| 词条 | Phenazocine |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 464200012 | IUPAC_name = (2R,6R,11R)-6,11-Dimethyl-3-(2-phenylethyl)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-8-ol | image = Phenazocine2DCSD.svg | width = 180 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = Schedule 9 | legal_CA = Schedule I | legal_UK = Class A | legal_UK_comment = Withdrawn | legal_US = Schedule II | legal_DE = Anlage I | routes_of_administration = Oral | bioavailability = | protein_bound = | excretion = | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 127-35-5 | ATC_prefix = N02 | ATC_suffix = AD02 | PubChem = 14707 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 391631 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = J0ND6N0AQC | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 46399 | C=22 | H=27 | N=1 | O=1 | molecular_weight = 321.45588 g/mol | smiles = C[C@H]1[C@H]2Cc3ccc(cc3[C@@]1(CCN2CCc4ccccc4)C)O | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C22H27NO/c1-16-21-14-18-8-9-19(24)15-20(18)22(16,2)11-13-23(21)12-10-17-6-4-3-5-7-17/h3-9,15-16,21,24H,10-14H2,1-2H3/t16-,21+,22+/m0/s1 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = ZQHYKVKNPWDQSL-KNXBSLHKSA-N | synonyms = Fenazocina, Phenazocinum, DEA No. 9715 }} Phenazocine (brand names Prinadol, Narphen) is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects. Effects of phenazocine include analgesia and euphoria, also may include dysphoria and hallucinations at high doses, most likely due to action at κ-opioid and σ receptors.[1] Phenazocine appears to be a much stronger analgesic with fewer side effects than pentazocine, probably due to a more favorable μ/κ binding ratio. Phenazocine is a much more potent analgesic than pentazocine and other drugs in the benzomorphan series, most probably due to the presence of an N-phenethyl substitution, which is known to boost μ-opioid activity in many classes of opioid analgesics.[2] Consequently, phenazocine is some 4x the potency of morphine as an analgesic. Also it does not cause spasm of the sphincter of Oddi, making it more suitable than morphine for the treatment of biliary or pancreatic pain.[3] HistoryPhenazocine was invented in the 1950s.[4][5] It was one of a number of benzomorphan opioids (including pentazocine, dezocine, and cyclazocine) developed in the search for non-addictive strong analgesics. Phenazocine was once widely used, and was mainly supplied as 5 mg tablets of the hydrobromide salt for sublingual use (Narphen, Prinadol and other names), but its use was discontinued in the United Kingdom in 2001.[6] Phenazocine was briefly used in the United States but fell out of favour for the above-mentioned reasons;{{which|date=May 2013}}{{Citation needed|date=May 2013}} it remains a Schedule II substance under the Comprehensive Drug Abuse Control & Prevention Act (aka Controlled Substances Act) of 1970 (CSA) but is not manufactured; other Schedule II narcotics not in use in the United States include bezitramide and metopon. The DEA ACSCN for phenazocine is 9715 and its 2013 annual manufacturing quota was 6 grammes.[7] See also
References1. ^{{cite journal |vauthors=Harris LS, Pierson AK | title=Some Narcotic Antagonists in the Benzomorphan Series | journal=Journal of Pharmacology and Experimental Therapeutics |date=February 1964 | pages=141–8 | volume= 143| issue= | pmid=14163985}} {{Analgesics}}{{Hallucinogens}}{{Opioidergics}}2. ^{{cite journal |vauthors=Feinberg AP, Creese I, Snyder SH | title=The opiate receptor: a model explaining structure-activity relationships of opiate agonists and antagonists | journal=Proceedings of the National Academy of Sciences USA |date=November 1976 | pages=4215–9 | volume=73 | issue=11 | pmid=186791 | doi=10.1073/pnas.73.11.4215 | pmc= 431391}} 3. ^{{cite journal | author=Hopton D. | title=Double-blind clinical trial of the analgesic effects of phenazocine hydrobromide (Narphen) compared with morphine sulphate in patients with acute abdominal pain | journal=Gut |date=January 1971 | pages=51–4 | volume=12 | issue= 1 | pmid=4929685 | doi=10.1136/gut.12.1.51 | pmc=1411461}} 4. ^{{cite journal | author= Clarke EG | title=Identification of Phenazocine, a Potent New Analgesic | journal=Nature | date=August 8, 1959 | pages=451–451 | volume= 184 | issue= Suppl 7 | pmid=13810504 | doi= 10.1038/184451a0}} 5. ^{{cite journal | author= Eckenhoff JE | title=Phenazocine, a new benzomorphan narcotic analgesic | journal=Anesthesiology | date=May–June 1959 | pages=355–8 | volume=20 | issue=3 | pmid=13650222 | doi= 10.1097/00000542-195905000-00016}} 6. ^{{cite web |date=February 2001 | url = http://www.connectingforhealth.nhs.uk/systemsandservices/data/readcodes/docs/tandc0201.pdf | archive-url = http://webarchive.nationalarchives.gov.uk/20081106082526/http://www.connectingforhealth.nhs.uk/systemsandservices/data/readcodes/docs/tandc0201.pdf | dead-url = yes | archive-date = 2008-11-06 | title = Monthly Release Terming and Coding Newsletter | format = PDF | publisher = NHS Information Authority | accessdate = 2008-01-11}} 7. ^http://www.deadiversion.usdoj.gov/fed_regs/quotas/2013/fr0620.htm 5 : Benzomorphans|Kappa agonists|Mu-opioid agonists|Phenols|Synthetic opioids |
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