Miscellaneous Quiz / anti-asthmatic agents

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Can you name the anti-asthmatic agents?

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HintAnswer
Plasma concentration of methylxanthine 5-20 mg/ml
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.
Metaproterenol class
Montelukast class
Budesonide class
SE: occasional liver toxicity
MOA: LTD4 receptor antagonist (prevents leukotriene-induced bronchoconstriction)
Salmetrol class
SE: comparable to placebo, rash, GI upset, bleeding, viral infections, may increase potential for malignant neoplasms
MOA: 5-lipooxygenase inhibitor --> decreased leukotriene production
MOA: b2 receptor agonist -> increased intracellular cAMP and smooth muscle relaxation -> relaxed airway smooth muscle -- somewhat resistant to receptor downregulation and desensiti
MOA: alters chloride channel function reducing mast cell degranulation and nerve conduction in lungs mediating cough
Cromolyn class
Formoterol class
Plasma concentration of methylxanthine > 20 mg/ml
Clearance by liver, rate varies widely -- fastest in children, slowest in neonates and infants, dose corrected needed in liver dz.
SE: inhaled (low), tachycardia, cardiac arrhythmias, tremulousness, muscle cramps, metabolic disturbances
Pirbuterol class
MOA: lowers IgE to undetectable levels: inhibit the binding of IgE to mast cells. Inhibits early and late responses to antigen challenge
Used systemically: very severe persistent asthma uncontrolled by ICS and LABA or for emergent severe asthma or exacerbation of symptoms
Used if beta-2-glucocorticoid combo is not effective. Not preferred, used as an alternative
Most effective bronchodilator is theophylline. Given as different salts, good PO absorption.
MOA: phosphodiesterase inhibitor --> increased cAMP and cGMP AND adenosine receptor antagonist --> smooth muscle relaxation. Mild to moderate bronchodilator
HintAnswer
Theophylline class
Added to inhaled corticosteroid for increased symptomatic relief in moderate to severe asthma. >12 hrs
MOA: increases release of norepinephrine used as a second-line asthma therapy
MOA: inhibits late phase of airway inflamm & hyperreactivity via inhibition of transcription of pro-inflamm mediators & enzymes. Inactivates phospholipase A2 preventing prod of pro
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
Possible contraindications or caution needed with sympathomimetics, SABAs, and LABAs for:
Tiotropium class
SE: increased mortality with monotherapy -- systemic effects are reduced by inhalation application
Mometasone furoate class
Prednisone class
Most effective med for symptomatic relief of acute bronchospasm. Used in mild to moderate asthma alone or in combo for severe asthma.
Methylprednisolone
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
Not appropriate for monotherapy
MOA: muscarinic receptor antagonist --> blocks parasympathetic bronchoconstriction and mucus release
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
SE: well tolerated, occasional N/V, bitter taste, sore throat, HA, cough, rhinitis
Plasma concentration of methylxanthine > 40 mg/ml
Caffiene class
Terbutaline class
L-albuterol class
Sympathomimetic drugs
More than one canister/month suggests inadequate asthma control. Regularly scheduled use is not recommended.
HintAnswer
SE: B1 effects: tachycardia, arrhythmia, angina pectoris
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
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
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
Beclomethasone class
Drug(s) which may cause older adults to experience confusion, agitation, and changes in glucose metabolism
Flunisolide class
Ipratropium class
Nedocromil class
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.
Triamcinolone class
Albuterol class
Theobromine class
Zileuton class
MOA: decreases vascular permeability and potentiates B-agonist effects on airway obstruction. Inhaled are more effective in the long term
Advantage = inexpensive and oral; Disadvantage = needs plasma monitoring, insomnia, serious toxicity of OD
MOA 2: Inhibits function of immune cells - inhibit cell growth, prevent release of inflammatory mediators and cytokines, susceptible to receptor down regulation and desensitization
Used as an inhaled agent. Most potent and effective. Mild persistent or exercise induced asthma, and moderate to severe asthma
Zafirlukast class
Always given in combo with anti-inflammatory. Used long-term mgmt of moderate and severe persistent asthma. Not for acute symptoms or exacerbation.
Omalizumab class

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