炭酸脱水酵素阻害薬、炭酸脱水酵素阻害剤

WordNet

limit, block, or decrease the action or function of; "inhibit the action of the enzyme"; "inhibit the rate of a chemical reaction"
control and refrain from showing; of emotions, desires, impulses, or behavior (同)bottle up, suppress
limit the range or extent of; "Contact between the young was inhibited by strict social customs"
an abundant nonmetallic tetravalent element occurring in three allotropic forms: amorphous carbon and graphite and diamond; occurs in all organic compounds (同)C, atomic number 6
a copy made with carbon paper (同)carbon_copy
a substance that retards or stops an activity

PrepTutorEJDIC

〈感情・欲望・行動・作用など〉‘を'抑制する / (…しないように)〈人〉‘を'抑制する,妨げる《+『名』+『from』+『名』(do『ing』)》
『炭素』(化学記号は『C』) / 〈C〉炭素棒 / 〈C〉《時に〈U〉》=carbon paper
抑制する人(物) / 化学反応抑制剤

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/04 08:03:56」(JST)

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Carbonic anhydrase inhibitors are a class of pharmaceuticals that suppress the activity of carbonic anhydrase. Their clinical use has been established as antiglaucoma agents, diuretics, antiepileptics, in the management of mountain sickness, gastric and duodenal ulcers, neurological disorders, or osteoporosis.^[1]^[2]^[3]

Medical Uses

Carbonic anhydrase inhibitors are primarily used for the treatment of glaucoma. They may also be used to treat seizure disorder and acute mountain sickness. Because they encourage solubilization and excretion of uric acid, they can be used in the treatment of gout.^[4]

Glaucoma

Acetazolamide is an inhibitor of carbonic anhydrase. It is used for glaucoma, epilepsy (rarely), idiopathic intracranial hypertension, and altitude sickness.

Methazolamide is also a carbonic anhydrase inhibitor. It has a longer elimination half-life than acetazolamide and is less associated with adverse effects to the kidney.^[5]^[6]^[7]

Dorzolamide is a sulfonamide and topical carbonic anhydrase II inhibitor. It is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension and who are insufficiently responsive to beta-blockers. Inhibition of carbonic anhydrase II in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport.^{[citation needed]}

Brinzolamide (trade name Azopt, Alcon Laboratories, Inc.) is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It exists as a number of isoenzymes, the most active of which is carbonic anhydrase II (CA-II). The combination of brinzolamide with timolol is marketed under the trade name Azarga.^{[citation needed]}

Diuretic

Acetazolamide can act as a mild diuretic by reducing NaCl and bicarbonate reabsorption in the proximal tubule. However, the distal segment partially compensates for the sodium loss, and the bicarbonaturia will produce a metabolic acidosis, further reducing the effect.

Epilepsy

Topiramate is a weak inhibitor of carbonic anhydrase, particularly subtypes II and IV. It is a sulfamate-substituted monosaccharide, related to fructose. In the US, it is approved by the U.S. Food and Drug Administration (FDA) as an anticonvulsant to treat epilepsy and Lennox-Gastaut syndrome, and also to prevent migraine headaches. In rare cases, the inhibition of carbonic anhydrase may be strong enough to cause metabolic acidosis of clinical importance.^{[citation needed]}

Altitude Sickness

At high altitude, the partial pressure of oxygen is lower and people have to breathe more rapidly to get adequate oxygen. When this happens, the partial pressure of CO2 in the lungs (pCO2) decreases (is "blown off"), causing a respiratory alkalosis. This would normally be compensated by the kidney excreting bicarbonate and causing compensatory metabolic acidosis, but this mechanism takes several days. A more immediate treatment is carbonic anhydrase inhibitors, which prevent bicarbonate uptake in the kidney and help correct the alkalosis.^[8] Carbonic anhydrase inhibitors have also been shown to improve chronic mountain sickness by reducing erythropoietin and the resulting polycytemia.^[9]

Contraindications

Hepatic cirrhosis^[10]

Adverse effects

Loss of bicarbonate may result in metabolic acidosis.^[11] Alkaline urine may increase the likelihood of kidney stones.

Natural sources

Ellagitannins extracted from the pericarps of Punica granatum, the pomegranate, such as punicalin, punicalagin, granatin B, gallagyldilactone, casuarinin, pedunculagin and tellimagrandin I, are carbonic anhydrase inhibitors.^[12]

References

^ Supuran CT, Scozzafava A, Conway J, ed. (2004). Carbonic anhydrase: its inhibitors and activators. Boca Raton: CRC Press. ISBN 978-0-415-30673-7. ^{[page needed]}
^ Supuran, Claudiu T; Scozzafava, Andrea (2000). "Carbonic anhydrase inhibitors and their therapeutic potential". Expert Opinion on Therapeutic Patents 10 (5): 575–600. doi:10.1517/13543776.10.5.575.
^ Supuran, Claudiu T.; Scozzafava, Andrea; Casini, Angela (2003). "Carbonic anhydrase inhibitors". Medicinal Research Reviews 23 (2): 146–89. doi:10.1002/med.10025. PMID 12500287.
^ Hyperuricemia Medication~medication at eMedicine
^ Bennett WM, Aronoff GR, Golper TA, et al, Drug Prescribing in Renal Failure, American College of Physicians, Philadelphia, PA, 1987^{[page needed]}
^ Product Information: Neptazane(R), methazolamide. Storz Ophthalmics Inc, Clearwater, FL, 1995a^{[page needed]}
^ Reynolds JEF (Ed): Martle: The Extra Pharmacopoeia (electronic version). Micromedex, Inc. Englewood, CO. 1995.^{[page needed]}
^ Swenson, Erik R. (2014). "Carbonic Anhydrase Inhibitors and High Altitude Illnesses". In Frost, Susan C.; McKenna, Robert. Carbonic Anhydrase: Mechanism, Regulation, Links to Disease, and Industrial Applications. Subcellular Biochemistry 75. pp. 361–86. doi:10.1007/978-94-007-7359-2_18. ISBN 978-94-007-7358-5. PMID 24146388.
^ Richalet, Jean-Paul; Rivera, Maria; Bouchet, Patrick; Chirinos, Eduardo; Onnen, Igor; Petitjean, Olivier; Bienvenu, Annick; Lasne, Francçoise; Moutereau, Stéphane; León-Velarde, Fabiola (2005). "Acetazolamide". American Journal of Respiratory and Critical Care Medicine 172 (11): 1427–33. doi:10.1164/rccm.200505-807OC. PMID 16126936.
^ Webster, L. T.; Davidson, C. S. (1956). "Production of Impending Hepatic Coma by a Carbonic Anhydrase Inhibitor, Diamox". Experimental Biology and Medicine 91 (1): 27–31. doi:10.3181/00379727-91-22159. PMID 13297699.
^ Leaf, Alexander; Schwartz, William B.; Relman, Arnold S. (1954). "Oral Administration of a Potent Carbonic Anhydrase Inhibitor (Diamox)". New England Journal of Medicine 250 (18): 759–64. doi:10.1056/NEJM195405062501803. PMID 13165895.
^ Satomi, H; Umemura, K; Ueno, A; Hatano, T; Okuda, T; Noro, T (1993). "Carbonic anhydrase inhibitors from the pericarps of Punica granatum L". Biological & pharmaceutical bulletin 16 (8): 787–90. PMID 8220326.

External links

Carbonic anhydrase inhibitors at the US National Library of Medicine Medical Subject Headings (MeSH)

MedlinePlus DrugInfo uspdi-202114

UpToDate Contents

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1. 利尿剤の作用機序 mechanism of action of diuretics
2. 開放隅角緑内障：治療 open angle glaucoma treatment
3. 特発性頭蓋内圧亢進症（偽脳腫瘍）：予後および治療 idiopathic intracranial hypertension pseudotumor cerebri prognosis and treatment
4. Overview of eye injuries in the emergency department
5. 尿細管性アシドーシスにおける腎結石症 nephrolithiasis in renal tubular acidosis

English Journal

Synthesis, characterization, antimicrobial activity and carbonic anhydrase enzyme inhibitor effects of salicilaldehyde-N-methyl p-toluenesulfonylhydrazone and its Palladium(II), Cobalt(II) complexes.

Alyar S1, Adem Ş2.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.Spectrochim Acta A Mol Biomol Spectrosc.2014 Oct 15;131:294-302. doi: 10.1016/j.saa.2014.04.121. Epub 2014 Apr 29.
We report the synthesis of the ligand, salicilaldehyde-N-methyl p-toluenesulfonylhydrazone (salptsmh) derived from p-toluenesulfonicacid-1-methylhydrazide (ptsmh) and its Pd(II) and Co(II) metal complexes were synthesized for the first time. The structure of the ligand and their complexes were inves
PMID 24835932

Cyclic tertiary sulfamates: Selective inhibition of the tumor-associated carbonic anhydrases IX and XII by N- and O-substituted acesulfame derivatives.

De Monte C1, Carradori S2, Secci D2, D'Ascenzio M2, Vullo D3, Ceruso M3, Supuran CT4.
European journal of medicinal chemistry.Eur J Med Chem.2014 Sep 12;84:240-6. doi: 10.1016/j.ejmech.2014.07.014. Epub 2014 Jul 8.
Carbonic anhydrase (hCA) IX and XII isoforms are over-expressed both in primary and in metastatic cell lines of hypoxic tumors and are innovative targets for cancer diagnosis and treatment. On the basis of the importance of the pharmacophoric sulfamate moiety (bioisostere of the sulfonamide group) p
PMID 25019479

Synthesis of a new series of N(4)-substituted 4-(2-aminoethyl)benzenesulfonamides and their inhibitory effect on human carbonic anhydrase cytosolic isozymes I and II and transmembrane tumor-associated isozymes IX and XII.

Sławiński J1, Brzozowski Z2, Zołnowska B2, Szafrański K2, Pogorzelska A2, Vullo D3, Supuran CT3.
European journal of medicinal chemistry.Eur J Med Chem.2014 Sep 12;84:59-67. doi: 10.1016/j.ejmech.2014.06.074. Epub 2014 Jul 5.
A series of novel N(4)-substituted 4-(2-aminoethyl)benzenesulfonamides 5-17 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), that is the cytosolic CA I and II, and tumor-associated isozymes CA IX and XII. Against the human CA I
PMID 25016228

Japanese Journal

プロスタグランジン薬,βブロッカー,炭酸脱水酵素阻害剤の3剤併用でコントロール不十分な症例に対するブリモニジン点眼液の追加処方

松浦一貴,寺坂祐樹,佐々木慎一
あたらしい眼科 31(7), 1059-1062, 2014-07
NAID 40020164236

網膜色素変性に伴う囊胞様黄斑浮腫に炭酸脱水酵素阻害薬の点眼加療が有効と思われた1例 (特集第67回日本臨床眼科学会講演集(3))

春田雅俊,佛坂扶美,山川良治
臨床眼科 68(5), 713-717, 2014-05
NAID 40020081143

炭酸脱水酵素阻害薬 (特集利尿薬およびそれに関連する話題)

小武海公明
循環器内科 75(3), 274-276, 2014-03
NAID 40020021022

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