Name of Medications: pilocarpine oral / PYYE loe-KAR-peen / pYlarphtyl / pylocarpine / pylocarpine / pylocarpine
Abbreviations
Low dosages of calcium alginate/phosphatolyl sulphate. SJögrens syndrome – visual analog scale.
What is pilocarpine?
Pilocarpine is used to treat dry mouth caused by Sjogren’s syndrome , or by radiation to treat head and neck cancer.
Pilocarpine may also be used for purposes not listed in this medication guide.
Pilocarpine affects nervous systems and increases salivary secretions in the mouth.
Pilocarpine has been prescribed as a treatment for dry mouth induced by Sjogren syndrome.
The treatment of the neck and throat cancer can be induced by radiotherapy.
Pilocarpine has other uses that are not listed within the medication guide.
The only adverse effect was sweating, and no serious drug-related adverse events were reported.
This new, low-dose pilocarpine formulation was well-tolerated and resulted in significant improvements in symptoms of dry mouth and other xerostomic conditions in patients with Sjogrens Syndrome.
Precautions
Pilocarpine should not be used for the treatment of allergic reactions.
Tell your doctor about any respiratory condition that may cause glaucoma or vision damage and is not causing any symptoms.
FDA Category C. The effects of pilocarapine on a baby’s health cannot be confirmed.
Proper Usage – dry mouth
dry mouth secondary to Sjogren’s syndrome or dry mouth caused by radiation therapy.
Before Using
If one decides to use this medicine, its risks should be balanced with its benefits.
Obviously, your physician can decide the situation with you.
It is important that you visit your dentist regularly even though this medicine may make your dry mouth feel better.
Having a dry mouth condition makes you more likely to have dental and other mouth problems.
Warnings
You should not take pilocarpine if you have glaucoma or asthma.
Pilocarpine side effects
Get emergency medical care when you are exhibiting an allergic response.
Pilocarpine has a tendency to be dangerous.
Stop taking pilocarpine right away if you have:
- numb breathing;
- fast or slow blood flow;
- severe pain in your chest and ear;
- confusion,
- shaking and a light-headed sensation that you could faint.
Pilocarpine can be taken for several different health problems.
How should I take pilocarpine?
Follow the directions on the prescription.
Do not use it more frequently or less frequently than the recommended dosage.
Take pilocarpine in a single dose.
Take Pilocarpine with food or water.
The drug is very susceptible to causing excessive sweat and dehydration.
Use pilocarpine daily for best results.
Make sure your medication is refilled before the prescription is complete.
Store in a room with no moisture.
What should I avoid when taking pilocarpine?
Pilocarpine is a drug that has a tendency towards blurry eyes, particularly when used under light.
Take care of anything driving which requires clear visual awareness.
Keep yourself from overheating in exercise or during chilly conditions.
Pilocarpine increases sweat, and increases risk of dehydrating.
Precautions
It may affect your sight, especially at night.
This is possible to cause lightheadedness as well as dizziness.
Make sure your reactions are known when you drive or use a car or a device which could cause harm or irritate you.
Those symptoms may cause serious health issues. consult a physician.
This can make you sweat much more frequently.
When it happens drink more fluids in order to offset sweat to avoid losing a lot of fluid or dehydrating.
Your doctor may tell you not to take pilocarpine.
Tell your doctor if you have or have ever had chronic bronchitis or another type of:
- chronic obstructive pulmonary disease (COPD;
- a group of lung diseases that includes chronic bronchitis and emphysema);
- kidney stones;
- gallstones;
- mental illness;
- any condition that affects your ability to think;
- gallbladder, heart, or liver disease.
- if you are pregnant, plan to become pregnant, or are breast-feeding.
Allergies
Get emergency medical help if you have any of these signs of an allergic reaction :
- hives ;
- difficult breathing;
- swelling of your face, lips, tongue, or throat.
Pilocarpine may cause serious side effects.
Stop using pilocarpine and call your doctor at once if you have:
- shortness of breath;
- fast or slow heart rate ;
- severe headache ,
- pounding in your neck or ears;
- confusion
A very serious allergic reaction to this drug is rare.
However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction , including: rash , itching /swelling (especially of the face/ tongue /throat), severe dizziness, trouble breathing .
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines.
Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals.
Pilocarpine may cause blurred vision, especially at night or in low light. Be careful if you drive or do anything that requires you to be able to see clearly.
Histories
Sjögren syndrome (SS), a chronic inflammatory disease that has slow-growing stages is caused by lymphadyte infiltrating exocrerine glands and results in xerostomias.
Generally Sjogrens Syndrome sufferers are affected by exocrine dysfunction which causes them to suffer symptomatic sluggish gastrointestinal symptoms if saliva is not activated.
In addition, the chronic disease causes significant deplorability causing deteriorating patient health and decreased resiliency.
Pilocarpine is a muscarinitic agent characterized by moderate -adrenergic activity.
Pilocarpin is a cholinergic medicine Used for Dry mouth after radiotherapy; dry mouth and dry eyes in Sjögren’s syndrome.
Also called Salagen® Available as Tablets.
Pilocarpine is prescribed to relieve dry mouth (sometimes called xerostomia) brought on by radiotherapy to the head or neck.
Pilocarpine can also be used to relieve some of the symptoms of Sjögren’s syndrome .
Sjögren’s syndrome can cause various symptoms, the most common being dry eyes and dry mouth. These symptoms are due to lack of moisture in exocrine glands.
In research studies, use of pilocarpine tablets significantly improved symptoms of intraoral dryness, oral discomfort, and dysphonia and patients’ global assessment of dry mouth as well as reduced the need for administration of oral comfort agents such as artificial saliva, water, and hard candy.
Patients treated with pilocarpine tablets also demonstrated a statistically significant increase in saliva production, measured as either whole-mouth or parotid salivary flow. It is through this mechanism that cholinergic stimulation of residual-functioning exocrine glandular tissue in patients with Sjogren’s syndrome get relieve.
Whole-mouth salivary flow rates were measured.
Results: A significantly greater proportion of patients in the 5-mg pilocarpine group showed improvement compared with the placebo group (P< or =.01) in global assessments of dry mouth, dry eyes, and other symptoms of dryness (P< or =.05). Salivary flow was significantly improved.
Adverse Events
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%).
A review of adverse experiences in patients who entered the study with a history of respiratory abnormalities, including asthma (placebo group, n=31; 2.5-mg pilocarpine group, n=27; and 5-mg pilocarpine group, n=27), showed a comparable incidence of adverse events as that reported in the total population.
In the 5-mg pilocarpine group, the most commonly reported events (≥10%) vs placebo, respectively, were sweating (55.6% vs 12.9%), headache (14.8% vs 22.6%), nausea (22.2% vs 12.9%), flu syndrome (14.8% vs 6.5%), diarrhea (11.1% vs 3.2%), dizziness.
Adverse effects, was not superior to that of 0.9% saline at relieving subjective oral dryness.
While a high incidence of hyperhidrosis (40.6%) is problematic in patients taking Salagen® tablets, the incidence in the present study was low (1 participant, 4.2%).
The following additional adverse events, albeit mild, were caused by the LPA formulation: hot flushes ( n = 3), as well as headache, dizziness, abdominal pain, and rhinitis ( n = 1 each). Such adverse events are known in patients taking Salagen tablets.
In addition, blood pressure or heart rate, and no drug-related serious events were reported, including hematopoietic, renal, or hepatotoxic effects.
No significant drug interactions were noted.
This study did not demonstrate any pulmonary safety issues in this patient population.
However, the package insert 16 for Salagen tablets (oral pilocarpine) does note that pilocarpine should be administered with caution and under close supervision to patients with controlled asthma, chronic bronchitis, or chronic obstructive pulmonary disease requiring medical therapy.
Drug Interactions
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary.
Pilocarpine dosage information
When pilocarpine is used to treat dry mouth caused by radiotherapy in people who have head and neck cancer, it is usually taken three times a day.
When pilocarpine is used to treat dry mouth in people who have Sjogren’s syndrome, it is usually taken four times a day.
Take pilocarpine at around the same times every day. Follow the directions.
Usual Adult dosage for Xerostomia.
The lowest efficient dose is recommended for maintenance.
The maximum dose is 10 mg.
A minimum 12-week follow-up is necessary.
Treatment of mouth dryness caused by salivary gland hypofunction caused by radiotherapy in the head and neck.
Doses in adults are generally 5 g. orally 4 times a daily dose .
Although the data show that pilocarpine-induced stimulation of salivary flow occurred within 30 minutes of ingestion of the first dose and was maintained through week 12, the onset of subjective benefit for various symptoms took 6 to 12 weeks.
As one could predict from pilocarpine’s pharmacological effect, this investigation also suggests that pilocarpine tablets, at doses of 20 mg/d, can stimulate exocrine gland secretion in other organ systems besides the eyes and mouth.
At study end point, statistically significant improvement was also observed in other sicca symptoms associated with SS, including nasal dryness, dry skin, vaginitis sicca, and the ability to expectorate.
These data therefore suggest that treatment with pilocarpine tablets not only offers relief of symptoms of dry mouth and dry eyes but of whole-body.
Pilocarpine tablets at 20 mg/d significantly improves other specific symptoms of salivary gland hypofunction in patients with Sjogren’s Syndrome, such as oral discomfort, nocturnal fluid ingestion, and the need for saliva substitutes.
Some benefit for dysphonia (v0cal cord) may also occur, as evidenced by the trend toward statistically significant improvement in the 5-mg pilocarpine group for this symptom.
Although the data show that pilocarpine-induced stimulation of salivary flow occurred within 30 minutes of ingestion of the first dose and was maintained through week 12, the onset of subjective benefit for various symptoms took 6 to 12 weeks.
Safety
Objective To assess the safety and efficacy of pilocarpine (Salagen) tablets as symptomatic treatment for dry mouth and dry eyes caused by Sjoren’s syncrome in a multicenter, double-blind, placebo-controlled trial. After providing written informed consent, 373 patients with primary or secondary SS and clinically significant dry mouth and dry eyes were randomized to receive 2.5-mg pilocarpine, 5-mg pilocarpine, or placebo tablets 4 times daily for 12 weeks. Symptoms were assessed by questionnaires with visual analog scales or categorical checkboxes. No statistically adverse effects were noted.
In rats, a dosage of 18 mg/kg/day, which yielded a systemic exposure approximately 100 times larger than the maximum systemic exposure observed clinically, resulted in a statistically significant increase in the incidence of benign pheochromocytomas in both males and females, and a statistically significant increase in the incidence of hepatocellular adenomas in female rats.
The tumorigenicity observed in rats was observed only at a large multiple of the maximum labeled clinical dose, and may not be relevant to clinical use. No evidence that pilocarpine has the potential to cause genetic toxicity was obtained.
Proper use
Please follow all directions.
Take no longer unless prescribed and take a smaller dosage as needed.
This may cause side effects.
The dentist can help keep dry mouths from forming and reduce swelling.
Dry mouth makes your mouth more prone to gum disease.
Headache
Drink plenty of water and ask your pharmacist to recommend a suitable painkiller.
If the headaches continue, let your doctor know
Increased sweating and flushing.
Take care not to become overheated during exercise or hot weather.
Drink several large glasses of water every day .
Vision
Blurred vision, eye irritation or pain, watery eyes.
Do not drive and do not use tools or machines if you cannot see clearly (particularly at night or if you have difficulty seeing in poor lighting)
Stomach
Diarrhea, constipation, tummy ache (abdominal pain).
Try to eat a well-balanced diet.
Drink plenty of water.
What happens if I miss a dose?
Missed dose
Do not take two doses together to make up for the missed dose.
Take missed doses when you can’t recall them. Take a little while.
Skip the scheduled dose in case it’s time for another dose.
Don’t use extra medicine for a missed dose.
If you miss a dose of this medicine, take it as soon as possible.
However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
What happens if I overdose?
Call Poison Help at 1-800-222-1222 if there are any medical emergencies.
A severe dose of pilocarpine can result in death.
Discussion
During 28 days of preparing the LPA fluid (drip hydration) the pilocarpine content was largely unchanged at four °C.
The results showed stable formulation when stored within test containers at the test condition.
Each dose was individually sealed in a Hybripack® tube based on the study findings, with the expire date indicating the specified duration in the dark and cool environment.
Immediately Sjogren’s Ssyndrome patients with wet mouth had a significant increase in saliva.
In addition, intraoral conditions and everyday life were improved by continuously administering LPA treatment.
Head & Neck Cancer Patients In a 12 week randomized, double-blind, placebo-controlled study in 207 patients (placebo, N=65; 5 mg, N=73; 10 mg, N=69), increases from baseline (means 0.072 and 0.112 mL/min, ranges -0.690 to 0.728 and -0.380 to 1.689) of whole saliva flow for the 5 mg (63%) and 10 mg (90%) tablet, respectively.
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.
Conclusions
The new LPA formulation (Drip Hydration) increased intraoral xerostoma conditions by increasing salivary secretion.
References
Delaleu A. Jonson S. Koller M. Sjöggens syndrome. A randomized, controlled trial. 114-105; p. 135. Theoretical and empirical studies. Salivary disorders in Sjögre’s syndrome: A vital oral-systemic connection. Am dentist association. 2009;136:281. Journal of Public Library and Archives. Google Scholars, Rostron. Comparisons of health and quality of life between sjögren syndrome and xerostomia patients. Gérodontology. 2001; 19:54. 59. PubMed Google Scholar niaah gh, Baker J, Vivino F. Comparing the side effects of pilocarpene versus cevimeline to xerostomia in a primary Sjögren syndrome.
A multicenter, randomized, double-blind, placebo-controlled dose titration study of oral pilocarpine for treatment of radiation-induced xerostomia in head and neck cancer patients. J Clin Oncol. 1993;111124- 1131 Google Scholar 10. Vitali ABombardieri SMoutopoulos HM et al.
Salagen tablets Physicians’ Desk Reference. 51st ed. Montvale, NJ Medical Economics Books1997;1546- 1547
