pilocarpine (systemic)

REMS

Dry mouth that may occur as a consequence of radiation therapy for cancer of the head and neck.
Dry mouth in patients with Sjögren syndrome.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Uncontrolled asthma;
Angle-closure glaucoma;
Iritis;
Lactation: Lactation.

Use Cautiously in:

Pulmonary disease (asthma, bronchitis, or chronic obstructive pulmonary disease);
Biliary tract disease or cholelithiasis;
Cardiovascular disease;
Retinal disease;
Nephrolithiasis;
Psychiatric or cognitive disorders;
OB: Safety not established in pregnancy;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, hypertension, tachycardia

Derm: flushing, sweating

EENT: amblyopia, epistaxis, rhinitis, voice change

GI: nausea, vomiting, dyspepsia, dysphagia

GU: urinary frequency

Neuro: dizziness, headache, tremors, weakness.

Misc: chills

Interactions ⬆ ⬇

Drug-drug:

Anticholinergics will ↓ effectiveness.
Bethanechol or ophthalmic cholinergics may result in ↑ cholinergic effects.
Beta-blockers may ↑ the risk of adverse cardiovascular reactions (conduction disturbances).

Availability ⬆ ⬇

(Generic available)

Tablets: 5 mg; 7.5 mg

Route/Dosage ⬆ ⬇

Patients with Head and Neck Cancer

PO (Adults ): 5 mg three times daily initially, then titrated to need/response; usual range 15–30 mg/day (no single should exceed 10 mg).

Patients with Sjögren Syndrome

PO (Adults ): 5 mg four times daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Stimulates cholinergic receptors, resulting in primarily muscarinic action, including stimulation of exocrine glands.
Other effects include:
- Increased sweating, gastric secretions,
- Increased bronchial secretions,
- Increased tone and motility of the urinary tract, gallbladder, and biliary duct smooth muscle.

Therapeutic effects:

Increased salivary gland secretion.

Classifications ⬆ ⬇

Therapeutic Classification: none assigned

Pharmacologic Classification: cholinergics

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed after oral administration.

Distribution: Unknown.

Metabolism/Excretion: Inactivated at neuronal synapses and in plasma. Some unchanged pilocarpine and metabolites are excreted in urine.

Half-Life: After 5-mg dose for 2 days: 0.8 hr; after 10-mg dose for 2 days: 1.3 hr.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	20 min	1 hr	3–5 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed.
Caution patient that pilocarpine may cause visual changes, especially at night; avoid driving or other activities requiring alertness until effects of medication are known.
Advise patient to drink adequate daily fluids (1500–2000 mL/day), especially if sweating occurs. Less than adequate fluid intake may lead to dehydration.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding.

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Indications ⬇