Abstract：
:Pharmacokinetics is a relatively young branch of the life sciences, which has developed rapidly in the last 15-20 years, thanks to a series of analytical achievements that have allowed drug concentrations to be measured in biological matrices with highly selective and sensitive methods. Most old drugs and all new drugs have been investigated in depth to determine their absorption, distribution, metabolism and elimination. This has produced a huge body of data which have characterized drugs through so-called fingerprint parameters. Today, pharmacokinetics plays a vital role throughout drug development from initial non-clinical studies to clinical trials. In new drug development, simultaneous efforts in pharmacodynamic and pharmacokinetic studies have produced a high degree of synergy, the most useful expression of which is the identification of a therapeutic window, where this can be achieved. Dose linearity/proportionality, gender effect, metabolism and possible polymorphism, studies on neonates/children and on elderly and diseased patients and the population approach, relative and absolute bioavailability, possible interactions and the possible presence of a deep compartment in the distribution are other important applications of pharmacokinetics. Major new developments in pharmaceutical technology which have produced controlled-release delivery systems and the market introduction of generics would never have occurred but for the active contribution of pharmacokinetics. This review is devoted to the investigations needed to prepare appropriate pharmacokinetic registration files for new drug applications (NDAs) and abbreviated or abridged new drug applications (ANDAs) required for generic drugs. Scientific literature, operating guidelines and personal experience are the basis of this review, which describes a number of relevant examples in several specific areas.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Marzo Adoi
10.1006/phrs.1997.0254subject
Has Abstractpub_date
1997-12-01 00:00:00pages
425-50issue
6eissn
1043-6618issn
1096-1186pii
S1043-6618(97)90254-1journal_volume
36pub_type
杂志文章,评审abstract：:Heart rate recovery at 1min (HRR1) is a strong predictor of all-cause mortality. The effects of statins on the autonomic nervous system may account for their beneficial effects in survival. Our aim was to determine if statin therapy improves heart rate recovery in hypercholesterolemic patients with type 2 diabetes mel...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2006.09.002
更新日期：2006-12-01 00:00:00
abstract：:Aminoglycoside antibiotics are employed clinically because of their potent bactericidal activities, less bacterial resistance, post-antibiotic effects and low cost. However, drugs belong to this class are well-known to cause nephrotoxicity, which limits their frequent clinical exploitation. Gentamicin, a commonly used...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2010.04.004
更新日期：2010-09-01 00:00:00
abstract：:Erdosteine was introduced in the market as a mucolytic agent for chronic pulmonary diseases more than 10 years ago. The drug contains two blocked sulphydryl groups one of which, after hepatic metabolization and opening of the thiolactone ring, becomes available both for the mucolytic and free radical scavenging and an...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2006.12.006
更新日期：2007-04-01 00:00:00
abstract：:Though the AMPA receptor has been implicated in several neurodegenerative processes (epilepsy, ischemia, spasticity), its role in cognition is yet to be clarified. The aim of this study was to assess in the rat the effects of the AMPA receptor antagonist NBQX (3.5, 7, 10, 20 and 30 mgkg(-1), i.p.) on learning and memo...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0898
更新日期：2002-01-01 00:00:00
abstract：:Epidemiological studies support an inverse correlation between HDL-C and cardiovascular disease. However, low HDL-C levels do not always segregate with premature disease. These include, LCAT deficiency and the apolipoproteinA-IMilano (AIM) variant. AIM has a cysteine for arginine at position 173 in the otherwise cyste...
journal_title：Pharmacological research
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.phrs.2016.05.001
更新日期：2016-09-01 00:00:00
abstract：:Diabetes is a chronic metabolic disease characterized by hyperglycemia and several associated biochemical abnormalities. Diabetes leads to multiorgan complications that collectively reduce life expectancy. Hematopoietic stem cells (HSCs) are nested within bone marrow (BM) niches whence they can be mobilized to the per...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2018.07.017
更新日期：2018-09-01 00:00:00
abstract：:Advanced glycation end products (AGEs) and their receptor (RAGE) axis contributes to diabetic nephropathy. An oral hypoglycemic agent, metformin may have a potential effect on the inhibition of glycation reactions. Further, since a pathophysiological crosstalk between renin-angiotensin system (RAS) and AGEs-RAGE axis ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2011.11.001
更新日期：2012-03-01 00:00:00
abstract：:Panax notoginseng (Burkill) F. H. Chen ex C. H. Chow (P. notoginseng) is a highly valued Chinese materia medica having a hemostatic effect and mainly used for the treatment of trauma and ischemic cardiovascular diseases. Stringent growth requirements, weak resistance to insect pests and plant diseases, arsenic contami...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2018.05.005
更新日期：2018-08-01 00:00:00
abstract：:Epidemiological studies suggest that diets with a high intake of vegetables and fruits may reduce the incidence of degenerative disorders including Alzheimer's disease. Berries are some of the popular fruits consumed worldwide. They are considered to be rich in anthocyanin pigments, a group belonging to the flavonoids...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2005.07.003
更新日期：2005-12-01 00:00:00
abstract：:Respiratory fluoroquinolones are currently considered by several guidelines among the most effective antimicrobial agents for the treatment of acute bacterial rhinosinusitis. The aim of this study was to assess levofloxacin penetration into paranasal sinuses mucosa of 15 patients with chronic rhinosinusitis 1h (n = 4)...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2006.10.003
更新日期：2007-01-01 00:00:00
abstract：:Cells continuously turn over proteins through cycles of synthesis and degradation in order to maintain a functional proteome and to exert a tight control in the levels of regulatory proteins. Selective degradation of proteins was initially thought to be an exclusive function of the ubiquitin-proteasome system, however...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2012.10.002
更新日期：2012-12-01 00:00:00
abstract：:We previously demonstrated that the typical mitochondrial uncoupler carbonyl cyanide m-chlorophenylhydrazone (CCCP) inhibited artery constriction, but CCCP was used only as a pharmacological tool. Niclosamide is an anthelmintic drug approved by FDA. Niclosamide ethanolamine (NEN) is a salt form of niclosamide and has ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.11.008
更新日期：2017-01-01 00:00:00
abstract：:Fecal microbiota transplant (FMT) has seen a historic emergence in last decade with its sojourn recently entering into a chequered path, due to a few reports of infection and subsequent mortality. Though FMT has been extensively reported, there is no comprehensive report on the delivery routes available for this non-p...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.104954
更新日期：2020-09-01 00:00:00
abstract：:Ozone has been used as a therapeutical agent and beneficial effects have been observed. However so far only a few biochemical and pharmacodynamic mechanisms have been elucidated. We demonstrate that controlled ozone administration may promote an oxidative preconditioning or adaptation to oxidative stress, preventing t...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0867
更新日期：2001-11-01 00:00:00
abstract：:Gamma-vinyl GABA (vigabatrin; VGB), an irreversible inhibitor of GABA-transaminase, was evaluated for its effect on the contractile responses to PGE(2) or its precursor arachidonic acid (AA) in guinea pig ileum (GPI) and non-pregnant rat uterus. Rationale behind this study was the rise in gamma-aminobutyric acid (GABA...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(03)00045-8
更新日期：2003-06-01 00:00:00
abstract：:Levosulpiride is the (-)-enantiomer of sulpiride. It has shown greater central antidopaminergic activity, antiemetic and antidyspeptic effects and lower acute toxicity than both the racemic and dextro forms. Several clinical studies indicate that levosulpiride has therapeutic efficacy in depressive and somatoform diso...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/1043-6618(95)80053-0
更新日期：1995-02-01 00:00:00
abstract：:The aim of this study was to investigate the effects of manganese chloride on gentamicin-induced nephrotoxicity in rats. Thirty-six adult Wistar Albino rats were divided into six equal groups. They were injected with gentamicin sulfate (100 mg kg(-1) per day i.p.) and manganese chloride (2 or 20 mg kg(-1) per day i.p....
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(03)00227-5
更新日期：2003-12-01 00:00:00
abstract：:Green tea (Camellia sinensis, Theaceace) is the second most popular beverage in the world and has been extensively studied for its putative disease preventive effects. Green tea is characterized by the presence of a high concentrations of polyphenolic compounds known as catechins, with (-)-epigallocatechin-3-gallate (...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2010.12.013
更新日期：2011-08-01 00:00:00
abstract：:Electrophysiological effects of bisaramil--a new antiarrhythmic drug under clinical trial--were investigated on isolated heart preparations, at a concentration range of 2.3-23 x 10(-6) M. Bisaramil dose dependently decreased the maximum rate of depolarization (Vmax), action potential amplitude (APA) and overshoot (OS)...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(05)80066-0
更新日期：1992-01-01 00:00:00
abstract：:The ataxin-2 binding protein 1 (A2BP1) gene is reported to be one of the susceptibility genes in schizophrenia, autism, and obesity. The aim of this study was to explore the association of A2BP1 gene polymorphisms with antipsychotic induced weight gain (AIWG) in Chinese Han population. Three hundred and twenty-eight p...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2015.06.003
更新日期：2015-09-01 00:00:00
abstract：:The blood-brain barrier (BBB) keeps the central nervous system (CNS) safe from various brain diseases, while the BBB makes it difficult for effective drugs to enter the CNS. Mfsd2a is specifically expressed on the cell membrane of brain-microvascular endothelial cell (BMEC) and is implicated in the delivery of some su...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2015.12.024
更新日期：2016-02-01 00:00:00
abstract：:In China, child and adolescent pediatricians often face challenges in treating children with the appropriate medications. Within the last 8 years, the Chinese government has already initiated a series of policies to promote development of age-appropriate medicines for children. In this study,we introduced the current ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.104412
更新日期：2019-10-01 00:00:00
abstract：:The first studies of histamine and diabetes date back to the 1950s. Since that time the involvement of histamine in diabetes was related to its well known vasoactive properties and permeability leakage effects. In particular, the first evidence for a correlation between histamine and diabetes arose in 1989 when an inc...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.06.021
更新日期：2016-09-01 00:00:00
abstract：:Curcumin, a bioactive polyphenol, is a yellow pigment of the Curcuma longa (turmeric) plant. Curcumin has many pharmacologic effects including antioxidant, anti-carcinogenic, anti-obesity, anti-angiogenic and anti-inflammatory properties. Recently, it has been found that curcumin affects lipid metabolism, and subseque...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.02.008
更新日期：2017-05-01 00:00:00
abstract：:Hydrogen sulfide (H2S) is an endogenously produced signaling molecule synthesized by cystathionine γ-lyase (CSE), cystathionine β-synthase (CBS) and 3-mercaptopyruvate sulfurtransferase (3-MST). Given that H2S exerts significant effects on bioenergetics and metabolism, the goal of the current study was to determine th...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2017.09.023
更新日期：2018-02-01 00:00:00
abstract：:Because many Ca2+ channel blocking agents are known to cause adverse systemic effects, in this study we tested the haemodynamic side effects of nimodipine with and without a mild hypoxic-ischaemic (HI) insult in a newborn piglet model. Fifteen min after completing a brief period of asphyxia we gave i.v. nimodipine as ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1996.0002
更新日期：1996-01-01 00:00:00
abstract：:Carbon-based nanomaterials have unique physicochemical properties relevant to the diagnosis and treatment of various diseases. There have been many reports indicating that carbon nanomaterials (CNMs) can interact and perturb biomolecules such as proteins and amyloid structures. This review is an attempt to reflect the...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.03.023
更新日期：2019-05-01 00:00:00
abstract：:Effect of moclobemide, a selective monoamine oxidase-type A enzyme inhibitor, was investigated on the body temperature of male mice. Moclobemide (15-30 mg kg(-1), i.p.) produced significant reductions of body temperature in both normal and yeast-induced hyperthermic male mice. The hypothermic effect of moclobemide was...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(03)00108-7
更新日期：2003-09-01 00:00:00
abstract：:In this study, we have addressed the pharmacogenomic basis of the response of gastrointestinal tumors to six anticancer drugs using a panel of fifteen cell lines derived from pancreatic, stomach and biliary tract cancers. We determined the constitutive expression levels of 96 genes, whose encoded proteins contribute t...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.09.007
更新日期：2016-11-01 00:00:00
abstract：:Autism-spectrum disorder (ASD) is a neurodevelopmental disorder characterized by persistent deficits in social communication and repetitive patterns of behavior. ASD is, however, often associated with medical comorbidities and gastrointestinal (GI) dysfunction is among the most common. Studies have demonstrated a corr...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2018.03.020
更新日期：2018-06-01 00:00:00
