Delving into the Latest Updates on Dorzolamide Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(4S,trans)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide, 4S,6S-dorzolamide, Dorzolamide hydrochloride (JP17/USP)

+ [5]

Target

CAs

Action

inhibitors

Mechanism

CAs inhibitors(Carbonic anhydrases inhibitors)

Therapeutic Areas

Eye Diseases

Active Indication

GlaucomaOcular Hypertension

Inactive Indication

Glaucoma, Open-Angle

Originator Organization

Merck & Co., Inc.

Active Organization

Santen Pharmaceutical Co., Ltd.

Inactive Organization

Merck Sharp & Dohme Corp.

Drug Highest PhaseApproved

First Approval Date

United States (09 Dec 1994),

Glaucoma, Open-AngleOcular Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC10H16N2O4S3

InChIKeyIAVUPMFITXYVAF-XPUUQOCRSA-N

CAS Registry120279-96-1

View All Structures (2)

This study is a double-blind randomized clinical trial in Diabetic patients (type 2) over 18 years of age who have diabetic macular edema with involvement of the central 1 millimeter (central macular thickness is more than 300 μm) and BCVA 20/30 or less who visit the retina clinic of Labbafinejad Hospital Are studied. (In patients with bilateral macular edema, only one eye is included in the study.) Complete ocular examinations (including best corrected visual acuity - anterior segment - intraocular pressure - dilated pupil funduscopy with severity of diabetic retinopathy), optical coherence tomography (OCT), EDI-OCT( Enhanced Depth Imaging Optical Coherence Tomography ) - as well as Optical coherence tomography angiography (OCTA ) are performed for all patients at baseline. Blood tests are also taken from patients for fasting blood sugar and HbA1C. Patients are then randomly divided into two groups. The first group is treated with injections of 1.25 mg of intravitreal bevacizumab monthly for 3 months (months 0, 1 and 2) with topical drops of Timolol twice a day and Dorzolamide twice a day. For the second group (control group), 3 injections of 1.25 mg of intravitreal bevacizumab monthly with artificial tears (twice a day as a placebo) are prescribed. Patients in both groups are visited 1 month after the third basic intravitreal bevacizumab (IVB) injection and complete ophthalmology examinations are performed and central thickness of macula is recorded based on the patient's OCT as well as the need for IVB re-injection. EDI (Enhanced Depth Imaging)-OCT and OCTA are performed again for all patients.

Start Date06 Oct 2021

Sponsor / Collaborator

Shahid Beheshti University of Medical Sciences

IRCT20210519051344N1

/ CompletedPhase 2IIT

Studying the effect of combination topical therapy using three medications (Dorzolamide drops, Ketorolac drops, Prednisolone drops) in treatment of Ivrin Gass syndrome (CME) post cataract surgery

Start Date22 Jun 2021

Sponsor / Collaborator

Tabriz University of Medical Sciences

100 Clinical Results associated with Dorzolamide Hydrochloride

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100 Translational Medicine associated with Dorzolamide Hydrochloride

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100 Patents (Medical) associated with Dorzolamide Hydrochloride

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1,459

Literatures (Medical) associated with Dorzolamide Hydrochloride

01 May 2025·European Journal of Pharmacology

Treatment of glaucoma with drug-loaded contact lenses: A systematic review and meta-analysis

Review

Author: Xu, Zihang ; Yu, Mingkun ; Wang, Xuan ; Ren, Cong ; Cao, Wenbo ; Zhang, Diya ; Guo, Bin ; Li, Jia ; Bi, Hongsheng

OBJECTIVEThis study is a systematical review regarding the glaucoma treatment with drug-loaded contact lenses. The effectiveness and safety about that were summarized, which providing effective suggestions and guidance for clinical research.METHODSThe studies published up to May 1, 2024 on the treatment of glaucoma with sustained-release contact lenses were searched from CNKI, Wanfang Data, VIP, PubMed, Embase, Cochrane Library, and Medline. CAMARADES was used to evaluate literature quality. The safety, endpoints of intraocular pressure reduction (IOPR) and duration of intraocular pressure (IOP) decline during glaucoma treatment were analyzed by means of qualitative and quantitative methods. The protocol registration number is CRD42024487157.RESULTS47 studies were included. In clinical trials, glaucoma patients showed a 50% reduction in IOP and no corneal tissue destruction after wearing contact lenses. In animal experiments, the endpoint IOPR [MD = 0.58, 95%CI (0.37, 0.80), P < 0.00001] of the medicated contact lenses group was significantly better than that of the eye drops group. Subgroup analysis showed that contact lenses loaded with timolol (TML), with TML + dorzolamide, and with TML + latanoprost, which compared to eye drops, had a better effect on reducing IOP, while contact lenses loaded with puerarin, latanoprost, and TML + bimatoprost showed no statistical difference. Most studies demonstrated the duration of IOP reduction and drugs release in vitro for ≥3 days during contact lenses treatment.CONCLUSIONMost drug-loaded contact lenses exhibit excellent effectiveness and safety. The nanoparticle-loaded contact lenses containing TML for glaucoma treatment is recommended in future clinical research.

01 Mar 2025·Veterinary Ophthalmology

Efficacy of perioperative 2% dorzolamide ophthalmic solution for reduction of postoperative ocular hypertension in dogs following routine phacoemulsification surgery: A prospective clinical trial

Article

Author: Camacho, Pilar ; Hu, Jennifer ; Lewin, Andrew C. ; Carter, Renee T. ; Liu, Chin‐Chi

AbstractObjectiveTo evaluate the efficacy of 2% dorzolamide ophthalmic solution for reduction of postoperative ocular hypertension (POH) following routine phacoemulsification surgery in dogs.Animals StudiedThirty one dogs (53 eyes) with naturally occurring cataracts undergoing routine phacoemulsification surgery.Procedure(s)A prospective, double‐masked, randomized, placebo‐controlled study design was utilized. Dogs received 2% dorzolamide ophthalmic solution or saline 1 h prior to surgery then three times daily for 21 days postoperatively in the operated eye(s). Intraocular pressure (IOP) was recorded 1 h prior to surgery and 3 h, 7 h, 22 h, 1 week and 3 weeks postoperatively. Statistical analyses were performed using chi‐squared and Mann–Whitney U test with a significance level of p < .05.ResultsPostoperative ocular hypertension (IOP ≥25 mmHg, <24 h after surgery) occurred in 28/53 (52.8%) eyes. There was significant reduction in the incidence of POH for eyes receiving dorzolamide (10/26 (38.4%) eyes) versus eyes receiving placebo (18/27 (66.7%) eyes) (p = .0384). Animals were followed for a median of 163 days after surgery. Thirty‐seven (37/53 (69.8%)) eyes were visual at final examination and 3/53 (5.7%) globes were enucleated postoperatively. At last follow‐up, there was no difference in visual status (p = .9280), need for topical IOP lowering medication (p = .8319) or incidence of glaucoma (p = .5880) based on treatment group.ConclusionsPerioperative administration of topical 2% dorzolamide reduced the incidence of POH after phacoemulsification in the dogs studied. However, this was not associated with differences in visual outcome, incidence of glaucoma or need for IOP‐lowering medications.

01 Feb 2025·Ophthalmology and Therapy

Randomized Clinical Trial of Intraocular Pressure-Lowering Medications on Preventing Spikes in Intraocular Pressure Following Intravitreal Anti-Vascular Endothelial Growth Factor Injections

Article

Author: Sathim, Wanwisa ; Samakhararaksakul, Rujira ; Chantiwas, Ratchada ; Arayangkoon, Eakkachai ; Rojananuangnit, Kulawan ; Katkingkaew, Kanokwan ; Seekhum, Natthapuch ; Soomsawasdi, Piriya ; Preawsampran, Nontakorn ; Pengrungreungwong, Sureeporn ; Tinpowong, Natnaree

INTRODUCTIONIntravitreal injections of anti-vascular endothelial growth factor (anti-VEGF) agents are a primary management option for retinal diseases. Acute elevation of intraocular pressure (IOP) is a complication associated with these injections that should be considered. This study investigated and compared the prophylactic effects of fixed combination anti-glaucoma medication on IOP spikes following intravitreal anti-VEGF injections.METHODSThis randomized double-blind clinical trial included one eye of each participant indicated for treatment with intravitreal injection of anti-VEGF agents (bevacizumab, aflibercept, and ranibizumab) and randomly allocated to one of the three prophylactic anti-glaucoma medications, with each drug further divided into one- and two-drop regimens before intravitreal injection. Participants with allergies or contraindications to medications were excluded from the pretreatment groups and were invited to participate in the control group.RESULTSThe study involved 308 participants: 89 in the dorzolamide/timolol group, 86 in the brimonidine/timolol group, 101 in the brinzolamide/brimonidine group, and 32 in the control group. Baseline characteristics and IOP were comparable across all groups. In the prophylactic premedication groups, mean IOP at 30 min were within 21 mmHg and returned to their baseline at 1 h. Mean IOP measurements between baseline and 30 min in the brimonidine/timolol two-drop regimen were not significantly different: 13.72 ± 4.63 vs 15.11 ± 4.39 mmHg, p = 0.096. In the control group, IOP significantly increased from baseline at 30 min and 1 h post-injection: 14.31 ± 4.10, 22.15 ± 8.64, and 18.36 ± 7.52 mmHg, respectively, p < 0.001.CONCLUSIONTopical fixed combination anti-glaucoma medication used as a prophylactic treatment before intravitreal anti-VEGF injections significantly prevented IOP spikes post-injection, with a comparable effect among three medications. Prophylactic treatment of IOP spikes should be considered as standard care to prevent further damage in patients with compromised retinal vascular and optic nerve perfusion.TRIAL REGISTRATIONTCTR20241005001, retrospectively registered.

100 Deals associated with Dorzolamide Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00653	Dorzolamide Hydrochloride	S01EC03	DB00869

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma	Japan	Santen Pharmaceutical Co., Ltd.	12 Mar 1999
Ocular Hypertension	Japan	Santen Pharmaceutical Co., Ltd.	12 Mar 1999

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


DMAC (EURETINA2024) Manual	Not Applicable	Dystrophy, Macular	32	Dorzolamidezolamide 2%	qfqeypsnxf(uyneshylre) = atfvplpnrr pnaoqifcfn (raquiqovox )	Negative	19 Sep 2024
				Saline	qfqeypsnxf(uyneshylre) = dolnnsdwao pnaoqifcfn (raquiqovox )
NCT00716586 (CTgov)	Phase 4	Macular Edema	44	2% dorzolamide	twicshwrvp(mxbbiwnqdd) = pybexwwfsg kpzfzpknhz (dgmeofdinb, jqdyigixgm - acdmisdvqw) View more	-	15 Oct 2021
ARVO2021	Not Applicable	Retinitis Pigmentosa	40	Topical 1.0% Dorzolamide	(afhlgoastx) = hrfghqdolw sdzktqvbbp (xpizcuvcxl )	-	01 Jun 2021
2018 ARVO Annual Meeting (ARVO2018)	Not Applicable	Bloodshot eye	30	Dorzolamide 2%	(ytqbxotmvv) = pfkvwptsbr twdsrsgwhq (ygwmpgryzm )	-	01 Jul 2018
				Placebo	(ytqbxotmvv) = onmyvnekre twdsrsgwhq (ygwmpgryzm )
ARVO2014	Not Applicable	Scleral Diseases	-	dorzolamide (Rabbit Sclera)	vsypmbkupe(pmhtrcqvwl) = adhwfgbzrc cpilhoujul (dxzczlivcw ) View more	-	01 Apr 2014
ARVO2012	Not Applicable	Ocular Hypotension	-	Agomelatine	(qgsnjsihbj) = vkxbprkdqx sfvcvbsovt (xxlfoybcek, ±1.4)	Positive	01 Mar 2012
				Control (saline + 1% DMSO)	(qgsnjsihbj) = uivpwetfrv sfvcvbsovt (xxlfoybcek )
ARVO2010	Not Applicable	Macular Edema	20	Topical 2% Dorzolamide	(vruumurjbm) = wahloiozna myszznegdt (ucbppovucr )	-	01 Apr 2010
				Topical Dorzolamide (Control Group)	(vruumurjbm) = crbycidbna myszznegdt (ucbppovucr )
ARVO2010	Not Applicable	-	-	Latanoprost monotherapy	(yknvosinun) = dbvrwhwgmn ycwrrufxnb (demjjfyqec ) View more	Positive	01 Apr 2010
				Latanoprost + Dorzolamide	(yknvosinun) = rosffqqhtz ycwrrufxnb (demjjfyqec ) View more
PO086 (AAO2007)	Not Applicable	Lipid Metabolism Disorders	120	Brimonidine Purite	(nimrmwzhkm) = eutoasqrre jfccsjfeun (ctszzfxknr, 21) View more	Positive	11 Nov 2007
				Dorzolamide	(nimrmwzhkm) = xwzjpdieff jfccsjfeun (ctszzfxknr, 16) View more