- 関
- dorzolamide
WordNet
- a complex consisting of an organic base in association with hydrogen chloride
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/12/29 17:15:13」(JST)
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Dorzolamide
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Systematic (IUPAC) name |
(4S,6S)-2-ethylamino-4-methyl-5,5-dioxo-
5λ6,7-dithiabicyclo[4.3.0]nona-8,10-diene-8-sulfonamide
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Clinical data |
Trade names |
Trusopt |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a602022 |
Pregnancy
category |
- US: C (Risk not ruled out)
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Legal status |
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Routes of
administration |
Topical (eye drops) |
Pharmacokinetic data |
Protein binding |
~33% |
Biological half-life |
4 months |
Identifiers |
CAS Number |
130693-82-2 N 120279-96-1 |
ATC code |
S01EC03 |
PubChem |
CID: 5284549 |
IUPHAR/BPS |
6810 |
DrugBank |
DB00869 Y |
ChemSpider |
4447604 Y |
UNII |
9JDX055TW1 Y |
KEGG |
D07871 N |
ChEBI |
CHEBI:4702 Y |
ChEMBL |
CHEMBL218490 Y |
Chemical data |
Formula |
C10H16N2O4S3 |
Molecular mass |
324.443 g/mol |
SMILES
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CCNC1CC(C)S(=O)(=O)c2sc(cc12)S(=O)(=O)N
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InChI
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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 Y
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Key:IAVUPMFITXYVAF-XPUUQOCRSA-N Y
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NY (what is this?) (verify) |
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 administered as a topical ophthalmic in the form of a 2% solution.[2]
Contents
- 1 History
- 2 Uses
- 3 Pharmacodynamics
- 4 Side effects
- 5 References
- 6 Further reading
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.
Further reading
- Kubinyi H (1999). "Chance favors the prepared mind--from serendipity to rational drug design". J Recept Signal Transduct Res 19 (1–4): 15–39. doi:10.3109/10799899909036635. PMID 10071748.
- Plummer C, MacKay E, Gelatt K (2006). "Comparison of the effects of topical administration of a fixed combination of dorzolamide-timolol to monotherapy with timolol or dorzolamide on IOP, pupil size, and heart rate in glaucomatous dogs". Vet Ophthalmol 9 (4): 245–9. doi:10.1111/j.1463-5224.2006.00469.x. PMID 16771760.
- Grover S, Apushkin M, Fishman G (2006). "Topical dorzolamide for the treatment of cystoid macular edema in patients with retinitis pigmentosa". Am J Ophthalmol 141 (5): 850–8. doi:10.1016/j.ajo.2005.12.030. PMID 16546110.
- Almeida G, Faria e Souza S (2006). "Effect of topical dorzolamide on rabbit central corneal thickness". Braz J Med Biol Res 39 (2): 277–81. doi:10.1590/S0100-879X2006000200015. PMID 16470316.
Drugs used for glaucoma preparations and miosis (S01E)
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Sympathomimetics |
- Apraclonidine
- Brimonidine (+timolol)
- Clonidine
- Dipivefrine
- Epinephrine
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Parasympathomimetics |
muscarinic |
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muscarinic/nicotinic |
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Acetylcholinesterase inhibitors |
- Demecarium
- Ecothiopate
- Stigmine (Fluostigmine
- Neostigmine
- Physostigmine)
- Paraoxon
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Carbonic anhydrase inhibitors/
(sulfonamides) |
- Acetazolamide
- Brinzolamide (+timolol)
- Diclofenamide
- Dorzolamide (+timolol)
- Methazolamide
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Beta blocking agents |
- Befunolol
- Betaxolol
- Carteolol
- Levobunolol
- Metipranolol
- Timolol
- Mepindolol
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|
Prostaglandin analogues (F2α) |
- Bimatoprost (+timolol)
- Latanoprost (+timolol)
- Tafluprost
- Travoprost (+timolol)
- Unoprostone
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Other agents |
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Index of the eye
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|
Description |
- Anatomy
- Physiology
- Phenomena
- appearance
- visual
- optical illusions
- proteins
- Development
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Disease |
- Congenital
- Corneal dystrophy
- Neoplasms and cancer
- Other
- Symptoms and signs
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Treatment |
- Procedures
- Drugs
- infection
- glaucoma and miosis
- mydriatics
- vascular
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UpToDate Contents
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English Journal
- Fundus Autofluorescence and SD-OCT Document Rapid Progression in Autosomal Dominant Vitreoretinochoroidopathy (ADVIRC) Associated with a c.256G > A Mutation in BEST1.
- Kellner S1,2, Stöhr H3, Fiebig B3,4, Weinitz S1,2, Farmand G1, Kellner U1,2, Weber BH3.
- Ophthalmic genetics.Ophthalmic Genet.2016 Jun;37(2):201-8. doi: 10.3109/13816810.2015.1033556. Epub 2016 Jan 15.
- PURPOSE: To report the variability of clinical findings, rapid concentric progression, and successful treatment of macular edema in autosomal dominant vitreoretinochoroidopathy (ADVIRC) associated with a heterozygous c.256G > A missense mutation in the bestrophin-1 (BEST1) gene.METHODS: Three
- PMID 26771239
- Angle closure caused by a plateau-like iris associated with an enlarged Soemmering's ring: a case report.
- Kitamura F1, Inoue T2, Kuroda U1, Tanihara H1.
- BMC ophthalmology.BMC Ophthalmol.2016 May 4;16(1):49. doi: 10.1186/s12886-016-0226-0.
- BACKGROUND: This study evaluated the anterior ocular segment in a pseudophakic eye with angle closure due to a plateau-like iris associated with Soemmering's ring, using ultrasound biomicroscopy (UBM) and anterior segment optical coherence tomography (AS-OCT).CASE PRESENTATION: A 60-year-old woman w
- PMID 27145815
- Efficacy of Bimatoprost Plus Timolol Fixed Combination in Open Angle Glaucoma Patients Previously Treated with Dorzolamide Plus Timolol Fixed Combination.
- Sacchi M1, Specchia C2,3, Williams SE4, Villani E1, Nucci P1.
- Current eye research.Curr Eye Res.2016 Apr 26:1-5. [Epub ahead of print]
- PURPOSE: To evaluate the efficacy and safety of bimatoprost plus timolol fixed combination (BTFC) in patients with primary open angle glaucoma (POAG) previously treated with dorzolamide plus timolol fixed combination (DTFC).MATERIALS AND METHODS: Retrospective, medical records review study. Medical
- PMID 27115319
Japanese Journal
- プロスタグランジン関連点眼液併用下でのβ遮断点眼液あるいは炭酸脱水酵素阻害点眼液から1%ドルソラミド塩酸塩・0.5%チモロールマレイン酸塩配合点眼液への変更時の眼圧下降効果と安全性
- 2剤併用を配合薬1剤に変更した場合の1年6カ月の眼圧下降効果
- 小林 茂樹,小林 守治
- あたらしい眼科 = Journal of the eye 30(7), 1011-1013, 2013-07-30
- NAID 10031189386
- 2剤併用を配合薬1剤に変更した場合の1年6ヵ月の眼圧下降効果 (第23回 日本緑内障学会)
Related Links
- Dorzolamide hydrochloride ophthalmic Solution, USP is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. 2 DOSAGE AND ADMINISTRATION The dose is one ...
- Timolol maleate has a molecular weight of 432.50. It is a white, odorless, crystalline powder which is soluble in water, methanol, and alcohol. Timolol maleate is stable at room temperature. COSOPT (dorzolamide hydrochloride ...
Related Pictures
★リンクテーブル★
[★]
- 英
- dorzolamide、
- 化
- 塩酸ドルゾラミド dorzolamide hydrochloride
- 商
- コソプト配合、トルソプト
[★]
ドルゾラミド
- 関
- dorzolamide hydrochloride
[★]
塩酸塩、ハイドロクロライド