flunisolide(nasal)

Action and Spectrum

Actions and Spectrum: 

• flunisolide is a synthetic corticosteroid used as an intranasal spray to treat the symptoms of allergic rhinitis, including sneezing, congestion, runny nose, and itching. The mechanism of action of flunisolide involves its anti-inflammatory and immunosuppressive properties, which help to reduce inflammation and swelling in the nasal passages. 
• flunisolide works by binding to glucocorticoid receptors in the cells of the nasal mucosa, which leads to the activation of anti-inflammatory genes and the inhibition of pro-inflammatory genes. This results in a reduction of inflammation and swelling in the nasal passages, which helps to alleviate the symptoms of allergic rhinitis. 
• The spectrum of activity of flunisolide intranasal is primarily limited to treating allergic rhinitis, including seasonal and perennial allergic rhinitis caused by environmental allergens such as pollen, dust, and animal dander. It is ineffective against other types of rhinitis, such as non-allergic rhinitis or rhinitis caused by infections. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Aftertaste (8-17%) 

Nasal burning/stinging (13-44%)  

1-10% 

Epistaxis 

Pharyngitis 

Nausea 

Nasal dryness 

Cough increased 

<1% 

Nasal ulceration 

Sinusitis 

Vertical growth suppression 

Hoarseness 

Abnormal sense of smell 

Black Box Warning

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: flunisolide is contraindicated in patients with known hypersensitivity to the medication or its components. Signs of an allergic reaction may include hives, itching, swelling, and difficulty breathing. 
• Untreated Infections: flunisolide should not be used in patients with untreated nasal, sinus, or other infections. The medication may mask the symptoms of infection and delay appropriate treatment. 
• Recent nasal surgery or injury: flunisolide should not be used in patients who have recently undergone or experienced a nasal injury. The medication may slow the healing process and increase the risk of infection. 
• Tuberculosis: flunisolide should not be used in patients with active or suspected tuberculosis. The medication may suppress the immune system and worsen the infection. 
• Immunodeficiency: flunisolide should be used cautiously in patients with a history of immunodeficiency disorders or taking immunosuppressive medications. The medication may further suppress the immune system and increase the risk of infections. 

Caution: 

• Children: flunisolide should be used with caution in children. While the medication is generally considered safe and effective for children over 6, limited information is available on the long-term effects of using intranasal corticosteroids in children. 
• Pregnancy and breast-feeding: flunisolide should be used cautiously in pregnant or breastfeeding women. While there is limited information on the safety of flunisolide during pregnancy or breastfeeding, the medication may cross the placenta or be excreted in breast milk. 
• Glaucoma and cataracts: flunisolide should be used cautiously in patients with a history of glaucoma or cataracts. The medication may increase intraocular pressure and worsen these conditions. 
• Hepatic impairment: flunisolide should be used cautiously in patients with hepatic impairment. The medication may be metabolized more slowly in patients with liver dysfunction, increasing the risk of side effects. 
• Diabetes: flunisolide should be used with caution in patients with diabetes. The medication may increase blood glucose levels and worsen glycemic control. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation:  

• flunisolide should be used cautiously in pregnant or breastfeeding women. 
• While there is limited information on the safety of flunisolide during pregnancy or breastfeeding, the medication may cross the placenta or be excreted in breast milk. 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

flunisolide is a synthetic corticosteroid used as an intranasal spray for treating allergic rhinitis and other nasal inflammatory conditions. It reduces inflammation in the nasal passages, relieving symptoms such as congestion, sneezing, and runny nose. 

Pharmacodynamics: 

• flunisolide is a potent synthetic corticosteroid that exerts its pharmacodynamic effects by binding to glucocorticoid receptors in target cells. These receptors are located in the cytoplasm of cells and are translocated to the nucleus when activated by flunisolide. Once in the nucleus, the activated receptors bind to specific DNA sequences, called glucocorticoid response elements (GREs), which leads to the activation or suppression of various genes involved in inflammation and immunity. 

• flunisolide’s primary pharmacodynamic effect is suppressing the production of inflammatory cytokines and chemokines. These molecules are released by immune cells and play a crucial role in developing allergic and inflammatory responses. By inhibiting their production, flunisolide reduces inflammation in the nasal passages and relieves symptoms such as congestion, sneezing, and runny nose. 

• Additionally, flunisolide inhibits the activity of inflammatory cells, such as eosinophils and mast cells, which are involved in developing allergic responses. This reduces the recruitment of these cells to the nasal tissues, further reducing inflammation. 

Pharmacokinetics: 

Absorption 

flunisolide is readily absorbed from the respiratory tract when administered as an inhaler. flunisolide’s systemic absorption is low when used as an inhaler, which is desirable since it reduces the risk of systemic side effects.  

Distribution 

flunisolide is distributed widely throughout the body but primarily to tissues with high corticosteroid receptors, such as the lungs. Flunisolide binds to plasma proteins to a moderate extent, around 60%.  

Metabolism 

flunisolide is metabolized in the liver, undergoing extensive biotransformation to several metabolites. The primary metabolites are inactive and are excreted in the urine.  

Elimination and Excretion 

The elimination of flunisolide and its metabolites occurs primarily through the kidneys. The elimination half-life of flunisolide is around 3-4 hours. 

Adminstartion

Administration: 

• flunisolide is a corticosteroid medication used to treat various respiratory conditions, such as asthma and allergic rhinitis. It works by reducing inflammation in the airways and nasal passages. 

• flunisolide is typically administered via inhalation using an inhaler or nebulizer. The recommended dose and frequency of use will depend on the patient’s age, condition, and severity of symptoms. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: flunisolide intranasal 

Pronunciation:  [ floo-NIS-oh-lide ] 

Why do we use flunisolide intranasal? 

flunisolide is a corticosteroid medication primarily used to treat respiratory conditions such as asthma and allergic rhinitis. Here are some common uses of flunisolide: 

• Asthma: flunisolide inhalation is used to prevent and treat asthma symptoms, including wheezing, shortness of breath, and chest tightness. 
• Allergic rhinitis: flunisolide nasal spray treats allergic rhinitis, an inflammation of the nasal passages caused by allergens such as pollen, dust mites, and animal dander. 
• Chronic Obstructive Pulmonary Disease (COPD): flunisolide inhalation may improve breathing and reduce symptoms in people with COPD. 
• Eosinophilic Esophagitis: flunisolide can also treat eosinophilic Esophagitis, an inflammatory condition affecting the esophagus.