Pilocarpine Hydrochloride Ophthalmic Solution - Uses, Dosage, and Side Effects

Overview:

Pilocarpine hydrochloride solution is a cholinergic muscarinic receptor agonist that contracts the muscle of iris sphincter, the pupil constricting to enhance nearest and intermediate visual acuity while keeping some pupillary response to light. It also contracts the muscle ciliary and might shift the eye to a myopic state. It is the first approved eyedrop by the FDA. The FDA acceptance of Pilocarpine hydrochloride ophthalmic solution is based on two key phases of three clinical studies, GEMINI 1 and GEMINI 2, which assessed the effectiveness, safety, and tolerability of Pilocarpine hydrochloride ophthalmic solution for the management of presbyopia.

How Does Pilocarpine Hydrochloride Ophthalmic Solution Work?

Presbyopia is a condition of loss of the eye’s capability to focus on near objects and occurs as a part of aging. Pilocarpine hydrochloride ophthalmic solution acts by inducing the eye pupil to constrict, which may assist with noticing or watching things nearly.

Pilocarpine hydrochloride is a cholinergic muscarinic agonist that triggers muscarinic receptors in smooth muscles like the iris sphincter and ciliary muscle. Pilocarpine hydrochloride ophthalmic solution contracts the muscle iris sphincter, tightening the pupil to enhance adjacent and middle visual acuity while keeping some pupillary response to light. Pilocarpine hydrochloride ophthalmic solution contracts the muscles of the ciliary and shifts the eye to a more myopic state.

Uses of Pilocarpine Hydrochloride Ophthalmic Solution:

Pilocarpine hydrochloride ophthalmic solution is used for the management of presbyopia in grown-ups.

Contraindication:

Pilocarpine hydrochloride ophthalmic solution is contraindicated in cases with understood hypersensitivity to the functional ingredient or to any of the excipients.

Dosage and Administration:

The advised dosage of Pilocarpine hydrochloride ophthalmic solution is one drop in individually on the eye one time daily. if more topical ophthalmic product is utilized, the products should be taken five minutes apart.

Dosage Forms and Strengths:

Pilocarpine hydrochloride ophthalmic solution is supplied as a 1.25 % solution which is 12.5 mg/mL.

Warnings and Precautions

• Poor Illumination- Patients are instructed to exert caution in night driving and additional hazardous works in poor illumination. In addition, miotics may cause accommodative spasms. They must be advised not to drive or use machinery if their vision is unclear.

• Risk of Retinal Detachment- Infrequent subjects of retinal detachment are notified with other miotics while utilized in sensitive individuals and in cases with pre-existing retinal disorders. Patients are recommended to aspire prompt medical care with the impulsive commencement of vision loss.

• Iritis- Pilocarpine hydrochloride ophthalmic solution is not suggested to be utilized when iritis is there due to adhesions, or synechiae may develop between the lens and the iris.

• Use with Contact Lenses- Contact lens users are instructed to vacate their lenses before the installation of Pilocarpine hydrochloride ophthalmic solution and to remain 10 minutes after dosing before replacing their contact lenses.

• Potential for Eye Injury or Contamination- To control eye damage or contamination, consideration should be handled to prevent touching the dispensing bottle to the eye or any further areas.

Adverse Reactions

Hypersensitivity is the main adverse reaction of the Pilocarpine hydrochloride ophthalmic solution.

Clinical Trials Experience

Due to the clinical trials being executed under widely differing situations, adverse reaction rates seen in the clinical practices of a medicine cannot instantly correspond to rates in the clinical trials of other medications. They may not reflect the rates noticed in the procedure. Pilocarpine hydrochloride ophthalmic solution was assessed in 375 cases with presbyopia in two randomized, double-masked, vehicle-controlled analyses that involved GEMINI (genetic evaluation of multimorbidity towards individualization of interventions) 1 and GEMINI 2 of thirty days duration. The most typical adverse reactions noted in more than five percent of cases were headache and conjunctival hyperemia. Ocular adverse responses noted in one to five percent of cases were blurred vision, pain in the eye, visual impairment, eye disturbance, and advanced lacrimation.

Use in Specific Populations

Pregnancy- There are no satisfactory and well-controlled studies. Pilocarpine hydrochloride ophthalmic solution has been performed in pregnant women. Oral intake of Pilocarpine in pregnant rats throughout organogenesis created maternal toxicity, anomalies in the skeletal system, and a deduction in fetal weight by 90 milligrams per kilogram per day. In a perinatal or postnatal analysis in rats, oral intake of Pilocarpine at the time of late gestation through lactation improved the rate of stillbirths at a dosage of 36 milligrams/kilogram/day. Reduced neonatal survival and decreased mean body weight of pups are reported at greater than or equal to eighteen mg/kg/day.

Lactation-There are no details available regarding the presence of Pilocarpine in human milk, the impacts on infants, or the consequences on milk production to disclose the risk of Pilocarpine hydrochloride ophthalmic solution to an infant at the time of lactation. The developmental and health advantages of breastfeeding are evaluated, as the mother’s clinical requirement for Pilocarpine hydrochloride ophthalmic solution and any adverse impacts on the breastfed child from Pilocarpine hydrochloride ophthalmic solution.

Pediatric Use- Presbyopia is a condition that does not appear in the pediatric population.

Geriatric Use- Certain notified clinical knowledge with Pilocarpine hydrochloride ophthalmic solution has not identified overall differences in security between old and young cases.

For Patients:

What Are the Uses of Pilocarpine Hydrochloride Ophthalmic Solution?

Pilocarpine hydrochloride ophthalmic solution is used in a condition of age-associated far-sightedness called presbyopia. It is a condition in which the eye lens fails its capacity to focus, creating difficulty in visualizing things up close.

How Should One Take Pilocarpine Hydrochloride Ophthalmic Solution?

• Pilocarpine hydrochloride ophthalmic solution is a 1.25 % solution to instill the eyes used to manage presbyopia. For the management of presbyopia, one drop of the 1.25 % solution is typically infused into the involved eyes one time a day. Observe the instructions on the prescription label thoroughly, and request the doctor clarify any element. Usage of Pilocarpine eye drops should be done precisely as mandated. Do not use an additional dose or a smaller dose or utilize it more frequently than specified by the doctor.

• Pilocarpine eye drops to manage the disease, but they will not fix it. Resume to utilize Pilocarpine eye drops even if one senses better. Do not quit utilizing Pilocarpine eye drops without discussing it with the doctor.

• In case of usage with another topical eye medication, instill it at least five minutes prior to or after Pilocarpine eye drops.

• Be cautious not to touch the bottle tip to the eyes, finger, face, or any other surfaces. If the tip touches another exterior region, bacteria may reach into the eye drops.

To Instill the Eye Drops, Follow These Instructions:

• First, wash the hands entirely with soap or any other disinfectant solution.

• Check the tip of the dropper to ensure it is not a damaged one.

• Do not touch the dropper tip against the eyes or anything else; eye drops and droppers should be maintained clean.

• While tilting the head around, pull down the lower lid of the eye with the index finger to develop a pocket.

• Maintain the dropper with the other hand close to the eye without touching it.

• Brace the other fingers of that hand against the face.

• While glancing up, slowly squeeze the dropper to make a single drop plunge into the pocket created by the lower eyelid. Take off the index finger from the lower eyelid.

• Close the eyes for two to three minutes and tilt the head down. Attempt not to blink or press the eyelids.

• Keep a finger on the tear duct, and gentle pressure is applied for two minutes.

• Wipe extra liquid from the face with a tissue.

• If you are to utilize more than a single drop in the same eye, wait at least five minutes prior to instilling the following drop.

• Substitute and compress the dropper bottle cap. Do not wipe the dropper tip.

• Clean the hands to clear any medication.

What Special Precautions Should Be Followed While Using Pilocarpine Hydrochloride Ophthalmic Solution?

• Inform the doctor and pharmacist in case of allergy to Pilocarpine, additional medications, or any components in the pilocarpine eye drops. Request the druggist for a checklist of the ingredients.

• Inform the doctor and pharmacist what medicine and nonprescription medicines, vitamins, nutritional complements, and herbal derivatives you plan to take while using Pilocarpine ophthalmic. The doctor may need to change the doses of the medicines or observe thoroughly for side effects.

• Inform the physician if the patient has or has a medical history of acute iritis like uveitis, swelling, and irritation of the inner part of the eye or retinal detachment.

• Notify the doctor in case of pregnancy, planning to become pregnant, or breastfeeding. If the patient becomes pregnant while using Pilocarpine eye drops, contact the doctor.

• Patients should have that Pilocarpine eye drops should not be instilled while they are using contact lenses. If the patient has contact lenses, clear them prior to using pilocarpine eye drops, they may place them back in ten minutes later.

• Patients should know that Pilocarpine eye drops may induce alteration in vision, especially at night or when there is inadequate light. Be careful if traveling at night or when accomplishing dangerous exercises in low lighting.

What to Do in Case of Missed Dose?

Instill or use the missed dose immediately when you recall it. Nevertheless, if it is almost time for the following dose, ignore the missed dosage and resume your standard dosing schedule. Do not use a double dose to compensate for a missed one.

What Side Effects Can This Medication Cause?

Pilocarpine eye drops or eye gel may induce side effects. Inform your doctor if there is any manifestation that is severe and does not go on its own-

• Blurred vision.

• Stinging sensation, burning sensation, or discomfort in the eye.

• Itching in the eye.

• Swelling of the eye.

• Headache.

A few side effects can be severe. If you feel any of the following manifestations, inform your doctor instantly:

• Sudden loss of vision.

• Sweating.

• Nausea and vomiting.

• Diarrhea.

How Is the Storage and Disposal of Pilocarpine Hydrochloride Done?

• Maintain the medicine in the receptacle it arrived in, tightly sealed and out of reach of kids. Keep it at room temperature and out from extra heat and moisture. It should not be kept in the bathroom.

• It is significant to maintain all medicine out of view and in contact with kids as many receptacles like weekly pill minders and those for eye drops, creams, patches, and inhalers are not child-immune, and young kids can unlock them efficiently. To guard young kids against poisoning, constantly lock protection caps and instantly put the medicine in a safe area that is up and out of their view and contact.

• Unnecessary medicines should be disposed of in particular methods to confirm that pets, children, and other individuals cannot swallow them. Nevertheless, you should not wash this medicine down the toilet. Rather, the best method to dispose of your medicine is via a medicine take-back program. Speak to your pharmacist or reach your local garbage department to understand take-back schedules in your community.

How to Manage Pilocarpine Hydrochloride Overdose?

Call the poison control helpline for an overdose patient, and reports are also known online. If the victim has crumpled, had a seizure, has difficulty breathing, or can not be aroused, instantly contact emergency services. Symptoms of overdose involve-

• Sweating.

• Nausea.

• Tremors.

• Mouth watering.

• Slow heart rate.

What Are the General Things That Should Be Informed to the Patient While Taking Pilocarpine Hydrochloride Ophthalmic Solution?

• Maintain all meetings with your doctor. Your doctor will compose specific eye tests to review your reaction to pilocarpine eye drops.

• Do not allow anyone else to utilize your medicine. Request your pharmacist for any queries you have about replenishing your medication.

• It is significant for you to maintain a documented list of all of the medicine and nonprescription medications you are having, as well as any by-products such as vitamins, minerals, and supplements. You should obtain this list every time you visit a doctor or are admitted to a hospital. It is also significant knowledge to carry with you in circumstances of emergencies.

For Doctors

Clinical Pharmacology

• Mechanism of Action- Pilocarpine hydrochloride, a cholinergic muscarinic agonist that triggers muscarinic receptors in smooth muscles like the iris sphincter muscle and ciliary muscle. Pilocarpine hydrochloride contracts the iris sphincter muscle, constricting the pupil to enhance adjacent and intermediate visual acuity while maintaining pupillary response to light. Pilocarpine hydrochloride contracts the ciliary muscle and may redirect the eye to a more myopic state.

• Pharmacokinetics- Systemic exposure to Pilocarpine was assessed in twenty-two individuals with Presbyopia. They were allocated one drop of Pilocarpine hydrochloride in each eye once per day for thirty days. The median Tmax value on day thirty was 0.3 hours post-dose, with an average of 0.2 to 0.5 hours post-dose.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis- Pilocarpine did not cause tumors in mice at any dose level examined. In mice, an oral dose of 18 mg/kg/day causes a statistically considerable upsurge in the chance of benign pheochromocytomas in both male and female rats and a statistically important upsurge in the chance of hepatocellular adenomas in female rats.

Mutagenesis- Pilocarpine had not revealed any possibility to induce genetic toxicity in a sequence of studies.

Impairment of Fertility- Pilocarpine on oral administration to male and female rats at a dose of 18 mg/kg/day induced deformed reproductive function, involving decreased fertility, reduced sperm motility, and morphologic proof of abnormal sperm.

Clinical Studies:

The effectiveness of Pilocarpine for the management of Presbyopia was explained in two 30-day Phase three, randomized, double-masked, vehicle-controlled analyses, that is, GEMINI one and GEMINI two. A final of 750 cases aged 40 years to 55 years old with presbyopia were randomized in two analyses. Participants were advised to take one drop of Pilocarpine or vehicle daily in each eye. In these two analyses, the ratio of participants achieving three lines or more in mesopic, high contrast, binocular space restored close visual acuity, without failing more than one line of repaired distance visual acuity with the same refractive correction was statistically significantly greater in the Pilocarpine group approximated to the group at day 30.

How to Supply or Storage and Handling?

Pilocarpine is provided as a sterile ophthalmic solution in uncolored low-density polyethylene ophthalmic dispenser bottles and tips, with shady green high-effect polystyrene caps as observed:

2.5 mL fill in five mL bottle - box involves one bottle.

NDC 0074-7098-01

2.5 mL fill in five mL bottles - a box containing three bottles.

NDC 0074-7098-03

2.5 mL fill in a five mL bottle - carton.

NDC 0074-7098-04

Storage:

Store at 15°Celsius to 25°Celsius which is 59°Fahrenheit to 77°Fahrenheit. After opening the seal, Pilocarpine can be utilized until the expiration date that is present on the bottle.

Patient Counseling Information

Night Driving- A warning is suggested with night driving and when dangerous actions are essayed in poor illumination.

Accommodative Spasm- Transient difficulties when switching focus between adjacent things and faraway objects may happen. Inform patients not to drive or utilize machinery if their vision is not clear.

When to Seek Physician Advice- Advise patients to seek prompt medical consideration with the impulsive beginning of vision loss.

Contact Lens Wear- Contact lenses are cleared before the installation of Pilocarpine. Wait 10 minutes after dosing prior to replacing contact lenses.

Avoiding Contamination of the Product- Do not touch the dropper tip part in any region, as this may spoil or pollute the contents.

Concomitant Topical Ocular Therapy- If more topical ophthalmic medication is being utilized, the drugs must be administered at least five minutes apart.