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Pharmacology
week 4 (respiratory)
75
Other
Not Applicable
02/02/2008

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Cards

Term
Asthma
Definition

chronic inflammatory disease of airways; predominantly disease of inflammation w/ superimposed bronchospasm causing reversible airway obstruction; all triggers produce same response in airways - constrictin of smooth muscle of airway, inflammation & edema of bronchial mucosa & increased productin of bronchial mucus

 

so, wheezing on exhalation 

Term
Asthma classification steps:
Definition
  • Mild intermittent: less than or equal to 2 days/wk and 2 nights/mo
  • Mild persistent: greater than 2/wk but less than 1x/day; greater than 2 nights/mo
  • Moderate persistent: daily; more than 1 night/wk
  • Severe persistent: continued & frequent
Term
Bronchodilators
Definition

drugs that reverse airway constriction (bronchi & bronchioles)

 

relax smooth muscles of the bronchial tree to reverse bronchospasm; this allows an increase in lumen of the bronchioles & alveolar ducts and a decrease in resistance to air flow

 

do not alter the underlying inflammatory process; used only for sympomatic relief of BRONCHIAL CONSTRICTION in conditions such as asthma, bronchitis, COPD

Term
3 classes of bronchodilators:
Definition

beta-adrenergic agonists

 

methylxanthines

 

muscarinic-receptor antagonists (anticholinergics) 

Term
Beta adrenergic agonists bronchodilators
Definition

adrenergic agents mimicking effects of sympathetic NS stimulation

 

catecholamines that stimulate adrenergic receptors directly, thereby stimulating cells that respond to morepinephrine and epinephrine and causing a sympathetic response: increased HR & force of cardiac contraction, vasoconstriction, bronchodilation, decreased gastric mobility, etc. 

Term
Beta adrenergic agonists bronchodilators
Definition

produce bronchodilation by stimulating cAMP production; cAMP is believed to be a bronchodilator

 

inhibit release of mast cell mediators

 

decrease vascular permiability

 

increase mucociliary clearance

Term
beta adrenergic agonist bronchodilators are nonselective beta agonists, meaning they:
Definition

affect both B1and B2 receptors & A1 receptors

 

cause bronchodilation (from B2 stim.), cardiac stimulation (tachycardia & cardiac arrhythmias from B1 stim.), and vasoconstriction/elevation in BP (from A1 stim.) 

Term
common beta adrenergic agonist bronchodilators:
Definition

Epinephrine

 

Ephedrine (generic)

 

Isoproterenol (affects B1 & B2 receptors; no affiity w/ A receptors) 

Term
most OTC bronchodilators contain epinephrine or ephedrine as the main active ingredient
Definition

they are potent, short-acting w/ almost immediate onset of action (< 1 min) & short duration of action (1-3 hrs)

 

effective for acute symptoms in the early phase; nave no effect in the late phase of asthma

 

pts who have frequent asthma exacerbations may overuse their inhaler, leading to systemic absorption sufficient to cause cardiac arrhythmias, hypertension,anxiety attacks, insomnia 

 

b/c of their nonselective actions, side effects, and tolerance develop't, inhaled forms of these drugs are seldom used in the ambulatory/impatient settings 

Term
epinephrine is used as a rescue drug given ____ for status asthmaticus & severe astha exacerbations unresponsive to ____ beta agonists.
Definition

sub-cutaneously

 

inhaled  

Term
Selective beta 2 agonists are classified into short- and long-acting agonist categories;  the long-acting agonists:
Definition

have a relatively slow onset of action & prolonged effect

 

not recommended for tx of acute bronchospasm b/c not a "quick-relief"/"rescue" medication

 

pts should use a short-acting B agonist PRN to control acute symptoms

 

BID dosing (12hrs/dose) to keep dilated all the time 

Term
long acting beta 2 agonists are very effective for:
Definition

maintenance tx in asthmatics requiring scheduled B agonist (moderate to severe asthma, adjunct to anti-inflammatory agents)

 

prodominance of nocturnal symptoms

 

prevention of exercise-induced asthma (EIA)

 

allergen- & histamine-caused bronchospasm 

Term

common long-acting beta 2 agonist:

 

salmeterol (Serevent) 

Definition
  • onset of action: 30 min; peak about 3 hrs; duration 12 hrs (12 hr half-life)
  • administered via inhaler
  • poorly absorbed into circ. via the lungs; w/ chronic use, it is detected in the serum at very low levels
  • large doses via inhalation (12-20 normal) have been associated w/ prolongation of the QT interval, which has the potential for producing ventricular arrhythmias
  • approved for use in kids 4yrs + ; elderly may require lower doses
  • headaches and cough = common side effects (well tolerated)
Term

common long-acting beta 2 agonist:

 

formeterol (Foradil) 

Definition
  • onset of action 15 min; peak 1-3 hrs; duration 12 hrs
  • aerolizer inhaler: easy to use delivery system that allows pts to "see, hear, feel" that they have correctly taken their meds (dry powder)
  • 1 dose BID
  • newly approved in US; comparable to salmeterol
  • approved for adults and kids 5 yrs + w/ reversible obstructive airway disease including those w/ nocturnal asthma
  • also indicated for the prevention of EIA in adults/kids 12 yrs +
  • not a "rescue med"
  • well tolerated
Term
short-acting beta 2 agonists
Definition
  • most effective drugs available for tx of acute pronchospasm & prevention of EID; recommended for all pts (rescue drug)
  • regular use offers no advantage over PRN use
  • onset of action = 5 min; peak 2 hrs; duration 4-6hrs; repetitive admin. produces incremental bronchodilation
  • avaiable as oral med, nasal sprays, MDIs
  • best route of admin = inhalation (metered dose)
  • oral are less effective, produce more adverse effects, and have a slower onset of action
  • oral syrup forms may be useful for some young kids and elderly w/ frequent mild symptoms
  • studies have shown that the equivalent bronchodilation can be achieved by either high doses (6-12 puffs) of a beta 2 agonist by MDI w/ a spacer/holing chamber under supervision or by nebulizer therapy
Term
adverse effects of short-acting beta 2 agonists:
Definition

relatively B2 agonist-selective in their action & produce more bronchodilation w/ fewer cardio. effects

 

tachycardia, palpitations, tremor & paradoxical bronchospasm can occur

 

high doses can cause hypokalemia

 

caution in pts w/ uncontrolled cardio disorders & convulsive disorders 

Term
common short-acting beta 2 agonist:
Definition
albuterol (Proventil, Ventolin)
Term
contraindications of short-acting B2 agonists:
Definition

caution in CHF, HTN, liver disease, elderly

 

caution in DM, glaucoma (they can increase blood glucose & intraocular pressure)

 

contraindicated in pts w/ hyperthyroidism & uncontrolled arrhythmias

 

Beta adrenergic blocking agents antagonize the effects of adrenergic agonists

Term

Bronchodilator:

 

Methylxanthines 

Definition
  • relax bronchial smooth muscle by increasing cAMP conc. through inhibition of phosphodiestrase, an enzyme that breaks down cAMP
  • other effects include: cardiac stim, vasodilation, diuresis, improved ciliary transport of mucus, and improved contractility of the diaphragm (excellent for COPD, not concerned in asthma)
  • chemically related to the natural metabolite xanthine, a precursor of uric acid (tea leaves, coffee leaves, cocoa leaves)
Term
Theophylline is the most important methylxanthine in clinical use
Definition

Aminophylline is the only form that can be administered IV

 

diferent preparations are not bioequivalent 

Term
Pharmacokinetics of theophylline:
Definition
  • well absorbed from oral liquids & uncoated tabs; absorption rate varies w/ type of preparation
  • half life = 3-15hrs in nonsmokers & 4-5hrs in smokers
  • metabolized by the liver & excreted by the kidney
  • therapeutic serum level: 10-20
  • narrow TI
  • drug levels must be drawn during therapy to ensure presence of therapeutic range
Term
Pharmacotherapeutics of theophylline:
Definition

prophylaxis & tx of chronic asthma

 

tx of bronchospasm r/t chornic bronchitis & emphysema (COPD)

 

used less frequently than in the past b/c more effective and safer meds are now available 

Term
adverse effects of theophylline:
Definition
  • those that are associated w/ plasma theophylline levels <20 are few
  • levels of 20-25: n/v/d, headaches, insomnia, restlessness, flushing, tachycardia, tremors, increased reflexes, fasciculations
  • levels >30: severe arrhythmias; seizures, or death
  • toxicity onsetmay be sudden, w/ arrhythmias and seizures as first sign (so always monitor BP)
Term
interactions with theophylline:
Definition
  • cimetidine, erythromycin, oral contraceptives, quinlones --> increased theophylline levels
  • cigarette/marijuana smoking, phenytoin, phenobarbital, rifampin --> decreased theophylline levels
  • concurrent use w/ B2 agonists causes additive effects
Term
contraindications of theophylline:
Definition

hyperthyroidism & uncontrolled arrhythmias

 

caution in CHF, HTN, liver disease, seizure disorders, elderly

 

there is no antidote for xanthine, standard aid measures (charcoal, emesis, gastric levage) must be used for toxicity

Term

Bronchodilator:

 

Muscarinic-receptor antagonists (anticholinergics) 

Definition
parasymp. stim. causes bronchial constriction & mucus secretions; anticholinergics are used to block these responses & maintain bronchial dilation of the airways
Term
common anticholinergic:
Definition
ipratropium bromide (Atrovent)
Term
Pharmacokinetics of anticholinergics:
Definition

onset 5-15 min; peak 1-2 hrs; duration 4-6 hrs

 

minimal systemic absorption (very safe)

Term
Pharmacotherapeutics of anticholinergics:
Definition
  • appear to be more effective for lower airways
  • first line choice in the tx of COPD
  • dose: 2 puffs QID
  • intranasal spray is used for the tx of perennial rhinitis & rhinorrhea (allergies)
Term
adverse effects of anticholinergics:
Definition

infrequent

 

systemic side effects are minimal

 

most common: cough, dry mouth, headaches 

Term
contraindications of anticholinergics:
Definition

hypersensitivity

 

no drug interactions 

Term
Anti-inflammatory agents
Definition

w/ the recognition that asthma is an inflammatory process, much progress has been made in the development & use of anti-inflammatory therapy

 

while these therapies are relatively ineffective in treating acute attacks, they do reduce frequency & severity 

Term
3 types of anti-inflammatory agents:
Definition

Glucocorticosteroids

 

Mast cell stabilizing agents

 

Leukotriene Antagonists 

Term

Anti-inflammatory agent:

 

Glucocorticosteroids 

Definition
  • corticosteroids are the "most potent and effective anti-inflammatory meds currently available"
  • aerosolized agents are safe, well tolerated, and can be used in kids
  • aggressive tx w/ these early in the disease may have benefit in limiting progression of disease
  • anti-inflammatory effects lead to improvement in severity of asthma symptoms, increased peak flow readings & decreased airway hyperresponsiveness
Term
Pharmacokynamics of Gluecocorticosteroids:
Definition
  • supress imflammation in airways by inhibiting infitration of inflammatory cells
  • decrease mucus secretion & edema of the airways and help repar damaged epithelium
  • increase the # and sensitivity of B2 receptors, improving response to B2 bronchodilators
Term
Pharmacotherapeutics of Glucocorticosteroids:
Definition
  • useful in tx of all types of persistent asthma in pts of all ages
  • useful in COPD
  • inhaled are preferred over PO steroids for long-term use
  • dosages of inhaled steroids depend on the severity of the disease; most pts can be maintained on BID dosing of the currently available preparations
  • intranasal inhaled steroids are used in the tx of seasonal & perennial allergic rhinitis
Term
contraindications of glucocorticosteroids:
Definition

no significant drug interactions

 

no significant contraindications

 

contraindicated in the primary tx of status asthmaticus (b/c/ not immediate onset) 

Term
adverse effects of glucocorticosteroids:
Definition
  • compared to PO steroids, very safe for all ages
  • most common from inhalation: hoarseness, dysphonia, aphagia, cough, oral candidiasis (thrush) with inappropriate use, cataracts
  • use of spacer device and rinsing mouth after inhalation decreases incidence of candidiasis
  • adverse effects of nasal inhalant: sneezing, epistaxis, HAs, n/v
  • daily use in kids/adolescents MAY cause supression of growth by a small amount
Term
common glucocorticosteroid:
Definition

fluticasone (Flovent)

 

ADVAIR DISCUS: (fluticasone + salmeterol)

  • combined glucocortico. & B agonist
  • use for long-term control 
Term
Nursing Considerations w/ glucocorticosteroids:
Definition

teach pt. to correctly use MDI/nasal inhaler

 

teach pt to use a spacer w/ MDIs so med doesn't end up in the lungs 

Term
Fluticasone has a ____ systemic bioavalability % which means that we will maintain localized bioavailability in the lungs which is ideal
Definition
small (2%)
Term

Anti-inflammatory agent:

 

Leukotriene Modifiers (antagonists) 

Definition
  • induce bronchoconstriction, mucus production & airway edema
  • prevent symptoms of asthma by supressing synthesis of leukotrienes or blocking their receptors
Term
common Leukotriene Modifier:
Definition
montelukest (Singulair)
Term
Pharmacotherapeutics of leukotriene modifiers:
Definition
  • most recent additions ot the list ofdrugs used to  control asthma
  • recommended as second line alternatives to ICS & long-acting B2 agonists
  • especially appropriate for the 10% of ashtmatics who are aspirin/NSAID-sensitive
Term
adverse effects of leukotriene modifiers:
Definition

HAs, dyspepsia (heartburn)

 

drug allergy

 

liver disease (not in montelukast) 

Term
contraindications of leukotriene modifiers:
Definition

hypersensitivity

 

approved for kids 2 yrs + (kids chewables shouldn't be swallowed whole) 

Term

Anti-inflammatory agent:

 

Mast Cell Stabilizer 

Definition
  • mast cells are located in many body tissues; during inflammatory response, they release histamine
    • neg. effects of histamine: bronchospasm, increased mucus production, leading to congestion, increased capillary permeability
  • inhibit mast cell degranulation, which prevents the release of histamine
Term
common mast cell stabilizer:
Definition

cromolyn sodium (Intal)

 

excellent; available as metered nasal spray, capsules for inhalation, nebulization solution, aerosol & oral form 

Term
Pharmacotherapeutics of Mast cell stablilizers:
Definition
  • second line alternatives for the tx of mild persistent asthma
  • primarily prescribed in kids b/c have no serious side effects
  • may be used for EIA (bronchodilator more effective)
  • disadvantage: requirement for TID-QID dosing in most pts
  • used in the tx of allergic rhinitis & allergic conjunctivitis
Term
Allergic Rhinitis
Definition

runny nose, sneezing, nasal congestion, headache, itching of the nose/eyes/throat

 

IgE-mediated allergic response to one or more airborne allergens

 

multiple risk factors, most common is family history:

  • both parents atopic: 50% risk of atopy in child
  • one parent/sibling: 29%
  • neither parent is atopic: 13% 
Term
tx for allergic rhinitis
Definition

Pt education

 

allergen avoidance

 

pharmacotherapy

 

allergen-specific immunotherapy 

Term

tx of allergic rhinitis:

 

Pharmacotherapy 

Definition

topical intranasal corticoids are the first step

  • proven to be more effective than antihistamines/docongestants
  • able to relieve: nasal itching, sneezing, runny nose, nasal congestion
  • inhibit inflammatory process leading to the late phase reaction of the allergic process; given prophylactically (prevent or reduce symptoms that occur w/ the early stage rxn)
  • available by prescription only
  • most common side effect: nasal irritaion, congestion, throat irritation, unpleasant bitter taste, cough 
Term
common topical intranasal corticosteroids:
Definition

fluticasone (Flonase)

 

mometasone (Nasonex) 

Term
Antihistamines
Definition
  • histamine is a chemical found in all of the body's cells and it is released into the bloodstream by the mast cells in response to the presence of antigens for which a person had developed antibodies & to which he/she may be allergic
antihistamines do not change the secretion or production of histamine, but block the action of histamine by competing w/ histamine for cell receptor sites

Term
in an allergic rxn, histamine:
Definition
  • increases secretion of body fluids such as gastric, intestinal fluids and bronchial/salivary secretions
  • causes pain and itching w/ stimulation of sensory nerve endings
  • contracts bronchial smooth muscle
  • dilates cerebral blood vessels
  • causes vasodilation, which may lead to flushing and hypotension
  • increases capillary permiability causing edema in the nose, eyes, and throat
  • these systemic effects may lead to life-threatening anaphylaxis
Term
Antihistamines/H1-receptor antagonists
Definition
block the activity of histamine by occupying the H1-receptor agents, inhibiting histamine induced vasodilation, secretions & itching
Term

Classification of antihistamines/H1-receptor antagonists:

 

1st & 2nd generation 

Definition
  • 1st generation: highly sedating; 10-40% of pts experience sedation; also, have various anticholinergic side effects: dry mouth, blurred vision, constipation, urinary retention, impotence
  • 2nd generation: have greater affinity for H1 receptors & longer duration of action; cause less sedation & anticholinergic effects b/c do not cross the blood-brain barrier in sufficient concs to affect histamine receptors in the brain
Term
common antihistamine/H1 receptor antagonists:
Definition

diphenhydramine (Benedryl)

 

loratadine (Claritin) 

 

 

Term
contraindications of antihistamines:
Definition

in use w/ MAO inhibitors, narrow-angle glaucoma, peptic ulcer, prostatic hypertrophy

 

caution in elderly - excessive sedation

 

not recommended w/ bronchitis/pneumonia: dry secretions making them more difficult to remove

 

antihistamines taken by young kids can cause drowsiness w/ first few administrations & paradoxic excitement (CNS excitation) w/ repeated use

Term
drug interactions with antihistamines:
Definition

anticholinergics, MAOIs, tricyclic antidepressants: increased severity of anticholinergic side effects (e.g. dry mouth, blurred vision, urinary rention)

 

ETOH: increased sedation 

Term
Decongestants
Definition
  • constrict blood vessels & reduce blood supply to the nasal mucosa, thus reducing swelling
  • basically sympathomimetics, i.e., they either mimic NE or enhance its release; NE activates A1 receptors leading to constriction of the blood vessels in the nasal passage & reduce membrane swelling
  • recommended for only 3-5 days of therapy
Term
side effects of decongestants:
Definition

excitation of the central NS (leading to insomia, restlessness, agitation), tachycardia, urinary retention & increase in BP; rebound congestion

 

 

should be avoided in HTN, DM, hyperthyroidism, CAD, or urinary obstructive disease 

Term
Common decongestant:
Definition
pseudoephedrine (Sudafed/Novafed)
Term

 

 

Antitussives 

Definition
  • used to supress the cough reflex which is a natural defensive mech.; may act either centrall or locally to decrease the frequency & intensity of cough
    • centrally acting agents: inhibit cough center of the medulla in the brain, thereby supressing the cough
    • Locally acting agents: act directly on the cough production at the site of irritation, inhibiting cough receptors in the throat, trachea, or lungs
Term
When is a cough suppressant/antitussive indicated?
Definition

only when the cough is so severe that it causes excessive fatigue & interrupts sleep

 

should only be used to inhibit frequency of dry, nonproductive cough that keeps pts awake

 

should not be used if the cough is productive (secretions can pool & cause pneumonia) 

Term

Classification of antitussives:

 

opioid agents & nonopioid agents 

Definition
opioid agents: codeine, hydrocodone (Hycodan): CNS effect on the cough center
 
nonopioid agents: dextromethorphan (Benylin DM, Pertussin ES): CNS effect; benzonatate (Tessalon): local anesthetic
Term
side effects of antitussives:
Definition
light-headedness, dizziness, sedation, abuse, liability (can cause resp. depression)
Term
Expectorants
Definition

used to facilitate expectoration; facilitate the secretion of fluid in the resp. tract, thus liquifying secretions and allowing for easier expectoration during a cough; this increase in flow lubricates the airway & may relieve the cough

 

these agnest also decrease the viscosity of mucus, making removal easier 

Term
Pharmacotherapeutics of expectorants:
Definition
  • relief of dry, unproductive cough that accompanies resp conditions such as colds, influenza, bronchitis, asthma
  • facilitation  of secretion removal in resp conditions associated w/ increased mucus prod
  • most effective at managing symptoms associated w/ URIs; generally not as effective for tx of persistent cough associated w/ smoking, asthma, emphysema
Term
contraindications of expectorants:
Definition

use w/ caution in clients w/ fever or severe persistent cough

 

preps that contain ETOH can cause severe symptoms in pts taking disulfiram 

Term
adverse effects of expectorants:
Definition
dizziness, HA, rash, stomach pain, nausea, diarrhea w/ large doses
Term
common expectorant
Definition
guaifenesin (Robitussin, Anti-Tuss)
Term
nursing implications for expectorants
Definition

WATER IS BEST

 

encourage fluid intake of 2000 ml/day

 

follow each dose of quaifenesin w/ a full glass of water 

Term
Mucolitics
Definition

agents reacting directly w/ mucus to make it thinner & more easily expectorated

 

used to promote mucus clearing in: pneumonia, bronchitis, COPD, TB, diagnositic procedures to obtain a mucus specimen

 

used to treat acetaminophen (Tylenol) overdose

Term
common mucolytic:
Definition
acetylcystine (Mucomyst)
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