前药列表¶
另见:天然药物来源 § 前体
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请不要把前体添加到本页里哦,而是添加到前体列表呢。 |
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**前药**是一类化合物,在经过给药后,会被代谢(也就是在体内转化)为具有药理活性的物质。[1] 无活性前药则是指那些在药理学上没有活性、但会在体内代谢为活性形式的化合物。与其直接给药某种药物,有时会改用其对应的前药,以改善药物的吸收、分布、代谢和排泄(ADME)特性呢。
当前药本身从胃肠道吸收较差时,人们常会专门设计前药来提高其生物利用度哦。前药也可以用来提高药物与其目标细胞或生理过程相互作用时的选择性,从而减少药物带来的不良或非预期效应嘛。
前药在由无活性物质转化为活性物质的过程中,可能会受到某个限速步骤的限制;在这种情况下,增加的通常只是作用持续时间,而不是作用强度呢。此外,与其非前药形式相比,前药还可能在药代动力学因素(也就是一种物质如何被吸收、分布、代谢和排泄)方面表现出其他差异哦。
作为前药发挥作用的娱乐性精神活性物质,包括GBL(GHB的前药)、赛洛西宾(赛洛辛的前药)、ALD-52(LSD的前药)等呢。
目录¶
抑制剂¶
- 1,4-BD(4-乙酰氧基丁醛的前药,而后者会进一步代谢为GHB)
- 4-CMC(3-CMC的前药,但会产生具有明显神经毒性的中间化学物质,例如环氧化物)
- 阿巴氯芬普拉卡比尔(R-巴氯芬的前药)
- 阿维扎封(地西泮的前药)
- 苯佐巴比妥(苯巴比妥的前药)
- 卡立普多(甲丙氨酯的前药)
- 氯尼普拉泮(氯硝西泮的前药)
- 可待因(吗啡的前药)
- 地西泮(奥沙西泮、去甲地西泮和替马西泮的前药)
- 乙基吗啡(吗啡的前药)
- 加巴喷丁恩那卡比(加巴喷丁的前药)
- GBL(GHB、4-乙酰氧基丁酸盐和4-乙酰氧基丁酸乙酯的前药)
- GBV(GHV的前药)
- 海洛因(口服时为吗啡的前药)
- 氢可酮(氢吗啡酮和去甲氢可酮的前药)
- 美达西泮(地西泮的前药)
- 吗啡(可待因的前药)
- 奥沙唑仑(去甲地西泮的前药)
- 羟考酮(羟吗啡酮的前药)
- 哌替啶(去甲哌替啶的前药)
- 利马扎封(利马唑仑和CCRIS 1930的前药)
- 曲马多(O-去甲曲马多和*N*-去甲曲马多的前药)
- 替马西泮(奥沙西泮的前药)
致幻剂¶
大麻类¶
- THC(11-羟基-THC的前药,这是人体内的主要代谢产物)
- THC-O-乙酸酯(THC的前药)
- THC-O-磷酸酯(THC的前药)
- 11-羟基-THC(11-去甲-9-羧基-THC的前药,这是人体内的次级代谢产物)
谵妄剂¶
- 鹅膏蕈氨酸(蝇蕈醇的前药)
解离剂¶
迷幻剂¶
- 1A-LSD(LSD的前药)
- 1B-LSD(可能是LSD的前药)
- 1P-ETH-LAD(疑似为ETH-LAD的前药)
- 1P-LSD(LSD的前药)
- 蟾毒色胺(DMT的前药)
- DOB(疑似为前药)
- 乙赛洛西宾(乙赛洛辛的前药)
- HOT-2(2C-T-2的前药)
- HOT-7(2C-T-7的前药)
- MDA(HHA的前药)
- MDMA(MDA、THM、THMA和HHMA的前药)
- 去甲伊博格碱(伊博格碱的前药)
- 去甲赛洛辛(赛洛辛的前药)
- 4-AcO-DMT(疑似为赛洛辛的前药)
- 赛洛西宾(赛洛辛的前药)
- ZDCM-04(DOC和咖啡因的前药)
益智药¶
兴奋剂¶
- 艾捉菲尼(莫达菲尼的前药)
- 安非他尼(苯丙胺的前药)
- 苄非他明(苯丙胺的前药)
- 咖啡因(副黄嘌呤、可可碱和苦茶碱的前药)
- 可卡因(去甲可卡因的前药)
- 屈昔多巴(去甲肾上腺素(去甲肾上腺素)的前药)
- 芬坎法明(苯丙胺和咖啡因的前药)
- L-DOPA(多巴胺的前药)
- 利右苯丙胺(右旋苯丙胺的前药)
- 尼古丁(可替宁的前药)
杂项¶
- 5-MT(蟾毒色胺的前药)
- 依托哌酮(mCPP的前药)
- 褪黑素(5-MT的前药)
- 纳洛酮(α-纳洛醇的前药)
- 萘法唑酮(mCPP的前药)
- 利培酮(帕利哌酮的前药)
- 舍曲林(去甲舍曲林(DMS)的前药)
- 曲唑酮(mCPP的前药)
- 司来吉兰(左甲基苯丙胺的前药)
兴奋剂¶
- 左旋咪唑(会在人类体内代谢为 aminorex(一种有毒的兴奋剂),但这并不被视为前药,因为这并不是它预期的或主要的作用哦)。可卡因中常常会掺入左旋咪唑,并可能导致左旋咪唑诱导性坏死综合征(LINES)。
- 人体内源性化合物列表
- ↑ C. G. Wermuth, C. R. Ganellin, P. Lindberg, L. A. Mitscher; Ganellin; Lindberg; Mitscher (1998). "Glossary of terms used in medicinal chemistry (IUPAC Recommendations 1998)". Pure and Applied Chemistry. 70 (5): 1129. https://doi.org/10.1351/pac199870051129
- ↑ Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/19502531
- ↑ The advantages of benzonal as an inducer of the liver mono-oxygenase enzyme system compared to phenobarbital. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/1305441
- ↑ Benzonal metabolism in guinea pigs. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2792358
- ↑ Deposition of diazepam and its metabolites in hair following a single dose of diazepam. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/27534563
- ↑ Biotransformation and pharmacokinetics of ethylmorphine after a single oral dose. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/7654478
- ↑ https://erowid.org/archive/rhodium/chemistry/ghb.html#GHV
- ↑ Sawynok J (January 1986). "The therapeutic use of heroin: a review of the pharmacological literature". Can. J. Physiol. Pharmacol. 64 (1): 1–6. doi:10.1139/y86-001. PMID 2420426.
- ↑ Morphine: pharmacokinetics and clinical practice. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2245160
- ↑ Development of a sensitive method for the determination of oxycodone and its major metabolites noroxycodone and oxymorphone in human plasma by liquid chromatography-tandem mass spectrometry. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26655109
- ↑ The excretion of pethidine and its derivatives (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1703639/
- ↑ <https://pubchem.ncbi.nlm.nih.gov/compound/826660/
- ↑ <https://pubchem.ncbi.nlm.nih.gov/compound/826660
- ↑ Metabolic profile of oxazepam and related benzodiazepines: clinical and forensic aspects. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/28903606
- ↑ Recent Advances in Anaesthesia and Intensive Care | https://books.google.co.uk/books?id=ei1edut0AqAC&pg=PA42&redir_esc=y#v=onepage&q&f=false
- ↑ Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/19515014
- ↑ https://www.erowid.org/library/books_online/pihkal/pihkal062.shtml
- ↑ Effects of 3,4-methylenedioxymethamphetamine (MDMA) and its main metabolites on cardiovascular function in conscious rats (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3874698/
- ↑ Short-term effects of 2,4,5-trihydroxyamphetamine, 2,4,5-trihydroxymethamphetamine and 3,4-dihydroxymethamphetamine on central tryptophan hydroxylase activity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/8496826
- ↑ Major and minor metabolites of cocaine in human plasma following controlled subcutaneous cocaine administration. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/17132243
- ↑ (S)-(-)-Cotinine, the major brain metabolite of nicotine, stimulates nicotinic receptors to evoke [3H]dopamine release from rat striatal slices in a calcium-dependent manner. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/10027825
- ↑ Active drug metabolites. An overview of their relevance in clinical pharmacokinetics. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2861928
- ↑ Metabolites of naloxone in human urine. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/5129377
- ↑ Atypical Psychotropic Agents | https://books.google.at/books?id=KfHEDgAAQBAJ&pg=PA460&redir_esc=y#v=onepage&q&f=false
- ↑ Comparative Pharmacology of Risperidone and Paliperidone. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2861928
- ↑ Engberg, G. O. R. A. N., Elebring, T. H. O. M. A. S., & Nissbrandt, H. (1991). Deprenyl (selegiline), a selective MAO-B inhibitor with active metabolites; effects on locomotor activity, dopaminergic neurotransmission and firing rate of nigral dopamine neurons. Journal of Pharmacology and Experimental Therapeutics, 259(2), 841-847.
- ↑ Determination of aminorex in human urine samples by GC-MS after use of levamisole. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/21531521
