| Serum levels and possible haemodynamic effects following anorectal application of an ointment containing nifedipine and lignocaine : a study in healthy volunteers. | |
| | |
MedLine Citation:
|
PMID: 17163278 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
OBJECTIVES: This study aimed to assess whether topical anorectal application of an ointment containing nifedipine (0.3% w/w) and lignocaine (lidocaine) [1.5% w/w] to healthy adult volunteers gives rise to pharmacologically relevant serum levels of the active ingredients and has any haemodynamic effects or side effects. METHODS: A dose of 3g of the ointment was circumferentially applied inside the anus to 12 healthy volunteers every 12 hours for 7 days. Blood samples were collected at 0, 30, 60, 240, 480 and 720 minutes after the first application; in addition, blood samples were collected at days 1 and 7 after multiple applications. Serum concentrations of nifedipine, its main metabolites and lignocaine were determined by a new high-performance liquid chromatography method established for the purpose of the study. Volunteers' blood pressure, heart rate, ECG status and laboratory parameters were monitored throughout the study. RESULTS: Topical application of the ointment to healthy volunteers did not produce therapeutically significant serum levels of the active ingredients and/or their active metabolites. Indeed, chromatographic signals of the active ingredients and/or nifedipine metabolites were only sporadically observed, below the quantification limits for the method, and consistent with therapeutically negligible concentrations. No serious local or systemic adverse events were observed throughout the study, and no subjects developed arrhythmias or significant ECG changes. Neither blood pressure nor mean heart rate varied significantly after application of a single dose. After multiple doses, mean systolic and diastolic blood pressure remained close to baseline levels for the duration of the study. The mean heart rate after multiple doses was about 5% below baseline level at days 1 and 7; however, these differences were not statistically significant. CONCLUSION: This study demonstrates the safety of topical anorectal application of an ointment containing nifedipine (0.3% w/w) and lignocaine (1.5% w/w) to healthy volunteers. |
| | |
Authors:
|
Pasquale Perrotti; Lucia Grumetto; Francesco Barbato; Carmine Antropoli |
Related Documents
:
|
9344638 - Attenuation in rat brain nitric oxide synthase activity in the coarctation model of hyp... 15321188 - Cardiovascular consequences of the concomitant administration of nifedipine and magnesi... 3288468 - Efficacy and tolerability of atenolol, nifedipine and their combination in the manageme... 10075388 - Reduced bcl-2 concentrations in hypertensive patients after lisinopril or nifedipine ad... 4419698 - Screening for hypertension: some epidemiological observations. 16944678 - Validation of a new noninvasive method to measure blood pressure and assess baroreflex ... |
Publication Detail:
|
Type: Clinical Trial; Journal Article |
Journal Detail:
|
Title: Clinical drug investigation Volume: 26 ISSN: 1173-2563 ISO Abbreviation: Clin Drug Investig Publication Date: 2006 |
Date Detail:
|
Created Date: 2006-12-13 Completed Date: 2007-02-05 Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 9504817 Medline TA: Clin Drug Investig Country: New Zealand |
Other Details:
|
Languages: eng Pagination: 459-67 Citation Subset: IM |
Affiliation:
|
Department of Gastroenterology, Chirurgia Gastroenterologica, A. Cardarelli Hospital, Naples, Italy. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Administration, Topical Adult Anal Canal / drug effects, metabolism Anesthetics, Local / administration & dosage, blood, pharmacokinetics Blood Pressure / drug effects*, physiology Chromatography, High Pressure Liquid / methods Electrocardiography Female Heart Rate / drug effects*, physiology Humans Lidocaine / administration & dosage*, blood, pharmacokinetics Male Middle Aged Nifedipine / administration & dosage*, blood, pharmacokinetics Ointments |
| Chemical | |
Reg. No./Substance:
|
0/Anesthetics, Local; 0/Ointments; 137-58-6/Lidocaine; 21829-25-4/Nifedipine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Cost-effectiveness analysis of schizophrenia relapse prevention : an economic evaluation of the ZEUS...
Next Document: Safety, efficacy and pharmacokinetics of ritonavir 400mg/saquinavir 400mg twice daily plus rifampici...