ドルゾラミド
- 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
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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 |
Clinical data |
Trade names |
Trusopt |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a602022 |
Pregnancy
category
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- US: C (Risk not ruled out)
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Legal status
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Routes of
administration
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Topical (eye drops) |
Pharmacokinetic data |
Protein binding |
~33% |
Half-life |
4 months |
Identifiers |
CAS Registry Number
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130693-82-2 N 120279-96-1 |
ATC code
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S01EC03 |
PubChem |
CID: 5284549 |
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
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324.443 g/mol |
SMILES
- 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
Key:IAVUPMFITXYVAF-XPUUQOCRSA-N Y
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N (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 optically applied in the form of a 2% eye drops.[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
- 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
- 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
Related Links
- Dorzolamide (trade name Trusopt) is a carbonic anhydrase inhibitor. It is an anti- glaucoma agent and topically applied in the form of eye drops. This drug, developed by Merck, was the first drug in human therapy (market introduction 1995) ...
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