NASAL PREPARATION ( NASAL
DECONGESTANT)
WHAT IS NASAL CONGESTION AND ITS PROBLEMS
Nasal congestion is the blockage of the nasal passages usually due to membranes lining the nose
becoming swollen from inflamed blood vessels
Nasal congestion has many causes and can range from a mild annoyance to a life-threatening condition.
Most people prefer to breathe through the nose (historically referred to as "obligate nasal
breathers").Nasal congestion in an infant in the first few months of life can interfere with breastfeeding
and cause life-threatening respiratory distress; in older children and adolescents it is often just an
annoyance but can cause other difficulties.
Nasal congestion can interfere with the hearing and speech. Significant congestion may interfere with
sleep, cause snoring, and can be associated with sleep apnea.
WHAT IS NASAL CONGESTION???
WHAT ARE NASAL DECONGESTANT???
A decongestant, or nasal decongestant, is a type of pharmaceutical drug that is used to relieve nasal
congestion in the upper respiratory tract. The active ingredient in most decongestant is either
pseudoephedrine or phenylephrine
Nasal decongestants are vasoconstrictive drugs extremely useful as nonprescription medication. Both
oral and tropical dosage forms are often chosen as therapy in the common cold
ADVANTAGES AND DISADVANTAGES OF DECONGESTANTS
ADVANTAGES DISADVATAGES
Drug degradation that is observed in GIT is absent Rebound congestion
Hepatic first pass metabolism is absent Aggravated sinusitis
Rapid drug absorption quick onset of action Short term stinging
Large bioavailability Irritation and tachyphylaxis
Ease of administration, non-invasive Sinus dryness and permanent damage can occur
Lower dose reduced side effects Rhinitis medicamentosa
Self administration Regular nose bleed
Should not be used for childrens as it can cause
loss of conciosness, convulsion and death
DOSAGE FORMS AVAILABLE
Nasal drops
Nasal sprays
Nasal gels
Nasal powders
MECHANISM OF DRUG ABSORPTION
The first mechanism involves an aqueous route of transport, which is also known as the paracellular
route. This route is slow and passive. There is an inverse log-log correlation between intranasal
absorption and the molecular weight of water-soluble compounds. Poor bioavailability was observed for
drug with a molecular weight greater than 1000 Daltons.
The second mechanism involves transport through a lipoidal route is also known as the transcellular
process and is responsible for the transport of lipophilic drugs that show a rate dependency on their
lipophilicity
Drug also cross cell membranes by an active transport route via carrier-mediated means or transport
through the opening of tight junctions. For examples, chitosan, a natural biopolymer from shellfish,
opens tight junctions between epithelial cells to facilitate drug transport.
MECHANISM OF ACTION
Nasal decongestants belong to the pharmacological class of sypathomimetic 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 decongestants
• Internally or systemic decongestant (e.g pseudoephedrine, phenylpropanolamine and phenylephrine)
• Topical decongestant: drops or sprays (e.g xylometazoline, phenylephrine, oxymetazoline, naphazoline)
• Inhalers: (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 EFFECTS OF SYSTEMIC DECONGESTANT
CNS effect: Nervousness, restlessness, headach and insomnia
CV effect: increase blood pressure and increase heart rate
Urinary sphincter constriction
Examples
Psedoephedrine
Phenylpropanolamine(PPA)
Phenylephrine
TOPICAL NASAL DECONGESTANT
Sprays Drops
ADVANTAGES ADVANTAGES
Have fast onset of action It is preffered for a small children
Cover large surface area DISADVANTAGES
Simple to use High risk of contamination
Inexpensive Limited coverage into nasal mucosa easy passage
into larynx
DISADVANTAGES
Imprecise dosage
Tendency for tip the bottle to become clogged
Inhalers Example of topical decongestant
ADVANTAGES Ephedrine HCL
Easy to be handle and carry Xylometazoline HCL
DISADVANTAGES Oxymetazoline HCL
Unobstructed airway and sufficient air flow Ipratropium bromide(antimuscarinic)
needed to distribute drug to nasal mucosa
HOW TO PREPARE NASAL DROPS AND NASAL SPRAYS?
Emulsions Suspensions
Wet gum method All the suspension are prepared by same
method with differences in some ingredients
Dry gum method
Solid particles are powdered in mortar
Bottle’s method
Little vehicle is added to make paste by grinding
Auxiliary method
them well
Vehicle is added to make up the final volume
