دورية أكاديمية
أعرض في EDS

Pharmacokinetics and dose proportionality of D2-agonist MK-458 (HPMC) in parkinsonism.

التفاصيل البيبلوغرافية
العنوان: Pharmacokinetics and dose proportionality of D2-agonist MK-458 (HPMC) in parkinsonism.
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
الوصف
تدمد:0312-5963
DOI:10.2165/00003088-199222030-00004