دورية أكاديمية
Pharmacokinetics and dose proportionality of D2-agonist MK-458 (HPMC) in parkinsonism.
العنوان: | Pharmacokinetics and dose proportionality of D2-agonist MK-458 (HPMC) in parkinsonism. |
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المؤلفون: | Cutler NR; California Clinical Trials, Beverly Hills, California., Reines SA, McLean LF, Sramek JJ, Porras AG, Hand EL |
المصدر: | Clinical pharmacokinetics [Clin Pharmacokinet] 1992 Mar; Vol. 22 (3), pp. 223-30. |
نوع المنشور: | Journal Article |
اللغة: | English |
بيانات الدورية: | Publisher: Country of Publication: Switzerland NLM ID: 7606849 Publication Model: Print Cited Medium: Print ISSN: 0312-5963 (Print) Linking ISSN: 03125963 NLM ISO Abbreviation: Clin Pharmacokinet Subsets: MEDLINE |
أسماء مطبوعة: | Publication: [Switzerland] : Adis, part of Springer Science+Business Media Original Publication: New York, ADIS Press. |
مواضيع طبية MeSH: | Antiparkinson Agents/*pharmacokinetics , Dopamine Agents/*pharmacokinetics , Lactose/*analogs & derivatives , Methylcellulose/*analogs & derivatives , Parkinson Disease/*metabolism, Administration, Oral ; Aged ; Antiparkinson Agents/adverse effects ; Antiparkinson Agents/blood ; Delayed-Action Preparations ; Dopamine Agents/adverse effects ; Dopamine Agents/blood ; Dose-Response Relationship, Drug ; Female ; Humans ; Lactose/adverse effects ; Lactose/blood ; Lactose/pharmacokinetics ; Male ; Methylcellulose/adverse effects ; Methylcellulose/blood ; Methylcellulose/pharmacokinetics ; Middle Aged ; Oxazines ; Parkinson Disease/blood ; Tablets |
مستخلص: | To investigate the pharmacokinetic profile, bioavailability, and dose proportionality of the D2-agonist MK-458 (hydroxypropylmethylcellulose tablet, a sustained release formulation), a 4-period crossover study was conducted in 10 patients with mild to moderate Parkinson's disease (mean age = 63 y; 1 woman, 9 men). Following a titration phase to induce tolerance, each patient was given single oral doses of 6, 12 and 18 mg and a single intravenous 40 micrograms dose (5 micrograms/h over 8h). The maximum concentrations of MK-458 observed in plasma after oral administration were 139, 240 and 344 ng/L for the 6, 12 and 18 mg doses, respectively, and occurred after 8.0, 9.0 and 5.5 h, respectively. Mean areas under the plasma concentration-time curves were 1728, 2849 and 5484 ng/L.h, respectively. The mean plasma half-life was 3.8 h and mean plasma clearance was 3390 ml/min (203.4 L/h). The bioavailability (approximately 5%) was very similar for the 3 tablet formulations tested. The disposition of MK-458 was independent of the dose over the range of doses studied. |
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المشرفين على المادة: | 0 (Antiparkinson Agents) 0 (Delayed-Action Preparations) 0 (Dopamine Agents) 0 (Oxazines) 0 (Tablets) 9004-67-5 (Methylcellulose) 99705-65-4 (MK 458) J2B2A4N98G (Lactose) |
تواريخ الأحداث: | Date Created: 19920301 Date Completed: 19920511 Latest Revision: 20181113 |
رمز التحديث: | 20221213 |
DOI: | 10.2165/00003088-199222030-00004 |
PMID: | 1348452 |
قاعدة البيانات: | MEDLINE |
تدمد: | 0312-5963 |
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DOI: | 10.2165/00003088-199222030-00004 |