The monoamine oxidase type B inhibitor rasagiline in the treatment of Parkinson disease: is tyramine a challenge?

Abstract:

:Rasagiline is an irreversible monoamine oxidase type B (MAO-B) inhibitor indicated for the treatment of the signs and symptoms of idiopathic Parkinson disease as initial monotherapy and as adjunct therapy to levodopa. Pharmacologic inhibition of monoamine oxidase type A (MAO-A), but not MAO-B, poses a risk of the "cheese effect," a hypertensive response to excess dietary tyramine, a biogenic sympathomimetic amine. Tyramine challenge studies, conducted to characterize rasagiline selectivity for the MAO-B enzyme and tyramine sensitivity, demonstrate that rasagiline, when used at the recommended dose, is selective for MAO-B and is not associated with heightened tyramine sensitivity. This conclusion is also supported by safety results from large clinical trials of rasagiline in Parkinson disease involving 2066 rasagiline-treated patients who did not require dietary tyramine restriction per protocol. In late 2009, US labeling for rasagiline was modified to state that dietary tyramine restrictions are not ordinarily required when rasagiline is administered at recommended doses. In addition, because rasagiline has been demonstrated to be selective for MAO-B at the approved dose of up to 1 mg/d, contraindications regarding concomitant use with sympathomimetic amines, use of sympathomimetic vasopressors in conjunction with general or local anesthesia, and use in patients with pheochromocytoma also were removed.

journal_name

J Clin Pharmacol

authors

Chen JJ,Wilkinson JR

doi

10.1177/0091270011406279

subject

Has Abstract

pub_date

2012-05-01 00:00:00

pages

620-8

issue

5

eissn

0091-2700

issn

1552-4604

pii

0091270011406279

journal_volume

52

pub_type

杂志文章,评审
  • Effects of acid-reducing agents on the pharmacokinetics of lopinavir/ritonavir and ritonavir-boosted atazanavir.

    abstract::A total of 71 HIV-negative healthy adults were randomized to 1 of 6 regimens to receive lopinavir/ritonavir tablets 400/100 mg twice daily (bid) or 800/200 mg once daily (qd) or atazanavir 300 mg + ritonavir 100 mg qd from study days 1 to 15 with a moderate-fat meal. One hour before breakfast, either omeprazole 40 mg ...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1177/0091270007313392

    authors: Klein CE,Chiu YL,Cai Y,Beck K,King KR,Causemaker SJ,Doan T,Esslinger HU,Podsadecki TJ,Hanna GJ

    更新日期:2008-05-01 00:00:00

  • Efficacy and safety of ketoprofen patch in patients with rheumatoid arthritis: a randomized, double-blind, placebo-controlled study.

    abstract::This study assessed the efficacy and safety of ketoprofen patch compared with placebo in patients who had rheumatoid arthritis and persistent wrist pain. Patients (N = 676)who had achieved systemic disease control with a disease-modifying antirheumatic drug and/or systemic corticosteroid, but still had persistent wris...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1177/0091270009355813

    authors: Kawai S,Uchida E,Kondo M,Ohno S,Obata J,Nawata Y,Sugimoto K,Oribe M,Nagaya I

    更新日期:2010-10-01 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

  • Artemisia Extract Improves Insulin Sensitivity in Women With Gestational Diabetes Mellitus by Up-Regulating Adiponectin.

    abstract::Gestational diabetes mellitus (GDM) has affected a great number of pregnant women worldwide. Artemisia extracts have been found to exhibit a potent antidiabetic effect in the treatment of type 2 diabetes mellitus. We aimed to examine the effects of Artemisia extract on insulin resistance and lipid profiles in pregnant...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1002/jcph.755

    authors: Sun X,Sun H,Zhang J,Ji X

    更新日期:2016-12-01 00:00:00

  • Effects of atorvastatin, an HMG-CoA reductase inhibitor, on hepatic oxidative metabolism of antipyrine.

    abstract::Possible effects of multiple-dose administration of atorvastatin on the pharmacokinetics of single-dose antipyrine were evaluated in this drug-drug interaction study. Twelve healthy male volunteers received three 200-mg capsules of antipyrine on days 1 and 22, and two 40-mg atorvastatin tablets in the morning on days ...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1996.tb04212.x

    authors: Yang BB,Hounslow NJ,Sedman AJ,Forgue ST

    更新日期:1996-04-01 00:00:00

  • A review of potential cardiovascular uses of intravenous glucagon administration.

    abstract::Glucagon is a counter-regulatory hormone that is classically used to treat hypoglycemia. However, it can elicit the generation of cAMP within the myocardium to cause positive inotropic and chronotropic effects without the need for beta-1 adrenoceptor stimulation. Glucagon has been used extensively to treat beta-blocke...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:

    authors: White CM

    更新日期:1999-05-01 00:00:00

  • Population Pharmacokinetics of Adjunctive Lacosamide in Pediatric Patients With Epilepsy.

    abstract::A pediatric population pharmacokinetic model including covariate effects was developed using data from 2 clinical trials in pediatric patients with epilepsy (SP0847 and SP1047). Lacosamide plasma concentration-time data (n = 402) were available from 79 children with body weights ranging from 6 to 76 kg, and a balanced...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/jcph.1340

    authors: Winkler J,Schoemaker R,Stockis A

    更新日期:2019-04-01 00:00:00

  • Dose proportionality and the effect of food on vildagliptin, a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers.

    abstract::Vildagliptin is a potent and selective dipeptidyl peptidase IV inhibitor in development for the treatment of type 2 diabetes that improves glycemic control by enhancing alpha- and beta-cell responsiveness to glucose. Two open-label, single-dose, randomized, crossover studies in healthy subjects (ages 18-45 years) inve...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1177/0091270007304313

    authors: Sunkara G,Sabo R,Wang Y,He YL,Campestrini J,Rosenberg M,Howard D,Dole WP

    更新日期:2007-09-01 00:00:00

  • Pharmacokinetics and acute safety of inhaled testosterone in postmenopausal women.

    abstract::This was a preliminary feasibility study to assess the pharmacokinetics and acute safety of a single dose of orally inhaled testosterone via the AERx system, a novel handheld aerosol delivery system in postmenopausal women. Twelve postmenopausal women stabilized on oral estrogen therapy were treated with a single dose...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1177/0091270004269840

    authors: Davison S,Thipphawong J,Blanchard J,Liu K,Morishige R,Gonda I,Okikawa J,Adams J,Evans A,Otulana B,Davis S

    更新日期:2005-02-01 00:00:00

  • CYP2C19 genotype is a major factor contributing to the highly variable pharmacokinetics of voriconazole.

    abstract::In vitro data on the metabolism of the antifungal voriconazole suggest that its pharmacokinetics might be influenced by the activity of CYP2C19, CYP2C9, and CYP3A. To elucidate the genetic influence of polymorphic enzymes on voriconazole metabolism, the authors pooled the pharmacokinetic data from 2 interaction studie...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1177/0091270008327537

    authors: Weiss J,Ten Hoevel MM,Burhenne J,Walter-Sack I,Hoffmann MM,Rengelshausen J,Haefeli WE,Mikus G

    更新日期:2009-02-01 00:00:00

  • Pharmacokinetics of dexketoprofen trometamol in healthy volunteers after single and repeated oral doses.

    abstract::The pharmacokinetics of dexketoprofen trometamol were evaluated in two studies using healthy volunteers. In the first study, the relative bioavailability of a single oral capsule of dexketoprofen free acid 25 mg or dexketoprofen trometamol 25 mg (given as 37 mg of the trometamol salt) was compared to ketoprofen 50 mg ...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:

    authors: Barbanoj MJ,Gich I,Artigas R,Tost D,Moros C,Antonijoan RM,García ML,Mauleón D

    更新日期:1998-12-01 00:00:00

  • The Clinical Pharmacology Consultation Service: results of a physician survey before and after implementation.

    abstract::A total of 175 physicians were surveyed by questionnaire before a Clinical Pharmacology Consult Service was started. Of those that responded, 72% thought the service would be helpful, although 40% said they would use the service no more than once a month. Most physicians (75%) preferred self-initiated consultations to...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1988.tb03096.x

    authors: Casner PR,Dillon KR

    更新日期:1988-01-01 00:00:00

  • Renin inhibition: a new approach to cardiovascular therapy.

    abstract::The renin-angiotensin system (RAS) functions as a primary regulator in the short-term and long-term control of blood pressure. Pharmacologic inhibition of the RAS with angiotensin-converting enzyme (ACE) inhibition is effective for treating systemic hypertension and congestive heart failure. As a more specific therapy...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1002/j.1552-4604.1994.tb04000.x

    authors: Frishman WH,Fozailoff A,Lin C,Dike C

    更新日期:1994-09-01 00:00:00

  • Calcium channel blockade in experimental aminoglycoside nephrotoxicity.

    abstract::Calcium channel blocker therapy has proved protective in certain models of ischemic-induced acute renal failure. This effect may be related to the prevention of calcium influx into injured cells or by the vasodilatory effects of verapamil that may result in an improvement in renal blood flow. In the current study, the...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1987.tb03076.x

    authors: Watson AJ,Gimenez LF,Klassen DK,Stout RL,Whelton A

    更新日期:1987-08-01 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

  • Effect of meals on the kinetics of etretinate.

    abstract::Eight healthy men received 100 mg oral doses of etretinate separated by two-week washout periods in an open, randomized, crossover study. Etretinate was administered during a complete fast, with a standard high fat breakfast, a standard high carbohydrate breakfast, and 16 ounces of whole milk. Plasma samples were obta...

    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.1552-4604.1985.tb02881.x

    authors: Colburn WA,Gibson DM,Rodriguez LC,Buggé CJ,Blumenthal HP

    更新日期:1985-11-01 00:00:00

  • Peripheral hemodynamic and humoral effects of oral zofenopril calcium (SQ. 26,991) in patients with congestive heart failure.

    abstract::In 14 patients with congestive heart failure (CHF) of various grade (NYHA class 2-4) the effects of zofenopril calcium (SQ 26,991) on blood pressure and forearm circulation were studied by venous occlusion plethysmography. Changes in plasma renin activity (PRA), aldosterone, Atrial natriuretic factor (ANF) and arginin...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1989.tb03282.x

    authors: Borghi C,Magelli C,Boschi S,Costa FV,Capelli M,Varani E,Magnani B,Ambrosioni E

    更新日期:1989-12-01 00:00:00

  • Drug-disease interactions: losartan effect is not downregulated by rheumatoid arthritis.

    abstract::Inflammatory conditions, such as rheumatoid arthritis, reduce response to calcium channel and beta-adrenergic antagonists but not the angiotensin II type 1 receptor (AT(1)R) antagonist valsartan. Inflammation also reduces clearance of some drugs or active metabolite, thereby reducing response. Active (n = 14) and cont...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1177/0091270006292163

    authors: Daneshtalab N,Lewanczuk RZ,Russell AS,Jamali F

    更新日期:2006-11-01 00:00:00

  • No Clinical Impact of CYP3A5 Gene Polymorphisms on the Pharmacokinetics and/or Efficacy of Maraviroc in Healthy Volunteers and HIV-1-Infected Subjects.

    abstract::Maraviroc is a C-C chemokine receptor type-5 antagonist approved for the treatment of HIV-1. Previous studies show that cytochrome P450 3A5 (CYP3A5) plays a role in maraviroc metabolism. CYP3A5 is subject to a genetic polymorphism. The presence of 2 functional alleles (CYP3A5*1/*1) confers the extensive metabolism phe...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,多中心研究

    doi:10.1002/jcph.1306

    authors: Vourvahis M,McFadyen L,Nepal S,Valluri SR,Fang A,Fate GD,Wood LS,Marshall JC,Chan PLS,Nedderman A,Haynes J,Savage ME,Clark A,Smith KY,Heera J

    更新日期:2019-01-01 00:00:00

  • Pharmacokinetics of oral dexamethasone and midazolam when administered with single-dose intravenous 150 mg fosaprepitant in healthy adult subjects.

    abstract::Aprepitant or its prodrug fosaprepitant, in combination with a corticosteroid and a 5-HT(3) receptor antagonist, are used to prevent chemotherapy-induced nausea and vomiting. This study evaluated the effect of fosaprepitant 150 mg on CYP3A4 metabolism. Fosaprepitant 150 mg has been submitted to regulatory agencies for...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1177/0091270010387792

    authors: Marbury TC,Ngo PL,Shadle CR,Jin B,Panebianco D,Caro L,Valentine J,Murphy G

    更新日期:2011-12-01 00:00:00

  • The effect of lovastatin on early restenosis.

    abstract::The effect of lovastatin given before percutaneous coronary angioplasty (PTCA) on early restenosis was investigated in men with mild to moderate hypercholesterolemia. Thirty-four hypercholesterolemic patients (serum LDL cholesterol 130-200 mg/dL) undergoing their first PTCA completed a 6-month prospective, double-blin...

    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.tb05017.x

    authors: Beigel Y,Zafrir N,Teplitzky Y,Neuman Y,Gavish D,Wurzel M,Fainaru M

    更新日期:1995-06-01 00:00:00

  • The application of stable isotopes to studies of drug bioavailability and bioequivalence.

    abstract::The increased availability of chemical intermediates and automated instrumentation has resulted in expanded use of stable isotopes for bioavailability and bioequivalence studies in recent years. Initially, stable isotopes were confined to the labeling of mass internal standard compounds for gas chromatography/mass spe...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1986.tb03551.x

    authors: Wolen RL

    更新日期:1986-07-01 00:00:00

  • Drug-drug and drug-food interactions between tenofovir disoproxil fumarate and didanosine.

    abstract::The drug-drug and drug-food interactions between tenofovir DF and didanosine EC were evaluated in 2 pharmacokinetic studies in healthy adult subjects. When 400 mg was dosed with tenofovir DF, mean didanosine AUC was increased by 44% to 60% following fasted or fed administration. Staggered coadministration (2 hour, fas...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1177/0091270005281351

    authors: Kearney BP,Sayre JR,Flaherty JF,Chen SS,Kaul S,Cheng AK

    更新日期:2005-12-01 00:00:00

  • Long-term efficacy and toxicity of high- and low-dose amiodarone regimens.

    abstract::Amiodarone is an effective antiarrhythmic drug for the control of potentially lethal and lethal ventricular arrhythmias (VA). In the United States, a high-dose regimen has been used at the expense of a high toxicity profile for the control of lethal VAs. Significant antiarrhythmic efficacy has also been established wi...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1002/j.1552-4604.1989.tb03354.x

    authors: Kerin NZ,Aragon E,Faitel K,Frumin H,Rubenfire M

    更新日期:1989-05-01 00:00:00

  • A computer-based, problem-solving system of instruction in clinical pharmacology.

    abstract::Advances in microcomputer technology provide new ways of incorporating PBL procedures in clinical pharmacology courses. Developments in graphics-user interfaces and analog/digital systems that display physiologic information directly on the monitor enable the computer to serve as a learning resource as laboratory clas...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1991.tb04962.x

    authors: Hutcheon DE,el-Gawly HW

    更新日期:1991-03-01 00:00:00

  • Effect of cyclosporine on the pharmacokinetics of aliskiren in healthy subjects.

    abstract::To explore the clinical relevance of inhibition of multidrug resistance transporter 1 and organic anion transporting polypeptide transporter, a drug-drug interaction study was conducted using aliskiren and cyclosporine. This was an open-label, single-sequence, parallel-group, single-dose study in healthy subjects. Sub...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1177/0091270010385934

    authors: Rebello S,Compain S,Feng A,Hariry S,Dieterich HA,Jarugula V

    更新日期:2011-11-01 00:00:00

  • Interaction between propranolol and propafenone in healthy volunteers.

    abstract::The effects of propafenone on the pharmacokinetics and pharmacodynamics of propranolol were evaluated in 12 healthy male subjects. Both propafenone and propranolol were each administered alone for one week followed by concomitant administration for an additional week. Blood samples, obtained at steady-state, were anal...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1002/j.1552-4604.1989.tb03373.x

    authors: Kowey PR,Kirsten EB,Fu CH,Mason WD

    更新日期:1989-06-01 00:00:00

  • Efficacy and pharmacokinetics of adefovir dipivoxil liquid suspension in patients with chronic hepatitis B and renal impairment.

    abstract::The study evaluated whether a liquid suspension of adefovir dipivoxil (ADV) is effective and safe when dose adjusted based on varying degrees of renal impairment in patients with chronic hepatitis B. Patients had stable mild, moderate, or severe renal impairment or end-stage renal disease. Twenty-eight patients were e...

    journal_title:Journal of clinical pharmacology

    pub_type: 杂志文章,多中心研究

    doi:10.1177/0091270010381385

    authors: Shiffman ML,Pol S,Rostaing L,Schiff E,Thabut D,Zeuzem S,Zong J,Frederick D,Rousseau F

    更新日期:2011-09-01 00:00:00

  • Early stopping of aerospace medical trials: application of sequential principles.

    abstract::A two-period, crossover trial was conducted in the hypobaric chamber on human subjects to compare the influence of inflight exercise (experimental) and restricted activity (control) on altitude decompression sickness (DCS) during simulated extravehicular activities. Out of 39 pairs (total of 78 exposures), 4 cases of ...

    journal_title:Journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1002/j.1552-4604.1994.tb02012.x

    authors: Kumar KV,Powell MR,Waligora JM

    更新日期:1994-06-01 00:00:00

  • Pharmacokinetics and bioavailability of the RRR and all racemic stereoisomers of alpha-tocopherol in humans after single oral administration.

    abstract::The plasma and red blood cell pharmacokinetics and bioavailability of the natural source (RRR, d) and all racemic (all rac, dl) stereoisomers of alpha-tocopherol were studied in 12 men in a double-blind randomized crossover study. Subjects were administered two 400-mg soft-gelatin capsules of either RRR or all rac alp...

    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.1552-4604.1993.tb03909.x

    authors: Ferslew KE,Acuff RV,Daigneault EA,Woolley TW,Stanton PE Jr

    更新日期:1993-01-01 00:00:00