Nasal Decongestant

Done by: Hibah AL-Abri Eyman AL-Harbi Jawaher AL-Amoudi

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 alphaadrenergic 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

Pseudoephedrine
Brand Name Decofed Its symptomatically relief of nasal congestion due to common cold, upper respiratory allergies and it promotes nasal or sinus drainage. CNS: nervousness, irritability, restlessness, headache and insomnia. CV: blood pressure and heart rate is irregular and palpitation. GIT: nausea, vomiting. Neuromuscular and skeletal: weakness, tremor.

Phenylephrine HCL
Neo-Synephrine

Indication

For Symptomatically relief of nasal and nasopharyngeal mucosal congestion and relief of redness of the eye due to irritation.
CNS: nervousness, irritability, restlessness, headache. CV: blood pressure and heart rate is irregular and palpitation. GIT: nausea, vomiting. Neuromuscular and skeletal: weakness, tremor.

Side effect

Dosage form

Solution oral drops, as HCL: Dimetapp decongestant infant drops: 7.5mg/0.8ml(15ml) Syrup, as HCL: 30mg/5ml (120ml, 480ml). Tablet, HCL:30mg, 60mg

Nasal decongestant (therapy should not exceed 3continuous day): 2-6 years: install 3 drops every 2-4 hours of 0.125% solution as needed. Children > 12yrs and adult: install 1-2 sprays or 1-2 drops every 4 hrs of 0.25% to 0.5%

Drug interaction

MAOI may increase blood pressure. Sympathomimetic may increase toxicity it can decrease effect of methyldopa, reserpine.

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Caution

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In elderly. hyperthyroidism. bradycardia. partial heart blocker.

Contraindication

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Hypersensitivity Hypertension Ventricular tachycardia

Topical Nasal Decongestant: Include:

sprays, drops, inhalers

1- sprays:
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.

2- drops:
It preferred for small children. Its disadvantage:
High risk of contamination. Limited coverage into nasal mucosa. Easy passage into larynx.

3- inhaler: 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. Stop topical & switch to the oral nasal decongestant or intranasal isotonic normal saline (50%), or intranasal steroids.
How to over come rebound congestion?

Example of topical decongestant:

Ephedrine HCL, Xylometazoline HCL, Oxymetazoline HCL, Ipratropium bromide (antimuscarinic).

Ephederdrine HCL Brand Name ephedrine Nasal Decongestant

Ipratropium Bromide (Antimuscarinic) Atrovent Rhinorrhoea associated with allergic and non allergic rhinitis. Apply 42 microgram as 2 spray into each nostril 2-3 times daily.

Indication

Dose

Instill 1-2 drops into each nostril up to 3 or 4 times daily.

Avoid excessive or prolonged used.

Side effect

Nasal dryness. Irritation. Nausea. Headache. Antimuscarinic affect: -GIT disturbance. -Palpitation. Urinary retention

caution

In infant under three Avoid spraying near months. eyes. Used with: -Myasthenia Gravis. -Narrow angle glaucoma. Benign prostatic hyperplasia.

Contraindications

Hypersensitivity to ephedrine. Cardiac arrhythmias. Angle-closure glaucoma.

Patient with hypersensitivity to Ipratropium Soya lecithin or related food products. Atropine Increase toxicity with anticholinergic or drug with anticholinergic properties

Drug interaction

Increase effect with: - Sympathomimetic agent. - Theophylline. - Cardiac glycoside. - Anesthetic. Decrease effect with: -Alpha and Beta adrenergic blockers.

Nasal drops: ephedrine HCL 0.5%.

Dosage form

Solution for nubulization 0.02%. Solution for oral inhalation 18mcg/actuation. Solution for intranasal spray 0.03% or 0.06%.

Thank you..