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Pharmacology COPD/Asthma Month 1 Week 3 Day 5
Pharmacology COPD/Asthma Month 1 Week 3 Day 5
90
Pharmacology
Graduate
05/24/2018

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Term
symptoms and severity of asthma
Definition
<2x/week- intermittent. >2x/week mild persistent, daily moderate persistent, throughout the day severe persistent (same for frequency of use of albuterol)
Term
nighttime awakening and severity of asthma
Definition
<2x/month- intermittent, 3-4x/month- mild persistnet, >1x/week mod persistent, every night severe persistent
Term
[image]
Describe the pathway and where different drugs for asthma or COPD work along it
Definition
ATP (AC) -> cyclic AMP -> bronchodilation -> PDE destroys cyclic AMP -> AMP. medications act on these enzymes to cause bronchodilation and inc production of cyclic AMP. Acetylcholine and adenosine -> bronchoconstriction. beta agonists activate adenylate cyclase -> inc cyclic AMP. muscarinic agonists inhibit effect of acetylcholine and prevents bronchoconstriction. theophylline and roflumilast inhibit PDE enzyme resulting in a dec in the destruction of cyclic AMP -> bronchodilation. Theophylline inhibits the effects of adenosine -> prevents bronchoconstriction
Term
Albuterol/Levalbuterol vs Pirbuterol receptor selectivity
Definition
[image]
Term
Step up approach for treatment of asthma
Definition
Intermittent (short acting beta agonist) -> low dose corticosteroid (alt leukotriene receptor agonist, theophylline) -> 2. inc dose of inhaled corticosteroid or add long acting beta agonist ->3. low inhaled corticosteroid and long acting beta agonist -> 4. med dose inhaled corticosteroid and long acting beta agonist (alt med inhaled corticosteroid + leukotriene receptor agonist/theophylline/zileuton -> 5. high dose inhaled corticosteroid + long acting beta agonist (omalizumab if allergies too) -> 6. high dose inhaled corticosteroid + long acting beta agonist + oral corticosteroids and omalizumab if allergies (short acting beta agonist as needed throughout)
Term
short acting beta 2 agonists
Definition
SABA, for acute bronchospasm, rescue inhaler, prevent exercise induced asthma. Albuterol (more potent), Levalbuterol, Pirbuterol. last 3-4 hrs
Term
albuterol vs levalbuterol
Definition
enantiomers, albuterol is racemic mixture of S and R, levalbuterol is just the R isomer (no compelling evidence that levalbuterol is better, it is also more expensive)
Term
long acting beta agonists
Definition
Salmeterol (Serevent)(aerosol powder for inhalation), Formoterol (Foradil)(capsule for inhalation or solution through nebulizer), use in combination with inhaled corticosteroids. Black box warning- can inc the rate of asthma related death when used as monotherapy. work in ~2hrs, last ~12 hrs, give 2xday
Term
Combination treatments
Definition
Salmeterol + fluticasone (Advair)
Formoterol + Budesonide (Symbicort)
Formeterol + Mometasone (Asmanex)
Term
inhaled corticosteroid MOA
Definition
direct local inflammatory, reduce hyperresponsiveness, inhibit inflammatory cell migration and activation, most beneficial and effective for long term control of asthma, reduce impairment in lungs and the risk of exacerbation in pts w asthma
Term
inhaled corticosteroid drugs
Definition
beclomethasone (bike in my zone), budesonide (bet on a zone), ciclesonide/desciclesonide (circle solid), flunisolide (fluky solid), fluticasone (flute in zone), mometasone (moment zone), triamcinolone (try my clone)
Term
inhaled corticosteroid properties chart
Definition
[image]
Term
considerations for inhaled corticosteroids
Definition
can cause systemic side effects, might affect growth velocity in pediatric pts, educate pts to rinse mouth w water after use (prevent fungal infection), takes ~1 week before it starts working
Term
anticholinergic indications
Definition
quick relief of mod-severe asthma in combination w short term beta agonist or as an alternative if pt is intolerant. reduces intrinsic vagal tone of airway
Term
anticholinergic asthma drugs
Definition
ipratropium (Atrovent)- metered dose inhaler or as solution to be administered through nebulization
tiotropium (Spiriva)- inhale contents of capsule
Term
Blurred vision, xerstomia (dry mouth) and tachycardia are side effects of?
Definition
anticholinergics
Term
pathway where leukotriene inhibitors work and leukotriene inhibitor MOA
Definition
pts exposed to allergen -> mast cells and eos release inflammatory markers -> initiates inflammatory cascade -> conversion of arachidonic acid by 5-lipoxygenase enzyme to cysteinyl leukotrienes -> leukotrienes act on cystLT1 receptor -> symptoms of asthma (mucus secretion, bronchoconstriction). Zileuton (Zi-Neuton) inhibits the production of leukotrienes (5-lipoxygenase inhibitor). Drugs that block the action of leukotriene on receptors: Montelukast (Singulair)(Mountain cast), Pranlukast (Prank cast), Zafirlukast (Accolate) (Za fire cast)
Term
leukotriene inhibitor agents indicated when
Definition
moderate to severe persistent asthma, recommended to use in combo w high dose corticosteroid and long term beta agonist. usually considered prior to chronic oral corticosteroids. not usually used as monotherapy
Term
common side effect of Montelukast
Definition
headache
Term
can cause hepatic injury, inc liver enzymes, contraindicated in pts w hepatic impariment
Definition
zafirlukast, zileutin
Term
mast cell stabilizers
Definition
work on inflammatory pathway. Cromolyn (Cromwell). Alternative agent for pts w mild persistent asthma. inferior to inhaled corticosteroids. can be used for exercise-induced bronchospasm. give as metered dose inhaler or nebulizer, can take 2-6 weeks to start working
Term
Methylxanthine MOA
Definition
block PDE enzyme, inc cyclic AMP -> bronchodilation (nonselective phosphodiesterase inhibitor) also anti inflammatory affect -> activation of histone, deacetylase enzyme, decreases the pro-inflammatory gene expression
Term
Methylxanthine indicated for
Definition
alt for step up therapy for pts w mild persistent asthma or as adjunctive therapy w inhaled corticosteroids
Term
Methylaxanthine delivery
Definition
give loading dose bc takes time to reach steady state. check blood lvl 30 min after loading dose bc can cause a lot of side effects and toxicity
Term
has side effects of tachycardia, headache, hypertension, nausea, and vomitting and at very high doses can cause hematemesis, hyperglycemia, hyperkalemia, seizures
Definition
methylxanthine (theophylline) (Elixophyllin)
Term
Cimetidine, Macrolides, Quinolones, Systemic Viral Illnesses, Zileutin, and Propanolol affect Methylxanthine clearance how?
Definition
decrease, CYP3A4 inhibitors
Term
Phenytonin, Rifampin, Carbamazepine, Smoking, Phenobarbital, High protein diet affect Methylxanthine clearance how?
Definition
increase, CYP3A4 inducers
Term
Immunomodulators are indicated when for asthma
Definition
step 5 and 6
Term
Immunomodulator agents
Definition
Omalizumaub (O mail mob) (Xolair)- sub q injection, Mepolizumab (me pale mob) (Nucala- sub q injection), Reslizumab (re sell mob)
Term
Omalizumab MOA
Definition
Monoclonal IgG antibody that inhibits the IgE receptor binding on mast cells and basophils
Term
Omalizumab indication
Definition
long-term use decreases asthma exacerbations and corticosteroid use, alt agent for pts w sensitivity to allergens and severe persistent asthma. but doesn't have any effect on baseline of FEV1 ratio
Term
has SE of anaphylactic reactions and injection-site reactions
Definition
Omalizumab, Mepolizumab, Reslizumab (Immunomodulators)
Term
Mepolizumab MOA
Definition
IgG monoclonal Ab that works by inhibiting the binding of interleukins to eosinophil cell surfaces
Term
Reslizumab MOA
Definition
interleukin-5 receptor antagonist
Term
Mesilzumab indication
Definition
add-on for maintenance treatment of severe asthma w an eosinophilic phenotype
Term
Oral corticoteroids indication
Definition
pts w poor asthma control, given as a short course up to 2 weeks, helps in reducing duration of symptoms and preventing hospitalization and relapse post-exacerbation
Term
metered-dose inhaler, pt education
Definition
inhaler w canister surrounded by plastic holder and mouthpiece, medication mixed w propellant. tell pt to shake before use, exhale before inhaling medication, seal mouthpiece w lips, breathe in slowly, hold for 10 sec then breathe out
Term
dry-powder inhaler pt education
Definition
hold discus in palm, push thumb grip until clicks into place, slide lever away, seal mouth around mouthpiece, breathe deeply and rapidly, hold breath 10 sec, close mouthpiece
Term
Twisthaler pt education
Definition
used for administering dry-powder medications, twist and lift off cap to load dose, exhale, then twist twisthaler horizontally and breathe in rapidly and deeply then hold breath 10 sec, then close cap
Term
Respimat
Definition
helps in delivering a slow mist of the medication to patients
Term
follow up for asthma pts depending on how well their symptoms are controlled
Definition
well-controlled- 1-6 mo intervals
not well controlled- step up 1-2 steps, reeval in 2-6 weeks
poorly controlled- short course of oral corticosteroids
Term
pregnancy and asthma
Definition
usually have worsening of symptoms, preferred to use albuterol as a rescue agent and bedesonide as a maintenance agent. avoid long-acting beta-agonists, avoid omalizumab and zileuton
Term
reversible component of COPD
Definition
causes small-airway disease, production of mucus and inflammatory cells, results in bronchial muscle contraction and airway resistance
Term
irreversible component of COPD
Definition
parenchymal destruction/lung tissue destruction, alveolar damage affecting gas exchange, results in loss of lungs being able to recoil and push the air outside of the lungs, these pts also have airway fibrosis
Term
glucocorticoids and asthma vs COPD
Definition
inhibit inflammation in asthma, variable effect in COPD
Term
GOLD level and FEV1
Definition
GOLD 1- FEV1 >80%, GOLD 2- 50-80% of predicted, GOLD 3- 30-50%, GOLD 4 <30%
Term
mMRC
Definition
Modified British Medical Research Council, questionnarie bc some pts can be at same GOLD lvl w diff symptoms, 0-4, greater # = worse dypsnea
Term
CAT score
Definition
COPD Assessment Test Score, incorporates other symptoms besides dyspnea, 0-40, higher number, worse symptoms
Term
Combined assessment for COPD to determine A, B, C, D
Definition
[image]
Term
Short acting beta-2 agonists for COPD
Definition
albuterol, levalbuterol
Term
Long acting beta-2 agonists for COPD
Definition
arformoterol, formoterol, indacaterol (lasts 24 hrs), oldaterol, salmeterol, vilanterol
Term
Anticholinergic agents for COPD
Definition
short term- ipratropium
long-term- aclininium, tiotropium, umeclidinium
Term
inhaled corticosteroids for COPD
Definition
beclomethasone (bike in my zone), Budesonide (bet on a zone), Ciclesonide (circle solid), Fluticasone (flute in zone), Mometasone (moment zone)
Term
PDE4-Inhibitor for COPD
Definition
Roflumilast (reduces inflammation and breakdown of cyclic AMP), adjunctive therapy for severe COPD pts or pts w prior history of hospitalization for acute exacerbation
Term
Treatment for COPD A
Definition
1st- short-acting muscarinic antagonist agent as needed or short-acting beta agonist. 2nd- long acting muscarinic antagonist or long-acting beta agonist or combo of short acting muscarinic antagonist + short-acting beta agonist. Alt- Theophylline
Term
Treatment for COPD B
Definition
1. long acting muscarinic antagonist or long-acting beta agonist 2. Combo of Long acting beta agonist + long acting muscarinic antagonist
Term
Treatment for COPD C
Definition
1. inhaled corticosteroid + long acting beta agonist or long acting muscarinic antagonist 2. long acting muscarining antagonist + long acting beta agonist
Term
Treatment for COPD D
Definition
1. inhaled corticosteroids + long acting beta agonist or long acting muscarinic agonist + long acting beta agonist
2. ICS + LAMA
or
ICS + LABA + LAMA
or
ICS + LABA + PDE4 inhibitor or
LAMA + LABA
or
LAMA + PDE4 inhibitor
Term
Treatment for COPD Exacerbations
Definition
short term bronchodilators (short acting beta agoninst and/or short term muscarinic antagonist) and glucocorticoids (prednisone)
Term
evaluating COPD A, B, C or D
Definition
0-1 hospital admission A or B. 2 or more hospitalizations C or D. mMRC 0-1 or CAT <10 A or C, mMRC >=2 or CAT>=10 B or D then eval GOLD level
Term
short term + long acting bronchodilators in COPD
Definition
not supported to be effective in COPD, inc side effects. prefer anticholinergic bronchodilator + long-acting beta 2 agonist over short acting beta-2 agonist + long acting beta-2 agonist
Term
has the side effects of sinus tachycardia and hypokalemia
Definition
beta agonists
Term
inhaled corticosteroids help how w COPD
Definition
improve symptoms, lung fuction, quality of life, reduce exacerbation frequency, specifically in pts w FEV1 <60%
Term
has the side effects of hoarseness of voice, skin bruising, oral candidiasis, pneumonia
Definition
inhaled corticosteroids
Term
has side effects of diarrhea, nausea, weight loss, insomnia, anxiety, depression, suicidal ideation
Definition
Rofumilast
Term
contraindicated in pts w moderate or severe hepatic impairment
Definition
Rofumilast
Term
antibiotic if COPD pt has infection
Definition
azithromycin or erythromycin
Term
signs and symptoms of cold
Definition
mild upper respiratory viral illness symptoms, sneezing, nasal congestion, rhinnorhea (runny nose), cough, sore throat, low grade fever, headache, malaise. but can be different depending on the virus, usually up to 10 days
Term
treatment for colds
Definition
treat the symptoms. intranasal ipratropium bromide (relieve rhinorrhea and sneezing, reduces volume of nasal discharge but doesn't affect nasal congestion), antihistamines, antitussives (for coughs, inhibits cough centers in the brain), expectorants (makes cough), decongestants, intranasal glucocorticoids. debate about whether these agents are effective in treating a cold or not
Term
has side effects of nasal dryness, blood-tinged mucus, epistaxis
Definition
intranasal ipratropium bromide
Term
2 antitussive agents
Definition
dextromethorphan (Delsym)-dec's sensitivity of the cough receptors and depresses the medullary cough centers in the brain
codeine- only works on CNS cough centers in the brain
Term
can cause the side effects at high dose of confusion, excitement, irritability, nervousness, serotonin syndrome w monoamine oxidase inhibitors
Definition
dextromethorphan
Term
cases side effects at high dose of altered mental status, visual disturbances, respiratory depression, constipation
Definition
codeine
Term
has black box warning that it can cause respiratory depression and death in some children who receive it following tonsillectomy or adenoidectomy
Definition
Codeine, if child is an ultra-rapid metabolizer (produce morphine when metabolized by CYP enzyme). not recommended to give codeine to children
Term
expectorant agent and how it works
Definition
guaifenesin- increases the effective hydration of the respiratory tract. reduces the mucus viscosity making it easier for pt to cough out. can be found in combo w codeine, dextromethorphan, phenylephrine, pseudoephedrine
Term
decongestant agents and how they work
Definition
pseudoephedrine (Sudafed)(weak stimulant to CNS), phenylephrine (Sudafed PE) (not as strong, less reaches systemic circulation), work by directly stimulating the alpha adrenergic receptors of the respiratory mucosa leading to vasoconstriction and dec blood flow to mucosa layer which helps in relieving congestion and directly stimulate beta adrenergic receptors causing bronchial dilation (only pseudoephedrine does this). both work on alpha-1 receptors but only pseudoephedrine also works on beta-2 receptors
Term
how intranasal itrapropium bromide works
Definition
relieve rhinorrhea and sneezing, reduces volume of nasal discharge but doesn't affect nasal congestion
Term
restrictions are placed on the sale of
Definition
pseudoephedrine becasue of illicit production of methamphetamine
Term
causes side effects of hypertension and bradycardia
Definition
pseudoephedrine and phenylephrine
Term
inhaled or intranasal glucocorticod agents and how they work
Definition
beneficial for allergic rhinitis but not helpful for cough or cold. beclomethasone and fluticasone.
Term
what is allergic rhinitis
Definition
allergies, most common chronic disease in pediatrics, inflammatory process that is IgE mediated and usually presents with symptoms such as nasal congestion, rhinorrhea, sneezing, nasal itching, lacrimation. can be seasonal, perennial (year-round), intermittent, persistent , or episodic
Term
allergic rhinitis vs asthma
Definition
allergic rhinitis affects upper respiratory tract, asthma affects lower respiratory tract, can have both together
Term
main therapy for allergic rhinitis
Definition
oral antihistamines, usually indicated for sneezing and itching. 1st gen- more sedating and more anticholinergic SEs (diphenhydramine/Benadryl), 2nd gen- less sedating (loratadine/Claritin, desloratadine/Clarinex, fexofenadine/Allegra (least sedating), Cetrizene (Zyrtec), Levocetirizene (xyzal)
Term
Intranasal antihistamines good for, agents
Definition
for allergic rhinitis, faster onset, high efficacy for nasal congestion but more expensive than oral antihistamines. olopatadine, azelastine, azelastine + fluticasone, indicated when symptoms affect quality of life
Term
SE of bitter taste, epistaxis, headache
Definition
intranasal antihistamines, olopatadine, azelastine, azelastine + fluticasone
Term
intranasal corticosteroids used for, agents
Definition
allergic rhinitis. triamcinolone, budesonide, flunisolide, fluticasone, mometasone, ciclesonide
Term
cause side effects of pharyngitis, epistaxis, cough, can affect taste, cause nasal burning or headache
Definition
intranasal corticosteroids, triamcinolone, budesonide, flunisolide, fluticasone, mometasone, ciclesonide
Term
intranasal decongestant, agent, MOA
Definition
oxymetazoline (Afrin), for allergic rhinitis, alpha adrenergic agonist -> nasal arteriolar vasoconstriction, most effective when given in combo w intranasal corticosteroids, do not use >3 days (rebound congestion)
Term
Treatment for increased lacrimation in allergic rhinitis, pt counselling
Definition
naphazoline (Clear Eyes)- vasoconstrictor, antihistamine eye drops- Zaditor, NSAID eye drops- Acular, corticosteroid eye drops- Alrex. All OTC. instruct pt to remove contact lenses before using
Term
causes SEs of ophthalmic irritation, mydiasis, photophobia
Definition
ophthalmic agents- naphazoline (Clear Eyes)- vasoconstrictor, antihistamine eye drops- Zaditor, NSAID eye drops- Acular, corticosteroid eye drops- Alrex
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