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14 Cards in this Set
- Front
- Back
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Albuterol (Proventil)
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Class: β2 Adrenoceptor Agonist (short acting)
MOA: G-coupled receptor Ligand binding moves receptor to active state G protein disassociates into Gα and β/γ dimer Gα activates adenylate cyclase ↑ cAMP in cell cAMP activates protein kinase A (PKA) PKA phosphorylates substrates that control Calcium in cell ↓ calcium concentration in cell Myosin light chain is unable to sustain contraction Other mechanisms: Gi mediated mechanism β2 receptors found on mast cells, macrophages and other pro-inflammatory and immune cells Dephosphorylation of MLC ↑ requirement for calcium Promotes relaxation Pharm: Bronchodilation ↓ inflammatory cytokine production ↓ responsiveness ↓ plasma exudation Indications: acute relief of bronchospasm Adverse: Seen with long term use -↑ asthma exacerbations -Loss of bronchoprotection Receptor Desensitization Causes? -Receptor down regulation -Genetic polymorphisms of beta receptor -Isomer effects: Levalbuterol (Xopenex) |
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Advair (fluticasone propionate and salmeterol)
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Class: Inhaled steroid and β2 Adrenoceptor Agonist (long acting)
MOA: Synergistic effect β2 receptor gene has GRE sites -Offset one of the mechanisms for desensitization Long acting β2 agonists -Promote translocation of glucocorticoid receptor into the nucleus with no ligand present -Accelerate the rate of translocation when ligand is present Salmeterol is long acting because it binds in an ecosite inside the receptor Binds in the membrane (High Log P) and creates a micro depot of drug Pharm: For β2 agonist- Bronchodilation ↓ inflammatory cytokine production ↓ responsiveness ↓ plasma exudation For Steroid- Anti-Inflammatory Effects -Inhibit accumulation of macrophages and leukocytes -Inhibit phagocytosis -Inhibit lysosomal enzyme release -Inhibit release of chemical mediators of inflammation Indications: controller for asthma Pharm effects in COPD- ↓ severity and ↓ frequency of exacerbations ↓ systemic inflammation ↓ rate of decline Adverse: For steroid - Oropharyngeal candidiasis, Dysphonia, Lead to decrease adherence and quality of life For β2 agonists - Seen with long term use -↑ asthma exacerbations -Loss of bronchoprotection Receptor Desensitization Causes? -Receptor down regulation -Genetic polymorphisms of beta receptor -Isomer effects: Levalbuterol (Xopenex) |
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Xanthine (Theophylline)
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Class: Bronchodilator
MOA: Inhibition of Phosphodiesterase Direct histone deacetylase activation Pharm effects: Bronchodilation Anti-inflammatory -↓ mediator release from inflammatory cells -↓ allergen response Adverse: Nausea, vomiting, headache, and insomnia Overdose: persistent vomiting, cardiac arrhythmias, and intractable seizures which can be lethal |
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Ipratropium (Atrovent)
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Class: Anticholinergic bronchodilator
MOA: Competitive antagonism of acetylcholine at M3 receptors in the lung Effects: t½ = 0.3 hour Adverse effects: Dry mouth, altered taste and coughing after administration |
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Tiotropium (Spiriva)
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Class: Anticholinergic bronchodilator
MOA: Competitive antagonism of acetylcholine at M3 receptors in the lung Effects: t½ = 35 hours Used in once a day dosing in COPD Adverse effects: Dry mouth, altered taste and coughing after administration |
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Montelukast (Singulair)
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Class: Leukotriene receptor inhibitor
MOA: Competitive antagonist of the cysteinyl leukotriene receptor Indications: Asthma and seasonal allergic rhinitis Adverse: Avoid ASA and NSAIDs |
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Zileuton (Zylfo)
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Class: Leukotriene formation inhibitor
MOA: Inhibits 5-lipooxygenase Indication: Prophylaxis and chronic treatment of asthma Adverse: Can cause liver problems Liver enzymes must be monitored during therapy |
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Omalizumab (Xolair)
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Class: Antibody
MOA: Murine anti-human monoclonal antibody Directed against a fragment that binds to the IgE receptor Only binds to free IgE ↓ free IgE by 99 % Down regulates receptor expression on basophils ↓ IgE mediated inflammation Indications: Nasopharyngitis, upper respiratory tract infection, headache 0.1 % anaphylaxis in 2-24 hours after administration Adverse: Black box warning |
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Infliximab (Remicade)
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Class: Antirheumatic
MOA: Monoclonal antibodies consisting of the ligand binding portion of the TNFα receptor Indications: RA Effects: Improve symptoms, do not cure disease Adverse: Increased risk for -TB -Invasive fungal infections -Sepsis -CNS demyelination |
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NSAIDs
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Acute therapy for gout
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Steroids
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Acute therapy for gout, RA
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Colchicine
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Mechanism:
arrests mitosis in metaphase by binding to the microtubular protein and preventing spindle formation Inhibits neutrophil migration and phagocytic activity in inflamed joints Inhibits the inflammatory response by inhibiting neutrophil activation Decreased - trafficking of phagocytosed particles to lysosomes - release of chemotactic factors - motility and adhesion of neutrophils - phosphorylation of neutrophil proteins Indicatitons: Acute therapy for gout Adverse Effect: Diarrhea |
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Allopurinol (Zyloprim)
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Class: Xanthine oxidase inhibitor
MOA: Oxidized to oxypurinol Oxypurinol’s elimination t1/2 much longer Non-competitive inhibitor of xanthene oxidase Decreases the biosynthesis of uric acid Hypoxanthine and xanthine -Soluble in blood -Renally excreted without crystal deposition Indications: Chronic therapy for gout |
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Probenecid
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Class: Uricosuric agent
MOA: Inhibits the basolateral anion exchanger of the proximal tubule Blocks the tubular reabsorption of urate -decreasing the concentration of urate in the plasma Development of urate stones in kidney or ureter Co-administration of calcium citrate to make urine less acidic Indications: Chronic therapy for gout Adverse: Sore gums |
