tetracaine/oxymetazoline intranasal (Rx)

Brand and Other Names:Kovanaze
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tetracaine/oxymetazoline intranasal

intranasal solution

  • (5.27mg/0.088mg)/0.2mL (equivalent to 6mg tetracaine HCl and 0.1mg oxymetazoline HCl)

Dental Anesthesia

Indicated for regional anesthesia when performing a restorative procedure on Teeth 4-13 and A-J

2 sprays (0.2 mL/spray) intranasally administered 4-5 minutes apart

Administer in the nostril ipsilateral 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 (0.2 mL) if adequate anesthesia to initiate the dental procedure has not been achieved 10 minutes after the second spray

Also see Administration

Dosage Forms & Strengths

tetracaine/oxymetazoline intranasal

intranasal solution

  • (5.27mg/0.088mg)/0.2mL (equivalent to 6mg tetracaine HCl and 0.1mg oxymetazoline HCl)

Dental Anesthesia

Indicated for regional anesthesia when performing a restorative procedure on Teeth 4-13 and A-J in children who weigh ≥40 kg

2 sprays (0.2 mL/spray) intranasally administered 4-5 minutes apart

Administer in the nostril ipsilateral to the maxillary tooth on which the dental procedure will be performed

Initiate the dental procedure 10 minutes after the second spray

Also see Administration

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Interactions

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              Serious - Use Alternative (2)

              • bupivacaine implant

                tetracaine, bupivacaine implant. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid additional local anesthetic administration within 96 hr following bupivacaine implantation. If use of additional local anesthetics is unavoidable based on clinical need, monitor for neurologic and cardiovascular effects related to local anesthetic systemic toxicity.

              • isocarboxazid

                isocarboxazid increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Avoid or Use Alternate Drug. MAOIs cause norepinephrine accumulation within adrenergic neurons. Significant hypertension can result if coadministered with alpha1 agonists.

              Monitor Closely (42)

              • acetaminophen

                tetracaine, acetaminophen. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • acetaminophen IV

                tetracaine, acetaminophen IV. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • acetaminophen rectal

                tetracaine, acetaminophen rectal. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • amitriptyline

                amitriptyline increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. TCAs inhibit norepinephrine uptake in adrenergic neurons, thereby increasing synaptic norepinephrine levels. Coadministration with alpha1 agonists may cause increased adrenergic receptor stimulation. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use alternant anesthetic in patients taking TCAs.

              • amoxapine

                amoxapine increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. TCAs inhibit norepinephrine uptake in adrenergic neurons, thereby increasing synaptic norepinephrine levels. Coadministration with alpha1 agonists may cause increased adrenergic receptor stimulation. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use alternant anesthetic in patients taking TCAs.

              • amyl nitrite

                tetracaine, amyl nitrite. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • azelastine

                oxymetazoline intranasal, azelastine. Other (see comment). Modify Therapy/Monitor Closely. Comment: Oxymetazoline has been known to slow the rate, but not affect the extent of absorption of concomitantly administered intranasal products. Do not administer other intranasal products with oxymetazoline intranasal.

              • bupivacaine implant

                tetracaine, bupivacaine implant. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Local anesthetics may increase the risk of developing methemoglobinemia when concurrently exposed to drugs that also cause methemoglobinemia.

              • chloroquine

                tetracaine, chloroquine. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • clomipramine

                clomipramine increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. TCAs inhibit norepinephrine uptake in adrenergic neurons, thereby increasing synaptic norepinephrine levels. Coadministration with alpha1 agonists may cause increased adrenergic receptor stimulation. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use alternant anesthetic in patients taking TCAs.

              • cromolyn sodium, intranasal

                oxymetazoline intranasal, cromolyn sodium, intranasal. Other (see comment). Modify Therapy/Monitor Closely. Comment: Oxymetazoline has been known to slow the rate, but not affect the extent of absorption of concomitantly administered intranasal products. Do not administer other intranasal products with oxymetazoline intranasal.

              • dapsone

                tetracaine, dapsone. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • desipramine

                desipramine increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. TCAs inhibit norepinephrine uptake in adrenergic neurons, thereby increasing synaptic norepinephrine levels. Coadministration with alpha1 agonists may cause increased adrenergic receptor stimulation. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use alternant anesthetic in patients taking TCAs.

              • doxepin

                doxepin increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. TCAs inhibit norepinephrine uptake in adrenergic neurons, thereby increasing synaptic norepinephrine levels. Coadministration with alpha1 agonists may cause increased adrenergic receptor stimulation. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use alternant anesthetic in patients taking TCAs.

              • hyaluronidase

                hyaluronidase, tetracaine. Other (see comment). Use Caution/Monitor. Comment: Hyaluronidase hastens the onset of local analgesia and reduces swelling, but increases systemic absorption of anesthetic. This decreases the duration of action and increases incidence of systemic reaction.

              • imipramine

                imipramine increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. TCAs inhibit norepinephrine uptake in adrenergic neurons, thereby increasing synaptic norepinephrine levels. Coadministration with alpha1 agonists may cause increased adrenergic receptor stimulation. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use alternant anesthetic in patients taking TCAs.

              • ipratropium intranasal

                oxymetazoline intranasal, ipratropium intranasal. Other (see comment). Modify Therapy/Monitor Closely. Comment: Oxymetazoline has been known to slow the rate, but not affect the extent of absorption of concomitantly administered intranasal products. Do not administer other intranasal products with oxymetazoline intranasal.

              • isosorbide dinitrate

                tetracaine, isosorbide dinitrate. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • isosorbide mononitrate

                tetracaine, isosorbide mononitrate. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nadolol

                nadolol increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. When beta-2 receptors are antagonized by nonselective beta blockers, alpha1 vasoconstriction may be unopposed, thus increasing hypertensive effect. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use an alternant anesthetic in patients taking nonselective beta blockers.

              • nitrofurantoin

                tetracaine, nitrofurantoin. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nitroglycerin IV

                tetracaine, nitroglycerin IV. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nitroglycerin PO

                tetracaine, nitroglycerin PO. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nitroglycerin sublingual

                tetracaine, nitroglycerin sublingual. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nitroglycerin topical

                tetracaine, nitroglycerin topical. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nitroglycerin transdermal

                tetracaine, nitroglycerin transdermal. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nitroglycerin translingual

                tetracaine, nitroglycerin translingual. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nitroprusside sodium

                tetracaine, nitroprusside sodium. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • nortriptyline

                nortriptyline increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. TCAs inhibit norepinephrine uptake in adrenergic neurons, thereby increasing synaptic norepinephrine levels. Coadministration with alpha1 agonists may cause increased adrenergic receptor stimulation. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use alternant anesthetic in patients taking TCAs.

              • olopatadine intranasal

                oxymetazoline intranasal, olopatadine intranasal. Other (see comment). Modify Therapy/Monitor Closely. Comment: Oxymetazoline has been known to slow the rate, but not affect the extent of absorption of concomitantly administered intranasal products. Do not administer other intranasal products with oxymetazoline intranasal.

              • penbutolol

                penbutolol increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. When beta-2 receptors are antagonized by nonselective beta blockers, alpha1 vasoconstriction may be unopposed, thus increasing hypertensive effect. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use an alternant anesthetic in patients taking nonselective beta blockers.

              • phenobarbital

                tetracaine, phenobarbital. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • phenytoin

                tetracaine, phenytoin. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • primaquine

                tetracaine, primaquine. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • propranolol

                propranolol increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. When beta-2 receptors are antagonized by nonselective beta blockers, alpha1 vasoconstriction may be unopposed, thus increasing hypertensive effect. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use an alternant anesthetic in patients taking nonselective beta blockers.

              • protriptyline

                protriptyline increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. TCAs inhibit norepinephrine uptake in adrenergic neurons, thereby increasing synaptic norepinephrine levels. Coadministration with alpha1 agonists may cause increased adrenergic receptor stimulation. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use alternant anesthetic in patients taking TCAs.

              • quinine

                tetracaine, quinine. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • safinamide

                oxymetazoline intranasal and safinamide both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor. Monitor patients for hypertension if safinamide is prescribed concomitantly with prescription or nonprescription sympathomimetics, including nasal, oral, or ophthalmic decongestants and cold remedies.

              • sotalol

                sotalol increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. When beta-2 receptors are antagonized by nonselective beta blockers, alpha1 vasoconstriction may be unopposed, thus increasing hypertensive effect. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use an alternant anesthetic in patients taking nonselective beta blockers.

              • sulfadiazine

                tetracaine, sulfadiazine. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • sulfisoxazole

                tetracaine, sulfisoxazole. Other (see comment). Use Caution/Monitor. Comment: Monitor for signs of methemoglobinemia when methemoglobin-inducing drugs are coadministered.

              • timolol

                timolol increases effects of oxymetazoline intranasal by pharmacodynamic synergism. Use Caution/Monitor. When beta-2 receptors are antagonized by nonselective beta blockers, alpha1 vasoconstriction may be unopposed, thus increasing hypertensive effect. When oxymetazoline is combined with intranasal tetracaine for dental anesthesia, avoid or use an alternant anesthetic in patients taking nonselective beta blockers.

              Minor (0)

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                Adverse Effects

                >10%

                Rhinorrhea (52%)

                Nasal congestion (32%)

                Nasal discomfort (26%)

                Oropharyngeal pain (14%)

                Lacrimation increased (13%)

                1-10%

                Intranasal hypoesthesia (10%)

                Pharyngeal hypoesthesia (10%)

                Headache (10%)

                Throat irritation (9%)

                Dysgeusia (8%)

                Rhinalgia (6%)

                Systolic BP increased (5%)

                Sneezing (4%)

                Diastolic BP increased (3%)

                Hypertension (3%)

                Bradycardia (3%)

                Sinus headache (3%)

                Dizziness (3%)

                Sensory disturbance (2%)

                Epistaxis (2%)

                Nasal dryness (2%)

                Oral discomfort (2%)

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                Warnings

                Contraindications

                History of allergy to or intolerance of tetracaine, benzyl alcohol, other ester local anesthetics, p-aminobenzoic acid (PABA), oxymetazoline, or any other component of the product

                Cautions

                May increase blood pressure; not studied in adults with BP >150/100 mmHg or those with inadequately controlled active thyroid disease

                Epistaxis reported; do not use in patients with a history of frequent nose bleeds (ie, ≥5/month)

                May cause dysphagia

                Tetracaine may cause methemoglobinemia (metHB), especially if coadministered with other drugs that also cause metHB; use in patients with history of congenital or idiopathic metHB is not advised; initial signs and symptoms of metHB (which may be delayed for up to several hours following exposure) are characterized by a slate grey cyanosis seen in, e.g., buccal mucous membranes, lips and nail beds; in severe cases, symptoms may include central cyanosis, headache, lethargy, dizziness, fatigue, syncope, dyspnea, CNS depression, seizures, dysrhythmia and shock

                Allergic or anaphylactic reactions reported, characterized by urticaria, angioedema, bronchospasm, and shock; if an allergic reaction occurs, seek emergency help immediately (see Contraindications)

                Methemoglobinemia

                • Use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly; patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition
                • Advise patients or caregivers to seek immediate medical attention if patient experiences the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue; discontinue Bicillin C-R and any other oxidizing agents; depending on severity of signs and symptoms, patients may respond to supportive care, including oxygen therapy and hydration; a more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen

                Drug interaction overview

                • Coadministration with MAOIs, nonselective beta adrenergic antagonists, or TCAs may cause hypertension and is not recommended; select an alternant anesthetic if these drugs cannot be discontinued
                • Do not use with other oxymetazoline-containing products (eg, Afrin); discontinue other intranasal oxymetazoline products 24 hr before use of tetracaine/oxymetazoline intranasal
                • Oxymetazoline is known to slow the rate, but not the extent of absorption of other intranasal drugs; do not coadminister with other intranasal products
                • Tetracaine may cause metHB, particularly if coadministered with other drugs that cause metHB (eg, sulfonamides, acetaminophen, acetanilide, aniline dyes, benzocaine, chloroquine, dapsone, naphthalene, nitrates and nitrites, nitrofurantoin, nitroglycerin, nitroprusside, pamaquine, p- aminosalicylic acid, phenacetin, phenobarbital, phenytoin, primaquine, quinine); monitor carefully for signs of metHB
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                Pregnancy & Lactation

                Pregnancy

                Limited published data on tetracaine use in pregnant women are not sufficient to inform any risks

                Published epidemiologic studies of nasal oxymetazoline used as a decongestant during pregnancy do not identify a consistent association with any specific malformation or pattern of malformations

                Lactation

                There are no data on the presence of tetracaine, oxymetazoline, or their metabolites in human milk, the effects on the breastfed infant, or the effects on milk production

                Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Tetracaine: Local anesthetic of the ester type and exerts its activity by blocking sodium ion channels required for the initiation and conduction of neuronal impulses

                Oxymetazoline: Imidazoline derivative with sympathomimetic activity; believed to be a mixed alpha1/2-adrenoceptor agonist and, by stimulating adrenergic receptors, it elicits vasoconstriction of dilated arterioles and reduces nasal blood flow

                Absorption

                Peak plasma concentration: 465 ng/mL (tetracaine); 1.78 ng/mL (oxymetazoline)

                Peak plasma time: 20 min (tetracaine); 5 min (oxymetazoline) AUC: 973 n·gh/mL (tetracaine); 4.24 n·gh/mL (oxymetazoline)

                Distribution

                Protein bound: 75-85% (tetracaine)

                Metabolism

                Tetracaine is rapidly and thoroughly cleaved by esterases in plasma and other tissues to PBBA and dimethylaminoethanol

                Oxymetazoline is converted to a glucuronide conjugate in vitro by UGT1A9

                Elimination

                Half-life: 2.6 hr (PBBA); 5.2 hr (oxymetazoline)

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                Administration

                Intranasal Administration

                For intranasal use only

                Administer in the nostril ipsilateral (same side) to the maxillary tooth on which the dental procedure will be performed

                Wait 10 minutes after administration to perform a test drill to confirm that the tooth involved is anesthetized

                A patient may not experience the same sensations of numbness or tingling of the lips and cheeks associated with injectable dental anesthetics

                Storage

                Store between 2-8°C (36-46°F); excursions permitted between 0-15°C (32-59°F)

                Discard any unused solution

                Do not use if drug is left out at room temperature for >5 days

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                Formulary

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                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.