Abstract:
:Levonantradol and its desacetylated metabolite (desacetyllevonantradol) produced a dose-dependent increase in the hot plate and tail flick response latencies following intrathecal administration in a dose range from 4 to 40 micrograms. No difference in potency between the two drugs was observed, as defined by the ED50 values obtained in either test. The duration of the effect of either drug was also dose dependent ranging from 30 to 120 minutes. No effect on placing, stepping or righting reflexes or the ability of the rats to negotiate a 60 degrees inclined plane was observed at these doses. At the highest doses, however, an exaggerated myoclonic response to abrupt muscle stretch was observed. None of those effects was antagonized by naloxone (2 mg/kg) administered intraperitoneally before or after levonantradol.
journal_name
J Clin Pharmacoljournal_title
Journal of clinical pharmacologyauthors
Yaksh TLdoi
10.1002/j.1552-4604.1981.tb02612.xsubject
Has Abstractpub_date
1981-08-01 00:00:00pages
334S-340Sissue
S1eissn
0091-2700issn
1552-4604journal_volume
21pub_type
杂志文章abstract::This was a double-blind, placebo-controlled, randomized, parallel, dose-escalation study to assess the pharmacokinetics, platelet response, safety, and tolerability of supratherapeutic doses of eltrombopag (100 mg, 150 mg, and 200 mg once daily) administered for 5 days to 33 healthy adult volunteers. Plasma eltrombopa...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1177/0091270010368677
更新日期:2011-03-01 00:00:00
abstract::Glasdegib is approved for treating acute myeloid leukemia in elderly patients at 100 mg once daily in combination with low-dose cytarabine. Exposure-efficacy analysis showed that the survival benefit of glasdegib was not glasdegib exposure-dependent. The relationship between glasdegib exposure and adverse event (AE) c...
journal_title:Journal of clinical pharmacology
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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
更新日期:1995-11-01 00:00:00
abstract::The integrated minimal model allows assessment of clinical diagnosis indices, for example, insulin sensitivity (SI ) and glucose effectiveness (SG ), from data of the insulin-modified intravenous glucose tolerance test (IVGTT), which is laborious with an intense sampling schedule, up to 32 samples. The aim of this stu...
journal_title:Journal of clinical pharmacology
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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
更新日期:1997-07-01 00:00:00
abstract::Two once-daily rivaroxaban dosing regimens were compared with warfarin for stroke prevention in patients with non-valvular atrial fibrillation in ROCKET AF: 20 mg for patients with normal/mildly impaired renal function and 15 mg for patients with moderate renal impairment. Rivaroxaban population pharmacokinetic (PK)/p...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章,多中心研究,随机对照试验
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更新日期:2014-08-01 00:00:00
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journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1177/00912709922008173
更新日期:1999-06-01 00:00:00
abstract::DS-1040, a low-molecular-weight imidazole derivative, inhibits the enzymatic activity of thrombin-activatable fibrinolysis inhibitor (TAFIa), enhancing endogenous tissue plasminogen activator-triggered fibrinolysis. This first-in-human, randomized, placebo-controlled, phase 1 study evaluated the safety, pharmacokineti...
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pub_type: 杂志文章,随机对照试验
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abstract::CPX-351, a dual-drug liposomal encapsulation of cytarabine and daunorubicin at a synergistic ratio, is approved in the United States for adults with newly diagnosed therapy-related acute myeloid leukemia or acute myeloid leukemia with myelodysplasia-related changes. Population pharmacokinetics analyses were performed ...
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journal_title:Journal of clinical pharmacology
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abstract::UCN-01 is a protein kinase inhibitor under development as a novel anticancer drug. The initial pharmacologic features in patients were not predicted from preclinical experiments. The distribution volume and the systemic clearance were much lower than those in experimental animals (mice, rats, and dogs), and the elimin...
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abstract::Amyotrophic lateral sclerosis (ALS) is a fatal disorder characterized by degeneration of the upper and lower motor neuron. Among the at least 25 known genes associated with familial (hereditary) and sporadic ALS, mutations in fused-in-sarcoma (FUS) and superoxide dismutase 1 (SOD1) have been extensively investigated i...
journal_title:Journal of clinical pharmacology
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journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1002/j.1552-4604.1981.tb01746.x
更新日期:1981-10-01 00:00:00
abstract::Udenafil, a cyclic guanosine monophosphate-specific phosphodiesterase type 5 inhibitor, has been developed to treat erectile dysfunction. We evaluated the effect of age on the pharmacokinetics and tolerability of udenafil. A single-center, open-label, parallel-group phase 1 study was conducted in healthy adult subject...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
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journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1981.tb02602.x
更新日期:1981-08-01 00:00:00
abstract::Reduced bioavailability (F) due to hepatic first-pass extraction of an oral dose (D) is a well-known pharmacokinetic phenomenon. An integrated solution for Michaelis-Menten kinetics of the first-pass effect is derived from the maximal metabolic rate (Vm), volume of distribution (Vd), first order absorption rate consta...
journal_title:Journal of clinical pharmacology
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doi:10.1002/j.1552-4604.1989.tb03320.x
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abstract::Azlocillin is an important acylureido penicillin antibiotic for the management of complex gram-negative infections particularly those caused by Pseudomonas species. The current studies demonstrate that it manifests dose-dependent pharmacokinetics during the usual regimens of clinical dosing, that enterohepatic recircu...
journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1987-07-01 00:00:00
abstract::Varenicline is a novel selective α4β2 nicotinic acetylcholine partial agonist developed for smoking cessation. Single- and multiple dose studies were conducted to investigate pharmacokinetics, safety, and tolerability of varenicline in healthy male Japanese smokers. The single-dose study was conducted as a double-blin...
journal_title:Journal of clinical pharmacology
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abstract::In the Phase I study, the new anthracycline aclacinomycin A was given to 22 advanced cancer patients on a schedule of daily intravenous administration for five days repeated every four weeks. The limiting toxicity was myelosuppression, which was severe at a dose of 30 mg/m2 per day for five days. Platelet nadirs were ...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1982.tb02686.x
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abstract::Meptazinol, m-(3-ethyl-1-methyl-hexahydro-1-H-azepin-3-yl) phenol hydrochloride is a centrally active opioid analgesic with a specificity for the mu-1 receptor. It has been reported to lack many of the side effects commonly observed with morphine and morphinelike drugs in man. The objective of this study was to assess...
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.1552-4604.1989.tb03272.x
更新日期:1989-11-01 00:00:00
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...
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更新日期:2005-12-01 00:00:00
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journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1990.tb03466.x
更新日期:1990-03-01 00:00:00
abstract::Several approaches are available to estimate the glomerular filtration rate (GFR) from the sinistrin clearance. To compare such approaches, GFR was estimated in six healthy volunteers, both after a bolus injection and a bolus dose followed by a 6-hour infusion. A recently developed high-performance liquid chromatograp...
journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1002/j.1552-4604.1997.tb04355.x
更新日期:1997-08-01 00:00:00
abstract::The steady-state pharmacokinetics of didanosine (DDI) and ketoconazole (KET) were evaluated when the agents were administered alone or concurrently to patients seropositive for the human immunodeficiency virus. Using a randomized, three-way crossover design, multiple oral doses of DDI (375 mg twice daily for 4 days), ...
journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1993-10-01 00:00:00
abstract::Atrial fibrillation is very common in the United States. After a search of Medline, EMBASE, and CINAHL, 4 trials evaluating inhibitors of the renin-angiotensin system were identified for prevention of new-onset atrial fibrillation, facilitation of electrical cardioversion of atrial fibrillation, and prevention of atri...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章,meta分析
doi:10.1177/0091270005283284
更新日期:2006-01-01 00:00:00
abstract::Olanzapine is an atypical antipsychotic medication indicated for the treatment of schizophrenia and other manifestations of psychotic illness. Common side effects include somnolence, constipation, weight gain, and postural hypotension. The authors report a case of hypotension accompanied by bradycardia in a normal, he...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
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更新日期:2002-01-01 00:00:00
abstract::Lormetazepam, an investigational hypnotic, was evaluated for efficacy and withdrawal phenomena in doses of 0.5, 1.0, 1.5, and 2.0 mg in four separate sleep laboratory protocols, each including four placebo baseline nights, seven drug nights, and three placebo withdrawal nights. A moderate degree of efficacy was shown ...
journal_title:Journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1002/j.1552-4604.1982.tb02645.x
更新日期:1982-11-01 00:00:00
abstract::This experiment represents the first time that it has been possible to measure a body fluid compartment by direct means during spaceflight. Based on the results observed in the five crewmen in this study, it is concluded that TBW decreases by 3.4% after 1 to 3 days of exposure to microgravity in the Space Shuttle. Som...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/j.1552-4604.1991.tb03663.x
更新日期:1991-10-01 00:00:00
abstract::Respiratory syncytial virus (RSV)-associated respiratory tract infection is a leading cause of hospitalizations in infants for which no effective treatment exists. RSV infection is also an important cause of respiratory disease in adults and immunocompromised patients. Presatovir (GS-5806) is an orally bioavailable an...
journal_title:Journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1002/jcph.1112
更新日期:2018-08-01 00:00:00