PHARMACOLOGY asthma, COPD, nasal steroids

What is the first line treatment for asthma, a.k.a. quick relief?
short acting β agonist (albuterol)
anticholinergics (ipratropium)
Systemic corticosteroids
What is the second line treatment for asthma, a.k.a. controllers?
inhaled corticosteroids (aerobid)
long acting β agonist (salmeterol)
leukotriene receptor antagonists (montelukast)Theophylline or cromolyn may also be considered

First line: How do the short acting β agonist work on the body?
-Sympathomimetic that results in smooth airway muscle relaxation
-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 – Class
short acting β agonist
Albuterol – Indication
treatment or prevention of bronchospasm in pt’s w/ reversible obstructive airway dz; prevention of exercise-induced bronchospasm
Albuterol – MOA
relaxes bronchial smooth muscle by action on β₂ receptors w/ little effect on HR
Albuterol – Pregnancy

Cat C

albuterol is the preferred short acting β agonist for use in asthma during pregnancy

Albuterol – Contraindications

hypersensitivity

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.

Albuterol – Adverse effects

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

Albuterol – Precautions
∗use w/ caution in pt’s with CV dz as β agonists can ↑ BP, ↑ HR, stimulate the CNS, and ↑ risk of arrhythmias
∗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
Albuterol – Metabolism & Excretion
Metabolism: liver extensively; CYP450: unknown
Excretion: urine primarily, feces; Half-life: 2.7-6h
First line: How do anticholinergic bronchodilators work on the body?
block the nerve responses (parasympathetic) that normally cause narrowing of airways. Commonly used in combination with a beta 2 bronchodilator such as albuterol.
Ipratropium (Atrovent) – Class
anticholinergic agent
Ipratropium (Atrovent) – Indication

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

Ipratropium (Atrovent) – MOA

blocks the action of acetylcholine at parasympathetic sites in bronchial smooth muscle causing bronchodilation

Drug of choice for beta-blocker induced bronchospasms

Ipratropium (Atrovent) – Pregnancy

Cat B

ok for pregnant women suffering w/ severe asthma exacerbations

Ipratropium (Atrovent) – Contraindications
hypersensitivity to ipratropium or atropine
Ipratropium (Atrovent) – Adverse effects

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

Ipratropium (Atrovent) – Precautions

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

Ipratropium (Atrovent) – PK/PD

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.

Ipratropium (Atrovent) – Pt education
Avoid contact with eyes; may cause temporary blurring of vision
First line: Systemic corticosteroids

none of these are on the study guide so don’t worry about it!

prednisone, prednisolone, methylprednisone

Second line: How do inhaled corticosteroids (ICS) work on the body?

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

Why would you use ICS?
∗Management of persistent asthma, all severity levels
∗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
NOTE!

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.

Flunisolide (Aerobid) – Class
inhaled corticosteroids
Flunisolide (Aerobid) – Indication

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.

Flunisolide (Aerobid) – MOA
↓ inflammation by suppression of migration of polymorphonuclear leukocytes & reversal of ↑ capillary permeability; does not depress hypothalamus
Flunisolide (Aerobid) – Pregnancy
Cat C
Flunisolide (Aerobid) – Contraindications
hypersensitivity
Flunisolide (Aerobid) – Adverse effects
n/v/d dyspepsia, flu like symptoms sore throat, HA, nasal congestion, URI, unpleasant taste, palpitations, abd pain, CP, ↓ appetite, edema, fever, candida infection, dizziness, nervous,
Flunisolide (Aerobid) – Precautions

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

Flunisolide (Aerobid) – Pt Education
∗ Rinse mouth after use
∗ 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
Second line: How do long acting β agonists work on the body?

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

How do long acting β agonists and corticosteroids complement each other?

Corticosteroids increase b2-receptor synthesis and decrease b2 desensitization

LABAs prime glucocorticoid receptors for steroid-dependent activation

Salmeterol (Serevent) – Class
long acting β agonist
Salmeterol (Serevent) – Indication
maintenance treatment of asthma & prevention of bronchospasm (as concomitant therapy) in pt’s with reversible obstructive airway dz, to include pt’s w/ sxs of nocturnal asthma, prevention of exercise-induced bronchospasm, & maintenance treatment of bronchospasm associated with COPD
Salmeterol (Serevent) – MOA
relaxes bronchial smooth muscle by selective action on β₂ receptors w/ little effect on HR; salmeterol acts locally in the lung
Salmeterol (Serevent) – Pregnancy

Cat C

β-agonists may interfere with uterine contractility if administered during labor – use only if clearly needed.

Salmeterol (Serevent) – Contraindications

hypersensitivity

monotherapy! it should never be used alone to treat asthma

Salmeterol (Serevent) – Adverse effects

Arrhythmias and/or tachycardia, cardiac arrest, death, headache, hyperglycemia, hypokalemia, muscle cramps, palpitations, prolongation of the QTc interval, tremor

rarely, paradoxical bronchospasm may occur

Salmeterol (Serevent) – Precautions
When added to usual asthma therapy, there may be an increase in asthma-related deaths. Only use salmeterol as additional therapy for patient not adequately controlled on other asthma-controller medications (eg, low- to medium-dose inhaled corticosteroids) or whose disease severity clearly warrants initiation of treatment with 2 maintenance therapies, including salmeterol – do not use salmeterol as monotherapy.
Salmeterol (Serevent) – PK/PD
Absorption: Salmeterol acts locally in the lung. Plasma levels do not predict therapeutic effect. Depending on dose, T max is 5 to 45 min
Distribution: Protein binding is 96%;
Metabolism: Extensively metabolized by hydroxylation.
Excretion: Eliminated in feces (60%) and urine (25%); t ½ is 6 days.
Salmeterol (Serevent) – Pt education
∗ do not use for acute exacerbations of asthma
∗ NEVER use a spacer device
∗ daily use is required to manage sxs
∗ do not exceed prescribed does (yes, it DID go into the nose!)
Salmeterol (Serevent) – drug/drug interactions
Beta-adrenergic blockers: Pulmonary effects of salmeterol may be blocked and may produce severe bronchospasm in patients with COPD.
Diuretics: ECG changes and hypokalemia associated with diuretics may worsen with coadministration.
MAOIs, tricyclic antidepressants: May increase CV effects of salmeterol.
Second line: How do leukotriene receptor agonists work on the body?

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.

Montelukast sodium (Singulair) – class
leukotriene receptor antagonist
Montelukast sodium (Singulair) – indication
prophylaxis and chronic treatment of asthma; relief of symptoms of seasonal allergic rhinitis & perennial allergic rhinitis; prevention of exercise-induced bronchospasm
Montelukast sodium (Singulair) – MOA
selective leukotriene receptor antagonist that inhibits the cysteinyl leukotriene receptor (these receptors have been correlated with the pathophys of asthma and allergic rhinitis).
Montelukast sodium (Singulair) – pregnancy
Cat B
Montelukast sodium (Singulair) – contraindications
hypersensitivity
Montelukast sodium (Singulair) – adverse effects
dizziness, fatigue, HA, fever, rash, dyspepsia, dental pain, gastroenteritis, ↑ LFTs, weakness, nasal congestion, epistaxis, sinusitis, URI, abd pain, psychomotor hyperactivity, somnolence, thirst, vomiting
Montelukast sodium (Singulair) – precautions

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

Montelukast sodium (Singulair) – pt education

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

Montelukast sodium (Singulair) – other
May be used as an alternative to inhaled corticosteroids in patients with mild persistent or aspirin-sensitive asthma
Effect is weaker than that of low-dose inhaled corticosteroids
Usually used as add-on therapy in asthma
Why use theophylline or cromolyn?

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

What are methylxanthines used for?
Cause relaxation of bronchial smooth muscle by blocking action of chemicals that cause contraction. Oral slow release theophylline is used to long term control. They are however irritating to the stomach. Available in IV form for used in acute asthma attack.
Theophylline – Class
methylxanthine
Theophylline – Indication

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.

Theophylline – MOA
Promote bronchodilation by competitively inhibiting phosphodiesterase, the enzyme that degrades cAMP, which in turn, increases intracellular cAMP
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 – Pregnancy
Cat C
Theophylline – Contraindications
hypersensitivity or allergy to corn as the premixed injection may contain corn-derived dextrose
Theophylline – Adverse effects
vomiting, insomnia, restlessness, seizures, increased heart rate, or a headache
Theophylline – Precautions

Theophylline may have mild anti-inflammatory effects. Monitoring of serum theophylline concentration is essential

Therapeutic index is low – think toxicity!

Theophylline – how to monitor
Monitoring Parameters serum drug levels, q24h during infusion
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
Theophylline – PK/PD
Metabolism: liver; CYP450: 1A2, 2E1, 3A3 substrate; Info: aminophylline converted to theophylline; active metabolites
Excretion: urine (10% unchanged); Half-life: 8.2h; Info: half-life altered by many concurrent illnesses
Theophylline – Pt education
Extended-release capsules should be taken 1 hour before or 2 hours after meals; immediate-release forms can be taken with food if GI upset occurs
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
Why use a nonsteroidal antiallergic?
to block the release or action of inflammatory chemicals in the body reducing symptoms of inflammation. Block degranulation of the mast cell. Not for acute attack.
and for Asthma prophylaxis. Prevention of bronchoconstriction before exposure to a known precipitant
Cromolyn (Intal) – Class

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)

Cromolyn (Intal) – Indication
may be used as an adjunct in the prophylaxis of allergic disorders, including asthma; prevention of exercise-induced bronchospasm
Cromolyn (Intal) – MOA
prevents the mast cell release of histamine, leukotrienes, and slow-reacting substance of anaphylaxis by inhibiting degranulation after contact with antigens
Cromolyn (Intal) – Pregnancy
Cat B
Cromolyn (Intal) – Contraindications
hypersensitivity, acute asthma attacks
Cromolyn (Intal) – Adverse effects
Bronchospasm, throat irritation, bad taste, cough, wheezing, nasal congestion, anaphylaxis
Cromolyn (Intal) – Precautions

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

Cromolyn (Intal) – Pt education
take 30 min before meals. clear as much mucus as possible before use. Rinse mouth after use to ↓ unpleasant aftertaste.
What drugs are used for mild COPD?
short acting β agonist
What drugs are used for moderate COPD?

in addition to those used in mild dz, add on:

anticholinergic
long acting β agonist

What drugs are used for severe COPD?

in addition to those used in mild & moderate dz, add on:

inhaled corticosteroid

What drugs are used for very severe COPD?

in addition to those used in mild, moderate, & severe dz; add on:

O2, consider surgery

What other drug might you consider for COPD?
theophylline
Bronchodilators & the older adult
Bronchodilators may cause increased adverse reactions; some older adults may not tolerate side effects such as tachycardia
Theophylline & the older adult
Theophylline clearance is reduced in the older adult, causing increased risk of drug toxicity and interaction
Corticosteroids & the older adult
High-dose inhaled corticosteroids and oral corticosteroids that are often used in COPD may cause or worsen osteoporosis in the older adult
Nebulization & the older adult
Nebulization treatment may be useful when older adults are unable to use inhalers correctly
Corticosteroids & pregnancy
ICS does not increase the risks of major malformations, preterm delivery, low birth weight, and pregnancy-induced hypertension
Cat B drugs
ipratropium, mast cell stabilizers, budesonide, montelukast and zafirlukast, and terbutaline, cromolyn
Cat C drugs
β-Adrenergic agonists (except terbutaline), theophylline, tiotropium, corticosteroids (except budesonide), zileuton, albuterol, aerobid, salmeterol
Theophylline & breastfeeding
Breastfeeding may have to be discontinued because the drug can cause serious toxicity in nursing infants
How do you treat mild, intermittent symptoms of allergic rhinitis?

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

How do you treat moderate, frequent symptoms of allergic rhinitis?

Regular- to high-dose intranasal corticosteroid

Add an oral or nasal antihistamine and decongestant if necessary

How do you treat moderate, persistant symptoms of allergic rhinitis?
Combination regimen consisting of intranasal corticosteroids plus a nonsedating or intranasal antihistamine and decongestant if necessary
How do you treat severe symptoms of allergic rhinitis?

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

Which antihistamines are sedating?

benadryl, Chlor-Trimeton

ethanolamine: diphenhydramine; clemastine fumarate, alkylamine: chlorpheniramine maleate

Which antihistamines are low-sedating?

zyrtec

piperadine: cetirizine HCl

Which antihistamines are nonsedating?

allegra, claritin

fexofenadine HCl, loratadine HCl, desloratadine

What are two 1st generation antihistamines that are OTC and on our test?
Diphenhydramine (Benadryl) & chlorpheniramine maleate (Chlor-Trimeton)
Diphenhydramine (Benadryl) – Class
Histamine H1 Antagonist, first gen
ethanolamine derivative
Diphenhydramine (Benadryl) – Indication
Symptomatic relief of allergic symptoms caused by histamine release including nasal allergies and allergic dermatosis
Adjunct to epinephrine in the treatment of anaphylaxis
Nighttime sleep aid
Prevention or treatment of motion sickness
Antitussive
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
Diphenhydramine (Benadryl) – MOA
Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract; anticholinergic and sedative effects are also seen
Diphenhydramine (Benadryl) – Pregnancy

Cat B

some toxicity seen in newborns if mom was taking a lot; not the antihistamine of choice for allergic rhinitis, n, or v in pregnancy

Diphenhydramine (Benadryl) – Contraindications

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

Diphenhydramine (Benadryl) – Adverse effects
sedation, sleepiness, dizzy, n, v, urinary retenion or frequency, thickening of bronchial secretions, stuffiness, anaphylaxis, dry mouth/throat, blurred vision
Diphenhydramine (Benadryl) – Precautions
use w/ caution in those that have asthma, CV dz, glaucoma, prostatic hyperplasia/GU obstruction, pyloroduodenal obstruction, or thyroid dysfunction
Diphenhydramine (Benadryl) – PK/PD
PK: Onset of action:
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
Diphenhydramine (Benadryl) – Pt education
Avoid use of other depressants, alcohol, or sleep-inducing medications unless approved by prescriber. It may cause drowsiness or dizziness (use caution when driving or need to be alert); or dry mouth, nausea, or vomiting.
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
Chlorpheniramine maleate (Chlor-Trimeton) – Class
Histamine H1 Antagonist, first gen
alkylamine derivative
Chlorpheniramine maleate (Chlor-Trimeton) – Indication
Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria
Chlorpheniramine maleate (Chlor-Trimeton) – MOA
competes w/ histamine for H₁ receptor sites on effector cells in the GI tract, blood vessels, & resp tract
Chlorpheniramine maleate (Chlor-Trimeton) – Pregnancy
Cat C
Chlorpheniramine maleate (Chlor-Trimeton) – Contraindications
Hypersensitivity to any component of the formulation
Narrow-angle glaucoma
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.
Chlorpheniramine maleate (Chlor-Trimeton) – Adverse effects
drowsiness, thickening of bronchial secretions, HA, dizzy, n, diarrhea, wt gain & appetite increase, urinary retention, diplopia, polyuria, pharyngitis, arthralgia, weakness
Chlorpheniramine maleate (Chlor-Trimeton) – Precautions

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

Chlorpheniramine maleate (Chlor-Trimeton) – PK/PD
PK: Half-life elimination, serum: 20-24 hours
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?

Traimcinolone acetonide (Nasacort)
Fluticasone propionate (Flonase)
Budesonide (Rhinocort)
Flunisolide (Nasarel)
Mometasone furoate (Nasonex)
And what is an intranasal mast cell stabilizer that will be on the test?

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)

And what is a Leukotriene Receptor Antagonist that will be on the test?

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

When should NasalCrom be started?
Should be started 3 to 4 weeks before a peak allergy season occurs
What is the effect of NasalCrom on the nose?
Their effect on the nose is short acting and makes compliance more difficult in that several doses are needed per day
What should you monitor for with NasalCrom?
Instruct patients to notify health care provider of any stinging effect after nasal instillation
Now on to the five intranasal steroids…
exciting!!!!!
Intranasal Steroids – Indication
Vasomotor rhinitis and relief of symptoms of seasonal or perennial rhinitis when effectiveness of antihistamines or tolerance to treatment develops
Intranasal Steroids – MOA
Potent glucocorticoid and weak mineralocorticoid activity
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
Intranasal Steroids – Effectiveness

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

Intranasal Steroids – Benefits
Relieve sneezing, nasal pruritus, rhinorrhea, and reactive mucosal edema
Minimal systemic absorption
Effectiveness depends on regular use and adequate nasal airway for delivery
Most do not alleviate ocular symptoms
Intranasal Steroids – Common concerns
Steroid phobia
Aversion of nasal sprays (Discomfort, Addiction)
Local irritation, mucosal changes; nosebleeds
Cataracts, glaucoma (STUDY CONCLUSION:
No increase risk of cataract in patients taking INS)
Intranasal Steroids – Pt education
Use patient information provided with product on how to use nebulizer, inhaler
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
Intranasal Steroids – Side effects
Pharyngitis, epistaxis, cough, headache, weakness, tired feeling, nausea, loss of appetite, weight loss; fever, chills, body aches, flu symptoms; easy bruising or bleeding, unusual weakness; white patches or sores inside your nose or mouth, or on your lips; or blurred vision, eye pain, or seeing halos around lights
Intranasal Steroids – Precautions

avoid in pts w/ adrenal suppression, delayed wound healing, immunosupression, infections, or ocular dz

especially in nasal infection, trauma, or s/p nasal surgery

Intranasal Steroids – Pregnancy

Cat B – budesonide

Cat C – flunisolide, fluticasone, triamcinolone, mometasone

Intranasal Steroids – Dosing differences

once a day spray – budesonide, fluticasone, triamcinolone, mometasone

twice a day (or more) spray – flunisolide

Intranasal Steroids – differences
there aren’t a lot of differences. I highly suspect this is one of those “which one is safe for pregnant women?” ones – which would be budesonide (Rhinocort)

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