Alcaftadine Ophthalmic Solution - Uses, Dosage, and Side Effects

Overview:

Ophthalmic Alcaftadine is available as a solution to be injected into the eye. It is usually injected once a day into the affected eyes. It relieves the itching caused by allergic pink eye. Alcaftadine belongs to the antihistamine medication class. It works by preventing the release of histamine, a substance in the body that causes allergic reactions. Alcaftadine is typically administered as an eye drop, which keeps its effects regional compared to localized, as Alcaftadine's main metabolite is a carboxylic acid metabolite with minimal systemic effects. It is used to treat itching caused by allergies in the eyes. Alcaftadine ophthalmic should not be used to treat contact lens-induced eye irritation.

How Does Alcaftadine Ophthalmic Solution Work?

Alcaftadine is an antihistamine with a strong affinity for histamine H1 and H2 receptors and a weaker affinity for H4 receptors. It also affects immune cell recruitment and has stabilizing effects on mast cells. To treat allergic conjunctivitis, it is designed as an eye drop. Microsomal enzymes do not appreciably metabolize it, while cytosolic enzymes quickly change it into a carboxylic acid metabolite. Proteins unbind both substances. The parent chemical and the carboxylic acid metabolite achieved peak serum concentrations within minutes. However, within three hours, they declined below detectable values in a pharmacokinetic trial of a 0.25 percent ophthalmic solution in healthy participants aged 18 to 55.

Uses:

This medication is used to treat allergic itchiness in the eyes. Alcaftadine is a type of antihistamine. It prevents the release of a natural substance (histamine) that causes allergic reactions. Avoid using this medication to treat red or irritated eyes caused by contact lenses. If this happens, contact the doctor for further instructions.

Dosage:

Alcaftadine 0.25 percent (2.5 mg/mL) topical ophthalmic solution. Once a day, place one drop in each eye. When using additional ophthalmic medications, a 5-minute interval between applications is recommended.

What Are the Drug Warnings?

For Pregnant and Breastfeeding Women:

• If a woman takes this medication while pregnant, immediately consult the doctor. If the benefits outweigh the risks, the drug should be used.

• There are no known side effects of Alcaftadine eye drops while breastfeeding. However, before taking any medication, consult with the doctor right away.

Other Warnings:

• Alcaftadine ophthalmic should not be used in children under the age of two.

• To avoid contaminating the dropper tip and solution, avoid touching the eyelids or surrounding areas with the bottle's dropper tip.

• Keep the bottle tightly closed when not using the medication.

• Alcaftadine ophthalmic should not be used to treat contact lens-induced eye irritation.

For Patients:-

What Is Allergic Conjunctivitis?

Allergic conjunctivitis is a frequent, commonly benign condition that is underappreciated. Although it rarely endangers vision, it can drastically lower a patient's quality of life. Simple allergic conjunctivitis has three subtypes: acute, seasonal, and persistent. There is a lot of overlap in the etiology and management of large papillary conjunctivitis and atopic conjunctivitis atopic, and vernal keratoconjunctivitis. These are all regarded as ocular allergies as a result. Although results and complication rates differ, initial treatment approaches can sometimes be comparable.

The symptoms of allergic conjunctivitis are:

• Itchy eyes with a strong desire to rub them.

• Red eyes.

• Mucus discharge that is watery or white and stringy.

• Eyelids that are swollen.

Learn More About Alcaftadine Ophthalmic Solution 0.25%:

When to Take Alcaftadine Ophthalmic Solution 0.25 %?

• Before taking this medication, read all instructions on the product package before using it to self-treat.

• Apply this medication to both eyes once a day or as directed by the doctor.

• Before each use, the patient needs to wash their hands. Do not touch the dropper tip or allow it to contact the eye or any other surface to avoid contamination.

• This product's preservative may be absorbed by contact lenses.

• Remove the contact lenses before using this medication, and keep them out of the eyes for at least 10 minutes after each dose.

• If a person has red eyes, avoid wearing contact lenses.

How Effective Is Alcaftadine Ophthalmic Solution 0.25 %?

By using this medication, allergic eye itching can be avoided. An antihistamine is Alcaftadine. It functions by obstructing the natural chemical histamine, which causes allergic reactions. Avoid using this drug to relieve red or itchy eyes from contact lenses. If this happens, speak with the doctor for additional advice.

Things to Inform the Doctor Before They Prescribe Alcaftadine Ophthalmic Solution 0.25 %:

• Inform the doctor about any drug allergies, including Alcaftadine and any of the components in the Alcaftadine solution.

• Inform the doctor about all prescription and over-the-counter drugs, vitamins, dietary supplements, and herbal products.

• Inform the doctor about pregnancy, planning to get pregnant, or nursing a baby. Call the doctor if one becomes pregnant while taking Alcaftadine.

• If the eyes are red, be aware that the person is not wearing contact lenses.

• Alcaftadine solution contains benzalkonium chloride, which soft contact lenses can absorb.

How to Take Alcaftadine Ophthalmic Solution 0.25 %?

Starting Alcaftadine Ophthalmic Solution 0.25 %:

Tilt the head back, look up, and pull the lower eyelid down to form a pouch. Place one drop into the eye as directed by the doctor while holding the dropper directly over the eye.

• Look down, close the eyes gently, and place a finger at the corner of the eye.

• Apply gentle pressure for one to two minutes before opening the eyes. It prevents the medication from draining out.

• Avoid blinking or rubbing the eye. Then, repeat these steps for the other eye.

• Do not rinse the dropper. Replace the dropper cap after each use.

• Take the medication regularly. Use it at the same time every day.

• If this product becomes contaminated, do not use it.

• Using contaminated eye medication can result in infection, serious eye damage, and vision loss.

Things to Do After You Start Taking Alcaftadine Ophthalmic Solution 0.25 %:

• Wash hands first. Tilt the head and gently pull the lower eyelid away from the eye by pressing the finger on the skin beneath the lower eyelid.

• Place the medicine in this location. Close the eyes gently by letting go of the eyelid. Keep eyes closed.

• Keep eyes closed. Close the eyes for one to two minutes to allow the medicine to be absorbed by the eye.

• Wash hands immediately after using the eye drops to remove any medicine that may have gotten on them.

What Are the Side Effects?

The ocular side effects of Alcaftadine ophthalmic solution are

• Irritation.

• Stinging.

• Redness.

• Pruritus.

• Eye discharge.

• Eye swelling.

• Eyelid edema.

• Erythema of the eyelid.

The nonocular side effects of Alcaftadine ophthalmic solution are

• Influenza.

• Nasopharyngitis.

• Headache.

Dietary Alterations:

Certain meals and medications can interact. The doctor will advise avoiding particular foods if this is detrimental in some circumstances. There are no specific foods in the case of Alcaftadine that should be avoided in the diet when receiving this medication.

What Should Be Done When You Miss a Dose?

If one needs to remember to take a dose, take it as soon as you remember it. Skip the missed dose if the next dose is approaching. Instead, take the next dose as usual. Avoid doubling the dose to catch up.

What Should Be Done to Treat Alcaftadine Ophthalmic Solution 0.25 % Overdose?

An eye drop overdose can cause severe side effects such as headaches, eye irritation, and dry eyes. Alcaftadine may be harmful when swallowed. In an overdose, supportive measures must be implemented as needed.

How to Store Alcaftadine Ophthalmic Solution 0.25 %?

Store the bottle at room temperature, tightly closed. Keep out of the bathroom. Keep all medications out of the reach of children and pets. Do not flush medications or pour them down the drain unless otherwise directed. When this product has expired or is no longer needed, properly dispose of it. Consult the pharmacist or a waste disposal company in the area.

How to Handle Alcaftadine Ophthalmic Solution 0.25 %?

Alcaftadine ophthalmic solution 0.25 % is packaged in a low-density polyethylene bottle with an opaque white polypropylene cap. Keep the solution at 15-25°C (59-77°F).

How to Dispose of Alcaftadine Ophthalmic Solution 0.25 %?

Unwanted medications should be disposed of in a specific manner. For example, avoid flushing this medication down the toilet. Instead, a medicine take-back program is the best way to dispose of the medication.

Avoid Self-Medication:

Avoid taking medication for a condition that was not prescribed. Also, do not suggest the medication to anyone with the same symptoms because the medication may show different effects in different individuals. Instead, consult the physician, discuss with them, and then take medicine.

Staying On Alcaftadine Ophthalmic Solution 0.25 %:-

Tips to Stay On Track:

Tips to stay on track with Alcaftadine ophthalmic solution:

• Take the drug as directed by the physician.

• Do not miss a dose or overdose to compensate for a missed dose. Inform the physician immediately.

• Also, schedule regular appointments with the physician to monitor the disease progression and recommend dose adjustments.

For Doctors:-

Indication:

• Alcaftadine ophthalmic solution is used to prevent the itching of eyes due to allergies.

• Alcaftadine is an antihistamine that works by blocking histamine that is responsible for allergic symptoms.

• Avoid using this medication to treat irritated or red eyes because of wearing contact lenses.

Pharmacology:

Mechanism of Action:

Alcaftadine is an H1 histamine receptor antagonist that inhibits histamine release from mast cells. As a result, chemotaxis has been reduced, and eosinophil activation has been inhibited.

Pharmacodynamics:

Following bilateral topical ocular administration of 0.25 % Alcaftadine ophthalmic solution, Alcaftadine enters the systemic circulation, quickly falling below quantifiable plasma concentrations of 0.01 ng/mL three hours later. Maximum plasma concentrations achieved were less than 0.12 ng/mL. The primary route of Alcaftadine elimination is metabolism to the active carboxylic acid metabolite, which occurs primarily through cytosolic enzymes. After one hour after dosing, the active carboxylic acid metabolite reaches peak plasma concentrations.

Ingredients:

Active Ingredient: 0.25 % Alcaftadine (2.5 mg/mL).

Inactive Ingredients: Disodium Edetate, pure water, Monobasic Sodium Phosphate, Sodium Chloride, Hydrochloric acid, and Sodium Hydroxide.

Absorption:

The mean plasma Cmax of Alcaftadine was approximately 60 pg/mL after bilateral topical ocular administration of Alcaftadine ophthalmic solution 0.25 %, and the median Tmax occurred at 15 minutes. Three hours after dosing, plasma Alcaftadine concentrations were below the lower limit of quantification (10 pg/mL). The active carboxylic acid metabolite's mean Cmax was approximately 3 ng/mL and occurred one hour after dosing. By 12 hours after dosing, the carboxylic acid metabolite's plasma concentrations were below the lower quantification limit (100 pg/mL). Following daily topical ocular administration, there were no changes in plasma exposure to Alcaftadine or the active metabolite or evidence of systemic accumulation.

Distribution:

Alcaftadine and its active metabolite have protein binding rates of 39.2 % and 62.7 %, respectively.

Metabolism:

Non-CYP450 cytosolic enzymes mediate Alcaftadine's active carboxylic acid metabolite. However, in vitro, studies revealed that neither Alcaftadine nor its carboxylic acid metabolite significantly inhibited major CYP450 enzyme reactions.

Elimination:

The carboxylic acid metabolite has an elimination half-life of about two hours after topical ocular administration. When Alcaftadine is administered orally, the carboxylic acid metabolite is primarily eliminated unchanged. In vitro, studies revealed that neither Alcaftadine nor its carboxylic acid metabolite significantly inhibited major CYP450 enzyme reactions.

Toxicity:

Overuse of 0.25 % Alcaftadine eye drops can cause ocular surface toxicity, possibly due to drug toxicity. Therefore, all patients should be informed about the potential side effects of using 0.25 % Alcaftadine eye drops excessively.

Warning and Precaution:

• Contact Lens Use - Do not use the contact lens if the eye is red. Also, do not use it to treat contact lens-related irritation. Before installation, remove the contact lenses. After the administration of Alcaftadine, the lenses can be reinserted.

• Topical Ophthalmic Use Only - Alcaftadine is for topical use only.

• Contamination of Tip and Solution - Avoid touching eyelids or surrounding areas with the bottle dropper tip to avoid contaminating the solution and dropper tip. Close the bottle tightly when not in use.

Dosage and Forms:

Store away from moisture and heat at room temperature. Avoid freezing. Close the bottle when it is not in use.

Two years and Older: One drop should be instilled into each eye once a day.

For adults: One drop should be instilled into each eye once a day.

Administration of the Drug:

To apply the eye drops:

• Tilt the head slightly and pull down the lower eyelid. Hold the dropper above the eye. Squeeze the drop, look up and away, and then close the eyes.

• Use drops prescribed by the doctor.

• Press the finger in the corner of the eye to keep the liquid from draining.

• Wait for ten minutes before using any other eye drops as the doctor prescribes.

• Avoid touching the tip of the dropper to any surface, including the eyes or hands. There could be serious damage to the eye, or vision loss if the dropper becomes contaminated.

Considerations for Administration:

• Follow the doctor's instructions exactly. Do not use in greater or lesser quantities or for longer than recommended.

• Use this medication only if not wearing contact lenses.

• A preservative in Alcaftadine ophthalmic may discolor soft contact lenses.

• After using Alcaftadine ophthalmic, wait at least 15 minutes before putting on the contact lenses. Before applying eye medication, wash the hands.

• Avoid eye drops if the liquid has particles or has changed color.

Contraindications:

Patients with hypersensitivity or other components in the medication should avoid using Alcaftadine ophthalmic solution.

Clinical Studies for Alcaftadine Ophthalmic Solution 0.25 %:

Conjunctival allergen challenge (CAC) studies were used to assess clinical efficacy. Alcaftdine was more effective as it prevented ocular itching in patients with allergic conjunctivitis caused by an ocular allergen challenge, both three minutes and 16 hours after administration. The safety of Alcaftadine was investigated in a 6-week randomized clinical trial involving 909 subjects.

Drug Interactions:

Drug interactions can cause medications to work differently or put a person at risk for serious side effects. Keep a list of all the products, including over-the-counter medications, prescriptions, and herbal supplements, and share it with the doctor. Do not begin, stop, or modify medications without consulting the doctor.

Drug interactions with Acaftadine are as follows.

• Fexinidazole - When Alcaftadine is combined with Fexinidazole, the risk or severity of adverse effects increases.

• Fluoxetine - When Fluoxetine is combined with Alcaftadine, the risk or severity of QTc prolongation increases.

• Hydroxyzine - When Hydroxyzine is combined with Alcaftadine, the risk or severity of QTc prolongation is increased.

• Haloperidol - When Haloperidol is combined with Alcaftadine, the risk or severity of QTc prolongation is increased.

• Pitolisant - Alcaftadine may enhance Pitolisant's QTc-prolonging activities.

• Ponesimod - When Ponesimod is combined with Alcaftadine, the risk or severity of bradycardia can be increased.

• Tenofovir Alafenamide - When combined with Alcaftadine, the serum concentration of Tenofovir Alafenamide can be increased.

• Hydrocyamine - Alcaftadine may enhance Hyoscyamine's anticholinergic activity.

Other Specifications:-

Alcaftadine Ophthalmic Solution 0.25 % in Pregnant Women:

No well-controlled and adequate studies on pregnant women exist. Animal reproduction studies do not always predict human responses. Alcaftadine should be used only if necessary during pregnancy.

Alcaftadine Ophthalmic Solution 0.25 % in Lactating Women:

It is unknown whether this medication is excreted in human milk. Many drugs are excreted in human milk, and Alcaftadine should be cautiously administered to a nursing woman.

Pediatric Patients:

There is no evidence of efficacy or safety in pediatric patients under the age of two years.

Geriatric Patients:

There were no overall differences in effectiveness or safety between elderly and younger subjects.