Phenylephrine hydrochloride

Uses and Indications

Phenylephrine Hydrochloride Ophthalmic Solution is indicated for the dilation of the pupil as an alpha-1 adrenergic receptor agonist.

There are no teratogenic or nonteratogenic effects associated with this drug.

Dosage and Administration

For patients aged 1 year and older, one drop of Phenylephrine Hydrochloride Ophthalmic Solution (available in 2.5% and 10% strengths) should be applied to the conjunctival fornix at intervals of 3 to 5 minutes, with a maximum of 3 drops per eye. To achieve a greater degree of mydriasis, the 10% strength is recommended.

For pediatric patients under 1 year of age, one drop of the 2.5% strength should be instilled into the conjunctival fornix at 3 to 5 minute intervals, also with a maximum of 3 drops per eye.

Contraindications

The 10% strength is contraindicated in patients with hypertension or thyrotoxicosis due to the potential for exacerbating these conditions. Additionally, it is contraindicated in pediatric patients less than 1 year of age because of an increased risk of systemic toxicity.

Warnings and Precautions

Topical ophthalmic use is the only approved route for administration; this product is not intended for injection.

Healthcare professionals should be aware of the potential for serious cardiovascular reactions associated with the 10% strength formulation. These reactions may include ventricular arrhythmias, some of which have resulted in fatal outcomes. It is imperative to monitor blood pressure in patients with pre-existing cardiovascular disease to mitigate risks.

Significant elevations in blood pressure have been observed, particularly in pediatric patients under the age of 5, as well as in individuals with cardiovascular disease or hyperthyroidism. For patients identified as high risk, it is recommended to monitor blood pressure following treatment to ensure patient safety.

Additionally, rebound miosis has been reported as a potential effect occurring one day after instillation. Healthcare providers should remain vigilant for this occurrence and counsel patients accordingly.

Side Effects

Patients may experience a range of ocular adverse reactions, including eye pain and stinging upon instillation, temporary blurred vision, and photophobia.

Cardiovascular adverse reactions have also been reported, with occurrences such as increases in blood pressure, syncope, myocardial infarction, tachycardia, arrhythmia, and subarachnoid hemorrhage. Serious cardiovascular reactions include ventricular arrhythmias, some of which have been fatal. It is important to note that significant elevations in blood pressure may occur, particularly in pediatric patients under 5 years of age, as well as in patients with pre-existing cardiovascular disease or hyperthyroidism. For patients at high risk, monitoring of blood pressure post-treatment is recommended.

Rebound miosis has been reported as an adverse reaction occurring one day after instillation. Additionally, overdosage of the medication may lead to a rapid rise in blood pressure, accompanied by symptoms such as headache, anxiety, nausea, vomiting, and ventricular arrhythmias.

Drug Interactions

Atropine-like drugs may enhance the adrenergic pressor response when administered concurrently. Clinicians should monitor patients for increased blood pressure and adjust dosages of adrenergic agents as necessary to mitigate this effect.

Potent inhalation anesthetic agents have the potential to amplify cardiovascular depressant effects. It is advisable to closely monitor cardiovascular status during the use of these anesthetics, and dosage adjustments may be required based on the patient's response to anesthesia.

Packaging & NDC

The table below lists all NDC Code configurations of Phenylephrine Hydrochloride, the U.S. brand-name prescription product. Columns show Packaging, Formulation Type, and Active Ingredient Strength.

Pediatric Use

In pediatric patients aged 1 year and older, phenylephrine hydrochloride ophthalmic solution 2.5% or 10% may be administered at a dosage of one drop every 3 to 5 minutes into the conjunctival fornix, with a maximum of 3 drops per eye per day. For patients under 1 year of age, only phenylephrine hydrochloride ophthalmic solution 2.5% is recommended, with the same dosing frequency and maximum limit of 3 drops per eye.

Phenylephrine hydrochloride ophthalmic solution 10% is contraindicated in pediatric patients less than 1 year of age due to an increased risk of systemic toxicity. Additionally, caution is advised when using phenylephrine hydrochloride ophthalmic solution 10% in pediatric patients under 5 years of age, as well as in those with hyperthyroidism or cardiovascular disease.

Geriatric Use

Elderly patients, defined as those aged 65 years and older, have not demonstrated any overall differences in safety and effectiveness compared to younger adult patients. Therefore, no specific dosage adjustments are necessary for this population.

However, healthcare providers should remain vigilant in monitoring geriatric patients for any potential age-related changes that may affect drug metabolism and response. It is essential to consider individual patient factors, including comorbidities and concurrent medications, when prescribing to elderly patients to ensure optimal therapeutic outcomes.

Pregnancy

Animal reproduction studies have not been conducted with topical phenylephrine. Therefore, it is not known whether phenylephrine can cause fetal harm when administered to a pregnant woman or affect reproductive capacity. Given the lack of data, phenylephrine hydrochloride should be administered to a pregnant woman only if clearly needed. Healthcare professionals should weigh the potential benefits against any unknown risks when considering the use of this medication in pregnant patients.

Lactation

It is not known whether phenylephrine hydrochloride ophthalmic solution 2.5% and 10% is excreted in human breast milk. Due to the potential for many drugs to be excreted in human milk, caution should be exercised when administering this medication to lactating mothers. Healthcare professionals should consider the risks and benefits of treatment in nursing women, particularly in relation to the possible effects on breastfed infants.

Renal Impairment

There is no specific information available regarding dosage adjustments, special monitoring, or safety considerations for patients with renal impairment. Healthcare professionals should exercise caution when prescribing to patients with reduced kidney function, as the absence of detailed guidance necessitates careful clinical judgment. Regular monitoring of renal function may be advisable in this patient population.

Hepatic Impairment

Patients with hepatic impairment have not been specifically studied in relation to the use of this medication. Consequently, there are no established dosage adjustments, special monitoring requirements, or precautions for individuals with compromised liver function. It is recommended that healthcare providers exercise caution when prescribing this medication to patients with hepatic impairment, given the lack of data on its safety and efficacy in this population. Regular monitoring of liver function may be prudent in these cases, although specific parameters are not defined in the available information.

Overdosage

Overdosage of phenylephrine can lead to significant cardiovascular and neurological effects. A notable consequence of overdosage is a rapid increase in blood pressure, which may pose serious health risks to the patient.

In addition to hypertension, symptoms may include headache, anxiety, nausea, vomiting, and the potential for ventricular arrhythmias. These manifestations require immediate attention to mitigate further complications.

Management of phenylephrine overdosage should involve the prompt administration of a rapidly acting alpha-adrenergic blocking agent, such as phentolamine. This intervention is critical in reversing the hypertensive effects and stabilizing the patient's condition. Healthcare professionals are advised to monitor the patient closely for any evolving symptoms and to provide supportive care as necessary.

Nonclinical Toxicology

Animal reproduction studies have not been conducted with topical phenylephrine. The potential for phenylephrine to cause fetal harm when administered to a pregnant woman or to affect reproductive capacity is not known. Therefore, phenylephrine hydrochloride should be administered to a pregnant woman only if clearly needed.

Postmarketing Experience

Reports of serious cardiovascular reactions, including ventricular arrhythmias and myocardial infarctions, have been documented in patients using phenylephrine 10%. These episodes, some of which have been fatal, typically occurred in individuals with pre-existing cardiovascular conditions. It is recommended that phenylephrine Hydrochloride Ophthalmic Solution 2.5% be utilized in these patients.

While a significant elevation in blood pressure is not common, it has been reported following conjunctival instillation of the recommended doses of phenylephrine 10%. The risk of elevated blood pressure is lower with phenylephrine 2.5%. Caution is advised when using phenylephrine 10% in pediatric patients under 5 years of age, as well as in patients with hyperthyroidism or cardiovascular disease. Monitoring of post-treatment blood pressure is essential for patients with cardiac and endocrine diseases, as well as for any patients who exhibit symptoms.

Rebound miosis has been observed one day after administration of phenylephrine hydrochloride ophthalmic solution, with re-instillation resulting in a diminished mydriatic effect.

The following adverse reactions have been identified following the use of phenylephrine hydrochloride ophthalmic solution. Due to the voluntary nature of these reports from a population of uncertain size, it is not always feasible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Ocular adverse reactions include eye pain, stinging upon instillation, temporary blurred vision, and photophobia. Cardiovascular adverse reactions encompass increases in blood pressure, syncope, myocardial infarction, tachycardia, arrhythmia, and subarachnoid hemorrhage. A marked increase in blood pressure has been particularly noted in low weight premature neonates, infants, and hypertensive patients. Cardiovascular effects have primarily been observed in hypertensive patients following the topical ocular use of phenylephrine hydrochloride ophthalmic solution 10%.

Patient Counseling

Healthcare providers should advise patients not to touch the dropper tip to any surface, as this may lead to contamination of the solution. It is important for patients to understand that maintaining the sterility of the dropper is crucial for their safety and the effectiveness of the treatment.

Additionally, healthcare providers should inform patients that they may experience sensitivity to light, particularly when their pupils are dilated. Patients should be counseled to protect their eyes in bright illumination to avoid discomfort and potential harm.

Storage and Handling

Phenylephrine Hydrochloride Ophthalmic Solution, USP is supplied in a container that must be kept tightly closed to maintain its integrity. It should be stored at a temperature range of 20° to 25°C (68° to 77°F), in accordance with USP Controlled Room Temperature guidelines.

To ensure optimal preservation, the solution must be protected from light and excessive heat. Once opened, the solution remains usable until the expiration date indicated on the bottle.

Additional Clinical Information

In patients aged 1 year and older, phenylephrine hydrochloride ophthalmic solution (2.5% or 10%) should be administered as one drop into the conjunctival fornix every 3 to 5 minutes, with a maximum of 3 drops per eye per day. For pediatric patients under 1 year of age, the 2.5% solution is to be instilled at the same intervals, also not exceeding 3 drops per eye.

Clinicians should counsel patients on proper administration techniques, emphasizing the importance of not touching the dropper tip to any surface to avoid contamination. Patients should also be informed about potential sensitivity to light and the need to protect their eyes from bright illumination while their pupils are dilated.

FDA Insert (PDF)

This document is the official FDA-approved prescribing information for Phenylephrine Hydrochloride as submitted by Lifestar Pharma LLC. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)