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45 Cards in this Set

  • Front
  • Back
Inhalation Corticosteroids mentioned?
Triamcinolone, Fluticasone, and Prednisolone
What are the actions of inhalational corticosteroids?
Inhibit leukotriene, prostaglandin, and thromboxane synthesis. Reduce bronchiolar smooth muscle contraction, vascular permeability, and airway mucus secretions.

Restore responsiveness of bronchial smooth muscle to beta agonists

Inhibit activity of mast cells, eosinophils, neutrophils, macrophages, and lymphocytes.
Adverse effects of inhalational corticosteroids?
Known to cause changes in microflora that can lead to oral candidiasis
What is the anticholinergic used for bronchodilation?
Ipratropium (oral-inhalation, or nasal)
Mechanism of action of Ipratropium
Synthetic quaternary antimuscarinic agent that is a competitive antagonist at muscarinic cholinergic receptors.

Action is to decrease formation of cGMP which decreases contractility of smooth muscles due to actions of cGMP on intracellular calcium
Adverse effects of Ipratropium?
Xerostomia is the most common side effect. It is not known to causes tremor or arrhythmias like beta agonists.
Which drug is a good choice for use in COPD pt's, especially those w/ psychogenis exacerbations
Ipratropium
Oral-inhalation powered drug that is used for the treatment of bronchospasm associated w/ COPD?
Tiotropium (spiriva)

Once daily dose, NOT used for asthma.

Pt's do not like this drug
What is the first line therapy for COPD when symptoms become persistent?
Inhaled anticholingergic therapy
Actions of Tiotropium?
Anticholinergic having both Bronchodilatory and Bronchoprotective actions. Acts on M1, M2, and M3 receptors (M3 are airway receptors)
Name the Methyl Xanthines (non-inhalational used orally/IV)
Aminophylline, THEOPHYLLINE, Dyphylline, Oxtriphylline

Theophylline is only one used for treatment of asthma
Actions of Methyl Xanthines?
Relax smooth muscle of bronchial airways and pulmonary blood vessels. Antiinflammatory and immunomodulatory

Additonal non-bronchodilatory effects: increase diaphragmatic strength, cortical alertness

Also a weak inhibition of phosphodiesterase, adenosine antagonist, and increases levels of epinephrine
Therapeutic effects of Methyl Xanthines?
Increase Repiratory Muscle Strength
Increase Resp. Muscle endurance
Increase central ventilatory drive
Bronchodilation

(stimulate skeletals, relaxes smooth, + Chrono/inotropic)
Adverse effects of Methyl Xanthines?
Tremor, Headaches, anxiert, nausea, diarrhea, overdoses can cause lethal CV effects, diuresis

Methyl Xanthines have many Drug Interactions
Main use of Theophylline and Aminophylline?
Treatment of acute exacerbations of reversible airway obstruction including status asthmaticus in pt's not responding to 1st line therapies and who have not have theophylline in previous 24 hours.

Theophylline also decreases sleep apnea in heart failure.
Name the two drugs discussed that inhibit mast cell degranulation?
Cromolyn Sodium and Nedocromil

These drugs can be used in combo w/ corticosteroids. Preparations are available OTC (Nasal solution)
Mechanism of action of Cromolyn?
Inhibition of mast cell degranulation by inhibiting IgE antibody-antigen induced Ca influx. Prevents histamine and SRS-A release.

Ineffective for treatment of acute attack. Can attentuate late phase response
Uses of Cromolyn?
Asthma in kids. Prophylactic agent in treatment of mild/moderate asthma.

Pretreatment block antigen and exercise induced asthma.

Good for pt's wakened during sleep due to asthma

MINIMAL SIDE EFFECTS
What are the three Leukotriene Antagonists and Lipoxygenase inhibitors mentioned?
Zileuton (Lox inhib)
Zafirlukast
Mantelukast (SAFEST OF 3)

NOT FOR TREATMENT OF ACUTE EXACERBATIONS
Name the Lipoxygenase inhibitor mentioned?
Zileuton
Contraindications of Zileuton?
Contraindicated in pat's w/ active liver disease or w/ transaminase elevations greater than 3 times upper limit.

Causes a flue like syndrome
Zafirlukast
orally active leukotriene receptor antagonist for tx of asthma. Controls persisten asthma symptoms in adults, kids over 5.
Selectively inhibitrs leukotriene types D4, E4 and leukotriene receptors

Inhibits activity of cytochrome isoenzymes CYP3A4 and CYP2C9
Montelukast (singular)
Oral for prophylaxis/chronic treatment of asthma. DOES NOT INHIBIT CYP2C9 and CYP3A4

Uses include asthma in children (>12mths), chronic treatment/prevention of asthma. Prevention of Aspirin induced asthma, seasonal allergies, and exercise induced asthma.
Rare side effect of Motelukast?
Systemic eosinophilia w/ clinical features of vasculitis (treated w/ corticosteroids).
Side effects shared by Montelukast, Zileuton, Zafirlukast?
All cause increase in hepatic enzymes and dsypepsia/headache
What is the monoclonal antibody used to treat asthma?
Omalizumab (monoclonal Ab directed against IgE)
Mechanism of Omalizumab?
Binds to human IgE preventing binding of IgE to cells associated w/ allergic response
Uses of Omalizumab?
Approved for use in pts >12 to treat allergic asthma inadequately controlled depsite use of inhaled corticosteroids.

SubQ injection
Soluble IL-4 Receptor mentioned
Nuvance
Nuvance action?
Soluble IL-4 receptor that is a cytokine antagonist. IL-4 stimulates production of IgE. May be a positive prophylactic therapy.
Investigational drug for COPF an Asthma?
Roflumilast
Roflumilast actions?
Inhibits PDE4 causeing higher cAMP levels and bronchodilation.
General action of Beta agonists?

General action of Theophylline?
Beta agonists function to increase conversion of ATP to cAMP.

Theophylline decreases the conversion of cAMP to AMP.
Actions of Sympathomimetics (beta 2 agonists)
Relaxation/dilation of bronchial smooth muscle. Long acting agents include Salmeterol, Formoterol, Foradil all used for prophylaxis.

Drugs also facilitate mucociliary transport of secretion and promote expectoration.
Beta2 adrenergics discussed?
Albuterol (onset 5 - 10 min)
Salmeterol/Pirbuterol/Formoterol: long acting
Isoproterenol not used much b/c of pro-arrhythmic effects

Salmeterol + Fluticasone = Advair (controversy).
Toxicities associated w/ Beta 2 Adrenergics
Skeletal muscle tremor, can cause tachycardia/arrhythmias. Excessive use of short acting sympathomimetics known to cause loss of responsiveness to drug. Corticoids used to restore response.
Isoetharine
Beta-2 agonist. Short acting, metabolized by COMT
Metaproterenol/Terbutaline
Longer acting (not metabolized by COMT)
Albuterol
Inhalation, not metabolized by COMT. Increased Beta-2 selectivity, usually most appropriate choice of aerosols in acute asthma attacks
Salmeterol
Beta 2 selective agonist. NOT FOR ACUTE. Used for long term tx of asthma and prevention of bronchospasm in adults w/ reversible COPD.
Side effects associated w/ Salmeterol?
Tachycardia, Hyperglycemia, Hyperkalemia
What is the Corticosteroid, Beta-agonist combination drug administered by inhalation for asthma?
Salmeterol:Fluticasone (ADVAIR)
Catecholamines used for Asthma?
Epinephrine, Isoproterenol,
Mechanism of action for Epinephrine?
Number 1 drug for treatment of status asthmaticus (can cause V.Fib).

Activates alpha and beta receptors. Alpha effects relieve mucosal edema and upper airway congestion. Used for tx of acute bronchospasm, resp. manifestations of anaphylaxis, or tx or severe asthma.
Isoproterenol?
Non-selective Beta agonist. Not used much b/c of cardiac effects.