| 词条 | Fenoldopam |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 461099753 | IUPAC_name = (RS)-6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol | image = Fenoldopam.svg | width = 200px | image2 = Fenoldopam 3d balls.png | chirality = Racemic mixture | tradename = Corlopam | Drugs.com = {{drugs.com|monograph|fenoldopam}} | pregnancy_US = B | legal_US = Rx-only | routes_of_administration = IV | bioavailability = | protein_bound = | metabolism = Hepatic (CYP not involved) | elimination_half-life = 5 minutes | excretion = Renal (90%) and fecal (10%) | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 67227-56-9 | ATC_prefix = C01 | ATC_suffix = CA19 | PubChem = 3341 | IUPHAR_ligand = 939 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00800 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 3224 | UNII_Ref = {{fdacite|changed|FDA}} | UNII = INU8H2KAWG | KEGG_Ref = {{keggcite|changed|kegg}} | KEGG = D07946 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 5002 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 588 | C=16 | H=16 | Cl=1 | N=1 | O=3 | molecular_weight = 305.76 g/mol | smiles = Clc1c3c(cc(O)c1O)C(c2ccc(O)cc2)CNCC3 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C16H16ClNO3/c17-15-11-5-6-18-8-13(9-1-3-10(19)4-2-9)12(11)7-14(20)16(15)21/h1-4,7,13,18-21H,5-6,8H2 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = TVURRHSHRRELCG-UHFFFAOYSA-N }}Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.[1] Fenoldopam is used as an antihypertensive agent.[2] It was approved by the Food and Drug Administration (FDA) in September 1997.[3] IndicationsFenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive crisis.[4] Since fenoldopam is the only intravenous agent that improves renal perfusion, in theory it could be beneficial in hypertensive patients with concomitant renal insufficiency.[5] PharmacologyFenoldopam causes arterial/arteriolar vasodilation leading to a decrease in blood pressure by activating peripheral D1 receptors.[6] It decreases afterload and also promotes sodium excretion via specific dopamine receptors along the nephron. The renal effect of fenoldopam and dopamine may involve physiological antagonism of the renin-angiotensin system in the kidney.[7] In contrast to dopamine, fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is evidence that it may have some alpha-1 [8] and alpha-2 adrenoceptor antagonist activity.[6] D1 receptor stimulation activates adenylyl cyclase and raises intracellular cyclic AMP, resulting in vasodilation of most arterial beds, including renal, mesenteric, and coronary arteries.[9] to cause a reduction in systemic vascular resistance. Fenoldopam has a rapid onset of action (4 minutes) and short duration of action (< 10 minutes) and a linear dose–response relationship at usual clinical doses.[10] Side effectsAdverse effects include headache, flushing, nausea, hypotension, reflex tachycardia, and increased intraocular pressure.[4][13] Contraindications, warnings and precautionsFenoldopam mesylate contains sodium metabisulfite, a sulfite that may rarely cause allergic-type reactions including anaphylactic symptoms and asthma in susceptible people. Fenoldopam mesylate administration should be undertaken with caution to patients with glaucoma or raised intraocular pressure as fenoldopam raises intraocular pressure.[11] Concomitant use of fenoldopam with a beta-blocker should be avoided if possible, as unexpected hypotension can result from beta-blocker inhibition of sympathetic-mediated reflex tachycardia in response to fenoldopam.[11] References1. ^{{cite journal |vauthors=Grenader A, Healy DP |title=Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells |journal=J. Pharmacol. Exp. Ther. |volume=258 |issue=1 |pages=193–8 |date=July 1991 |pmid=1677038 |doi= |url=}} {{Sympatholytic antihypertensives}}{{Dopaminergics}}2. ^{{cite journal |vauthors=Oliver WC, Nuttall GA, Cherry KJ, Decker PA, Bower T, Ereth MH |title=A comparison of fenoldopam with dopamine and sodium nitroprusside in patients undergoing cross-clamping of the abdominal aorta |journal=Anesth. Analg. |volume=103 |issue=4 |pages=833–40 |date=October 2006 |pmid=17000789 |doi=10.1213/01.ane.0000237273.79553.9e |url=http://www.anesthesia-analgesia.org/cgi/pmidlookup?view=long&pmid=17000789}} 3. ^http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Label_ApprovalHistory accessed November 14, 2011 4. ^1 {{Cite book | author=Shen, Howard | title=Illustrated Pharmacology Memory Cards: PharMnemonics | year=2008 | publisher=Minireview | isbn=1-59541-101-1 | page=9}} 5. ^USMLE WORLD 2009 Step1 QBanks, Pharmacology, Pharma50q, Q NO 18 6. ^1 {{cite journal |vauthors=Nichols AJ, Ruffolo RR, Brooks DP |title=The pharmacology of fenoldopam |journal=Am. J. Hypertens. |volume=3 |issue=6 Pt 2 |pages=116S–119S |date=June 1990 |pmid=1974439 |doi= |url=}} 7. ^{{cite journal |author=Gildea JJ |title=Dopamine and angiotensin as renal counterregulatory systems controlling sodium balance |journal=Curr. Opin. Nephrol. Hypertens. |volume=18 |issue=1 |pages=28–32 |date=January 2009 |pmid=19077686 |pmc=2847451 |doi=10.1097/MNH.0b013e32831a9e0b |url=}} 8. ^{{cite journal |vauthors=Martin SW, Broadley KJ |title=Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade |journal=Br. J. Pharmacol. |volume=115 |issue=2 |pages=349–55 |date=May 1995 |pmid=7670737 |pmc=1908310 |doi= 10.1111/j.1476-5381.1995.tb15884.x|url=}} 9. ^{{cite journal |vauthors=Hughes AD, Sever PS |title=Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries |journal=Blood Vessels |volume=26 |issue=2 |pages=119–27 |year=1989 |pmid=2474340 |doi= |url=}} 10. ^Epstein, Murray MD, "Diagnosis and Management of Hypertensive Emergencies," clinical Cornerstone. Hypertension Vol2. No 1. 11. ^1 2 NDA 19-922/S-005: Corlopam RA06497-R1-9/03 brand of Fenoldopam Mesylate Injection, USP 5 : Benzazepines|D1-receptor agonists|Phenols|Chloroarenes|Peripherally selective drugs |
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