nasal decongestant

Nasal Decongestant

Done by:Hibah AL-Abri

Eyman AL-HarbiJawaher AL-Amoudi

Nasal DecongestantNasal Decongestant::

Nasal decongestants are Nasal decongestants are vasoconstrictive drugs extremely vasoconstrictive drugs extremely useful as nonprescription medication. useful as nonprescription medication. Both oral and topical dosage forms Both oral and topical dosage forms are often chosen as therapy in the are often chosen as therapy in the common cold.common cold.

Mechanism of actionMechanism of action::

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

PseudoephedrinePseudoephedrinePhenylephrine Phenylephrine HCLHCL

Brand Brand NameName

Decofed® Decofed® Neo-Synephrine®Neo-Synephrine®

IndicationIndication

Its symptomatically relief Its symptomatically relief of nasal congestion due to of nasal congestion due to

common cold, upper common cold, upper respiratory allergies and it respiratory allergies and it

promotes nasal or sinus promotes nasal or sinus drainage.drainage.

For Symptomatically For Symptomatically relief of nasal and relief of nasal and nasopharyngeal nasopharyngeal

mucosal congestion mucosal congestion and relief of redness and relief of redness

of the eye due to of the eye due to

irritation.irritation.

Side effectSide effect

CNS:CNS: nervousness, nervousness, irritability, restlessness, irritability, restlessness, headache and insomnia.headache and insomnia.

CV:CV: ↑blood pressure and ↑blood pressure and heart rate is irregular and heart rate is irregular and palpitation.palpitation.

GITGIT: nausea, vomiting.: nausea, vomiting.

Neuromuscular and Neuromuscular and skeletal:skeletal: weakness, weakness, tremor.tremor.

CNSCNS: nervousness, : nervousness, irritability, irritability, restlessness, restlessness, headache.headache.

CV:CV: ↑blood pressure ↑blood pressure and heart rate is and heart rate is irregular and irregular and palpitation.palpitation.

GITGIT: nausea, : nausea, vomiting.vomiting.

Neuromuscular and Neuromuscular and skeletalskeletal: weakness, : weakness, tremor.tremor.

Dosage form Dosage form

Solution oral drops, Solution oral drops, as HCL: Dimetapp® as HCL: Dimetapp® decongestant infant decongestant infant drops: drops: 7.5mg/0.8ml(15ml)7.5mg/0.8ml(15ml)

Syrup, as HCL: Syrup, as HCL: 30mg/5ml (120ml, 30mg/5ml (120ml, 480ml).480ml).

Tablet, HCL:30mg, Tablet, HCL:30mg, 60mg60mg

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

Drug interaction Drug interaction

MAOI may increase MAOI may increase blood pressure. blood pressure.

Sympathomimetic Sympathomimetic may increase toxicity may increase toxicity it can decrease effect it can decrease effect

of methyldopa, of methyldopa, reserpine.reserpine.

______

CautionCaution

__________

In elderly.In elderly.

hyperthyroidism.hyperthyroidism.

bradycardia.bradycardia.

partial heart partial heart blocker. blocker.

Contraindication Contraindication ________

HypersensitivityHypersensitivity

HypertensionHypertension

VentricularVentricular

tachycardiatachycardia

Topical Nasal DecongestantTopical Nasal Decongestant::

Include: Include:

sprays, sprays,

drops, drops,

inhalersinhalers

11 - -sprayssprays::

Its advantages: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:Its disadvantage:• Imprecise dosageImprecise dosage• Tendency for tip the bottle to become Tendency for tip the bottle to become

clogged.clogged.

22 - -dropsdrops::

It preferred for small children.It preferred for small children.

Its disadvantage:Its disadvantage:– High risk of contamination.High risk of contamination.– Limited coverage into nasal Limited coverage into nasal

mucosa.mucosa.– Easy passage into larynx.Easy passage into larynx.

33 - -inhalerinhaler::

Easy to be handle and carry. Easy to be handle and carry.

Disadvantage:

Unobstructed airway and sufficient air flow needed to

distribute drug to nasal mucosa.

Side effect of topical Side effect of topical decongestantdecongestant::

• 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 Example of topical decongestantdecongestant::

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

Ephederdrine Ephederdrine HCL HCL

Ipratropium Ipratropium Bromide Bromide

(Antimuscarinic)(Antimuscarinic)

Brand NameBrand Name ephedrine® ephedrine® Atrovent® Atrovent®

IndicationIndication

Nasal Nasal Decongestant Decongestant

Rhinorrhoea Rhinorrhoea associated with associated with allergic and non allergic and non allergic rhinitis. allergic rhinitis.

DoseDose

Instill 1-2 drops Instill 1-2 drops into each nostril into each nostril

up to 3 or 4 up to 3 or 4 times daily.times daily.

Apply 42 Apply 42 microgram as 2 microgram as 2 spray into each spray into each nostril 2-3 times nostril 2-3 times

daily.daily.

Side effectSide effect

Avoid excessive or Avoid excessive or prolonged used. prolonged used.

Nasal dryness.Nasal dryness.

Irritation. Irritation.

Nausea.Nausea.

Headache.Headache.

Antimuscarinic Antimuscarinic affect:affect:

-GIT disturbance.-GIT disturbance.

-Palpitation.-Palpitation.

Urinary retentionUrinary retention

cautioncaution

In infant under In infant under three months. three months.

Avoid spraying Avoid spraying near eyes.near eyes.

Used with:Used with:

-Myasthenia -Myasthenia Gravis.Gravis.

-Narrow angle -Narrow angle glaucoma.glaucoma.

Benign prostatic Benign prostatic hyperplasia.hyperplasia.

ContraindicatioContraindications ns

Hypersensitivity to Hypersensitivity to ephedrine.ephedrine.

Cardiac arrhythmias.Cardiac arrhythmias.

Angle-closure Angle-closure glaucoma. glaucoma.

Patient with Patient with hypersensitivity tohypersensitivity to

IpratropiumIpratropiumSoya lecithin Soya lecithin or related food or related food products.products.AtropineAtropine

Drug Drug

interactioninteraction

Increase effect with:Increase effect with:

- Sympathomimetic - Sympathomimetic agent.agent.

- Theophylline.- Theophylline.

- Cardiac glycoside.- Cardiac glycoside.

- Anesthetic.- Anesthetic.

Decrease effect with:Decrease effect with:

-Alpha and Beta -Alpha and Beta adrenergic blockers.adrenergic blockers.

Increase toxicity Increase toxicity with with anticholinergic or anticholinergic or drug with drug with anticholinergic anticholinergic properties properties

Dosage Dosage formform

•Nasal Nasal drops: drops: ephedrine ephedrine HCL 0.5%. HCL 0.5%.

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

Thank Thank you..you..