Oxymetazoline

Oxymetazoline is an alpha-1A adrenoceptor agonist belonging to Nasal Decongestants.

Oxymetazoline is used in treating Rosacea.

Oxymetazoline is Rapidly absorbed from intranasal tissues. The Plasma protein binding: 56.7-57.5% and Minimally metabolised in the liver by microsomal enzymes and get excreted Via urine (30% as unchanged drug); faeces (10%).

Elimination half-life: 5-8 days.

The onset of action of Oxymetazoline was Within 5 to 10 minutes.

The Duration of time for Oxymetazoline was within 12 hours.

The Tmax of Oxymetazoline is approximately 30 minutes to 1 hour after oral administration.

The Cmax of oxymetazoline nasal spray or drops is typically achieved within 15 to 30 minutes after administration.

Oxymetazoline shows common side effects like burning. stinging. increased nasal discharge. dryness inside the nose. sneezing. nervousness. nausea. dizziness.

Oxymetazoline is available in the form of nasal spray, nasal drops, eye drops and topical cream.

Oxymetazoline is available in India, Germany, Canada, Italy, USA

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.

Oxymetazoline is used in the treatment of Rosacea and nasal decongestion.

Oxymetazoline binds to α₁- and α₂-adrenoceptors, which are Gq-protein-coupled receptors that promote vascular smooth muscle contraction by increasing intracellular calcium levels in response to ligand activation.

Oxymetazoline is approved for use in the following clinical indications

Rosacea: Treatment of persistent facial erythema associated with rosacea and nasal decongestion in adults.

Nasal

Nasal congestion

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.

Oxymetazoline is available in various strengths as 0.05%, 0.1%, 0.025%.

Oxymetazoline is available in the form of nasal spray, nasal drops, eye drops and topical cream.

Nasal: Acute coronary disease, cardiac asthma, angle-closure glaucoma, rhinitis sicca, inflammation or lesions of the skin around the nostrils or nasal mucosa, pheochromocytomas, trans-sphenoidal hypophysectomy or nasal surgery exposing the dura mater. Concomitant use or within 2 weeks after stopping treatment with MAOIs.

Disease-related concerns:

• Cardiovascular disease: May affect blood pressure; use with caution in patients with uncontrolled hypertension or hypotension, orthostatic hypotension or with severe, unstable, or uncontrolled cardiovascular disease. May potentiate vascular insufficiency; use with caution in patients with cerebral or coronary insufficiency, scleroderma, thromboangiitis obliterans, and Raynaud phenomenon.

• Glaucoma: Use may increase the risk of angle closure glaucoma in patients with narrow-angle glaucoma; use with caution.

• Sjögren syndrome: Use with caution in patients with Sjögren syndrome.

Other warnings/precautions:

• Appropriate use: For topical use only; not for oral, ophthalmic, or intravaginal use; avoid contact with eyes and lips. Do not apply to open wounds or irritated skin.

Pregnancy Category C: Teratogenicity studies have been performed in animals.

High-fat meal may decrease the rate but not the extent of absorption. Management: May administer with meals.

• Common Adverse effects:

Blurred vision fast, irregular, or pounding heartbeat headache, dizziness, drowsiness, or lightheadedness high blood pressure increase in runny or stuffy nose nervousness trembling trouble in sleeping weakness

• Less Common Adverse effects:

Bloody nose blurred vision chest pain or discomfort difficulty swallowing dizziness headache lightheadedness, dizziness, or fainting nervousness pounding in the ears slow or fast, irregular heartbeat ulcers in the nose unusual tiredness

• Rare Common Adverse effects:

Burning. stinging. increased nasal discharge. dryness inside the nose. sneezing. nervousness. nausea. dizziness.

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.

The common side effects of Oxymetazoline include the following headache, dizziness, abdominal pain, diarrhea, and nausea.

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.

Pharmacodynamic

Oxymetazoline is an adrenergic α₁- and α₂-agonist and a direct-acting sympathomimetic drug. By stimulating adrenergic receptors, oxymetazoline causes vasoconstriction of dilated arterioles and reduces blood flow.In a radioligand competition study, oxymetazoline displayed higher affinity at α_1A-adrenoceptors compared to α_2B-adrenoceptors, but with higher potency at α_2B-adrenoceptors.When sprayed intranasally, oxymetazoline relieved relief nasal congestion and improved nasal airflow in patients with acute coryzal rhinitis for up to 12 hours following a single dose.

Pharmacokinetics

• Absorption:

Oxymetazoline is primarily administered as a nasal spray or drops and is rapidly absorbed into the bloodstream through the nasal mucosa. When administered topically for skin redness or irritation, oxymetazoline can also be absorbed through the skin.

• Distribution:

Oxymetazoline is distributed throughout the body after absorption, and it has a high affinity for alpha-adrenergic receptors. It can cross the blood-brain barrier, which may contribute to its potential side effects.

• Metabolism:

Oxymetazoline is metabolized primarily in the liver by cytochrome P450 enzymes, primarily CYP2D6 and CYP3A4, into inactive metabolites that are excreted in the urine.

• Excretion:

Oxymetazoline and its metabolites are primarily excreted in the urine. The elimination half-life of oxymetazoline is approximately 5-8 hours, which means it takes this long for the body to eliminate half of the drug from the bloodstream.

• https://www.rxlist.com/dopram-drug.htm
• https://www.mims.com/india/drug/info/Oxymetazoline?type=full&mtype=generic
• https://go.drugbank.com/drugs/DB00561
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7003846/