Pilocarpine

Mechanism-of-action classes: Cholinergic Agonists; Cholinergic Muscarinic Agonists.

• Pilocarpine hydrochloride tablets, USP are indicated for 1) the treatment of symptoms of dry mouth from salivary gland hypofunction caused by radiotherapy for cancer of the head and neck; and 2) the treatment of symptoms of dry mouth in patients with Sjogren's syndrome.

• Pilocarpine hydrochloride tablets are contraindicated in patients with uncontrolled asthma, known hypersensitivity to pilocarpine, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle closure) glaucoma.contraindicated

Regardless of the indication, the starting dose in patients with moderate hepatic impairment should be 5 mg twice daily, followed by adjustment based on therapeutic response and tolerability. Patients with mild hepatic insufficiency do not require dosage reductions. The use of pilocarpine in patients with severe hepatic insufficiency is not recommended. If needed, refer to the Hepatic Insufficiency subsection of the Precautions section of this label for definitions of mild, moderate and severe hepatic impairment. Head & Neck Cancer Patients: The recommended initial dose of pilocarpine hydrochloride tablets is 5 mg taken three times a day. Dosage should be titrated according to therapeutic response and tolerability. The usual dosage range is 15-30 mg per day. (Not to exceed 10 mg per dose.) Although early improvement may be realized, at least 12 weeks of uninterrupted therapy with pilocarpine hydrochloride tablets may be necessary to assess whether a beneficial response will be achieved. The incidence of the most common adverse events increases with dose. The lowest dose that is tolerated and effective should be used for maintenance. Sjogren's Syndrome Patients: The recommended dose of pilocarpine hydrochloride tablets is one tablet (5 mg) taken four times a day. Efficacy was established by 6 weeks of use.

Cardiovascular Disease: Patients with significant cardiovascular disease may be unable to compensate for transient changes in hemodynamics or rhythm induced by pilocarpine. Pulmonary edema has been reported as a complication of pilocarpine toxicity from high ocular doses given for acute angle-closure glaucoma. Pilocarpine should be administered with caution in and under close medical supervision of patients with significant cardiovascular disease. Ocular: Ocular formulations of pilocarpine have been reported to cause visual blurring which may result in decreased visual acuity, especially at night and in patients with central lens changes, and to cause impairment of depth perception. Caution should be advised while driving at night or performing hazardous activities in reduced lighting. Pulmonary Disease: Pilocarpine has been reported to increase airway resistance, bronchial smooth muscle tone, and bronchial secretions. Pilocarpine hydrochloride should be administered with caution to and under close medical supervision in patients with controlled asthma, chronic bronchitis, or chronic obstructive pulmonary disease requiring pharmacotherapy.

Head & Neck Cancer Patients: In controlled studies, 217 patients received pilocarpine, of whom 68% were men and 32% were women. Race distribution was 91% Caucasian, 8% Black, and 1% of other origin. Mean age was approximately 58 years. The majority of patients were between 50 and 64 years (51%), 33% were 65 years and older and 16% were younger than 50 years of age. The most frequent adverse experiences associated with pilocarpine hydrochloride tablets were a consequence of the expected pharmacologic effects of pilocarpine. Adverse Event Pilocarpine HCl Placebo 10 mg t.i.d. (30 mg/day) 5 mg t.i.d. (15 mg/day) (t.i.d.) n=121 n=141 n=152 Sweating 68% 29% 9% Nausea 15 6 4 Rhinitis 14 5 7 Diarrhea 7 4 5 Chills 15 3 <1 Flushing 13 8 3 Urinary Frequency 12 9 7 Dizziness 12 5 4 Asthenia 12 6 3 In addition, the following adverse events (≥3% incidence) were reported at dosages of 15-30 mg/day in the controlled clinical trials: Adverse Event Pilocarpine HCl Placebo 5-10 mg t.i.d. (15-30 mg/day) (t.i.d.) n=212 n=152 Headache 11% 8% Dyspepsia 7 5 Lacrimation 6 8 Edema 5 4 Abdominal Pain 4 4 Amblyopia 4 2 Vomiting 4 1 Pharyngitis 3 8 Hypertension 3 1 The following events were reported with treated head and neck cancer patients at incidences of 1% to 2% at dosages of 7.5 to 30 mg/day: abnormal vision, conjunctivitis, dysphagia, epistaxis, myalgias, pruritus, rash, sinusitis, tachycardia, taste perversion, tremor, voice alteration. The following events were reported rarely in treated head and neck cancer patients (<1%): Causal relation is unknown.

Pregnancy: Teratogenic effects Pregnancy Category C: 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 (mg/m 2 ) 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 body surface area (mg/m 2 ) 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 body surface area (mg/m 2 ) estimates) and above. There are no adequate and well-controlled studies in pregnant women. Pilocarpine hydrochloride tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Metabolism

In a multiple-dose pharmacokinetic study in male volunteers following 2 days of 5 or 10 mg of oral pilocarpine hydrochloride tablets given at 8 a.m., noontime, and 6 p.m., the mean elimination half-life was 0.76 hours for the 5 mg dose and 1.35 hours for the 10 mg dose. T max values were 1.25 hours and 0.85 hours.

MANAGEMENT OF OVERDOSE: Fatal overdosage with pilocarpine has been reported in the scientific literature at doses presumed to be greater than 100 mg in two hospitalized patients. 100 mg of pilocarpine is considered potentially fatal. Overdosage should be treated with atropine titration (0.5 mg to 1.0 mg given subcutaneously or intravenously) and supportive measures to maintain respiration and circulation. Epinephrine (0.3 mg to 1.0 mg, subcutaneously or intramuscularly) may also be of value in the presence of severe cardiovascular depression or bronchoconstriction. It is not known if pilocarpine is dialyzable.

• Mar 22, 1994NDANDA020237Advanz Pharma
• Dec 22, 2004ANDAANDA076963Innogenix
• Oct 14, 2005ANDAANDA077220Lannett Co Inc
• Mar 31, 2006ANDAANDA077248Impax Labs
• Jun 22, 2010NDANDA200890Sandoz
• Aug 13, 2019ANDAANDA212377Aurobindo Pharma Usa
• Oct 28, 2021NDANDA214028Abbvie
• Oct 17, 2023NDANDA217836Orasis Pharms

1. 1Drug Ineffective44113%
2. 2Headache41213%
3. 3Nausea2056.2%
4. 4Vision Blurred2046.2%
5. 5Visual Impairment2046.2%
6. 6Pain1966.0%
7. 7Fatigue1815.5%
8. 8Off Label Use1745.3%
9. 9Eye Pain1624.9%
10. 10Dizziness1554.7%
11. 11Dyspnoea1444.4%
12. 12Eye Irritation1384.2%
13. 13Arthralgia1354.1%
14. 14Fall1273.9%
15. 15Diarrhoea1233.7%

Recent PubMed references pinned to Pilocarpine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Effect of the PPARγ Agonist Pioglitazone on Rat Behavior and Expression of Epileptogenesis-Related Genes during the Latent Phase of the Lithium-Pilocarpine Model.
  Biochemistry. Biokhimiia · 2026 · Kharisova AR, Zubareva OE, Kovalenko AA, et al.
  PMID 42219391DOI 10.1134/S0006297926600183
• De Novo Chromosome-Level Assembly of the Endangered Pilocarpus Microphyllus Highlights Genomic Resources for Conservation and Sustainable Pilocarpine Extraction.
  Genome biology and evolution · 2026 · Sobreiro MB, Magalhães L, Argolo LA, et al.
  PMID 41885800DOI 10.1093/gbe/evag070
• Enhancing presbyopia treatment: A comparative study of 1% Pilocarpine monotherapy versus combination with 0.09% Bromfenac.
  Indian journal of ophthalmology · 2026 · Jain A, Sen S, Imchen MT, et al.
  PMID 41884911DOI 10.4103/IJO.IJO_1354_25
• Pilocarpine in the Management of Allergic Rhinosinusitis.
  International journal of pharmaceutical compounding · 2026 · Theodoropoulou LM, Cullen NA
  PMID 41819131
• Comparison of pilocarpine- versus exercise-induced sweat sodium concentration across exercise intensities in trained athletes.
  Physiological reports · 2026 · Harris CT, Hunt L, Shepherd SO, et al.
  PMID 41532800DOI 10.14814/phy2.70724
• Beta-Arrestin2-Biased Activation by Pilocarpine Suppresses Microglial Inflammatory Response.
  Journal of neurochemistry · 2025 · Xie Y, Wang K, Wang S, et al.
  PMID 41457680DOI 10.1111/jnc.70334
• Effect of Pilocarpine on the Iridocorneal Angle Following Phaco-Kahook Dual Blade Goniotomy in Japanese Glaucoma Patients.
  Journal of glaucoma · 2026 · Yata N, Hollό G, Ishida T, et al.
  PMID 41400444DOI 10.1097/IJG.0000000000002666
• Preclinical Evaluation of a Pilocarpine-(R)-Lipoic Acid Eye Drop for Presbyopia.
  Translational vision science & technology · 2025 · Robb E, Triyasakorn K, Christidhis J, et al.
  PMID 41235858DOI 10.1167/tvst.14.11.17

The 10 most recently updated of 76 ClinicalTrials.gov registrations naming Pilocarpine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Contamination of Young Children Hair During Acute Cannabis Intoxication
  Not yet recruiting · Interventional · 15 enrolled · University Hospital, Toulouse
  NCT07524088updated 2026-04-13
• Safety and Efficacy of Nyxol Eye Drops as a Single Agent and With Adjunctive Low-Dose Pilocarpine Eye Drops in Subjects With Presbyopia
  Completed · Phase 3 · Interventional · 333 enrolled · Ocuphire Pharma, Inc.
  NCT05646719updated 2026-03-12
• Novel Point-of-care Sweat Chloride Testing Device for Monitoring CFTR Function
  Not yet recruiting · Interventional · 300 enrolled · Emory University
  NCT07414810updated 2026-02-17
• Pilocarpine Use After Kahook Goniotomy
  Recruiting · Phase 3 · Interventional · 142 enrolled · Montefiore Medical Center
  NCT03933631updated 2025-11-10
• Safety and Efficacy of Nyxol With Pilocarpine Eye Drops in Subjects With Presbyopia
  Completed · Phase 2 · Interventional · 150 enrolled · Ocuphire Pharma, Inc.
  NCT04675151updated 2025-10-10
• Optimal Treatment Protocol for Selective Laser Trabeculoplasty
  Active not recruiting · Interventional · 400 enrolled · Vastra Gotaland Region
  NCT03798223updated 2025-10-03
• Optimal Treatment Protocol for Selective Laser Trabeculoplasty - Repeat Trial
  Enrolling by invitation · Interventional · 400 enrolled · Vastra Gotaland Region
  NCT05159960updated 2025-09-30
• Evaluation of NV701 (Pilocarpine 1.25%) Compared With Vuity (Pilocarpine 1.25%) on Pupil Size in Subjects With Presbyopia
  Completed · Early phase 1 · Interventional · 55 enrolled · Novus Vision LLC
  NCT06783686updated 2025-09-05
• Quality of Life in Presbyopic Patients Who Are Treated With Qlosi
  Recruiting · Phase 4 · Interventional · 36 enrolled · Southern College of Optometry
  NCT07113210updated 2025-08-12
• KERMIT: Sweat Patch for Early Kidney Disease Detection
  Not yet recruiting · Interventional · 52 enrolled · University of Ioannina
  NCT07047664updated 2025-07-02

Frequently asked questions

How does Pilocarpine work?

Mechanism-of-action classes: Cholinergic Agonists; Cholinergic Muscarinic Agonists.

What is Pilocarpine used for?

According to FDA labeling, Pilocarpine carries indications including: Pilocarpine hydrochloride tablets, USP are indicated for 1) the treatment of symptoms of dry mouth from salivary gland hypofunction caused by radiotherapy for cancer of the head and neck; and 2) the treatment of symptoms of dry mouth in patients with Sjogren's syndrome.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Pilocarpine?

Pilocarpine is classified as Other parasympathomimetics, Parasympathomimetics, Cholinergic Receptor Agonist, Cholinergic Agonists, Cholinergic Muscarinic Agonists, Decreased Intraocular Fluid Pressure, Pupillary Constriction.

What are the brand names for Pilocarpine?

Pilocarpine is marketed under brand names including Isoptocarpine, Pilocar, Qlosi, Salagen, Vuity.

What are the contraindications for Pilocarpine?

Pilocarpine labeling lists contraindications including: Pilocarpine hydrochloride tablets are contraindicated in patients with uncontrolled asthma, known hypersensitivity to pilocarpine, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle closure) glaucoma.. Always consult the full prescribing information and a clinician.