Exam 3 - Week 8: Respiratory Drugs Flashcards
Prototype Respiratory Drugs
- Acetylcysteine (Mucomyst)
- Guaifenesis (Robitussin)
- Epinephrine (Adrenaline)
- Isoproterenol (Isuprel)
- Albuterol (Proventil)
- Ipratropium (Atrovent)
- Aminophylline (Theophylline)
- Cromolyn (Intal)
- Zafirlukast (Accolate)
- Beclomethasone (Vanceril)
- Dextromethorphan (DM)
- Pseudoephedrine (Sudafed)
- Diphenhydramine (Benadryl)
What is the most common condition affecting the upper respiratory tract?
Inflammatory conditions leading to the overproduction of secretion (mucus)
2 Approaches to Mucus Drugs
Mucolytic
Expectorant
Mucolytic
Breaks up mucus into smaller units
ex: Acetylcysteine (Mucomyst)
Expectorant
Reduces viscosity of secretions
ex: guaifenesin (Robitussin(
How do mucolytics and expectorants differ?
They both have the same outcome, but the expectorant makes the mucus more watery rather than breaking it up (it dilutes it)
The goal of bronchodilating drugs is…
to dilate bronchi in order to maximize airflow but with the fewest SE
Epinephrine is a _______ bronchodilator with significant cardiac effects
Non-selective!
Isoproterenol (Isuprel) is a _____ Beta Stimulating Bronchodilator
Non-Selective
Albuterol is a relatively ____ Beta 2 Agonist
selective
Ipratropium (Atrovent) is what class/type of drug and what does it do?
Anticholinergic bronchodilator
it relaxes smooth muscle in the bronchial tree and is used for maintenance therapy
Aminophylline (Theophylline) is what class/type of drug and what does it do?
Methylated Xanthine
It has a direct effect on smooth muscle (oral or IV) to bronchodilate
Prototype Mucolytic Drug
acetylcysteine (Mucomyst)
Action of acetylcysteine (Mucomyst)
Breaks up bonds of mucoprotein molecules from resp. secretions into smaller, more soluble, and less viscous strands
Also effects similar changes in DNA and cell debris and works best at pH 7-9
What is the absorption like for acetylcysteine
Very little absorption occurs
It undergoes Nebulization - Nebulizer form is mixed with saline so the mucomyst will act on the mucus and then stay there with little absorbed
ADRs of Acetylcysteine
FEW
Some N/V - probably from odor, Stomatitis, Rhinorrhea,
Bronchospasm could occur in asthmatics - assess airways
What is a unique aspect of acetylcysteine
It has a rotten egg odor (this can limit compliance)
As an inhalant, acetylcysteine acts as a mucolytic, but as a liquid it is…
the antidote for acetaminophen poisoning
It is important to allow the patient to do what after nebulization of acetylcysteine
Wash face after nebulization to remove the sticky coating left by the drug (it smells like rotten egg remember)
How long is acetylcysteine infused for if its as an acetaminophen antidote
72 hour for Oral; 21 Hour for IV
Prototype drug expectorant/bronchomucotropic
guaifenesin (Robutussin)
Action of guaifenesin
Directly irritates the gastric mucosa - then because it is upsetting the stomach a gastropulmonary reflex action occurs producing more watery secretions to be coughed up
It irritates gastric mucosa to increase volume and reduced viscosity of respiratory secretions (called gastropulmonary reflex action)
ADRs of guaifenesin
RARE!
Occasional GI irritation
What is very important to be doing while taking an expectorant like guaifenesin
HYDRATE! - to decrease viscosity the drug is pulling water from the body to loosen secretions so you need to be having fluids since fluids are being pulled from you
guaifenesin is a ___ drug
OTC
What may contribute to gastric upset when taking guaifenesin
if taken on an empty stomach
How does guaifenesin effect coughing?
it does not stop the cough it just helps get secretions up
epinephrine (as a respiratory drug)
Sympathomimetic (non-selective); bronchodilator
Action of epinephrine as a respiratory drug
Stimulates Alpah, Beta 1 and Beta 2 receptors
Stimulating Alpha receptors…
causes VASOCOCNSTRICTION (which is good for airways as it can reduce mucosal edema)
Stimulating Beta 1 Receptors …
stimulates heart rate and force of contraction of the heart as well as cardiac irritability
We would prefer if EP did not do this but we will fix it later
Stimulating Beta 2 Receptors…
induces bronchial smooth muscle relaxation
What receptors do we want the EP stimulation to occur on the most
Alpha and Beta 2 moreso than Beta 1
Absorption / Routes for EP
Oral cannot be used as it is destroyed by enzymes
Parenteral is a good route for absorption
Aerosol allows it to be contained to the respiratory tract
Often it is given SUBQ or Aerosol - almost never IV
ADRs of Epinephrine
Nervousness Fear Insomnia Tremors Tachycardia Palpitation HA Dyspnea
Caution using EP when?
People with CAD, HTN, and Hyperthyroidism
What drugs should never be given concurrently with EP and why?
MAO Inhibitors because it will precipitate severe HTN
When is EP mostly used as a bronchodilator
Mostly in acute emergencies by EMS, in the ER, or in someone with acute bronchoconstriction
Can be a little overboard unless emergency
-ol may indicate a drug is what
A beta 2 Stimulator - Induces bronchial smooth muscle relaxation
Prototype drug that is a Sympathomimetic, Non-selective Beta Stimulating Bronchodilator
isoproterenol (Isuprel)
isoproterenol (Isuprel)
Sympathomimetic - mimics Symp.NS
Non selective Beta Stimulating Bronchodilator - only impacts beta receptors but will effect both 1 and 2
Action of isoproterenol
Stimulates beta 1 (stimulates heart) and beta 2 (bronchodilation and decreasing tone and motility of the GI tract and uterus)
DOES NOT AHVE ALPHA 1 EFFECTS - but still has Beta 1 effects which is not great
Preferred Route of Administration for isoproterenol (Isuprel)
oral and sublingual are poor routes so parenteral and inhalation are preferred or IV
ADRs of isoproterenol (Isuprel)
Tachycardia Palpitation HA Nausea Tremor Insomnia
THE MORE IT IS USED THE LESS EFFECTIVE IT MAY BE - VERY EFFECTIVE AT FIRST BUT NOT GIVEN OVER AND OVER
____ is one of the most powerful bronchodilators
isoproterenol (Isuprel)
What is the issue with isoproterenol and EP
they both stimulate Beta 1
Prototype drug that is a Sympathomimetic Selective Beta 2 Stimulating Bronchodilator
albuterol (Proventil, Ventolin)
“vent” for ventilation
Action of albuterol
Beta 2 stimulation leading to smooth muscle of bronchial tree and peripheral vasculature relaxation
At high doses what can happen with albuterol
it can begin to effect beta 1 but at normal doses it does not
Preferred route of albuterol absorption
Inhalation (almost always)
Oral only gets 30-40% bioavailability
ADRs of Albuterol
FEW!! - More effects if huffed, but when used properly almost nothing - may feel little jitteriness d.t sympathomimetic properties
Peripheral dilation leading to decreased BP causing Tachycardia
Other: Tremors, Palpitations, Nervousness, HA, Dizziness, NV, Anxiety, Lethargy, Tinnitus
What does it mean that Albuterol is a SABA
SABA = short acting beta2 agonist
So it is a short acting RESCUE INHALER for needing help breaking things up NOW
How does EP and Albuterol onset and duration differ
EP begins quicker but lasts shorter
Albuterol is slightly longer for onset but lasts longer
Caution using Albuterol with what patients
Those with Diabetes, HTN, Cqardiac Disorders (esp. arrhythmias)
LABA
Long acting beta2 agonists
ex: salmeterol (serevent)
NOT rescuse inhalers, prevent bronchoconstriction through common use
Prototype SAAMA drug
ipratropium (Atrovent)
What class is ipratropium (Atrovent)
Anticholinergic Bronchodilator - Inhaled Short Acting Muscarinic Antagonist (SAAMA)
What NS is ipratropium impacting
PNS rather than SNS
What situations is ipratropium used for
For maintenance and prevention of bronchoconstriction NOT an acute acting agent as it takes longer to work and is never given for immediate distress since it is working on the PNS
SAAMA drugs like ipratropium are often given to ___ patients
COPD
Action of ipratropium (Atrovent)
Blocks cholinergic receptors to reduce bronchial tone
Does NOT seem to affect volume or viscosity of sputum
Absorption of ipratropium
inhalation allows little absorption (less than 1%) so it has an almost exclusive effect on the mouth and airway when it works
Distribution of Ipratropium
since little is absorbed it has a negligible effect - it works directly on the mouth and airways
ADRs of Ipratropium
FEW!!
Dry mouth or Pharyngeal Irritation
Recommended Dosage for Ipratropium
As an MDI (Measured Dose Inhaler) it is recommended to take 2 inhalations (puffs) QID with up to a maximum of 12 inhalations in a 24 hour period
Combivent
vent = breathing; combi = combination drug
This is a combo fo ipratropium and albuterol which could be useful for both immediate and later effects simultaneously
Prototype Drug Bronchodilator and Methylated Xanthine
Aminophylline (Theophylline)
Action of Aminophylline
Inhibits phosphodiesterase - allows cAMP to increase leading to smooth muscle relaxation (esp bronchial), heart stimulation, stimulated CNS, and renal excretion
Stimulates the medullary respiratory center as well
____ is also a methylated xanthine
caffeine
Absorption/Route of aminophylline
Oral and Parenteral routes - IM is irritating so a capsule or IV form is given
What is the distribution/Therapeutic level of aminophylline and when does maximum levels occur
max levels in 2 hours
therapeutic levle = 8-25 mcg/mL
ADRs of Aminophyllines
- GI (anorexia, NV from vomiting center stim, abd. discomfort)
- CNS (nervousness, insomnia, irritability, headache, severe convulsion and coma)
- CV (tachycardia, severe hypotension and arrhythmia)
- Renal - urinary frequency
TONS of SE - helps airways open but has a lot of major ADRs (similar to caffeine)
Why do smokers need higher dosages of aminophylline
because the half life of aminophylline is shorter in smoker than non smokers - so they need a higher dosage since they excrete and such more
What should always be done when taking aminophylline
take it with food to decrease GI irritability
How commonly is aminophylline used
Nowadays it is not a common drug to see used
Prototype Drug Antiallergic/Histamine Inhibitor/Mast Cell Stabilizer
cromolyn sodium (Intal)
Action of cromolyn sodium
Inhibits histamine and other inflammation mediators by stabilizing the cytoplasmic membrane of mast cells
So it stabilizes and stops major inflammation rather than acting on a receptor or anything
Since cromolyn sodium stops mast cells before releasing histamines…
it is a GOOD PREVENTOR - but is not good for stopping an acute attack already occurring and inflammation already ocurring
Route for Cromyln Sodium
Inhalation - Rapid but only 10% will penetrate deep into the lungs
Comes as an MDI, turbo inhaler, nasal spray, and opthalmic solution for allergic eye disorders
ADR of cromyln sodium
only common one is throat irritation
cromolyn sodium is used for …
asthma PROPHYLAXIS (prevention) - it has no use in an acute attack
What education should be done for people on cromolyn sodium
always rinse mouth after inhalation treatment because it can disrupt mouth flora
cromolyn sodium is good for use in ___ and has minimal ___
children; ADRs
If cromolyn sodium is used 15 minutes prior, it can even prevent
excercise induced asthma attacks
Prototype Leukotriene Receptor Antagonist (LRA) drug
zafirlukast (Accolate)
“Dr Seuss Drug” - weird name
Action of zafirlukast
it competes for leukotriene receptor sites (blocks them) and blocks inflammatory response (bronchoconstriction and inflammatory cell infiltration) as a result of leukotrienes
Blocks leukotriene receptors - a cytokine that causes inhlammation - so it prevents inflammation from occurring
Is ziafirlukast good for acute treatment?
No, it is a maintenance therapy and prophylaxis use only - it will not reverse bronchospasms in acute attack
Why is the idea that zafirlukast is a maintenance therapy stressed
because most other drugs are fast or for prevention, and on a resp. treatment on a floor would be something like albuterol so this is very STRICLY for prevention
What is important to know about the absorption of zafirlukast
if taken with food bioavailability is decreased 40% - DO NOT TAKE WITH FOOD
It does come in a tablet form
ADRs of zafirlukast
GI issues
HA
ELEVATED LIVER FXN TESTS (may need a baseline liver test and get it done periodically)
Why must caution be done hen giving zafirlukast alongside warfarin and aspirin
Warfarin - the two can increase warfarin concentration and elevated PT
Aspirin - with ASA the plasma levels of zafirlukast will increase
When should zafirlukast be taken
“Empty Stomach Teaching”
So one hour before meals or two hours after
Corticosteroids
the most effective anti-inflammatory drugs (anti-inflammatory in respiratory as well)
can be oral, inhaled, parenteral (depending on situation acuteness)
Inhaled version only for lungs
Prototype Inhaled Corticosteroid (ICS)
beclomethasone (Vanceril)
-asone on a drug name means what
corticosteroid
Action of beclomethasone
exact mechanism in astham is poorly understood - however it involves antibody formation suppression
it blocks enzymes that produce the inflammatory process in tissues
Important to know: IT DECREASES INFLAMMATION!!!
ADRs of beclomaethasone
Hoarseness
Dry Mouth
LOCALIZED THRUSH INFECTION
What should be done after taking beclomethasone
rinse your mouth out so the steroid does not deposite in the mouth and allow yeast overgrowth
What is a potential SE from taking beclomethasone to be aware of
It could be absorbed systemically a little causing a systemic steroid response in the body - most effective long term control treatment
Corticosteroids are mainly used in what situations (respiratory-wise)
mostly for prevention but cna be used acute depending on the form
-ol means what
beta 2 stimulant
Anti-tussive
suppress the cough reflex
it makes you cough less unlike the mucus drugs
Avoid using anti-tussives in what patients
ones that need the cough to keep airways clear
What else can be used as an antitussive
codeine and other mild narcotic agents
Prototype drug that is antitussive, non opioid
dextromethorphan (DM)
an OTC Antitussive that is not an opioid
Action of dextromethorphan
acts CENTRALLY to suppress medullary cough center (elevating cough threshold) but has NO analgesic or addictive properties
It suppresses the cough center of the brain
dextromethorphan has No ___ or ___ properties, but at high doses…
analgesic or addictive properties: but at high doses it can give a high/buzz so its harder to get now
ADRs of Dextromethorphan
INFREQUENT (unless taken too much)
GI distress and drowsiness
Dextromethorphan is a synthetic opiate derivative so what does this mean for those taking it
it is devoid of analgesic and respiratory depressant effects (except in overdose)
While it may be similar to opioids that may explain why high doses cause a high and why it decreases coughing normally
There is some questioning as to the effectiveness of what drug?
dextromethorphan - some research shows it may do next to nothing in reality
What would a drug with DM (ex: Robitussin DM) in the name mean
it means its a drug mixed with dextromethorphan
___ is a very effective anti tussive that is natural
honey
Why does mixing DM and something like robitussin present a problem
because youre giving DM to decrease coughing but robitussin increases breakup of secretions you need to cough up - its counterproductive
Decongestant Drugs
decrease nasal congestion secondary to inflammation in the upper respiratory tract
Prototype Decongestant Drug
pseudoephedrine (Sudafed)
Action of pseudoephedrine
Stimulates Alpha and Beta adrenergic receptors directly and also causes NEP release (mild EP basically) which causes effects on the cardiac, respiratory, uterine, CNS, and vascular systems
How does pseudoephedrine act on the cardiac system as a decongestant
vasoconstriction and cardiac stimulation (may increase BP)
do not give to someone with HTN
How does pseudoephedrine act on the respiratory system as a decongestant
bronchial muscle relaxation - but less prominent than with EP
How does pseudoephedrine act on uterine activity
it decreases activity
How does pseudoephedrine act on the CNS
acts as a stimulant on the cerebral cortex and medulla somewhat
How does pseudoephedrine act on the vascular system
it causes vasoconstriction (shrinking the mucous membranes) but less so than with EP
How does pseudoephedrine shrink mucus membranes
through vasoconstriction
The main way that pseudoephedrine causes its decongestant effect is how
through vasoconstriction that shrinks inflamed membranes and improves drainage/airflow
pseudoephedrine is almost like a mild what
epinephrine - both are in the sympathetic nervous system family
How does alpha 1 effects impact decongestion
it decreases things and decreases swelling and congestion in the nasal passageway through vasoconstriction
Route of pseudoephedrine
oral
What is important to know about the distribution of pseudoephedrine
it crosses the blood brain barrier
ADRs of pseudoephedrine
MINIMAL - though CV effects like tachycardia and flushing can occur
When should pseudoephedrine not be taken
avoid taking near bedtime as stimulation can occur leading to you being awake
What is the issue with pseudoephedrine as a former-OTC and now current BTC (Behidn the counter) drug
it is used to make methamphetamines
it is now behind the counter and amount bought by a person is tracked by the CDC
Sometimes Sudafex is still seen as an OTC, but what is true about this current version
it is just the trade name drug - it does not have pseudoephedrine as its active ingredient but rather other mild decongestion drugs that do not work the same and are not used to make methamphetamines
Antihistamines
drugs used to treat symptoms associated with allergies for the most part
Prototype Antihistamine (H1 blocking) Drug
diphenydramine (Benadryl)
Other than as an antihistamine, what is diphenhydramine sometimes used for
its sleep SE so use as a hypnotic (Bendaryl)
Action of diphenhydramine
- Competes with histamine for H1 receptor sites preventing physiologic action of histamine
- Inhibits release of AcH
- Sedative effect
By competing for H1 receptor sites and blocking histamine, what effects does that have on the body when taking diphenhydramine
- Smooth muscle restriction will be stopped (bronchi and GI) or constrict others (fine blood vessels)
- Vascular - inhibits vasoconstrictor effects of histamine and more important vasodilator effects
- Cap Permeability - storongly antagonizes histamine action to increase cap permeability and formation of edema
What action of histamine does diphenhydramine NOT effect and why?
The stimulation of gastric secretion as this effect is on H2 receptors not H1
Why does diphenhdyramine inhibit AcH release
It does this to block PNS muscarinic glands making mucus in order to decrease production
this makes it useful for colds as well as allergies
Only take diphenhydramine…
close to bedtime
Route of Diphenhdyramine
Oral, well absorbed, or IV - or even topical
ADRs of Diphenhydramine
Rarely Serious!!! - Often disappear with continued therapy
CNS: SEDATION, dizziness, tinnitus, lassitude, blurred vision, diplopia
GI: Loss of appetite, NV, epigastric dsitress, constipation, diarrhea, dry mouth
Other: urinary frequency, palpitations, hypotension, HA, tingling, weakness of hand (atropine like action of H1 blockers)
Potential Allergic Manifestations in the form of DERMATITIS when applied topically
MOST OF THESE ADRs DO NOT OCCUR
After taking diphenhydramine do not…
operate heavy machinery like a car
Diphenhydramine should never be taken with…
alcohol!!! - it will enhance sedative effects and is a potentially deadly mixture because ROH is a CNS depressant and this is a sedative that can lead to death
If diphenhdyramine is taken enough…
tolerance can occur
Diphenhydramine is often used as a ____ and ___
antihistamine AND hypnotic
An expectorant drug like guaifenesin is often used to relieve:
A. A persistent dry hacking cough
B. Bronchial irritation
C. Vascular congestions
D. Chest or upper airway congestions
Answer: D. chest or upper airway congestion
could be A in a way if they want mucus getting out
The optimal therapeutic range for theophylline (Theodur) is:
A. 8-15 mcg/mL
B. 30-35 mcg/mL
C. 2-5 mcg/mL
D. 20-25 mcg/mL
Answer: A. 8-15 mcg/mL
Which of the following is indicated for treatment of an acute asthma attack?
A. Beclomethasone
B. Zafirlukast
C. Ipratropium
D. Albuterol
Answer: D. Albuterol
Stumper inhaled steroids should be given cautiously to patients with…
A. DM
B. Hypotension
C. Active Respiratory Infection
D. Hypothyroidism
Answer: C. Active Respiratory Infection
Can allow overwhelming infeciton when given steroids - suppresses the immune system by suppressing inflammation
Psuedoephedrine works by …
A. mimicking the PNS
B. mimicking the SNS
C. Blocking the PNS
D. Blocking the SNS
Answer: B: Mimicking the SNS
it mimicks the SNS like a mild EP