New pharmacokinetic methods: I. Estimation of mean serum concentration from trough serum concentration.

Abstract:

:An equation is derived to estimate mean steady state serum concentration (Css) from trough steady state serum concentration (Cmin) which can be used for drugs with either linear or nonlinear pharmacokinetic properties. In 15 subjects receiving phenytoin monotherapy, estimated Css did not differ significantly from measured Css, while Cmin differed significantly (P less than .0001) from measured Css and estimated Css. Clearance (CL) and elimination half-life (t1/2) values determined by stable isotope tracer methods or by standard equations and measured Css or estimated Css did not differ significantly, while CL and t1/2 values calculated with standard equations and Cmin differed significantly (P less than .02) from values obtained by any of the other three methods. We conclude: 1) Cmin values and CL and t1/2 values calculated with Cmin values may differ significantly from Css values and CL and t1/2 values calculated with Css; 2) accurate estimates of Css and of CL and t1/2 can be obtained using our procedure to correct a Cmin value to an estimated Css value.

journal_name

J Clin Pharmacol

authors

Browne TR,Greenblatt DJ,Szabo GK,Evans JE,Evans BA

doi

10.1002/j.1552-4604.1990.tb03612.x

subject

Has Abstract

pub_date

1990-06-01 00:00:00

pages

482-8

issue

6

eissn

0091-2700

issn

1552-4604

journal_volume

30

pub_type

杂志文章
  • Clonidine clearance matures rapidly during the early postnatal period: a population pharmacokinetic analysis in newborns with neonatal abstinence syndrome.

    abstract::The population pharmacokinetic (PK) profile of oral clonidine was characterized in newborns with neonatal abstinence syndrome, and significant covariates affecting its PK parameters were identified. Plasma clonidine concentration data were obtained from a clinical trial in which 36 newborns, aged 1 to 25 days (postnat...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1177/0091270010370587

    authors: Xie HG,Cao YJ,Gauda EB,Agthe AG,Hendrix CW,Lee H

    更新日期:2011-04-01 00:00:00

  • Model-Based Selection and Recommendation for Subcutaneous Abatacept Dose in Patients With Polyarticular Juvenile Idiopathic Arthritis.

    abstract::The selective T-cell costimulation modulator abatacept is approved for treatment of adult rheumatoid arthritis (RA) and polyarticular juvenile idiopathic arthritis (pJIA; 6-17 years [intravenous] and 2-17 years [subcutaneous]). An extrapolation approach was taken to determine subcutaneous weight-tiered doses of abatac...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/jcph.1797

    authors: Gandhi Y,Passarell JA,Roy A,Murthy B

    更新日期:2020-12-07 00:00:00

  • The recruitment of normal healthy volunteers: a review of the literature on the use of financial incentives.

    abstract::Unresolved issues of ethical, methodological, and legal concerns in the use of normal healthy volunteers persist. Financial incentives in their recruitment offer a unique ethical dilemma because of questions surrounding payment. A review of literature was conducted to obtain research systematically examining volunteer...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:

    authors: Tishler CL,Bartholomae S

    更新日期:2002-04-01 00:00:00

  • Pharmacokinetics, safety, and tolerability of the oral Renin inhibitor aliskiren in patients with hepatic impairment.

    abstract::Aliskiren is the first in a new class of orally active, direct renin inhibitors for the treatment of hypertension. This open-label, nonrandomized, single-center, parallel-group study compared the pharmacokinetics and safety of a single 300-mg oral dose of aliskiren in patients with mild, moderate, or severe hepatic im...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1177/0091270006294404

    authors: Vaidyanathan S,Warren V,Yeh C,Bizot MN,Dieterich HA,Dole WP

    更新日期:2007-02-01 00:00:00

  • Risk factors not addressed in antihypertensive therapy based solely on blood pressure control.

    abstract::There has been a considerable revolution in the field of hypertension therapy. We have gone through an era in which patients with severe hypertension and those with accelerated hypertension had a very short life expectancy. Currently blood pressure can be readily controlled with a marked improvement in longevity. We h...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1002/j.1552-4604.1993.tb03957.x

    authors: Somberg J,Ehrenpreis S,Shroff G,Khosla S

    更新日期:1993-03-01 00:00:00

  • Comparative pharmacokinetics and renal effects of cyclosporin A and cyclosporin G in renal allograft recipients.

    abstract::Cyclosporin G (CSG) has produced less nephrotoxicity than cyclosporin A (CSA) at equivalent doses in animal models. Conflicting results have been reported concerning differences in the pharmacokinetics of CSA and CSG in preclinical studies, and no data exist regarding the effect of steady-state oral administration of ...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,多中心研究,随机对照试验

    doi:10.1002/j.1552-4604.1997.tb04339.x

    authors: Gruber SA,Gallichio M,Rosano TG,Kaplan SS,Hughes SE,Urbauer DL,Singh TP,Lempert N,Conti DJ,Stein DS,Drusano G

    更新日期:1997-07-01 00:00:00

  • Effects of dimepramine fumarate on physiological and cognitive behaviors of Parkinson patients.

    abstract::Nine patients 55 to 74 years old with Parkinson's disease were tested before and after treatment with 50 to 225 mg dimepramine fumarate (CIBA G-31406) for about three weeks daily in order to determine the drug's effects on electrodermal responsiveness to a series of unpredictably occurring loud sounds. Twelve control ...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1979.tb01625.x

    authors: Oscar-Berman M,Gade A,Feldman RG,Saavedra MA

    更新日期:1979-10-01 00:00:00

  • Specific and pronounced impacts of lisinopril and lisinopril plus simvastatin on erythrocyte antioxidant enzymes.

    abstract::Angiotensin-converting enzyme inhibitors are effective at reducing blood pressure, whereas statins decrease plasma cholesterol impeding atherosclerosis. It is hypothesized that these medications may improve blood pressure and serum cholesterol by modifying the antioxidative status and energy metabolism of erythrocytes...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1177/0091270009344854

    authors: Kaminsky Y,Suslikov A,Kosenko E

    更新日期:2010-02-01 00:00:00

  • The effect of food on the oral bioavailability and the pharmacodynamic actions of the insulinotropic agent nateglinide in healthy subjects.

    abstract::Nateglinide (Starlix, SDZ DJN 608 or A-4166), a new insulinotropic agent, is intended to be administered prior to a meal in order to improve early insulin release in non-insulin-dependent diabetes mellitus patients. The effects of a meal on the oral bioavailability and pharmacodynamic actions of nateglinide were inves...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1177/00912709922007606

    authors: Karara AH,Dunning BE,McLeod JF

    更新日期:1999-02-01 00:00:00

  • A Mechanism-Based Pharmacokinetic/Pharmacodynamic Model for Bococizumab, a Humanized Monoclonal Antibody Against Proprotein Convertase Subtilisin/Kexin Type 9, and Its Application in Early Clinical Development.

    abstract::Bococizumab (RN316/PF-04950615), a humanized monoclonal antibody, binds to secreted proprotein convertase subtilisin/kexin type 9 (PCSK9) and prevents its downregulation of low-density lipoprotein receptor, leading to improved clearance and reduction of low-density lipoprotein cholesterol (LDL-C) in plasma. A mechanis...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/jcph.867

    authors: Udata C,Garzone PD,Gumbiner B,Joh T,Liang H,Liao KH,Williams JH,Meng X

    更新日期:2017-07-01 00:00:00

  • A Mechanism-Based Population Pharmacokinetics Model of Erythropoietin in Premature Infants and Healthy Adults Following Multiple Intravenous Doses.

    abstract::The objective of the current study was to develop a population pharmacokinetics (PK) model for erythropoietin (Epo) in premature infants and healthy adults to characterize the variation in PK, and to study the differences in Epo PK in these 2 populations. Thirteen very low-birth-weight premature infants (<1500 g at bi...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/jcph.1368

    authors: D'Cunha R,Widness JA,Yan X,Schmidt RL,Veng-Pedersen P,An G

    更新日期:2019-06-01 00:00:00

  • Multiple doses of sitagliptin, a selective DPP-4 inhibitor, do not meaningfully alter pharmacokinetics and pharmacodynamics of warfarin.

    abstract::Sitagliptin is an orally active, highly selective dipeptidyl peptidase IV (DPP-4) inhibitor for treatment of type 2 diabetes mellitus. This randomized, open-label, 2-part, 2-period crossover study assessed pharmacokinetics/pharmacodynamics of warfarin in the presence/absence of multiple-dose sitagliptin. Twelve partic...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1177/0091270009341653

    authors: Wright DH,Herman GA,Maes A,Liu Q,Johnson-Levonas AO,Wagner JA

    更新日期:2009-10-01 00:00:00

  • Cyclosporine and nonsteroidal antiinflammatory drugs: exploring potential drug interactions and their implications for the treatment of rheumatoid arthritis.

    abstract::A series of clinical pharmacology studies was performed to screen for possible pharmacokinetic/dynamic contributions to drug interactions reported in rheumatoid arthritis patients receiving cyclosporine and nonsteroidal antiinflammatory drugs (NSAIDs). No clinically relevant pharmacokinetic changes in any of the drugs...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/j.1552-4604.1997.tb04311.x

    authors: Kovarik JM,Mueller EA,Gerbeau C,Tarral A,Francheteau P,Guerret M

    更新日期:1997-04-01 00:00:00

  • Effect of probenecid on response to bumetanide in man.

    abstract::We administered 0.5-and 1.0-mg doses of bumetanide intravenously to eight normal subjects with and without pretreatment with probenecid. Probenecid did not effect either the cumulative response or the time course of response of bumetanide. These results are in contrast to results reported in dogs but consistent with s...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1981.tb01772.x

    authors: Brater DC,Chennavasin P

    更新日期:1981-07-01 00:00:00

  • When are bioavailability studies required? A German proposal.

    abstract::The Bundesinstitut für Arzneimittel und Medizinprodukte (BfArM), the German drug regulation authority, issued guidelines for determining whether bioavailability/bioequivalence studies are required for certain drugs. This decision tree is based on pharmacodynamic, pharmacokinetic, and physicochemical criteria. Details ...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1998.tb04385.x

    authors: Gleiter CH,Klotz U,Kuhlmann J,Blume H,Stanislaus F,Harder S,Paulus H,Poethko-Müller C,Holz-Slomczyk M

    更新日期:1998-10-01 00:00:00

  • Population pharmacokinetic analyses to evaluate the influence of intrinsic and extrinsic factors on exposure of prasugrel active metabolite in TRITON-TIMI 38.

    abstract::Serial pharmacokinetic (PK) sampling in 1159 patients from TRITON-TIMI 38 was undertaken. A multilinear regression model was used to quantitatively predict prasugrel's active metabolite (Pras-AM) concentrations from its 2 downstream inactive metabolites. Population-based methods were then applied to Pras-AM concentrat...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1177/0091270009337942

    authors: Wrishko RE,Ernest CS 2nd,Small DS,Li YG,Weerakkody GJ,Riesmeyer JR,Macias WL,Rohatagi S,Salazar DE,Antman EM,Wiviott SD,Braunwald E,Ni L

    更新日期:2009-08-01 00:00:00

  • An apomorphine-induced vomiting model for antiemetic studies in man.

    abstract::Apomorphine-induced vomiting is often used for preclinical efficacy testing of putative antiemetics in normal volunteers. The usual technique of individual intravenous titration for finding the threshold emitic dose of apomorphine in each subject is slow and tedious. We used a uniform dose of 0.05 mg/kg apomorphine gi...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1978.tb02427.x

    authors: Proctor JD,Chremos AN,Evans EF,Wasserman AJ

    更新日期:1978-02-01 00:00:00

  • Aminoglutethimide in the treatment of Cushing's syndrome.

    abstract::The efficacy and tolerability of aminoglutethimide for the treatment of Cushing's syndrome was assessed in 66 cases three of which are described in the present paper. Aminoglutethimide provided palliation from the signs and symptoms of hypercorticism in 13 of 21 patients with metastatic adrenocortical carcinoma and fo...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1976.tb01504.x

    authors: Misbin RI,Canary J,Willard D

    更新日期:1976-11-01 00:00:00

  • Short-term effects of beta blockers atenolol, nadolol, pindolol, and propranolol on lipoprotein metabolism in normolipemic subjects.

    abstract::The short-term effect of the blockade of the beta-adrenergic receptors on serum lipoproteins and the plasma activities of the enzymes involved in the metabolism of the serum lipoproteins: lipoprotein lipase (LPL), hepatic lipase (HL) and lecithin: cholesterol acyltransferase (LCAT) was evaluated in ten healthy normoli...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1987.tb03052.x

    authors: Harvengt C,Heller FR,Martiat P,Van Nieuwenhuyze Y

    更新日期:1987-07-01 00:00:00

  • Effect of high-dose aspirin on CYP2E1 activity in healthy subjects measured using chlorzoxazone as a probe.

    abstract::The authors evaluated the effect of high-dose aspirin at a therapeutic dose, using chlorzoxazone as a probe for CYP2E1 enzyme activity. In a randomized, open-label, 2-way crossover study, 10 healthy men were treated 3 times daily for 6 days with 1 g aspirin or placebo. On day 7, 1 dose of 400 mg chlorzoxazone was admi...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1177/0091270005282635

    authors: Park JY,Kim KA,Park PW,Ha JM

    更新日期:2006-01-01 00:00:00

  • Comparative bioavailability of a premixed, ready-to-use formulation of intravenous amiodarone with traditional admixture in healthy subjects.

    abstract::Intravenous amiodarone is an effective agent for the treatment of recurrent ventricular fibrillation and hemodynamically unstable ventricular tachycardia. PM101 Premixed Injection is a new formulation of intravenous amiodarone that uses a cyclodextrin to maintain amiodarone in the aqueous phase. Eighty-eight subjects ...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1177/0091270010395938

    authors: Cushing DJ,Adams MP,Cooper WD,Agha B,Souney PF

    更新日期:2012-02-01 00:00:00

  • The role of the clinical pharmacist in medical education.

    abstract::The clinical pharmacist is an integral member of the Docent team at the University of Missouri--Kansas City School of Medicine with duties in both teaching and patient care. These doctoral-level clinical pharmacists have sole responsibility for providing instruction in basic pharmacology and pharmacokinetics and for t...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1981.tb05700.x

    authors: Covinsky JO

    更新日期:1981-04-01 00:00:00

  • Analgesic effect of isoxepac on postmeniscectomy pain: a controlled trial.

    abstract::The analgesic efficacy of 100 and 200 mg isoxepac was compared with that of 50 mg indomethacin in a double-blind, single-dose, between-patient (parallel) study with placebo control. Oral doses were administered to 120 patients whose postoperative plan justified administration of analgesics on the morning of the day fo...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1002/j.1552-4604.1982.tb02653.x

    authors: Honig WJ,Pelgrom R,Chadha DR

    更新日期:1982-02-01 00:00:00

  • Patients treated with first-generation HCV protease inhibitors exhibit high ribavirin concentrations.

    abstract::Anemia is a well-known RBV-related event in HCV therapy which is exacerbated by the addition of telaprevir and boceprevir. This retrospective study evaluated and compared ribavirin exposure and parameters able to influence hemoglobin decrease in a large population of patients treated with dual or triple therapy. Patie...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/jcph.454

    authors: Bodeau S,Nguyen-Khac E,Solas C,Bennis Y,Capron D,Duverlie G,Brochot E

    更新日期:2015-05-01 00:00:00

  • Pharmacokinetics, safety, and pharmacologic effects of fosinopril sodium, an angiotensin-converting enzyme inhibitor in healthy subjects.

    abstract::The pharmacokinetics, pharmacodynamics, and safety of fosinopril sodium (SQ 28,555), a new orally active angiotensin-converting enzyme (ACE) inhibitor, was evaluated in 73 healthy men in two separate studies. In study I, doses ranging from 10 to 640 mg were administered once daily for 3 days to seven groups of five su...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1002/j.1552-4604.1991.tb01887.x

    authors: Duchin KL,Waclawski AP,Tu JI,Manning J,Frantz M,Willard DA

    更新日期:1991-01-01 00:00:00

  • Combined administration of quinidine and propafenone for atrial fibrillation: the CAQ-PAF study.

    abstract::Propafenone and its 5-hydroxy metabolite exhibit different electrophysiological properties. Objectives of the CAQ-PAF study were (1) to develop a strategy favoring propafenone instead of 5-hydroxypropafenone in plasma following oral administration of propafenone and (2) to evaluate the potential of low-dose quinidine ...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1177/0091270011399574

    authors: O'Hara GE,Philippon F,Gilbert M,Champagne J,Michaud V,Charbonneau L,Pruneau G,Hamelin BA,Geelen P,Turgeon J

    更新日期:2012-02-01 00:00:00

  • First-line therapy option with low-dose bisoprolol fumarate and low-dose hydrochlorothiazide in patients with stage I and stage II systemic hypertension.

    abstract::This 30-center, randomized, double-blind, placebo-controlled, parallel-group study was designed to (1) establish that 6.25 mg of hydrochlorothiazide (HCTZ) given once daily with 5 mg of bisoprolol fumarate can contribute to antihypertensive effectiveness in patients with stage I and stage II (mild to moderate) systemi...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,多中心研究,随机对照试验

    doi:10.1002/j.1552-4604.1995.tb05009.x

    authors: Frishman WH,Burris JF,Mroczek WJ,Weir MR,Alemayehu D,Simon JS,Chen SY,Bryzinski BS

    更新日期:1995-02-01 00:00:00

  • Diurnal variation in the pharmacokinetics of nizatidine in healthy volunteers and in patients with peptic ulcer disease.

    abstract::Six healthy volunteers and six patients with asymptomatic duodenal ulcer disease received placebo or 300 mg nizatidine once at night or twice daily (morning and evening) for a week in a random, cross-over fashion. Steady-state serum nizatidine concentrations and gastric pH were measured over a 24-hour period. No signi...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/j.1552-4604.1995.tb04029.x

    authors: Jamali F,Thomson AB,Kirdeikis P,Tavernini M,Zuk L,Marriage B,Simpson I,Mahachai V

    更新日期:1995-11-01 00:00:00

  • A Retrospective Review of the Efficiency of First-Dose Therapeutic Drug Monitoring of Gentamicin, Amikacin, and Vancomycin in the Pediatric Population.

    abstract::Therapeutic drug monitoring (TDM) has become standard clinical practice for gentamicin, amikacin, and vancomycin to optimize efficacy and reduce toxicity. TDM after the first dose of antibiotic was adopted in our institution. This study aims to evaluate if target therapeutic drug concentrations could be achieved more ...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/jcph.1509

    authors: Lim WXS,Chua WBB,Chua JM,Lee Q,Chan JW,Sultana R,Poh BH

    更新日期:2020-01-01 00:00:00

  • Comparative effects of dopaminergic agonists on cardiovascular, renal, and renin-angiotensin systems in hypertensive patients.

    abstract::The role of dopaminergic receptors on renal function has been extensively studied. Recently dopaminergic receptor has been classified in two subtypes D1 and D2, which seem to have different modulatory function. However, the role of dopaminergic receptors on cardiovascular function and more specifically the potential r...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1002/j.1552-4604.1992.tb03788.x

    authors: Luchsinger A,Velasco M,Urbina A,Morillo J,Romero E,Alvarez R,Pieretti OH

    更新日期:1992-01-01 00:00:00