pilocarpine ophthalmic (Rx)

Brand and Other Names:Isopto Carpine, Vuity
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

ophthalmic solution

  • 1% (Isopto Carpine; generic)
  • 1.25% (Vuity)
  • 2% (Isopto Carpine; generic)
  • 4% (Isopto Carpine; generic)

Open-Angle Glaucoma or Ocular Hypertension Intraocular Pressure

Indicated for reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension

1%, 2%, or 4% solution: Apply 1-2 gtt up to q6hr; adjust concentration and frequency as necessary to control IOP

Pilocarpine-naïve patients: Initiate with 1% concentration as higher concentrations are often not tolerated

Acute Angle-Closure Glaucoma

Prior to pilocarpine ophthalmic, treatment with secretory suppressants and hyperosmotic agents may be needed to lower IOP to <50 mmHg and relieve iris ischemia

Initial (1% or 2% solution): Instill 1 gtt to affected eye(s) up to 3 times over 30 minutes

If laser iridoplasty or iridomy is used to break the attack, 1 gtt of 4% solution should be administered before procedure

Following laser iridoplasty (1% solution): 1 gtt to affected eye(s) QID until an iridotomy can be performed

Postoperative Elevated IOP

Indicated for prevention of postoperative elevated IOP associated with laser surgery

1%, 2%, or 4% solution: Instill 1-2 gtt to eye(s) 15-60 minutes before surgery

If 2 drops administered, instill 5 minutes apart

Miosis Induction

1%, 2%, or 4% solution: Instill 1-2 gtt to eye(s)

If 2 drops administered, instill 5 minutes apart

Presbyopia

Vuity only

Indicated for the treatment of presbyopia in adults

1.25% solution: Instill 1 gtt in each eye qDay

Dosage Forms & Strengths

ophthalmic solution

  • 1% (Isopto Carpine; generic)
  • 2% (Isopto Carpine; generic)

Primary Congenital Glaucoma

For the induction of miosis before goniotomy or trabeculotomy

<2 years: Instill 1 gtt TID of 1% ophthalmic solution

≥2 years: Instil 1 gtt 15-60 minutes before surgery of 1% or 2% ophthalmic solution

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Adverse Effects

1-10%

≥5%

  • Isopto Carpine
    • Headache/brow ache
    • Accommodative change
    • Blurred vision
    • Eye irritation
    • Visual impairment (dim, dark, or “jumping” vision)
    • Eye pain
  • Vuity
    • Headache
    • Conjunctival hyperemia

1-5% (Vuity)

  • Blurred vision
  • Eye pain
  • Visual impairment
  • Eye irritation
  • Increased lacrimation
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Warnings

Contraindications

Hypersensitivity to drug or component

Cautions

Advised caution if driving at night and other hazardous occupations in poor illumination; miotics may cause accommodative spasm; caution patient not to drive or use machinery if vision is not clear

Miotics may cause rare cases of retinal detachment when used in certain susceptible individuals and those with preexisting retinal disease; thorough examination of the retina including funduscopy advised in all patients before initiating

Do not use when iritis is present

Pediatric use

  • Caution advised with use in pediatric patients with primary congenital glaucoma for control of IOP as cases of a paradoxical increase in IOP have been reported
  • Not recommended in pediatric patients diagnosed with glaucoma secondary to anterior segment dysgenesis or uveitis (especially if uveitis is active)
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Pregnancy & Lactation

Pregnancy

No adequate and well-controlled trials have been conducted in pregnant women

In a retrospective case series of 15 women with glaucoma, 4 patients used ophthalmic pilocarpine either prepregnancy, during pregnancy, or postpartum; there were no adverse effects observed in patients or in their infants

Animal studies

  • Oral administration to pregnant rats throughout organogenesis and lactation did not produce adverse effects at clinically relevant doses

Lactation

Unknown if excreted in human milk

Pilocarpine and/or its metabolites are excreted in the milk of lactating rats

Systemic levels of pilocarpine following topical ocular administration are low and it is not known whether measurable levels would be present in maternal milk following topical ocular administration

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

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Pharmacology

Mechanism of Action

The drug acts through direct stimulation of muscarinic receptors and smooth muscle including the iris and secretory glands. Contracts the ciliary muscle, causing increased tension on scleral spur and opening of trabecular meshwork spaces to facilitate outflow of aqueous humor; outflow resistance is reduced, lowering intraocular pressure (IOP).

Also produces miosis through contraction of iris sphincter muscle; miosis relieves appositional angle narrowing and closure, which lowers IOP in certain types of angle-closure glaucoma

Absorption

Isopto Carpine Day 8; 4% QID

  • Peak plasma time: 0.5-1 hr
  • Peak plasma concentration: 3.7 ng/mL
  • AUC: 7.7 ng⋅hr/mL

Vuity Day 30; once daily

  • Peak plasma time: 0.3 hr
  • Peak plasma concentration: 1.95 ng/mL
  • AUC: 4.14 ng⋅hr/mL
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Administration

Ophthalmic Administration

For topical ophthalmic use only

Avoid touching dispensing bottle to the eye or to any other surface to prevent eye injury or contamination

Contact lens wearers: Remove lenses before instillation of drops; wait 10 minutes after dose administration before reinserting contact lenses

Use with other topical ophthalmic medication

  • May be used in combination with beta-blockers, carbonic anhydrase inhibitors, sympathomimetics, or hyperosmotic agents
  • Administered ophthalmic drops at least 5 minutes apart

Storage

Isopto Carpine: Store at 20-25ºC (68-77ºF), excursions permitted to 15-30ºC (59-86ºF)

Vuity: Store at 15-25ºC (59-77ºF)

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Images

BRAND FORM. UNIT PRICE PILL IMAGE
Salagen (pilocarpine) oral
-
7.5 mg tablet
Salagen (pilocarpine) oral
-
5 mg tablet
Salagen (pilocarpine) oral
-
7.5 mg tablet
Isopto Carpine ophthalmic (eye)
-
1 % drops
Isopto Carpine ophthalmic (eye)
-
4 % drops
Isopto Carpine ophthalmic (eye)
-
2 % drops
pilocarpine ophthalmic (eye)
-
4 % drops
pilocarpine ophthalmic (eye)
-
1 % drops
pilocarpine ophthalmic (eye)
-
4 % drops
pilocarpine ophthalmic (eye)
-
1 % drops
pilocarpine ophthalmic (eye)
-
2 % drops
pilocarpine ophthalmic (eye)
-
4 % drops
pilocarpine ophthalmic (eye)
-
2 % drops
pilocarpine ophthalmic (eye)
-
1 % drops
pilocarpine ophthalmic (eye)
-
2 % drops
pilocarpine ophthalmic (eye)
-
4 % drops
pilocarpine oral
-
5 mg tablet
pilocarpine oral
-
5 mg tablet
pilocarpine oral
-
5 mg tablet
pilocarpine oral
-
5 mg tablet
pilocarpine oral
-
7.5 mg tablet
pilocarpine oral
-
7.5 mg tablet
pilocarpine oral
-
7.5 mg tablet

Copyright © 2010 First DataBank, Inc.

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Patient Handout

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Patient Education
pilocarpine oral

PILOCARPINE - ORAL

(PYE-loe-KAR-peen)

COMMON BRAND NAME(S): Salagen

USES: This medication is used to treat symptoms of dry mouth due to a certain immune disease (Sjogren's syndrome) or from saliva gland damage due to radiation treatments of the head/neck for cancer. Pilocarpine belongs to a class of drugs known as cholinergic agonists. It works by stimulating certain nerves to increase the amount of saliva you produce, making it easier and more comfortable to speak and swallow.

HOW TO USE: Take this medication by mouth with or without food, usually 3-4 times daily, or as directed by your doctor.To reduce your risk of side effects, your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor's instructions carefully.Dosage is based on your medical condition and response to treatment. If you have liver problems, your doctor may direct you to start taking this drug only twice daily. The usual maximum adult dose is 30 milligrams each day.Take this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.You may continue to drink water or use saliva substitutes as needed for moisture in your mouth.You may start to feel some benefit in 1 to 2 weeks. However, it may take up to 3 months to feel the full benefit. Tell your doctor if your condition persists or worsens.

SIDE EFFECTS: See also Precautions.Sweating, nausea, runny nose, chills, flushing, frequent urge to urinate, dizziness, weakness, diarrhea, and blurred vision may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.This medication may cause an increase in tears. This can be helpful if you have dry eyes (such as with Sjogren's syndrome). Tell your doctor if runny eyes become a problem.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if any of these unlikely but serious side effects occur: slow/fast heartbeat, shakiness (tremor), fainting, lung problems (such as increased wheezing/cough/phlegm), mental/mood changes (such as confusion, agitation), severe stomach/abdominal pain.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking this medication, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: breathing problems (such as asthma, chronic bronchitis, chronic obstructive pulmonary disease-COPD), certain eye conditions (such as night blindness, acute iritis, narrow-angle glaucoma), heart disease (such as chest pain, heart failure, heart attack, slow heartbeat), low or high blood pressure, liver problems, gallbladder disease (such as gallstones), kidney stones, mental/mood disorders (such as depression, psychoses, thinking/understanding problems like dementia, Alzheimer's), stomach problems (such as chronic heartburn, ulcer).This drug may make you dizzy or cause vision problems, especially at night. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness or clear vision, especially at night, until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).If pilocarpine makes you sweat heavily, drink plenty of fluids so that you do not become dehydrated. If you are unable to drink enough fluids, talk with your doctor right away.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Caution is advised when using this drug in the elderly because they may be more sensitive to its effects, especially dizziness, diarrhea, and increased urge to urinate.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is not known whether this drug passes into breast milk. Discuss the risks and benefits with your doctor before breast-feeding.

DRUG INTERACTIONS: The effects of some drugs can change if you take other drugs or herbal products at the same time. This can increase your risk for serious side effects or may cause your medications not to work correctly. These drug interactions are possible, but do not always occur. Your doctor or pharmacist can often prevent or manage interactions by changing how you use your medications or by close monitoring.To help your doctor and pharmacist give you the best care, be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products) before starting treatment with this product. While using this product, do not start, stop, or change the dosage of any other medicines you are using without your doctor's approval.Some products that may interact with this drug include: beta blockers (such as propranolol, metoprolol).Pilocarpine may cause drugs with "drying" effects (some antihistamines, anticholinergics such as certain drugs for asthma, over-active bladder, and Parkinson's) to work less well. Examples of affected drugs include chlorpheniramine, diphenhydramine, atropine, belladonna alkaloids, ipratropium, and tolterodine. These medications can also worsen dry mouth, causing pilocarpine to work less well. Consult your doctor or pharmacist for more information.Check the labels on all your medicines (such as cough-and-cold products) because they may contain ingredients that could have a drying effect. Ask your pharmacist for more details.This document does not contain all possible drug interactions. Keep a list of all the products you use. Share this list with your doctor and pharmacist to lessen your risk for serious medication problems.

OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: diarrhea that doesn't stop, heavy sweating, severe trouble breathing, severe wheezing, stomach cramps, vomiting, very slow/fast heartbeat, severe confusion.

NOTES: Do not share this medication with others.Keep all regular medical and laboratory appointments so that your doctor can monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

STORAGE: Store at room temperature between 68-77 degrees F (20-25 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.