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 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. 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

Phenylephrine HCL Pseudoephedrine Neo-Synephrine®Decofed® Brand Name For Symptomatically relief of nasal and nasopharyngeal mucosal congestion and relief of redness of the eye due to irritation. Its symptomatically relief of nasal congestion due to common cold, upper respiratory allergies and it promotes nasal or sinus drainage. Indication CNS: nervousness, irritability, restlessness, headache. CV: ↑ blood pressure and heart rate is irregular and palpitation. GIT: nausea, vomiting. Neuromuscular and skeletal: weakness, tremor. 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. Side effect

Nasal decongestant (therapy should not exceed 3continuous day): 2-6 years: install 3 drops every 2-4 hours of 0.125% solution as needed.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%Children > 12yrs and adult: install 1-2 sprays or 1-2 drops every 4 hrs of 0.25% to 0.5% 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 Dosage form ___ MAOI may increase blood pressure. Sympathomimetic may increase toxicity it can decrease effect of methyldopa, reserpine. Drug interaction

In elderly. hyperthyroidism. hyperthyroidism. bradycardia. bradycardia. partial heart blocker. partial heart blocker._____Caution HypersensitivityHypertensionVentricular tachycardia tachycardia____Contraindication

Topical Nasal Decongestant: Include:sprays,drops,inhalers

1- sprays: Its advantages: Have fast onset of action.Have fast onset of action. Cover large surface area.Cover large surface area. Simple to use.Simple to use. Inexpensive.Inexpensive. Its disadvantage: Imprecise dosageImprecise dosage Tendency for tip the bottle to become clogged.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. –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).

Ipratropium Bromide (Antimuscarinic) Ephederdrine HCL Atrovent®ephedrine® Brand Name Rhinorrhoea associated with allergic and non allergic rhinitis. Nasal Decongestant Indication Apply 42 microgram as 2 spray into each nostril 2-3 times daily. Instill 1-2 drops into each nostril up to 3 or 4 times daily. Dose

Nasal dryness. Irritation. Irritation.Nausea. Headache. Headache. Antimuscarinic affect: Antimuscarinic affect: -GIT disturbance. -Palpitation. Urinary retention Avoid excessive or prolonged used. Side effect Avoid spraying near eyes. Used with: -Myasthenia Gravis. -Narrow angle glaucoma. Benign prostatic hyperplasia. In infant under three months. caution

Patient with hypersensitivity to Patient with hypersensitivity to  Ipratropium  Soya lecithin or related food products.  Atropine Hypersensitivity to ephedrine. Cardiac arrhythmias. Angle-closure glaucoma. Angle-closure glaucoma.Contraindications Increase toxicity with anticholinergic or drug with anticholinergic properties Increase effect with: - Sympathomimetic agent. - Theophylline. - Theophylline. - Cardiac glycoside. - Cardiac glycoside. - Anesthetic. - Anesthetic. Decrease effect with: -Alpha and Beta adrenergic blockers. -Alpha and Beta adrenergic blockers. Drug interaction

Solution for nubulization 0.02%. Solution for nubulization 0.02%. Solution for oral inhalation 18mcg/actuation. Solution for oral inhalation 18mcg/actuation. Solution for intranasal spray 0.03% or 0.06%. Solution for intranasal spray 0.03% or 0.06%. Nasal drops: ephedrine HCL 0.5%.Nasal drops: ephedrine HCL 0.5%. Dosage form Dosage form

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