Abstract：
:The hypolipidaemic agent pravastatin differs from other US Food and Drug Administration (FDA)-approved HMG-CoA reductase inhibitors (e.g. lovastatin and simvastatin) because it has greater hydrophilicity, as a result of the hydroxyl group attached to its decalin ring. The hydrophilic nature of pravastatin accounts for its minimal penetration into the intracellular space of nonhepatic tissues, including an apparent inability to cross the blood-brain barrier. The drug is also well tolerated because it is rapidly absorbed and excreted, and does not accumulate in plasma even with repeated administration. Pravastatin is taken up into the liver by an active transport carrier system, and the hepatic extraction ratio is high (0.66). The drug and its metabolites are cleared through both hepatic and renal routes (53 and 47%, respectively). The dual route of elimination reduces the need for dosage adjustment if the function of either of these organs is impaired. Dosage adjustments are also not required on the basis of age or gender. Furthermore, the drug can be given without regard to food intake, an important consideration for compliance since lipid-lowering therapy is generally required long term. The drug is approximately 50% protein bound, and, therefore, compared with other members of its class the tendency for displacement of highly protein bound drugs such as warfarin is decreased. This minimal potential for drug-drug interactions is important for patients who are taking multiple drugs because of concomitant medical problems. However, as with any HMG-CoA reductase inhibitor, caution should be exercised when pravastatin is given with nicotinic acid (niacin), gemfibrozil or cyclosporin, because of increased risk for myopathy in patients receiving combination therapy.
journal_name
Clin Pharmacokinetjournal_title
Clinical pharmacokineticsauthors
Quion JA,Jones PHdoi
10.2165/00003088-199427020-00002subject
Has Abstractpub_date
1994-08-01 00:00:00pages
94-103issue
2eissn
0312-5963issn
1179-1926journal_volume
27pub_type
杂志文章,评审abstract：:20 routine patients with endogenous depression were investigated in a kinetic and 4 week treatment study. Steady-state plasma nortriptyline concentrations above 200 microgram/L were associated with a highly significant poorer therapeutic outcome. The correlations between the 24, 48 and 72 hour concentrations and stead...
journal_title：Clinical pharmacokinetics
pub_type： 临床试验,杂志文章
doi：10.2165/00003088-197904020-00005
更新日期：1979-03-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Iron-rich transfusions and/or a compensatory increase in iron absorption ultimately result in iron loading in patients with β-thalassaemia. Hence, without iron chelation, iron accumulates relentlessly. Deferiprone has been shown to be capable of reducing the iron burden in patients with β-thala...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/11536630-000000000-00000
更新日期：2011-01-01 00:00:00
abstract：:Part I of this article, which appeared in the previous issue of the Journal, covered the following agents: histamine H2-receptor antagonists (cimetidine, ranitidine, famotidine, nizatidine); muscarinic-M1-receptor antagonists (pirenzepine); proton pump inhibitors (omeprazole); site-protective agents (colloidal bismuth...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199019020-00002
更新日期：1990-08-01 00:00:00
abstract：:The effects of liver disease on pharmacokinetics and pharmacodynamics are highly variable, and difficult to predict as the mechanisms of these effects are not well understood. Since the majority of the published literature is concerned with cirrhotic liver disease, this review also focuses mainly on this area. Four di...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199529050-00005
更新日期：1995-11-01 00:00:00
abstract：:Ertugliflozin, a selective inhibitor of sodium-glucose cotransporter 2 (SGLT2), is approved in the US, EU, and other regions for the treatment of adults with type 2 diabetes mellitus (T2DM). This review summarizes the ertugliflozin pharmacokinetic (PK) and pharmacodynamic data obtained during phase I clinical developm...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s40262-020-00875-1
更新日期：2020-08-01 00:00:00
abstract：:Dorzolamide is a carbonic anhydrase inhibitor for topical ophthalmic application. It is used in the treatment of glaucoma to lower the intraocular pressure. After absorption via the cornea and stroma, it inhibits carbonic anhydrase in the ciliary process, which leads to a reduction of aqueous humour production and the...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200241030-00004
更新日期：2002-01-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:NXY-059 (disufenton sodium, Cerovive, a nitrone with neuroprotective and free radical trapping properties (in experimental stroke) is under development for the treatment of acute stroke. The objectives of this study were to develop a population pharmacokinetic model for NXY-059 in acute stroke...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,多中心研究,随机对照试验
doi：10.2165/00003088-200544080-00007
更新日期：2005-01-01 00:00:00
abstract：:Ethnic or racial differences in pharmacokinetics and pharmacodynamics have been attributed to the distinctions in the genetic, physiological and pathological factors between ethnic/racial groups. These pharmacokinetic/pharmacodynamic differences are also known to be influenced by several extrinsic factors such as soci...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200645100-00001
更新日期：2006-01-01 00:00:00
abstract：BACKGROUND:Lorazepam is one of the preferred agents used for intravenous treatment of status epilepticus (SE). We combined data from two pediatric clinical trials to characterize the population pharmacokinetics of intravenous lorazepam in infants and children aged 3 months to 17 years with active SE or a history of SE....
journal_title：Clinical pharmacokinetics
pub_type： 临床试验,杂志文章,多中心研究,随机对照试验
doi：10.1007/s40262-016-0486-0
更新日期：2017-08-01 00:00:00
abstract：:The effects of diabetes mellitus on the pharmacokinetics and pharmacodynamics of drugs have been well described in experimental animal models; however, only minimal data exist for humans and the current knowledge regarding the effects of diabetes on these properties remains unclear. Nevertheless, it has been observed ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/11631900-000000000-00000
更新日期：2012-08-01 00:00:00
abstract：:The pharmacokinetic effect of extracorporeal elimination can be evaluated from the extracorporeal elimination rate constant, from the amount of drug removed, and from extracorporeal clearance. To compare the validity of these approaches in clinical practice, the effect of multiple plasma exchanges on the steady-state ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-198510060-00004
更新日期：1985-11-01 00:00:00
abstract：:To investigate the influence of the presence of oedema on the pharmacokinetics and pharmacodynamics of furosemide (frusemide) we selected 9 hospitalised patients (mean age 70.3 years, range 59 to 84 years) with severe congestive heart failure (NYHA III to IV) and an assessed amount of peripheral oedema of at least 5 k...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-199222040-00006
更新日期：1992-04-01 00:00:00
abstract：:Although individualised antihypertensive therapy is widely recommended, prospective methods for optimising treatment are hampered by the paucity of basic information about dose-plasma concentration-response relationships for commonly used drugs. Concentration-effect analysis has been applied to a number of therapeutic...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199426060-00005
更新日期：1994-06-01 00:00:00
abstract：:Histamine H2-receptor antagonists are a unique class of compounds. Pharmacologically they are characterised as a family by their ability to inhibit the secretion of gastric acid, and kinetically they are classified as a family by their similarity in absorption, distribution and elimination. All the H2-receptor antagon...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199120030-00004
更新日期：1991-03-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:The aim of this study was to investigate the pharmacokinetics, safety, and tolerability of riociguat after single and multiple oral doses of 1 or 2 mg three times daily (tid), and to determine the effect of smoking on riociguat pharmacokinetics in Chinese men. METHODS:In a randomized, double-...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,随机对照试验
doi：10.1007/s40262-015-0337-4
更新日期：2016-05-01 00:00:00
abstract：:According to recent clinical consensus, pharmacotherapy of inflammatory bowel disease (IBD) is, or should be, personalized medicine. IBD treatment is complex, with highly different treatment classes and relatively few data on treatment strategy. Although thorough evidence-based international IBD guidelines currently e...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s40262-018-0639-4
更新日期：2018-09-01 00:00:00
abstract：:Necitumumab is a second-generation, recombinant, human immunoglobulin G1, epidermal growth factor (EGFR) receptor antibody that specifically blocks the ligand binding site of EGFR. Necitumumab potentially acts by blocking ligand epidermal growth factor (EGF) binding-mediated activation of the EGFR signaling pathway, i...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-016-0452-x
更新日期：2017-05-01 00:00:00
abstract：:Direct-acting antivirals (DAAs) are known victims (substrate) and perpetrators (cause) of drug-drug interactions (DDIs). These DAAs are used for the treatment of hepatitis C virus (HCV) infections and are highly effective drugs. Drugs used for cardiovascular risk management are frequently used by HCV-infected patients...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s40262-018-0710-1
更新日期：2019-05-01 00:00:00
abstract：:The ability to deliver safe and effective moderate sedation is crucial to the ability to perform invasive procedures. Sedative drugs should have a quick onset of action, provide rapid and clear-headed recovery, and be easy to administer and monitor. A number of drugs have been demonstrated to provide effective sedatio...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200645090-00001
更新日期：2006-01-01 00:00:00
abstract：:A change in drug clearance with age is considered an important factor in determining the high prevalence of adverse drug reactions associated with prescribing medications for the elderly. Despite this, no general principles have been available to guide drug administration in the elderly, although a substantial body of...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-199834050-00003
更新日期：1998-05-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Daclatasvir is a potent, pangenotypic once-daily hepatitis C virus (HCV) NS5A inhibitor that is approved for the treatment of chronic HCV infection. The objective of this analysis was to characterize the pharmacokinetics of daclatasvir in subjects with chronic HCV infection. METHODS:A populati...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-016-0504-2
更新日期：2017-10-01 00:00:00
abstract：BACKGROUND:The imatinib trough plasma concentration (C(min)) correlates with clinical response in cancer patients. Therapeutic drug monitoring (TDM) of plasma C(min) is therefore suggested. In practice, however, blood sampling for TDM is often not performed at trough. The corresponding measurement is thus only remotely...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/11596990-000000000-00000
更新日期：2012-03-01 00:00:00
abstract：:Vedolizumab is a humanized anti-α4β7 integrin monoclonal antibody that selectively blocks trafficking of memory T cells to inflamed gut tissue by inhibiting the α4β7-mucosal addressin cell adhesion molecule-1 (MAdCAM-1) interaction. Approved for treating patients with moderately to severely active ulcerative colitis (...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s40262-017-0546-0
更新日期：2017-11-01 00:00:00
abstract：:Clarithromycin is a semisynthetic macrolide antibiotic, structurally related to erythromycin. It has a more favourable pharmacokinetic profile than erythromycin, thus allowing twice-daily administration and possibly increasing compliance among outpatients. Clarithromycin is well absorbed from the gastrointestinal trac...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199325030-00003
更新日期：1993-09-01 00:00:00
abstract：:Drug-drug, drug-formulation and drug-meal interactions are of clinical concern for orally administered drugs that possess a narrow therapeutic index. This review presents the current status of information regarding interactions which may influence the gastrointestinal (GI) absorption of orally administered drugs. Abso...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199936030-00004
更新日期：1999-03-01 00:00:00
abstract：BACKGROUND:Entecavir is an orally administered guanosine nucleoside analog with activity against hepatitis B virus (HBV) polymerase, which is approved for the treatment of chronic hepatitis B (CHB) infection in adults and children ≥2 years old (USA and EU). OBJECTIVE:To develop simplified entecavir dosing recommendati...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-016-0420-5
更新日期：2016-12-01 00:00:00
abstract：:Obesity is associated with physiological changes that can alter the pharmacokinetic parameters of many drugs. Vancomycin and the aminoglycosides are the only antibacterials that have been extensively investigated in the obese population. The apparent volume of distribution (Vd) and total body clearance of vancomycin a...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200038050-00003
更新日期：2000-05-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Tesamorelin is a synthetic analogue of growth hormone-releasing factor (GRF), which increases basal and pulsatile growth hormone (GH) secretion and subsequently increases insulin-like growth factor (IGF)-1. Limited information is available about the pharmacokinetics of this compound. Consequen...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,随机对照试验
doi：10.1007/s40262-014-0202-x
更新日期：2015-03-01 00:00:00
abstract：:Vemurafenib is an orally administered small-molecule inhibitor of the oncogenic BRAF kinase that is indicated for the treatment of patients with unresectable or metastatic melanoma harbouring BRAF V600 mutations. Vemurafenib is absorbed rapidly after a single oral dose of 960 mg, reaching maximum drug concentration ap...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s40262-017-0523-7
更新日期：2017-09-01 00:00:00
abstract：:Aminoglycosides are important antibacterial agents for the treatment of serious infection. Evidence suggests that high peak plasma concentrations must be achieved early in the course of treatment if these agents are to be effective, but prolonged high concentrations may cause ototoxicity and nephrotoxicity. Peak plasm...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199427010-00004
更新日期：1994-07-01 00:00:00
