Safety and Pharmacokinetics of Kovacaine Nasal Spray

This study has been completed.
Sponsor:
Collaborator:
University of Pennsylvania
Information provided by:
St. Renatus, LLC
ClinicalTrials.gov Identifier:
NCT01304316
First received: February 18, 2011
Last updated: February 23, 2011
Last verified: February 2011
  Purpose

The purpose of this study is to determine the pharmacokinetics/pharmacodynamics and safety of a nasal spray containing the anesthetic drug tetracaine in combination with oxymetazoline


Condition Intervention Phase
Dental Anesthesia Safety
Drug: 3% tetracaine hydrochloride plus 0.05% oxymetazoline hydrochloride
Phase 2

Study Type: Interventional
Study Design: Endpoint Classification: Safety Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Supportive Care
Official Title: Cardiovascular Changes and Tetracaine Pharmacokinetics Following Intranasal Administration of Standard and High Doses of Kovacaine Mist (Tetracaine Hydrochloride With Oxymetazoline Hydrochloride) in Healthy Volunteers

Resource links provided by NLM:


Further study details as provided by St. Renatus, LLC:

Primary Outcome Measures:
  • Change from Baseline in Blood Pressure [ Time Frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes ] [ Designated as safety issue: Yes ]
  • Change from Baseline in Pulse Rate [ Time Frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes ] [ Designated as safety issue: Yes ]
  • Change from Baseline in Oxygen Saturation Levels [ Time Frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes ] [ Designated as safety issue: Yes ]

Secondary Outcome Measures:
  • Pharmacokinetics of oxymetazoline, tetracaine, and its major metabolite parabutylaminobenzoic acid, following the intranasal administration of both the standard dose and the proposed maximum recommended dental dos of Kovacaine [ Time Frame: Baseline, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100, 110, 120 minutes ] [ Designated as safety issue: No ]
    Extra-vascular, non-compartmental analysis is used to derive pharmacokinetic parameters; estimated from observed plasma concentration values, the dose administered, the AUCs, and the terminal elimination phase rate constant for each dose group


Enrollment: 12
Study Start Date: September 2010
Study Completion Date: November 2010
Primary Completion Date: November 2010 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Kovacaine Nasal Spray Drug: 3% tetracaine hydrochloride plus 0.05% oxymetazoline hydrochloride
Each subject received the standard dose (3 sprays in each nostril with 4 minutes between each pair of sprays) followed 1 to 3 weeks later by the high dose (as 6 sprays in each nostril).
Other Name: Kovacaine Nasal Spray

Detailed Description:

The purpose of this study was to determine the safety and pharmacokinetics of the standard dose of intranasal Kovacaine Mist of 0.6 mL (18 mg tetracaine HCl with 0.3 mg oxymetazoline HCl) and a proposed maximum recommended dental dose of 1.2 mL (36 mg tetracaine HCl with 0.6 mg oxymetazoline HCl). The primary objectives were to determine if either dose significantly changed blood pressure readings (systolic and diastolic), pulse rate, or oxygen saturation levels from baseline pretreatment values and to determine the safety profile of both doses. The secondary objectives were to establish the pharmacokinetics of oxymetazoline, tetracaine, and its major metabolite (parabutylaminobenzoic acid) following the intranasal administration of both doses. Each subject received the standard dose (3 sprays in each nostril with 4 minutes between each pair of sprays) followed 1 to 3 weeks later by the high dose (as 6 sprays in each nostril).

  Eligibility

Ages Eligible for Study:   18 Years and older
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Male or female between 18 and 65 years of age
  • BMI between19 and 29 kg/m2
  • Sufficiently healthy as determined by the investigator to receive the test medications and undergo the scheduled study procedure
  • Can breathe through both nostrils
  • Females of child-bearing potential must have a negative urine pregnancy test and must have been using adequate means of birth control for at least one month prior to study entry and during the study
  • Screening BP ≤ 140/90
  • Screening SpO2 ≥ 96
  • Can understand and sign the informed consent document
  • Can communicate with the investigator
  • Can understand and comply with the requirements of the protocol.

Exclusion Criteria:

  • A clinically relevant history or presence of respiratory, thyroid, gastrointestinal, renal, hepatic, hematological, lymphatic, cardiovascular, psychiatric, neurologic, musculoskeletal, genitourinary, infective, inflammatory, immunological, dermatological, or connective tissue disease or disorder or a clinically relevant history or presence of narrow angle glaucoma and in men benign prostatic hypertrophy, Hashimoto"s Thyroiditis, lymphocytic thyroiditis, or uncontrolled diabetes
  • Clinically significant abnormalities in laboratory values
  • Clinically relevant sinus/nasal surgical history
  • Current condition, such as nasal congestion or sinus infection, that may influence responses to study medication
  • History of recurrent nose bleeds
  • History of pseudocholinesterase deficiency or previous prolonged paralysis with succinylcholine or "difficulty waking up from general anesthesia"
  • Allergic to or intolerant of tetracaine, benzocaine, other ester local anesthetics, or para-aminobenzoic acid (as found in PABA-containing sunscreens)
  • Allergic to or intolerant of oxymetazoline or preservatives found in these solutions
  • History of alcoholism and/or drug abuse
  • Have taken a monamine oxidase inhibitor, or vasopressor drug within the past 3 weeks
  • Have received or taken local anesthetics within 72 hours of the first or second treatment visits
  • Are nursing, pregnant, suspected of being pregnant, or trying to become pregnant (Females will be required to take a urine pregnancy test at each study visit to rule out pregnancy)
  • Have used any investigational drug and/or participated in any clinical trial within 30 days of baseline
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT01304316

Locations
United States, Pennsylvania
University of Pennsylvania, School of Dental Medicine
Philadelphia, Pennsylvania, United States
Sponsors and Collaborators
St. Renatus, LLC
University of Pennsylvania
Investigators
Principal Investigator: Elliot V Hersh, DMD, MS, PhD University of Pennsylvania
  More Information

No publications provided

Responsible Party: Jim Mulvahill, St. Renatus, LLC
ClinicalTrials.gov Identifier: NCT01304316     History of Changes
Other Study ID Numbers: SR 2-02
Study First Received: February 18, 2011
Last Updated: February 23, 2011
Health Authority: United States: Food and Drug Administration

Additional relevant MeSH terms:
Tetracaine
Oxymetazoline
Phenylephrine
Anesthetics, Local
Anesthetics
Central Nervous System Depressants
Physiological Effects of Drugs
Pharmacologic Actions
Sensory System Agents
Peripheral Nervous System Agents
Central Nervous System Agents
Therapeutic Uses
Adrenergic alpha-Agonists
Adrenergic Agonists
Adrenergic Agents
Neurotransmitter Agents
Molecular Mechanisms of Pharmacological Action
Sympathomimetics
Autonomic Agents
Nasal Decongestants
Vasoconstrictor Agents
Cardiovascular Agents
Respiratory System Agents
Cardiotonic Agents
Mydriatics
Adrenergic alpha-1 Receptor Agonists
Protective Agents

ClinicalTrials.gov processed this record on August 21, 2014