Integrated Science I - Exam 2 Drugs

Beta-2 Agonist for Acute Therapy (Albuterol targets R/S isomers; Levalbuterol specifically targets R isomer) Stimulates b2 receptors; activates adenylate cyclase and increases cAMP to produce relaxation of smooth muscles; bronchodilation Treats bronchospasm R/T asthma, bronchitis; rapid reversal of airway obstriction Common: nervousness, tremor, palpitation, tachycardia, bad taste, throat irritation Serious: Urticaria, QT Prolongation, arrhythmia, paradoxical bronchospasm Contraindication: allergy, uncontrolled cardiac dysrhythmias (esp. tachy-arrhythmia)

Beta-2 Agonist for Acute Therapy (Long-Acting BA) Stimulates b2 receptors; activates adenylate cyclase and increases cAMP to produce relaxation of smooth muscles; bronchodilation Treats bronchospasm R/T asthma, bronchitis; reduce impairment and risk Common: nervousness, tremor, palpitation, tachycardia, bad taste, throat irritation Serious: Urticaria, QT Prolongation, arrhythmia, paradoxical bronchospasm Contraindication: allergy, uncontrolled cardiac dysrhythmias (esp. tachy-arrhythmia)

Methylxanthines (plant alkaloid product) (related to beta-agonist but has longer T_1/2 but slower onset) Block phosphodiesterase enzymes, which lead to increased cAMP in bronchial smooth muscle leading to relaxation Used to releve bronchospasms in asthma, chronic bronchitis, emphysema; has large interpatient variability in clearance Common: N/V, anorexia Serious: Cardiac arrhythmia, seizure, death

Anticholinergic (Atrovent T_1/2 - 2 hours, Handihaler T_1/2 - 5-6 days) Blocks postganglionic vagal pathway to decrease vagal tone and cause vasodilation; Atrovent is a quaternary amine Prevents bronchospasm associatd with chronic bronchitis or emphysema, Symptomatic relief of rhinitis (Handihaler can be used qid) Common: N/V, diarrhea, nasal congestion, dyspnea, dry mouth Contraindication: allergy to atropine, Myasthenia gravis, narrow angle glaucoma, Tiotropium should not be used with Ipratropium

Corticosteroid Inhalants (typical first-line of Tx) Increases number and sensitvity of B2 receptors; Inhibits neutrophil and eosinophil invasion into tissues and Inhibits synthesis of inflammatory substances from cells Reduces inflammation thereby reducing mucus production and swelling of airways Common: sinusitis, rhinitis, hoarseness, headache, nausea, diarrhea, oral Candidiasis Serious (rare): Adrenal suppression at high doses, osteoporosis/indefinite growth suppression in kids, bronchospasm, peptic ulcers

Leukotriene receptor antagonist/modifier Blocks leukotriene receptors, preventing leukotrienes from participating in inflammatory responses; Zyflo works by inhibiting the enzyme that makes leukotriene; metabolized by CYP450 Treats chronic asthma and seasonal rhinitis in adults and chilren Common: Flu-like symptoms Serious: Angioedema, Anaphylaxis, Churg-Strauss syndrome (may be coincidental) Contraindications: Hypersensitivity to active component or any components of preparation

Mast cell stabilizer Prevents the release of histamine and inflammatory mediators from mast cells by stabilizing membranes which reduces the release of inflammatory and bronchoconstructive substances reducing bronchoconstriction Treats prophylaxis of asthma and allergic disorders, certain opthalamic disorders and (unlabeled) food allergies, prevents/treats seasonal rhinitis; has slow onset of 1-2 weeks Contraindications: Hypersensitivity to cromolyn, may have acute asthma attack due to slow onset

Monoclonal Antibody preparations Inhibits IgE binding to mast cell and basophil receptors, preventing degranulation and reducing the release of allergic response mediators Indicated for patients who do not respond to inhaled corticosteroids, is injectable and very costly; developed by mice IgE which is then "humanized"

Antihistamine/H1 Antagonist (1st generation OTC) Blocks H1 receptors so that histamine cannot bind; Meds cross BBB and can produce central effects (more sedating) Used for "cold remedies" Adverse: Dry mouth, blurred vision, constipation Contraindications: breastfeeding women, men with BPH, patients with glaucoma

Antihistamine/H1 Antagonist (2nd generation OTC except Allegra/D) Blocks H1 receptors so that histamine cannot bind; less sedating because it does not cross BBB Used for "cold remedies" Adverse: fewer anticholinergic effects

Alpha 1 Agonist/Decongestant (Intranasal OTC) stimulates a1 to produce vasoconstriction; is also a component of many OTC cold formulas Decreases swelling, edema and stuffy nasal passages Adverse: Tachycardia, increased BP, dysrhythmias, restlessness, insomnia, anxiety, tremor, rebound phenomenon Contraindications: HTN (may have increased effects of HTN), CAD, do not used with TCAs, beta blockers, MAOIs

Alpha 1 Agonist/Decongestant (Systemic OTC) stimulates a1 to produce vasoconstriction; is also a component of many OTC cold formulas Decreases swelling, edema and stuffy nasal passages Adverse: Tachycardia, increased BP, dysrhythmias, restlessness, insomnia, anxiety, tremor, rebound phenomenon Contraindications: HTN (may have increased effects of HTN), CAD, do not used with TCAs, beta blockers, MAOIs

Prescriptive Corticosteroid (Local effects) Intranasal antiinflammatory, decreases release of inflammatory mediators Onset may require several weeks Adverse: irritates nasal passages Contraindications: Pregnancy, may possibly decrease growth rate in children

Expectorant Decreases the vicosity of mucus to aid in elimination

Antitussive Depresses medullary cough center to prevent coughs