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Tetracaine and Oxymetazoline

Pronunciation

(TET ra kane & oks i met AZ oh leen)

Index Terms

  • Kovanaze
  • Oxymetazoline and Tetracaine
  • Tetracaine Hydrochloride and Oxymetazoline Hydrochloride

Pharmacologic Category

  • Adrenergic Agonist Agent
  • Imidazoline Derivative
  • Local Anesthetic

Pharmacology

Tetracaine: Local ester anesthetic that blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction.

Oxymetazoline: Imidazoline derivative with sympathomimetic activity that stimulates alpha-adrenergic receptors in the arterioles of the nasal mucosa to produce vasoconstriction.

Time to Peak

Median:

Pediatric patients 4 to 15 years of age: Oxymetazoline: ~10 to 30 minutes; Tetracaine metabolite (PBBA): ~20 to 30 minutes.

Adults: Oxymetazoline: 5 minutes; Tetracaine metabolite (PBBA): 20 minutes.

Half-Life Elimination

Pediatric patients 4 to 15 years of age: Oxymetazoline: ~1.6 to 4.3 hours; Tetracaine metabolite p-butylaminobenzoic acid (PBBA): ~1.6 to 2.8 hours.

Adults: Oxymetazoline: ~5.2 hours; Tetracaine metabolite (PBBA): ~2.6 hours.

Use: Labeled Indications

Anesthesia, dental: Regional anesthesia when performing a restorative procedure on teeth 4-13 and A-J in adults and children who weigh 40 kg or more.

Contraindications

Hypersensitivity to or intolerance of tetracaine, benzyl alcohol, other ester local anesthetics, p-aminobenzoic acid (PABA), oxymetazoline, or any component of the formulation.

Dosing: Adult

Anesthesia, dental: Intranasal: 2 sprays administered 4 to 5 minutes apart in the nostril ipsilateral (same side) to the maxillary tooth on which the dental procedure will be performed. Initiate the dental procedure 10 minutes after the second spray. May administer 1 additional spray 10 minutes after the second initial spray if inadequate anesthesia.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Anesthesia, dental: Children and Adolescents ≥3 years and ≥40 kg: Intranasal: 2 sprays administered 4 to 5 minutes apart in the nostril ipsilateral (same side) to the maxillary tooth on which the dental procedure will be performed. Initiate the dental procedure 10 minutes after the second spray.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer′s labeling (has not been studied).

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer′s labeling (has not been studied); use with caution in patients with severe impairment.

Administration

For intranasal use only. Administer ipsilateral (same side) to the maxillary tooth on which the dental procedure will be performed. Wait 10 minutes following administration to perform a test drill to confirm that the tooth involved is anesthetized. Avoid use with other intranasal products, including other oxymetazoline-containing nasal sprays. Discontinue oxymetazoline-containing products 24 hours prior to administration of tetracaine/oxymetazoline.

Storage

Store between 2°C and 8°C (36°F and 46°F); excursions permitted between 0°C and 15°C (32°F and 59°F). Discard any unused solution. Do not use if kept at room temperature for >5 days.

Drug Interactions

Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. Monitor therapy

AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy

Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy

Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Monitor therapy

Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Monitor therapy

Ergot Derivatives: May enhance the hypertensive effect of Alpha1-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. Avoid combination

FentaNYL: Alpha1-Agonists may decrease the serum concentration of FentaNYL. Specifically, fentanyl nasal spray serum concentrations may decrease and onset of effect may be delayed. Monitor therapy

Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Avoid combination

Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Consider therapy modification

MAO Inhibitors: May enhance the hypertensive effect of Alpha1-Agonists. While linezolid is expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to linezolid specific monographs for details. Exceptions: Linezolid; Tedizolid. Avoid combination

Methemoglobinemia Associated Agents: Tetracaine (Topical) may enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Monitor therapy

Nitric Oxide: May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when nitric oxide is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine. Monitor therapy

Prilocaine: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine in infants receiving such agents. Monitor therapy

Sodium Nitrite: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Sodium Nitrite. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Monitor therapy

Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy

Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy

Tricyclic Antidepressants: May enhance the vasopressor effect of Alpha1-Agonists. Tricyclic Antidepressants may diminish the vasopressor effect of Alpha1-Agonists. Monitor therapy

Warnings/Precautions

Concerns related to adverse effects:

• Anaphylactic Reactions: Allergic or anaphylactoid reactions, including urticaria, angioedema, bronchospasm, and shock may occur.

• Dysphagia: Has been reported; monitor patients for dysphagia.

• Epistaxis: Has been reported. Avoid use in patients with a history of frequent nose bleeds (≥5 per month); if administration cannot be avoided, monitor patients with frequent nose bleeds carefully.

• Hypertension: May occur; monitor patients for increased blood pressure. Use is not recommended in patients with uncontrolled hypertension.

• Methemoglobinemia: Tetracaine may cause methemoglobinemia, particularly when used in combination with other drugs associated with drug-induced methemoglobin (eg, acetaminophen, acetanilide, aniline dyes, benzocaine, chloroquine, dapsone, naphthalene, nitrates and nitrites, nitrofurantoin, nitroglycerin, nitroprusside, pamaquine, p-aminosalicylic acid, phenacetin, phenobarbital, phenytoin, primaquine, quinine, sulfonamides). Use with caution in patients with glucose-6-phosphate dehydrogenase deficiency; use is not recommended in patients with a history of congenital or idiopathic methemoglobinemia.

Disease-related concerns:

• Hepatic impairment: Patients with severe hepatic impairment may be at greater risk of developing toxic plasma concentrations of tetracaine due to inability to metabolize local anesthetics. Monitor patients with hepatic disease for signs of local anesthetic toxicity.

• Pseudocholinesterase deficiency: Patients with pseudocholinesterase deficiency may be at a greater risk of developing toxic plasma concentrations of tetracaine due to inability to metabolize local anesthetics. Monitor for signs of local anesthetic toxicity.

• Thyroid disease: Use is not recommended in patients with inadequately controlled active thyroid disease.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP 1997; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer′s labeling.

Other warnings/precautions:

• Appropriate use: Avoid use with other intranasal products, including other oxymetazoline-containing nasal sprays. Discontinue oxymetazoline-containing products 24 hours prior to administration of tetracaine/oxymetazoline.

Monitoring Parameters

Blood pressure; monitor for dysphagia, epistaxis, and signs of local anesthetic toxicity, especially in patients with hepatic impairment or pseudocholinesterase deficiency.

Pregnancy Considerations

Adverse events have been observed in some animal reproduction studies using this combination subcutaneously. See individual monographs.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nosebleed, rhinorrhea, rhinitis, pharyngitis, throat pain, watery eyes, headache, or change in taste. Have patient report immediately to prescriber severe headache, dizziness, passing out, vision changes, difficulty swallowing, or signs of methemoglobinemia (blue or gray color of the lips, nails, or skin; abnormal heartbeat; seizures; severe dizziness or passing out; severe headache; fatigue; loss of strength and energy; or shortness of breath) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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