匹那西泮

匹那西泮
臨床資料
其他名稱	9-chloro-6-phenyl-2-prop-2-ynyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-3-one
AHFS/Drugs.com	国际药品名称
给药途径	Oral
ATC碼	N05BA14 (WHO) ;
法律規範狀態
法律規範	加：Schedule IV; 德：Anlage III; 美：附表IV;
藥物動力學數據
药物代谢	Hepatic
排泄途徑	Renal
识别信息
	IUPAC命名法 7-chloro-5-phenyl-1-prop-2-yn-1-yl-1,3-dihydro-2H-1,4-benzodiazepin-2-one; ;
CAS号	52463-83-9
PubChem CID	40391;
DrugBank	? ;
ChemSpider	36899 ;
UNII	5286RBZ882;
KEGG	D07314 ;
ChEMBL	ChEMBL1213352 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID3023475 ;
ECHA InfoCard	100.052.650
化学信息
化学式	C18H13ClN2O
摩尔质量	308.8
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES Clc3cc\1c(N(C(=O)C/N=C/1c2ccccc2)CC#C)cc3;
	InChI InChI=1S/C18H13ClN2O/c1-2-10-21-16-9-8-14(19)11-15(16)18(20-12-17(21)22)13-6-4-3-5-7-13/h1,3-9,11H,10,12H2 ; Key:MFZOSKPPVCIFMT-UHFFFAOYSA-N ;

匹那西泮（英语：Pinazepam），商品名为Domar和Duna，是一种苯二氮䓬类药物。^[1]它具有抗焦虑、抗惊厥、镇静和骨骼肌松弛作用。^[2]

匹那西泮及其代谢物去甲西泮在子宫内转移至发育中的胎儿，但母亲血浆药物水平通常显着高于胎儿。^[3]

匹那西泮与其他苯二氮䓬类药物的不同之处在于它在苯二氮䓬结构的N-1位具有炔丙基。它的毒性低于地西泮，在动物研究中，它似乎具有抗焦虑和抗激动的特性，具有有限的睡眠和运动协调损害特性。^[4]^[5]匹那西泮在口服后被吸收迅速。匹那西泮的主要活性代谢产物是去炔丙基匹那西泮（即去甲西泮）和奥沙西泮。^[6]在人体中，匹那西泮作为一种纯抗焦虑剂发挥作用，因为它不具有任何显着的苯二氮䓬类药物的其他药理学特性。匹那西泮不会对智力、运动和睡眠造成损害，因此它比其他苯二氮䓬类药物更适合在白天使用。^[7]^[8]^[9]老年人的消除半衰期较长。^[10]

参见

苯二氮䓬类

参考资料

^ Schütz H, Holland EM, Kazemian-Erdmann F, Schölermann K. [Screening of the new benzodiazepine derivative, pinazepan, and its major metabolites]. Arzneimittel-Forschung. September 1988, 38 (9): 1372–5. PMID 3146986.
^ Janbroers, J. M. Pinazepam: review of pharmacological properties and therapeutic efficacy. Clinical Therapeutics. 1984, 6 (4): 434–450 [2023-01-25]. ISSN 0149-2918. PMID 6147192. （原始内容存档于2023-01-25）.
^ Pacifici GM, Cuoci L, Guarneri M, Fornaro P, Arcidiacono G, Cappelli N, et al. Placental transfer of pinazepam and its metabolite N-desmethyldiazepam in women at term. European Journal of Clinical Pharmacology. 1984, 27 (3): 307–10. PMID 6150857. S2CID 1389302. doi:10.1007/BF00542165.
^ Universal Guide to Diazepam. fastukmeds.to. [2021-08-23].
^ Diazepam Injection BP - Summary of Product Characteristics (SmPC) - (emc). www.medicines.org.uk. [2021-08-23]. （原始内容存档于2023-01-25）.
^ Dinis-Oliveira, Ricardo Jorge. Metabolic profile of oxazepam and related benzodiazepines: clinical and forensic aspects. Drug Metabolism Reviews. Sep 14, 2017, 49 (4): 451–463 [2023-01-25]. ISSN 1097-9883. PMID 28903606. S2CID 4528255. doi:10.1080/03602532.2017.1377223. （原始内容存档于2023-01-25）.
^ Janbroers JM. Pinazepam: review of pharmacological properties and therapeutic efficacy. Clinical Therapeutics. 1984, 6 (4): 434–50. PMID 6147192.
^ Pacifici GM, Placidi GF, Fornaro P, Gomeni R. Pharmacokinetics of pinazepam in healthy volunteers. International Journal of Clinical Pharmacology Research. 1983, 3 (5): 331–7. PMID 6147314.
^ Pacifici GM, Placidi GF, Fornaro P, Gomeni R. Pinazepam: a precursor of N-desmethyldiazepam. European Journal of Clinical Pharmacology. 1982, 22 (3): 225–8. PMID 6809477. S2CID 1977572. doi:10.1007/BF00545219.
^ Pacifici GM, Cuoci L, Placidi GF, Fornaro P, Gomeni R. Elimination kinetics of desmethyldiazepam in two young and two elderly subjects. European Journal of Drug Metabolism and Pharmacokinetics. Jan 1982, 7 (1): 69–72. PMID 6802645. S2CID 21836038. doi:10.1007/bf03189546.

外部链接

Inchem - Pinazepam （页面存档备份，存于互联网档案馆）

[1] Schütz H, Holland EM, Kazemian-Erdmann F, Schölermann K. [Screening of the new benzodiazepine derivative, pinazepan, and its major metabolites]. Arzneimittel-Forschung. September 1988, 38 (9): 1372–5. PMID 3146986.

[2] Janbroers, J. M. Pinazepam: review of pharmacological properties and therapeutic efficacy. Clinical Therapeutics. 1984, 6 (4): 434–450 [2023-01-25]. ISSN 0149-2918. PMID 6147192. （原始内容存档于2023-01-25）.

[3] Pacifici GM, Cuoci L, Guarneri M, Fornaro P, Arcidiacono G, Cappelli N, et al. Placental transfer of pinazepam and its metabolite N-desmethyldiazepam in women at term. European Journal of Clinical Pharmacology. 1984, 27 (3): 307–10. PMID 6150857. S2CID 1389302. doi:10.1007/BF00542165.

[4] Universal Guide to Diazepam. fastukmeds.to. [2021-08-23].

[5] Diazepam Injection BP - Summary of Product Characteristics (SmPC) - (emc). www.medicines.org.uk. [2021-08-23]. （原始内容存档于2023-01-25）.

[6] Dinis-Oliveira, Ricardo Jorge. Metabolic profile of oxazepam and related benzodiazepines: clinical and forensic aspects. Drug Metabolism Reviews. Sep 14, 2017, 49 (4): 451–463 [2023-01-25]. ISSN 1097-9883. PMID 28903606. S2CID 4528255. doi:10.1080/03602532.2017.1377223. （原始内容存档于2023-01-25）.

[7] Janbroers JM. Pinazepam: review of pharmacological properties and therapeutic efficacy. Clinical Therapeutics. 1984, 6 (4): 434–50. PMID 6147192.

[8] Pacifici GM, Placidi GF, Fornaro P, Gomeni R. Pharmacokinetics of pinazepam in healthy volunteers. International Journal of Clinical Pharmacology Research. 1983, 3 (5): 331–7. PMID 6147314.

[9] Pacifici GM, Placidi GF, Fornaro P, Gomeni R. Pinazepam: a precursor of N-desmethyldiazepam. European Journal of Clinical Pharmacology. 1982, 22 (3): 225–8. PMID 6809477. S2CID 1977572. doi:10.1007/BF00545219.

[10] Pacifici GM, Cuoci L, Placidi GF, Fornaro P, Gomeni R. Elimination kinetics of desmethyldiazepam in two young and two elderly subjects. European Journal of Drug Metabolism and Pharmacokinetics. Jan 1982, 7 (1): 69–72. PMID 6802645. S2CID 21836038. doi:10.1007/bf03189546.

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