Effect of monatepil, a calcium channel blocker in ocular hypertensive rabbits
More details
Hide details
Department of Pharmacology, Institute of Pharmacy, Nirma University, Gujarat, India
Department of Pharmacology, L. M. College of Pharmacy, Gujarat, India
Department of Pharmacy, NIMS University, Shobha Nagar, Rajasthan, India
Submission date: 2016-08-11
Acceptance date: 2016-11-16
Online publication date: 2017-03-10
Publication date: 2019-12-19
Corresponding author
Shital S Panchal   

Department of Pharmacology, Institute of Pharmacy, Nirma University, Ahmedabad 382481, Gujarat, India. Tel.: +91 2717 241901; fax: +91 2717 241916.
Pol. Ann. Med. 2017;24(2):171-174
Increased ocular hypertension is one of the main characteristics of glaucoma. Monatepil belongs to a class of calcium channel blockers with special characteristic of α1-adrenergic receptor blocking effect. Calcium channel blockers and α1-adrenergic receptor blocker act as antihypertensive agents.

Monatepil has been studied for its effect on ocular hypertension in experimental glaucoma and for its mechanism of action for effect in glaucoma.

Material and methods:
After pretreatment with topical monatepil (1%), 5% dextrose has been administered intravenously through marginal ear vein in healthy New Zealand white rabbits. Pilocarpine (1%) was used as the reference standard. Freshly prepared 50 units of α-chymotrypsin was injected in the posterior chamber of the eye to induce chronic model of glaucoma. After achievement of steady ocular hypertension, single dose treatment with monatepil (1%) and pilocarpine (1%) was given. To find possible mechanism of action, interaction of monatepil with pilocarpine and indomethacin has been studied.

Results and discussion:
Topical administration of monatepil prevented acute increase in intraocular pressure. Monatepil (1%) and pilocarpine (1%) produced a significant decrease in intraocular pressure in α-chymotrypsin induced chronic ocular hypertensive rabbits. Indomethacin (1%) and pilocarpine (1%) pretreatment did not alter intraocular pressure lowering effect of monatepil.

Monatepil give beneficial effect in ocular hypertension by enhancement of aqueous humor outflow.

None declared.
Whitson JT. Glaucoma: a review of adjunctive therapy and new management strategies. Expert Opin Pharmacother. 2007;8(18):3237–3249.
Shah GB, Sharma S, Mehta AA, Goyal RK. Oculohypotensive effect of angiotensin-converting enzyme inhibitors in acute and chronic models of glaucoma. J Cardiovasc Pharmacol. 2000;36(2):169–175.
Kaneko Y, Oha M, Inoue T, et al. Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm's canal endothelial cells. Sci Rep. 2016;6:19640.
Uusitalo H, Kähönen M, Ropo A, et al. Improved systemic safety and risk-benefit ratio of topical 0.1% timolol hydrogel compared with 0.5% timolol aqueous solution in the treatment of glaucoma. Graefes Arch Clin Exp Ophthalmol. 2006;244(11):1491–1496.
Brubaker RF. The physiology of aqueous humor formation. In: Drance SM, Neufeld AH, eds. Glaucoma. Applied Pharmacology in Medical Treatment. New York: Grune & Startton; 1984:35–70.
Kelly SP, Walley TJ. Effect of calcium antagonist nifedipine on intraocular pressure in normal subjects. Br J Ophthalmol. 1988;72(3):216–218.
Santafé J, Martínez de Ibarreta MJ, Segarra J, Melena J. Along lasting hypotensive effect of topical diltiazem on the intraocular pressure in conscious rabbits. Naunyn Schmiedebergs Arch Pharmacol. 1997;355(5):645–650.
Mittag TW, Tormay A, Messenger M, Podos SM. Ocula hypotension in the rabbit. Receptor mechanisms of pirbuterol and nylidrin. Invest Ophthalmol Vis Sci. 1985;26(2):163–169.
Netland PA, Ericson KA. Calcium channel blockers in glaucoma management. Ophthalmol Clin North Am. 1995;8:327–334.
Panchal SS, Mehta AA, Santani DD. Effect of potassium channel openers in acute and chronic models of glaucoma. Taiwan J Ophthalmol. 2016;6(3):131–135.
Phelps CD, Asseff CF, Weisman RL, Podos SM, Becker B. Blood reflux into Schlemm's canal. Arch Ophthalmol. 1972;88(6):625–631.
Alm A, Bill A. The effect of stimulation of the cervical sympathetic chain on retinal oxygen tension and on uveal, retinal and cerebral blood flow in cats. Acta Physiol Scand. 1973;88(1):84–94.
Gasser P. Ocular vasospasm: a risk factor in the pathogenesis of low-tension glaucoma. Int Ophthalmol. 1989;13(4):281–290.
Bonomi L, Tomazzoli L, Jaria D. An improved model of experimentally induced ocular hypertension in the rabbit. Invest Ophthalmol. 1976;15(9):781–784.
Sears D, Sears M. Blood-aqueous barrier and alphachymotrypsin glaucoma in rabbits. Am J Ophthalmol. 1974;77(3):378–383.
Ling Z, Thompson WY, Potter DE. Multiple cyclic nucleotide phosphodiesterases in human trabecular meshwork cells. Invest Ophthalmol Vis Sci. 1999;40(8):1745–1752.
Crawford K, Kaufman PL. Pilocarpine antagonizes prostaglandin F2 alpha-induced ocular hypotension in monkeys. Evidence for enhancement of Uveoscleral outflow by prostaglandin F2 alpha. Arch Ophthalmol. 1987;105(8):1112–1116.
Gupta SK, Agarwal R, Galpalli ND, Srivastava S, Agrawal SS, Saxena R. Comparative efficacy of pilocarpine, timolol and latanoprost in experimental models of glaucoma. Methods Find Exp Clin Pharmacol. 2007;29(10):665–671.
Monica ML, Hesse RJ, Messerli FH. The effect of a calciumchannel blocking agent on intraocular pressure. Am J Ophthalmol. 1983;96(6):814.
Abelson MB, Gilbert CM, Smith LM. Sustained reduction of intraocular pressure in humans with the calcium channel blocker verapamil. Am J Ophthalmol. 1988;105(2):155–159.
Roth M, Eickelberg O, Kohler E, Erne P, Block LH. Ca2+ channel blockers modulate metabolism of collagens within the extracellular matrix. Proc Natl Acad Sci USA. 1996;93(11):5478–5482.
Mayama C. Calcium channels and their blockers in intraocular pressure and glaucoma. Eur J Pharmacol. 2014;739:96–105.
Ikeno A, Nose I, Fukuya F, Takeyama K, Hosoki K, Karasawa T. Antihypertensive effects of AJ-2615, a new calcium antagonist with a1-adrenergic blocking activity in experimental hypertensive animals. J Cardiovasc Pharmacol. 1993;21:815–821.
Minato H, Ikeno A, Yamada T, et al. Inhibitory effect of the new calcium antagonist AJ-2615 on progression of atherosclerosis in cholesterol-fed rabbits. J Cardiovasc Pharmacol. 1993;21(4):663–669.
Altan-Yaycioglu R, Yaycioglu O, Tufan H, Akova YA, Ozkardes H. The effects of systemic alpha-1 adrenergic antagonists on pupil diameter in rats. Curr Eye Res. 2007;32(3):217–221.
Journals System - logo
Scroll to top