What are the best medications for sinus pressure relief. How do decongestants and antihistamines work to alleviate sinus symptoms. Which over-the-counter and prescription options are most effective for treating sinus pressure and congestion.

Understanding Sinus Pressure: Causes and Symptoms

Sinus pressure is a common and often uncomfortable condition that affects millions of people worldwide. But what exactly causes this pressure, and how can it be effectively treated? Let’s delve into the root causes and symptoms of sinus pressure to better understand this prevalent issue.

The sinuses are hollow spaces within the bones surrounding the nose, designed to produce mucus that keeps the nasal passages clean and lubricated. When these cavities become blocked or inflamed, it can lead to a buildup of pressure, resulting in discomfort and pain.

Common Causes of Sinus Pressure

• Infections (e.g., flu, common cold)
• Allergies (including hay fever)
• Injury to the nasal area
• Migraines

These factors can cause the tissue inside the nose to swell, blocking the sinuses and creating pressure. The symptoms of sinus pressure often include:

• Pain or pressure in the eyes, cheeks, or forehead
• Stuffy or runny nose
• Headache

Is sinus pressure always a sign of infection? Not necessarily. While infections can certainly cause sinus pressure, allergies and injuries can also lead to similar symptoms. It’s important to identify the underlying cause to determine the most effective treatment approach.

The Role of Decongestants in Alleviating Sinus Pressure

Decongestants play a crucial role in managing sinus pressure by targeting the root cause of the discomfort. These medications work by narrowing the blood vessels in the nasal passages, which helps reduce swelling and allows air to flow more freely through the sinuses.

How quickly do decongestants work to relieve sinus pressure? Many people experience relief within 30 minutes to an hour after taking a decongestant, though the full effects may take longer to manifest.

Types of Decongestants

Decongestants come in various forms, including pills and nasal sprays. Some common types include:

1. Naphazoline (e.g., Privine)
2. Oxymetazoline (e.g., Afrin, Dristan, Nostrilla)
3. Phenylephrine (e.g., Neo-Synephrine, Sinex)
4. Pseudoephedrine (e.g., Sudafed 12-hour tablets)

Are all decongestants suitable for everyone? No, certain individuals should exercise caution when using decongestants. It’s important to consult a healthcare provider before using these medications if you have any of the following conditions:

• Diabetes
• Glaucoma
• Heart conditions
• High blood pressure
• Prostate issues
• Thyroid problems

Additionally, it’s crucial to follow the dosage instructions carefully and avoid using multiple decongestants simultaneously to prevent potential side effects or complications.

Antihistamines: A Powerful Ally Against Allergy-Induced Sinus Pressure

For those whose sinus pressure stems from allergies, antihistamines can be a game-changer. These medications work by blocking the effects of histamine, a chemical released by the immune system in response to allergens.

How do antihistamines differ from decongestants in treating sinus pressure? While decongestants primarily focus on reducing swelling and opening up nasal passages, antihistamines target the allergic response itself, helping to prevent or reduce allergy symptoms that can lead to sinus pressure.

Common Antihistamines for Sinus Pressure Relief

Several types of antihistamines are available, both over-the-counter and by prescription. Some popular options include:

1. Azelastine nasal sprays (prescription only, e.g., Astepro, Astelin)
2. Loratadine (e.g., Claritin)
3. Cetirizine (e.g., Zyrtec)
4. Fexofenadine (e.g., Allegra)

Can antihistamines cause drowsiness? Some antihistamines, particularly older formulations, can cause drowsiness. However, newer “second-generation” antihistamines are less likely to have this side effect. Always read the label carefully and consult with a healthcare provider if you have concerns about potential side effects.

Over-the-Counter Pain Relievers: Additional Support for Sinus Discomfort

While decongestants and antihistamines target the underlying causes of sinus pressure, over-the-counter pain relievers can provide additional relief from the discomfort associated with this condition.

Which pain relievers are most effective for sinus pressure? The efficacy of pain relievers can vary from person to person, but some commonly used options include:

• Acetaminophen (e.g., Tylenol)
• Ibuprofen (e.g., Advil, Motrin)
• Naproxen (e.g., Aleve)

These medications can help alleviate pain and reduce inflammation, providing relief from sinus pressure symptoms. However, it’s essential to follow dosage instructions carefully and be aware of potential interactions with other medications you may be taking.

Combination Medications: A Comprehensive Approach to Sinus Relief

For those seeking a multi-faceted approach to sinus pressure relief, combination medications can offer a convenient solution. These products typically combine multiple active ingredients to address various aspects of sinus discomfort simultaneously.

What are the benefits of using combination medications for sinus pressure? Combination medications can provide comprehensive relief by targeting multiple symptoms at once, potentially reducing the need for multiple separate medications. However, it’s important to be aware of all the active ingredients to avoid accidentally doubling up on certain medications.

Examples of Combination Medications

• Decongestant + Antihistamine combinations (e.g., Claritin-D, Zyrtec-D)
• Decongestant + Pain reliever combinations (e.g., Advil Sinus Congestion & Pain)
• Decongestant + Antihistamine + Pain reliever combinations (e.g., Tylenol Sinus + Headache)

Are combination medications suitable for everyone? While combination medications can be effective, they may not be appropriate for all individuals. Those with certain medical conditions or who are taking other medications should consult with a healthcare provider before using combination products to ensure safety and avoid potential interactions.

Nasal Corticosteroids: Long-Term Management of Chronic Sinus Issues

For individuals dealing with chronic sinus pressure, particularly due to allergies or recurrent sinusitis, nasal corticosteroids can provide long-term relief. These medications work by reducing inflammation in the nasal passages, helping to prevent sinus pressure from developing.

How long does it take for nasal corticosteroids to work? Unlike decongestants or antihistamines, which can provide relatively quick relief, nasal corticosteroids may take several days to a few weeks to reach their full effectiveness. Consistent use is key to achieving optimal results.

Common Nasal Corticosteroids

• Fluticasone (e.g., Flonase)
• Mometasone (e.g., Nasonex)
• Budesonide (e.g., Rhinocort)
• Triamcinolone (e.g., Nasacort)

Are nasal corticosteroids safe for long-term use? When used as directed, nasal corticosteroids are generally considered safe for long-term use. However, as with any medication, it’s important to follow the instructions carefully and consult with a healthcare provider if you have any concerns or experience unexpected side effects.

Natural Remedies: Complementary Approaches to Sinus Pressure Relief

While medications can be highly effective in treating sinus pressure, many individuals also find relief through natural remedies. These approaches can be used alongside conventional treatments or as standalone options for those seeking alternative solutions.

Can natural remedies be as effective as medications for sinus pressure relief? The effectiveness of natural remedies can vary from person to person, and scientific evidence supporting their use is often limited. However, many people report finding relief through these methods, particularly for mild cases of sinus pressure.

Popular Natural Remedies for Sinus Pressure

• Nasal irrigation with saline solution
• Steam inhalation
• Essential oils (e.g., eucalyptus, peppermint)
• Hydration and increased fluid intake
• Warm compresses applied to the face
• Elevation of the head while sleeping

Is it safe to combine natural remedies with conventional medications? In many cases, natural remedies can be safely used alongside conventional treatments for sinus pressure. However, it’s always wise to consult with a healthcare provider before combining approaches, especially if you’re taking prescription medications or have underlying health conditions.

When to Seek Professional Medical Help for Sinus Pressure

While many cases of sinus pressure can be effectively managed with over-the-counter medications and home remedies, there are instances where professional medical attention is necessary. Recognizing when to seek help is crucial for preventing complications and ensuring proper treatment.

What are the signs that sinus pressure requires medical attention? Consider consulting a healthcare provider if you experience any of the following:

• Severe pain or pressure in the face or head
• Symptoms lasting more than 10 days without improvement
• High fever (above 101°F or 38.3°C)
• Thick, discolored nasal discharge
• Changes in vision
• Swelling around the eyes
• Persistent headaches unrelieved by over-the-counter pain medications

Can untreated sinus pressure lead to complications? In some cases, yes. Severe or chronic sinus issues left untreated can potentially lead to more serious conditions, such as chronic sinusitis, sinus infections that spread to nearby areas, or in rare cases, meningitis. This underscores the importance of seeking professional medical advice when symptoms are severe or persistent.

Diagnostic Tools and Advanced Treatments

When you consult a healthcare provider for sinus pressure, they may use various diagnostic tools to determine the underlying cause and appropriate treatment. These may include:

• Physical examination
• Nasal endoscopy
• Imaging studies (e.g., CT scans, MRI)
• Allergy testing

Based on the findings, your healthcare provider may recommend advanced treatments such as:

• Prescription-strength medications
• Immunotherapy for allergies
• Balloon sinuplasty
• Sinus surgery (in severe cases)

By seeking professional help when necessary, you can ensure that your sinus pressure is properly diagnosed and treated, potentially preventing complications and improving your overall quality of life.

The 10 best medications for sinus pressure

Sinus pressure can occur when illness, injury, or allergies cause tissue swelling inside the nasal passages. Decongestants, antihistamines, and other medications can help relieve it.

The best medication for sinus pressure will depend on several factors, including the cause of the problem and a person’s circumstances.

This article looks at some of the most suitable medications for sinus pressure.

The sinuses are hollow spaces in the bones that surround the nose. They produce mucus to keep the nostrils clean and lubricated.

If an infection, allergy, or injury causes the tissue inside the nose to swell up, this can block the sinuses and lead to sinus pressure. A person may feel pressure or pain in their:

• eyes
• cheeks
• forehead

People may also experience a stuffy or runny nose or a headache.

Common causes of sinus pressure include:

• infections, including flu and the common cold
• allergies, including hay fever
• injury
• migraine

Decongestants narrow the blood vessels in the nose. This allows the swollen tissue to shrink and enables air to pass through the sinuses more easily.

Pill and spray decongestants are available. Pseudoephedrine and phenylephrine products are only suitable for adults and children over 4 years of age.

When taking over-the-counter (OTC) decongestants, it is important to follow the advice on the label. Additionally, people should not use more than one decongestant at once.

Sometimes, decongestants can interfere with prescription medicines. Anyone already taking prescription medication or who has one of the following medical conditions should also speak with their doctor before taking a decongestant:

• diabetes
• glaucoma
• a heart condition
• high blood pressure
• prostate issues
• thyroid issues

The possible side effects of decongestants include:

• nervousness
• dizziness
• sleeping problems
• high blood pressure
• heart palpitations

Examples of decongestants include the following.

1. Naphazoline

Naphazoline is usually an eye drop product. People can use it if they have a cold, allergy, or eye irritation. Privine is a type of naphazoline.

2. Oxymetazoline

Oxymetazoline is a nasal spray. People can use it to relieve sinus pressure if they have a cold or allergies, including hay fever.

Afrin, Dristan, Nostrilla, and Vicks Sinus Nasal Spray are all types of oxymetazoline.

3. Phenylephrine

Phenylephrine can ease stuffiness and sinus pressure and is available as a pill or a nasal spray.

Neo-Synephrine, Sinex, Rhinall, and the pill form of Sudafed-PE all contain phenylephrine.

4. Pseudoephedrine

People with colds or allergies can use pseudoephedrine to ease sinus pressure. This medication comes in tablet or liquid form. Sudafed 12-hour tablets contain pseudoephedrine.

People can take antihistamines to treat allergies. Allergies occur when the immune system reacts to a substance that is not harmful and releases chemicals that doctors call histamines. For example, people may be allergic to pet dander, pollen, or dust.

Antihistamines block the effects of histamine and ease allergy symptoms, which can include sinus pressure.

The possible side effects of these medicines include:

• vision changes, such as blurry vision
• dry mouth
• loss of appetite
• feeling dizzy
• feeling drowsy
• feeling nervous, irritable, or excitable

People should speak with a doctor before taking antihistamines if they are pregnant or have the following health conditions:

• diabetes
• epilepsy
• heart disease
• high blood pressure
• overactive thyroid
• glaucoma

Different types of antihistamines are available from drug stores or on prescription from a doctor. Some last between 4 and 6 hours, while others can last for 12–24 hours.

However, driving or operating heavy machinery after taking some types of antihistamines may not be safe. People should always follow the instructions on the packet.

Common types of antihistamines include the following.

5. Azelastine nasal sprays

Azelastine nasal spray is only available on prescription. Doctors may call it Astepro or Astelin.

Adults and children over the age of 6 years can use this medication. Azelastine has a half life — the time it takes for the amount of a drug’s active substance to reduce by half in the body — of around 20 hours.

6. Loratadine

Loratadine comes as a liquid or a tablet and is available over the counter. Claritin is its brand name.

Adults and children over the age of 2 years can use it. However, it is unsuitable for children who weigh less than 30 kilograms. People tend to use this medication just once a day.

OTC pain medication can also help ease the discomfort of sinus pressure.

Different medicines work in different ways and have different risks and side effects. People should always follow the instructions on the label.

Examples of OTC pain medications include the following.

7. Acetaminophen

Acetaminophen changes the way the body senses pain. It is available as a tablet or liquid.

People should always follow the instructions on the packet and only take one product containing acetaminophen at a time. This is because taking too much can cause liver damage. Additionally, anyone who is allergic to acetaminophen should not take it.

Possible serious side effects of acetaminophen include:

• a rash
• hives
• itching
• swelling in the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• red, irritated, or peeling skin
• difficulty breathing or swallowing

Anyone who experiences any of these side effects should seek emergency medical attention.

8. Ibuprofen

Ibuprofen is a type of nonsteroidal anti-inflammatory drug (NSAID). It works by reducing swelling, which can help ease sinus pressure.

Anyone who is allergic to ibuprofen should not take this medication. Additionally, some people who are allergic to aspirin are also allergic to ibuprofen.

In some individuals, ibuprofen can cause bleeding in the gut. According to the Food and Drug Administration (FDA), people who are most at risk are:

• those aged 60 years or over
• those who have had stomach ulcers or bleeding problems in the past
• anyone who is also taking a blood thinning or steroid drug
• anyone who is also taking another NSAID, such as aspirin or naproxen
• anyone who has three or more alcoholic drinks daily while also taking ibuprofen
• people who take ibuprofen for longer periods

Other medications that may help ease sinus pressure include the following.

9. Steroids

Steroid nasal sprays can ease the swelling that leads to sinus pressure. They are available over the counter and on prescription from a doctor.

They are generally safe, but as with all medicines, they can pose risks. For example, some people may get nose bleeds. In rare cases, steroid nasals sprays can cause eye problems, such as glaucoma and cataracts.

10. Antibiotics

Bacterial infections can sometimes cause sinus pressure. When this is the case, antibiotics will clear the underlying infection.

These medications are only available from a doctor, who will usually recommend taking them for between 3 and 28 days.

Common side effects include:

• nausea or vomiting
• diarrhea
• bloating
• indigestion
• loss of appetite
• stomach pain

Other treatments for sinus pressure include:

• Inhaling steam: Inhaling the steam from a bowl of hot water or a warm shower can help ease the symptoms of sinus pressure.
• Warming compress: A person can try placing a warm compress over the nose and forehead.
• Drinking lots of fluids: It is always important to stay hydrated when experiencing illness.
• Using a saline nasal spray: According to the American College of Allergy, Asthma, and Immunology, rinsing the nose with a saline spray can help clear the nasal passages.

Sinus pressure can feel like a pain or tightness around the eyes, nose, and forehead. It is usually a symptom of an infection, allergy, or injury.

There are many medicines for sinus pressure, including decongestants and antihistamines. The right one depends on several factors, including the cause of the problem.

The 10 best medications for sinus pressure

Sinus pressure can occur when illness, injury, or allergies cause tissue swelling inside the nasal passages. Decongestants, antihistamines, and other medications can help relieve it.

The best medication for sinus pressure will depend on several factors, including the cause of the problem and a person’s circumstances.

This article looks at some of the most suitable medications for sinus pressure.

The sinuses are hollow spaces in the bones that surround the nose. They produce mucus to keep the nostrils clean and lubricated.

If an infection, allergy, or injury causes the tissue inside the nose to swell up, this can block the sinuses and lead to sinus pressure. A person may feel pressure or pain in their:

• eyes
• cheeks
• forehead

People may also experience a stuffy or runny nose or a headache.

Common causes of sinus pressure include:

• infections, including flu and the common cold
• allergies, including hay fever
• injury
• migraine

Decongestants narrow the blood vessels in the nose. This allows the swollen tissue to shrink and enables air to pass through the sinuses more easily.

Pill and spray decongestants are available. Pseudoephedrine and phenylephrine products are only suitable for adults and children over 4 years of age.

When taking over-the-counter (OTC) decongestants, it is important to follow the advice on the label. Additionally, people should not use more than one decongestant at once.

Sometimes, decongestants can interfere with prescription medicines. Anyone already taking prescription medication or who has one of the following medical conditions should also speak with their doctor before taking a decongestant:

• diabetes
• glaucoma
• a heart condition
• high blood pressure
• prostate issues
• thyroid issues

The possible side effects of decongestants include:

• nervousness
• dizziness
• sleeping problems
• high blood pressure
• heart palpitations

Examples of decongestants include the following.

1. Naphazoline

Naphazoline is usually an eye drop product. People can use it if they have a cold, allergy, or eye irritation. Privine is a type of naphazoline.

2. Oxymetazoline

Oxymetazoline is a nasal spray. People can use it to relieve sinus pressure if they have a cold or allergies, including hay fever.

Afrin, Dristan, Nostrilla, and Vicks Sinus Nasal Spray are all types of oxymetazoline.

3. Phenylephrine

Phenylephrine can ease stuffiness and sinus pressure and is available as a pill or a nasal spray.

Neo-Synephrine, Sinex, Rhinall, and the pill form of Sudafed-PE all contain phenylephrine.

4. Pseudoephedrine

People with colds or allergies can use pseudoephedrine to ease sinus pressure. This medication comes in tablet or liquid form. Sudafed 12-hour tablets contain pseudoephedrine.

People can take antihistamines to treat allergies. Allergies occur when the immune system reacts to a substance that is not harmful and releases chemicals that doctors call histamines. For example, people may be allergic to pet dander, pollen, or dust.

Antihistamines block the effects of histamine and ease allergy symptoms, which can include sinus pressure.

The possible side effects of these medicines include:

• vision changes, such as blurry vision
• dry mouth
• loss of appetite
• feeling dizzy
• feeling drowsy
• feeling nervous, irritable, or excitable

People should speak with a doctor before taking antihistamines if they are pregnant or have the following health conditions:

• diabetes
• epilepsy
• heart disease
• high blood pressure
• overactive thyroid
• glaucoma

Different types of antihistamines are available from drug stores or on prescription from a doctor. Some last between 4 and 6 hours, while others can last for 12–24 hours.

However, driving or operating heavy machinery after taking some types of antihistamines may not be safe. People should always follow the instructions on the packet.

Common types of antihistamines include the following.

5. Azelastine nasal sprays

Azelastine nasal spray is only available on prescription. Doctors may call it Astepro or Astelin.

Adults and children over the age of 6 years can use this medication. Azelastine has a half life — the time it takes for the amount of a drug’s active substance to reduce by half in the body — of around 20 hours.

6. Loratadine

Loratadine comes as a liquid or a tablet and is available over the counter. Claritin is its brand name.

Adults and children over the age of 2 years can use it. However, it is unsuitable for children who weigh less than 30 kilograms. People tend to use this medication just once a day.

OTC pain medication can also help ease the discomfort of sinus pressure.

Different medicines work in different ways and have different risks and side effects. People should always follow the instructions on the label.

Examples of OTC pain medications include the following.

7. Acetaminophen

Acetaminophen changes the way the body senses pain. It is available as a tablet or liquid.

People should always follow the instructions on the packet and only take one product containing acetaminophen at a time. This is because taking too much can cause liver damage. Additionally, anyone who is allergic to acetaminophen should not take it.

Possible serious side effects of acetaminophen include:

• a rash
• hives
• itching
• swelling in the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• red, irritated, or peeling skin
• difficulty breathing or swallowing

Anyone who experiences any of these side effects should seek emergency medical attention.

8. Ibuprofen

Ibuprofen is a type of nonsteroidal anti-inflammatory drug (NSAID). It works by reducing swelling, which can help ease sinus pressure.

Anyone who is allergic to ibuprofen should not take this medication. Additionally, some people who are allergic to aspirin are also allergic to ibuprofen.

In some individuals, ibuprofen can cause bleeding in the gut. According to the Food and Drug Administration (FDA), people who are most at risk are:

• those aged 60 years or over
• those who have had stomach ulcers or bleeding problems in the past
• anyone who is also taking a blood thinning or steroid drug
• anyone who is also taking another NSAID, such as aspirin or naproxen
• anyone who has three or more alcoholic drinks daily while also taking ibuprofen
• people who take ibuprofen for longer periods

Other medications that may help ease sinus pressure include the following.

9. Steroids

Steroid nasal sprays can ease the swelling that leads to sinus pressure. They are available over the counter and on prescription from a doctor.

They are generally safe, but as with all medicines, they can pose risks. For example, some people may get nose bleeds. In rare cases, steroid nasals sprays can cause eye problems, such as glaucoma and cataracts.

10. Antibiotics

Bacterial infections can sometimes cause sinus pressure. When this is the case, antibiotics will clear the underlying infection.

These medications are only available from a doctor, who will usually recommend taking them for between 3 and 28 days.

Common side effects include:

• nausea or vomiting
• diarrhea
• bloating
• indigestion
• loss of appetite
• stomach pain

Other treatments for sinus pressure include:

• Inhaling steam: Inhaling the steam from a bowl of hot water or a warm shower can help ease the symptoms of sinus pressure.
• Warming compress: A person can try placing a warm compress over the nose and forehead.
• Drinking lots of fluids: It is always important to stay hydrated when experiencing illness.
• Using a saline nasal spray: According to the American College of Allergy, Asthma, and Immunology, rinsing the nose with a saline spray can help clear the nasal passages.

Sinus pressure can feel like a pain or tightness around the eyes, nose, and forehead. It is usually a symptom of an infection, allergy, or injury.

There are many medicines for sinus pressure, including decongestants and antihistamines. The right one depends on several factors, including the cause of the problem.

metered nasal spray, 50 µg/dose

Mometasone furoate monohydrate is a white to off-white powder, practically insoluble in water, sparingly soluble in methanol, ethanol and isopropanol, soluble in acetone and chloroform, and readily soluble in tetrahydrofuran ; the molecular weight is 539.45.

Mechanism of action

Mometasone is a topical corticosteroid with local anti-inflammatory effects at doses that have minimal systemic effects.

Mometasone significantly inhibits the release of LT from leukocytes in allergic patients. In addition, it is an inhibitor of the production of Th3 cytokines – IL-4 and IL-5 – from human CD4+ T cells.

Pharmacodynamics

In two clinical studies using data from the analysis of nasal secretion for antigens, mometasone nasal spray demonstrated anti-inflammatory activity in both the early and late phase of allergic reactions. This was expressed in a decrease in the activity (compared with placebo) of the level of histamine and the activity of eosinophils and a decrease in the number (compared with the original) of eosinophils, neutrophils and adhesive proteins of epithelial cells. The clinical significance of these facts is unknown.

In patients with seasonal allergic rhinitis, mometasone demonstrated a clinically significant onset of action within 12 hours of the first dose.

In patients with acute rhinosinusitis with signs or symptoms of a bacterial infection, the use of mometasone as an adjunct to antibiotic treatment resulted in a significant decrease in the total score for nasal (purulent rhinorrhea, nasopharyngeal mucus and nasal congestion) and non-nasal (sinus headache, facial pain/tense/soreness and cough) symptoms.

In patients with uncomplicated mild to moderate acute rhinosinusitis in the absence of signs or symptoms of bacterial infection, mometasone has been shown to be effective as monotherapy. In addition, there was no evidence of increased recurrence of rhinosinusitis or predisposition to bacterial infections after discontinuation of mometasone monotherapy.

Two phase I studies conducted to evaluate the systemic exposure and tolerability of mometasone in children aged 3 to 12 years showed no clinically significant systemic effects and mometasone was well tolerated. The third phase I study in children aged 6 to 12 years showed a short-term decrease in the growth rate of the lower extremities within the normal range.

Phase II and III studies did not reveal any suppression of the hypothalamic-pituitary-adrenal axis after mometasone and demonstrated that mometasone can alleviate allergic symptoms in pediatric patients aged 3 to 12 years with seasonal and chronic allergic rhinitis. Pharmacokinetics

Pharmacokinetics

Absorption 0.25 pg/ml. Mometasone suspension is very poorly absorbed from the gastrointestinal tract, and a small amount of mometasone that can be accidentally swallowed and absorbed undergoes significant first-pass metabolism through the liver before excretion in the urine and bile.

Distribution

In vitro binding of mometasone to blood proteins ranged from 98 to 99% in the concentration range from 5 to 500 ng/ml.

Metabolism

Any accidentally swallowed and absorbed part of mometasone undergoes significant metabolism with the formation of several metabolites. The main metabolites are not found in plasma. When incubated in vitro “> in vitro one of the minor metabolites formed is 6β-hydroxymomethasone furoate. In liver microsomes, the formation of the metabolite occurs with the participation of CYP3A4.

Elimination

Effective 1/2″>T _1/2 mometasone from blood plasma after intravenous administration is 5. 8 hours. The absorbed part of mometasone is excreted as metabolites mainly with bile and to a limited extent with urine. treatment of patients with seasonal allergic rhinitis (aged 12 years and older) were studied in six A total of 2544 patients were enrolled in these studies, of whom 718 were randomized to receive mometasone 200 mcg once daily.0003

The results of three phase III clinical trials (14- or 28-day) involving 788 patients treated with mometasone or placebo, which evaluated its effectiveness, are presented in Table 1. The primary endpoint of efficacy after 1 week in study 192-200 there was a change from baseline in the mean total nasal symptom score as assessed by the clinician using the TNSS scale ( Total nasal symptom score ). In studies C93-013 and I94-001 the primary efficacy endpoint was the change from baseline in the mean total nasal symptom score as assessed by patients on days 1–15.

Table 1

Effect of mometasone in phase III randomized, placebo-controlled trials in patients with seasonal allergic rhinitis

Primary endpoint	1 time per day		Mometasone 200 mcg once daily		Placebo
	n	Mean	n	Mean	n	Mean
Study I92-200
TNSS 1 – Baseline	122	8. 1	122	8.1	110 9010 2	8
TNSS 1 – change from baseline by day 8 (%) 2	120	-4.3 3 (-53%)	120	-4, 7 3 (− 59%)	106	−2.6 (−34%)
Study C93-013
TNSS 900 07 4 – Baseline			111	7 .6	116	7.6
TNSS 4 – change from baseline for days 1-15 (%) 2			111	− 2.3 3 (−25%)	116	−1.5 (−17%)
Research I94-001
baseline			104	7. 4	103	7.3
TNSS 4 – change from baseline for days 1-15 (%) 2			104	− 2.8 3 (−35%)	103	-0.9 (-10%)

¹ Physician’s total assessment of nasal symptoms. Summary assessment of individual nasal symptoms (rhinorrhea, nasal congestion, nasal itching and sneezing). Symptoms were rated on a scale of 0=none, 1=mild, 2=moderate, 3=severe.

² The percentage change is the difference between the post-treatment mean score and the baseline mean score divided by the baseline mean score multiplied by 100.

³ p<0.01 compared with placebo.

⁴ Patient’s overall assessment of nasal symptoms. Summary assessment of individual nasal symptoms (rhinorrhea, nasal congestion, nasal itching and sneezing). Symptoms were scored on the following scale: 0=none, 1=mild, 2=moderate, 3=severe.

Perennial allergic rhinitis in adolescents and adults. The safety and efficacy of mometasone in patients (aged 12 years and older) with perennial allergic rhinitis was studied in three 12-week phase III clinical trials involving 875 patients treated with mometasone or placebo. The primary efficacy endpoint was the change from baseline in the mean total score of nasal symptoms, as assessed by the patient on a scale of TNSS from day 1 to day 15. The results of these studies are presented in Table 2.

Table 2

Mean total score of nasal symptoms according to the TNSS scale ¹ in studies involving patients with perennial allergic rhinitis

9010 9

Primary endpoint	Mometasone , 200 mg once daily		Placebo
	n	Mean	n	Mean
Study C92-280
Baseline	160	6. 6	160	6.9
Day change from baseline 1st–15th (%) 2	160	−1.5 3 (−21%)	158	−1.0 (−13%)
Research I92- 293
Baseline	129	6.3	124	6.2
Change from baseline on days 1-15 (%) 2 90 102	127	−1.7 3 Baseline 9 0102	154	6.1	148	6
Change from baseline on days 1-15 (%) 2	154	−2.2 4 (−37%)	148	−1.3 (−22%)

90 003

¹ Total assessment of individual nasal symptoms (rhinorrhea, nasal congestion, itchy nose and sneezing). Symptoms were rated on the following scale: 0=none, 1=mild, 2=moderate, 3=severe.

² The percentage change is the difference between the mean score after treatment and the mean score at baseline divided by the baseline mean score multiplied by 100.

³ p=0.01 vs. placebo.

⁴ p<0.01 vs. placebo.

Seasonal and perennial allergic rhinitis in children. The safety and efficacy of mometasone in pediatric patients with seasonal and perennial allergic rhinitis was studied in two clinical trials involving 645 children aged 3 to 11 years who received mometasone or placebo. Patients were treated for 4 weeks for both seasonal and perennial allergic rhinitis. In the case of seasonal allergic rhinitis, the primary efficacy endpoint was the change from baseline in the mean nasal symptom total score (on a scale of TNSS ) as assessed by a physician on the 8th day. In the case of perennial allergic rhinitis, the primary efficacy endpoint was the change from baseline in the physician-assessed mean total nasal symptom score at day 15. The results of these studies are presented in Table 3.

Table 3

Mean Nasal Symptom Score TNSS ¹ as assessed by physicians in studies involving pediatric patients with allergic rhinitis

Primary endpoint	Mometasone 10 mcg once daily		Placebo
	n	Mean 9 0102	n	Average
Survey C95-161 seasonal allergic rhinitis
Baseline	135	8.1	134	8
Change in compared to baseline on day 8 (%) 2	134	−2.8 3 (−34%)	130	−1.9 (−24%)
Baseline	186	6. 8	190	6.8
Change from baseline on Day 15 (%) 9 0134 2	185	−2.8 4 (−39%)	188	−2.2 (−32%)

¹ Total assessment of individual nasal symptoms (rhinorrhea, nasal congestion, nasal itching and sneezing). Symptoms were rated on the following scale: 0=none, 1=mild, 2=moderate, 3=severe.

² The percentage change is the difference between the mean score after treatment and the mean score at baseline divided by the baseline mean score multiplied by 100.

³ p=0.01 vs. placebo.

⁴ p=0.02 vs. placebo.

Mild to moderate uncomplicated acute rhinosinusitis

In two clinical studies involving 1954 patients aged 12 years or older with mild to moderate uncomplicated acute rhinosinusitis, mometasone 200 mcg twice daily significantly improved symptoms of acute rhinosinusitis, compared with placebo, as assessed on a major symptom scale of MSS ( Major symptom score ) including symptom cluster (facial pain/tightness/tenderness, sinus headache, rhinorrhea, nasopharyngeal runoff, and nasal congestion) over a 15-day treatment period (study P02683 : p <0. 001 study P02692 : p=0.038). The addition of amoxicillin 500 mg three times a day to treatment did not lead to a significant difference compared with placebo in reducing the symptoms of uncomplicated mild to moderate acute rhinosinusitis when assessed on a scale of MSS (table 4).

Table 4

MSC Main Symptom Summary

9 0111 −4.13 (− 49.3%)

9011 1,242

9011 1 −3.38 (−42, 5%)

9 0111 A-B

Index	Mometasone 200 mcg once daily (A)		Mometasone 200 mcg twice daily (B)		Amoxicillin 50 mg 3 times a day (C)		Placebo (D)
	n	Two-stage mean 1	n 9 0102	Two-stage average 1	n	Two-stage mean 1	n	Two-stage mean 1
Study P02683
Baseline 2	243	8. 17	234	8.28	251	8.53	252	8.36
Actual score, days 2–15 (initial assessment)	240	4.16 3	234	3.8 3.4	249	4.4	247	4.61
Change from baseline, days 2–15 ( %)	240	−4.01 (−49.8%)	233	−4.51 3.5 (-55.6%)	249	247	−3.75 (−45.6%)
Study P02692
Baseline 2	229	7.69	236	7.7	233	7.55	7.72
Actual score, days 1–15 6	229	3. 99	236	3.95 3	233	4.17	242	4.36
Change from baseline, days 1 –15th 6 (initial estimate) (%)	229	-3.70 (-46.7%)	236	-3.76 3.4 (-48.4%)	233	242	−3.36 (−41.5%)
Pairwise comparison of MSS change from baseline and 95% CI
	A –C	A–D	B–C	B–D	C–D
Study P02683
Change from baseline, days 2-15	0.5 (0.1, 0.9)	-0.12 (-0.28, 0.51)	-0.26 (-0.66, 0.13)	-0.38 (-0.78, 0.01)	-0.76 (-1.16, -0. 36)	−0.38 (−0.76, 0.01)
Study P02692
Change from comparison with baseline, days 1–15 6 (initial assessment )	0.06 (-0.32, 0.44)	-0.32 (-0.7, 0.064)	-0.34 (-0.72, 0.04)	-0, 38 (-0.76, -0)	-0.4 (-0.78, -0.02)	-0.02 (-0.4, 0.36)

¹ A two-way mean was obtained from the ANOVA model for effect on treatment, location, and duration of symptoms (days 7–14 or 15–28).

² In study P02683 The baseline was an in-office assessment performed jointly by patient and clinician. In study P02692 , baseline was the average of three patient-only diary assessments.

³ p<0.05 vs. placebo.

⁴ p ≤0.05 compared with amoxicillin.

⁵ p<0. 05 vs. mometasone 200 mcg once daily.

⁶ Day 1 includes project manager evaluation for patients in Study 9 only0006 P02692 .

In addition, a 14-day follow-up was conducted in four treatment groups. The results of this observation showed that the recurrence rate of rhinosinusitis was comparable across all treatment groups.

Nasal polyps

In clinical trials for the treatment of nasal polyps, mometasone showed a significant improvement in patients compared with placebo in clinically relevant endpoints such as nasal congestion and nasal polyp size (Table 5).

Table 5

Efficacy of mometasone in two randomized, placebo-controlled trials in patients with nasal polyps

Study score	Mometasone, 200 mcg, once daily 90 102	Mometasone, 200 mcg, twice daily day	Placebo	P-value for mometasone, 200 µg, once daily versus placebo	P-value for mometasone, 200 µg, twice daily, versus placebo
Study P01925	n=115	n=122	n=117
Assessment of the initial level of bilateral polyp severity 1	4. 21	4.27	4.25
Mean change in bilateral polyp score from baseline 2	02	−0.96	−0.5	<0.001	0.01
Baseline nasal congestion score 3	2.29 9010 2	2.35	2.28
Mean change in nasal congestion score from baseline 4	−0.47	−0.61	−0.24	0.001	<0.00 1
Study P01926	n=102	n=102	n=106
bilateral polyp 1	4	4.1	4.17
Mean change in bilateral polyp score from baseline 2	−0. 78	−0.96	−0.62	0.33	0.04
Estimated baseline nasal congestion 3	2.23	2.2	2.18
Mean change in nasal congestion score from baseline 4	-0.42	-0.66	-0.23	0.01	<0.001

^{1901 35 Polyps in each nasal passage were assessed by the investigator based on endoscopic imaging on a scale of 0 to 3, where 0 means no polyps; 1 – polyps in the middle part of the nasal passage, not reaching the lower edge of the middle turbinate; 2 – polyps reach the lower edge of the middle turbinate, but do not reach the lower edge of the inferior turbinate; 3 – polyps reach or are located below the edge of the inferior turbinate, or polyps are located medial to the middle turbinate (score reflects the sum of the scores of the left and right nasal passages).}

² Relative to last assessment over the entire four-month treatment period.

³ Nasal congestion/nasal obstruction was assessed daily by the patient on a scale of 0 to 3, where 0 is no symptoms; 1 – mild symptoms; 2 – moderate symptoms and 3 – severe symptoms.

⁴ Mean value for the first month of treatment.

Treatment of symptoms of seasonal or perennial allergic rhinitis in adults, adolescents and children aged 3 to 11 years; as adjunctive treatment to antibiotics for acute episodes of rhinosinusitis when signs or symptoms of a bacterial infection are present in adults and children 12 years of age and older; treatment of symptoms associated with mild to moderate uncomplicated acute rhinosinusitis in the absence of signs or symptoms of a bacterial infection in adults and children 12 years of age and older; treatment of nasal polyps in adults 18 years of age and older.

In rare cases, immediate-type hypersensitivity reactions (eg, bronchospasm, dyspnea) may occur after intranasal use of mometasone.

Very rare cases of anaphylaxis and angioedema have been reported.

Taste and odor disturbances have been reported very rarely.

Clinical trial experience

Since clinical trials are conducted under different conditions, the frequency of adverse reactions observed in clinical trials may not reflect the rates observed in practice and should not be compared with the frequency obtained in clinical trials of another drug . Information on adverse reactions obtained in clinical studies is used to identify adverse reactions associated with the use of drugs, and an approximate estimate of their frequency.

Allergic rhinitis

Adults and adolescents over 12 years of age. Table 6 shows pooled data from clinical studies on the frequency of adverse reactions associated with the use of mometasone.

Table 6

Mometasone-associated adverse reactions occurring at a frequency of ≥1% or more frequently than placebo

¹ 50 to 800 mcg mometasone furoate per day.

Treatment-related local side effects reported in clinical studies, such as headache, epistaxis (eg, frank bleeding, bloody mucus and blood spots), pharyngitis, and nasal ulcers, are commonly seen with corticosteroid nasal spray . In addition, with a frequency equal to or less than placebo, burning (2 vs 3%) and irritation (2 vs 2%) in the nose were noted.

Nosebleeds were generally self-limiting, mild, and more common than placebo (5%), but comparable or less than nasal corticosteroids studied as active controls (up to 15%) . The frequency of all other effects was comparable to placebo.

Children aged 3 to 11 years. In the pediatric population, the incidence of adverse events, such as headache (3%), epistaxis (6%), nasal irritation (2%) and sneezing (2%), was comparable to placebo.

Acute rhinosinusitis as adjunctive treatment to antibiotics

pain (2%), pharyngitis (1%), nasal burning (1%) and nasal irritation (1%). Nosebleeds were of mild severity and were also observed at a frequency comparable to placebo (5% vs. 4%, respectively).

Mild to moderate acute uncomplicated rhinosinusitis

In patients treated with mometasone for mild to moderate acute rhinosinusitis, the overall incidence of adverse events was comparable to placebo and similar to that observed in patients with allergic rhinitis.

Nasal polyps

In patients treated with mometasone for nasal polyps, the overall incidence of adverse events was comparable to placebo and similar to that observed in patients with allergic rhinitis.

Less common adverse reactions (<1%) observed in clinical studies

occurring in more than one patient).

From the blood and lymphatic system: lymphadenopathy.

From the side of the heart: palpitations, tachycardia.

On the part of the organ of vision: lacrimation, conjunctivitis, dry eyes, blurred vision.

On the part of the organ of hearing and labyrinth: pain in the ear, tinnitus.

From the gastrointestinal tract: abdominal pain, constipation, diarrhea, gastritis, nausea, tongue pathology, dental disease.

General disorders and conditions at the injection site: dry mouth, exacerbation of allergies, chest pain, edema, incl. face, fever, flu-like symptoms, thirst, taste perversion.

Infections and infestations: non-herpetic fever, infection, bacterial infection.

Lab tests: elevated liver enzymes.

From the musculoskeletal system and connective tissue: arthralgia, myalgia.

From the nervous system: tremor, dizziness, migraine.

From the side of the psyche: depression, paranoia, drowsiness.

Respiratory, thoracic and mediastinal: dysphonia, bronchitis, shortness of breath, laryngitis, ulceration of the nasal septum, sinusitis, wheezing.

From the skin and subcutaneous tissues: acne, dermatitis, erythematous rash.

Vascular: arterial hypertension.