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CHAPTER 72 DRUGS FOR ALLERGIC RHINITIS, COUGH, AND COLDS

I. DRUGS FOR ALLERGIC RHINITIS


- an inflammatory disorder that affects the upper airway, lower airway,
and eyes
- symptoms are sneezing, rhinorrhea (runny nose), pruritus (itching)
and nasal congestion
(caused by dilation of nasal blood vessels)

Forms: seasonal – also known as hay fever or rose fever


- occurs in the spring and fall in reaction to outdoor allergens,
including fungi and
pollens from weeds, grasses, and trees

perennial – (nonseasonal) triggered by indoor allergens, especially


the house dust mite and pet
dander

A. ANTIHISTAMINES
1. Oral – first line drugs for allergic rhinitis
- can relieve sneezing, rhinorrhea, and nasal itching
- do not reduce nasal congestion
- no value against the common cold
- most effective if taken prophylactically, even when symptoms are
absent
- sedation is the most common adverse effect
- anticholinergic effects (dry mouth, constipation, urinary
hesitancy) may occur

What is the role of antihistamines in the treatment of the common cold?

What is the role of antihistamines in the treatment of allergic rhinitis?

2. Azelastine (trade name: Astelin) Nasal Spray


- only antihistamine available for intranasal use
- dispensed in a metered spray device
- usual dosage is two sprays in each nostril twice daily
- bitter taste in the mouth is the most common side effect

3. OTC – Benadryl, Chlor-Trimenton


- sedation is a problem with these agents
- Claritin, Claritin D now OTC – less sedating
- prescription = Clarinex, Zyrtec, Allegra

B. INTRANASAL GLUCOCORTICOIDS
- Flonase, Beconase, Nasonex, Nasolide
- most effective drugs for treating seasonal and perennial rhinitis
- over 90% of patients respond
- because of their anti-inflammatory actions, can prevent or suppress all of
the major symptoms of
allergic rhinitis (congestion, rhinorrhea, sneezing, nasal itching, and
erythema)
- now considered a first-line therapy drug
- administered using a metered spray device
- for seasonal allergic rhinitis - - maximal effects may require a week
or more to develop
- for perennial rhinitis - - maximal responses may take 2 – 3 weeks to
develop
- if nasal passages are blocked, they should be cleared with a
topical decongestant
prior to glucocorticoid administration
Adverse Effects: generally mild, include drying of the nasal mucosa
and burning or itching sensation
- caused by the vehicle employed for administration and
not by the steroids
themselves
- aqueous vehicles are much less irritating than
non-aqueous

C. INTRANASAL CROMOLYN SODIUM (TRADE NAME: NASALCROM)


- used to both prevent and treat allergic rhinitis
- very safe and effective
- reduces symptoms by suppressing release of histamine and other
inflammatory mediators from mast
cells
- most effective when taken prior to onset of symptoms
- beneficial effects may take a week or two to develop
- administered with a metered spray device
- if nasal congestion is present, a topical decongestant should be
used prior to administering
cromolyn

What are the principle drugs used to treat allergic rhinitis?

D. SYMPATHOMIMETICS (DECONGESTANTS)
- phenylephrine
- reduces nasal congestion by stimulating alpha1-adrenergic receptors on
nasal blood vessels, causing
vasoconstriction, in turn causing shrinkage of swollen membranes
followed by nasal drainage
- topical administration vasoconstriction is both rapid and intense
- oral administration responses are delayed, moderate and
prolonged
- only relieves stuffiness in allergic rhinitis patients
- do not reduce rhinorrhea, sneezing or itching

Adverse Effects:
rebound congestion – develops when topical agents are used more
than a few days
- with prolonged use, the effects of each application wears off
and congestion becomes
progressively more severe
- to overcome this condition, the patient must use
progressively larger and
more frequent doses
- to break this cycle of escalating congestion and
increased drug use, abrupt
decongestant withdrawal will work but is
extremely uncomfortable
- less drastic approach is to discontinue drug use in one
nostril at a time
- can be minimized by limiting use of topical agents to 3 – 5
days

CNS Stimulation – most common


- symptoms include restlessness, irritability, anxiety, and
insomnia

Cardiovascular Effects – for individuals with HTN or coronary artery


disease, widespread
vasoconstriction can be hazardous
- generalized vasoconstriction is most likely with oral agents

Hemorrhagic Stroke – phenylpropanolamine was removed from the


market because it was
shown to cause subarachnoid and intracerebral hemorrhage in
women (but not in men)
- unknown if other alpha agonists (phenylephrine, ephedrine,
pseudoephrine) also pose
a risk of hemorrhagic stroke

Abuse – by causing CNS stimulation, can produce subjective effects


similar to those of
amphetamine, subject to abuse
- employed as decongestants, abuse is most common with
pseudoephedrine and
ephedrine (sold as Sudafed, for example)
- although these agents are available without
prescription and are not regulated
under the Controlled Substances Act, pharmacies
are beginning to
keep them behind the counter so as to hamper
inappropriate use

II. DRUGS FOR COUGH


- cough is often beneficial, serving to remove foreign matter and excess
secretions from the bronchial
tree
- productive cough is characteristic of chronic lung disease (emphysema,
asthma, bronchitis) and
should not be suppressed
- not all cough is useful, frequently serves only to deprive us of comfort or
sleep

A. ANTITUSSIVES
- drugs that suppress cough

1. Opioid Antitussives – codeine and hydrocodone


- act in the CNS to elevate cough threshold
- hydrocodone is somewhat more potent than codeine and carries a
greater liability for abuse

a. Codeine – most effective cough suppressant


- active orally and can decrease both the frequency and
intensity of cough
- doses are low, about one-tenth those needed to relieve pain
- risk of physical dependence is small
- can suppress respiration
- in the event of overdose, respiratory depression may
prove fatal
- Narcan can be administrated to reverse overdose
effects

B. NONOPIOID ANTITUSSIVES
1. Dextromethorphan – most effective nonopioid cough medicine
- acts in the CNS
- although a derivative of the opioids, it does not produce euphoria
or physical dependence and
lacks any potential for abuse
- does not depress respiration

2. Others –
Diphenhydramine – mechanism of antitussive action is unclear
- has sedative and anticholinergic properties
- cough suppression is achieved only at doses that
produces prominent
sedation

Benzonatate (tessalon perles) – structural analog of a local


anesthetic
- dispensed in tiny yellow capsules which should be swallowed
intact, since chewing
will anesthetize the mouth and pharynx

What are the most frequently used drugs for cough suppression?

What is the most effective nonopiod cough suppressant available?


C. EXPECTORANTS AND MUCOLYTICS
1. Expectorants – a drug that renders cough more productive by stimulating
the flow of respiratory tract
secretions
- in almost all cases, efficacy is doubtful
- guaifenesin (glyceryl guaiacolate) may be an exception to
this rule

2. Mucolytics – a drug that reacts directly with mucus to make it more


watery
- this action helps make cough more productive
- administered by in halation
- can cause bronchospasm
- because of its sulfur content, mucomyst has the additional
drawback of smelling like
rotten eggs
- mucinex is a new drug OTC that is administered orally on a dosing
schedule of Q12

III. COLD REMEDIES: COMBINATION PREPARATIONS


- acute upper respiratory infection of viral origin
- symptoms are rhinorrhea, nasal congestion, cough, sneezing, sore throat,
hoarseness, headache,
malaise, and myalgia; fever is common in children but rare in adults
- no cure for the cold
- because colds are caused by viruses, there is no justification for the
routine use of
antibacterial drugs
- combination cold remedies should be reserved for patients with multiple
symptoms
- combination chosen should contain only those agents that are
appropriate for the symptoms to
be treated
- combination cold remedies frequently contain two or more of the
following:
• nasal decongestant
• antitussive
• analgesic
• antihistamine – included to suppress secretion of mucus
• caffeine – added to offset sedative effects of antihistamine
- brand-name product can be reformulated and the sold under the same
name
- without carefully reading the label, the consumer has no assurance
that the brand name
product purchased this year contains the same amounts of the
same drugs that were
present in last year’s version of that combination product