Pilocarpine

Source: Wikipedia, the free encyclopedia.
Pilocarpine
Clinical data
Trade namesIsopto Carpine, Salagen, Vuity, others
AHFS/Drugs.comMonograph
MedlinePlusa608039
License data
Pregnancy
category
  • AU: B3
ATC code
Legal status
Legal status
Pharmacokinetic data
Elimination half-life0.76 hours (5 mg), 1.35 hours (10 mg)[3]
Excretionurine
Identifiers
  • (3S,4R)-3-Ethyl-4-((1-methyl-1H-imidazol-5-yl)methyl)dihydrofuran-2(3H)-one
JSmol)
  • O=C2OC[C@H](Cc1n(cnc1)C)[C@@H]2CC
  • InChI=1S/C11H16N2O2/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2/h5,7-8,10H,3-4,6H2,1-2H3/t8-,10-/m0/s1 checkY
  • Key:QCHFTSOMWOSFHM-WPRPVWTQSA-N checkY
  (verify)

Pilocarpine is a medication used to reduce

primary open angle glaucoma, and to constrict the pupil after dilation.[1][5][6] However, due to its side effects it is no longer typically used for long-term management.[7] Onset of effects with the drops is typically within an hour and lasts for up to a day.[1] By mouth it is used for dry mouth as a result of Sjögren syndrome or radiation therapy.[8]

Common side effects of the eye drops include irritation of the eye, increased tearing, headache, and blurry vision.

aqueous humor to drain from the eye.[1]

Pilocarpine was isolated in 1874 by Hardy and Gerrard and has been used to treat glaucoma for more than 100 years.[11][12][13] It is on the World Health Organization's List of Essential Medicines.[14] It was originally made from the South American plant Pilocarpus.[11]

Medical uses

Pilocarpine stimulates the secretion of large amounts of

sweat.[15] It is used to prevent or treat dry mouth, particularly in Sjögren syndrome, but also as a side effect of radiation therapy for head and neck cancer.[16]

It may be used to help differentiate Adie syndrome from other causes of unequal pupil size.[17][18]

It may be used to treat a form of

dry eye called aqueous deficient dry eye (ADDE)[19]

Surgery

Pilocarpine is sometimes used immediately before certain types of corneal grafts and cataract surgery.[20][21] It is also used prior to YAG laser iridotomy. In ophthalmology, pilocarpine is also used to reduce symptomatic glare at night from lights when the patient has undergone implantation of phakic intraocular lenses; the use of pilocarpine would reduce the size of the pupils, partially relieving these symptoms.[dubious ] The most common concentration for this use is pilocarpine 1%.[citation needed] Pilocarpine is shown to be just as effective as apraclonidine in preventing intraocular pressure spikes after laser trabeculoplasty.[22]

Presbyopia

In 2021, the

US Food and Drug Administration approved pilocarpine hydrochloride as an eyedrop treatment for presbyopia, age-related difficulty with near-in vision. It works by causing the pupils to constrict, increasing depth of field, similar to the effect of pinhole glasses. Marketed as Vuity, the effect lasts for more than 6 hours.[23][24]

Other

Pilocarpine is used to stimulate sweat glands in a sweat test to measure the concentration of chloride and sodium that is excreted in sweat. It is used to diagnose cystic fibrosis.[25]

Adverse effects

Use of pilocarpine may result in a range of adverse effects, most of them related to its

non-selective action as a muscarinic receptor agonist. Pilocarpine has been known to cause excessive salivation, sweating, bronchial mucus secretion, bronchospasm, bradycardia, vasodilation, and diarrhea. Eye drops can result in brow ache and chronic use in miosis. It can also cause temporary blurred vision or darkness of vision, temporary shortsightedness, hyphema
and retinal detachment.

Pharmacology

Pilocarpine is a drug that acts as a muscarinic receptor agonist. It acts on a subtype of muscarinic receptor (

accommodative spasm) it causes the eye's lens to thicken and move forward within the eye. This movement causes the iris (which is located immediately in front of the lens) to also move forward, narrowing the Anterior chamber angle. Narrowing of the anterior chamber angle increases the risk of increased intraocular pressure.[26]

Society and culture

Preparation

Plants in the genus Pilocarpus are the only known sources of pilocarpine, and commercial production is derived entirely from the leaves of Pilocarpus microphyllus (Maranham Jaborandi). This genus grows only in South America, and Pilocarpus microphyllus is native to several states in northern Brazil.[27]

Pilocarpine is extracted from the powdered leaf material in a multi-step process. First the material is treated with ethanol acidified with hydrochloric acid, and the solvents removed under reduced pressure. The resultant aqueous residue is neutralized with ammonia and put aside until the resin has completely settled. It is then filtered and concentrated by sugar solution to a small volume, made alkaline with ammonia, and finally extracted with chloroform. The solvent is removed under reduced pressure.[verification needed]

[28]

Trade names

Pilocarpine is available under several trade names such as: Diocarpine (Dioptic), Isopto Carpine (Alcon), Miocarpine (CIBA Vision), Ocusert Pilo-20 and -40 (Alza), Pilopine HS (Alcon), Salagen (MGI Pharma), Scheinpharm Pilocarpine (Schein Pharmaceutical), Timpilo (Merck Frosst), and Vuity (AbbVie).

Research

Pilocarpine is used to induce chronic

IgA
antibodies.

Veterinary

Pilocarpine is given in moderate doses (about 2 mg) to induce emesis in cats that have ingested foreign plants, foods, or drugs. One feline trial determined it was effective, even though the usual choice of

]

References

  1. ^ a b c d e f g "Pilocarpine". The American Society of Health-System Pharmacists. Archived from the original on 28 December 2016. Retrieved 8 December 2016.
  2. ^ "Vuity- pilocarpine hydrochloride solution/ drops". DailyMed. Retrieved 19 December 2021.
  3. PMID 15243470
    .
  4. .
  5. .
  6. ^ "Glaucoma and ocular hypertension. NICE guideline 81". National Institute for Health and Care Excellence. November 2017. Retrieved 19 September 2019. Ocular hypertension... alternative options include carbonic anhydrase inhibitors such as brinzolamide or dorzolamide, a topical sympathomimetic such as apraclonidine or brimonidine tartrate, or a topical miotic such as pilocarpine, given either as monotherapy or as combination therapy.
  7. S2CID 73438590
    . Pilocarpine is no longer routinely used for long term IOP control due to a poor side effect profile
  8. .
  9. ^ "Pilocarpine ophthalmic Use During Pregnancy | Drugs.com". www.drugs.com. Archived from the original on 28 December 2016. Retrieved 28 December 2016.
  10. .
  11. ^ from the original on 2016-12-29.
  12. .
  13. .
  14. . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  15. ^ "Pilocarpine". MedLinePlus. U.S. National Library of Medicine. Archived from the original on 2010-03-06.
  16. PMID 26867879
    .
  17. .
  18. .
  19. .
  20. ^ Parker J (2017). Descemet Membrane Endothelial Keratoplasty (DMEK): A Review (PDF) (Thesis). Leiden University.
  21. .
  22. .
  23. .
  24. ^ Vuity Label, Revised: 10/2021. Linked from FDA page for Vuity
  25. .
  26. .
  27. .
  28. .
  29. .
  30. .

External links

  • "Pilocarpine". Drug Information Portal. U.S. National Library of Medicine.