Pilocarpine eye drops (Salagen) is a cholinergic receptor activating drug that causes miosis when topically used in the eyes. This reduces resistance to the aqueous humor resulting in a reduction in the intraocular pressure in patients with angle-closure glaucoma.

Pilocarpine eye drops Uses:

• Elevated intraocular pressure:
  • It is used to reduce elevated intraocular pressure (IOP) in the following conditions
    • Open-angle glaucoma
    • Ocular hypertension or
    • As part of a 4-drug medical management regimen in acute angle-closure glaucoma when the patient cannot be seen by an ophthalmologist for ≥1 hour (off label use)
• Miosis:
  • Induction of miosis
• Prevention of postoperative elevated IOP:
  • It is used to prevent elevation of IOP associated with laser surgery after the operation

Pilocarpine eye drops Dose in Adults:

Pilocarpine eye drops Dose in the treatment of Elevated intraocular pressure: Ophthalmic:

• Open-angle glaucoma:
  • 1 drop of 1%, 2%, or 4% solution in eye(s) up to 4 times a day
  • In pilocarpine-naive patients start with 1% concentration.
• Angle-closure glaucoma, acute:
  • 1 drop of 2% solution in the affected eye as part of a 4-drug regimen
  • It can be repeated in 30 - 60 minutes if IOP remains elevated (eg, >40 mm Hg).

Pilocarpine eye drops Dose in the treatment of Miosis:

• Ophthalmic:
  • 1 drop (or 2 drops 5 minutes apart) of 1%, 2%, or 4% solution in affected eye(s)

Pilocarpine eye drops Dose in the Prevention of postoperative elevated IOP:

• Ophthalmic:
  • 1 drop (or 2 drops 5 minutes apart) of 1%, 2%, or 4% solution in affected eye(s) 15 - 60 minutes before surgery

Pilocarpine eye drops Dose in  Childrens

Pilocarpine eye drops Dose in the treatment of open-angle glaucoma and elevated intraocular pressure:

• Infants and Children <2 years:
  • Ophthalmic: 1% Solution: 1 drop in affected eye(s) 3 times a day
• Children ≥2 years and Adolescents:
  • Note: Individualize Solution strength and frequency of instillation. It depends on degree of pressure elevation and patient miotic response.
  • Ophthalmic: 1%, 2%, or 4% solution:
    • one drop in affected eye(s) up to 4 times a day
  • Pilocarpine-naive patients, Start with the 1% concentration

Pilocarpine eye drops Dose in the treatment of acute angle-closure glaucoma:

• Infants and Children <2 years:
  • Ophthalmic: 1% solution:1 drop in affected eye(s) 3 times a day
• Children ≥2 years and Adolescents:
  • Ophthalmic: 1% or 2% solution: Initial: 1 drop in affected eye(s) up to 3 times over a 30-minute period
  • Premedication with secretory suppressants and hyperosmotic may be needed to lower intraocular pressure to less than 50 mm Hg and relieve iris ischemia
  • If laser iridoplasty or iridomy is required, 1 drop of 4% solution before the procedure; after laser iridoplasty, 1 drop of 1% solution 4 times a day until an iridotomy can be performed.

Pilocarpine eye drops Dose in the treatment of Miosis induction before goiniotomy or trabeculectomy:

• Infants and Children:
  • Ophthalmic: 1% or 2% solution:
    • 1 drop in the eye(s) 15 - 60 minutes before surgery
• Adolescents:
  • Ophthalmic: 1%, 2%, or 4% solution:
    • 1 or 2 drops in the affected eye 5 minutes apart.

Pregnancy Risk Factor C

• Studies on animal reproduction have not been done.

Pilocarpine use during breastfeeding:

• It is unknown if pilocarpine is excreted in breast milk.
• Pilocarpine (ophthalmic) should be administered with caution to women who are lactating.

Dose in Kidney Disease:

Manufacturer has not provided dose adjustment in labeling.   

Dose in Liver disease:

Manufacturer has not provided dose adjustment in labeling.   

Side effects of Pilocarpine eye drops:

• Cardiovascular:
  • Hypertension
  • Tachycardia
• Gastrointestinal:
  • Diarrhea
  • Nausea
  • Salivation
  • Vomiting
• Ocular:
  • Burning
  • Ciliary spasm
  • Conjunctival Vascular Congestion
  • Corneal Granularity (Gel 10%)
  • Lacrimation
  • Lens Opacity
  • Myopia
  • Retinal Detachment
  • Supraorbital Or Temporal Headache
  • Visual Acuity Decreased
• Respiratory:
  • Bronchial Spasm
  • Pulmonary Edema
• Miscellaneous:
  • Diaphoresis

Contraindications to Pilocarpine eye drops:

The manufacturer has not indicated any contraindications on the labeling.

Canadian labeling:

• Hypersensitivity to any pilocarpine content
• Acute iritis and anterior uveitis are conditions where pupillary constriction can be undesirable.

Warnings and precautions

• Ophthalmic effects
  • Pilocarpine may cause visual impairment, especially at night and with less light. Avoid driving at night, or working in occupations that require low illumination.
  • Miotics may cause accommodative spasm.
• Asthma
  • Asthma: Use caution
• Cardiovascular disease
  • Cholinergic drugs for the eyes may exacerbate myocardial dysfunction (American Heart Association). 
  • Avoid use in cases of acute heart failure, recent cardiac infarction (MI), hypertension or hypotension.
• GI disease:
  • Avoid GI spasm or peptic ulcer disease.
• Hyperthyroidism:
  • Hyperthyroidism: Use caution
• Ocular inflammation:
  • If the patient has itchis, do not use. Acute inflammatory diseases of anterior chamber should not be treated with miotics.
• Parkinson disease
  • Parkinson's disease: Be cautious
• Retinal disease
  • Retinal detachment is rare. Patients with previous retinal disease should be cautious. Before beginning therapy, it is advisable to have a thorough examination of the retina.
• Occlusion of the urinary tract:
  • If the patient has a blocked urinary tract, be cautious.

Pilocarpine (ophthalmic): Drug Interaction

Monitoring parameters:

• Intraocular pressure for acute angle closure glaucoma after 30 - 60 minutes of pilocarpine
• Funduscopic exam before starting the therapy
• Visual field testing

How to administer Pilocarpine eye drops?

Ophthalmic:

• Gently apply pressure with fingers to the lacrimal sac for 2 minutes after administration
• Remove contact lenses before instillation and wait 10 - 15 minutes before reinserting.
• Avoid instillation of multiple drugs together, Separately administer other ophthalmic agents by at least 5 minutes apart
• When treating acute angle-closure glaucoma, separate administration of other ophthalmic agents by more than 1 minute
• Avoid contact of the tip of the dropper to the eye, fingertips, or other surfaces.

Mechanism of action of Pilocarpine (Salagen):

It can cause miosis through direct stimulation of the cholinergic receptors (by contraction iris sphincter), loss accommodation (due constriction ciliary muscle), and lowers intraocular pressure (due reduced resistance to the flow aqueous humor).

The beginning of action

• Miosis: 10 - 30 minutes;
• Intraocular pressure drops: 1 hour

Peak effect:

• 0.5 - 1 hour

Duration:

• Miosis: 4 - 8 hours;
• Intraocular pressure reduction: 4 - 12 hours

International Brand Names of Pilocarpine eye drops:

• Isopto Carpine
• Odan-Pilocarpine
• Apicarpine
• Asthenopin
• Carpine
• Isopto Carpina
• Isopto Carpine
• Isopto Pilocarpina
• Isopto Pilocarpine
• Isopto-Carpine
• Liocarpina
• Locarp
• Medicarpine
• Miokar
• P.D.
• OcuCarpine
• Ocucarpine
• Ocusert Pilo-20
• Ocusert Pilo-40
• Ocusert Pilocarpine
• Oftan-Pilocarpin
• V. Carpine Liquifilm Ophthalimic Solution
• Pil Ofteno
• Pilo
• Pilocan
• Pilocar
• Pilocarpol
• Pilogel
• Pilogel HS
• Pilokarpin
• Pilomann
• Pilomin
• Pilopes
• Pilopine-HS
• Pilopos
• Pilopt Eye Drops
• Pilotina
• Pilotonina
• Sno Pilo
• Spersacarpin
• Spersacarpine
• Zhenrui

Pilocarpine eye drops Brand Names in Pakistan: