Drugs affecting the

Respiratory
System
Coughs, colds and
allergic rhinitis

Copyright ©2020 F.A. Davis

Company
Outline

Allergic Rhinitis
Intranasal steroids
Antihistamines
Intranasal Cromolyn
Sympathomimetics (Decongestants)

Drugs for Coughs & Colds

Expectorants
Anitussives (Opioid & Non-Opioid)
Mucolytic Agents
 Drugs for Allergic
Rhinitis

Intranasal steroids
Antihistamines
Intranasal Cromolyn
Sympathomimetics
(Decongestants)
Intranasal Glucocorticoids (INGC)

The MOST effective/ 1st line drugs for

prevention & treatment of seasonal &
perennial rhinitis
Intranasal 1 to 2 times daily
90% of patients respond well
Avoid if nasal trauma or ulcers, untreated URI
MOA: decrease inflammation & edema
Word ending for steroids: “sone” (see next slide)
ADRs:
Systemic effects rare
Local reactions: drying of nasal mucosa; nasal irritation,
sneezing, burning or itching sensation; sore throat,
epistaxis, headache
Intranasal Glucocorticoids (INGC)

Administered via a metered-dose spray: May take up to 2-3 weeks

for benefit
INGC Administration Tips

Clear nasal passages of mucus.

Rinse mouth with water after each use
Have patient tilt head forward, directing the
nozzle slightly away from the midline to avoid
contact with the septum.
Aim to deliver the dose throughout the lining of
the nasal cavity.
Do not blow nose for at least one minute post
after administration
Antihistamines (MOA)
Antihistamines

Reduce or prevent most physiological effects of histamine

at the histamine 1 (H1) receptor site
Strongly block the action of histamine
Decrease the flare-and-itch response
Uses:
Relief of symptoms of mild to moderate allergic
disorders including allergic rhinitis, allergic conjunctivitis,
uncomplicated urticaria, & angioedema
Antihistamines: Clinical Use

Respiratory allergies
Hypersensitivity reactions
Urticaria and angioedema
Nighttime sleep aid
Motion sickness/antiemetic
Antihistamine Precautions

First Generation
Cautions
Pregnancy category B
Sedation and drowsiness; reduced mental alertness
Contraindicated
Newborns and infants
Second Generation
Pregnancy
Pregnancy categories B and C
Children
Fexofenadine: age less than 6 years
Loratadine: age 2+ years
Cetirizine and desloratadine syrup: age 6+ months
First-Generation Antihistamines: ADRs

Sedation or fatigue Diplopia

Dizziness Tremors
Headache Increased/decreased
Tinnitis appetite
Lassitude Epigastric distress
Disturbed coordination Constipation
Nausea or vomiting Diarrhea
Irritability/nervousness Dry mouth
Blurred vision Urinary retention
Dysuria
 Adverse Effects: H1
Antihistamines

First Generation
Antihistamines
Second-Generation Antihistamines:
ADRs
Drowsiness is greatly reduced
Minimal incidence of dry mouth (5% or less)
Symptoms caused by first-generation antihistamines can be
alleviated by switching to second-generation antihistamines
1st Generation Antihistamines
Patient Education

1st generation antihistamines – take at bedtime to avoid

sedation
If taken during day, caution the patient about safety measures w/
driving, operating machinery, & ambulating. Sedation usually
decreased w/ repeated doses.
2nd Generation Antihistamines

Poorly cross the blood-brain barrier

Have a low affinity for H1 receptors in the CNS
Because of these characteristics – do not cause the
sedation seen in
the first generation antihistamines
Decongestants

Uses
Common cold
Allergic rhinitis
Methods of delivery
Liquid, tablet, capsule, nasal spray, drops
Sympathomimetics
Decongestants: Contraindications

Patients on concurrent MAOI therapy

Patients with severe hypertension or coronary artery disease
Oral Decongestants: ADRs

More common
Restlessness and tremors
Less common or rare
Transient hypertension, arrhythmia, and cardiovascular collapse, with
hypotension
Sympathomimetics
(Decongestants)
MOA: activate alpha1 adrenergic receptors on nasal blood vessels
-> vasoconstriction
Decongestants reduce nasal congestion & swelling.
Oral pseudoephedrine (OTC Restrictions- see below)
Topical: phenylephrine, oxymetazoline, tetrahydrozoline
Adverse effects
Rebound congestion (topicals) used for more than 5 days
CNS stimulation (oral) – restlessness, anxiety, insomnia
CV effects (oral) – tachycardia, inc. BP
Use cautiously HTN, dysrhythmias, cerebrovascular disease
Risk for Abuse – pseudoephedrine used to make
methamphetamines
Topical Decongestants: ADRs

Transient stinging
Burning
Sneezing
Dryness
Local irritation
Rebound congestion with prolonged use
Clinical Use for Nasal Congestion

Oral decongestant
Temporarily relieve nasal congestion
Promote nasal or sinus drainage
Relieve eustachian tube congestion
Topical decongestant
Symptomatically relieve nasal congestion
Relieve ear blockage and pressure pain
Decongestants: Short- vs Acting

Short-acting
Better tolerated and have fewer ADRs
Long-acting
Useful for patients who require all-day or all-night relief, if patient can
tolerate
Topical Decongestants: ADRs

Transient stinging
Burning
Sneezing
Dryness
Local irritation
Rebound congestion with prolonged use
Sympathomimetics:Patient
education
Instruct patient not to overuse the agent because maybe habit-
forming w/ episodes of rebound engorgement. Limit
number of days med used.
**Do not exceed 2 doses/ 24 hrs for 3-5 days
Daily dose: 2-3sprays/nostril q 12 hr
Have patient limit caffeine intake
Take early in day – insomnia
Advise patient to take in sitting position when administering
Maintain adequate hydration.
Refrain from smoking when congested.
Avoid caffeine-containing products.
Question

When assessing a patient who is to receive a decongestant, the APRN

will recognize that a potential contraindication to this drug would be
which condition?

a. Glaucoma
b. Fever
c. Peptic ulcer disease
d. Allergic rhinitis
Drugs for Coughs and
Colds
Antitussives
Expectorants
Mucolytic Agents
Expectorants

An agent that increases the flow of fluid in the respiratory tract.

Reduces the viscosity of bronchial & tracheal secretions
facilitates secretions by the cough reflex & ciliary action.
Expectorants

Indication - dry, nonproductive cough, mucous

Pharmacokinetics: absorbed PO,

metabolized liver, excreted kidneys

Forms - syrup, tablet, liquid, capsule, sustained-

release capsule
Expectorants: Guaifenesin

The only expectorant ingredient listed by the U.S. Food and

Drug Administration (FDA) panel as having scientific
evidence of safety and efficacy
Aids in symptomatic treatment of cough caused by the
common cold and mild upper respiratory infections
Found in many cough syrups
Uses
used to decrease mucus viscosity
convert a nonproductive cough into a productive cough
Other names: glyceryl guaiacolate, guiatuss, humibid,
robitussin, antituss, mucinex
Guaifenesin: Precautions

Do not use for persistent cough

Do not use for cough related to heart failure or angiotensin-
converting enzyme (ACE) inhibitor therapy
Do not use for cough with high fever or lasting longer than 7 days
Expectorants: Guaifenesin

ADRs
Most common
GI upset, nausea, and vomiting
Less common
Drowsiness, diarrhea, dizziness, rash, and headache
Guaifenesin: False Laboratory
Readings
Guaifenesin may cause false readings in certain laboratory
determinations of 5-hydroxyindoleacetic acid (5-HIAA) and
vanillylmandelic acid (VMA).
Expectorants: Guaifenesin

Pregnancy C
Contact primary care provider
Cough persists > 1 week
High fever
Rash
Persistent HA
Give with full glass of H2O to help liquefy & loosen mucus in
airways
Note – liquid formulations contain 3.5% to 10% alcohol
Antitussive Agents

Used to self-treat coughs

Exact mechanism of action poorly understood

Opioid vs. Non-opioid antitussive agents

Opioid
codeine

Nonopioid:
benzonatate (Tessalon Perles)

dextromethorphan (Vicks-Formula 44, Robitussin -DM)

Antitussives: Precautions

Do not use for persistent or chronic cough caused by smoking,

asthma, or emphysema.
Do not use if you have excessive respiratory secretions.
Do not self-medicate for cough lasting longer than 7 days.

Antitussives: Lifestyle Management

Increase fluid intake.
Refrain from or quit smoking.
Avoid respiratory irritants and people with respiratory infections.
Antitussives: OpioidCodeine
(Schedule II)
Indication: coughing
MOA: narcotic analgesic; mu receptor agonist
Forms: PO, rectal
ADRs: sedation, confusion, resp. depression, hypotension, N/V, seizures
Contraindications: Hypersensitivity, asthma pts, respiratory
depression, severe renal, hepatic, CV, GI, neurologic, or pulmonary disease,
Pregnancy/ Lactation (neonatal opiod withdrawal), Alcoholics
Warning: Opioid Abuse, fatal overdose in children.
Drug Interactions: Many! CYP issues, other depressants
Note: CYP2D6 poor metabolizers may not achieve adequate analgesia vs.
Ultra-rapid metabolizers (see Module 1 lecture) – incr. toxicity (e.g., resp.
depr/ death) due to rapid conversion (life-threatening amts of morphine)
Antitussives: Non-Opioid
Benzonatate
Benzonatate (Tessalon Perles)
Indication: dry, hacking, nonproductive cough
interfering with rest & sleep
Pharmacokinetics: onset 15-20 min,
duration 3-8 h
Antitussives: Non-Opioid
Benzonatate
Pharmacodynamics: anesthetizes stretch
receptors in respiratory passages, lungs, pleura
(responsible for cough reflex)
S/E: drowsiness, chilly sensation, HA, GI upset,
constipation, burning sensation in eyes
Toxicity: Restlessness, tremors, seizures and
unconsciousness, profound CNS depression and death can
follow.
Take only as prescribed. Keep away from children!
Contraindication: Hypersensitivity to tetracaine-
type topical anesthesia (bronchospasm)
Antitussives: Non-Opioid
Benzonatate (cont)
Drug
Interactions
CNS depressants
ETOH
Rx Principles
do not suppress
productive cough
determine cause of
cough
do not operate car or
machinery
Antitussives: Non-Opioid
Dextromethorphan
Pharmacodynamics: Suppresses cough
reflex by direct action of the cough center in the
medulla.
Pharmacokinetics: action begins within 15-
30 minutes
Almost equal in it’s antitussive potency to codeine,
but with little or no CNS depression. Also, fewer GI
problems.
Antitussives: Non-Opioid
Dextromethorphan
Contraindications
do not use in patient receiving MAO inhibitors within the
preceding 2 weeks because of concomitant use can
cause decreased BP, coma, death
Use with caution with asthma & other respiratory
problems - drug will immobilize secretions
Syrup, tablets, & lozenges not recommended for children
under 2 yo.
Pregnancy C category
Mucolytic Agents

Acetylcysteine (Mucomyst, mucosil)

Indication
abnormally viscous mucous secretions with acute &
chronic bronchopulmonary disease.
MOA
works directly on mucus to reduce thickness & make
secretions less tenacious. Alters metabolism of
acetaminophen to decrease injury to the liver in
overdose
Mucolytic Agents

Pharmacokinetics
absorbed GI; metabolism liver
MOA
splits disulfide linkage of mucoproteins; reduces
viscosity, facilitates removal of secretions - liquefies
secretions
restores hepatic concentration of glutathione necessary
for inactivation of hepatotoxic acetaminophen
metabolite
Mucolytic Agents

S/E: bronchospasms, stomatitis, rhinorrhea, N/V,

Caution: bronchial asthma, elderly, debilitated
Can cause bronchospasms

Patient education: Disguise odor of rotten eggs if

given PO by mixing w/ 4 ounces of iced soft drink or juice &
give w/ a straw
The
End