oxymetazoline topical

Action and Spectrum

Actions and spectrum: 

oxymetazoline is a selective alpha-1 adrenergic receptor agonist with vasoconstrictive properties. When applied topically, it acts as a nasal decongestant and is commonly used to relieve nasal congestion caused by allergies, sinusitis, or the common cold. 

The primary action of oxymetazoline is to constrict blood vessels in nasal passages, which helps to reduce congestion and swelling. By narrowing the blood vessels, it decreases blood flow to the nasal mucosa, leading to decreased inflammation and nasal congestion. This allows for improved airflow and relief of nasal symptoms. 

The spectrum of oxymetazoline topical is primarily focused on nasal congestion. It is specifically formulated for intranasal use and is not intended for use on other areas of the body. oxymetazoline nasal sprays or drops are available OTC and by prescription, depending on the strength and formulation. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

inflammatory lesions Worsening of rosacea (1%) 

erythema at Application-site (1%) 

dermatitis at Application-site (2%) 

pruritus at Application-site (1%) 

pain at Application-site (1%) 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with the use of oxymetazoline topical. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Closed-angle glaucoma: oxymetazoline may increase intraocular pressure and worsen symptoms of glaucoma, particularly in individuals with closed-angle glaucoma. 
• Severe hypertension (high blood pressure): oxymetazoline can potentially elevate blood pressure, and its use should be avoided in individuals with severe hypertension or uncontrolled high blood pressure. 
• Cardiovascular disease: Individuals with a history of heart disease, coronary artery disease, arrhythmias, or other cardiovascular conditions should use oxymetazoline topical with caution, as it may have cardiovascular effects. 
• Hyperthyroidism: oxymetazoline may stimulate the thyroid gland, and its use should be approached cautiously in individuals with hyperthyroidism. 

Caution: 

• Cardiovascular conditions: Individuals with underlying cardiovascular conditions, such as heart disease, high blood pressure, or irregular heart rhythm, should use oxymetazoline topical with caution. The medication can potentially increase heart rate and blood pressure. 
• Thyroid disorders: oxymetazoline can stimulate the thyroid gland, so individuals with thyroid disorders, such as hyperthyroidism, should use the medication cautiously and under medical supervision. 
• Prostate enlargement: Men with an enlarged prostate (benign prostatic hyperplasia) should exercise caution when using oxymetazoline topical, as it may worsen urinary symptoms. 
• Narrow-angle glaucoma: oxymetazoline can increase intraocular pressure, so individuals with narrow-angle glaucoma should avoid using the medication. 
• Pregnancy and lactation: The safety of oxymetazoline topical during pregnancy and lactation is not well established.  
• Children and elderly: Special caution should be exercised when using oxymetazoline topical in children and elderly individuals, as they may be more susceptible to its side effects.

Comorbidities: 

• Cardiovascular disease: Individuals with cardiovascular conditions such as high blood pressure, heart disease, or arrhythmias should use oxymetazoline topical with caution. The medication can potentially increase heart rate and blood pressure. 
• Diabetes: oxymetazoline may affect blood sugar levels, so individuals with diabetes should monitor their blood sugar closely while using the medication. 
• Allergies or hypersensitivity: Individuals with known allergies or hypersensitivity to oxymetazoline or similar medications should avoid using oxymetazoline topical. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: It is unknown whether drug gets excreted into human milk.  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

oxymetazoline topical is a selective alpha-adrenergic agonist that acts as a vasoconstrictor. When applied topically, the blood vessels constrict in the nasal passages, leading to a reduction in nasal congestion and swelling.

The exact mechanism of action of oxymetazoline involves activation of alpha-adrenergic receptors, primarily the alpha-1 receptors, on the smooth muscle cells. 

By activating these receptors, oxymetazoline causes vasoconstriction, which leads to a decreased blood flow to nasal mucosa. This helps to reduce congestion and improve breathing. The vasoconstrictive effect also reduces nasal swelling and inflammation.  

Pharmacodynamics: 

The pharmacodynamics of oxymetazoline topical involve its interaction with alpha-adrenergic receptors in the nasal mucosa. oxymetazoline is a selective alpha-1 adrenergic agonist, which means it specifically targets and activates alpha-1 adrenergic receptors on smooth muscle cells of the blood vessels in the nasal passages. 

When oxymetazoline is applied topically, it binds to and activates these alpha-1 receptors. This activation leads to vasoconstriction or narrowing of the blood vessels in the nasal mucosa. As a result, blood flow to the nasal tissue is reduced, leading to a decrease in nasal congestion and swelling.  

Pharmacokinetics: 

Absorption 

When applied topically to the nasal mucosa, oxymetazoline is readily absorbed. The drug is absorbed through blood vessels in the nasal passages and enters the systemic circulation. 

Distribution 

Once absorbed, oxymetazoline is distributed throughout the body. It binds to alpha-adrenergic receptors in the blood vessels, including those in the nasal mucosa, leading to vasoconstriction. 

Metabolism 

oxymetazoline undergoes metabolism primarily in the liver. The main metabolic pathway involves enzymatic oxidation, primarily mediated by the enzyme cytochrome P450 2D6 (CYP2D6). The metabolites formed are primarily inactive. 

Elimination and excretion 

The metabolites of oxymetazoline are excreted primarily in the urine. The elimination half-life of oxymetazoline is relatively short, ranging from 3 to 6 hours. 

Adminstartion

Administration: 

oxymetazoline topical products are typically available in the form of nasal sprays or nasal drops. 

• Read the instructions: Carefully read the product label and accompanying instructions provided by the manufacturer or healthcare professional. Follow the recommended dosage, frequency, and duration of use. 
• Prepare the nasal spray or drops: If using a nasal spray, remove the protective cap and shake the container gently. If using nasal drops, open the bottle and ensure the dropper is clean. 
• Position yourself: Stand or sit upright with your head tilted slightly forward. If possible, blow your nose gently to clear any mucus or blockages before administering the medication. 
• Administer the medication: Hold the nasal spray or dropper close to one nostril, aiming slightly away from the center of the nose. Press the pump or squeeze the dropper to release the appropriate number of sprays or drops as directed by the instructions. 
• Breathe in gently: Inhale slowly and gently through the nostril while administering the medication. Avoid sniffing forcefully, as this can hinder proper absorption. 
• Repeat for the other nostril: If instructed to use the medication in both nostrils, repeat the process for the other nostril. 
• Clean and store: Replace the protective cap on the nasal spray bottle or close the nasal drops bottle tightly. Clean the nasal spray nozzle or dropper if necessary and store the product according to the instructions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: oxymetazoline topical 

Pronounced: (ox-ee-met-AZ-oh-leen TOP-i-kal)  

Why do we use oxymetazoline topical? 

• Nasal congestion relief: oxymetazoline nasal sprays or drops are frequently used to relieve nasal congestion caused by allergies, sinusitis, or the common cold. It works by blood vessels constriction in the nasal passages, reducing swelling and congestion. 
• Nasal decongestion prior to medical procedures: oxymetazoline nasal sprays may be used to shrink nasal blood vessels before certain medical procedures, such as nasal endoscopy or nasal surgery. This helps improve visibility and reduce bleeding during the procedure.