Oxymetazoline Hcl - Dosage and Warnings

Overview

Oxymetazoline hydrochloride is an imidazole derivative and a potent, direct-acting alpha-adrenergic agonist with affinity to alpha1- and alpha2-adrenoceptors. Oxymetazoline hydrochloride is available in various forms with various clinical implications. The topical formulation of the medication is used for treating persistent facial redness in adults.

As an effective decongestant, Oxymetazoline hydrochloride is available in over-the-counter intranasal sprays. It is used to relieve nasal and sinus congestion caused by various conditions, like the common cold, upper respiratory allergies, and hay fever. Oxymetazoline hydrochloride and tetracaine combination intranasal spray are used for regional anesthesia during dental procedures in children and adults.

In July 2020, the Food and Drug Administration approved an ophthalmic formulation of the drug Oxymetazoline hydrochloride in adults who have acquired blepharoptosis or ptosis. It is the first FDA-approved medical treatment for this medical condition.

Dosage and Administration-

For nasal congestion or stuffiness:

• Adults and children six years and older - Two or three drops or sprays of 0.05 percent solution in each nostril every 10 to 12 hours. Use it at most two times in twenty-four hours.

• Children up to 6 years of age - The doctor should determine usage and dose.

What Is the Clinical Use of Oxymetazoline Hydrochloride Nasal Spray?

It temporarily relieves nasal congestion due to the following:

• Common cold.

• Hay fever.

• Upper respiratory allergies.

• It temporarily relieves sinus congestion and pressure.

• It shrinks swollen nasal membranes to breathe more freely.

Warnings

• Oxymetazoline hydrochloride is not recommended for children unless advised by a doctor.

• Avoid taking Oxymetazoline hydrochloride if a person has narrow-angle glaucoma or has undergone recent trans-nasal surgery.

• If a patient has diabetes, heart disease, high blood pressure, or hyperthyroidism, inform the doctor before taking Oxymetazoline hydrochloride.

• Consult a doctor if a person has liver or kidney problems before using Oxymetazoline hydrochloride.

Use in Specific Population-

• Allergies- If a patient has any unusual allergy or allergy to food, preservatives, or dyes, they should inform the doctor before using Oxymetazoline.

• Pediatric- Children can be especially susceptible to the effects of Oxymetazoline hydrochloride, which may increase the chance of side effects during treatment.

• Geriatric- Many medicines have not been tested on older people. Therefore, it is yet to be known whether Oxymetazoline works the same way in younger adults or if they cause any different side effects or problems in older people.

• Breastfeeding- There are no adequate studies on women to determine infant risk while using this medication during breastfeeding. Although, the potential benefits against the potential risks before taking this medication when breastfeeding should be considered.

Drug Interactions-

• Drug-Drug Interactions: Oxymetazoline hydrochloride can interact with antidepressants, ergot alkaloids, and MAO inhibitors.

• Drug-Food Interactions: Oxymetazoline hydrochloride can interact with caffeine. Therefore, avoid or limit caffeine intake as it may increase the risk of adverse effects such as nausea, sleep problems, nervousness, rapid heartbeat, or tremor.

• Drug-Disease Interactions: If a patient has diabetes, high blood pressure, heart disease, hyperthyroidism, enlarged prostate gland, or narrow-angle glaucoma, inform the doctor before taking Oxymetazoline hydrochloride.

For Patients:

What Are Colds, Allergies, and Hay Fever?

• Colds- The common cold is a viral nose and throat infection. It is usually harmless and can last for seven to ten days. The symptoms include a runny nose, sore throat, sneezing, coughing, headaches, and body aches. Cold is treated with medications and home remedies.

• Allergies- They can occur when the immune system reacts to a foreign substance such as pollen, pet dander, bee venom, or food. Our immune system produces substances known as antibodies. The immune system creates antibodies that identify harmful allergens when a person has allergies. When a person is exposed to the allergen, the immune system's reaction can inflame the skin, sinuses, airways, or digestive system. The severity of allergies usually varies from person to person, ranging from minor irritation to anaphylaxis. While most allergies cannot be cured, treatments can help relieve the allergy symptoms.

• Hay Fever- Hay fever is also called allergic rhinitis, and it causes cold-like symptoms, like a runny nose, itchy eyes, sneezing, congestion, and sinus pressure. But unlike a cold, hay fever is not caused by a virus. Hay fever is caused by an allergic response to a harmless indoor or outdoor substance that the body identifies as a harmful substance (allergen). Common allergens that trigger hay fever symptoms are pollen and dust mites. The tiny flecks of skin shedding by cats, dogs, or other animals with fur or feathers also can be allergens. It can be treated with medications.

Why Is Oxymetazoline Hydrochloride Prescribed?

Oxymetazoline hydrochloride is used to relieve nasal discomfort caused due to colds, allergies, and hay fever. It is also used for reducing sinus congestion and pressure. Oxymetazoline hydrochloride is not used for treating children younger than six years unless a doctor has recommended it.

Children six to twelve should use Oxymetazoline hydrochloride carefully, and always be done under adult supervision. Oxymetazoline hydrochloride comes under a class of medications called nasal decongestants, and it works by narrowing the blood vessels in the nasal passages.

How Oxymetazoline Hydrochloride Should Be Used?

• Oxymetazoline hydrochloride comes in liquid form to spray into the nose. It is usually advised to use every ten to twelve hours as needed, but at most twice in 24 hours.

• Patients are advised to follow the directions on the package label carefully or as written on the prescription label. Oxymetazoline hydrochloride should be used exactly as directed by the doctor. It should not be used more or less or more often than prescribed by the doctor or directed on the label.

• If Oxymetazoline hydrochloride is used more often or for a longer time than recommended, the congestion can get worse, or it may improve but come back after a while. Oxymetazoline hydrochloride should be used for up to three days. If the symptoms do not improve after three days of treatment, stop using Oxymetazoline and contact the doctor.

• Oxymetazoline hydrochloride is only made to use in the nose, and it should not be swallowed.

• The spray dispenser should not be shared with anyone else to prevent the spread of infection. The dispenser tip can be rinsed with hot water or wiped clean afterward.

What Special Precautions Should Be Followed?

• If a patient is allergic to Oxymetazoline or any of the ingredients in the Oxymetazoline, then it should be informed to the doctor.

• If the patient is allergic to any other medication, it should also be informed to the doctor.

• The doctor should be informed about all the prescription and nonprescription drugs that the patient is taking.

• Any herbal, vitamin, dietary, etc. products used by the patient should be informed to the doctor.

• If a patient has or has ever had diabetes, high blood pressure, or difficulty in urination due to an enlarged prostate gland, thyroid, or heart disease, they should be informed to the doctor.

• If a patient is pregnant, breastfeeding, or planning for pregnancy, the doctor should inform them.

• If patients become pregnant while using Oxymetazoline, they should contact the doctor.

Directions for Use

Oxymetazoline hydrochloride should be used only as advised by the doctor.

Check the label for directions before using the medication.

• For nasal spray, first, insert the tip of the bottle into one nostril while closing the other nostril. Now spray towards the sides of the nostril. Keep the head straight and breathe gently. Repeat the same process for another nostril.

• Tilt the head back for nasal drops while holding the dropper over the dose, and apply the prescribed number of drops to the nose. Now bend the head slightly forward and move it left and right gently. Avoid sneezing or blowing the nose for at least a few minutes after using the drops.

What Should Be Done if a Dose Is Missed?

The missed dose can be used as soon as the patient remembers it. However, the missed dose can be skipped if it is almost time for the next dose. Do not use the medication more than prescribed to compensate for the missed dose.

What Are the Side Effects of Oxymetazoline Hydrochloride?

• Burning or stinging sensation.
• Increased nasal discharge.
• Dryness inside the nose.
• Frequent sneezing.
• Nervousness.
• Nausea.
• Dizziness.
• Headache.
• Difficulty falling asleep or staying asleep.
• Fast or slow heartbeat.

Storage and Disposal- The spray dispenser should be kept at room temperature and away from sunlight. After use, the dispenser should not be flushed down the toilet; instead, it should be disposed of so that pets or children cannot consume it. Contact the local garbage disposal/recycling center to dispose of the medication.

What Should Be Done in Case of Oxymetazoline Overdose?

If a person has used too much Oxymetazoline or has swallowed the medication, the poison control helpline number should be dialed immediately. If the person cannot breathe or has collapsed, they should be immediately rushed to the nearest hospital.

Other Information-

• It is important to keep a written list of all the prescription and nonprescription drugs the patient takes.
• The list should be brought in every appointment with a doctor.
• The list should be carried out in case of an emergency.

For Doctors

Indications:

• Oxymetazoline hydrochloride is prescribed in adults for the topical treatment of persistent facial erythema associated with rosacea.

• Ophthalmic Oxymetazoline is indicated for treating acquired blepharoptosis in adults.

• When combined with tetracaine intranasally, Oxymetazoline hydrochloride is used for regional anesthesia while performing a restorative procedure on teeth 4 to 13 and A-J in adults and children who weigh 40 pounds or more.

• Oxymetazoline hydrochloride can be found in over-the-counter nasal products as a nasal decongestant.

• For off-label uses, Oxymetazoline hydrochloride has been used during nasal intubation and ear, nose, and throat surgery to improve airway visualization and minimize post-operative bleeding.

Pharmacodynamics

Oxymetazoline hydrochloride is an adrenergic alpha 1- and alpha 2-agonist and a direct-acting sympathomimetic drug. By stimulating the adrenergic receptors, Oxymetazoline hydrochloride causes vasoconstriction of dilated arterioles, thereby reducing blood flow.

In a radioligand competition study, Oxymetazoline hydrochloride displayed higher affinity at alpha 1A-adrenoceptors than alpha 2B-adrenoceptors but with higher potency at alpha 2B-adrenoceptors.

When sprayed intranasally, Oxymetazoline relieved nasal congestion and improved nasal airflow in patients suffering from acute coryzal rhinitis for up to twelve hours following a single dose.

An early in vitro study demonstrated that Oxymetazoline exerts anti-oxidant actions, inhibiting microsomal lipid peroxidation and mediating hydroxyl radical scavenging activity, which suggests that Oxymetazoline hydrochloride has a beneficial effect against oxidants in tissue damage during inflammation.

Mechanism of Action

Oxymetazoline binds to alpha 1- and alpha 2-adrenoceptors, Gq-protein-coupled receptors that promote contraction of vascular smooth muscle by increasing the intracellular calcium levels in response to ligand activation. Rosacea is a condition with transient and persistent facial erythema.

By stimulating alpha 1A-adrenoceptors and causing vasoconstriction, Oxymetazoline hydrochloride is believed to diminish the symptoms of erythema. In blepharoptosis, it is hypothesized that Oxymetazoline hydrochloride works by stimulating alpha-adrenergic receptors on the Muller muscle that elevates the upper eyelid and causes muscle contraction. Oxymetazoline hydrochloride is used in combination with tetracaine for local anesthesia in dentistry.

Such combination use adds beneficial effects like the vasoconstrictor counteracts the local anesthetic agent's vasodilatory action, constricting dilated arterioles and reducing blood flow to the applied area. Oxymetazoline hydrochloride relieves nasal congestion by vasoconstricting the respiratory microvasculature in resistance and capacitance blood vessels in the human nasal mucosa, which decreases nasal mucosal blood flow, edema, and airflow resistance.

Pharmacokinetics:

• Absorption- Imidazole derivatives like Oxymetazoline hydrochloride are readily absorbed in the mucosal membranes, particularly in children. In adult patients with erythema associated with rosacea, the mean, standard deviation Cmax was 60.5 picograms per milliliter, and the AUC from time 0 to 24 hours was 895 picograms per hour per milliliters following topical administration of first-dose of Oxymetazoline hydrochloride.

Following once-a-day topical applications for 28 days, the mean SD Cmax was 66.4 picograms per milliliter, and the AUC0-24 hour was 1050 per milliliter. Following twice-a-day applications for 28 days, the mean SD Cmax was 68.8 picograms per milliliter, and the AUC0-24 hour was 1530 picograms per hour per milliliter.

Following single-drop ocular administration of Oxymetazoline hydrochloride in healthy adult patients, the mean SD Cmax was 30.5 picograms per milliliter, and the area under the concentration-time curve was 468 picograms per hour per milliliters. The median Tmax was two hours, ranging from 0.5 to 12 hours.

Following nasal administration of an 0.6 milliliters combination product containing tetracaine and Oxymetazoline hydrochloride in adult subjects, the maximum concentrations of Oxymetazoline hydrochloride were reached within ten minutes. The mean Cmax was 1.78 nanograms per milliliters, and the AUC0-inf value was 4.24 nanograms per hour per milliliters, with a median Tmax of five minutes.

• Protein Binding- In vitro, Oxymetazoline hydrochloride is 56.7 percent to 57.5 percent bound to human plasma proteins.

• Metabolism- In vitro, Oxymetazoline hydrochloride was metabolized by human liver enzymes minimally to produce mono-oxygenated and dehydrogenated metabolites. About 95.9 percent of the total dose of Oxymetazoline hydrochloride remained as an unchanged parent compound after a two-hour incubation with human liver microsomes. When incubated in rat, rabbit, and human liver post-mitochondrial supernatant fractions from homogenized tissue fractions, Oxymetazoline hydrochloride was more efficiently metabolized by rabbit liver fractions than by rat or human liver fractions. At concentrations at least 130-fold more significant than the usual therapeutic intranasal dose, CYP2C19 was suggested to be involved in the oxidation of Oxymetazoline hydrochloride following intranasal administration. However, human metabolites have not been fully characterized, and they remain speculated based on in vitro studies using rat and rabbit liver fractions and microsomes. The O-glucuronide metabolite catalyzed by UGT1A9 was identified in vitro.

• Route of Elimination- The excretion of Oxymetazoline hydrochloride following nasal, topical, or ophthalmic administration has not been fully characterized in humans, and it is considered that the predominant route of elimination of Oxymetazoline hydrochloride at clinically relevant concentrations is renal excretion.

• Half-Life- Following ocular administration in healthy subjects (adults), the mean terminal half-life was 8.3 hours, ranging from 5.6 to 13.9. The terminal half-life of Oxymetazoline hydrochloride following nasal administration of the combination product containing Oxymetazoline and tetracaine in adult subjects was approximately 5.2 hours.

Toxicity

Case reports have revealed unintended overdose in children and adults, leading to dizziness, headaches, chest pain, stroke, myocardial infarction, visual disturbances, arrhythmia, hypotension, or hypertension. Accidental ingestion of imidazoline derivatives (topical solution), including Oxymetazoline hydrochloride, in children has shown adverse events requiring hospitalization, like nausea, vomiting, lethargy, decreased respiration, tachycardia, bradycardia, hypertension, hypotension, sedation, somnolence, stupor, mydriasis, drooling, hypothermia, and coma. Possible rebound nasal congestion, nasal mucosa irritation, and adverse systemic effects, especially in children, including adverse cardiovascular events, have also been reported with overdosage and prolonged or too frequent intranasal use of Oxymetazoline hydrochloride. Overdose should be managed with close monitoring, supportive care, and symptomatic treatment.