関: dorzolamide hydrochloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/14 00:22:26」(JST)

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Dorzolamide (trade name Trusopt) is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour.^[1] It is optically applied in the form of a 2% eye drops.^[2]

History

This drug, developed by Merck, was the first drug in human therapy (market introduction 1995) which resulted from structure-based drug design. It was developed to circumvent the systemic side effects of acetazolamide which has to be taken orally.^[2]

Uses

Dorzolamide hydrochloride is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.

Pharmacodynamics

It lowers IOP by about 20%.^[2]

Side effects

Ocular stinging, burning, itching and bitter taste.^[2] it causes shallowing of the anterior chamber and leads to transient myopia.

References

^ Dorzolamide at Drugs.com. Revised: 12/2011
^ ^a ^b ^c ^d KD Tripari MD. Essentials of Medical Pharmacology (5 ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 88. ISBN 81-8061-187-6.

UpToDate Contents

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1. 網膜色素変性症：治療 retinitis pigmentosa treatment
2. 原発性乳児緑内障 primary infantile glaucoma

English Journal

From dorzolamide 2%/timolol 0.5% to brinzolamide 1%/timolol 0.5% fixed combination: a 6-month, multicenter, open-label tolerability switch study.

Rossi GC, Pasinetti GM, Sandolo F, Bordin M, Bianchi PE.SourceUniversity Eye Clinic of Pavia, IRCCS Policlinico San Matteo Foundation, Pavia, Piazzale Golgi 19, 27100 Pavia , Italy +1 39 0382 503730 ; +1 39 0382 527006 ; gemma.rossi.md@gmail.com.
Expert opinion on pharmacotherapy.Expert Opin Pharmacother.2011 Nov;12(16):2425-31. Epub 2011 Jun 16.
Purpose: To assess ocular surface status and tolerability after switching glaucoma patients from dorzolamide/timolol to brinzolamide/timolol fixed combination (FC). Methods: Six-month, multicenter, open-label, prospective study that switched 72 patients from dorzolamide/timolol to brinzolamide
PMID 21679090

Heterocyclic compounds as carbonic anhydrase inhibitor.

Husain A, Madhesia D.SourceDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University) , Hamdard Nagar, New Delhi , India.
Journal of enzyme inhibition and medicinal chemistry.J Enzyme Inhib Med Chem.2011 Oct 10. [Epub ahead of print]
The carbonic anhydrases (CAs, EC 4.2.1.1) constitute interesting targets for the design of pharmacological agents useful in the treatment or prevention of a variety of disorders such as, glaucoma, acid-base disequilibria, epilepsy, and other neuromuscular diseases, altitude sickness, edema, and obes
PMID 21981003

Japanese Journal

第21回日本緑内障学会併用薬の違いによる1%ドルゾラミドの視神経乳頭血流増加作用

大黒幾代,片井麻貴,田中祥恵 [他]
あたらしい眼科 28(6), 868-873, 2011-06
NAID 40018899912

緑内障および高眼圧症患者を対象とした1%ドルゾラミド塩酸塩/0.5%チモロールマレイン酸塩の配合点眼液(MK-0507A)の第3相二重盲検比較試験

北澤克明,新家眞,MK-0507A研究会
日本眼科学会雑誌 115(6), 495-507, 2011-06
NAID 40018883951

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リンク元	「ドルゾラミド」
拡張検索	「dorzolamide hydrochloride」

「ドルゾラミド」

Dorzolamide
Systematic (IUPAC) name
	(4S,6S)-2-ethylamino-4-methyl-5,5-dioxo-; 5λ6,7-dithiabicyclo[4.3.0]nona-8,10-diene-8-sulfonamide
Clinical data
Trade names	Trusopt
AHFS/Drugs.com	monograph
MedlinePlus	a602022
Pregnancy; category	US: C (Risk not ruled out);
Legal status	US: ℞-only;
Routes of; administration	Topical (eye drops)
Pharmacokinetic data
Protein binding	~33%
Half-life	4 months
Identifiers
CAS Registry Number	130693-82-2 120279-96-1
ATC code	S01EC03
PubChem	CID: 5284549
DrugBank	DB00869
ChemSpider	4447604
UNII	9JDX055TW1
KEGG	D07871
ChEBI	CHEBI:4702
ChEMBL	CHEMBL218490
Chemical data
Formula	C10H16N2O4S3
Molecular mass	324.443 g/mol
	SMILES CCNC1CC(C)S(=O)(=O)c2sc(cc12)S(=O)(=O)N;
	InChI InChI=1S/C10H16N2O4S3/c1-3-12-8-4-6(2)18(13,14)10-7(8)5-9(17-10)19(11,15)16/h5-6,8,12H,3-4H2,1-2H3,(H2,11,15,16)/t6-,8-/m0/s1 ; Key:IAVUPMFITXYVAF-XPUUQOCRSA-N ;
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