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Pilocarpine Hydrochloride
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  • AHFS Monographs

Pilocarpine Hydrochloride

Class: Parasympathomimetic (Cholinergic) Agents
VA Class: AU900
Chemical Name: (3S-cis)-2(3H)-furanone, 3-ethyl-dihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl] mono-hydrochloride
Molecular Formula: C11H16N2O 2
CAS Number: 54-71-7
Brands: Salagen

Medically reviewed by Drugs.com on Jul 22, 2021. Written by ASHP.

Introduction

Cholinergic agonist; binds to muscarinic receptors.

Uses for Pilocarpine Hydrochloride

Radiation-induced Dry Mouth

Symptomatic treatment of radiation-induced dry mouth (xerostomia) in patients with head and neck cancer.

Dry Mouth Secondary to Sjögren Syndrome

Symptomatic treatment of dry mouth in patients with Sjögren syndrome.

There are few comparative studies of pilocarpine and cevimeline (a similar muscarinic agonist). Although both drugs can increase salivary flow and improve symptoms of dry mouth, adverse effects may differ based on differences in selectivity and affinity for muscarinic receptors. (See Actions.)

Pilocarpine Hydrochloride Dosage and Administration

Administration

Oral Administration

Administer orally 3–4 times daily.

Dosage

Available as pilocarpine hydrochloride; dosage expressed in terms of the salt.

Adults

Radiation-induced Dry Mouth
Oral

Initially, 5 mg 3 times daily; titrate dosage based on therapeutic response and tolerance.

Usual dosage range is 15–30 mg daily given in divided doses (not to exceed 10 mg per dose).

Adverse effects are dose related; use lowest effective and tolerated dosage for maintenance therapy.

At least 12 weeks of continuous therapy may be necessary to achieve therapeutic benefit.

Dry Mouth Secondary to Sjögren Syndrome
Oral

Recommended dosage is 5 mg 4 times daily. To minimize incidence of sweating, some clinicians recommend initiating therapy at a low dosage (e.g., 2 mg once or twice daily), then gradually increasing up to 5...