PILOCARPINE HYDROCHLORIDE 
PILOCARPINE NITRATE
(pye-loe-kar'peen)
Adsorbocarpine, Isopto Carpine, Minims Pilocarpine  , Miocarpine , Ocusert, Pilo, Pilocar, Salagen
Classifications: eye preparation; miotic (antiglaucoma agent); autonomic nervous system agent; direct-acting cholinergic (parasympathomimetic)
Pregnancy Category: C
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0.25%, 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 8%, 10% ophthalmic solution; 4% ophthalmic gel; 20 mcg/h, 40 mcg/h ocular insert; 5 mg tablets
Tertiary amine that acts directly on cholinergic receptor sites, thus mimicking acetylcholine. Induces miosis, spasm of accommodation,
and fall in intraocular pressure (IOP) that may be preceded by a transitory rise.
Decrease in IOP results from stimulation of ciliary and papillary sphincter muscles, which pull iris away from filtration
angle, thus facilitating outflow of aqueous humor. Also decreases production of aqueous humor.
Open-angle and angle-closure glaucomas; to reduce IOP and to protect the lens during surgery and laser iridotomy; to counteract
effects of mydriatics and cycloplegics following surgery or ophthalmoscopic examination; to treat xerostomia.
Secondary glaucoma, acute iritis, acute inflammatory disease of anterior segment of eye; pregnancy (category C), lactation.
Bronchial asthma; hypertension. Ocular therapeutic system: Not used in acute infectious conjunctivitis, keratitis, retinal detachment, or when intense miosis is required.
Acute Glaucoma
Adult/Child: Ophthalmic 1 drop of 1–2% solution in affected eye q5–10min for 3–6 doses, then 1 drop q1–3h until IOP is reduced
Chronic Glaucoma
Adult/Child: Ophthalmic 1 drop of 0.5–4% solution in affected eye q4–12h or 1 ocular system (Ocusert) q7d
Miotic
Adult/Child: Ophthalmic 1 drop of 1% solution in affected eye
Xerostomia
Adult: PO 5 mg t.i.d., may increase up to 10 mg t.i.d.
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Instillation
- Note: During acute phase, physician may prescribe instillation of drug into unaffected eye to prevent bilateral attack of acute
glaucoma.
- Apply gentle digital pressure to periphery of nasolacrimal drainage system for 1–2 min immediately after instillation
of drops to prevent delivery of drug to nasal mucosa and general circulation.
CNS: Oral (asthenia, headaches, dizziness, chills). Special Senses: Ciliary spasm with brow ache, twitching of eyelids, eye pain with change in eye focus, miosis, diminished vision in poorly illuminated areas, blurred vision, reduced visual acuity, sensitivity, contact allergy, lacrimation, follicular conjunctivitis, conjunctival
irritation, cataract, retinal detachment. GI: Nausea, vomiting, abdominal cramps, diarrhea, epigastric distress, salivation. Respiratory: Bronchospasm, rhinitis. CV: Tachycardia. Body as a Whole: Tremors, increased sweating, urinary frequency.
Drug: The actions of pilocarpine and carbachol are additive when used concomitantly. Oral form may cause conduction disturbances with beta blockers. Antagonizes the effects of concurrent anticholinergic drugs (e.g., atropine, ipratropium). Food: high-fat meal decreases absorption of pilocarpine.
Absorption: Topical penetrates cornea rapidly; readily absorbed from GI tract. Onset: Miosis 10–30 min; IOP reduction 60 min; salivary stimulation 20 min. Peak: Miosis 30 min; IOP reduction 75 min; salivary stimulation 60 min. Duration: Miosis 4–8 h; IOP reduction 4–14 h (7 d with Ocusert); salivary stimulation 3–5 h. Metabolism: Inactivated at neuronal synapses and in plasma. Elimination: Excreted in urine. Half-Life: 0.76–1.35 h.
Assessment & Drug Effects
- Be aware that hourly tonometric tests may be done during early treatment because drug may cause an initial transitory increase
in IOP.
- Monitor changes in visual acuity.
- Monitor for adverse effects. Brow pain and myopia tend to be more prominent in younger patients and generally disappear with
continued use of drug.
Patient & Family Education
- Understand that therapy for glaucoma is prolonged and that adherence to established regimen is crucial to prevent blindness.
- Do not drive or engage in potentially hazardous activities until vision clears. Drug causes blurred vision and difficulty
in focusing.
- Discontinue medication if symptoms of irritation or sensitization persist and report to physician.
- Do not breast feed while taking this drug without consulting physician.
Ocular Therapeutic System (Ocusert)
- Review information/directions about inserting the ocular system included in the drug package with health care provider. Demonstrate
to establish ability to adjust, insert, and remove the system.
- Unit is placed in the eye cul-de-sac, where it remains for a week. Slow release of drug provides a nonfluctuating concentration
of pilocarpine in the ciliary body and iris.
- Induced myopia, miosis, and spasm of accommodation are less than that produced by eyedrops. However, since transient blurring
and dimness of vision may occur following Ocusert insertion, have patient do so at bedtime; myopia will be at a stable level
in the a.m.
- Several hours after Ocusert insertion, induced myopia decreases to a low base level that persists for the life of the therapeutic
system.
- Notify physician if following symptoms do not subside: Conjunctival irritation with mild erythema and increase in mucus secretion;
generally accompany early use of Ocusert.
- Wash system with cool tap water before replacing it into cul-de-sac if it contacts an unclean surface.
- If retention of the system is a problem, the superior conjunctival cul-de-sac may be a preferred site for insertion. This
location is also preferred during sleep.
- To change placement: Ocusert may be transferred from the lower conjunctival sac to the superior sac by closing eyelids, rolling
the eye toward the nose and, with gentle digital pressure through the closed eyelid, directly moving the system. Avoid moving
it over the colored part of the eye.
- Remove system and replace with a new one if an unexpected increase in drug action occurs (sudden miosis, ciliary spasm, decreased
visual acuity).
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