Term
| Properties that facilitate systemic drug delivery via the lungs include: |
|
Definition
The absorptive surface area in the lung is very large (surface area of alveoli >
100m2) and its aqueous volume is small
- Epithelial cells are generally permeable to drugs
- Drugs are usually not metabolized in the lung |
|
|
Term
| Are drugs metabolized in the lung? |
|
Definition
|
|
Term
| Aeorsolized drugs may be rapidly absorbed into the systemic circulation with high/low bioavialability? |
|
Definition
|
|
Term
| Potential problems for using the lungs for drug delivery: |
|
Definition
Formulating and delivering drugs as aerosols (particle size should be
1-5 um for maximum absorption)
- Slowing the absorption rate so that drug effects last longer
- Minimizing systemic absorption if a local effect is desired |
|
|
Term
| Advantages for using inhalation drugs for lung disease: |
|
Definition
- Drug is administered directly to the target tissue
- Onset of drug action is rapid
- May be fewer systemic effects (which increases the therapeutic index)
- Can use drugs that are not effective orally |
|
|
Term
| Problems in using inhalation drugs for lung disease: |
|
Definition
- Drug design and delivery is more complicated, because drugs must be retained
in the lung and not absorbed
- Delivery systems can be difficult to use effectively because they require hand-diaphragm
coordination (hard in kids & elderly) |
|
|
Term
| Asthma is typically characterized by: |
|
Definition
acute episodes of reversible bronchoconstriction
superimposed upon chronic airway inflammation, hyperresponsiveness,
obstruction, and remodeling; histologically, goblet cell hyperplasia, thickened
basement membranes, and an eosinophillic infiltrate are observed |
|
|
Term
| Drug therapy in asthma aims to: |
|
Definition
| relieve bronchospasm & control inflammation |
|
|
Term
| Beta-2 agonists activate: |
|
Definition
| adenlylate cyclase --> increases cAMP levels & inactivating mysoin light chain kinase |
|
|
Term
| Short acting Beta-2 agonists include: |
|
Definition
| albuterol, biolterol, pirbuterol, terbutalene |
|
|
Term
| Short acting Beta-2 agonists are used for: |
|
Definition
| relief of breakthrough symptoms & immediate prevention of exercise-induced asthma |
|
|
Term
| Long acting Beta-2 agonists include: |
|
Definition
salmeterol & fomoterol
given with corticosteroids to improve asthma control |
|
|
Term
|
Definition
| loss of responsiveness to a drug after prolonged treatment |
|
|
Term
| Is tachyplylaxis common in SABA and LABA? |
|
Definition
|
|
Term
| Systemic effects of B-2 agonists (tachycardia: B-1 mediated, skeletal muscle tremor: B-2 mediated) are relatively rare when: |
|
Definition
| B-2 agonists are given by inhalation |
|
|
Term
|
Definition
| intracellular receptors --> alter gene expression --> decreases cellular production of inflammatory mediators & reduces the # of inflammatory cells |
|
|
Term
| Corticosteroids block formation of: |
|
Definition
| arachadonic acid from membrane phospholipids |
|
|
Term
| systemic effects of Corticosteroids include: |
|
Definition
adrenal insufficiency (suppression of pituitary-adrenal axis), suppression of cellular immunity (esp. lymphocytes), metabolic effects: glucose intolerance (hyperglycemia, DM), protein catabolism (muscle wasting), osteoporosis, growth retardation (children)
effects mitigated with given via inhalation |
|
|
Term
| Beclomehasone, budesonide, fluisonide, fluticasone, trimacinolone are examples of: |
|
Definition
| inhaled glucocoricosteroids used to treat asthma |
|
|
Term
| Primary drugs for controlling all but mildest forms of asthma: |
|
Definition
| inhaled glucocorticosteroids |
|
|
Term
| Inhaled glucocoritcosteroids are often administered in combination with: |
|
Definition
|
|
Term
| How do inhaled glucocorticosteroids improve lung function? |
|
Definition
| suppress inflammation --> decrease bronchial hyperreactivity, reduce frequency of asthma attacks, reduce use of SABA |
|
|
Term
| Systemic effects of inhaled glucocorticosteroids? |
|
Definition
rarely; at higher doses, there is a small risk of cateracts & osteoperosis
local adverse effects: oral candidiasis & hoarseness |
|
|
Term
|
Definition
| 5-lipoxygenase, preventing the production of leukotrienes form arachidonic acid |
|
|
Term
| Montelukast & Zafirlukast are examples of: |
|
Definition
| Leukotriene receptor antagonists |
|
|
Term
| leukotriene receptor antagonists (Montelukast, Zafirlukast) are what type of antagonists? |
|
Definition
| competitive antagonists @ the cysLT receptor, type 1 |
|
|
Term
| leukotriene receptor antagonists have what type of effect? |
|
Definition
| anti-inflammatory; cause bronchodilation |
|
|
Term
| How are leukotriene receptor antagonists administered? |
|
Definition
|
|
Term
| adverse effects of leukotriene receptor antagonists: |
|
Definition
|
|
Term
| These are used as alternatives or in addition to corticosteroids for persistent asthma (esp. in cases of aspirin senstive asthma & for patients that have problems using an inhaler) |
|
Definition
| leukotriene receptor antagonists |
|
|
Term
| Cromolyn & Nedocromil interfere with the action of: |
|
Definition
| chloride channels; interfere with activation of mast cells & eosinophils, preventing the release of allergic mediators |
|
|
Term
| These drugs prevent the activation of mast cells and eosinophils in asthma: |
|
Definition
|
|
Term
| Cromolyn & Nedocromil are administered: |
|
Definition
|
|
Term
| Cromolyn & Nedocromil are more/less effective than corticosteroids? |
|
Definition
|
|
Term
| Do Cromolyn & Nedocromil produce bronchodilation? |
|
Definition
|
|
Term
| adverse effects of Cromolyn & Nedocromil: |
|
Definition
|
|
Term
| Used instead of corticosteroids as a prophylaxis for exercise and alergen-induced asthma in children during their growth spurt |
|
Definition
|
|
Term
|
Definition
| recombinant humanized monoclonal antibody that binds to free IgE in the circulation & blocks its attachment to mast cells & basophils, preventing the cells from responding to allergens |
|
|
Term
| how is Omalizumab administered? |
|
Definition
| subcutaneously, every 2-4 weeks |
|
|
Term
| who should use Omalizumab? |
|
Definition
patients with:
1) Moderate to severe persistent asthma
2) Frequent asthma exacerbations, often requiring hospitalization
3) Symptoms inadequately controlled by inhaled steroids
4) High levels of allergen-specific IgE
it's expensive though! ($500-1,000/dose) |
|
|
Term
| How to manage severe persistent (continual) asthma? |
|
Definition
High dose inhaled glucocorticoid
plus a long-acting inhaled Beta-2 agonist |
|
|
Term
| How to manage moderate persistent asthma symptoms? |
|
Definition
Low dose inhaled glucocorticoid plus
a long-acting inhaled Beta-2 agonist or a medium-dose inhaled
glucocorticoid |
|
|
Term
| How to manage mild persistent asthma?(More than Twice a Week but Less than Daily) – |
|
Definition
| Low dose inhaled glucocorticoid |
|
|
Term
| How to manage mild intermittent symptoms of asthma (Less than Twice a Week)? |
|
Definition
|
|
Term
| How to give quick relieve to all asthma patients? |
|
Definition
|
|
Term
| COPD is characterized by: |
|
Definition
histologically by thickening of the airway walls, infiltration with
lymphocytes, macrophages, and neutrophils, loss of alveolar attachments,and the collapse of bronchiolar lumen;
patients present with progressive
dyspnea, cough, and sputum production |
|
|
Term
| Is COPD an allergic disease? |
|
Definition
|
|
Term
| What is central to symptom control in COPD? |
|
Definition
|
|
Term
| Inhaled or systemic treatment for COPD? |
|
Definition
|
|
Term
| Drug combinations have these advantages in COPD: |
|
Definition
| may be more efficacious & less toxic than high doses of single drugs |
|
|
Term
|
Definition
inhaled muscarinic antagonist
short acting (6-8hrs) |
|
|
Term
|
Definition
inhaled muscarinic antagonist
long acting (24+ hrs) |
|
|
Term
| Inhalde muscarinic antagonists (ipratropium, tiotropium) are used to manage: |
|
Definition
|
|
Term
| Adverse effects of anti-cholinergic drugs include: |
|
Definition
| dry mouth, urinary retention (esp in patients with prostatic hypertrophy), increased intraocular pressure (bad in patients with glaucoma) |
|
|
Term
| Anti-cholinergic drugs cause what to happen in patients with COPD? |
|
Definition
bronchodilation
often better than B2 agonists for patients with COPD |
|
|
Term
|
Definition
| PDE, producing bronchodilation |
|
|
Term
|
Definition
| purinergic receptors, which blocks bronchoconstriction |
|
|
Term
| Theophylline is administered: |
|
Definition
| orally, --> systemic effects |
|
|
Term
| Patients taking theophylline should be monitored because of its: |
|
Definition
|
|
Term
| Why does theophylline have many drug interactions? |
|
Definition
| it interferes with CYP enzymes |
|
|
Term
| Adverse effects of theophylline include: |
|
Definition
| N/V, skeletal tremor, insomnia, arrhythmias, seizures |
|
|
Term
| Management of COPD: Stage 0 (FEV 100% predicted), at risk: |
|
Definition
| smoking cessation + influenza vaccination |
|
|
Term
| Management of COPD: Stage 1 (FEV 80-100% predicted), mild: |
|
Definition
| add short acting broncodilator as needed |
|
|
Term
| Management of COPD: Stage 2 (FEV 50-80% predicted), moderate: |
|
Definition
| add long acting bronchodilator |
|
|
Term
| Management of COPD: Stage 3 (FEV 30-50% predicted), severe: |
|
Definition
| add inhaled glucocorticoid |
|
|
Term
| Management of COPD: Stage 4 (FEV <30% predicted), very severe: |
|
Definition
| add long term O2 therapy for respiratory failure |
|
|
