Miscellaneous / anti-asthmatic agents

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Can you name the anti-asthmatic agents?

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HintAnswer
SE: increased mortality with monotherapy -- systemic effects are reduced by inhalation application
MOA: lowers IgE to undetectable levels: inhibit the binding of IgE to mast cells. Inhibits early and late responses to antigen challenge
Zileuton class
Low risk for adverse SE at recommended dose. Reduce SE with spacer and rinsing mouth; use lowest dose; use in combo w/ LABA. Monitor growth in kids - poorly controlled asthma may d
Used as an inhaled agent. Most potent and effective. Mild persistent or exercise induced asthma, and moderate to severe asthma
Used for long-term control in mild persistent asthma (secondary to corticoids) In combo ICS, allergic rhinitis. Improves lung function, reduces need for SABA, prevents exacerbation
SE: well tolerated, occasional N/V, bitter taste, sore throat, HA, cough, rhinitis
L-albuterol class
Caffiene class
Pirbuterol class
Plasma concentration of methylxanthine 5-20 mg/ml
Used in adjunctive therapy only for patients > 12 yrs who have allergies and moderate to severe persistent asthma inadequately controlled with ICS. Given SC q 2-4 weeks
SE: occasional liver toxicity
Salmetrol class
Cromolyn class
Terbutaline class
Plasma concentration of methylxanthine > 40 mg/ml
Drug(s) which in older adults may be associated with dose-dependent reduction in bone mineral content. Needs to be given with Ca supplements and Vit D.
More than one canister/month suggests inadequate asthma control. Regularly scheduled use is not recommended.
Metaproterenol class
Used as 1st line therapy for COPD or in combo with b2/steroid for moderate asthma for relief of acute bronchospasm. Added to SABA or given if SABA not tolerated
Ipratropium class
Used if beta-2-glucocorticoid combo is not effective. Not preferred, used as an alternative
HintAnswer
Albuterol class
MOA: b2 receptor agonist -> increased intracellular cAMP and smooth muscle relaxation -> relaxed airway smooth muscle -- somewhat resistant to receptor downregulation and desensiti
Prednisone class
MOA: decreases vascular permeability and potentiates B-agonist effects on airway obstruction. Inhaled are more effective in the long term
Added to inhaled corticosteroid for increased symptomatic relief in moderate to severe asthma. >12 hrs
Clearance by liver, rate varies widely -- fastest in children, slowest in neonates and infants, dose corrected needed in liver dz.
Formoterol class
Mometasone furoate class
Omalizumab class
Theophylline class
Advantage = inexpensive and oral; Disadvantage = needs plasma monitoring, insomnia, serious toxicity of OD
SE: comparable to placebo, rash, GI upset, bleeding, viral infections, may increase potential for malignant neoplasms
Sympathomimetic drugs
Zafirlukast class
Used systemically: very severe persistent asthma uncontrolled by ICS and LABA or for emergent severe asthma or exacerbation of symptoms
Most effective med for symptomatic relief of acute bronchospasm. Used in mild to moderate asthma alone or in combo for severe asthma.
Limit to 5-10 days. Many SE: change in glucose metabolism, increased appetite, wt gain, fluid retention, mood changes, peptic ulcer, HTN, adrenal suppression (cushings), candiasis
MOA: 5-lipooxygenase inhibitor --> decreased leukotriene production
Tiotropium class
Budesonide class
Most effective bronchodilator is theophylline. Given as different salts, good PO absorption.
SE: dose dependent tox (monitor plasma levels), low anorexia, N/V, abd discomfort, HA, anxiety. May cause nervousness and insomnia. High level of seizures and arrhythmias.
Triamcinolone class
HintAnswer
MOA 2: Inhibits function of immune cells - inhibit cell growth, prevent release of inflammatory mediators and cytokines, susceptible to receptor down regulation and desensitization
SE: inhaled (low), tachycardia, cardiac arrhythmias, tremulousness, muscle cramps, metabolic disturbances
MOA: alters chloride channel function reducing mast cell degranulation and nerve conduction in lungs mediating cough
Always given in combo with anti-inflammatory. Used long-term mgmt of moderate and severe persistent asthma. Not for acute symptoms or exacerbation.
Theobromine class
MOA: LTD4 receptor antagonist (prevents leukotriene-induced bronchoconstriction)
Drug(s) which may cause older adults to experience confusion, agitation, and changes in glucose metabolism
SE: B1 effects: tachycardia, arrhythmia, angina pectoris
Not appropriate for monotherapy
Nedocromil class
Possible contraindications or caution needed with sympathomimetics, SABAs, and LABAs for:
MOA: phosphodiesterase inhibitor --> increased cAMP and cGMP AND adenosine receptor antagonist --> smooth muscle relaxation. Mild to moderate bronchodilator
Flunisolide class
Montelukast class
Used in long-term prevention of symptoms, PROPHYLACTIC use only. Use if nonresponder to steroid, want to reduce steroid dose when used in combo or when inciting stimulus is known
MOA: increases release of norepinephrine used as a second-line asthma therapy
Beclomethasone class
MOA: muscarinic receptor antagonist --> blocks parasympathetic bronchoconstriction and mucus release
MOA: inhibits late phase of airway inflamm & hyperreactivity via inhibition of transcription of pro-inflamm mediators & enzymes. Inactivates phospholipase A2 preventing prod of pro
Methylprednisolone
Plasma concentration of methylxanthine > 20 mg/ml

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