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This collection combines attributed Wikipedia excerpts and original SciAtlas bilingual definitions under CC BY-SA 4.0. Excerpts were extracted and shortened; machine-assisted Chinese translations are labeled. Original entries provide further reading. Language versions may differ in emphasis and do not replace standards. Concepts can appear in several disciplines; consult standards and original literature for rigorous use.

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Pharmacokinetics

Inverse agonist

反向激动剂

在药理学中,反向激动剂是与激动剂结合相同受体但诱导与激动剂相反的药理反应的药物。中性拮抗剂在缺乏激动剂或反向激动剂的情况下没有活性,但可以阻断其中任何一种的活性;事实上,它们有时被称为阻滞剂(例子包括α阻滞剂、β阻滞剂和钙通道阻滞剂)。反向激动剂与激动剂具有相反的作用,但两者的作用都可以被拮抗剂阻断。反向激动剂反应的先决条件是受体在没有任何配体的情况下必须具有组成型(也称为内在或基础)活性水平。激动剂将受体的活性增加至基础水平以上,而反向激动剂将受体的活性降低至基础水平以下。

In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either; they are in fact sometimes called blockers (examples include alpha blockers, beta blockers, and calcium channel blockers). Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists. A prerequisite for an inverse agonist response is that the receptor must have a constitutive (also known as intrinsic or basal) level of activity in the absence of any ligand. An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level.

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Pharmacokinetics

Functional selectivity

功能选择性

功能选择性(或激动剂运输、偏向激动、偏向信号传导、配体偏向和差异接合)是相对于同一受体上的参考配体(通常是内源激素或肽),某些信号转导途径的配体依赖性选择性。当受体具有多种可能的信号转导途径时,可以存在功能选择性。因此,每个途径被激活的程度取决于哪个配体与受体结合。功能选择性或偏向信号传导在 G 蛋白偶联受体 (GPCR) 中得到最广泛的表征。许多偏向激动剂,例如作为镇痛药或抗增殖药物测试的毒蕈碱 M2 受体激动剂,或介导疼痛的阿片受体激动剂,在各种受体家族中显示出增加有益特性同时减少副作用的潜力。

Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor. Functional selectivity can be present when a receptor has several possible signal transduction pathways. To which degree each pathway is activated thus depends on which ligand binds to the receptor. Functional selectivity, or biased signaling, is most extensively characterized at G protein coupled receptors (GPCRs). A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects.

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Pharmacokinetics

Non-competitive inhibition

非竞争性抑制

非竞争性抑制是酶抑制的一种类型,其中抑制剂降低酶的活性并与酶结合得同样好,无论它是否已经结合底物。这与竞争性抑制不同,竞争性抑制在抑制剂存在的情况下酶底物的结合亲和力会降低。无论底物是否已经结合,抑制剂都可以与酶结合,但如果它在一种状态或另一种状态下与酶结合具有更高的亲和力,则称为混合抑制剂。

Non-competitive inhibition is a type of enzyme inhibition where the inhibitor reduces the activity of the enzyme and binds equally well to the enzyme regardless of whether it has already bound the substrate. This is unlike competitive inhibition, where binding affinity for the substrate in the enzyme is decreased in the presence of an inhibitor. The inhibitor may bind to the enzyme regardless of whether the substrate has already been bound, but if it has a higher affinity for binding the enzyme in one state or the other, it is called a mixed inhibitor.

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Pharmacokinetics

Mechanism of action

作用机制

在药理学中,术语“作用机制”(MOA) 是指药物产生其药理作用的特定生化相互作用。作用机制通常包括提及药物结合的特定分子靶标,例如酶或受体。根据药物的化学结构以及在那里发生的特定作用,受体位点对药物具有特定的亲和力。不与受体结合的药物通过简单地与体内的化学或物理性质相互作用而产生相应的治疗效果。以这种方式起作用的药物的常见例子是抗酸剂和泻药。相比之下,作用模式 (MoA) 描述了由于活体暴露于某种物质而导致的细胞水平的功能或解剖学变化。

In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect. A mechanism of action usually includes mention of the specific molecular targets to which the drug binds, such as an enzyme or receptor. Receptor sites have specific affinities for drugs based on the chemical structure of the drug, as well as the specific action that occurs there. Drugs that do not bind to receptors produce their corresponding therapeutic effect by simply interacting with chemical or physical properties in the body. Common examples of drugs that work in this way are antacids and laxatives. In contrast, a mode of action (MoA) describes functional or anatomical changes, at the cellular level, resulting from the exposure of a living organism to a substance.

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Pharmacokinetics

Mode of action

作用方式

在药理学和生物化学中,作用模式 (MoA) 描述了由于活体暴露于某种物质而导致的功能或解剖学变化。相比之下,作用机制(MOA)描述了分子水平上的这种变化。作用模式在化学物质分类中很重要,因为它代表了分子机制和生理结果之间的中间复杂程度,特别是当确切的分子靶标尚未阐明或存在争议时。化学物质的作用机制可能是“与 DNA 结合”,而其更广泛的作用模式是“转录调节”。然而,尚无明确的共识,并且术语“作用模式”也经常被使用,特别是在农药研究中,来描述分子机制,例如对特定核受体或酶的作用。

In pharmacology and biochemistry, mode of action (MoA) describes a functional or anatomical change, resulting from the exposure of a living organism to a substance. In comparison, a mechanism of action (MOA) describes such changes at the molecular level. A mode of action is important in classifying chemicals, as it represents an intermediate level of complexity in between molecular mechanisms and physiological outcomes, especially when the exact molecular target has not yet been elucidated or is subject to debate. A mechanism of action of a chemical could be "binding to DNA" while its broader mode of action would be "transcriptional regulation". However, there is no clear consensus and the term mode of action is also often used, especially in the study of pesticides, to describe molecular mechanisms such as action on specific nuclear receptors or enzymes.

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Pharmacokinetics

Indirect agonist

间接激动剂

在药理学中,间接激动剂或间接作用激动剂是增强内源性神经递质的释放或作用但对神经递质受体本身没有特异性激动剂活性的物质。间接激动剂通过不同的机制发挥作用,包括转运蛋白阻断、诱导递质释放和抑制递质崩溃。

In pharmacology, an indirect agonist or indirect-acting agonist is a substance that enhances the release or action of an endogenous neurotransmitter but has no specific agonist activity at the neurotransmitter receptor itself. Indirect agonists work through varying mechanisms to achieve their effects, including transporter blockade, induction of transmitter release, and inhibition of transmitter breakdown.

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Pharmacokinetics

Intrinsic activity

效能 (药理学)

内在活性(IA)和最大功效(Emax)是指药物-受体复合物产生最大功能反应的相对能力。这必须与亲和力和 EC50 区分开来,亲和力是药物与其分子靶标结合能力的衡量标准,EC50 是药物效力的衡量标准,与功效和亲和力成正比。 Stephenson (1956) 引入“功效”一词来描述激动剂产生的反应的不同方式,即使它们占据相同数量的受体。高效激动剂可以产生受体系统的最大反应,同时在该系统中占据相对较低比例的受体。功效和内在活性之间存在区别。

Intrinsic activity (IA) and maximal efficacy (Emax) refer to the relative ability of a drug-receptor complex to produce a maximum functional response. This must be distinguished from the affinity, which is a measure of the ability of the drug to bind to its molecular target, and the EC50, which is a measure of the potency of the drug and which is proportional to both efficacy and affinity. This use of the word "efficacy" was introduced by Stephenson (1956) to describe the way in which agonists vary in the response they produce, even when they occupy the same number of receptors. High efficacy agonists can produce the maximal response of the receptor system while occupying a relatively low proportion of the receptors in that system. There is a distinction between efficacy and intrinsic activity.

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Pharmacokinetics

Multivalued treatment

多值治疗

在统计学中,特别是在实验设计中,多值处理是可以采用两个以上值的处理。这与医学文献中的剂量反应模型有关。

In statistics, in particular in the design of experiments, a multi-valued treatment is a treatment that can take on more than two values. It is related to the dose-response model in the medical literature.

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Pharmacokinetics

Off-target activity

脱靶活动

脱靶活性是指药物的生物活性与其预期生物靶点不同且不针对其预期生物靶点。它最常导致副作用。然而,在某些情况下,可以利用脱靶活性来达到治疗目的。这方面的一个例子是抗盐皮质激素和利尿剂螺内酯的重新利用,它们被发现会产生女性化和男性乳房发育的副作用,作为抗雄激素用于治疗女性痤疮和多毛症等雄激素依赖性疾病。二甲双胍还会导致脱靶活动。

Off-target activity is biological activity of a drug that is different from and not directed at that of its intended biological target. It most commonly contributes to side effects. However, in some cases, off-target activity can be taken advantage of for therapeutic purposes. An example of this is the repurposing of the antimineralocorticoid and diuretic spironolactone, which was found to produce feminization and gynecomastia as side effects, for use as an antiandrogen in the treatment of androgen-dependent conditions like acne and hirsutism in women. Metformin also causes off-target activity.

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Pharmacokinetics

In vivo supersaturation

体内过饱和

体内过饱和是口服化合物在通过胃肠道时发生过饱和的行为。通常这些化合物具有弱碱性(pKa 在 5 至 8 范围内)并且在水溶液中溶解度相对较低。体内过饱和是一种最近出现的现象,由 Yamashita 等人首先观察到。 2003年。

In vivo supersaturation is the behavior of orally administered compounds that undergo supersaturation as they pass through the gastrointestinal (GI) tract. Typically these compounds have a weakly basic nature (pKa in the range of 5 to 8) and a relatively low solubility in aqueous solutions. In vivo supersaturation is a recent phenomenon that was first observed by Yamashita et al. in 2003.

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Pharmacokinetics

Medical prescription

处方

医疗方面的处方(在北美通常缩写为 ℞ 或 Rx)是医生或其他注册医疗保健专业人员与药剂师的正式沟通,授权他们为特定患者配发特定处方药。从历史上看,这是医生给药剂师的指示,列出了要配制到治疗中的材料——符号℞(大写字母R,交叉表示缩写)来自中世纪处方的第一个词,拉丁语配方(字面意思是“你服用”),它给出了要配制的材料清单。对内容、谁可以开处方以及如何传输处方的要求因国家/地区而异;许多司法管辖区使用电子处方系统。

A prescription in the medical context, often abbreviated as ℞ or Rx in North America, is a formal communication from physicians or other registered healthcare professionals to a pharmacist, authorizing them to dispense a specific prescription drug for a specific patient. Historically, it was a physician's instruction to an apothecary listing the materials to be compounded into a treatment—the symbol ℞ (a capital letter R, crossed to indicate abbreviation) comes from the first word of a medieval prescription, Latin recipe (lit. 'you take'), that gave the list of the materials to be compounded. Requirements for content, who may prescribe, and how prescriptions are transmitted vary by country; many jurisdictions use electronic prescribing systems.

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Pharmacokinetics

Combination therapy

联合疗法

联合疗法或多疗法是使用一种以上药物或方式的疗法。通常,该术语指使用多种疗法来治疗单一疾病,并且通常所有疗法都是药物疗法(尽管它也可能涉及非药物疗法,例如药物和谈话疗法的结合来治疗抑郁症)。 “药物”联合疗法可以通过开具/施用单独的药物或在可用的情况下包含超过一种活性成分的剂型(例如固定剂量组合)来实现。复方用药是一个相关术语,指使用多种药物(无论它们是针对相同还是单独的病症/疾病)。有时,“综合药物”用于指药物联合治疗。

Combination therapy or polytherapy is therapy that uses more than one medication or modality. Typically, the term refers to using multiple therapies to treat a single disease, and often all the therapies are pharmaceutical (although it can also involve non-medical therapy, such as the combination of medications and talk therapy to treat depression). 'Pharmaceutical' combination therapy may be achieved by prescribing/administering separate drugs, or, where available, dosage forms that contain more than one active ingredient (such as fixed-dose combinations). Polypharmacy is a related term, referring to the use of multiple medications (without regard to whether they are for the same or separate conditions/diseases). Sometimes "polymedicine" is used to refer to pharmaceutical combination therapy.

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Pharmacokinetics

Drug pleiotropy

药物多效性

在药理学中,多效性包括药物的所有作用,而不是专门开发药物的作用。它可能包括有害的不利影响,但通常用于表示额外的有益影响。例如,他汀类药物是 HMG-CoA 还原酶抑制剂,主要通过减少胆固醇合成发挥作用,但据信还具有其他有益作用,包括充当抗氧化剂和稳定动脉粥样硬化斑块。类固醇药物,如泼尼松和泼尼松龙,具有多效性作用,包括全身作用,其原因与内源性类固醇激素的作用相同:全身的细胞都有可以对其做出反应的受体,因为内源性受体是内分泌信使。

In pharmacology, pleiotropy includes all of a drug's actions other than those for which the agent was specifically developed. It may include adverse effects which are detrimental ones, but is often used to denote additional beneficial effects. For example, statins are HMG-CoA reductase inhibitors that primarily act by decreasing cholesterol synthesis, but which are believed to have other beneficial effects, including acting as antioxidants and stabilizing atherosclerotic plaques. Steroid drugs, such as prednisone and prednisolone, have pleiotropic effects, including systemic ones, for the same reason that endogenous steroid hormones do: cells throughout the body have receptors that can respond to them, because the endogenous ones are endocrine messengers.

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Pharmacokinetics

Guide to Pharmacology

药理学指南

IUPHAR/BPS 药理学指南是一个开放访问网站,充当有关许可药物和其他小分子生物靶点信息的门户。 《药理学指南》(标准缩写为 GtoPdb)是由国际基础与临床药理学联合会 (IUPHAR) 和英国药理学会 (BPS) 联合开发的。它取代并扩展了原来的 2009 IUPHAR 数据库(标准缩写 IUPHAR-DB)。 《药理学指南》旨在提供所有药理学目标的简明概述,供科学界和临床界的所有成员以及感兴趣的公众使用,并提供有关选定目标集的详细信息的链接。特色信息包括药理学数据、靶标和基因命名法,以及配体的精选化学信息。

The IUPHAR/BPS Guide to PHARMACOLOGY is an open-access website, acting as a portal to information on the biological targets of licensed drugs and other small molecules. The Guide to PHARMACOLOGY (with GtoPdb being the standard abbreviation) is developed as a joint venture between the International Union of Basic and Clinical Pharmacology (IUPHAR) and the British Pharmacological Society (BPS). This replaces and expands upon the original 2009 IUPHAR Database (standard abbreviation IUPHAR-DB). The Guide to PHARMACOLOGY aims to provide a concise overview of all pharmacological targets, accessible to all members of the scientific and clinical communities and the interested public, with links to details on a selected set of targets. The information featured includes pharmacological data, target, and gene nomenclature, as well as curated chemical information for ligands.

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Pharmacokinetics

Drug vectorization

药物矢量化

在药理学和医学中,药物的矢量化是指(细胞内)以塑料、贵金属或硅纳米粒子或脂质体为目标,药理活性物质通过吸附可逆地结合或附着。 CNRS的研究人员设计了一种利用聚氰基丙烯酸烷基酯(PACA)纳米粒子作为“载体”来克服多重耐药性问题的方法。作为一个正在发展的概念,药物纳米载体有望通过克服半透膜和血脑屏障等生物屏障,在向肿瘤组织输送多种药物方面发挥重要作用。

In pharmacology and medicine, vectorization of drugs refers to (intracellular) targeting with plastic, noble metal or silicon nanoparticles or liposomes to which pharmacologically active substances are reversibly bound or attached by adsorption. CNRS researchers have devised a way to overcome the problem of multidrug resistance using polyalkyl cyanoacrylate (PACA) nanoparticles as "vectors". As a developing concept, drug nanocarriers are expected to play a major role in delivering multiple drugs to tumor tissues by overcoming semi-permeable membranes and biological barriers such as the blood–brain barrier.

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Pharmacokinetics

Functional analog (chemistry)

功能類似物 (化學)

在化学和药理学中,功能类似物是具有相似的物理、化学、生化或药理学特性的化合物。功能类似物不一定是具有相似化学结构的结构类似物。药理功能类似物的一个例子是吗啡、海洛因和芬太尼,它们具有相同的作用机制,但芬太尼在结构上与其他两者有很大不同,剂量也有显着差异。

In chemistry and pharmacology, functional analogs are chemical compounds that have similar physical, chemical, biochemical, or pharmacological properties. Functional analogs are not necessarily structural analogs with a similar chemical structure. An example of pharmacological functional analogs are morphine, heroin and fentanyl, which have the same mechanism of action, but fentanyl is structurally quite different from the other two with significant variance in dosage.

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Pharmacokinetics

Drug titration

药物滴定

药物滴定是调整药物剂量以获得最大益处而不产生副作用的过程。当药物的治疗指数较窄时,滴定尤其重要,因为药物有效的剂量与发生副作用的剂量之间的范围很小。通常需要滴定的药物类型的一些例子包括胰岛素、抗惊厥药、血液稀释剂、抗抑郁药和镇静剂。在某些情况下,建议逐渐停药而不是突然停药。糖皮质激素长期使用后应逐渐减量,以避免肾上腺皮质功能不全。药物滴定也用于I期临床试验。实验药物的剂量逐渐增加,直到副作用变得无法忍受。找到合适剂量的临床试验称为剂量范围研究。

Drug titration is the process of adjusting the dose of a medication for the maximum benefit without adverse effects. When a drug has a narrow therapeutic index, titration is especially important, because the range between the dose at which a drug is effective and the dose at which side effects occur is small. Some examples of the types of drugs commonly requiring titration include insulin, anticonvulsants, blood thinners, anti-depressants, and sedatives. Titrating off of a medication instead of stopping abruptly is recommended in some situations. Glucocorticoids should be tapered after extended use to avoid adrenal insufficiency. Drug titration is also used in phase I of clinical trials. The experimental drug is given in increasing dosages until side effects become intolerable. A clinical trial in which a suitable dose is found is called a dose-ranging study.

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Pharmacokinetics

FK962

FK962(专业术语)

FK962 是一种作为生长抑素释放增强剂的化合物。它刺激神经生长和神经突伸长,并已在动物模型中进行了研究,以期在治疗阿尔茨海默病和视网膜神经病等疾病方面具有潜在的应用。

FK962 is a compound which acts as an enhancer of somatostatin release. It stimulates nerve growth and neurite elongation, and has been researched in animal models for potential applications in the treatment of conditions such as Alzheimer's disease and retinal neuropathy.

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Pharmacokinetics

Toxicology

毒理学

毒理学是一门与生物学、化学、药理学和医学交叉的科学学科,涉及化学物质对生物体的不利影响的研究以及毒素和毒物暴露的诊断和治疗实践。剂量与其对暴露生物体的影响之间的关系在毒理学中具有重要意义。影响化学毒性的因素包括剂量、接触时间(无论是急性还是慢性)、接触途径、物种、年龄、性别和环境。毒理学家是毒物和中毒方面的专家。作为更大的循证实践运动的一部分,存在着一场基于证据的毒理学运动。毒理学目前正在为癌症研究领域做出贡献,因为一些毒素可以用作杀死肿瘤细胞的药物。

Toxicology is a scientific discipline, overlapping with biology, chemistry, pharmacology, and medicine, that involves the study of the adverse effects of chemical substances on living organisms and the practice of diagnosing and treating exposures to toxins and toxicants. The relationship between dose and its effects on the exposed organism is of high significance in toxicology. Factors that influence chemical toxicity include the dosage, duration of exposure (whether it is acute or chronic), route of exposure, species, age, sex, and environment. Toxicologists are experts on poisons and poisoning. There is a movement for evidence-based toxicology as part of the larger movement towards evidence-based practices. Toxicology is currently contributing to the field of cancer research, since some toxins can be used as drugs for killing tumor cells.

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Pharmacokinetics

Zoopharmacognosy

动物生药学

动物生药学是非人类动物通过选择、摄入或局部施用具有药用特性的植物、土壤和昆虫来进行自我治疗的行为,以预防或减少病原体、毒素甚至其他动物的有害影响。该术语源自希腊语“zoon”(“动物”)、“pharmacon”(“药物”)和“gnosis”(“知识”)。动物生药学的一个例子发生在狗吃草来诱发呕吐时。然而,行为比这更加多样化。动物摄入或使用非食物,如粘土、木炭,甚至有毒植物和无脊椎动物,显然是为了防止寄生虫感染或中毒。动物是否真正自我治疗仍然是一个颇有争议的话题,因为早期证据大多是间接证据或轶事。然而,最近的研究采用了实验性的、假设驱动的方法。

Zoopharmacognosy is a behaviour in which non-human animals self-medicate by selecting and ingesting or topically applying plants, soils and insects with medicinal properties, to prevent or reduce the harmful effects of pathogens, toxins, and even other animals. The term derives from Greek words zoon ("animal"), pharmacon ("drug, medicine"), and gnosis ("knowledge"). An example of zoopharmacognosy occurs when dogs eat grass to induce vomiting. However, the behaviour is more diverse than this. Animals ingest or apply non-foods such as clay, charcoal and even toxic plants and invertebrates, apparently to prevent parasitic infestation or poisoning. Whether animals truly self-medicate remains a somewhat controversial subject because early evidence is mostly circumstantial or anecdotal. However, more recent examinations have adopted an experimental, hypothesis-driven approach.

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Pharmacokinetics

Toxicant

毒剂

毒物是指任何有毒物质,无论是人造的还是天然存在的。相比之下,毒素是生物体(例如植物、动物、昆虫、细菌)自然产生的毒物。空气、土壤、水或食物中都存在不同类型的有毒物质。

A toxicant is any toxic substance, whether artificial or naturally occurring. By contrast, a toxin is a poison produced naturally by an organism (e.g. plant, animal, insect, bacterium). The different types of toxicants can be found in the air, soil, water, or food.

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Pharmacokinetics

Structured intermittent therapy

结构化间歇疗法

结构化间歇疗法 (SIT) 是由马克·戴布尔 (Mark Dybul)、安东尼·福奇 (Anthony Fauci) 和美国国立卫生研究院的其他研究科学家于 2000 年初创造的,作为 HIV 患者减少治疗的一种形式。 HIV+患者服用抗HIV药物7天,然后7天不服用药物。一般来说,接受持续高效抗逆转录病毒治疗 (HAART) 积极治疗的 HIV 患者寿命较长,但他们无法完全消除 HIV 病毒,并且会出现许多不良副作用。 HAART 的长期毒性和经济费用使其不适合作为 HIV 患者的标准长期治疗。因此,设计了一项关于以结构化间歇方式给药的简短研究。

Structured intermittent therapy (SIT) was coined in early 2000 by Mark Dybul, Anthony Fauci, and other research scientists from the National Institute of Health, as a form of reduced treatment for patients with HIV. HIV+ patients took anti-HIV drugs for seven days, and then took no drugs for seven days. Generally, patients with HIV who were being treated aggressively with continuous highly active antiretroviral therapy (HAART) lived longer lives, but they were not able to eliminate the HIV virus altogether and experienced many undesirable side effects. The long-term toxicity and financial expense of HAART makes it undesirable as the standard, long-term treatment for HIV patients. Consequently, a short study on administering medications in a structured intermittent manner was designed.

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Pharmacokinetics

Tolerability

耐受性

在药理学中,耐受性是指患者可以耐受药物的明显不良反应的程度。特定药物的耐受性可以在一般意义上进行讨论,也可以作为临床研究的一部分进行量化测量。通常,它是通过“退出”率来衡量的,即由于极端不良反应而放弃参与研究的患者的比率。然而,耐受性通常与药物旨在治疗的疾病的严重程度有关。例如,癌症患者在化疗研究期间可能会忍受明显的疼痛或不适,希望延长生存期或找到治愈方法,而经历良性病症(例如头痛)的患者则不太可能这样做。

In pharmacology, tolerability refers to the degree to which overt adverse effects of a drug can be tolerated by a patient. Tolerability of a particular drug can be discussed in a general sense, or it can be a quantifiable measurement as part of a clinical study. Usually, it is measured by the rate of "dropouts", or patients that forfeit participation in a study due to extreme adverse effects. Tolerability, however, is often relative to the severity of the medical condition a drug is designed to treat. For instance, cancer patients may tolerate significant pain or discomfort during a chemotherapeutic study with the hope of prolonging survival or finding a cure, whereas patients experiencing a benign condition, such as a headache, are less likely to.

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Pharmacokinetics

Threshold dose

阈值剂量

阈剂量是在动物中引发最小可检测生物效应的药物的最小剂量。在极低剂量下,某些药物不产生生物反应。剂量增加到阈值剂量以上会导致生物反应百分比增加。已经建立了几个基准来描述特定剂量的药物对特定物种的影响,例如未观察到的效应水平(NOEL)、未观察到的不良效应水平(NOAEL)和最低观察到的不良效应水平(LOAEL)。它们是通过审查现有研究和动物研究而建立的。在风险评估中应用阈值剂量可以保护人体临床试验的参与者并评估长期暴露于某些物质的风险。

Threshold dose is the minimum dose of drug that triggers minimal detectable biological effect in an animal. At extremely low doses, biological responses are absent for some of the drugs. The increase in dose above threshold dose induces an increase in the percentage of biological responses. Several benchmarks have been established to describe the effects of a particular dose of drug in a particular species, such as no-observed-effect-level (NOEL), no-observed-adverse-effect-level (NOAEL), and lowest-observed-adverse-effect-level (LOAEL). They are established by reviewing the available studies and animal studies. The application of threshold dose in risk assessment safeguards the participants in human clinical trials and evaluates the risks of chronic exposure to certain substances.

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Pharmacokinetics

Therapeutic interfering particle

治疗性干扰粒子

治疗干扰颗粒是一种抗病毒制剂,可降低特定病毒感染性疾病的复制率和发病机制。治疗干扰颗粒通常是从被靶向的病毒基因组部分工程化的生物制剂(即核酸)。与缺陷干扰颗粒 (DIP) 类似,该试剂与受感染细胞内的病原体竞争关键的病毒复制资源,降低病毒复制率并导致发病机制减少。但是,与 DIP 相比,TIP 被设计为具有大于 1 (R0>1) 的体内基本繁殖比 (R0)。 “TIP”一词于 2011 年首次推出,基于 2003 年的作用机制模型。

A therapeutic interfering particle is an antiviral preparation that reduces the replication rate and pathogenesis of a particular viral infectious disease. A therapeutic interfering particle is typically a biological agent (i.e., nucleic acid) engineered from portions of the viral genome being targeted. Similar to Defective Interfering Particles (DIPs), the agent competes with the pathogen within an infected cell for critical viral replication resources, reducing the viral replication rate and resulting in reduced pathogenesis. But, in contrast to DIPs, TIPs are engineered to have an in vivo basic reproductive ratio (R0) that is greater than 1 (R0>1). The term "TIP" was first introduced in 2011 based on models of its mechanism-of-action from 2003.

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Pharmacokinetics

Tapering (medicine)

逐渐减量(医学)

在医学上,逐渐减少是指逐渐减少药物剂量以减少或停止用药的做法。一般来说,逐渐减量是为了避免或尽量减少因神经生物学适应药物而引起的戒断症状。由于这种身体依赖性,可能需要逐渐减量的精神药物包括阿片类药物、选择性血清素再摄取抑制剂、抗精神病药、抗惊厥药和苯二氮卓类药物。

In medicine, tapering is the practice of gradually reducing the dosage of a medication to reduce or discontinue it. Generally, tapering is done to avoid or minimize withdrawal symptoms that arise from neurobiological adaptation to the drug. Prescribed psychotropic drugs that may require tapering due to this physical dependence include opioids, selective serotonin reuptake inhibitors, antipsychotics, anticonvulsants, and benzodiazepines.

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Pharmacokinetics

Cyanide

氰化物

在化学中,氰化物(来自希腊语 kyanos“深蓝色”)是一种含有 C=N 官能团的无机化合物。该基团称为氰基,由与氮原子三键连接的碳原子组成。离子氰化物含有氰化物阴离子-C=N。这种阴离子具有剧毒,会导致氰化物中毒。可溶性氰化物盐如氰化钠(NaCN)、氰化钾(KCN)和氰化四乙铵([(CH3CH2)4N]CN)也具有剧毒。共价氰化物含有-C=N基团,如果该基团通过单个共价键与碳原子连接,则通常称为腈。例如,在乙腈CH3-CeqN中,氰化物基团与甲基-CH3键合。在四氰基甲烷 C(−CeqN)4 中,四个氰基与碳键合。虽然腈通常不释放氰化物离子,但氰醇会释放氰化物离子,因此有毒。

In chemistry, a cyanide (from Greek kyanos 'dark blue') is an inorganic chemical compound that contains a C≡N functional group. This group, known as the cyano group, consists of a carbon atom triple-bonded to a nitrogen atom. Ionic cyanides contain the cyanide anion −C≡N. This anion is extremely toxic and causes cyanide poisoning. Soluble cyanide salts such as sodium cyanide (NaCN), potassium cyanide (KCN) and tetraethylammonium cyanide ([(CH3CH2)4N]CN) are also highly toxic. Covalent cyanides contain the −C≡N group, and are usually called nitriles if the group is linked by a single covalent bond to carbon atom. For example, in acetonitrile CH3−C≡N, the cyanide group is bonded to methyl −CH3. In tetracyanomethane C(−C≡N)4, four cyano groups are bonded to carbon. Although nitriles generally do not release cyanide ions, the cyanohydrins do and are thus toxic.

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Pharmacokinetics

Chronic toxicity

慢性毒性

慢性毒性是由于长期接触污染物或其他应激源而产生的不利影响,是水生毒理学的一个重要方面。与慢性毒性相关的不良反应可能是直接致命的,但更常见的是亚致死的,包括生长、繁殖或行为的变化。慢性毒性与急性毒性相反,急性毒性在较短的时间内发生至较高的浓度。可以进行各种毒性测试来评估不同污染物的慢性毒性,通常至少持续生物体寿命的 10%。水生慢性毒性测试的结果可用于确定水生生物保护的水质指南和法规。

Chronic toxicity, the development of adverse effects as a result of long term exposure to a contaminant or other stressor, is an important aspect of aquatic toxicology. Adverse effects associated with chronic toxicity can be directly lethal but are more commonly sublethal, including changes in growth, reproduction, or behavior. Chronic toxicity is in contrast to acute toxicity, which occurs over a shorter period of time to higher concentrations. Various toxicity tests can be performed to assess the chronic toxicity of different contaminants, and usually last at least 10% of an organism's lifespan. Results of aquatic chronic toxicity tests can be used to determine water quality guidelines and regulations for protection of aquatic organisms.

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Pharmacokinetics

Cytotoxicity

細胞毒性

细胞毒性是指物质或制剂损伤或杀死活细胞的能力,反映了药理学、毒理学和生物医学中的关键参数。它与细胞抑制作用不同,细胞抑制作用抑制细胞生长和增殖而不导致细胞死亡。细胞毒性剂可诱导一系列细胞反应,包括抑制细胞生长、诱导细胞凋亡或坏死性细胞死亡以及破坏代谢或结构细胞完整性。评估细胞毒性对于评估药物化合物、化学品和生物材料的安全性和有效性至关重要,因为它有助于预测潜在的不良反应并指导治疗开发。

Cytotoxicity refers to the capacity of a substance or agent to damage or kill living cells, reflecting a critical parameter in pharmacology, toxicology, and biomedicine. It is distinct from cytostatic effects, which inhibit cell growth and proliferation without causing cell death. Cytotoxic agents can induce a range of cellular responses, including inhibition of cell growth, induction of apoptotic or necrotic cell death, and disruption of metabolic or structural cellular integrity. Assessing cytotoxicity is fundamental for evaluating the safety and efficacy of pharmaceutical compounds, chemicals, and biomaterials, as it helps predict potential adverse effects and guides therapeutic development.

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Pharmacokinetics

Coliform index

大肠菌指数

大肠菌指数是根据粪便细菌计数对水纯度进行的评级。这是为确保足够的水质而进行的众多测试之一。大肠菌是主要起源于温血动物肠道的微生物。通过检测大肠菌群,尤其是众所周知的耐热大肠菌群,人们可以确定水是否可能受到粪便污染;即是否接触过人类或动物粪便。了解这一点很重要,因为许多致病微生物是从人类和动物粪便转移到水中的,人们可以从水中摄入并感染它们。被粪便污染的水通常含有致病细菌,可引起疾病。

The coliform index is a rating of the purity of water based on a count of fecal bacteria. It is one of many tests done to assure sufficient water quality. Coliform bacteria are microorganisms that primarily originate in the intestines of warm-blooded animals. By testing for coliforms, especially the well known Escherichia coli (E. coli), which is a thermotolerant coliform, one can determine if the water has possibly been exposed to fecal contamination; that is, whether it has come in contact with human or animal feces. It is important to know this because many disease-causing organisms are transferred from human and animal feces to water, from where they can be ingested by people and infect them. Water that has been contaminated by feces usually contains pathogenic bacteria, which can cause disease.

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