Pilocarpine

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Salagen; Belgium: Isopto Carpine, Pilo; Cyprus: Isopto Carpine, Pilopine-HS; Czech Republic: Pilocarpin, Pilogel, Pilopos; Denmark: Pilokarpin; Finland: Isopto Carpine, Minims Pilocarpine, Salagen; France: Pilocarpine; Germany: Pilocarpin, Pilomann, Pilopos, Salagen, Spersacarpin; Greece: Cidren, Dispercarpine, Isopto Carpine, Pilocarpine, Pilocollyre, Pilofar, Pilogel, Prothenol, Saglion, Salagen, Salivoral, Sumario, Xerocarp; Hungary: Humacarpin, Salagen; Ireland: Minims Pilocarpine, Pilocarpine, Pilogel, Salagen; Italy: Dropilton, Piloca, Pilocarpina, Salagen; Lithuania: Pilokarpin; Luxembourg: Asthenopin, Isopto Carpine, Pilocarpine, Pilomann, Salagen, Spersacarpine; Netherlands: Minims Pilocarpine, Pilogel; Poland: Isoptocarpine, Pilocarpinum, Pilogel, Pilomann, Salagen; Portugal: Salagen; Romania: Dropil; Slovakia: Pilocarpin, Pilokarpin; Slovenia: Salagen; Spain: Colircusí Pilocarpina, Isopto Carpina, Salagén; Sweden: Isopto Pilokarpin, Pilokarpin, Salagen; UK: Minims Pilocarpine, Pilogel, Salagen.

North America

Canada: Akarpine, Diocarpine, Isopto Carpine, Minims Pilocarpine, Pilocarpine, Pilocarpinum Muriaticum, Pilopine, Salagen; USA: Carpine, Pilocarpine, Pilopine, Salagen.

Latin America

Argentina: Isopto Carpina, Klonocarpina, Omaclopil, Sonadryl, Wetol; Brazil: Isopto Carpine, Pilocan, Pilocarpina; Mexico: Pil.

Asia

Japan: Adsorbocarpine, Pilocarpine, Salagen, Sanpilo.

Drug combinations

Pilocarpine and Carteolol

Pilocarpine and Hydroxypropyl Methylcellulose

Pilocarpine and Metipranolol

Pilocarpine and Timolol

Pilocarpine, D-Panthenol, Pyridoxine (Vitamin B~6~), and Salicylic Acid

Other Pilocarpine combinations: Dexpanthenol

Chemistry

Pilocarpine: C~11~H~16~N~2~O~2~. Mw: 208.26. 2(3H)-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-, (3S-cis)-. CAS-92-13-7.

Pilocarpine Hydrochloride: C~11~H~16~N~2~O~2~ HCl. Mw: 244.72. 2(3H)-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-, monohydrochloride, (3S-cis)-. CAS-54-71-7.

Pharmacologic Category

Antiglaucoma Agents; Miotics. Cholinergic Agonist. (ATC-Code: N07AX01; S01EB01).

Mechanism of action

Directly stimulates cholinergic receptors in eye causing miosis (by contraction of iris sphincter), loss of accommodation (by constriction of ciliary muscle), and lowering of intraocular pressure (with decreased resistance to aqueous humor outflow).

Therapeutic use

Management of chronic simple glaucoma, chronic and acute angle-closure glaucoma. Symptomatic treatment of xerostomia caused by salivary gland hypofunction resulting from radiotherapy for cancer of head and neck or Sjögren’s syndrome.

Pregnancy and lactiation implications

Lactation not recommended.

Unlabeled use

Counter effects of cycloplegics.

Contraindications

Hypersensitivity to pilocarpine or any component of the formulation. Acute inflammatory disease of anterior chamber of eye. Tablets also contraindicated in uncontrolled asthma, angle-closure glaucoma, severe hepatic impairment.

Warnings and precautions

Use with caution in cardiovascular disease (may have difficulty compensating for transient changes in hemodynamics or rhythm induced by pilocarpine). May cause decreased visual acuity, especially at night or with reduced lighting. Use caution with controlled asthma, chronic bronchitis or COPD (may increase airway resistance, bronchial smooth muscle tone, and bronchial secretions). Use caution with cholelithiasis, biliary tract disease, and nephrolithiasis.

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