antazoline and xylometazoline

Action and Spectrum

Actions and spectrum: 

• antazoline: antazoline is an antihistamine. It works by blocking the histamine, a substance in the body that causes allergic symptoms. In Otrivine Antistin Eye Drops, antazoline helps relieve symptoms associated with eye allergies, such as itching, redness, and irritation. 
• xylometazoline: xylometazoline is a decongestant. It constricts the blood vessels in the eyes, reducing blood flow and decreasing swelling. This helps to relieve redness and puffiness in the eyes. It can also alleviate symptoms associated with eye congestion. 

The combination of these two ingredients makes Otrivine Antistin Eye Drops effective in providing relief from various eye allergy symptoms, including itching, redness, irritation, and congestion. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Skin sensitization 

Hypersensitivity reactions 

blurred vision 

Headache 

Allergic reactions 

Increased blood pressure 

Sweating 

Palpitations 

Drowsiness 

Black Box Warning

Black Box Warning: 

There was no specific black box warning associated with antazoline and xylometazoline. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Patients with a known hypersensitivity or allergy to antazoline, xylometazoline, or any of the other ingredients in the formulation should not use the combination product. 
• Closed-Angle Glaucoma: Use of the combination may be contraindicated in individuals with closed-angle glaucoma due to the potential for increased intraocular pressure from the use of decongestants like xylometazoline. 
• Severe Cardiovascular Conditions: Individuals with severe cardiovascular conditions, such as severe hypertension, severe coronary artery disease, or arrhythmias, may be advised to avoid the combination due to the potential cardiovascular effects of decongestants. 
• Children Under a Certain Age: Some combination products may have age restrictions and may not be recommended for very young children. 

Caution: 

• Thyroid Disorders: People with hyperthyroidism or uncontrolled thyroid disorders may be at greater risk of cardiovascular side effects when using decongestants like xylometazoline. 
• Enlarged Prostate: Men with an enlarged prostate (benign prostatic hyperplasia) should exercise caution as decongestants may worsen urinary symptoms. 
• Eye Conditions: Individuals with pre-existing eye conditions like glaucoma, especially open-angle glaucoma, should use this combination with caution, as decongestants can increase intraocular pressure. 
• Pregnancy and Lactation: Pregnant and breastfeeding individuals should consult a healthcare professional before using the combination to weigh the potential risks and benefits.

Comorbidities: 

• Cardiovascular Disease: Individuals with a history of heart disease, high blood pressure (hypertension), arrhythmias, or coronary artery disease may need to use the combination product cautiously. Decongestants like xylometazoline can potentially elevate blood pressure and heart rate. 
• Diabetes: People with diabetes should be aware that decongestants, like xylometazoline, can affect blood sugar levels. Monitor blood glucose carefully and consult a healthcare professional if you have concerns. 
• Hyperthyroidism: Patients with hyperthyroidism should use the combination product with caution because decongestants can exacerbate symptoms of hyperthyroidism. 
• Prostate Enlargement: Men with an enlarged prostate (benign prostatic hyperplasia) should exercise caution when using the combination, as decongestants can worsen urinary symptoms. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: C 

Lactation: excreted into human milk: unknown  

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: 

Otrivine Antistin Eye Drops combine two active ingredients, antazoline and xylometazoline, to address eye allergy symptoms. antazoline is an antihistamine that blocks the effects of histamine, a compound involved in allergic reactions, reducing itching,

redness, and irritation. xylometazoline is a decongestant that constricts blood vessels, reducing eye swelling and congestion. Together, these ingredients provide relief from various eye allergy symptoms, making Otrivine Antistin Eye Drops a valuable tool in managing eye discomfort caused by allergies.  

Pharmacodynamics: 

• antazoline: antazoline is an antihistamine that exerts its effects by blocking the action of histamine. Histamine is responsible for causing itching, redness, and inflammation in the eyes during allergies. antazoline competes with histamine for binding to its receptors in the eyes, preventing histamine from triggering these symptoms. This results in the alleviation of itchiness and redness, making it a valuable component for treating eye allergies. 
• xylometazoline: xylometazoline is a vasoconstrictor or decongestant. It acts by constricting blood vessels in the eyes. The constriction reduces the blood flow to the area and, in turn, decreases swelling and congestion. xylometazoline’s decongestant action helps in relieving eye irritation and puffiness associated with allergic responses. 

When used in combination, these pharmacodynamic actions of antazoline and xylometazoline make Otrivine Antistin Eye Drops effective in providing relief from eye allergy symptoms, including itching, redness, and congestion.  

Pharmacokinetics: 

Absorption 

• antazoline: When applied as eye drops, antazoline is absorbed directly through the conjunctival blood vessels on the surface of the eye, providing local action. 
• xylometazoline: Like antazoline, xylometazoline is also absorbed through the conjunctival blood vessels. 

Distribution 

• antazoline and xylometazoline: After absorption, both antazoline and xylometazoline primarily act locally in the eye. Limited systemic distribution occurs, as they are not intended for widespread distribution throughout the body. 

Metabolism 

• antazoline: antazoline may undergo metabolism in the liver through various enzymatic pathways; however, most of it is excreted unchanged in urine. 
• xylometazoline: Like antazoline, xylometazoline can undergo hepatic metabolism, but the majority is excreted in its unchanged form. 

Elimination and excretion 

• antazoline and xylometazoline: Both antazoline and xylometazoline are primarily excreted through the renal system via urine. They have a short duration of action in the eye due to this excretion. 

Adminstartion

Administration: 

• Wash your hands thoroughly with soap and water. 
• Shake the eye drop bottle well if required by the product instructions. 
• Tilt your head back or lie down and look upward. 
• Gently pull down the eyelid to create a small pocket. 
• Hold eye drop bottle close to your eye but avoid touching your eye or eyelashes. 
• Squeeze the bottle to release the prescribed number of drops into the pocket created by your lower eyelid. 
• Close your eye gently and keep it closed for a moment to allow the eye drop to spread across your eye. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: antazoline and xylometazoline 

Pronounced: (an-TAZ-oh-leen-and- zye-loh-met-AZ-oh-leen)  

Why do we use antazoline and xylometazoline? 

Otrivine Antistin Eye Drops can provide relief from itchy eyes, which may be caused by allergies or environmental irritants. These eye drops can reduce eye redness, making the eyes appear less bloodshot. They can help relieve eye congestion or discomfort related to eye allergies or minor eye irritations. These eye drops are commonly used to manage allergic conjunctivitis, whether it is due to seasonal allergies or perennial allergies