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Egan's Ch. 32
Airway Pharmacology
| Question | Answer |
|---|---|
| What are the three phases of drug action? | drug administration phase, pharmacokinetic phase, pharmacodynamic phase |
| drug administration phase | method by which a drug dose is made available to the body; (How are we going to deliver it?) |
| What is the most common route of drug administration to a pulmonary patient? | aerosol therapy |
| What are the three most common devices used to administer inhaled aerosols? | MDI (metered-dose inhaler), SVN (small volume nebulizer), DPI (dry-powder inhaler) |
| What are the ADVANTAGES of inhaled aerosols? | can use smaller doses (as compared to the systemic route), onset of drug is rapid, delivery is targeted to specific organ needing treatment, less systemic side effects |
| What are the DISADVANTAGES of inhaled aerosols? | the number of variables affecting the delivered dose AND lack of knowledge of device performance by patients & caregivers |
| pharmacokinetic phase | time course & disposition of drug in body based on its absorption, distribution, metabolism & elimination |
| Inhaled bronchoactive aerosols are intended for local effects in the airway; UNDESIRED systemic effects result from what? | absorption and distribution throughout the body |
| What is the difference between a fully ionized aerosol drug and a non-ionized aerosol drug? | A fully ionized drug has little or NO systemic side effects (it is not absorbed across lipid membranes) whereas a non-ionized drug produces systemic side effects (it is lipid soluble & diffuses across cell membranes and into bloodstream) |
| What is an example of a fully ionized aerosol drug? | Ipratropium |
| What is an example a non-ionized aerosol drug? | Atropine (side effects: mydriasis: dilation of pupils AND blurred vision) |
| What is the L/T ratio? | Lung availability/total systemic availability; quantifies efficiency of aerosol drug to lung; L/T ratio=Lung availability/(Lung + GI Availability) |
| Using the L/T ratio, which aerosol delivery method is more efficient? | MDI (46%) works a little better than DPI (23%) |
| Pharmacodynamic phase | describes the MECHANISM OF ACTION by which a drug molecule causes its effects in the body |
| What are drug effects caused by? | the combination of a drug with a matching receptor |
| The nervous system is divided into what two paths? | Central & Peripheral |
| Central Nervous System | brain & spinal cord |
| Peripheral Nervous System | sensory (receives impulses), somatic (sends voluntary impulses: ex: putting hand in fire and pulling it out), autonomic (sends involuntary impulses ex: breathing) |
| What three things make up the autonomic (involuntary) system? | parasympathetic, muscarinic (M3), Sympathetic |
| Parasympathetic receptors | CHOLINERGIC: acetylcholine> cGMP> bronchoconstriction |
| Sympathetic receptors | ADRENERGIC: norepinephrine (epinephrine)> cAMP> bronchodilation |
| What is cAMP constantly being degraded by? | phosphodiesterase |
| Muscarinic (M3) | acts like parasympathetic; stimulates acetylcholine receptors specifically at parasympathetic nerve-ending sites |
| What is the usual neurotransmitter in the sympathetic system? | norepinephrine (epinephrine), aka adrenaline |
| What is the usual neurotransmitter in the parasympathetic system? | acetylcholine |
| Adrenergic directly dilates what? | the bronchial tree; antiadrenergic blocks receptor for epinephrine |
| Cholinergic causes what? | bronchoconstriction; Don't want that, so you need and anti-cholinergic drug that BLOCKS the constriction (Atrovent-would never give by itself) |
| indications for Adrenergic short-acting agents | rescue drugs good for about 4 hours; for relief of acute obstructive airflow obstruction; albuterol and levalbuterol |
| Albuterol | 2.5 mg qid (4 times a day); Beta-2 |
| Indications for Adrenergic long-acting agents | drugs that will last 12 hours (bid), in MDIs and DPI; salmeterol, formoterol, arformoterol; for maintenance of bronchodilation with obstructive lung disease |
| What is the most common use of adrenergic bronchodilators? | improve the flow rates in asthma & exercise induced asthma, acute and chronic bronchitis, emphysema, bronchiectasis, cystic fibrosis and other obstructive airway states |
| Racemic epinephrine | adrenergic bronchodilator; reduces airway swelling after extubation or with acute upper airway inflammation from croup, epiglottitis or bronchiolitis or to control airway bleeding during endoscopy |
| alpa-receptor stimulation | causes vasoconstriction and a vasopressor effect (increased blood pressure) |
| beta-1-receptor stimulation | causes increased heart rate and myocardial contractility |
| beta-2-receptor stimulation | relaxes bronchial smooth muscle, stimulates mucociliary activity, and has some inhibitory action on inflammatory mediator release |
| Why would you choose Xopenex over Albuterol? | When patient comes in with a high heart rate |
| Levalbuterol | 1.25 (.63) mg TID/QID; beta-2 |
| What is the main side effect of beta-2 selective agents? | tremor |
| What are the potential adverse effects with use of adrenergic bronchodilators? | dizziness, hypokalemia, worsening ventilation/perfusion ratio (decrease in PaO2/SpO2) |
| What are the specific actions suggested to evaluate patient response to bronchodilator therapy? | pre & post bronchodilator studies, ABG or pulse oximetry, blood glucose & potassium (if available), and blood pressure |
| What are the two inhaled anticholinergic bronchodilators? | Ipratropium and tiotropium (both used for COPD) |
| What is combined anticholinergic and beta-agonist indicated for? | Ipratropium bromide & albuterol (Duoneb) is indicated for patients with COPD or asthma |
| What is the mode of action of anticholinergic bronchodilators? | act as competitive antagonists for acetylcholine on airway smooth muscle |
| What are the adverse effects of anticholinergic bronchodilators? | atrovent produces side effects and eyes can accidentally be sprayed by MDI or nebulizer mask |
| What are the side effects seen with anticholinergic aerosol agents? | cough & dry mouth |
| What are the two mucus-controlling agents? | N-acetyl-cysteine (called Muco Mist) and Dornase alfa |
| N-acetyl cysteine (NAC) comes in what two concentrations? | 10% and 20% |
| How is NAC given to patient? | either by nebulization or by direct tracheal installation |
| How does NAC work? | breaks down disulfide bonds of the mucus, thinning it, so patient can cough it out themselves |
| What can NAC cause? | bronchospasm due to irritating side effects (reason why you never give it without bronchodilator- Albuterol) |
| What patients get treated with Dornase alfa? | Patients with Cystic Fibrosis |
| What is the mode of action of Dornase alfa? | It breaks down protein bonds (DNA) and thins it |
| What is the other name for Dornase alfa? | Pulmozyme |
| Inhaled corticosteroids will help reduce swelling if it is ________, it wont help if it's _________ | Inflammatory; bronchoconstriction |
| What is the mode of action of inhaled corticosteroids? | they act on intracellular receptors |
| What are the three types of drugs that prevent asthma from happening? | (1) Cromolyn sodium (2) Antileukotrienes (3) Monoclonal antibodies or anti-IgE agents REMEMBER THESE 3 ARE NOT RESCUE DRUGS |
| What are the indications for use of nonsteroidal antiasthma drugs? | Prophylatic management of asthma; offers NO BENEFIT for acute airway obstruction in asthma |
| Pentamindine isethionate | treats pneumonia caused by pneumocystis jiroveci which is seen in patients with AIDS |
| Ribavirin | treats respiratory syncytial virus using SPAG generator |
| Inhaled tobramycin | used to fight pseudomonas aeruginosa in patients with cystic fibrosis |
| Inhaled zanamivir | treats influenza A; Tamiflu |
| Nitric oxide | treatment of pulmonary hypertension most common side effect: hypotension |