Incomplete and delayed bioavailability of sublingual nitroglycerin☆
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Effectiveness of sublingual immunization: Innovation for preventing infectious diseases
2019, Mucosal Vaccines: Innovation for Preventing Infectious DiseasesChallenges and innovations of drug delivery in older age
2018, Advanced Drug Delivery ReviewsCitation Excerpt :A key limitation in using ODTs in the elderly is the reduction in saliva production with ageing [115], which is likely to impact on ODT disintegration and drug absorption. Nitroglycerin sublingual tablets, which are well known to have a variable dissolution rate [116], are reported to be absorbed at a much slower rate in the older patients relative to in younger patients [117]. Whereas sublingual tablets do work better, when patients with a dry mouth wet their mouth first, wetting does not assist in the action of sublingual spray [118] and the spray formulation does not require an adequate saliva production [119].
Critical appraisal of the clinical utility of sublingual immunotherapy in allergy
2016, Contemporary Clinical Trials CommunicationsCitation Excerpt :So, the small molecules administered by a sublingual way quickly reach the general circulation shunting the bowel or the liver [31,32]. The obtained plasmatic concentration is maximal approximately 5 min after administration, with a global bioavailability of about 70% [37,38]. The local environment in the mouth is regarded as a site of natural immune tolerance [15].
Mechanisms mediating nitroglycerin-induced delayed-onset hyperalgesia in the rat
2016, NeuroscienceCitation Excerpt :While in one study in migraineurs GTN administration did not produce allodynia or hyperalgesia as measured by quantitative sensory testing (Ladda et al., 2006), in contrast, in other studies GTN has been shown to have extracranial effects on nociception in migraineurs, but not in non-migraineurs (Sandrini et al., 2002; Di Clemente et al., 2009; Perrotta et al., 2011) and has been shown to reduce nociceptive thresholds relative to placebo (Thomsen et al., 1996). These latter studies used 0.9–1.2 mg GTN, oral or sublingual, which gives rise to plasma levels in the ng/ml range (Noonan and Benet, 1985), similar to that following μg/min intravenous administration (Imhof et al., 1982; Bogaert, 1994). This raises the intriguing possibility that migraine is a more generalized condition, impacting structures outside the head and neck.
Organic nitrate metabolism and action: Toward a unifying hypothesis and the future-a dedication to Professor Leslie Z. Benet
2013, Journal of Pharmaceutical SciencesCitation Excerpt :From the mid-1980s to the late 1990s, Professor Benet and his associates carried out many pivotal studies that greatly enhanced our understanding of the pharmacological properties of nitroglycerin (NTG) and its dinitrate metabolites, namely, 1,2-glyceryl dinitrate (1,2-GDN) and 1,3-glyceryl dinitrate (1,3-GDN). Expanding on the assay originally described by Miyazaki et al.,1 Benet’s group utilized electron capture detection to determine the plasma concentrations of these organic nitrates (ORNs),2–4 which allowed them to characterize the metabolism and pharmacokinetics of NTG and its dinitrate metabolites after different routes of administration,5 including the intravenous/vascular route,6–8 cutaneous/transdermal application,9–14 sublingual8 and oral dosing.15–17 Benet and his group then followed with several studies that delineated the pharmacokinetic-pharmacodynamic relationships of NTG and its dinitrate metabolites in dogs,18,19 healthy volunteers,20,21 and in elderly conscious patients.22
Sublingual mucosa: A new vaccination route for systemic and mucosal immunity
2011, CytokineCitation Excerpt :Oral mucosa, including buccal (the cheek lining), sublingual (s.l.) (underside of the tongue), and gingival mucosa, have recently received much attention as novel delivery sites for therapeutic drugs because they do not subject proteins and/or peptides to the degradation associated with gastrointestinal administration. Among oral mucosal routes, the s.l. route is commonly used for immunotherapeutic treatment of allergies because it quickly absorbs antigen, allowing direct entry into the bloodstream without passing through the intestine or liver and thereby eliciting allergen-specific tolerance [20–23]. No cases of anaphylactic shock were observed in recent human studies of s.l. administered immunotherapy targeting allergies [24–26].
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This study was supported in part by Grant HL32243 from the National Institutes of Health, Bethesda, Maryland, and by a grant from Key Pharmaceuticals, Inc., Miami, Florida. During the course of this study.
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Dr. Noonan received support as an American Foundation for Pharmaceutical Education James F. Hoge Memorial Fellow.