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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/10/30 22:11:29」(JST)
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Carteolol
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| Systematic (IUPAC) name |
| (RS)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2(1H)-one |
| Clinical data |
| Trade names |
Ocupress |
| AHFS/Drugs.com |
Micromedex Detailed Consumer Information |
| MedlinePlus |
a601078 |
| Pregnancy cat. |
C (US) |
| Legal status |
℞ Prescription only |
| Routes |
Eye drops |
| Pharmacokinetic data |
| Bioavailability |
85% |
| Metabolism |
Hepatic, active with 8-hydrocarteolol |
| Half-life |
6–8 hours |
| Excretion |
Renal (50-70%) |
| Identifiers |
| CAS number |
51781-06-7 |
| ATC code |
C07AA15 S01ED05 |
| PubChem |
CID 2583 |
| DrugBank |
DB00521 |
| ChemSpider |
2485 Y |
| UNII |
8NF31401XG Y |
| KEGG |
D07624 Y |
| ChEBI |
CHEBI:3437 Y |
| ChEMBL |
CHEMBL839 Y |
| Chemical data |
| Formula |
C16H24N2O3 |
| Mol. mass |
292.373 g/mol |
SMILES
- O=C2Nc1cccc(OCC(O)CNC(C)(C)C)c1CC2
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InChI
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InChI=1S/C16H24N2O3/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20) Y
Key:LWAFSWPYPHEXKX-UHFFFAOYSA-N Y
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Y (what is this?) (verify)
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Carteolol (trade names Cartrol, Ocupress, Teoptic, Arteolol, Arteoptic, Calte, Cartéabak, Carteol, Cartéol, Cartrol, Elebloc, Endak, Glauteolol, Mikelan, Poenglaucol, Singlauc) is a non-selective beta blocker used to treat glaucoma.
References[edit]
External links[edit]
- El-Kamel A, Al-Dosari H, Al-Jenoobi F (2006). "Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride.". Drug Deliv 13 (1): 55–9. doi:10.1080/10717540500309073. PMID 16401594.
- Kuwahara K, Oizumi N, Fujisawa S, Tanito M, Ohira A (2005). "Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro.". Cornea 24 (2): 213–20. doi:10.1097/01.ico.0000141232.41343.9d. PMID 15725891.
- Trinquand C, Romanet J, Nordmann J, Allaire C (2003). "[Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study]". J Fr Ophtalmol 26 (2): 131–6. PMID 12660585.
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Ophthalmologicals: antiglaucoma preparations and miotics (S01E)
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| Sympathomimetics |
- Apraclonidine
- Brimonidine (+timolol)
- Clonidine
- Dipivefrine
- Epinephrine
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| Parasympathomimetics |
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muscarinic
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muscarinic/nicotinic
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Acetylcholinesterase inhibitors
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- 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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anat (g/a/p)/phys/devp/prot
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proc, drug (S1A/1E/1F/1L)
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Adrenergics
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Receptor ligands
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α1
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- Agonists: 5-FNE
- 6-FNE
- Amidephrine
- Anisodamine
- Anisodine
- Cirazoline
- Dipivefrine
- Dopamine
- Ephedrine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Indanidine
- Levonordefrin
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetrahydrozoline
Antagonists: Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- CI-926
- Corynanthine
- Dapiprazole
- DL-017
- Domesticine
- Doxazosin
- Eugenodilol
- Fenspiride
- GYKI-12,743
- GYKI-16,084
- Hydroxyzine
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- Mephendioxan
- Metazosin
- Monatepil
- Moxisylyte
- Naftopidil
- Nantenine
- Neldazosin
- Nicergoline
- Niguldipine
- Pelanserin
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Piperoxan
- Prazosin
- Quinazosin
- Ritanserin
- RS-97,078
- SGB-1,534
- Silodosin
- SL-89.0591
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tibalosin
- Tiodazosin
- Tipentosin
- Tolazoline
- Trimazosin
- Upidosin
- Urapidil
- Zolertine
- Note that many TCAs, TeCAs, antipsychotics, ergolines, and some piperazines like buspirone and trazodone all antagonize α1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
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α2
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- Agonists: (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Ephedrine
- Ergotamine
- Epinephrine
- Esproquin
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- Levonordefrin
- Lofexidine
- Medetomidine
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rilmenidine
- Romifidine
- Talipexole
- Tetrahydrozoline
- Tizanidine
- Tolonidine
- Urapidil
- Xylazine
- Xylometazoline
Antagonists: 1-PP
- Adimolol
- Aptazapine
- Atipamezole
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fluparoxan
- GYKI-12,743
- GYKI-16,084
- Idazoxan
- Mianserin
- Mirtazapine
- MK-912
- NAN-190
- Olanzapine
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- SB-269,970
- Setiptiline
- Spiroxatrine
- Sunepitron
- Tolazoline
- Yohimbine
* Note that many atypical antipsychotics and azapirones like buspirone (via metabolite 1-PP) antagonize α2-adrenergic receptors as well.
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β
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Reuptake inhibitors
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NET
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- Selective norepinephrine reuptake inhibitors: Amedalin
- Atomoxetine (Tomoxetine)
- Ciclazindol
- Daledalin
- Edivoxetine
- Esreboxetine
- Lortalamine
- Mazindol
- Nisoxetine
- Reboxetine
- Talopram
- Talsupram
- Tandamine
- Viloxazine; Norepinephrine-dopamine reuptake inhibitors: Amineptine
- Bupropion (Amfebutamone)
- Fencamine
- Fencamfamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Methylphenidate
- Nomifensine
- O-2172
- Radafaxine; Serotonin-norepinephrine reuptake inhibitors: Bicifadine
- Desvenlafaxine
- Duloxetine
- Eclanamine
- Levomilnacipran
- Milnacipran
- Sibutramine
- Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors: Brasofensine
- Diclofensine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- JNJ-7925476
- JZ-IV-10
- Methylnaphthidate
- Naphyrone
- NS-2359
- PRC200-SS
- SEP-225,289
- SEP-227,162
- Tesofensine; Tricyclic antidepressants: Amitriptyline
- Butriptyline
- Cianopramine
- Clomipramine
- Desipramine
- Dosulepin
- Doxepin
- Imipramine
- Lofepramine
- melitracen
- Nortriptyline
- Protriptyline
- Trimipramine; Tetracyclic antidepressants: Amoxapine
- Maprotiline
- Mianserin
- Oxaprotiline
- Setiptiline; Others: Cocaine
- CP-39,332
- Ethanol
- EXP-561
- Fezolamine
- Ginkgo biloba
- Indeloxazine
- Nefazodone
- Nefopam
- Pridefrine
- Tapentadol
- Tedatioxetine
- Teniloxazine
- Tofenacin
- Tramadol
- Ziprasidone
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VMAT
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- Ibogaine
- Reserpine
- Tetrabenazine
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Enzyme inhibitors
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Anabolism
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PAH
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TH
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- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
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AAAD
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- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
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DBH
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- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
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PNMT
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- CGS-19281A
- SKF-64139
- SKF-7698
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Catabolism
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MAO
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- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A selective: Amiflamine
- Bazinaprine
- Befloxatone
- Befol
- Brofaromine
- Cimoxatone
- Clorgiline
- Esuprone
- Harmala alkaloids (Harmine,
- Harmaline
- Tetrahydroharmine
- Harman
- Norharman, etc)
- Methylene blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective:
- Ladostigil
- Lazabemide
- Milacemide
- Mofegiline
- Pargyline
- Rasagiline
- Safinamide
- Selegiline (also D-Deprenyl)
* Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine.
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COMT
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- Entacapone
- Nitecapone
- Tolcapone
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Others
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Precursors
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- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
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Cofactors
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- Ferrous Iron (Fe2+)
- S-Adenosyl-L-Methionine
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal Phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
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Others
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- Activity enhancers: BPAP
- PPAP; Release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanclofine
- Guanethidine
- Guanoxan; Toxins: 6-OHDA
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List of adrenergic drugs
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UpToDate Contents
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English Journal
- Effects of topical carteolol on retinal arterial blood flow in primary open-angle glaucoma patients.
- Kawai M, Nagaoka T, Takahashi A, Sato E, Yoshida A.SourceDepartment of Ophthalmology, Asahikawa Medical University, 2-1-1-1 Midorigaoka Higashi, Asahikawa 078-8510, Japan. m-kawai@asahikawa-med.ac.jp
- Japanese journal of ophthalmology.Jpn J Ophthalmol.2012 Sep;56(5):458-63. doi: 10.1007/s10384-012-0156-1. Epub 2012 Jun 14.
- PURPOSE: Our aim was to evaluate the effects of topical carteolol on retinal arterial blood flow (RBF) in patients with primary open-angle glaucoma.METHODS: Sixteen patients received carteolol topically for 90 days. Changes in RBF in the major retinal artery were evaluated using laser Doppler veloci
- PMID 22695833
- Effects of a long-acting ophthalmic formulation of carteolol containing alginic acid on the corneal epithelial barrier function and water retentive effect.
- Tokuda N, Inoue J, Yamazaki I, Ueno S, Fujisawa S.SourceDepartment of Ophthalmology, St. Marianna University School of Medicine, Kanagawa, Japan. tokunao@nifty.com
- Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics.J Ocul Pharmacol Ther.2012 Apr;28(2):123-8. doi: 10.1089/jop.2011.0101. Epub 2012 Jan 4.
- PURPOSE: Effects of a long-acting ophthalmic formulation of carteolol containing alginic acid on the corneal epithelial barrier function and its water retentive effect were investigated.METHODS: Using 10 healthy adult subjects, 2% Mikelan Ophthalmic Solution(®) (MK) was instilled in the eye once da
- PMID 22217390
- Carvedilol blocks the cloned cardiac Kv1.5 channels in a β-adrenergic receptor-independent manner.
- Jeong I, Choi BH, Yoon SH, Hahn SJ.SourceDepartment of Physiology, Medical Research Center, College of Medicine, The Catholic University of Korea, Seoul 137-701, Republic of Korea.
- Biochemical pharmacology.Biochem Pharmacol.2012 Feb 15;83(4):497-505. doi: 10.1016/j.bcp.2011.11.019. Epub 2011 Nov 28.
- Carvedilol, a non-selective β-adrenergic blocker, is widely used for the treatment of angina pectoris and hypertension. We examined the action of carvedilol on cloned Kv1.5 expressed in CHO cells, using the whole-cell patch clamp technique. Carvedilol reduced the peak amplitude of Kv1.5 and acceler
- PMID 22146582
Japanese Journal
- カルテオロール塩酸塩2%/ラタノプロスト0.005%配合点眼液(OPC-1085EL点眼液)の薬物動態と安全性
- カルテオロール塩酸塩持続性点眼液とラタノプロスト点眼液の併用療法とラタノプロスト・チモロールマレイン酸塩配合点眼液の眼圧下降効果および安全性の比較
- カルテオロール塩酸塩LA点眼液「わかもと」のヒト角膜上皮細胞への影響と保存効力の検討
Related Links
- Carteolol is in a group of drugs called beta-blockers. Beta-blockers affect the heart and circulation (blood flow through arteries and veins). Carteolol is used to treat hypertension (high blood pressure). Carteolol may also be used for ...
- Carteolol is a beta1 and beta2 (non-selective) adrenergic receptor-blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. Carteolol ...
Related Pictures
★リンクテーブル★
[★]
- 英
- carteolol
- 商
- カルテロール、カルノノン、チオグール、チスタロール、ブロキレート、ブロキレートＰＦ、ベタメノール、ミケラン Mikelan、ミケランLA、メルカトア、リエントン
- 化
- 塩酸カルテオロール carteolol hydrochloride
- 関
- 交感神経拮抗薬一覧。眼科用剤
- β1抑制作用が過剰となりにくい
適応
添付文書
- http://www.info.pmda.go.jp/go/pack/1319701Q1021_1_12/1319701Q1021_1_12?view=body
- http://www.info.pmda.go.jp/go/pack/2123005F1206_1_04/2123005F1206_1_04?view=body
[★]
- 関
- carteolol