Pilocarpine (Salagen) oral formulation is used in the treatment of patients with dry mouth secondary to radiation of the head and neck. It may also be used in patients with Sjogren's syndrome.

Pilocarpine Uses:

• Xerostomia:
  • It is used for the symptomatic treatment of dry mouth that occurs due to salivary gland dysfunction in patients undergoing radiotherapy of the head and neck region.
  • It may be used for dry mouth in patients with Sjogren's syndrome.

Pilocarpine Dose in Adults

Dose in the treatment of Xerostomia: Oral:

• Associated with head and neck cancer:
  • Initial: 5 mg three times a day.
  • The dose may be treated based on the clinical response and tolerability.
  • The usual dosage range is  15 to 30 mg per day;
  • The maximum dose is 10 mg/dose.
• Sjögren syndrome:
  • 5 mg four times a day.

Use in Children:

Not indicated.   

Pregnancy Category: C

• The drug was not evaluated in animal reproduction studies.

Pilocarpine use during breastfeeding:

• It is unknown if the drug will be excreted into breast milk.
• The manufacturer suggests that infants are evaluated for side effects and to weigh the benefits of treatment in comparison to the risks.

Dose in Kidney Disease:

There are no dosage adjustments provided in the manufacturer’s labeling.   

Dose in Liver disease:

• Mild impairment (Child-Pugh score 5 to 6):
  • Adjustment in the dose is not necessary.
• Moderate impairment (Child-Pugh score 7 to 9):
  • Initial dose: 5 mg two times a day
  • Adjust the dose based on the patients' response and tolerance.
• Severe impairment (Child-Pugh score 10 to 15):
  • It is not recommended in patients with severe liver disease.

Common Side Effects of Pilocarpine:

• Cardiovascular:
  • Flushing
• Central Nervous System:
  • Chills
  • Dizziness
  • Headache
• Gastrointestinal:
  • Nausea
• Genitourinary:
  • Urinary Frequency
• Neuromuscular & Skeletal:
  • Weakness
• Respiratory:
  • Rhinitis
• Miscellaneous:
  • Diaphoresis

Less Common Side Effects Of Pilocarpine:

• Cardiovascular:
  • Edema
  • Facial Edema
  • Hypertension
  • Palpitation
  • Tachycardia
• Central Nervous System:
  • Pain
  • Fever
  • Somnolence
• Dermatologic:
  • Pruritus
  • Rash
• Gastrointestinal:
  • Diarrhea
  • Dyspepsia
  • Vomiting
  • Constipation
  • Flatulence
  • Glossitis
  • Salivation Increased
  • Stomatitis
  • Taste Perversion
• Genitourinary:
  • Vaginitis
  • Urinary Incontinence
• Neuromuscular & Skeletal:
  • Myalgias
  • Tremor
• Ocular:
  • Lacrimation
  • Amblyopia
  • Abnormal Vision
  • Blurred Vision
  • Conjunctivitis
• Otic:
  • Tinnitus
• Respiratory:
  • Cough Increased
  • Dysphagia
  • Epistaxis
  • Sinusitis
• Miscellaneous:
  • Allergic Reaction
  • Voice Alteration

Contraindications to Pilocarpine:

• Hypersensitivity to pilocarpine and any component of the formulation
• Uncontrolled asthma
• It is not recommended for patients with acute iritis and angle-closure eye glaucoma.

Warnings and precautions

• Cardiovascular disease
  • Patients suffering from cardiovascular disease should be cautious when using it, as they might experience a transient rhythm and/or hemodynamic changes.
• Cholelithiasis
  • Patients suffering from biliary tract diseases or cholelithiasis should be cautious.
• Hepatic impairment
  • Patients with advanced or severe liver disease should not use it. 
  • Moderate hepatic impairment may require a reduction of the dose. This should be avoided and used with caution.
• Nephrolithiasis
  • Smooth muscle spasms may occur. Patients with kidney stones should be cautious about using the drug as it can cause a urteral reflux and precipitate renal colic.
• Respiratory problems
  • Pilocarpine can increase bronchial smooth muscles tone and secretions. It also increases resistance to airway obstruction. 
  • Patients with chronic bronchitis, asthma, or chronic obstructive lung disease should not use it.

Pilocarpine (systemic): Drug Interaction

Monitoring Parameters:

Monitor ECG and the response to therapy.   

How to administer Pilocarpine?

• It should not be administered with a high-fat meal.
• Patients must be advised to take plenty of water to avoid dehydration.   

Mechanism of action of Pilocarpine:

It increases salivary gland secretion, such as sweat and salivary cells, and increases the tone and flexibility of the urinary tract.

The beginning of action:

• 20 minutes;
• Maximum effect: 1 hour

Duration:

• 3 to 5 hours

Half-life elimination:

• 0.76 to 1.35 hours;
• mild to moderate hepatic impairment: 2.1 hours

Time to peak, serum:

• 0.85 to 1.25 hours (increased to 1.47 hours with a high-fat meal)

Excretion:

• Urine

International Brands of Pilocarpine:

• Salagen

Pilocarpine Brand Names in Pakistan: