Pilocarpine is a cholinergic agonist that activates muscarinic receptors on smooth muscles. Pilocarpine is available as an ophthalmic solution and oral tablet. The ophthalmic solution formulation is indicated for the treatment of glaucoma and as a miosis inducting agent, both postoperatively and after ophthalmoscopic examination. Additionally, a 1.25% (Vuity) and 0.4% (Qlosi) ophthalmic solution is approved for the treatment of presbyopia. An ocular 'system' that releases pilocarpine continuously, Ocusert, is also available. The ocular systems are contact lens-type devices that provide a 7-day treatment. Ophthalmic solutions are preferred over the device when an intense miotic response is indicated. The oral formulation is approved for the treatment of symptoms of xerostomia caused by radiotherapy for cancer of the head and neck. The pilocarpine tablets (Salagen) are also approved for the management of xerostomia associated with Sjogren's syndrome or radiation therapy.
NOTE: Drug name confusion has been reported with the brand name Salagen (generic name pilocarpine), used to treat dry mouth due to Sjogren's syndrome or radiation therapy, and the generic name selegiline (brand name Eldepryl), a MAO-inhibitor used for Parkinson's disease. Both drugs are available in 5 mg tablets. Confusion has occurred with both verbal and written prescription orders. To lessen drug name confusion, consider listing both the brand and generic names on prescriptions.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Oral Administration
-Administer pilocarpine with a full glass of water.
Ophthalmic Administration
-Instruct patient on proper application of ocular system, eye gel, or eye solution. Apply ocular system at bedtime in order to reach a stable level of pilocarpine-induced myopia by morning.
-Do not to touch the tip of the dropper or tube to the eye, fingertips, or other surface.
-If administering ophthalmic solution with other topical ophthalmic agents, allow at least 5 minutes between administration times.
-Remove contact lenses prior to instilling the ophthalmic solution, and wait 10 minutes after dosing before reinserting the lenses.
Parasympathetic stimulation can cause systemic effects especially from oral dosage of pilocarpine. The ocular systems generally are less likely than the ophthalmic solutions to produce systemic effects. If they occur, the miotic should be withdrawn. Systemic symptoms are listed below under oral preparation. Children appear to be more susceptible to systemic effects.
Adverse reactions to ophthalmic pilocarpine generally are confined to ophthalmic effects, although systemic reactions are not unusual. Myopia and night blindness are fairly common. The elderly are more susceptible, and special care is required for night driving. Photophobia, which can be alleviated by wearing dark glasses, or changes in visual field can occur. Ciliary body spasm occasionally precedes retinal detachment. Sudden or rapid release of pilocarpine from an ocular system can precipitate ciliary body spasm. If spasm becomes severe, withdrawal of the miotic may be necessary. Ocular pain can be experienced, possibly as a head or brow ache (5% or more). In 5% or more of patients using the ophthalmic solution, ocular irritation, conjunctival hyperemia, accommodative changes, ocular pain, and visual impairment (dim, dark, or "jumping" vision) occurred. During postmarketing use, cases of vitreous detachment, vitreomacular traction, retinal tear, and retinal detachment have been reported. A foreign body sensation or irritation can occur when an ocular system is inserted.
Blurred vision has been reported with both the tablet (1% to 2%) and ophthalmic (at least 5%) preparations of pilocarpine. Additionally, up to 6% of patients taking the tablet and 1% to 5% of patients receiving the ophthalmic solution experienced increased lacrimation. Other ocular adverse effects reported with the tablet formulation include amblyopia (4%), conjunctivitis (1% to 2%), glaucoma (less than 1%), and miosis.
Adverse reactions seen with orally administered pilocarpine are an exaggeration of its parasympathetic effect. Hyperhidrosis (sweating) is a frequent adverse effect reported in 29% to 68% of patients. Other effects include chills (3% to 15%), edema (up to 5%), flushing (8% to 13%), epistaxis (1% to 2%), pruritus (1% to 2%), and rash (1% to 2%). Adverse effects reported in less than 1% of patients taking the tablet formulation include hypothermia, seborrhea, cyst, photosensitivity reaction, drug-induced body odor, alopecia, contact dermatitis, xerosis, eczema, erythema nodosum, exfoliative dermatitis, herpes simplex, skin ulcer, and vesiculobullous rash.
Gastrointestinal adverse effects reported with orally administered pilocarpine include diarrhea (4% to 7%), dysphagia (1% to 2%), dyspepsia (7%), abdominal pain (3% to 4%), taste perversion (1% to 2%), nausea (up to 15%), and vomiting (up to 4%). GI effects reported in less than 1% of patients include anorexia, appetite stimulation, esophagitis, bilirubinemia, cholelithiasis, colitis, xerostomia, eructation, gastritis, gastroenteritis, gastrointestinal disorder, gingivitis, hepatitis, abnormal liver function tests, melena, pancreatitis, parotid gland enlargement, salivary gland enlargement, taste loss, taste perversion, tooth disorder, and tongue disorder.
Cardiovascular adverse effects reported with orally administered pilocarpine include sinus tachycardia (1% to 2%) and hypertension (up to 3%). Adverse effects reported in less than 1% of patients taking the tablet formulation include bradycardia, ECG abnormality, palpitations, chest pain (unspecified), angina pectoris, arrhythmia, hypotension, intracranial hemorrhage, myocardial infarction, and syncope. After overdoses, AV block, bradycardia, and PVCs have been reported.
Headache has been reported with administration of both the tablet (11% to 13%) and ophthalmic (at least 5%) formulations of pilocarpine. Adverse effects reported in less than 1% of patients taking the tablet formulation include peripheral edema, hypoglycemia, migraine, death, moniliasis, neck pain, neck rigidity.
Leukopenia, hematuria, abnormal platelets, thrombocythemia, thrombocytopenia, thrombosis, abnormal WBC, and lymphadenopathy have been reported in less than 1% of patients receiving pilocarpine tablets.
Patients taking pilocarpine tablets have reported dizziness (5% to 12%), asthenia (2% to 12%), and tremor (up to 2%). Anxiety, confusion, depression, abnormal dreams, hyperkinesis, hypesthesia, nervousness, paresthesias, speech disorder, aphasia, emotional lability, insomnia, leg cramps, abnormal thinking, and twitching have been reported in less than 1% of patients receiving pilocarpine tablets.
Adverse effects reported in less than 1% of patients receiving the tablet formulation include arthralgia, arthritis, bone disorder, spontaneous bone fractures, pathological fracture, myasthenia, tendon disorder, and tenosynovitis.
Adverse reactions seen with orally administered pilocarpine include voice change (1% to 2%), rhinitis (5% to 14%), pharyngitis (2% to 3%), and sinusitis (1% to 2%). Adverse reactions reported in less than 1% of patients who receive the tablet formulation include increased sputum, stridor, bronchitis, dyspnea, hiccups, laryngismus (laryngospasm), laryngitis, pneumonia, viral infection, voice alteration, and yawning.
Increased urinary frequency (9% to 12%) has been reported with pilocarpine use. Adverse effects reported in less than 1% of patients taking the tablet formulation include breast pain, dysuria, mastitis, menorrhagia, metrorrhagia, ovarian disorder, pyuria, salpingitis, urethral pain, urinary impairment, urinary urgency, vaginal pain, vaginal hemorrhage, and vaginal moniliasis.
Absolute contraindications for pilocarpine are related to dosage form and can be relevant to the condition being treated. Some contraindications may not be applicable to ophthalmic use and others not applicable to oral use.
Drug name confusion has been reported with the brand name Salagen (generic name pilocarpine), used to treat dry mouth due to Sjogren's syndrome or radiation therapy, and the generic name selegiline (brand name Eldepryl), a MAO-inhibitor used for Parkinson's disease. Both drugs are available in 5 mg tablets. Confusion has occurred with both verbal and written prescription orders. To lessen drug name confusion, consider listing both the brand and generic names on prescriptions.
There have been no overall differences in safety and efficacy observed between elderly and younger patients with any of the pilocarpine preparations.
Rare cases of retinal detachment and retinal tear have been reported with miotics, including ophthalmic pilocarpine. Individuals with pre-existing retinal disease are at increased risk. A thorough examination of the retina including funduscopy is advised in all patients prior to the initiation of ophthalmic pilocarpine. Instruct drug recipients to seek immediate medical care for sudden onset of flashing lights, floaters, or vision loss. It is not known whether this association may occur with oral pilocarpine use, as the systemic blood level related to retinal detachment is unknown.
Use of pilocarpine oral tablets is contraindicated when miosis is undesirable, such as in patients who have closed-angle glaucoma.
Use of pilocarpine oral tablets and ophthalmic gel is contraindicated when miosis is undesirable, such as in patients with acute iritis. Use of the ophthalmic solution is not recommended when iritis is present because adhesions (synechiae) may form between the iris and the lens.
Contact lenses should be removed before treatment with pilocarpine ophthalmic solution and can be reinserted 10 minutes after the dose has been instilled.
Oral pilocarpine is contraindicated in patients with uncontrolled asthma and should be used with caution in patients with controlled asthma or chronic obstructive pulmonary disease (COPD) (e.g., chronic bronchitis) requiring pharmacotherapy. Pilocarpine may stimulate the mucous cells of the respiratory tract and increase bronchial smooth muscle tone and airway resistance. Some combination preparations of pilocarpine contain sodium bisulfite and should be used with caution in patients with a known sulfite hypersensitivity, especially in patients with a history of asthma.
There are no adequate and well-controlled studies of pilocarpine in pregnant patients to determine a drug-associated risk; therefore, use pilocarpine during pregnancy only if the benefits to the mother outweigh the potential risks to the fetus. Data from a retrospective case series identified no drug-related adverse effects in 4 patients or their infants following exposure to ophthalmic pilocarpine either pre-pregnancy, during pregnancy, or postpartum. In animal studies, systemically-administered pilocarpine was associated with a reduction in the mean fetal body weight and an increase in the incidence of skeletal variations when given to pregnant rats at a dosage of 90 mg/kg/day [approximately 26 times the maximum recommended dose for a 50 kg human when compared on the basis of body surface area (BSA) estimates]. These effects may have been secondary to maternal toxicity. In another study, oral administration of pilocarpine to female rats during gestation and lactation at a dosage of 36 mg/kg/day (approximately 10 times the maximum recommended dose for a 50 kg human when compared on the basis of BSA estimates) resulted in an increased incidence of stillbirths; decreased neonatal survival and reduced mean body weight of pups were observed at dosages of 18 mg/kg/day (approximately 5 times the maximum recommended dose for a 50 kg human when compared on the basis of BSA estimates) and above. Animal reproduction studies have not been conducted with ophthalmic pilocarpine hydrochloride.
It is not known whether pilocarpine is excreted in human milk. According to the manufacturer of oral pilocarpine, because many drugs are excreted in human milk and because of the potential for serious adverse reactions in breast-feeding infants from pilocarpine, a decision should be made whether to discontinue breast-feeding or to discontinue the drug, taking into account the importance of the drug to the mother. The manufacturers of ophthalmic pilocarpine recommend caution if the drug is administered to a breast-feeding woman. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. To minimize the amount of drug that reaches systemic circulation, apply pressure over the tear duct by the corner of the eye for 1 minute after each application to the eye.
Pilocarpine should be used with caution in patients with biliary tract disease or cholelithiasis. Pilocarpine causes contractions of the gallbladder or biliary smooth muscle and biliary obstruction, cholangitis, or cholecystitis may occur.
Oral pilocarpine should be used with caution in patients with hepatic disease. Dosage reduction is recommended for patients with moderate hepatic impairment. Data are lacking in patients with severe hepatic impairment (Child-Pugh score 10 to 15); pilocarpine is not recommended in these patients.
Pilocarpine should be used with caution in patients with cardiac disease. Pilocarpine induces transient changes in heart rhythm or hemodynamics and patients with cardiac disease may not be able to compensate for these changes. Pulmonary edema can occur in patients being treated with ophthalmic pilocarpine in high doses for acute closed-angle glaucoma.
Pilocarpine should be used cautiously in patients with nephrolithiasis. Pilocarpine increases ureteral smooth muscle tone and may precipitate renal colic, especially in patients with nephrolithiasis.
Oral pilocarpine may have dose-related central nervous system effects which could exacerbate conditions of psychiatric disturbances (e.g., psychosis) or cognitive disturbances.
Miotics, including pilocarpine, may cause accommodative spasm. Advise patients against driving or operating machinery if vision is not clear (i.e., blurred vision). Additionally, patients may experience temporary dim or dark vision. Caution is recommended during night driving or while performing other hazardous activities in pool illumination.
Pilocarpine ophthalmic solution should be used with caution when using it in infants, children, and adolescents with primary congenital glaucoma for control of intraocular pressure (IOP) as cases of paradoxical increase in IOP have been reported. Also, the ophthalmic solution is not recommended in pediatric patients with glaucoma secondary to anterior segment dysgenesis or uveitis (especially with active uveitis). The safety and efficacy of the ophthalmic gel or oral tablets have not been established in pediatric patients, including neonates, infants, children, and adolescents.
For the treatment of increased intraocular pressure (IOP) in patients with glaucoma or ocular hypertension or for the prevention of increased IOP associated with laser surgery:
-for the treatment of open-angle glaucoma or ocular hypertension:
Ophthalmic dosage (ophthalmic solution):
Adults: Instill 1 drop into the eye(s) up to 4 times per day. Pilocarpine-naive patients should be started on the lowest available concentration as higher concentrations are often not tolerated initially. The frequency of administration and concentration of the ophthalmic solution administered are determined by the severity of the elevated intraocular pressure and the miotic response of the patient. To limit systemic exposure to pilocarpine, patients may be instructed to perform punctal occlusion for 2 minutes after administration.
Children and Adolescents 2 years and older: Instill 1 drop into the eye(s) up to 4 times per day. Pilocarpine-naive patients should be started on the lowest available concentration as higher concentrations are often not tolerated initially. The frequency of administration and concentration of the ophthalmic solution administered are determined by the severity of the elevated intraocular pressure and the miotic response of the patient. To limit systemic exposure to pilocarpine, patients may be instructed to perform punctal occlusion for 2 minutes after administration.
Infants and Children younger than 2 years: Instill 1 drop of the 1% ophthalmic solution into affected eye(s) 3 times daily.
Ophthalmic dosage (ophthalmic gel):
Adults: Apply a one-half inch ribbon in the lower conjunctival sac of the affected eye(s) once daily at bedtime.
Ophthalmic dosage (ocular insert):
Adults: Apply 1 ocular system delivering 20 or 40 mcg/hour, once every 7 days.
-for treatment of acute angle-closure glaucoma:
NOTE: Prior to treatment with pilocarpine ophthalmic solution, secretory suppressants and hyperosmotic agents may be needed to lower intraocular pressure below 50 mmHg and relieve iris ischemia.
Ophthalmic dosage (ophthalmic solution):
Adults: For initial management, instill 1 drop of 1% or 2% solution into affected eye(s) up to 3 times over a 30 minute period. If laser iridoplasty or iridomy is used to break the attack, instill 1 drop of 4% solution prior to the procedure. After laser iridoplasty, instill 1 drop of 1% solution 4 times daily until an iridotomy can be performed.
Children and Adolescents 2 years and older: For initial management, instill 1 drop of 1% or 2% solution into affected eye(s) up to 3 times over a 30 minute period. If laser iridoplasty or iridomy is used to break the attack, instill 1 drop of 4% solution prior to the procedure. After laser iridoplasty, instill 1 drop of 1% solution 4 times daily until an iridotomy can be performed.
Infants and Children younger than 2 years: Instill 1 drop of the 1% ophthalmic solution into affected eye(s) 3 times daily.
-for the prevention of increased intraocular pressure associated with laser surgery:
Ophthalmic dosage (ophthalmic solution):
Adults: Instill 1 drop (or 2 drops 5 minutes apart) of 1%, 2%, or 4% ophthalmic solution into the affected eye(s) 15 to 60 minutes prior to surgery.
For miosis induction:
Ophthalmic dosage (ophthalmic solution):
Adults: Instill 1 drop (or 2 drops 5 minutes apart) of 1%, 2%, or 4% ophthalmic solution into the eye(s).
Infants, Children, Adolescents: For the induction of miosis prior to goniotomy or trabeculectomy, instill 1 drop of 1% or 2% ophthalmic solution into the eye 15 to 60 minutes prior to surgery.
For the treatment of presbyopia:
Ophthalmic dosage (Vuity only):
Adults: 1 drop instilled in each eye once daily. An additional dose in each eye may be administered 3 to 6 hours after the first dose.
Ophthalmic dosage (Qlosi only):
Adults: 1 drop instilled in each eye once daily. An additional dose in each eye may be administered 2 to 3 hours after the first dose for an effect up to 8 hours. Administer on a daily basis, or as needed, up to two doses per day.
For the treatment of xerostomia and/or dry eye disease*:
-for the treatment of xerostomia due to salivary gland hypofunction due to radiotherapy for cancer of the head and neck:
Oral dosage:
Adults: 5 mg PO 3 times daily, initially. Titrate dose according to response and tolerance. Usual dose: 15 to 30 mg/day. Max: 10 mg/dose.
-for the treatment of xerostomia and/or dry eye disease* in persons with Sjogren's syndrome:
Oral dosage:
Adults: 5 mg PO once daily for 1 to 2 weeks, then 5 mg PO twice daily for 1 to 2 weeks, then 5 mg PO 3 times daily for 1 to 2 weeks, then 5 mg PO 4 times daily.
Maximum Dosage Limits:
-Adults
10 mg/dose or 30 mg/day PO; ophthalmic maximum is dependent on indication and dosage form.
-Geriatric
10 mg/dose or 30 mg/day PO; ophthalmic maximum is dependent on indication and dosage form.
-Adolescents
Safety and efficacy of the oral formulation has not been established; ophthalmic solution maximum is dependent on indication.
-Children
Safety and efficacy of the oral formulation has not been established; ophthalmic solution maximum is dependent on indication.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Regardless of the indication, the initial dosage of oral pilocarpine in patients with moderate hepatic impairment is 5 mg PO twice daily; adjust dosage based on response. Patients with mild hepatic impairment do not require dosage adjustment. Data are lacking in patients with severe hepatic impairment; oral pilocarpine is not recommended.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
Acebutolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Amitriptyline: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Amoxapine: (Major) Amoxapine may antagonize some of the effects of parasympathomimetics. However, bethanechol has occasionally been used therapeutically to offset some of the adverse antimuscarinic effects of cyclic antidepressants. Due to their anticholinergic actions, some cyclic antidepressants, such as amoxapine, may potentially antagonize the therapeutic actions of cholinergic agonists.
Anticholinergics: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Atenolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Atenolol; Chlorthalidone: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Atropine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Atropine; Difenoxin: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Belladonna; Opium: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Benztropine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Beta-blockers: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Betaxolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Bethanechol: (Moderate) Pilocarpine and bethanechol are both cholinergic agonists. Coadministration is expected to result in additive parasympathomimetic effects.
Bisoprolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Bisoprolol; Hydrochlorothiazide, HCTZ: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Brimonidine; Timolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Budesonide; Glycopyrrolate; Formoterol: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Carteolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Carvedilol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Cevimeline: (Moderate) Cevimeline and pilocarpine are both cholinergic agonists. Coadministration is expected to result in additive parasympathomimetic effects.
Chlordiazepoxide; Amitriptyline: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Chlordiazepoxide; Clidinium: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Chlorpromazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Cholinesterase inhibitors: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Clomipramine: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Codeine; Phenylephrine; Promethazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Codeine; Promethazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Desipramine: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Dicyclomine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Diphenoxylate; Atropine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Disopyramide: (Moderate) Disopyramide possesses clinically significant antimuscarinic properties and these appear to be dose-related. It is possible that disopyramide could antagonize the muscarinic actions of cholinergic agonists. Clinicians should be alert to this possibility.
Donepezil: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Donepezil; Memantine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Dorzolamide; Timolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Doxepin: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Esmolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Flavoxate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Fluphenazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Galantamine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Glycopyrrolate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Glycopyrrolate; Formoterol: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Guanidine: (Moderate) Guanidine and pilocarpine are both cholinergic agonists. Coadministration is expected to result in additive parasympathomimetic effects.
Homatropine; Hydrocodone: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Hyoscyamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Imipramine: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Indacaterol; Glycopyrrolate: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Labetalol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Levobunolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Maprotiline: (Major) Maprotiline may antagonize some of the effects of parasympathomimetics. However, bethanechol has occasionally been used therapeutically to offset some of the adverse antimuscarinic effects of cyclic antidepressants. Due to their anticholinergic actions, some cyclic antidepressants like maprotiline may potentially antagonize the therapeutic actions of the cholinesterase-inhibitors used for the treatment of dementia.
Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Methscopolamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Metoprolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Metoprolol; Hydrochlorothiazide, HCTZ: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Nadolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Nebivolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Nebivolol; Valsartan: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Neostigmine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Neostigmine; Glycopyrrolate: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided. (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Nortriptyline: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Oxybutynin: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Perphenazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Perphenazine; Amitriptyline: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced. (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Phenobarbital; Hyoscyamine; Atropine; Scopolamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Phenothiazines: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Physostigmine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Pindolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Pralidoxime: (Moderate) Pilocarpine and pralidoxime are both cholinergic agonists. Coadministration is expected to result in additive parasympathomimetic effects.
Prochlorperazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Promethazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Promethazine; Dextromethorphan: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Promethazine; Phenylephrine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Propantheline: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Propranolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Protriptyline: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Pyridostigmine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Rivastigmine: (Major) Cholinergic agonists can cause additive pharmacodynamic effects if used concomitantly with cholinesterase inhibitors. Concurrent use is unlikely to be tolerated by the patient and should be avoided.
Scopolamine: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Sotalol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Thioridazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Timolol: (Moderate) Systemically administered pilocarpine (e.g., when used for the treatment of xerostomia or xerophthalmia) should be administered with caution in patients taking beta-blockers because of the possibility of cardiac conduction disturbances. The risk of conduction disturbances with beta-blockers and ophthalmically administered pilocarpine is low.
Tricyclic antidepressants: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Trifluoperazine: (Moderate) Avoid using pilocarpine in combination with other drugs known to have anticholinergic effects as the therapeutic efficacy of either agent may be reduced.
Trihexyphenidyl: (Major) The muscarinic actions of drugs known as parasympathomimetics, including both direct cholinergic receptor agonists and cholinesterase inhibitors, can antagonize the antimuscarinic actions of anticholinergic drugs, and vice versa.
Trimipramine: (Moderate) Tricyclic antidepressants (TCAs) may antagonize some of the effects of parasympathomimetics (e.g., cholinesterase inhibitors) due to their anticholinergic activity. However, parasympathomimetics like bethanechol have occasionally been used historically to offset some of the adverse peripheral antimuscarinic (anticholinergic) effects of TCAs, such as dry mouth, constipation, or urinary retention. For years, physostigmine was used as an adjunct to the treatment of TCA overdose; however, its efficacy was limited to addressing anticholinergic effects. Additionally, case reports suggest that harmful effects such as seizures and bradyarrhythmias progressing to asystole, especially in patients with cardiac conduction abnormalities at baseline, are possible. For these reasons, physostigmine is no longer considered a standard of care in the treatment of TCA overdose.
Trospium: (Moderate) Pharmacologically, parasympathomimetic drugs enhance muscarinic/cholinergic function. Because trospium is an antimuscarinic, the muscarinic actions of drugs known as parasympathomimetics, including direct cholinergic agonists, could be antagonized when used concomitantly with trospium.
Pilocarpine is a cholinergic muscarinic receptor agonist. By directly stimulating these receptors, pilocarpine causes smooth muscles, such as the iris sphincter muscle and ciliary muscle, to contract. Contraction of the iris sphincter muscle constricts the pupil producing miosis and improving near and intermediate visual acuity while maintaining some pupillary response to light. Contraction of the ciliary muscle may shift the eye to a more myopic or nearsighted state. In glaucoma, the intraocular pressure rises to an unacceptable level, producing pain and abnormal vision; if untreated, it can cause loss of sight. In open-angle glaucoma, pilocarpine contracts the ciliary muscle, increasing the outflow of aqueous humor, which reduces intraocular pressure. In closed-angle glaucoma, pilocarpine-induced miosis opens the angle of the anterior chamber of the eye, through which aqueous humor exits. Pilocarpine also counteracts the mydriatic effects of sympathomimetic agents used in ophthalmologic examinations. By overcoming the mydriatic effect of atropine, pilocarpine has been used alternately with atropine to break adhesions between the iris and the lens. Administered orally, pilocarpine stimulates secretions of the exocrine glands. All secretory glands may be affected, including an increase in salivary flow.
Pilocarpine is administered orally and via the ophthalmic route. Pilocarpine does not bind to human plasma proteins over a concentration range of 5 to 25,000 ng/mL. The mechanism for inactivation of pilocarpine is not clear, but thought to occur at the neuronal synapses and in plasma. Pilocarpine and its degradation products are excreted in the urine.
Affected cytochrome P450 isoenzymes: none
-Route-Specific Pharmacokinetics
Oral Route
Following oral administration of pilocarpine the elimination half-life ranges from 0.75 to 1.35 hours. Peak effect is achieved in about 1 hour. This can be longer if the drug is taken with food. The duration of action is 3 to 5 hours.
Other Route(s)
Ophthalmic Route
Following application of a 1% solution to the eye, a drop in pressure occurs within 60 minutes that persists for 4 to 14 hours. Duration of action depends on the strength of pilocarpine used, usually between 0.5% to 4%. Systemic exposure was evaluated in 14 healthy subjects who received 2 drops of the 4% ophthalmic solution in both eyes 4-times daily for 8 days. Plasma concentrations reached steady-state after topical application with a mean Cmax of 3.7 ng/mL and AUC of 7.7 ng x hour/mL on day 8. The Tmax on day 8 ranged from 0.5 to 1 hour. In 22 patients with presbyopia, 1 drop of the 1.25% ophthalmic solution was administered in each eye once daily for 30 days. The mean Cmax and AUC values on Day 30 were 1.95 ng/mL and 4.14 ng x hour/mL, respectively. The median Tmax on Day 30 was 0.3 hours (range: 0.2 to 0.5 hours). Systemic exposure was evaluated in 12 healthy subjects who received 2 doses daily in each eye, 2 hours apart, for 8 days of the 0.4% ophthalmic solution. The overall median Tmax in plasma after Day 8 dosing was 2.20 hr and the mean (SD) overall plasma Cmax and AUC0-t after Day 8 dosing were 897.2 (287.2) pg/mL and 2699 (741.4) hr x pg/mL, respectively. The mean T1/2 after Day 8 dosing was 3.96 hr. The ocular system allows a sustained release of pilocarpine over 7 days, with maximal effect being achieved in 1.5 to 2 hours after the system is applied. A standard rate of release from an ocular system is either 20 mcg or 40 mcg/hour. The ophthalmic gel generally is used once daily, and a 1-time application can reduce the intraocular pressure for 18 to 24 hours. Use of these preparations can cause a period of pilocarpine-induced myopia.
Pilocarpine is bound to serum and ocular tissues. Whether pilocarpine is distributed is not known, but it apparently does not accumulate in ocular tissue. Pilocarpine penetrates into ocular tissue through the cornea, the amount varying according to a number of factors.
-Special Populations
Hepatic Impairment
In patients with mild to moderate hepatic impairment (n = 12), the pilocarpine AUC is approximately doubled, the total plasma clearance is reduced by 30%, and the half-life is increased to 2.1 hours following oral administration of a single 5 mg dose.
Renal Impairment
There are no significant differences in the pharmacokinetics of oral pilocarpine in patients with renal impairment (mean CrCl 25.4 mL/minute) compared to normal healthy volunteers.