Pilocarpine (ophthalmic)
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Adeel Jamil, M.D. [2]
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Overview
Pilocarpine (ophthalmic) is a cholinergic agent that is FDA approved for the treatment of reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension, acute angle-closure glaucoma, prevention of postoperative elevated IOP associated with laser surgery and induction of miosis. Common adverse reactions include headache, accommodative change, blurred vision, eye irritation, visual impairment and eye pain..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
- Pilocarpine Hydrochloride Ophthalmic Solution is indicated for the:
- Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension
- Management of acute angle-closure glaucoma
- Prevention of postoperative elevated IOP associated with laser surgery
- Induction of miosis
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Pilocarpine (ophthalmic) in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Pilocarpine (ophthalmic) in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Pilocarpine (ophthalmic) FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Pilocarpine (ophthalmic) in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Pilocarpine (ophthalmic) in pediatric patients.
Contraindications
- None.
Warnings
Poor Illumination
- Patients should be advised to exercise caution in night driving and other hazardous occupations in poor illumination. In addition, miotics may cause accommodative spasm. Patients should be advised not to drive or use machinery if vision is not clear.
Pre-existing Retinal Disease
- As with all miotics, rare cases of retinal detachment have been reported when used in certain susceptible individuals and those with pre-existing retinal disease; therefore, a thorough examination of the retina including funduscopy is advised in all patients prior to the initiation of therapy.
Iritis
- Pilocarpine Hydrochloride Ophthalmic Solution is not recommended to be used when iritis is present.
Primary Congenital Glaucoma
- Caution is advised when using Pilocarpine Hydrochloride Ophthalmic Solution in pediatric patients with primary congenital glaucoma for control of intraocular pressure (IOP) as cases of a paradoxical increase in IOP have been reported. In addition, the use of Pilocarpine Hydrochloride Ophthalmic Solution is not recommended in pediatric patients diagnosed with glaucoma secondary to anterior segment dysgenesis or uveitis (especially if uveitis is active).
Contact Lens Wear
- Contact lens wearers should be advised to remove their lenses prior to the instillation of Pilocarpine Hydrochloride Ophthalmic Solution and to wait 10 minutes after dosing before reinserting their contact lenses.
Adverse Reactions
Clinical Trials Experience
- Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
- The safety data described below reflect exposure in four controlled clinical trials of 90 days to 2 years duration in 317 patients diagnosed with open-angle glaucoma or ocular hypertension. In the four clinical trials, patients were treated with Pilocarpine Hydrochloride Ophthalmic Solution 2%, two to four times daily or with Pilocarpine Hydrochloride Ophthalmic Solution 1%, 1.75% or 2% in fixed combination with betaxolol 0.25%, two or three times daily. The most frequently reported adverse reactions occurring in ≥ 5% of patients in the pilocarpine 2% populations were: headache/browache, accommodative change, blurred vision, eye irritation, visual impairment (dim, dark, or "jumping" vision), and eye pain.
- The adverse reaction profile reported for the use of Pilocarpine Hydrochloride Ophthalmic Solution in pediatric patients is comparable to that seen in adult patients.
Postmarketing Experience
There is limited information regarding Pilocarpine (ophthalmic) Postmarketing Experience in the drug label.
Drug Interactions
There is limited information regarding Pilocarpine (ophthalmic) Drug Interactions in the drug label.
Use in Specific Populations
Pregnancy
- Animal reproduction studies have not been conducted with pilocarpine hydrochloride. It is also not known whether pilocarpine hydrochloride can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Pilocarpine Hydrochloride Ophthalmic Solution should be given to a pregnant woman only if clearly needed.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Pilocarpine (ophthalmic) in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Pilocarpine (ophthalmic) during labor and delivery.
Nursing Mothers
- It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Pilocarpine Hydrochloride Ophthalmic Solution is administered to a nursing woman.
Pediatric Use
- Safety and effectiveness of pilocarpine hydrochloride ophthalmic solution in pediatric patients have been established.
Geriatic Use
- No overall differences in safety or effectiveness have been observed between elderly and younger patients.
Gender
There is no FDA guidance on the use of Pilocarpine (ophthalmic) with respect to specific gender populations.
Race
There is no FDA guidance on the use of Pilocarpine (ophthalmic) with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Pilocarpine (ophthalmic) in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Pilocarpine (ophthalmic) in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Pilocarpine (ophthalmic) in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Pilocarpine (ophthalmic) in patients who are immunocompromised.
Administration and Monitoring
Administration
- Ophthalmic
Monitoring
There is limited information regarding Pilocarpine (ophthalmic) Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Pilocarpine (ophthalmic) and IV administrations.
Overdosage
- Systemic toxicity following topical ocular administration of pilocarpine is rare, but occasionally patients who are sensitive may develop sweating and gastrointestinal overactivity following the suggested dosage and administration. Overdosage can produce sweating, salivation, nausea, tremors and slowing of the pulse and a decrease in blood pressure. In moderate overdosage, spontaneous recovery is to be expected and is aided by intravenous fluids to compensate for dehydration. For patients demonstrating severe poisoning, atropine, the pharmacologic antagonist to pilocarpine, should be used.
Pharmacology
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Pilocarpine (ophthalmic)
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| Systematic (IUPAC) name | |
| (3S,4R)-3-Ethyl-4-((1-methyl-1H-imidazol-5-yl)methyl)dihydrofuran-2(3H)-one | |
| Identifiers | |
| CAS number | 54-71-7 (hydrochloride) |
| ATC code | N07 S01EB01 (WHO) |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox |
| Mol. mass | 208.257 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 0.76 hours (5 mg), 1.35 hours (10 mg)[1] |
| Excretion | urine |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status |
Prescription Only (S4)(AU) [[Prescription drug|Template:Unicode-only]](US) |
| Routes | gtts, p.o. |
Mechanism of Action
- Pilocarpine hydrochloride is a direct acting cholinergic parasympathomimetic agent which acts through direct stimulation of muscarinic receptors and smooth muscle such as the iris and secretory glands.
- Pilocarpine contracts the ciliary muscle, causing increased tension on the scleral spur and opening of the trabecular meshwork spaces to facilitate outflow of aqueous humor. Outflow resistance is reduced, lowering intraocular pressure (IOP). Pilocarpine also produces miosis through contraction of the iris sphincter muscle. Miosis relieves appositional angle narrowing and closure, which lowers IOP in certain types of angle-closure glaucoma.
Structure
- Pilocarpine Hydrochloride Ophthalmic Solution is a cholinergic agonist prepared as a sterile topical ophthalmic solution. The active ingredient is represented by the chemical structure:
Pharmacodynamics
There is limited information regarding Pilocarpine (ophthalmic) Pharmacodynamics in the drug label.
Pharmacokinetics
- Systemic exposure to pilocarpine was evaluated in 14 healthy subjects administered 2 drops of pilocarpine hydrochloride ophthalmic solution 4% to both eyes four times daily for eight days. A comparison of Cmax values on Days 5 and 8 indicated that pilocarpine concentrations in plasma reached steady-state following topical administration of Pilocarpine Hydrochloride Ophthalmic Solution 4%. The mean (SD) Cmax and AUC0-last values on Day 8 were 3.7 (3.2) ng/mL and 7.7 (8.4) ngxhour/mL, respectively. The Tmax values on Day 8 ranged from 0.5 to 1 hour.
Nonclinical Toxicology
There is limited information regarding Pilocarpine (ophthalmic) Nonclinical Toxicology in the drug label.
Clinical Studies
- In clinical trials reported in the medical literature, pilocarpine ophthalmic solution reduced intraocular pressure (IOP) by 3-7 mmHg in patients with open-angle glaucoma. Pilocarpine ophthalmic solution has also been shown to be effective in the induction of miosis, in the prevention of postoperative elevated IOP, and in the management of acute angle-closure glaucoma.
How Supplied
- Pilocarpine Hydrochloride Ophthalmic Solution 1%, 2% and 4% is supplied sterile in natural low density polyethylene plastic ophthalmic DROP-TAINER®* dispensers and green low density polyethylene tips with green polypropylene caps.
15 mL in 15 mL bottles
1%: NDC 61314-203-15
2%: NDC 61314-204-15
4%: NDC 61314-206-15
Storage
Store at 15°- 25°C (59° - 77°F) and protect from freezing.
Images
Drug Images
{{#ask: Page Name::Pilocarpine (ophthalmic) |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}
Package and Label Display Panel
NDC 61314-203-15 Rx Only
FALCON
PHARMACEUTICALS®
Pilocarpine
Hydrochloride
Ophthalmic
Solution
1%
15 mL STERILE
AFFILIATE OF QUALITY RX
ALCON
LABORATORIES, INC.
{{#ask: Label Page::Pilocarpine (ophthalmic) |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}
Patient Counseling Information
Avoiding Contamination of the Product
- Do not touch dropper tip to any surface, as this may contaminate the contents.
Night Driving
- Caution is advised with night driving and when hazardous activities are undertaken in poor illumination.
Accommodative Spasm
- Pilocarpine Hydrochloride Ophthalmic Solution may cause problems when changing focus between near objects and distant objects. Do not drive or use machinery if vision is not clear.
Contact Lens Wear
- Contact lens should be removed prior to the instillation of Pilocarpine Hydrochloride Ophthalmic Solution. Wait 10 minutes after dosing before reinserting contact lenses.
Concomitant Topical Ocular Therapy
- If more than one topical ophthalmic medication is being used, the medicines must be administered at least 5 minutes apart.
Systemic Exposure
- To limit exposure to pilocarpine to the eye alone, close eyes gently and apply pressure with finger to the corner of eye by the nose for 2 minutes after instillation of Pilocarpine Hydrochloride Ophthalmic Solution.
Rx Only
Printed in USA
- DROP-TAINER is a registered trademark of Alcon Research, Ltd.
Dist. By:
Falcon Pharmaceuticals, Ltd.
Fort Worth, Texas 76134 USA
Mfd. by:
Alcon Laboratories, Inc.
6201 South Freeway
Fort Worth, Texas 76134 USA
1-800-757-9195
9006010-1010
Precautions with Alcohol
Alcohol-Pilocarpine (ophthalmic) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Pilocarpine (ophthalmic) Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Pilocarpine (ophthalmic) Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.
- ↑ Mervyn Gornitsky, George Shenouda, Khalil Sultanem, Howard Katz, Michael Hier, Martin Black, Ana M Velly (2004). "Double-blind randomized, placebo-controlled study of pilocarpine to salvage salivary gland function during radiotherapy of patients with head and neck cancer". Oral Surgery, Oral Medicine, Oral Pathology, Oral Radiology and Endodontology. 98 (1): 45–52.