Loading...
Loading...
Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Oxymetazoline Hydrochloride
Brand Name
Zicam Extreme Congestion Relief
Generic Name
Oxymetazoline Hydrochloride
Active Ingredient
OxymetazolineCategory
Vasoconstrictor [EPC]
Salt Form
Hydrochloride
Variants
1
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| .5 mg/mL | SPRAY | NASAL | 10237-464 |
Detailed information about Zicam Extreme Congestion Relief
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Zicam Extreme Congestion Relief, you must consult a qualified healthcare professional.
Oxymetazoline is a potent vasoconstrictor and alpha-adrenergic agonist used primarily to treat nasal congestion, ocular redness, persistent facial erythema associated with rosacea, and acquired blepharoptosis.
Dosage for oxymetazoline depends strictly on the formulation and the condition being treated.
Specific dosage adjustments for renal (kidney) impairment are not typically required for topical oxymetazoline due to its low systemic absorption. However, caution should be exercised in patients with severe renal disease if systemic effects occur.
No specific dosage adjustments are provided for hepatic (liver) impairment. As with renal impairment, the localized nature of the drug limits systemic exposure.
Clinical trials for the 1% cream and 0.1% ophthalmic solution included elderly patients, and no overall differences in safety or effectiveness were observed. However, elderly patients may be more sensitive to the cardiovascular effects (such as increased blood pressure) of sympathomimetic amines.
If you miss a dose, take it as soon as you remember. However, if it is nearly time for your next scheduled dose, skip the missed dose and resume your regular schedule. Do not double the dose to catch up. For the nasal spray, missing a dose is generally not an issue as it is often used on an as-needed basis (within the 3-day limit).
Signs of oxymetazoline overdose, particularly if swallowed or used excessively, include:
In the event of an overdose or accidental ingestion, especially by a child, contact a Poison Control Center or seek emergency medical attention immediately.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose or extend the duration of use without medical guidance.
When used as a nasal spray, common side effects are usually localized to the site of application and include:
For the 1% topical cream (Rhofade), common side effects include application site dermatitis (skin irritation), worsening of inflammatory lesions of rosacea, and application site erythema (redness).
These effects may occur as the drug is absorbed systemically or as a reaction to the formulation:
Rarely, oxymetazoline can cause systemic cardiovascular or neurological effects:
> Warning: Stop taking Oxymetazoline and call your doctor immediately if you experience any of these serious symptoms.
The most significant long-term risk of oxymetazoline (nasal) is the development of chronic nasal congestion and mucosal atrophy (thinning of the lining of the nose). Prolonged use can lead to the loss of the normal ciliary function (the tiny hairs that clear mucus), making the patient more prone to sinus infections and chronic irritation. For the topical cream, long-term use has been studied for up to one year, with skin irritation being the primary ongoing concern.
No FDA black box warnings currently exist for Oxymetazoline. However, the FDA does mandate strong warnings on OTC packaging regarding the duration of use (the 3-day rule) to prevent rebound congestion and warnings regarding accidental ingestion by children.
Report any unusual symptoms or persistent side effects to your healthcare provider. If you suspect you have developed a dependency on the nasal spray, consult an ear, nose, and throat (ENT) specialist for a tapering schedule.
Oxymetazoline is a potent medication that must be used with caution. The most critical safety point for patients using the nasal spray is the 3-day limit. Using the product for longer than three consecutive days can cause the nasal tissues to swell more than they did originally, creating a cycle of dependency and chronic congestion known as rhinitis medicamentosa.
There are no FDA black box warnings for Oxymetazoline. It is generally considered safe when used exactly as directed for short durations.
Routine lab tests are not typically required for short-term oxymetazoline use. However, for patients using the 1% cream or 0.1% drops long-term, doctors may monitor:
While oxymetazoline does not typically cause drowsiness, some patients may experience dizziness or blurred vision (especially with eye drops). If you experience these symptoms, do not drive or operate heavy machinery until your vision clears and you feel steady.
There is no direct interaction between alcohol and oxymetazoline. However, alcohol can cause vasodilation (widening of blood vessels), which may worsen nasal congestion or the facial redness of rosacea, potentially counteracting the effects of the medication.
If oxymetazoline nasal spray has been used for longer than 3-5 days, do not stop it abruptly if you experience severe rebound congestion. Your healthcare provider may recommend a tapering schedule, such as stopping the spray in one nostril at a time or using a saline-only spray to bridge the transition. In some cases, a short course of nasal corticosteroids may be prescribed to reduce the inflammation caused by withdrawal.
> Important: Discuss all your medical conditions, especially heart or thyroid problems, with your healthcare provider before starting Oxymetazoline.
Oxymetazoline is not known to significantly interfere with common laboratory blood or urine tests. However, its effect on intraocular pressure may interfere with tonometry tests during eye exams.
For each major interaction, the mechanism usually involves either pharmacodynamic synergy (both drugs increasing blood pressure via different or similar pathways) or interference with the clearance of neurotransmitters like norepinephrine. The clinical consequence is typically an increased risk of cardiovascular strain. The management strategy is generally to avoid the combination or to monitor blood pressure and heart rate closely during use.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including those purchased over-the-counter.
Oxymetazoline must NEVER be used in the following circumstances:
In these cases, a healthcare provider must perform a careful risk-benefit analysis:
Patients who are allergic to other imidazoline derivatives (such as xylometazoline, naphazoline, or tetrahydrozoline) may also be allergic to oxymetazoline. If you have had a reaction to 'redness-relief' eye drops or other long-acting nasal sprays in the past, inform your healthcare provider before use.
> Important: Your healthcare provider will evaluate your complete medical history, including any history of heart disease or glaucoma, before prescribing or recommending Oxymetazoline.
Oxymetazoline is classified as FDA Pregnancy Category C. This means that animal reproduction studies have shown an adverse effect on the fetus, or there are no adequate and well-controlled studies in humans. It is unknown whether oxymetazoline can cause fetal harm when administered to a pregnant woman or if it can affect reproduction capacity.
Oxymetazoline should be used during pregnancy only if clearly needed and if the potential benefit justifies the potential risk to the fetus.
It is not known whether oxymetazoline is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when oxymetazoline is administered to a nursing woman. Given the low systemic absorption of topical forms, the amount reaching the infant is likely very small, but mothers should monitor the infant for any signs of restlessness or sleep disturbances.
Elderly patients (65 years and older) may be more prone to the side effects of sympathomimetic amines. Specifically, they have a higher prevalence of underlying cardiovascular disease, prostatic hypertrophy, and glaucoma, all of which require cautious use of oxymetazoline. In clinical trials for Rhofade and Upneeq, no specific dosage adjustments were required for the elderly, but close monitoring of blood pressure is recommended.
Oxymetazoline has not been specifically studied in patients with renal impairment. However, because only about 30% of a systemically absorbed dose is excreted by the kidneys, and systemic levels are already very low, significant accumulation is unlikely in patients with mild to moderate renal disease. No specific GFR-based adjustments are provided in the standard labeling.
There are no specific studies or dosage adjustments for oxymetazoline in patients with hepatic impairment. The drug does not appear to be heavily metabolized by the liver, suggesting that liver dysfunction should not significantly impact the clearance of the drug.
> Important: Special populations, particularly pregnant women and the elderly, require individualized medical assessment before using vasoconstrictors.
Oxymetazoline is a direct-acting sympathomimetic amine that acts as an agonist on alpha-adrenergic receptors. It has a high affinity for alpha-1A receptors, which are prevalent in the smooth muscles of the blood vessels in the nasal mucosa and the skin. It also acts on alpha-2A receptors. By binding to these receptors, oxymetazoline triggers the G-protein signaling pathway, leading to an increase in intracellular calcium and subsequent contraction of the vascular smooth muscle. This results in vasoconstriction, which reduces the volume of the nasal mucosa (nasal decongestion), reduces the diameter of facial capillaries (rosacea treatment), and contracts the Müller's muscle (eyelid elevation).
| Parameter | Value |
|---|---|
| Bioavailability | Minimal (Topical/Nasal) |
| Protein Binding | Not extensively characterized |
| Half-life | 5 - 8 hours |
| Tmax | 0.5 - 2 hours (if systemic absorption occurs) |
| Metabolism | Negligible by CYP enzymes |
| Excretion | Renal 30%, Fecal 10% |
Oxymetazoline belongs to the therapeutic class of topical nasal decongestants and the pharmacological class of alpha-adrenergic agonists. Other medications in this class include phenylephrine, naphazoline, and xylometazoline. Unlike phenylephrine, which is relatively short-acting, oxymetazoline is classified as a long-acting decongestant.
Common questions about Zicam Extreme Congestion Relief
Oxymetazoline is primarily used as a topical nasal decongestant to provide temporary relief from nasal stuffiness caused by the common cold, hay fever, or allergies. It is also found in eye drops to reduce redness caused by minor irritations and in specialized prescription formulations for other conditions. Specifically, a 1% cream version is used to treat the persistent facial redness associated with rosacea in adults. Additionally, a 0.1% eye drop formulation is approved for treating acquired blepharoptosis, which is the drooping of the upper eyelid. Because it is a potent vasoconstrictor, it works by narrowing blood vessels in the area where it is applied.
The most common side effects of oxymetazoline nasal spray include temporary stinging, burning, or dryness in the nasal passages, along with sneezing and an initial increase in nasal discharge. When used as a cream for rosacea, patients frequently report skin irritation, redness, or a worsening of inflammatory acne-like lesions at the application site. For the eye drop formulations, common side effects include eye irritation, blurred vision, or a dry eye sensation. Most of these effects are localized and temporary, occurring shortly after the medication is applied. If these symptoms persist or become severe, you should contact your healthcare provider for guidance.
There is no known direct chemical interaction between alcohol and oxymetazoline that would cause a dangerous reaction. However, alcohol is a known vasodilator, meaning it causes blood vessels to widen, which is the exact opposite of what oxymetazoline is trying to achieve. Drinking alcohol can worsen nasal congestion and increase the facial flushing associated with rosacea, potentially making the medication less effective. Furthermore, alcohol can increase the risk of headaches or dizziness, which are also potential side effects of oxymetazoline. It is generally advisable to limit alcohol consumption if you are using this medication to treat congestion or skin redness.
Oxymetazoline is classified as Pregnancy Category C, which means there is limited data from well-controlled studies in pregnant women. While systemic absorption from a nasal spray or eye drop is generally low, there is a theoretical risk that the vasoconstrictive effects could affect blood flow if used in large amounts. Animal studies have shown some adverse effects, but these have not been definitively confirmed in humans. Pregnant women should only use oxymetazoline if the potential benefits clearly outweigh the risks and only under the direct supervision of their doctor. It is especially important to avoid overuse or exceeding the recommended dose during pregnancy.
One of the primary advantages of oxymetazoline is its rapid onset of action, especially when used as a nasal spray. Most patients begin to feel relief from nasal congestion within 5 to 10 minutes of administration. The effects are also long-lasting, typically providing decongestion for up to 12 hours, which allows for twice-daily dosing. For the rosacea cream, the reduction in facial redness may be noticed within 1 to 3 hours after application. For the eyelid-lifting drops, the effect usually begins within 2 hours and can last for several hours throughout the day.
If you have used oxymetazoline nasal spray for the recommended duration of 3 days or less, you can stop taking it suddenly without any issues. However, if you have used the spray for an extended period, stopping suddenly may cause 'rebound congestion,' where your nasal passages swell significantly. This happens because the blood vessels have become dependent on the medication to stay constricted. To avoid this, healthcare providers often recommend a gradual taper or the use of saline sprays to help the nasal lining recover. If you find it difficult to breathe after stopping the spray, consult an ear, nose, and throat specialist.
If you miss a dose of oxymetazoline, you should take it as soon as you remember, unless it is almost time for your next scheduled dose. In that case, simply skip the missed dose and return to your regular dosing schedule; do not double the dose to make up for the one you missed. Since the nasal spray is often used on an as-needed basis for symptom relief, a missed dose is usually not a clinical concern. For prescription versions like the rosacea cream or ptosis drops, consistency is more important for maintaining results. Always follow the specific instructions provided by your prescribing physician regarding missed doses.
There is no clinical evidence to suggest that oxymetazoline causes weight gain. Because it is applied topically to the nose, eyes, or skin, very little of the medication enters the systemic circulation in healthy individuals using the drug as directed. Weight gain is typically associated with systemic medications like oral corticosteroids or certain antidepressants, not localized vasoconstrictors. If you experience unexpected weight gain while using oxymetazoline, it is likely due to another underlying cause or a different medication. You should discuss any significant changes in your weight with your healthcare provider to determine the cause.
Oxymetazoline can interact with several types of medications, particularly those that also affect blood pressure or the sympathetic nervous system. It is strictly contraindicated with Monoamine Oxidase Inhibitors (MAOIs), and caution is required when using it alongside tricyclic antidepressants or certain blood pressure medications like beta-blockers. Using it with other decongestants can also increase the risk of side effects like a racing heart or nervousness. Before starting oxymetazoline, it is vital to provide your doctor or pharmacist with a full list of all prescription and over-the-counter drugs you are taking. This includes herbal supplements and vitamins, as some can have additive effects on your heart rate.
Yes, oxymetazoline is widely available as a generic medication, particularly in its 0.05% nasal spray and 0.025% ophthalmic solution forms. These generic versions are sold over-the-counter and are typically much less expensive than brand-name products like Afrin or Visine. However, some newer and more specialized formulations, such as the 1% cream for rosacea (Rhofade) and the 0.1% drops for drooping eyelids (Upneeq), may still be under patent protection. For these prescription-only products, a generic version may not be available yet. You can check with your pharmacist to see if a generic equivalent exists for the specific formulation your doctor has prescribed.
Other drugs with the same active ingredient (Oxymetazoline)