Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
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 (41)
- 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.
- 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)
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%)
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
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.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)
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
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
