Tetrahydrozoline is an intranasal and ophthalmic topical vasoconstrictor. It is administered intranasally to treat nasal congestion associated with acute or chronic rhinitis, sinusitis, the common cold, and hay fever and other allergies. The effectiveness of xylometazoline for relieving nasal congestion and its adverse effect profile are similar to other imidazoline derivatives. Excessive or prolonged nasal use can cause nasal mucosa irritation; nasal use should generally not exceed 3 consecutive days since some degree of rebound congestion usually results. Tetrahydrozoline is administered ophthalmically to relieve redness of the eye due to minor ocular irritants. This drug was approved by the FDA in 1954.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Inhalation Administration
Intranasal Inhalation Administration
-To avoid the spread of infection, do not use the container for more than one person.
-Bedtime instillation usually assures sleep undisturbed by the need for additional medication before morning, or by insomnia from central stimulation.
Tyzine Nasal Drops:
-Instillation of the nose drops can be most conveniently accomplished with the patient in the lateral head-low position.
Tyzine Nasal Solution:
-The spray should be administered with the head held upright. To spray, squeeze bottle quickly and firmly and sniff briskly.
Ophthalmic Administration
-For topical application to the eye only.
-Wash hands before and after use. Tilt the head back slightly and pull the lower eyelid down with the index finger. Squeeze the prescribed number of drops into the conjunctival sac and gently close eyes for 1-2 minutes. Do not blink.
-Care should be taken to avoid contamination. Do not touch the tip of the dropper to the eye, fingertips, or other surface.
-Do not share tetrahydrozoline ophthalmic drops between patients.
Local application of tetrahydrozoline nasal solution can be associated with nasal irritation (i.e., burning or stinging of the mucosa), sneezing or nasal dryness. Rebound nasal congestion can also occur, and is characterized by chronic swelling of the nasal mucosa resulting in chronic redness, swelling and rhinitis .
Systemic sympathomimetic effects including headache, drowsiness, weakness, tremor, light-headedness, insomnia, and palpitations can occasionally occur after intranasal administration of tetrahydrozoline.
Ocular adverse reactions associated with tetrahydrozoline ophthalmic solution include ocular irritation (burning or stinging), ocular pain, and changes in vision (e.g., blurred vision or visual impairment). Temporary enlargement of the pupils (mydriasis) may also occur following ophthalmic administration of tetrahydrozoline .
Serious and life-threatening adverse events requiring hospitalization have been reported to the FDA after children <=5 years of age accidentally ingested over-the-counter (OTC) tetrahydrozoline ophthalmic drops and nasal sprays. No deaths were reported; however, events such as nausea, vomiting, lethargy, sinus tachycardia, respiratory depression, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, and coma have occurred. Serious adverse events can occur following ingestion of only a small amount (1-2 ml) in young children. Since most of these OTC products do not contain child-resistant closures, it is imperative that patients store these products out of reach of children. If a child accidentally swallows these drops, call the National Capital Poison Center (1-800-222-1222) and seek emergency medical attention immediately.
Ophthalmic solutions of tetrahyrozoline may exacerbate closed-angle glaucoma and are contraindicated for use in these patients.
Tetrahydrozoline 0.1% nasal solution is contraindicated in neonates, infants and children less than 6 years of age. Tetrahydrozoline 0.05% nasal solution is not to be used for pediatric patients less than 2 years of age. Safety and efficacy of tetrahydrozoline ophthalmic solution products have not been established in pediatric patients less than 6 years of age.
Tetrahydrozoline nasal solution should not be combined with MAOI therapy. The combination of an MAOI and a sympathomimetic drug may result in hypertensive crisis.
Contact lenses should be removed prior to ophthalmic administration of tetrahydrozoline.
Tetrahydrozoline should be used cautiously in patients with cardiovascular disease (e.g., coronary artery disease or hypertension).
Tetrahydrozoline should be used cautiously in patients with metabolic-endocrine diseases (e.g., hyperthyroidism or diabetes mellitus).
Tetrahydrozoline use is likely best avoided in pregnancy due to the lack of data regarding safety to the fetus. Animal reproduction studies have not been conducted with tetrahydrozoline nasal or ophthalmic products. It is also not known whether the drug can cause fetal harm when administered during pregnancy or if these products can affect reproduction capacity. Pediatric patients are known to be particularly sensitive to the toxic effects of the imidazolines such as when there is systemic absorption of nasal or ophthalmic tetrahydrozoline.
While it is not known whether tetrahydrozoline is secreted in human milk or if it affects milk production, tetrahydrozoline nasal solution is considered to be compatible during breast-feeding.
For the relief of redness of the eye due to minor eye irritations or xerophthalmia:
Ophthalmic dosage (tetrahydrozoline 0.05% ophthalmic solution):
Adults: Instill 1 to 2 drops of 0.05% ophthalmic solution into the eye(s) up to 4 times per day.
Children and Adolescents 6 to 17 years: Instill 1 to 2 drops of 0.05% ophthalmic solution into the eye(s) up to 4 times per day.
For symptomatic relief of nasal congestion and congestion of the nasopharyngeal mucosa:
Intranasal dosage (Tyzine 0.1% nasal spray or drops):
Adults: 3 to 4 sprays (or 2 to 4 drops) in each nostril as needed, never more often than every 3 hours. Less frequent administration is usually sufficient as relief is maintained for 4 to 8 hours.
Children and Adolescents 6 to 17 years: 3 to 4 sprays (or 2 to 4 drops) in each nostril as needed, never more often than every 3 hours. Less frequent administration is usually sufficient as relief is maintained for 4 to 8 hours.
Intranasal dosage (Tyzine 0.05% nasal drops):
Children 2 to 6 years: 2 to 3 drops in each nostril as needed, never more often than every 3 hours. Less frequent administration is usually sufficient as relief is maintained for 4 to 6 hours.
Maximum Dosage Limits:
-Adults
8 drops/day 0.05% ophthalmic solution in each affected eye; 32 sprays/day 0.1% nasal spray in each nostril; 32 drops/day 0.1% nasal drops in each nostril.
-Geriatric
8 drops/day 0.05% ophthalmic solution in each affected eye; 32 sprays/day 0.1% nasal spray in each nostril; 32 drops/day 0.1% nasal drops in each nostril.
-Adolescents
8 drops/day 0.05% ophthalmic solution in each affected eye; 32 sprays/day 0.1% nasal spray in each nostril; 32 drops/day 0.1% nasal drops in each nostril.
-Children
6 to 12 years: 8 drops/day 0.05% ophthalmic solution in each affected eye; 32 sprays/day 0.1% nasal spray in each nostril; 32 drops/day 0.1% nasal drops in each nostril.
2 to 5 years: 24 drops/day 0.05% nasal drops in each nostril.
Less than 2 years: Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
No dosage adjustments are needed.
Patients with Renal Impairment Dosing
No dosage adjustments are needed.
*non-FDA-approved indication
Isocarboxazid: (Major) In general, tetrahydrozoline should not be combined with monoamine oxidase inhibitors (MAOIs). The combination of an MAOI and a sympathomimetic drug, including those given via nasal or ophthalmic routes, may result in hypertensive crisis. Avoid use during and up to 2 weeks following discontinuation of the MAOI. Consider alternative treatments for the patient's condition.
Linezolid: (Moderate) Linezolid may enhance the hypertensive effect of tetrahydrozoline. Closely monitor for increased blood pressure during coadministration. Linezolid is an antibiotic that is also a weak, reversible nonselective inhibitor of monoamine oxidase (MAO). Therefore, linezolid has the potential for interaction with adrenergic agents, such as tetrahydrozoline.
Monoamine oxidase inhibitors: (Major) In general, tetrahydrozoline should not be combined with monoamine oxidase inhibitors (MAOIs). The combination of an MAOI and a sympathomimetic drug, including those given via nasal or ophthalmic routes, may result in hypertensive crisis. Avoid use during and up to 2 weeks following discontinuation of the MAOI. Consider alternative treatments for the patient's condition.
Nafarelin: (Moderate) If use of a topical nasal decongestants is necessary during therapy with intranasal nafarelin, the decongestant should not be used for at least 2 hours after nafarelin is administered.
Nicotine: (Minor) Vasoconstricting nasal decongestants such as oxymetazoline, phenylephrine, pseudoephedrine, and tetrahydrozoline prolong the time to peak effect of nasally administered nicotine (i.e., nicotine nasal spray); however, no dosage adjustments are recommended.
Phenelzine: (Major) In general, tetrahydrozoline should not be combined with monoamine oxidase inhibitors (MAOIs). The combination of an MAOI and a sympathomimetic drug, including those given via nasal or ophthalmic routes, may result in hypertensive crisis. Avoid use during and up to 2 weeks following discontinuation of the MAOI. Consider alternative treatments for the patient's condition.
Rasagiline: (Moderate) The concomitant use of rasagiline and sympathomimetics was not allowed in clinical studies; therefore, caution is advised during concurrent use of rasagiline and sympathomimetics including non-prescription nasal and ophthalmic decongestants. Although sympathomimetics are contraindicated for use with other non-selective monoamine oxidase inhibitors (MAOIs), hypertensive reactions generally are not expected to occur during concurrent use with rasagiline because of the selective monoamine oxidase-B (MAO-B) inhibition of rasagiline at manufacturer recommended doses. One case of elevated blood pressure has been reported in a patient during concurrent use of the recommended dose of rasagiline and ophthalmic tetrahydrozoline. It should be noted that the MAO-B selectivity of rasagiline decreases as the dose increases above the recommended daily dose and interactions with sympathomimetics may be more likely to occur at these higher doses.
Selegiline: (Moderate) Monitor blood pressure for hypertension during concomitant use of selegiline and tetrahydrozoline. Although tetrahydrozoline is only used by ophthalmic and nasal routes, the use of these drugs together may produce substantial elevations in blood pressure. If a hypertensive crisis occurs, selegiline should be discontinued immediately and therapy to lower blood pressure should be instituted immediately.
Tranylcypromine: (Major) In general, tetrahydrozoline should not be combined with monoamine oxidase inhibitors (MAOIs). The combination of an MAOI and a sympathomimetic drug, including those given via nasal or ophthalmic routes, may result in hypertensive crisis. Avoid use during and up to 2 weeks following discontinuation of the MAOI. Consider alternative treatments for the patient's condition.
Zavegepant: (Moderate) Administer intranasal decongestants at least 1 hour after zavegepant administration. Simultaneous coadministration may decrease zavegepant absorption which may reduce its efficacy.
Tetrahydrozoline stimulates alpha-adrenergic receptors. Tetrahydrozoline possesses vasoconstrictor and decongestant actions when applied to nasal mucosa, resulting in vasoconstriction of the smaller arterioles of the nasal passages. This action promotes drainage and improves ventilation. Ophthalmic administration causes vasoconstriction of conjunctival blood vessels thereby providing relief from minor eye irritations.
Tetrahydrozoline is administered ophthalmically and intranasally. Information on the absorption, distribution and elimination of the drug is not available.
-Route-Specific Pharmacokinetics
Other Route(s)
Ophthalmic Route
Following topical application of tetrahydrozoline hydrochloride solutions to the conjunctiva, local vasoconstriction usually occurs within a few minutes and may persist for 4-8 hours. Occasionally, enough tetrahydrozoline may be absorbed to produce systemic effects.
Intranasal Route
Following intranasal topical application of tetrahydrozoline hydrochloride solutions, local vasoconstriction usually occurs within a few minutes and may persist for 4-8 hours. Occasionally, enough tetrahydrozoline may be absorbed to produce systemic effects.