COUGH AND COLD
PREPARATIONS





ANTIHISTAMINE
Diphenhydramine
DECONGESTANTS
MUCOLYTICS
Acetylcysteine
EXPECTORANTS
Guaifenesin
COUGH SUPPRESSANTS
Codeine
DM (dextromethorphan)
Global Strategy for the Diagnosis,
Management, and Prevention of
Chronic Obstructive Pulmonary Disease
NHLBI/WHO Global Initiative for Chronic
Obstructive Lung Disease (GOLD)
Workshop Summary 2008
 Mucolytic (mucokinetic, mucoregulator)
agents. (ambroxol, erdosteine,
carbocysteine, iodinated glycerol): Although
a few patients with viscous sputum may
benefit from mucolytics (124, 125), the
overall benefits seem to be very small.
Therefore, the widespread use of these
agents cannot be recommended on the
basis of the present evidence (Evidence D).

There is no evidence to support the use of heliox, DNase or
mucolytics for the treatment of acute asthma in childhood.
British Guideline
on the Management of Asthma, 2008

UK, Feb 2009
Table 2
Overview of the Evidence for Cold Therapies in Children
Therapy
Study findings
Cough (Cochrane review [seven studies])5; one RCT10
Antihistamines
Two studies: no benefit
Antihistamine/decongestant
Two studies: no benefit
combination
Codeine plus guaifenesin (Robitussin
One study: no benefit
AC)
Dextromethorphan (Delsym)
Two studies: no benefit
Dextromethorphan plus guaifenesin
One study: no benefit
(Robitussin DM)
Dextromethorphan plus salbutamol*
One study: no benefit
Mucolytic (e.g., Letosteine*)
One study: benefit
Other combinations
One study: no benefit
Congestion and rhinorrhea (Cochrane reviews [four studies]6)
Antihistamines
Two studies (one using astemizole†):
benefit
Antihistamine/decongestant
Two studies: no benefit
combination
Decongestants
No studies
2007 American Academy of Family
Physicians.
Antihistamines
Drugs that directly
compete with histamine for
specific receptor sites

Two histamine receptors
 H1 (histamine1)
 H2 (histamine2)
H1
histamine receptor- found
on smooth muscle,
endothelium, and central
nervous system tissue; causes
vasodilation,
bronchoconstriction, smooth
muscle activation, and
separation of endothelia cellss
(responsible for hives), and pain
and itching due to insect stings
H1 antagonists are
commonly referred to as
antihistamines
 Antihistamines have
several properties
 Antihistaminic
 Anticholinergic
 Sedative
Antihistamines: Indications
Management of:
 Nasal allergies
 Seasonal or perennial allergic rhinitis
(hay fever)
 Allergic reactions
 Motion sickness
 Histamine-mediated disorders
 Allergic rhinitis (hay fever, mould and dust allergies)
 Anaphylaxis
 Angioneurotic edema
 Drug fevers
 Insect bite reactions
 Urticaria (itching)
ACCP Cough guideline


Patients with acute cough (as well as postnasal drip [PND]
and throat clearing) associated with the common cold can be
treated with a first-generation antihistamine/decongestant
(A/D) preparation (brompheniramine and sustained-release
pseudoephedrine). Naproxen can also be administered to
help decrease cough in this setting. Level of evidence, fair;
benefit, substantial; grade of recommendation, A
In patients with the common cold, newer generation
nonsedating antihistamines are ineffective for reducing
cough and should not be used. Level of evidence, fair;
benefit, none; grade of recommendation, D
Pratter MR. Cough and the common
cold: ACCP evidence-based clinical
practice guidelines. Chest 2006
Jan;129(1 Suppl):72S-4S.
Antihistamines
Ex: Diphenhydramine, chlorphenamine, brompheniramine
MOA: H1 blocker; competes with receptor
sites in resp. tract, GI, blood vessels
Adv eff:


CNS drowsiness, headache, fatigue,
nervousness, dizziness
Anticholinergic (drying) effects, most common




Dry mouth
Difficulty urinating
Constipation
Changes in vision
 Arrhythmia, hallucinations, heart block, paradoxic excitability,
respiratory depression, sedation, tachycardia,
 GIT: appetite increase, weight gain,
diarrhea, n/v
 Arthralgia, pharyngitis
Antihistamines:
Contraindicated in the presence of acute
asthma attacks and lower respiratory
diseases
 Use with caution in increased intraocular
pressure, cardiac or renal disease,
hypertension, asthma, COPD, peptic ulcer
disease, BPH, or pregnancy

Nonsedating/Peripherally Acting
Antihistamines
Developed to eliminate unwanted side
effects, mainly sedation
 Work peripherally to block the actions of
histamine; thus, fewer CNS side effects
 Longer duration of action (increases
compliance)
 Examples: cetirizine (virlix),
fexofenadine(allegra)

ACCP Evidence-based Clinical
Practice Guidelines,
1.
In patients with the common cold, newer
generation nonsedating antihistamines are
ineffective for reducing cough and should not be
used. Level of evidence, fair; benefit, none; grade
of recommendation, D
Pratter MR. Cough and the common
cold: ACCP evidence-based clinical
practice guidelines. Chest 2006
Jan;129(1 Suppl):72S-4S.
Oral Decongestants





Prolonged decongestant
effects,
but delayed onset
Effect less potent than
topical
No rebound congestion
MOA: Exclusively
adrenergics
Example:
pseudoephedrine,
Sinutab, Dristan, Tylenol
cold, Sudafed

Adverse effect:
agitation, anorexia,
dysrhythmia,
dystonic reactions,
headache,
hypertension,
irritability, nausea,
palpitations, seizure,
sleeplessness,
tachycardia,
vomiting

Phenylpropanolamine has
been associated with an
increased risk of
hemorrhagic stroke
(bleeding into the brain or
into tissue surrounding the
brain) in women. Men may
also be at risk. Although
the risk of hemorrhagic
stroke is low, the U.S.
Food and Drug
Administration (FDA)
recommends restricted
use of
phenylpropanolamine.
Topical Nasal Decongestants
MOA:
Adrenergics
 Constrict small blood vessels that supply
URI structures
 As a result these tissues shrink, and nasal secretions in
the swollen mucous membranes are better able to drain
 Topical adrenergics
 Prompt onset
 Potent
 Sustained use over several days causes rebound
congestion, making the condition worse

COMPOSITION:
Each 1 mL of solution contains:
Phenylephrine HCl
5 mg
Pheniramine Maleate
2 mg
Nasal Decongestants:
Decongestants may cause
hypertension, palpitations, and CNS
stimulation
 Repeated use of nasal decongestants
causes a decreased sensitivity to their
vasoconstrictor effect and a rebound
phenomenon with increased nasal
congestion and discharge.
 Clients on medication therapy for
hypertension should check with their
physician before taking OTC
decongestants

Topical Nasal
Decongestants (cont’d)

Intranasal steroids
 beclomethasone dipropionate
 flunisolide
 fluticasone
MUCOLYTICS
Mucolytics
ACETYLCYSTEINE
MOA: free sulfhydryl grp opens up
disulfide bonds in mucoproteins
= ↓ viscosity
Adv rxns: GI n/v; unpleasant odor
CNS: drowsiness, chills
Resp: bronchospasm, rhinorrhea,
hemoptysis
local irritation, clamminess, rash
Dose: 1 sachet through inh.
Mucolytic
Ambroxol


MOA: breakdown of acid mucopolysaccharide fibers;
stimulates synthesis and release of surfactant by type II
pneumocytes; stimulates the ciliary activity thereby
improving mucokinesis (transport of mucous),
 Ambroxol is a metabolite of bromhexine
Adv effects: allergic responses such as skin eruption,
urticaria or engioneurotic edema may occur. While used for a
long time, epigastric pain, nausea and dizziness may occur.
Expectorants:
Reflex stimulation
 Agent causes irritation of the GI tract
 Loosening and thinning of respiratory tract
secretions occur in response to this irritation
 Example: guaifenesin
Direct stimulation
 The secretory glands are stimulated directly to
increase their production of respiratory tract fluids
 Examples: iodine-containing products such as
iodinated glycerol and potassium iodide
COUGH AND COLD PREPARATIONS
Expectorants
GUAIFENESIN
MOA: stimulates resp tract secretions
= ↑ secretions ↓ viscosity
Adv rxns: GI n/v, stomach pains
CNS drowsiness, headaches
Rashes
Dose:100 mg q 4-6
COUGH AND COLD PREPARATIONS
ANTITUSSIVES: OPIOIDS
CODEINE
MOA:: central; depression of medullary center
binds to opiate receptors in the CNS,
= altered perception & response to pain
Analgesic / Narcotic / Antitussive
Adv effects
CNS: drowsiness, dizziness, lightheadedness, malaise, headache,
restlessness  CNS depression
Resp: shortness of breath, dyspnea
CVS: tachycardia or bradycardia, hypotension
GIT: anorexia, nausea, vomiting
Hepatic: altered liver enzymes (ALT, AST)
gut: decreased iromatopm. Iretera; spasm
Derma: rash, urticaria, burning at IV site
Dose: 30 mg q 6-8h; SR 60 mg BID max 120 mg/day
COUGH AND COLD DRUGS
ANTITUSSIVES
DEXTROMETHORPHAN (DM)
MOA: central: depresses medullary center but
lacking narcotic properties exc in overdose
• Suppress the cough reflex by numbing the
stretch receptors in the respiratory tract and
preventing the cough reflex from being
stimulated
Adv reactions
CNS: drowsiness, dizziness, coma
Resp depression
GIT: n/v, constipation, abdominal
discomfort
Dose: 10-20mg q 4 or 30 mg q 6-8
OTC Restrictions for cough
and cold preparations
Medicine and Healthcare products Regulatory Agency in the UK
has banned the sale of over the counter cough and cold medicines
for babies and young children under the age of 2 as a precautionary
measure against accidental overdose because of an increase in
reports of adverse reactions linked to overdose.
 The cough and cold medicines which will no longer be licensed for
children under the age of 2 years, contain the ingredients:





brompheniramine, chlorphenamine & diphenhydramine (antihistamines);
dextromethorphan and pholcodine (antitussives);
guaifenesin and ipecacuanha (expectorants);
phenylephrine, pseudoephedrine, ephedrine, oxymetazoline and xylometazoline
(decongestants).
Royal Pharm Society Great Brit, Mar 2009
OTC cough and cold
restrictions



Health Canada has advised the public that certain over-the-counter cough
and cold medicines should not be used in children under 6 years
of age, following a review of additional data. The Agency also says that
cough and cold medicines marketed for use in children will require
enhanced labelling and packaging and that it is working with
manufacturers to revise the labelling of these products.
New Zealand(2). In December 2007, the Medicines Adverse Reactions
Committee (MARC) reviewed the safety and efficacy of cough and cold
medicines in children and recommended that these products should be
contraindicated in children under two years of age, based on limited
evidence for efficacy in this age group, an absence of evidence-based
dosing, and evidence of significant toxicity in overdose.
The affected products are those containing bromhexine, brompheniramine,
chlorpheniramine, dextromethorphan, diphenhydramine, doxylamine,
guaifenesin, ipecacuanha, oxymetazoline, phenylephrine, pholcodine,
promethazine, pseudoephedrine, triprolidine and xylometazoline.
No.2, 2009
COUGH AND COLD
PREPARATIONS

COMBINATION PREPARATIONS
Colvan: DM + Guaifenesin + Chlorpheniramine +
paracetamol
Dynatussin DM + Guaifenesin + Phenylpropanolamine
+ Na citrate
Tuseran DM + phenylpropanolamine + guiafenesin
Eurocof Guaiafenesin + chlorpheniramine + Na citrate
ACCP cough guideline

In patients with cough and acute upper respiratory tract
infection (URTI), because symptoms, signs, and even sinus
imaging abnormalities may be indistinguishable from acute
bacterial sinusitis, the diagnosis of bacterial sinusitis should
not be made during the first week of symptoms. (Clinical
judgment is required to decide whether to institute antibiotic
therapy.) Level of evidence, fair; benefit, none; grade of
recommendation, D
Pratter MR. Cough and the common
cold: ACCP evidence-based clinical
practice guidelines. Chest 2006
Jan;129(1 Suppl):72S-4S.
Management of Stable COPD
Other Pharmacologic Treatments
 Antibiotics: Only used to treat infectious
exacerbations of COPD
 Antioxidant agents: No effect of nacetylcysteine on frequency of
exacerbations, except in patients not treated
with inhaled glucocorticosteroids
 Mucolytic agents, Antitussives,
Vasodilators: Not recommended in stable
COPD
32
The art of medicine consists of amusing the patient while nature
cures the disease.
- Voltaire