long acting β agonist (salmeterol)
leukotriene receptor antagonists (montelukast)Theophylline or cromolyn may also be considered
-Bronchodilation reduces airway resistance as shown by increased FEV1, mid-expiratory flow rate, and vital capacity
-Increased cAMP inhibits the release of mediators from mast cells in the airways, producing a mild antiinflammatory effect
albuterol is the preferred short acting β agonist for use in asthma during pregnancy
overdose can be fatal!
Overdose symptoms may include nervousness, headache, tremor, dry mouth, chest pain or heavy feeling, rapid or uneven heart rate, pain spreading to the arm or shoulder, nausea, sweating, dizziness, seizure (convulsions), feeling light-headed or fainting.
chest pain, palpitations, tremor, nervousness, hypokalemia, ↑ BP, HA, dizziness, insomnia, cough, hoarseness, sore throat, runny nose, drymouth & throat, muscle pain, diarrhea.
rarely, paradoxical bronchospasm may occur
∗use w/ caution in pt’s with DM as β agonists can ↑ serum glucose
∗use w/ caution in pt’s with glaucoma as β agonists can ↑ intraocular pressure
∗use w/ caution in pt’s with hyperthyroidism as β agonists can ↑ thyroid activity
∗use w/ caution in pt’s with hypokalemia as β agonists can ↓ serum K⁺
∗use w/ caution in pt’s with seizure disorders as β agonists can stimulate the CNS
Excretion: urine primarily, feces; Half-life: 2.7-6h
anticholinergic bronchodilator used in bronchospasm associated w/ COPD, bronchitis, & emphysema (& asthma exacerbations but is more effective in COPD than asthma)
Drug of choice for beta-blocker induced bronchospasms
blocks the action of acetylcholine at parasympathetic sites in bronchial smooth muscle causing bronchodilation
Drug of choice for beta-blocker induced bronchospasms
ok for pregnant women suffering w/ severe asthma exacerbations
URI, bronchitis, sinusitis, CP, palpitations, HA, dizziness, dyspepsia, nausea, UTI, back pain, dyspnea, rhinitis, cough, pharyngitis, ↑ sputum, flu-like syndrome
rarely, paradoxical bronchospasm may occur
NOT FOR RESCUE THERAPY. This med should only be used in acute exacerbations of asthma IN CONJUNCTION WITH a short acting β agonist for acute episodes
use with caution in pt’s w/ narrow angle glaucoma, myasthenia gravis, & prostatic hyperplasia/bladder neck obstructions
Absorption: Mean bioavailability is 7% (inhalation). Ipratropium is not readily absorbed.
Distribution: 0 to 9% is protein bound.
Metabolism: Partially metabolized.
Excretion: The t ½ is approximately 2 h (inhalation or IV). Following IV administration, approximately half of the dose is excreted unchanged in the urine.
none of these are on the study guide so don’t worry about it!
prednisone, prednisolone, methylprednisone
Reduce airflow obstruction by reducing airway inflammation in the bronchioles
Modify the body’s immune responses to various stimuli
Suppress cytokine production, airway eosinophil recruitment, and the release of inflammatory mediators
∗Most potent /effective controller asthma medication
∗Broad action on inflammatory processes
∗MDI, DPI, nebulizer solution
∗Improves symptoms, pulmonary function
∗Reduces exacerbations (urgent visits, emergency care, hospitalizations, quick-relief medications, oral CS)
∗Reduces airway hyperresponsiveness:
∗HPA suppression is noted in adults receiving 32 puffs/day of an inhaled steroid over a period of 1 month – monitor for adrenal insufficiency
∗Inhaled corticosteroids (ICS) provide local therapeutic action with minimal systemic effects
ICS are in both Asthma/COPD and Upper Respiratory Infections
I will only include Flunisolide (Aerobid) here because it is oral. The other five ICS are nasal and I will group them together under URI as it is done on the professor’s slides [Budesonide (Rhinocort), Flunisolide (Nasarel), Fluticasone propionate (Flonase), Mometasone furoate (Nasonex),
& Triamcinolone acetonide (Nasacort)]
Also note! Just for fun, there are TWO Flunisolides – Aerobid & Nasarel.
Long-term prevention of bronchospasm in patients with asthma
Aerobid (flunisolide) Inhaler is indicated in the maintenance treatment of asthma as prophylactic therapy. Aerobid is also indicated for asthma patients who require systemic corticosteroid administration, where adding Aerobid may reduce or eliminate the need for the systemic corticosteroids.
Aerobid Inhaler is NOT indicated for the relief of acute bronchospasm.
pts treated w/ Aerobid (flunisolide) should be observed for any systemic corticosteroid effect, including suppression of bone growth in children. Particular care should be taken in post-op pt’s or during periods of stress for ↓ in adrenal function.
Also safety issues: bone density, bruising
Corticosteroids may mask infection or predispose to infection, especially fungal; subcapsular cataracts; glaucoma; adrenocortical insufficiency; psychic derangements; GI bleeding; diabetes mellitus, reactivation of tuberculosis
∗ use at regular intervals for effectiveness
∗ do not use as emergency therapy for asthma attacks
∗ Do not abruptly stop medication administration
∗ Discard canister when doses should have been used; canister cannot be accurately checked
cause relaxation of bronchial smooth muscle. Slowly cleared from body so effects are long lasting (onset of action is also longer).
Not used in acute asthma attack
Corticosteroids increase b2-receptor synthesis and decrease b2 desensitization
LABAs prime glucocorticoid receptors for steroid-dependent activation
β-agonists may interfere with uterine contractility if administered during labor – use only if clearly needed.
monotherapy! it should never be used alone to treat asthma
Arrhythmias and/or tachycardia, cardiac arrest, death, headache, hyperglycemia, hypokalemia, muscle cramps, palpitations, prolongation of the QTc interval, tremor
rarely, paradoxical bronchospasm may occur
Distribution: Protein binding is 96%;
Metabolism: Extensively metabolized by hydroxylation.
Excretion: Eliminated in feces (60%) and urine (25%); t ½ is 6 days.
∗ NEVER use a spacer device
∗ daily use is required to manage sxs
∗ do not exceed prescribed does (yes, it DID go into the nose!)
Diuretics: ECG changes and hypokalemia associated with diuretics may worsen with coadministration.
MAOIs, tricyclic antidepressants: May increase CV effects of salmeterol.
block the production or action of inflammatory mediators called leukotrienes, reducing inflammation and relaxing airway smooth muscle and reducing mucus production.
Not used for acute attack.
will not interrupt the bronchoconstrictor response to ASA or NSAIDs; use caution with those drugs
rarely, can cause systemic eosinophilia and vasculitis or behavorial changes
Advise patient with asthma or asthma and allergic rhinitis to take prescribed dose once daily in the evening – best taken 1 hour before meals or 2 hours after.
Caution patient with asthma that medication is not to be used to treat acute asthma attacks. Instruct patient to always have a short-acting beta-agonist available for acute treatment of asthma symptoms
Effect is weaker than that of low-dose inhaled corticosteroids
Usually used as add-on therapy in asthma
Theophylline may be used either as an adjunctive therapy in conjunction with ICS or as an alternative agent, but is not recommended as a preferred therapy
Cromolyn sodium is an alternative option
treatment of symptoms and reversible airway obstruction due to chronic asthma or other chronic lung diseases
a mild to moderate bronchodilator used as alternative, not preferred, therapy for step 2 care (for mild persistent asthma) or as adjunctive therapy with ICS in patients > 5 years of age.
Act as a direct central nervous system stimulant, resulting in vasoconstriction and stimulation of the vagal center, which causes bradycardia
In large doses, cause a positive inotropic effect on myocardium and a positive chronotropic effect on SA node
Theophylline may have mild anti-inflammatory effects. Monitoring of serum theophylline concentration is essential
Therapeutic index is low – think toxicity!
Many drugs and physiologic variables affect theophylline metabolism, and dosage adjustment is required
Serum concentration monitoring should take place:
Whenever signs of toxicity are suspected
On initiation of drug and dosage titration until steady state therapeutic concentration is reached
Routinely every 6 months in children and yearly in adults
Excretion: urine (10% unchanged); Half-life: 8.2h; Info: half-life altered by many concurrent illnesses
Do not change brands of theophylline without consulting provider
Notify provider if nausea, vomiting, insomnia, jitteriness, headache, rash, severe GI pain, restlessness, convulsions, or irregular heartbeat occurs
Avoid caffeine-containing beverages and other stimulants
and for Asthma prophylaxis. Prevention of bronchoconstriction before exposure to a known precipitant
nonsteroidal antiallergic – mast cell stabilizer
Note – Cromolyn is another double drug on this test, as Intal here (nebulizer) and later on as NasalCrom (nasal spray)
use w/ caution in pt’s with a h/o arrhythmias, hepatic or renal impairment
need to be tapered off
now only available in Nebulizer form, the inhalers were discontinued
in addition to those used in mild dz, add on:
long acting β agonist
in addition to those used in mild & moderate dz, add on:
in addition to those used in mild, moderate, & severe dz; add on:
O2, consider surgery
Antihistamine, preferably nonsedating, or a decongestant
If the pt is unable to take an oral antihistamine, consider the use of a nasal antihistamine, intranasal cromolyn, or a leukotriene receptor antagonist
Regular- to high-dose intranasal corticosteroid
Add an oral or nasal antihistamine and decongestant if necessary
Combination regimen consisting of a nonsedating antihistamine with or without a decongestant and intranasal corticosteroid
Consider the use of an oral steroid for 5 days and the use of oxymetazoline as needed for no longer than 3 days
ethanolamine: diphenhydramine; clemastine fumarate, alkylamine: chlorpheniramine maleate
piperadine: cetirizine HCl
fexofenadine HCl, loratadine HCl, desloratadine
Adjunct to epinephrine in the treatment of anaphylaxis
Nighttime sleep aid
Prevention or treatment of motion sickness
Management of Parkinsonian syndrome including drug-induced extrapyramidal symptoms
Topically for relief of pain and itching associated with insect bites, minor cuts and burns, or rashes due to poison ivy, poison oak, and poison sumac
some toxicity seen in newborns if mom was taking a lot; not the antihistamine of choice for allergic rhinitis, n, or v in pregnancy
Hypersensitivity; acute asthma; neonates or premature infants; breast-feeding; use as a local anesthetic (injection)
she mentioned breast feeding like 4 times with this one
Maximum sedative effect: 1-3 hours
Duration: 4-7 hours
Metabolism: Extensively hepatic via CYP2D6; minor CYP1A2, 2C9 and 2C19; smaller degrees in pulmonary and renal systems; significant first-pass effect
Bioavailability: Oral: ~40% to 70%
Half-life elimination: 2-10 hours; Elderly: 13.5 hours
Time to peak, serum: 2-4 hours
Excretion: Urine (as unchanged drug
Report persistent sedation, confusion, or agitation; changes in urinary pattern; blurred vision; sore throat, respiratory difficulty, or expectorating; or lack of improvement or worsening or condition
bladder neck obstruction or symptomatic prostate hypertrophy
during acute asthmatic attacks
stenosing peptic ulcer or pyloroduodenal obstruction
In elderly pts, the anticholinergic action may cause significant confusional symptoms, constipation, or problems voiding urine.
watch for CNS depression
use w/ caution in those w/ CV dz, ↑ intraocular pressure, prostatic hyperplasia/GU obstruction, asthma or chronic breathing disorders, or thyroid dysfunction
Metabolism: Substrate of CYP2D6 (minor), 3A4 (major); Inhibits CYP2D6 (weak)
On to more classes of drugs for allergic rhinitis…
What are some intranasal steroids that will be on the test?
Fluticasone propionate (Flonase)
Mometasone furoate (Nasonex)
Cromolyn sodium (NasalCrom)
this drug was covered above in asthma (Intal the nebulizer) so I’m only going to highlight the differences here (NasalCrom is a nasal spray)
montelukast sodium (Singulair)
this was covered above in asthma so I’m not going to do another drug card here as it is in the same form and everything – only major difference is dosing
Inhibit cells, including mast cells, eosinophils, neutrophils, macrophages, lymphocytes, and mediators such as histamine, leukotrienes, and cytokines
Exert direct local antiinflammatory effects with minimal systemic effects
Effectively control the four major symptoms of allergic rhinitis—rhinorrhea, congestion, sneezing, and nasal itch
The most effective agents for the management of allergic rhinitis because of their direct reduction of nasal inflammation and their ability to reduce nasal hyperreactivity
Should be used for at least 3-4 weeks before a decision is made as to whether they are effective (1 inhaler)
Can be used with asthmatic patients and with those who have comorbid nasal polyposis. Intranasal steroids may help shrink nasal polyps
Minimal systemic absorption
Effectiveness depends on regular use and adequate nasal airway for delivery
Most do not alleviate ocular symptoms
Aversion of nasal sprays (Discomfort, Addiction)
Local irritation, mucosal changes; nosebleeds
Cataracts, glaucoma (STUDY CONCLUSION:
No increase risk of cataract in patients taking INS)
Do not exceed recommended dosage
Clear secretions from nasal passages before using; use decongestants if necessary
Effects are not immediate; results require regular use and may take up to 7 days
avoid in pts w/ adrenal suppression, delayed wound healing, immunosupression, infections, or ocular dz
especially in nasal infection, trauma, or s/p nasal surgery
Cat B – budesonide
Cat C – flunisolide, fluticasone, triamcinolone, mometasone
once a day spray – budesonide, fluticasone, triamcinolone, mometasone
twice a day (or more) spray – flunisolide