagal pathways; vagal stimulation produces bronchoconstriction.
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Ipratroprium bromide
-Advantage |
It's a quaternary amine, so it isn't absorbed well systemically - so can't have as many side effects
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Tiotroprium advantage
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Has long half life, so can be used just once daily
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Anticholinergic metabolism and excretion
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Little metabolism of either, excreted unchanged in urine and feces
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Corticosteroids MOA
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Prevents neutrophils and eosinophils from coming to airway. Prevents production of inflammatory chemicals. Thereby reduces mucus production and swelling.
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Corticosteroids also
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Increases the number and sensitivity of B2 receptors.
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Corticosteroids (4)
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Beclomethasone (Beclovent® Vanceril® QVAR80® )
Budesonide (Pulmicort®) Fluticasone / salmeterol (Advair®) Triamcinolone acetonide (Azmacort®) |
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Corticosteroids elimination
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Both renal and fecal
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Serious adverse effects of corticosteroids
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Adrenal suppression
Osteoporosis Growth suppression Bronchospasm Peptic ulcer |
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Common adverse effects of corticosteroids
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Oral candidiasis
Sinusitis Rhinitis Hoarseness |
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Leukotrines made from
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Lipoxygenase converting arachidonic acid to leukotrines
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Leukotrine receptor antagonists MOA
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Prevents leukotrines from participating in inflammatory response
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Leukotrine antagonist (1)
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Montelukast (Singulair)
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Why might compliance be better with leukotrine antagonists
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B/c administered orally, so especially easier for children to take
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Serious adverse effects of leukotrine modifiers
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Angioedema
Anaphylaxis Churg Strauss syndrome |
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Common adverse effects of leukotrine modifiers
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Flu like symptoms
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Leukotrine modifiers metabolism
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CYP 450 enzymes
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Monoclonal antibodies MOA
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Inhibits IgE binding to receptors on mast cells and basophils, preventing degranulation (release of allergic response mediators).
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Problem with monoclonal antibodies
Intended recipient |
Expensive and injectable only
People who do not respond to inhaled corticosteroids |
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Monoclonal antibodies (1)
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Omalizumab (Xolair)
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Decongestants MOA
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A1 stimulation, producing vasoconstriction - restricted blood flow so less edema and mucus production.
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Topical decongestants (3)
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Oxymetazoline (Afrin®, Allerest®)
Phenylephrine (Neo-synephrine®) Topical spray Xylometazoline (Otrivin ®) |
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Systemic degongestant (1)
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Pseudoephedrine (Sudafed®)
Systemic extended release tablets |
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Serious adverse effects of decongestants
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Cardiovascular collapse
Arrythmia Tachycardia |
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Common adverse effects of decongestants
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Sneezing
Burning Irritation HTN Insomnia Agitation, tremor |
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Topical decongestants should not be used longer than
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3 days
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Antihistamines MOA
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Block H1 receptors, preventing inflammation and mucus production
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Effects of histamine (3)
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Stimulates nerve endings to cause pain and itchy
Dilates arterioles so BP goes down and reflex tachycardia is initiated Causes increased permeability of capillaries so causes edema and hives |
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Do antihistamines have any effect on histamine release?
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No
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1st generation antihistamines (3)
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Dimenhydrinate (Dramamine)
Diphenhydramine HCl (Benadryl) Chlorpheniramine (Chlor-Trimeton) |
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2nd generation antihistamines (4)
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Cetirizine (Zyrtec)
loratidine (Claritin) des-loratidine (Clarinex) fexofenadine (Allegra®, Allegra D) |
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Two notes about first generation antihistamines
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More sedative
More distribution in the CNS |
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Note about second generation antihistamines
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Have longer half-lives
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Other useful effects of antihistamines
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Sedation
Antiemetic Anticholinergic for rhinitis |
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Corticosteroids for treatment of the cold MOA
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Antinflammatory effects in the nose spray; limited absorption so doesn't affect rest of the body
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Intranasal inflammatory sprays (4)
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Corticosteroids - Rx
Triamcinolone acetonide (Nasacort) Budesonide (Rhinocort) Fluticasone (Flonase) |
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Intranasal spray MOA
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Decrease inflammatory effect in nose
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Cough produced by
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Cough center in the medulla
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Antitussives
-2 general actions |
Inhibit cough through
1. Action with trachea 2. Action with medulla |
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Expectorants MOA
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Make respiratory mucus thin so it can be removed
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The only safe expectorant
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Guaifenesin (Robitussin, Mucinex)
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Other cough medicines
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Opioids like codeine - used at lower levels than pain control
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Antitussives with Dextromethorphan (an isomer of opioid): MOA
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Dextromethorphan (Robitussin-DM, Mucinex-DM, Delsym)
Acts at medulla to depress cough |
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Antitussives with codeine (1)
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Tussionex, Tussi-organidin
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Non-codeine antitussives (1) and MOA
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Benzonatate (Tessalon Perles)
Numbs trachea, so can't send cough signal to medulla |
