Pilocarpine hydrochloride
Pilocarpine hydrochloride
Pilocarpine
(pie-low- CAR-peen)
Pregnancy Category: C Adsorbocarpine Akarpine Diocarpine Isopto Carpine Miocarpine Pilocar Pilopine HS Piloptic- 1/2 -1, -2, -3, -4, and -6 Pilopto-Carpine Pilostat Salagen Scheinpharm Pilocarpine (Rx)
Pilocarpine ocular therapeutic system
Pilocarpine ocular therapeutic system (Ocusert Pilo-20 and -40)
Pilocarpine
(pie-low- CAR-peen)
Pregnancy Category: C Ocusert Pilo-20 and -40 (Rx)

Classification: Direct-acting cholinergic agent (miotic)

Action/Kinetics: Hydrochloride Solution : 4-14 hr. Hydrochloride Gel: Onset: 60 min; peak effect: 3-12 hr; duration: 18-24 hr. Nitrate: The ocular therapeutic system is placed in the cul-de-sac of the eye for release of pilocarpine. The drug is released from the ocular therapeutic system three times faster during the first few hours and then decreases (within 6 hr) to a rate of 20 or 40 mcg/hr for 1 week. Ocular system: onset: 60 min. peak effect: 1.5-2 hr; duration: 7 days. When used to treat dry mouth due to radiotherapy in head and neck cancer clients, pilocarpine stimulates residual functioning salivary gland tissue to increase saliva production.

Uses: HCl: Chronic simple glaucoma (especially open-angle). Chronic angle-closure glaucoma, including after iridectomy. Acute angle-closure glaucoma (alone or with other miotics, epinephrine, beta-adrenergic blocking agents, carbonic anhydrase inhibitors, or hyperosmotic agents). To reverse mydriasis (i.e., after cycloplegic and mydriatic drugs). Pre- and postoperative intraocular tension. The nitrate product is also used for emergency miosis. Salagen (Pilocarpine HCl) has been approved for treatment of radiation-induced dry mouth in head and neck cancer clients, as well as in Sjogren's syndrome. Ocular Therapeutic System: Glaucoma alone or with other ophthalmic medications. Investigational: Hydrochloride used to treat xerostomia in clients with malfunctioning salivary glands.

Contraindications: Inflammatory eye disease, acute-angle glaucoma, history of retinal detachment, ocular hypotension, asthma, epilepsy, parkinsonism, gangrene, diabetes, CV disease, GI or GU tract obstruction, spastic GI conditions, vasomotor instability, severe bradycardia or hypotension, recent MI, lactation, in those receiving choline esters or depolarizing neuromuscular blocking drugs.

Special Concerns: Use with caution in those with narrow angles (angle closure may result), in those with known or suspected cholelithiasis or biliary tract disease, and in clients with controlled asthma, chronic bronchitis, or COPD. Safety and efficacy have not been established in children.

Side Effects: After ophthalmic use:Painful contraction of ciliary muscle, pain in eye, blurred vision, spasms of accommodation, darkened vision, failure to accommodate to darkness, twitching, headaches, painful brow. Use of pilocarpine ocular system: Conjunctival irritation, including mild erythema with or without a slight increase in mucous secretion upon initial use.
Oral use (tablets). Dermatologic: Sweating, flushing, rash, pruritus. GI: N&V;, dyspepsia, diarrhea, abdominal pain, taste perversion, anorexia, increased appetite, esophagitis, tongue disorder. CV: Hypertension, tachycardia, bradycardia, ECG abnormality, palpitations, syncope. CNS: Dizziness, asthenia, headache, tremor, anxiety, confusion, depression, abnormal dreams, hyperkinesia, hypesthesia, nervousness, paresthesias, speech disorder, twitching. Respiratory: Sinusitis, rhinitis, pharyngitis, epistaxis, increased sputum, stridor, yawning. Ophthalmic: Lacrimation, amblyopia, conjunctivitis, abnormal vision, eye pain, glaucoma. GU: Urinary frequency, dysuria, metrorrhagia, urinary impairment. Body as a whole: Chills, edema, body odor, hypothermia, mucous membrane abnormality. Miscellaneous: Dysphagia, voice alteration, myalgias, seborrhea.

Overdose Management: Treatment: Titrate with atropine (0.5-1 mg SC or IM) and supportive measures to maintain circulation and respiration. If there is severe cardiovascular depression or bronchoconstriction, epinephrine (0.3-1 mg SC or IV) may be used.

How Supplied: Pilocarpine hydrochloride: Device: 20 mcg/hr, 40 mcg/hr; Ophthalmic gel: 4%; Ophthalmic Solution: 0.25%, 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 8%; Tablet: 5 mg. Pilocarpine ocular therapeutic system: Device: 20 mcg/hr, 40 mcg/hr

Dosage
Pilocarpine Hydrochloride ?Ophthalmic Gel, 4% Glaucoma.
Adults and adolescents: 1/2-in. ribbon in the lower conjunctival sac of the affected eye(s) once daily at bedtime.
?Ophthalmic Solution, 1/4%, 1/2%, 1%, 2%, 3%, 4%, 5%, 6%, 8%
Doses listed are all for adults and adolescents.
Chronic glaucoma.
1 gtt of a 0.5%-4% solution q.i.d.
Acute angle-closure glaucoma.
1 gtt of a 1% or 2% solution q 5-10 min for three to six doses; then, 1 gtt q 1-3 hr until pressure is decreased.
Miotic, to counteract sympathomimetics.
1 gtt of a 1% solution.
Miosis, prior to surgery.
1 gtt of a 2% solution q 4-6 hr for one or two doses before surgery.
Miosis before iridectomy.
1 gtt of a 2% solution for four doses immediately before surgery.
?Ocular System
Insert and remove as directed on package insert or by physician. Ocusert Pilo-20 is approximately equal to the 0.5% or 1% drops, while Ocusert Pilo-40 is approximately equal to the 2% or 3% solution.
?Tablets (Salagen) Treat radiation-induced dry mouth in head and neck cancer clients.
Initial: 5 mg t.i.d.; then up to 10 mg t.i.d., if needed.