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词条 Meptazinol
释义

  1. References

  2. External links

{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 462248630
| IUPAC_name = (RS)-3-(3-Ethyl-1-methylazepan-3-yl)phenol
| image = Meptazinol.svg
| width = 150
| chirality = Racemic mixture
| tradename = Meptid
| Drugs.com = {{drugs.com|international|meptazinol}}
| licence_EU =
| licence_US =
| pregnancy_AU =
| pregnancy_US =
| pregnancy_category =
| legal_AU = Schedule 4
| legal_CA =
| legal_UK = POM
| legal_US =
| legal_status =
| dependency_liability = Low
| routes_of_administration = Oral, IM, IV
| bioavailability =
| protein_bound =
| metabolism = The peak analgesic effect is seen within 30–60 minutes and lasts about 3–4 hours
| elimination_half-life = Half-life (1.4–4 hours)
| excretion = The drug is rapidly metabolized to the glucuronide, and mostly excreted in the urine
| CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 59263-76-2
| ATC_prefix = N02
| ATC_suffix = AX05
| ATC_supplemental =
| PubChem = 41049
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank =
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 37469
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 18Y7S5JKZD
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D08182
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 314437
| C=15 | H=23 | N=1 | O=1
| smiles = OC1=CC=CC(C2(CCCCN(C2)C)CC)=C1
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C15H23NO/c1-3-15(9-4-5-10-16(2)12-15)13-7-6-8-14(17)11-13/h6-8,11,17H,3-5,9-10,12H2,1-2H3
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = JLICHNCFTLFZJN-UHFFFAOYSA-N
| synonyms =
| density =
| melting_notes =
| boiling_point =
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| specific_rotation =
| sec_combustion =
}}

Meptazinol (trade name Meptid) is an opioid analgesic developed by Wyeth in the 1970s.[1] Indications for use in moderate to severe pain, most commonly used to treat pain in obstetrics (childbirth).

Meptazinol is a 3-phenylazepane derivative, whereas the other phenazepanes like ethoheptazine and proheptazine are 4-phenylazepanes.

A partial µ-opioid receptor agonist, its mixed agonist/antagonist activity affords it a lower risk of dependence and abuse than full µ agonists like morphine. Meptazinol exhibits not only a short onset of action, but also a shorter duration of action relative to other opioids such as morphine, pentazocine, or buprenorphine.[2]

References

1. ^{{ cite patent | country = US | status = patent | number = 4197239 | title = Hexahydroazepine, Piperidine and Pyrrolidine Derivatives | gdate = 1980-04-08 | inventor = Cavalla JF, Shepherd RG, White AC | assign1 = Wyeth }}
2. ^{{ cite journal |vauthors=Holmes B, Ward A | title = Meptazinol. A Review of its Pharmacodynamic and Pharmacokinetic Properties and Therapeutic Efficacy | journal = Drugs | year = 1985 | volume = 30 | issue = 4 | pages = 285–312 | pmid = 2998723 | doi=10.2165/00003495-198530040-00001}}

External links

  • {{MeshName|Meptazinol}}
{{Analgesics}}{{Opioidergics}}{{analgesic-stub}}

3 : Synthetic opioids|Azepanes|Phenols

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