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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            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

            FormularyPatient Discounts

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            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.
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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.