The Experts below are selected from a list of 315 Experts worldwide ranked by ideXlab platform
Daniel Hoyer - One of the best experts on this subject based on the ideXlab platform.
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interaction of the α adrenoceptor agonist Oxymetazoline with serotonin 5 ht1a 5 ht1b 5 ht1c and 5 ht1d receptors
European Journal of Pharmacology, 1991Co-Authors: Philippe Schoeffter, Daniel HoyerAbstract:Oxymetazoline was recognized with nanomolar affinity by 5-HT1A, 5-HT1B and 5-HT1D binding sites and mimicked the effects of 5-hydroxytryptamine with about the same potency and intrinsic activity as the endogenous amine in the corresponding functional tests. At 5-HT1C receptors, Oxymetazoline behaved as a mixed agonist-antagonist. Clonidine had minimal activity. Methiothepin antagonized the effects of Oxymetazoline (7.4
Oxymetazoline is a full and potent agonist at 5-HT1A, 5-HT1B and 5-HT1D receptors and a partial agonist at 5-HT1C receptors. -
Interaction of the α-adrenoceptor agonist Oxymetazoline with serotonin 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors
European Journal of Pharmacology, 1991Co-Authors: Philippe Schoeffter, Daniel HoyerAbstract:Oxymetazoline was recognized with nanomolar affinity by 5-HT1A, 5-HT1B and 5-HT1D binding sites and mimicked the effects of 5-hydroxytryptamine with about the same potency and intrinsic activity as the endogenous amine in the corresponding functional tests. At 5-HT1C receptors, Oxymetazoline behaved as a mixed agonist-antagonist. Clonidine had minimal activity. Methiothepin antagonized the effects of Oxymetazoline (7.4
Elliot V Hersh - One of the best experts on this subject based on the ideXlab platform.
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two recent advances in local anesthesia intranasal tetracaine Oxymetazoline and liposomal bupivacaine
Current Oral Health Reports, 2017Co-Authors: Elliot V Hersh, Mana Saraghi, Paul A MooreAbstract:This paper reviews the efficacy, safety, and clinical utility of two novel formulations of local anesthetics; intranasal 3% tetracaine plus 0.05% Oxymetazoline and 1.3% liposomal bupivacaine. Intranasal 3% tetracaine/Oxymetazoline when delivered into the ipsilateral nostril of the target tooth has a success rate of 84–90% in completing a single restorative procedure from the second premolar forward. The maximum recommended dose is 18 mg tetracaine/0.3 mg Oxymetazoline (three 0.2-ml sprays). The most common adverse effects are nasal congestion and nasal runniness. Liposomal bupivacaine is administered by infiltration injection solely for postoperative pain control and appears to provide analgesic and opioid-sparing effects in knee arthroplasty, bunionectomy, hemorrhoidectomy, and laparotomy. The maximum recommended dose is 20 ml or 266 mg although for dental impaction surgery, a maximum of 10 ml or 133 mg is all that may be required. Intranasal tetracaine/Oxymetazoline is currently FDA approved only for single maxillary restorative procedures in patients weighing 88 lb or greater. Further clinical trials should include more invasive dental procedures and pediatric patients. The utility of liposomal bupivacaine following dental surgery needs to be further explored.
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Two Recent Advances in Local Anesthesia: Intranasal Tetracaine/Oxymetazoline and Liposomal Bupivacaine
Current Oral Health Reports, 2017Co-Authors: Elliot V Hersh, Mana Saraghi, Paul A MooreAbstract:This paper reviews the efficacy, safety, and clinical utility of two novel formulations of local anesthetics; intranasal 3% tetracaine plus 0.05% Oxymetazoline and 1.3% liposomal bupivacaine. Intranasal 3% tetracaine/Oxymetazoline when delivered into the ipsilateral nostril of the target tooth has a success rate of 84–90% in completing a single restorative procedure from the second premolar forward. The maximum recommended dose is 18 mg tetracaine/0.3 mg Oxymetazoline (three 0.2-ml sprays). The most common adverse effects are nasal congestion and nasal runniness. Liposomal bupivacaine is administered by infiltration injection solely for postoperative pain control and appears to provide analgesic and opioid-sparing effects in knee arthroplasty, bunionectomy, hemorrhoidectomy, and laparotomy. The maximum recommended dose is 20 ml or 266 mg although for dental impaction surgery, a maximum of 10 ml or 133 mg is all that may be required. Intranasal tetracaine/Oxymetazoline is currently FDA approved only for single maxillary restorative procedures in patients weighing 88 lb or greater. Further clinical trials should include more invasive dental procedures and pediatric patients. The utility of liposomal bupivacaine following dental surgery needs to be further explored.
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intranasal tetracaine and Oxymetazoline a newly approved drug formulation that provides maxillary dental anesthesia without needles
Current Medical Research and Opinion, 2016Co-Authors: Elliot V Hersh, Mana Saraghi, Paul A MooreAbstract:AbstractBackground: An intranasal formulation of 3% tetracaine and 0.05% Oxymetazoline (Kovanaze) received FDA approval on 29 June 2016. This formulation appears to provide sufficient local anesthesia to perform routine dental restorative (filling) procedures in maxillary teeth from second premolar forward.Objectives: The aim of this paper is to provide an overview of the efficacy, pharmacokinetics and tolerability of 3% tetracaine plus 0.05% Oxymetazoline when administered intranasally.Methods: The literature was reviewed employing the search terms intranasal delivery, tetracaine, Oxymetazoline and dental local anesthesia employing the search engines PubMed Plus, Scopus and the Web of Science. The search was limited to double-blind, randomized, placebo or sham-controlled trials except for phase 1 and phase 2 pharmacokinetic and safety data.Results: A total of five relevant publications appeared in the peer reviewed literature. Three per cent tetracaine plus 0.05% Oxymetazoline produced a success rate of ...
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the cardiovascular effects and pharmacokinetics of intranasal tetracaine plus Oxymetazoline preliminary findings
Journal of the American Dental Association, 2012Co-Authors: Helen Giannakopoulos, Anthony T Cacek, Paul A Moore, Lawrence M Levin, Joli C Chou, Matthew Hutcheson, Stacey A Secreto, Elliot V HershAbstract:ABSTRACT Background The authors evaluated the cardiovascular effects and pharmacokinetics of an intranasal 3 percent tetracaine/0.05 percent Oxymetazoline spray developed to provide needle-free anesthesia of maxillary teeth. Methods The authors administered to 12 participants a proposed maximum recommended dose (MRD) (18 milligrams tetracaine/0.3 mg Oxymetazoline) as three bilateral pairs of 0.1-milliliter nasal sprays. They administered two times this dose (36 mg tetracaine/0.6 mg Oxymetazoline) as six bilateral pairs one to three weeks later. The authors recorded the patients’ heart rate, blood pressure and oxygen saturation. They drew blood samples at baseline and 15 times during the two hours after drug administration. Results Physiological measures remained fairly stable throughout the two-hour period, with small but significant decreases ( P Conclusions Intranasal tetracaine/Oxymetazoline mist generally was well tolerated in study participants. Clinical Implications The safety profile and pharmacokinetics of this intranasal formulation indicate that it appears to be generally well tolerated in patients for achieving anesthesia of the maxilla. Additional safety and efficacy data are required, particularly in patients with cardiovascular disease and other comorbidities.
Philippe Schoeffter - One of the best experts on this subject based on the ideXlab platform.
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interaction of the α adrenoceptor agonist Oxymetazoline with serotonin 5 ht1a 5 ht1b 5 ht1c and 5 ht1d receptors
European Journal of Pharmacology, 1991Co-Authors: Philippe Schoeffter, Daniel HoyerAbstract:Oxymetazoline was recognized with nanomolar affinity by 5-HT1A, 5-HT1B and 5-HT1D binding sites and mimicked the effects of 5-hydroxytryptamine with about the same potency and intrinsic activity as the endogenous amine in the corresponding functional tests. At 5-HT1C receptors, Oxymetazoline behaved as a mixed agonist-antagonist. Clonidine had minimal activity. Methiothepin antagonized the effects of Oxymetazoline (7.4
Oxymetazoline is a full and potent agonist at 5-HT1A, 5-HT1B and 5-HT1D receptors and a partial agonist at 5-HT1C receptors. -
Interaction of the α-adrenoceptor agonist Oxymetazoline with serotonin 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors
European Journal of Pharmacology, 1991Co-Authors: Philippe Schoeffter, Daniel HoyerAbstract:Oxymetazoline was recognized with nanomolar affinity by 5-HT1A, 5-HT1B and 5-HT1D binding sites and mimicked the effects of 5-hydroxytryptamine with about the same potency and intrinsic activity as the endogenous amine in the corresponding functional tests. At 5-HT1C receptors, Oxymetazoline behaved as a mixed agonist-antagonist. Clonidine had minimal activity. Methiothepin antagonized the effects of Oxymetazoline (7.4
Paul A Moore - One of the best experts on this subject based on the ideXlab platform.
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two recent advances in local anesthesia intranasal tetracaine Oxymetazoline and liposomal bupivacaine
Current Oral Health Reports, 2017Co-Authors: Elliot V Hersh, Mana Saraghi, Paul A MooreAbstract:This paper reviews the efficacy, safety, and clinical utility of two novel formulations of local anesthetics; intranasal 3% tetracaine plus 0.05% Oxymetazoline and 1.3% liposomal bupivacaine. Intranasal 3% tetracaine/Oxymetazoline when delivered into the ipsilateral nostril of the target tooth has a success rate of 84–90% in completing a single restorative procedure from the second premolar forward. The maximum recommended dose is 18 mg tetracaine/0.3 mg Oxymetazoline (three 0.2-ml sprays). The most common adverse effects are nasal congestion and nasal runniness. Liposomal bupivacaine is administered by infiltration injection solely for postoperative pain control and appears to provide analgesic and opioid-sparing effects in knee arthroplasty, bunionectomy, hemorrhoidectomy, and laparotomy. The maximum recommended dose is 20 ml or 266 mg although for dental impaction surgery, a maximum of 10 ml or 133 mg is all that may be required. Intranasal tetracaine/Oxymetazoline is currently FDA approved only for single maxillary restorative procedures in patients weighing 88 lb or greater. Further clinical trials should include more invasive dental procedures and pediatric patients. The utility of liposomal bupivacaine following dental surgery needs to be further explored.
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Two Recent Advances in Local Anesthesia: Intranasal Tetracaine/Oxymetazoline and Liposomal Bupivacaine
Current Oral Health Reports, 2017Co-Authors: Elliot V Hersh, Mana Saraghi, Paul A MooreAbstract:This paper reviews the efficacy, safety, and clinical utility of two novel formulations of local anesthetics; intranasal 3% tetracaine plus 0.05% Oxymetazoline and 1.3% liposomal bupivacaine. Intranasal 3% tetracaine/Oxymetazoline when delivered into the ipsilateral nostril of the target tooth has a success rate of 84–90% in completing a single restorative procedure from the second premolar forward. The maximum recommended dose is 18 mg tetracaine/0.3 mg Oxymetazoline (three 0.2-ml sprays). The most common adverse effects are nasal congestion and nasal runniness. Liposomal bupivacaine is administered by infiltration injection solely for postoperative pain control and appears to provide analgesic and opioid-sparing effects in knee arthroplasty, bunionectomy, hemorrhoidectomy, and laparotomy. The maximum recommended dose is 20 ml or 266 mg although for dental impaction surgery, a maximum of 10 ml or 133 mg is all that may be required. Intranasal tetracaine/Oxymetazoline is currently FDA approved only for single maxillary restorative procedures in patients weighing 88 lb or greater. Further clinical trials should include more invasive dental procedures and pediatric patients. The utility of liposomal bupivacaine following dental surgery needs to be further explored.
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intranasal tetracaine and Oxymetazoline a newly approved drug formulation that provides maxillary dental anesthesia without needles
Current Medical Research and Opinion, 2016Co-Authors: Elliot V Hersh, Mana Saraghi, Paul A MooreAbstract:AbstractBackground: An intranasal formulation of 3% tetracaine and 0.05% Oxymetazoline (Kovanaze) received FDA approval on 29 June 2016. This formulation appears to provide sufficient local anesthesia to perform routine dental restorative (filling) procedures in maxillary teeth from second premolar forward.Objectives: The aim of this paper is to provide an overview of the efficacy, pharmacokinetics and tolerability of 3% tetracaine plus 0.05% Oxymetazoline when administered intranasally.Methods: The literature was reviewed employing the search terms intranasal delivery, tetracaine, Oxymetazoline and dental local anesthesia employing the search engines PubMed Plus, Scopus and the Web of Science. The search was limited to double-blind, randomized, placebo or sham-controlled trials except for phase 1 and phase 2 pharmacokinetic and safety data.Results: A total of five relevant publications appeared in the peer reviewed literature. Three per cent tetracaine plus 0.05% Oxymetazoline produced a success rate of ...
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the cardiovascular effects and pharmacokinetics of intranasal tetracaine plus Oxymetazoline preliminary findings
Journal of the American Dental Association, 2012Co-Authors: Helen Giannakopoulos, Anthony T Cacek, Paul A Moore, Lawrence M Levin, Joli C Chou, Matthew Hutcheson, Stacey A Secreto, Elliot V HershAbstract:ABSTRACT Background The authors evaluated the cardiovascular effects and pharmacokinetics of an intranasal 3 percent tetracaine/0.05 percent Oxymetazoline spray developed to provide needle-free anesthesia of maxillary teeth. Methods The authors administered to 12 participants a proposed maximum recommended dose (MRD) (18 milligrams tetracaine/0.3 mg Oxymetazoline) as three bilateral pairs of 0.1-milliliter nasal sprays. They administered two times this dose (36 mg tetracaine/0.6 mg Oxymetazoline) as six bilateral pairs one to three weeks later. The authors recorded the patients’ heart rate, blood pressure and oxygen saturation. They drew blood samples at baseline and 15 times during the two hours after drug administration. Results Physiological measures remained fairly stable throughout the two-hour period, with small but significant decreases ( P Conclusions Intranasal tetracaine/Oxymetazoline mist generally was well tolerated in study participants. Clinical Implications The safety profile and pharmacokinetics of this intranasal formulation indicate that it appears to be generally well tolerated in patients for achieving anesthesia of the maxilla. Additional safety and efficacy data are required, particularly in patients with cardiovascular disease and other comorbidities.
Brian J Lipworth - One of the best experts on this subject based on the ideXlab platform.
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fluticasone reverses Oxymetazoline induced tachyphylaxis of response and rebound congestion
American Journal of Respiratory and Critical Care Medicine, 2010Co-Authors: S Vaidyanathan, Peter A Williamson, K L Clearie, Faisel Khan, Brian J LipworthAbstract:Rationale: Chronic use of intranasal decongestants, such as Oxymetazoline, leads to tachyphylaxis of response and rebound congestion, caused by α-adrenoceptor mediated down-regulation and desensitization of response.Objectives: We evaluated if tachyphylaxis can be reversed by intranasal fluticasone propionate, and the relative α1- and α2-adrenoceptor components of tachyphylaxis using the α1-antagonist prazosin.Methods: In a randomized, double-blind, placebo-controlled, crossover design, 19 healthy subjects received intranasal Oxymetazoline, 200 μg three times a day for 14 days, followed by the addition of fluticasone, 200 μg twice a day for a further 3 days. At Days 1, 14, and 17, participants received a single dose of oral prazosin, 1 mg, or placebo with measurements made before and 2 hours later.Measurements and Main Results: Outcomes evaluated were peak nasal inspiratory flow, nasal resistance, blood flow, and Oxymetazoline dose–response curve (DRC). On Day 14 versus Day 1, inspiratory flow decreased (...
