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Prostaglandin analogues: current treatment option for glaucoma

Medicinal Chemistry Research volume 25, pages 1031–1048 (2016)Cite this article

Abstract

Glaucoma is a progressive optic neuropathy and is the world’s second leading cause of blindness. It is a multifactorial disease that is etiologically complex where elevated intraocular pressure in the eye is the major risk factor. Prostaglandin analogues are the first-line drugs in today’s glaucoma therapy. These are 20 carbon atom naturally occurring fatty acid derivatives biosynthesized from arachidonic acid. They involve COX pathway where arachidonic acid interacts with COX in the presence of oxygen and heme and produces PGG2. It is a cyclic endoperoxide with very short half life and generates PGH2 through its peroxidase activity. PGH2 further produces PGE2 in the presence of PGE isomerase, PGD2 by the actions of isomerases or glutathione-S-transferase and PGF2α by an endoperoxide reductase system. Various synthetic analogues of these naturally occurring prostaglandins have been discussed in the current review which act by decreasing the intraocular pressure through a pathway which increases the uveoscleral and trabecular outflow. The tromethamine salt of PGF2α was the first prostaglandin analogue used as an antiglaucoma agent, and later on it was replaced by various FP (latanoprost, bimatoprost, travoprost, tafluprost, etc.), EP (butaprost) and DP (BW245C, ZK118182, AL 6598) analogues. Most of the drugs are prodrugs and after hydrolysis give their respective acids in the aqueous humor. Inspite of the side effects, these are widely used alone or in combination.

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Acknowledgments

We would like to thanks All India Council of Technical Education and Department of Science and Technology, New Delhi for the research grant.

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  1. UGC-Center of Advanced Study (UGC-CAS), University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India

    Poonam Piplani, Deepali Aggarwal, Vasudha Abbhi & Lovneet Saini

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Piplani, P., Aggarwal, D., Abbhi, V. et al. Prostaglandin analogues: current treatment option for glaucoma. Med Chem Res 25, 1031–1048 (2016). https://doi.org/10.1007/s00044-016-1563-5

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Keywords

  • Glaucoma
  • Intraocular pressure
  • Arachidonic acid
  • Prostaglandins
  • Uveoscleral outflow
  • Trabecular outflow