Oxymetazoline
Drug name : Oxymetazoline
Trade name :
Afrin Nasal Spray
Anefrin Nasal Spray
Dristan Nasal Spray
Mucinex Nasal Spray
Nostrilla Nasal Spray
Vicks Sinex Nasal Spray
Classification : Oxymetazoline
Nasal Decongestants
Drugs designed to treat inflammation of the nasal passages, generally the result of an infection
(more often than not the common cold) or an allergy related condition, e.g., hay fever. The
inflammation involves swelling of the mucous membrane that lines the nasal passages and
results in inordinate mucus production. The primary class of nasal decongestants are
vasoconstrictor agents
Dosage Form : Oxymetazoline
Afrin 12 Hour: 0.05% (30 mL) [contains benzalkonium chloride, disodium edta,
polyethylene glycol, propylene glycol]
Afrin Extra Moisturizing: 0.05% (30 mL [DSC])
Afrin Menthol Spray: 0.05% (15 mL)
Afrin Nasal Spray: 0.05% (15 mL)
Afrin Nasal Spray: 0.05% (15 mL, 20 mL, 30 mL) [contains benzalkonium chloride,
disodium edta]
Afrin NoDrip Extra Moisture: 0.05% (15 mL) [contains benzalkonium chloride]
Afrin NoDrip Original: 0.05% (15 mL) [contains benzalkonium chloride]
Afrin NoDrip Sinus: 0.05% (15 mL) [contains benzalkonium chloride, menthol]
Afrin Sinus: 0.05% (15 mL)
Use : Oxymetazoline
Relieving nasal congestion due to the common cold, hay fever, other upper respiratory tract
allergies, or sinus infection. Due to its vasoconstricting properties, oxymetazoline is also used to
treat nose bleeds and eye redness due to minor irritation
Mechanism of action : Oxymetazoline
Oxymetazoline is a sympathomimetic that selectively agonizes 1 and, partially, 2 adrenergic
receptors. Since vascular beds widely express 1 receptors, the action of oxymetazoline results
in vasoconstriction. In addition, the local application of the drug also results in vasoconstriction
due to its action on endothelial postsynaptic 2receptors; systemic application of 2 agonists, in
contrast, causes vasodilation because of centrally-mediated inhibition of sympathetic tone via
presynaptic 2 receptors. Vasoconstriction of vessels results in relief of nasal congestion in two
ways: first, it increases the diameter of the airway lumen; second, it reduces fluid exudation from
postcapillary venules. It can reduce nasal airway resistance (NAR) up to 35.7% and nasal
mucosal blood flow up to 50%.
Drug characteristic : Oxymetazoline
Pharmacology
Stimulates alpha-adrenergic receptors in the arterioles of the nasal mucosa to
produce vasoconstriction
Oxymetazoline is readily absorbed orally. Effects on receptors from
Pharmacokinetics
systemically absorbed oxymetazoline hydrochloride may persist for up to 7
hours after a single dose. The elimination half-life in humans is 58 hours. It
is excreted unchanged both by the kidneys (30%) and in feces (10%).
Onset of Action
Within seconds
Duration of Action
Up to 12 hours
Contraindications
Hypersensitivity to oxymetazoline or any component of the formulation
Adverse fetal or neonatal effects have not been observed following normal
maternal doses of oxymetazoline during the third trimester of pregnancy.
Adverse events have been noted in case reports following large doses or
Pregnancy
extended use. Decongestants are not the preferred agents for the treatment of
Considerations
rhinitis during pregnancy. Short-term (<3 days) use of intranasal
oxymetazoline may be beneficial to some patients although its safety during
pregnancy has not been studied
Although no information exists on the use of oxymetazoline specifically
during breastfeeding, very little should reach the infant through breastmilk
Breastfeeding
because of the local administration and limited absorption into the maternal
bloodstream. It has been recommended over oral systemic decongestants such
as pseudoephedrine during breastfeeding
Safety factor for treatment: Oxymetazoline
Suf xes
Afrin
R/ only
Nasal
Spray
Yes
High alert
No
LASA
Avamis
Spray
Storage
Nasal
15 and 30 degrees C.
Store away from heat,
moisture, and light.
Drug interaction: Oxymetazoline
Drug
Reaction
Management
May diminish the vasoconstricting effect of
Alpha1-Blockers
Alpha1-Agonists. Similarly, Alpha1-Agonists
may antagonize Alpha1-Blocker vasodilation.
Monitor therapy
May enhance the hypertensive effect of
AtoMOXetine
Sympathomimetics.
enhance
the
AtoMOXetine
tachycardic
effect
may
of
Monitor therapy
Sympathomimetics. Monitor therapy
Cannabinoid-Containing
May enhance the tachycardic effect of
Products
Sympathomimetics. Exceptions:Cannabidiol.
Doxofylline
Sympathomimetics
may
enhance
the
adverse/toxic effect of Doxofylline.
Monitor therapy
Monitor therapy
May enhance the hypertensive effect of
Alpha1-Agonists. Ergot Derivatives may
Ergot Derivatives
enhance
the
vasoconstricting
effect
of Avoid combination
Alpha1-Agonists. Exceptions: Ergoloid
Mesylates.
Alpha1-Agonists may decrease the serum
concentration of FentaNYL. Specifically,
FentaNYL
fentanyl nasal spray serum concentrations Monitor therapy
may decrease and onset of effect may be
delayed.
Iobenguane I 123
Sympathomimetics
may
diminish
the
therapeutic effect of Iobenguane I 123.
Avoid combination
Reduce initial doses of
May enhance the hypertensive effect of
Linezolid
Sympathomimetics. Specific dose adjustment
recommendations
are
not
presently
available. Consider therapy modification
sympathomimetic
agents,
and
closely
monitor for enhanced
pressor response, in
patients
linezolid.
receiving
Sympathomimetics
May enhance the adverse/toxic effect of other
Sympathomimetics.
Monitor therapy
May enhance the hypertensive effect of
Tedizolid
Sympathomimetics. Tedizolid may enhance Monitor therapy
the tachycardic effect of Sympathomimetics.
May enhance the vasopressor effect of
Tricyclic Antidepressants
Alpha1-Agonists. Tricyclic Antidepressants
may diminish the vasopressor effect of
Monitor therapy
Alpha1-Agonists.
Rections should be monitoring: Oxymetazoline
Cardiovascular
Very rare (less than 0.01%): Tachycardia, palpitations, increased blood pressure
Gastrointestinal
Very rare (less than 0.01%): Nausea
General
The most commonly reported side effects were discomfort or irritation in the nose, mouth or
throat, and sneezing.
Nervous system
Very rare (less than 0.01%): Insomnia, nervousness, tremor, anxiety, restlessness, irritability,
headache
Ocular
Rare (less than 0.1%): Eye irritation, dryness, discomfort/redness
Respiratory
Rare (less than 0.1%): Discomfort or irritation in the nose, mouth or throat, sneezing
Frequency not reported: Rhinitis medicamentosa (after prolonged or heavy use)
Parameter patients health : Oxymetazoline
Relieve sinus congestion and pressure due to the common cold, hay fever, other upper
respiratory tract allergies, or sinus infection
Toxicity : Oxymetazoline
In most countries, the use of topical nasal decongestants is limited to a maximum of 10
days because of the risk of developing rebound mucosal swelling and rhinitis medicamentosa. To
determine whether topical nasal decongestants can be safely used for 10 days in patients with
chronic inflammation of the nasal mucosa. ouble-blind, randomized, controlled, parallel study.
Thirty-five patients with vasomotor rhinitis selected from our outpatient department. Eighteen
patients received oxymetazoline hydrochloride (0.5 mg/mL) nasal spray containing the
preservative benzalkonium chloride (0.1 mg/mL), and the other 17 were treated
with oxymetazoline nasal spray without benzalkonium chloride. Before and after the treatment,
recordings of the nasal mucosa and minimal cross-sectional area were made with
rhinostereometry and acoustic rhinometry, followed by histamine hydrochloride challenge tests.
Symptoms of nasal stuffiness were estimated on visual analog scales (0-100) in the morning and
the evening, just before the nasal spray was used. No rebound swelling was found after the 10day treatment in the 2 groups with either of the methods or as estimated by symptom scores. In
the group receiving oxymetazolinecontaining benzalkonium chloride, but not in the other group,
the histamine sensitivity was significantly reduced after treatment (P<.001). It is safe to use
topical nasal oxymetazoline with or without benzalkonium chloride for 10 days in patients with
vasomotor rhinitis. However, this study indicates that benzalkonium chloride in nasal
decongestant sprays affects the nasal mucosa also after short-term use.
If accidentally ingested, standard methods to remove unabsorbed drugs should be
considered. There is no specific antidote for oxymetazoline, although its pharmacological effects
may be reversed by adrenergic antagonists such as phentolamine. In the event of a possibly
life-threatening overdose (such as a hypertensive crisis), benzodiazepines should be considered
to decrease the likelihood of seizures and convulsions, as well as reduce anxiety and to lower
blood pressure. In children, oxymetazoline may produce profound central nervous system
depression due to stimulation of central 2 receptors and imidazoline receptors, much
likeclonidine
Patient counseling : Oxymetazoline
Use oxymetazoline solution as directed by your doctor. Check the label on the medicine for
exact dosing instructions.
To use nose drops, gently blow your nose. Lie down and tilt your head back. Breathe through
your mouth. Insert the dropper tip in the nose no more than 1/3 inch. Try not to touch the
dropper tip to the inside of your nose. Place the correct number of drops in your nose.
Continue to lie down with your head tilted back for 2 minutes.
To use a nose spray, gently blow your nose. Do not tilt your head back when using the nose
spray. Place the tip of the spray container into the nose. Using a finger from your other hand,
press against the opposite nostril to close it off. Breathe gently through the open nostril and
squeeze the spray container. If you are using more than 1 spray, wait for 1 to 2 minutes
between sprays. After using the medicine, rinse the tip of the spray unit in hot water and dry
with a clean tissue to prevent contamination.
If you miss a dose of oxymetazoline solution and are using it regularly, use it as soon as
possible. If it is much more than 1 hour since your missed dose, skip the missed dose and go
back to your regular dosing schedule. Do not use 2 doses at once.
Pharmaceutical Care : Oxymetazoline
Do not use oxymetazoline solution for more than 3 days unless advised to do so by your
health care provider. Frequent or long-term use of oxymetazoline solution may cause nasal
congestion to recur or worsen.
Do not share oxymetazoline solution with anyone else; this may cause the infection to
spread.
Diabetes patients - Oxymetazoline solution may affect your blood sugar level. Your doctor
may need to change the amount of diabetes medicine you are taking.
Oxymetazoline solution is not recommended for use in CHILDREN younger than 6 years of
age. Safety and effectiveness in this age group have not been confirmed.
Do NOT use oxymetazoline solution if:
you are allergic to any ingredient in oxymetazoline solution
you are also taking furazolidone or a monoamine oxidase (MAO) inhibitor (eg,
phenelzine)
Reference : Oxymetazoline
1.
"Oxymetazoline: Drug Information Provided by Lexi-Comp: Merck Manual Professional".
Merck.com. Retrieved 2013-04-15.
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oxymetazoline for prevention of epistaxis on nasotracheal intubation". J Clin Anesth 2 (1):
1620. doi:10.1016/0952-8180(90)90043-3. PMID 2310576.
3. Krempl, G.A. & A.D. Noorily (1995). "Use of oxymetazoline in the management of
epistaxis". Ann Otol Rhinol Laryngol 104 (9 Pt 1): 7046. PMID 7661519.
4. "VISINE Original Red Eye Drops | VISINE products". Visine.com. Retrieved 2013-0415.
5. Westfall Thomas C, Westfall David P, "Chapter 6. Neurotransmission: The Autonomic and
Somatic Motor Nervous Systems" (Chapter). Brunton LL, Lazo JS, Parker KL: Goodman &
Gilman's The Pharmacological Basis of Therapeutics.
6. Biaggioni Italo, Robertson David, "Chapter 9. Adrenoceptor Agonists & Sympathomimetic
Drugs" (Chapter). Katzung BG: Basic & Clinical Pharmacology
7. Widdicombe (1997). "Microvascular anatomy of the nose". Allergy 52 (40 Suppl): 711.
8. The Journal of Laryngology & Otology, Volume 100 , Issue 03, pp 285-288
9. Ramey; E Bailen; RF Lockey (2006). "Rhinitis medicamentosa". J Investig Allergol Clin
Immunol 16 (3): 148155.
10. Marple B, Roland P, Benninger M (2004). "Safety review of benzalkonium chloride used as a
preservative in intranasal solutions: an overview of conflicting data and
opinions". Otolaryngol Head Neck Surg 130 (1)
11. Rayburn WF, Anderson JC, Smith CV, Appel LL, Davis SA (1990). "Uterine and fetal
Doppler flow changes from a single dose of a long-acting intranasal decongestant". Obstet
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