Pilocarpine hydrochloride

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Overview

What is Pilocarpine hydrochloride?

Pilocarpine Hydrochloride Tablets contain pilocarpine hydrochloride, a cholinergic agonist for oral use. Pilocarpine hydrochloride is a hygroscopic, odorless, bitter tasting white crystal or powder which is soluble in water and alcohol and virtually insoluble in most non-polar solvents. Pilocarpine hydrochloride, with a chemical name of (3-)-2(3)-Furanone, 3-ethyldihydro-4-[(1 -methyl-1-imidazol-5-yl) methyl] monohydrochloride, has a molecular weight of 244.72.

Each 5 mg Pilocarpine Hydrochloride Tablet for oral administration contains 5 mg of pilocarpine hydrochloride. Inactive ingredients in the tablet, the tablet's film coating, and polishing are: carnauba wax, hypromellose, microcrystalline cellulose, stearic acid, titanium dioxide and other ingredients.

Each 7.5 mg Pilocarpine Hydrochloride Tablet for oral administration contains 7.5 mg of pilocarpine hydrochloride. Inactive ingredients in the tablet, the tablet's film coating, and polishing are: carnauba wax, hypromellose, microcrystalline cellulose, stearic acid, titanium dioxide, FD&C blue # 2 aluminum lake, and other ingredients.

What does Pilocarpine hydrochloride look like?

What are the available doses of Pilocarpine hydrochloride?

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What should I talk to my health care provider before I take Pilocarpine hydrochloride?

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How should I use Pilocarpine hydrochloride?

Pilocarpine Hydrochloride Tablets 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.

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 subsection of the section of this label for definitions of mild, moderate and severe hepatic impairment.

Head & Neck Cancer Patients:

Sjogren's Syndrome Patients:

What interacts with Pilocarpine hydrochloride?

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What are the warnings of Pilocarpine hydrochloride?

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What are the precautions of Pilocarpine hydrochloride?

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What are the side effects of Pilocarpine hydrochloride?

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What should I look out for while using Pilocarpine hydrochloride?

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.

Cardiovascular Disease:

Ocular:

Pulmonary Disease:

What might happen if I take too much Pilocarpine hydrochloride?

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How should I store and handle Pilocarpine hydrochloride?

The recommended storage temperature is at 2°C to 8°C (36°F to 46°F). Do not freeze or shake. Protect from light. Keep Mircera in the original package until use.Storage of prefilled syringes over the recommended temperature (2°C to 8°C), when necessary, is permissible only for temperatures up to 25°C (77°F) and for no more than 30 days.The recommended storage temperature is at 2°C to 8°C (36°F to 46°F). Do not freeze or shake. Protect from light. Keep Mircera in the original package until use.Storage of prefilled syringes over the recommended temperature (2°C to 8°C), when necessary, is permissible only for temperatures up to 25°C (77°F) and for no more than 30 days.Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371Pilocarpine Hydrochloride Tablets, 5 mg, are white, film coated, debossed round tablets, coded SAL 5. Each tablet contains 5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2801-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Pilocarpine Hydrochloride Tablets, 7.5 mg, are blue, film coated, debossed round tablets, coded SAL 7.5. Each tablet contains 7.5 mg pilocarpine hydrochloride. They are supplied as follows:NDC 0228-2837-11 bottles of 100 with a child-resistant closure.Store up to 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).Manufactured for:Activis Elizabeth LLC200 Elmora Avenue,Elizabeth, NJ 07207 USAby: Patheon Inc.Toronto, Ontario, L5N 7K940-9055Rev – Jan 2009201371

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Pharmacodynamics:

In a study of 12 healthy male volunteers there was a dose-related increase in unstimulated salivary flow following single 5 and 10 mg oral doses of pilocarpine hydrochloride tablets. This effect of pilocarpine on salivary flow was time-related with an onset at 20 minutes and a peak effect at 1 hour with a duration of 3 to 5 hours (See Pharmacokinetics section).

Head & Neck Cancer Patients:

Sjogren's Syndrome Patients:

Pharmacokinetics:

When taken with a high fat meal by 12 healthy male volunteers, there was a decrease in the rate of absorption of pilocarpine from pilocarpine hydrochloride tablets. Mean T were 1.47 and 0.87 hours, and mean C were 51.8 and 59.2 ng/mL for fed and fasted, respectively.

Limited information is available about the metabolism and elimination of pilocarpine in humans. Inactivation of pilocarpine is thought to occur at neuronal synapses and probably in plasma. Pilocarpine and its minimally active or inactive degradation products, including pilocarpic acid, are excreted in the urine. Pilocarpine does not bind to human or rat plasma proteins over a concentration range of 5 to 25,000 ng/mL. The effect of pilocarpine on plasma protein binding of other drugs has not been evaluated. In patients with mild to moderate hepatic impairment (N=12), administration of a single 5 mg dose resulted in a 30% decrease in total plasma clearance and a doubling of exposure (as measured by AUC). Peak plasma levels were also increased by about 30% and half-life was increased to 2.1 hrs.

There were no significant differences in the pharmacokinetics of oral pilocarpine in volunteer subjects (N=8) with renal insufficiency (mean creatinine clearances 25.4 mL/min; range 9.8 – 40.8 mL/min) compared to the pharmacokinetics previously observed in normal volunteers.

Clinical Studies:

Head & Neck Cancer Patients:

A 12 week randomized, double-blind, placebo-controlled study in 207 patients (142 men, 65 women) was conducted in patients whose mean age was 58.5 years with a range of 19 to 77; the racial distribution was Caucasian 95%, Black 4%, and other 1%. In this population, a statistically significant improvement in mouth dryness occurred in the 5 and 10 mg pilocarpine hydrochloride tablets treated patients compared to placebo treated patients. The 5 and 10 mg treated patients could not be distinguished. (See section for flow study details.)

Another 12 week, double-blind, randomized, placebo-controlled study was conducted in 162 patients whose mean age was 57.8 years with a range of 27 to 80; the racial distribution was Caucasian 88%, Black 10%, and other 2%. The effects of placebo were compared to 2.5 mg three times a day of pilocarpine hydrochloride tablets for 4 weeks followed by adjustment to 5 mg three times a day and 10 mg three times a day. Lowering of the dose was necessary because of adverse events in 3 of 67 patients treated with 5 mg of pilocarpine hydrochloride tablets and in 7 of 66 patients treated with 10 mg of pilocarpine hydrochloride tablets. After 4 weeks of treatment, 2.5 mg of pilocarpine hydrochloride tablets three times a day was comparable to placebo in relieving dryness. In patients treated with 5 mg and 10 mg of pilocarpine hydrochloride tablets, the greatest improvement in dryness was noted in patients with no measurable salivary flow at baseline.

In both studies, some patients noted improvement in the global assessment of their dry mouth, speaking without liquids, and a reduced need for supplemental oral comfort agents.

In the two placebo-controlled clinical trials, the most common adverse events related to drug, and increasing in rate as dose increases, were sweating, nausea, rhinitis, diarrhea, chills, flushing, urinary frequency, dizziness, and asthenia. The most common adverse experience causing withdrawal from treatment was sweating (5 mg t.i.d.≤1%; 10 mg t.i.d.=12%).

Sjogren's Syndrome Patients:

Arthritis Rheum

A 12-week, randomized, double-blind, parallel-group, placebo-controlled study was conducted in 256 patients (14 men, 242 women) whose mean age was 57 years with a range of 24 to 85 years. The racial distribution was as follows: Caucasian 91%, Black 6%, and other 3%.

The effects of placebo were compared with those of pilocarpine hydrochloride tablets 5 mg four times a day (20 mg/day) for 6 weeks. At 6 weeks, the patients' dosage was increased from 5 mg pilocarpine hydrochloride tablets q.i.d. to 7.5 mg q.i.d. The data collected during the first 6 weeks of the trial were evaluated for safety and efficacy, and the data of the second 6 weeks of the trial were used to provide additional evidence of safety.

After 6 weeks of treatment, statistically significant global improvement of dry mouth was observed compared to placebo. “Global improvement” is defined as a score of 55 mm or more on a 100 mm visual analogue scale in response to the question, “Please rate your present condition of dry mouth (xerostomia) compared with your condition at the start of this study. Consider the changes to your dry mouth and other symptoms related to your dry mouth that have occurred since you have taken this medication.” Patients' assessments of specific dry mouth symptoms such as severity of dry mouth, mouth discomfort, ability to speak without water, ability to sleep without drinking water, ability to swallow food without drinking, and a decreased use of saliva substitutes were found to be consistent with the significant global improvement described.

Another 12 week randomized, double-blind, parallel-group, placebo-controlled study was conducted in 373 patients (16 men, 357 women) whose mean age was 55 years with a range of 21 to 84. The racial distribution was Caucasian 80%, Oriental 14%, Black 2%, and 4% of other origin. The treatment groups were 2.5 mg pilocarpine tablets, 5 mg pilocarpine hydrochloride tablets, and placebo. All treatments were administered on a four times a day regimen.

After 12 weeks of treatment, statistically significant global improvement of dry mouth was observed at a dose of 5 mg compared with placebo. The 2.5 mg (10 mg/day) group was not significantly different than placebo. However, a subgroup of patients with rheumatoid arthritis tended to improve in global assessments at both the 2.5 mg q.i.d. (9 patients) and 5 mg q.i.d. (16 patients) dose (10-20 mg/day). The clinical significance of this finding is unknown.

Patients' assessments of specific dry mouth symptoms such as severity of dry mouth, mouth discomfort, ability to sleep without drinking water, and decreased use of saliva substitutes were also found to be consistent with the significant global improvement described when measured after 6 weeks and 12 weeks of pilocarpine hydrochloride tablets use.

Non-Clinical Toxicology

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.

Cardiovascular Disease:

Ocular:

Pulmonary Disease:

Pilocarpine should be administered with caution to patients taking beta-adrenergic antagonists because of the possibility of conduction disturbances. Drugs with parasympathomimetic effects administered concurrently with pilocarpine would be expected to result in additive pharmacologic effects. Pilocarpine might antagonize the anticholinergic effects of drugs used concomitantly. These effects should be considered when anticholinergic properties may be contributing to the therapeutic effect of concomitant medication (e.g., atropine, inhaled ipratropium).

While no formal drug interaction studies have been performed, the following concomitant drugs were used in at least 10% of patients in either or both Sjogren's efficacy studies: acetylsalicylic acid, artificial tears, calcium, conjugated estrogens, hydroxychloroquine sulfate, ibuprofen, levothyroxine sodium, medroxyprogesterone acetate, methotrexate, multivitamins, naproxen, omeprazole, paracetamol, and prednisone.

Pilocarpine toxicity is characterized by an exaggeration of its parasympathomimetic effects. These may include: headache, visual disturbance, lacrimation, sweating, respiratory distress, gastrointestinal spasm, nausea, vomiting, diarrhea, atrioventricular block, tachycardia, bradycardia, hypotension, hypertension, shock, mental confusion, cardiac arrhythmia, and tremors.

The dose-related cardiovascular pharmacologic effects of pilocarpine include hypotension, hypertension, bradycardia, and tachycardia. Pilocarpine should be administered with caution to patients with known or suspected cholelithiasis or biliary tract disease.

Contractions of the gallbladder or biliary smooth muscle could precipitate complications including cholecystitis, cholangitis, and biliary obstruction. Pilocarpine may increase ureteral smooth muscle tone and could theoretically precipitate renal colic (or "ureteral reflux"), particularly in patients with nephrolithiasis.

Cholinergic agonists may have dose-related central nervous system effects. This should be considered when treating patients with underlying cognitive or psychiatric disturbances.

Hepatic Insufficiency:

Reference: Pugh RNH, Murray-Lyon IM, Dawson JL, Pietroni MC, Williams R. Transection of the oesophagus for bleeding oesophageal varices. 1973; 60:646-9.

Head & Neck Cancer Patients:

The most frequent adverse experiences associated with pilocarpine hydrochloride tablets were a consequence of the expected pharmacologic effects of pilocarpine.

In addition, the following adverse events (≥3% incidence) were reported at dosages of 15-30 mg/day in the controlled clinical trials:

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.

Body as a whole: body odor, hypothermia, mucous membrane abnormality

Cardiovascular: bradycardia, ECG abnormality, palpitations, syncope

Digestive: anorexia, increased appetite, esophagitis, gastrointestinal disorder, tongue disorder

Hematologic: leukopenia, lymphadenopathy

Nervous: anxiety, confusion, depression, abnormal dreams, hyperkinesia, hypesthesia, nervousness, paresthesias, speech disorder, twitching

Respiratory: increased sputum, stridor, yawning

Skin: seborrhea

Special senses: deafness, eye pain, glaucoma

Urogenital: dysuria, metrorrhagia, urinary impairment

In long-term treatment were two patients with underlying cardiovascular disease of whom one experienced a myocardial infarct and another an episode of syncope. The association with drug is uncertain.

Sjogren's Syndrome Patients:

In addition, the following adverse events (≥3% incidence) were reported at dosages of 20 mg/day in the controlled clinical trials:

The following events were reported in Sjogren's patients at incidences of 1% to 2% at dosing of 20 mg/day: accidental injury, allergic reaction, back pain, blurred vision, constipation, increased cough, edema, epistaxis, face edema, fever, flatulence, glossitis, lab test abnormalities, including chemistry, hematology, and urinalysis, myalgia, palpitation, pruritus, somnolence, stomatitis, tachycardia, tinnitus, urinary incontinence, urinary tract infection, and vaginitis.

The following events were reported rarely in treated Sjogren's patients (<1%) at dosing of 10-30 mg/day: Causal relation is unknown.

Body as a whole: chest pain, cyst, death, moniliasis, neck pain, neck rigidity, photosensitivity reaction

Cardiovascular: angina pectoris, arrhythmia, ECG abnormality, hypotension, hypertension, intracranial hemorrhage, migraine, myocardial infarction

Digestive: anorexia, bilirubinemia, cholelithiasis, colitis, dry mouth, eructation, gastritis, gastroenteritis, gastrointestinal disorder, gingivitis, hepatitis, abnormal liver function tests, melena, nausea & vomiting, pancreatitis, parotid gland enlargement, salivary gland enlargement, sputum increased, taste loss, tongue disorder, tooth disorder

Hematologic: hematuria, lymphadenopathy, abnormal platelets, thrombocythemia, thrombocytopenia, thrombosis, abnormal WBC

Metabolic and Nutritional: peripheral edema, hypoglycemia

Musculoskeletal: arthralgia, arthritis, bone disorder, spontaneous bone fracture, pathological fracture, myasthenia, tendon disorder, tenosynovitis

Nervous: aphasia, confusion, depression, abnormal dreams, emotional lability, hyperkinesia, hypesthesia, insomnia, leg cramps, nervousness, paresthesias, abnormal thinking, tremor

Respiratory: bronchitis, dyspnea, hiccup, laryngismus, laryngitis, pneumonia, viral infection, voice alteration

Skin: alopecia, contact dermatitis, dry skin, eczema, erythema nodosum, exfoliative dermatitis, herpes simplex, skin ulcer, vesiculobullous rash

Special Senses: cataract, conjunctivitis, dry eyes, ear disorder, ear pain, eye disorder, eye hemorrhage, glaucoma, lacrimation disorder, retinal disorder, taste perversion, abnormal vision

Urogenital: breast pain, dysuria, mastitis, menorrhagia, metrorrhagia, ovarian disorder, pyuria, salpingitis, urethral pain, urinary urgency, vaginal hemorrhage, vaginal moniliasis

The following adverse experiences have been reported rarely with ocular pilocarpine: A-V block, agitation, ciliary congestion, confusion, delusion, depression, dermatitis, middle ear disturbance, eyelid twitching, malignant glaucoma, iris cysts, macular hole, shock, and visual hallucination.

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.

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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