Nasal Decongestant

Done by:
Ravi J. Shah
 :Nasal Decongestant

Nasal decongestants are

vasoconstrictive drugs extremely useful
as nonprescription medication. Both oral
and topical dosage forms are often
chosen as therapy in the common cold.
 :Mechanism of action

Nasal decongestants belong to the

pharmacological class of sympathomimetic
amines. Decongestant stimulates alpha-
adrenergic agonist, by constriction of blood
vessels, reducing its supply to the nose,
decrease the amount of blood in sinusoid
vessels and decrease mucosal edema.
 :Types of nasal decongestant

• Internally or systemic decongestant: (e.g.

pseudoephedrine, phenylpropanolamine (PPA)
and phenylephrine).
• Topical decongestant: drops or sprays (e.g.
xylometazoline, phenylephrine, oxymetazoline,
naphazoline).
• Inhaler: (1-desoxyephedrine and
propylhexedrine).
 :Systemic nasal decongestant

Mechanism of action:

Potent direct acting alpha-adrenergic

stimulator with weak beta-Adrenergic
activity, causes vasoconstriction of the
arterioles of the nasal mucosa and
conjunctive, activates the dilator muscle of
the pupil to causes contraction, and produce
systemic arterial vasoconstriction.
 Side effect of systemic
:decongestant

• CNS effect: Nervousness, restlessness,

headach and insomnia.
• CV effect: increase blood pressure and
increase heart rate.
• Urinary sphincter constriction
:Examples of systemic decongestant

– Pseudoephedrine
– Phenylpropanolamine (PPA)
– phenylephrine
 OH
OH

NH2
HO NHCH3

CH3

Phenylpropanolamine, Mixed MOA, Phenylephrine, Vasocontriction used

Alpha receptor agonist with local anaesthetic

OH

NHCH3

CH3

pseudoephedrine, act by indirect mechanism

Phenylephrine HCL Pseudoephedrine

Neo-Synephrine® Decofed® Brand Name

For Symptomatically Its symptomatically relief of

relief of nasal and nasal congestion due to
nasopharyngeal mucosal common cold, upper
congestion and relief of respiratory allergies and it
redness of the eye due promotes nasal or sinus Indication
to irritation. drainage.

CNS: nervousness, CNS: nervousness,

irritability, restlessness, irritability, restlessness,
headache. headache and insomnia.
CV: ↑blood pressure and
CV: ↑blood pressure and
heart rate is irregular and
palpitation. heart rate is irregular and
palpitation. Side effect
GIT: nausea, vomiting.
Neuromuscular and GIT: nausea, vomiting.
skeletal: weakness, Neuromuscular and skeletal:
tremor. weakness, tremor.
Nasal decongestant Solution oral drops, as
(therapy should not HCL: Dimetapp®
exceed 3continuous day): decongestant infant
•2-6 years: install 3 drops:
drops every 2-4 hours of 7.5mg/0.8ml(15ml)
0.125% solution as Syrup, as HCL:
needed. 30mg/5ml (120ml,
480ml). Dosage form
•Children > 12yrs and
adult: install 1-2 sprays Tablet, HCL:30mg,
or 1-2 drops every 4 hrs 60mg
of 0.25% to 0.5%

MAOI may increase blood

pressure.
Sympathomimetic may
increase toxicity it can
___ decrease effect of Drug interaction
methyldopa, reserpine.
 In elderly.
hyperthyroidism.
bradycardia. Caution
partial heart
blocker. _____

Hypersensitivity
Hypertension
Ventricular Contraindication
tachycardia ____
 :Topical Nasal Decongestant

Include:

sprays,
drops,
inhalers
 :sprays -1
Its advantages:
• Have fast onset of action.
• Cover large surface area.
• Simple to use.
• Inexpensive.

Its disadvantage:
• Imprecise dosage
• Tendency for tip the bottle to become
clogged.
 :drops -2

It preferred for small children.

Its disadvantage:
– High risk of contamination.
– Limited coverage into nasal mucosa.
– Easy passage into larynx.
 :inhaler -3

Easy to be handle and carry.

 :Disadvantage

Unobstructed airway and sufficient air

flow needed to
.distribute drug to nasal mucosa
 Side effect of topical
:decongestant

• Local irritation.
• Rebound congestion
Note:
the patient must follow the instruction in
label duration & frequency of use, if not
they follow it can cause rebound congestion
well be developed.

– Cause of rebound congestion:

ischemic as result of local vasoconstriction
of the drug or local irritation of the drug.
– How to over come rebound congestion?
Stop topical & switch to the oral nasal
decongestant or intranasal isotonic normal
saline (50%), or intranasal steroids.
:Example of topical decongestant

Ephedrine HCL, Xylometazoline HCL,

Oxymetazoline HCL, Ipratropium
bromide (antimuscarinic).
 N

N
H

R= CH3

Oxymetazoline
H2C

CH3
CH3
H3C

OH CH3
CH3
Xylometazoline
H2C

CH3
CH3
H3C

CH3
 Ipratropium Ephederdrine
Bromide HCL
(Antimuscarinic)
Atrovent® ephedrine® Brand Name

Rhinorrhoea Nasal
associated with Decongestant
allergic and non Indication
allergic rhinitis.

Apply 42 Instill 1-2 drops

microgram as 2 into each nostril
spray into each up to 3 or 4 times Dose
nostril 2-3 times daily.
daily.
 Nasal dryness. Avoid excessive or
Irritation. prolonged used.
Nausea.
Headache.
Antimuscarinic Side effect
affect:
-GIT disturbance.
-Palpitation.
Urinary retention
Avoid spraying near In infant under three
eyes. months.
Used with:
-Myasthenia caution
Gravis.
-Narrow angle
glaucoma.
Benign prostatic
hyperplasia.
 Patient with Hypersensitivity to
hypersensitivity to ephedrine.
Ipratropium Cardiac arrhythmias.
Soya lecithin or Angle-closure Contraindications
related food glaucoma.
products.
Atropine

Increase toxicity Increase effect with:

with anticholinergic - Sympathomimetic
or drug with agent.
anticholinergic - Theophylline.
properties Drug
- Cardiac glycoside. interaction
- Anesthetic.
Decrease effect with:
-Alpha and Beta
adrenergic blockers.
• Solution for •Nasal drops:
nubulization 0.02%. ephedrine HCL
• Solution for oral 0.5%.
inhalation
18mcg/actuation.
• Solution for Dosage
intranasal spray form
0.03% or 0.06%.
Thank
you..