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Tetracaine and Oxymetazoline

Medically reviewed by Drugs.com. Last updated on Sep 19, 2020.

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.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

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.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

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

Bupivacaine: Local Anesthetics may enhance the adverse/toxic effect of Bupivacaine. Management: Avoid using any additional local anesthetics within 96 hours after insertion of the bupivacaine implant (Xaracoll). Monitor therapy

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

Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Consider therapy modification

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. Avoid combination

Esketamine: Decongestants (Nasally Administered) may diminish the therapeutic effect of Esketamine. Management: Patients who require a nasal decongestant on an esketamine dosing day should administer the nasal decongestant at least 1 hour before esketamine. Consider therapy modification

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

Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Monitor therapy

Iobenguane Radiopharmaceutical Products: Alpha1-Agonists may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer these drugs until at least 7 days after each iobenguane dose. 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

Local Anesthetics: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Monitor therapy

Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Monitor therapy

Monoamine Oxidase 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. Avoid combination

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

Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Management: Concomitant use of ozanimod with sympathomimetic agents is not recommended. If combined, monitor patients closely for the development of hypertension, including hypertensive crises. Consider therapy modification

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

Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. 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 therapeutic effect of Alpha1-Agonists. Tricyclic Antidepressants may diminish the therapeutic effect of Alpha1-Agonists. Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Also see individual agents.

>10%:

Ophthalmic: Increased lacrimation (13%)

Respiratory: Rhinorrhea (52%), nasal congestion (32%), nasal discomfort (26%), oropharyngeal pain (14%)

1% to 10%:

Cardiovascular: Increased systolic blood pressure (5%), bradycardia (3%), hypertension (3%), increased diastolic blood pressure (3%)

Central nervous system: Headache (10%), hypoesthesia (intranasal: 10%; pharyngeal: 10%), nasal cavity pain (6%), dizziness (3%), abnormal sensory symptoms (2%)

Gastrointestinal: Dysgeusia (8%), oral discomfort (2%), dysphagia (1%)

Respiratory: Throat irritation (9%), sneezing (4%), nasal mucosa ulcer (3%), sinus headache (3%), dry nose (2%), epistaxis (2%)

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: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).

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.

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

What is this drug used for?

• It is used before dental care to numb the area.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Nosebleed

• Runny nose

• Stuffy nose

• Sore throat

• Throat pain

• Watery eyes

• Headache

• Change in taste

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Severe headache

• Dizziness

• Passing out

• Vision changes

• Trouble swallowing

• Methemoglobinemia like 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.

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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