dipivefrin Ophthalmic

Action and Spectrum

Actions and spectrum: 

Action: 

dipivefrin ophthalmic is a prodrug of epinephrine (adrenaline), which means that it is converted into epinephrine when it enters the eye. Epinephrine has several effects on the eye that help reduce intraocular pressure (IOP) and manage conditions like glaucoma. These actions include: 

• Decreased Aqueous Humor Production: Epinephrine reduces the production of aqueous humor, which is the clear fluid that fills the front part of the eye. This reduction in fluid production lowers IOP. 
• Improved Aqueous Humor Outflow: Epinephrine increases the drainage or outflow of aqueous humor from the eye, helping to further lower IOP. 
• Constriction of Blood Vessels: Epinephrine constricts the blood vessels in the eye, which can also help reduce IOP. 

Spectrum: 

dipivefrin ophthalmic is primarily used to lower intraocular pressure in patients with open-angle glaucoma & ocular hypertension. These conditions are characterized by increased pressure within the eye, which may lead to optic nerve damage and vision loss.  

dipivefrin ophthalmic is applied topically to the eye, and its effects are localized to the ocular tissues. It does not have systemic effects throughout the body, as the prodrug is converted to epinephrine within the eye. This localized action helps minimize side effects that might be associated with systemic epinephrine use. 

Drug Interaction

Adverse Reaction

Frequency not defined 

discomfort 

stinging 

Swelling 

blurred vision 

increased sensitivity 

allergic reactions 

Eye irritation 

Burning 

hypertension 

Inflammation 

Pain 

Mydriasis 

headache 

tachycardia 

Black Box Warning

Black Box Warning: 

There were no specific black box warnings associated with dipivefrin ophthalmic. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals with a known hypersensitivity or allergy to dipivefrin or any of its components should not use the medication. 
• Narrow-Angle Glaucoma: dipivefrin is not recommended for patients with narrow-angle glaucoma, as it can exacerbate the condition by causing the pupil to dilate. 
• Cardiovascular Disease: The use of dipivefrin may be cautioned in individuals with severe cardiovascular disease, including certain arrhythmias, as it can have cardiovascular effects due to its similarity to epinephrine. 
• Corneal Abrasions or Lesions: The medication should not be applied to eyes with corneal abrasions or lesions, as it can cause discomfort or irritation. 
• Pregnancy and Lactation: The safety of dipivefrin during pregnancy and breastfeeding is not well-established. Healthcare providers should carefully assess the potential risks and benefits in pregnant or breastfeeding individuals.

Caution: 

• Systemic Effects: Although dipivefrin is primarily used in the eye and has localized effects, it is a prodrug of epinephrine, which can potentially lead to systemic effects. Caution is advised in patients with certain cardiovascular conditions, such as arrhythmias or hypertension, as systemic absorption can affect heart rate and blood pressure. 
• Diabetes: The use of dipivefrin can affect blood glucose levels. Diabetic patients should be monitored for changes in their glucose levels, and adjustments to their diabetes management may be necessary. 
• Psychiatric Conditions: Patients with a history of psychiatric conditions, including anxiety or panic disorders, should be closely monitored for potential exacerbation of their symptoms. 
• Corneal Health: dipivefrin can cause transient stinging or burning upon instillation, and it should be used with caution in patients with corneal abrasions or lesions. 
• Pediatric and Geriatric Patients: Special caution and monitoring may be required when using dipivefrin in pediatric and geriatric patients, as they may have unique response profiles.

Comorbidities: 

• Migraines: Migraine sufferers may be more prone to ocular conditions, including glaucoma. 
• Aging-Related Eye Conditions: Age-related macular degeneration (AMD) and other age-related eye conditions may be comorbid with glaucoma, especially in older individuals. 
• Thyroid Disorders: Conditions like hyperthyroidism can affect eye health and may be comorbid with glaucoma. 
• Medication Use: Some medications, especially corticosteroids, can increase the risk of glaucoma. Other medications may be used to manage comorbid conditions. 
• Neurological Conditions: Conditions like Alzheimer’s disease may coexist with glaucoma and can affect a patient’s ability to adhere to glaucoma treatment. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: B 

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: 

dipivefrin ophthalmic is a medication used in the field of ophthalmology to treat conditions such as glaucoma and ocular hypertension. Its pharmacological action is based on being a prodrug of epinephrine, which means it is converted into epinephrine within the eye after application.

Epinephrine acts to lower intraocular pressure (IOP) through several mechanisms, including reducing the production of aqueous humor (the fluid in the eye), increasing its outflow, and constricting blood vessels within the eye. These actions collectively help decrease IOP, which is essential in managing conditions like glaucoma. The localized nature of its action minimizes systemic side effects, making it a valuable treatment option in ophthalmic care.  

Pharmacodynamics: 

• Aqueous Humor Production: Epinephrine, the active metabolite of dipivefrin, reduces the production of aqueous humor. By decreasing its production, it helps to lower intraocular pressure (IOP). 
• Aqueous Humor Outflow: Epinephrine enhances the drainage or outflow of aqueous humor from the eye. It acts on the trabecular meshwork and Schlemm’s canal to improve the aqueous humor’s drainage, which further contributes to IOP reduction. 
• Constriction of Blood Vessels: Epinephrine constricts blood vessels, including the small blood vessels within the eye. This vasoconstrictive effect reduces blood flow within the eye and can lead to a decrease in IOP. 
• Increased Uveoscleral Outflow: Epinephrine may also increase uveoscleral outflow, another mechanism for reducing IOP. This effect involves the drainage of aqueous humor through the ciliary muscle and the suprachoroidal space. 

Pharmacokinetics: 

Absorption 

dipivefrin is applied topically as eye drops. Upon instillation, it is absorbed through the cornea and conjunctiva, entering the anterior chamber of the eye where it undergoes enzymatic hydrolysis to form its active metabolite, epinephrine. 

Distribution 

The distribution of dipivefrin is primarily localized within the eye where it exerts its pharmacological effects. Its active metabolite, epinephrine, acts locally to reduce intraocular pressure (IOP). 

Metabolism 

dipivefrin undergoes enzymatic hydrolysis within the eye, primarily in the ciliary body and iris, to convert into epinephrine, which is responsible for its pharmacological actions. This conversion is a crucial step in its activation. 

Elimination and excretion 

dipivefrin and its metabolite, epinephrine, are not significantly systemically absorbed, so they are not subject to systemic excretion or renal clearance. The metabolite remains localized within the eye, where it exerts its effects on intraocular pressure. 

Adminstartion

Administration: 

• Wash Hands: Before administering the eye drops, thoroughly wash your hands to ensure they are clean and free from any potential contaminants. 
• Position Yourself: Find a stable and comfortable position, either sitting down or standing in front of a mirror. This will make it easier to administer the eye drops accurately. 
• Tilt the Head Back: Tilt your head backward and look upward. You can do this by either lying down and letting your head hang over the edge of a bed or tilting your head backward while seated. 
• Create a Pouch: Using your non-dominant hand, gently pull-down lower eyelid to create a pocket between the eyelid and the eye. This is where the eye drops will be placed. 
• Administer the Eye Drops: Hold the eye drop container with your dominant hand. Carefully squeeze the container to release one drop of the medication into the pouch you created in step 5. Be sure to avoid touching the tip of the container to prevent contamination. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: dipivefrin Ophthalmic 

Pronounced: (dye-PIV-uh-frin oh-THAL-mik)  

Why do we use dipivefrin Ophthalmic? 

dipivefrin is often prescribed to lower intraocular pressure (IOP) in individuals with open-angle glaucoma, the most common form of glaucoma. By reducing IOP, dipivefrin helps slow the progression of the disease and preserve vision. Ocular hypertension refers to elevated IOP in the absence of optic nerve damage. Individuals with ocular hypertension have a higher risk of developing glaucoma. dipivefrin can be used to manage and reduce IOP in these individuals as a preventive measure.