Adult: For the symptomatic relief of congestion associated with upper respiratory allergies, hay fever, common cold, sinusitis, and otitis media: As 0.05% nasal spray: Usual dose: 1-2 sprays into each nostril 2-3 times daily as necessary. Max treatment duration: 5-7 consecutive days. Alternatively, 2-3 sprays into each nostril bid for up to 3 days. Max: 2 doses per 24 hours. As 0.05% nasal drops: Usual dose: Instill 1-2 drops into each nostril 2-3 times daily. Max treatment duration: 5-7 consecutive days. Child: As 0.01% nasal drops: ≤4 weeks Instill 1 drop into each nostril 2-3 times daily; 5 weeks to 1 year Instill 1-2 drops into each nostril 2-3 times daily. Max treatment duration: 5-7 consecutive days. As 0.025% nasal drops: 1-6 years Usual dose: Instill 1-2 drops into each nostril 2-3 times daily. Max treatment duration: 5-7 consecutive days. As 0.05% nasal drops: >6 years Same as adult dose. As 0.05% nasal spray: >12 years Usual dose: 1-2 sprays into each nostril 2-3 times daily as necessary. Max treatment duration: 5-7 consecutive days.
Topical/Cutaneous Persistent facial erythema associated with rosacea
Adult: As 1% cream: Apply a pea-sized amount once daily to thinly cover the entire face.
Contraindications
Nasal: Acute coronary disease, cardiac asthma, angle-closure glaucoma, rhinitis sicca, inflammation or lesions of the skin around the nostrils or nasal mucosa, phaeochromocytoma, trans-sphenoidal hypophysectomy or nasal surgery exposing the dura mater. Concomitant use or within 2 weeks after stopping treatment with MAOIs.
Special Precautions
Patient with severe, uncontrolled or unstable CV disease; angina, uncontrolled hypo- or hypertension, orthostatic hypotension, cerebral or coronary insufficiency, thromboangiitis obliterans, Raynaud’s phenomenon, scleroderma, Sjogren’s syndrome; diabetes mellitus, thyroid disease (e.g. hyperthyroidism), porphyria, prostatic hyperplasia or urinary obstruction, occlusive vascular disease; angle-closure glaucoma (topical). Children. Pregnancy and lactation.
Adverse Reactions
Significant: Exacerbated vascular insufficiency, acute angle-closure glaucoma; local nasal effects (e.g. burning, stinging, sneezing, increased nasal discharge), rhinitis medicamentosa and rebound nasal congestion (frequent or long-term use). Cardiac disorders: Rarely, tachycardia, palpitations. Eye disorders: Rarely, eye irritation, dryness, redness or discomfort. Gastrointestinal disorders: Dry mouth or throat. Rarely, nausea. Injury, poisoning and procedural complications: Application site reactions (e.g. dermatitis, pruritus, erythema, pain). Investigations: Rarely, increased blood pressure. Nervous system disorders: Rarely, headache. Psychiatric disorders: Rarely, insomnia, anxiety. Respiratory, thoracic and mediastinal disorders: Rarely, nasal dryness, discomfort or irritation; epistaxis. Skin and subcutaneous tissue disorders: Worsening inflammatory lesions of rosacea (topical). Vascular disorders: Rarely, reactive hyperaemia.
Overdosage
Nasal: Symptoms: Mydriasis, nausea, fever, cyanosis, tachycardia, dyspnoea, lung oedema, psychic disturbance, cardiac arrhythmia, hypertension, cardiac arrest, and inhibited CNS functions (e.g. somnolence, decreased body temperature, bradycardia, shock-like hypotension, apnoea, loss of consciousness). Management: Symptomatic and supportive treatment. May administer phentolamine to reduce the increased blood pressure. May require artificial ventilation and intubation in serious cases.
Drug Interactions
Increased risk of arrhythmias and hypertension with TCAs, appetite suppressants, amphetamine-like psychostimulants. May antagonise the effects of β-blockers and other antihypertensive agents (e.g. methyldopa, bethanidine, debrisoquine, guanethidine). Increased risk of ergotism with ergot alkaloids (e.g. ergotamine, methysergide). May cause additive CV toxicity with antiparkinsonian agents (e.g. bromocriptine). Increased risk of dysrhythmias with cardiac glycosides. Potentially Fatal: May cause significant hypertensive effects when given concomitantly with MAOIs.
Action
Description: Oxymetazoline, a direct-acting sympathomimetic amine, stimulates the α-adrenergic receptors in the nasal mucosal blood vessels to produce local vasoconstriction and decongestion. It also decreases erythema through direct vasoconstriction, when used topically. Onset: Local vasoconstriction: Within 5-10 minutes (nasal). Duration: Local vasoconstriction: Up to 12 hours (nasal). Pharmacokinetics: Absorption: Rapidly absorbed from intranasal tissues. Distribution: Plasma protein binding: 56.7-57.5%. Metabolism: Minimally metabolised in the liver by microsomal enzymes. Excretion: Via urine (30% as unchanged drug); faeces (10%). Elimination half-life: 5-8 days.
Chemical Structure
Oxymetazoline Source: National Center for Biotechnology Information. PubChem Database. Oxymetazoline, CID=4636, https://pubchem.ncbi.nlm.nih.gov/compound/Oxymetazoline (accessed on Jan. 22, 2020)
S01GA04 - oxymetazoline ; Belongs to the class of sympathomimetics used as ophthalmologic decongestants. R01AA05 - oxymetazoline ; Belongs to the class of topical sympathomimetic agents used as nasal decongestants.
References
Afrin No Drip Severe Congestion (Bayer HealthCare LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/04/2020.Anon. Oxymetazoline (Nasal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/04/2020.Anon. Oxymetazoline (Topical). AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 08/04/2020.Anon. Oxymetazoline (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/04/2020.Axcel Oxymetazoline Nasal Drops (Kotra Pharma [M] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 08/04/2020.Boots Blocked Nose Relief 0.05% w/v Nasal Spray (The Boots Company PLC). MHRA. https://products.mhra.gov.uk/. Accessed 08/04/2020.Buckingham R (ed). Oxymetazoline Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/04/2020.Preston CL (ed). Oxymetazoline Drug Interactions. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/05/2020.Rhofade Cream (Aclaris Therapeutics, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/04/2020.Rhofade Cream (Allergan). U.S. FDA. https://www.fda.gov/. Accessed 08/04/2020.Vicks Sinex Decongestant Nasal Spray (Procter & Gamble [Health & Beauty Care] Limited). MHRA. https://products.mhra.gov.uk/. Accessed 08/04/2020.Vicks Sinex Soother Nasal Spray (Procter & Gamble [Health & Beauty Care] Limited). MHRA. https://products.mhra.gov.uk/. Accessed 08/04/2020.
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