Fluocinonide and Flunisolide
What is the difference between Fluocinonide and Flunisolide?
- Fluocinonide and Flunisolide belong to the class of synthetic pharmaceutical drugs/chemicals commonly known as corticosteroids.
- Corticosteroids primarily include steroid hormones (glucocorticoids and mineralocorticoids) and regulate immune response, stress, metabolism, electrolyte level and behavior.
- Chemically they are anti-inflammatory (anti swelling) molecules and available in different forms such as cream and ointments (for skin), nasal spray (for nose or lungs), pills or liquid (for oral use) and injection (for muscles, veins or joints).
- Corticosteroids are used to treat a variety of medical illness such as arthritis (joint pain or inflammation), skin allergy, allergic reactions, asthma, hepatitis, inflammatory diseases, cancer and many more.
- Fluocinonide (marketed under brand name Dermacin, Fluonex, Lonide, Vanos, Lidex, Lidex-E, Lyderm, etc) is a glucocorticoid corticosteroid and widely used topically (directly to the body surface) in the form of cream, ointment, or gel.
- Fluocinonide works as an anti-inflammatory agent to cure various skin disorders i.e. eczema and dermatitis. The medicine helps to treat skin redness, itching, dryness, crusting, scaling, and inflammation.
- Flunisolide is a corticosteroid which is used intranasal in the form of spray/ solution.
- Flunisolide is recommended to treat seasonal allergies, hay fever and allergic rhinitis (allergic inflammation of the nasal airways).
Flunisolide Nasal Spray Solution
Why is this medication prescribed?
- Flunisolide, a corticosteroid, is used to prevent year-round cold or flu symptoms produced by an allergic reaction e. nasal congestion, sneezing, itching, and runny or stuffed nose.
- The drug is also used to treat allergic rhinitis.
- Allergic rhinitis is a medical illness that is caused by an allergicinflammation of the nasal airways. It usually occurs when an allergen is inhaled by an individual with a sensitized immune system. Allergic reaction in nasal airways may cause recurrent sinusitis and increase the risk of developing asthma.
- The drug is also used as a prophylactic therapy to reduce the symptoms of asthma and improve lung function.
Pharmacophore structure: Information about the chemical structure of the drug
Flunisolide belongs to the class of organic synthetic compounds commonly known as 21-hydroxysteroids. Principally, it carries a hydroxyl group at 21 position of the backbone, therefore named as 21-hydroxysteroid. The detailed classification of Flunisolide is as follows
|Super Class||Lipids and lipid-like molecules|
|Class||Steroids and steroid derivatives|
Chemical information of the drug
- Flunisolide is a synthetic pharmaceutical glucocorticoid and chemically named as (1S,2S,4R,8S,9S,11S,12S,13R,19S)-19-fluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.0²,⁹.0⁴,⁸.0¹³,¹⁸]icosa-14,17-dien-16-one.
- It is white to creamy white crystalline powder with a molecular formula C24H31FO
- Molecular weight of Flunisolide is 434.497743 g/mol and melting point is 226-230.
- Flunisolide is soluble in organic solvents (i.e. methanol, acetone etc), while insoluble in water.
What is the source of drug (natural or synthetic)?
- Flunisolide is a synthetic (man-made) pharmaceutical adreno-corticosteroid.
What is the available strength of the drug?
- Flunisolide is available as nasal solution (Flunisolide nasal spray 0.025% w/w) with a metered dose inhaler/spray unit.
- The formulation contains Flunisolide, butylated hydroxytoluene, benzalkonium chloride, citric acid, edetate disodium, polysorbate 20, propylene glycol, sodium citrate, polyethylene glycol 400, sorbitol and water.
- Each unit of Flunisolide contains 25 ml that can deliver 200 metered spray.
- Each spray of the unit deliver metered spray of 100 mg formulation containing 29 mcg of Flunisolide.
What is the generic and brand name of Flunisolide?
- The drug is available under generic name Flunisolide Nasal spray or solution.
- The Flunisolide is marketed under different brand names such as AeroBid (Roche), Bronalide (Krewel), Nasalide (Teva Santé), Nasarel, Rhinalar (Syntex) and Syntaris (Teva).
How the Flunisolide medicine works (mode of action)?
- The principle mode of action of Flunisolide is mediated through binding and subsequent activation of glucocorticoid receptors, which results in suppression of immune responses and inflammation.
- Glucocorticoid receptors are involved in regulation of development,metabolism, and immune response.
- As a response of Flunisolide binding, glucocorticoid receptors get activated and up regulate the expression of anti inflammatory proteins (biomolecules, which reduce the swelling/inflammation).
- The effect of topical Flunisolide is not immediate and requires regular use for at least a few days to get relief.
What are the recommended doses of Flunisolide nasal spray/solution?
The concentration of Flunisolide in nasal spray or solution is 0.025%. However, the dose varies depending upon paediatric and adult uses.
- The prescribed dose of Flunisolide nasal solution for adult generally ranges between 2 or 3 sprays (58 mcg) in each nostril for 2-3 times per day (total 232 -348 mcg/day).
- The maximum dose limit for adult is 8 sprays for per day in each nostril (464 mcg/day).
- For pediatric use (children between 6-14 year age), only one spray (29 mcg) in each nostril for 3 times per day (total 174 mcg/day)
- or 2 spray in each nostril for 2 times per day (total dose 232 mcg/day).
- The maximum daily limit for paediatric uses of Flunisolide nasal solution is 4 sprays in each nostril per day (total dose 232 mcg/day).
- Flunisolide nasal solution is not prescribed for children below the age of 6 years.
What are the pharmacokinetic properties of the drug?
- Flunisolide is rapidly absorbed and metabolized in the liver to less active primary metabolite (S beta-OH ) and to glucuronide and sulfate conjugates.
- The average plasma half life of the drug is 1.8 hours in human body.
- It has been observed that following administration half of the drug is recovered in urine and the remaining half in stool.
- Only 20% of the total oral supplied Flunisolide enter in to systematic circulation unmetabolized.
- Each nasal spray of Flunisolide nasal solution contains 29 mcg of the drug.
- The clinical effectiveness of Flunisolide is primarily due to the direct topical effect rather than the indirect outcome through systemic absorption.
Which pregnancy category (A; B; C; D; X) has been assigned to Flunisolide?
- The pregnancy category C (risk cannot be ruled out) has been assigned to Flunisolide by FDA.
- The medication has been recommended during pregnancy only when benefit outweighs risk.
How to prepare the drugs?
The drug is available in ready to use in nasal solution form (0.025 % and 25 ml per pack) and applied directly as inhaler. The Flunisolide nasal solution is supplied in a white, HDPE (high density polyethylene) bottle. The bottle/container is built-in with a protective cap, metered nasal spray pump, and white actuator. Each unit contains ~ 200 metered nasal spray and instruction leaflet.
How to use Flunisolide nasal solution?
Flunisolide is available as nasal solution to inhale/spray through the nose. Generally it is recommended to inhale 1-4 times a day at specific time intervals. Before use, please read carefully the written instructions leaflet provided along with the medication. Follow the illustrated directions as prescribed for proper use of medication.
For proper use of nasal inhaler, please follow these steps:
- Wash your hands before use of the inhaler.
- Clear your nasal passage.
- To use nasal spray break the seal and remove the safety clip and plastic cap of the nasal inhaler.
- Shake properly every time before the use of inhaler.
- Put in the tip of the nasal inhaler into one of your nostril (~0.6 cm).
- Close the other nostril gently with your finger tip and tilt your head slightly forward and, keeping the bottle upright.
- Press the inhaler to release the drug and sniff gently in through the nose, keeping your mouth closed.
- Hold the breath for a few seconds.
- Take away the inhaler from your nose.
- Clean gently the tip of the nasal inhaler with a tissue paper.
- Re-place the plastic cap.
- Evade blowing your nose for 15 minutes after using this medication
- Repeat the step again in other nostril. Wipe the applicator tip and replace the plastic cap.
- Repeat the steps each time during use of inhaler.
- Repeat the Step 1. Wash your hands again after use of the medication.
Follow the instruction as per on the prescription label, and if you have any queries regarding the use ask pharmacist, doctor or respiratory therapist. Do not overuse the inhaler as prescribed by your doctor. Do not stop using Flunisolide without talking to your doctor.
How to store the Flunisolide drug?
Flunisolide is stored at room temperature 20° to 25°C (68° to 77°F). The container should be tightly closed and away from excess heat, direct sun light and reach of children. Do not freeze or store the medicine at extreme cold too.
How to dispose the Flunisolide?
- Throw away unused and opened, outdated or no longer used container.
- Also dispose the old medicine after the expiration date.
- Talk to your pharmacist about the proper disposal of your medication.
Does Flunisolide has approval from government / FDA /or any other related agencies?
- The drug has received its official approval from US Food and Drug Administration (FDA) in September 1981.
Other uses of the drug
- Flunisolide nasal solution may also be used to treat other allergic problems not listed here.
What special dietary precautions should I follow?
- Follow a routine protein rich and potassium rich diet and avoid high sodium salt
What special precautions should I follow?
- Do not use the medicine during anasthma
- Do not use the medicine if you are hypersensitive to any of the ingredients.
- Do not use the medicine in the presence of nasal mucosal infection.
- Do not use the medicine if you are suffering from chicken pox or measles. These conditions can be deadly or very serious due to steroid medication.
What are the possible side effects of “Flunisolide” drug?
Long term controlled clinical trial studies with Flunisolide nasal solution suggested that adverse reactions associated with the drug use are primarily nasal mucous membrane. The most common problem in 45% of the patients is nasal burning and stinging. The most common side effect of Flunisolide use are cough, crusting of nose, nose bleeding, temporary dryness or irritation in nose/throat, pain or sores in nose sneezing and taste/smell problems. If the side effects persist for a long time or get worse consult immediately with your doctor.
- Prolonged use and high dose result in absorption of Flunisolide in blood stream and therefore may cause severe tiredness, headache, weight loss, swelling of ankles/feet, vision problems and increased thirst/urination. If such symptoms appear tell your doctor right away.
- It has been observed that some medical conditions (disease) may also associate with too much use of Flunisolide, which are similar to overdose of other corticosteroid drugs. These include hyperadrenocorticism (cataracts, menstrual irregularities, and cushingoid features), infections, corneal perforation, and reduction in bone density and ocular toxicities (elevated intraocular pressure).
- Severe allergic reaction is rare but if you notice persistent sore throat, ear pain, fever, chills, white patches or itching/swelling (especially of the face/tongue/throat), seek immediate medical attention .
- However, these side effects rarely occur (due to topical use and low dose). The risk factor rises only when a high dose of Flunisolide is used for a long time.
What should I do in case of overdose?
- Flunisolide overdose usually occurs when someone by mistake or deliberately takes more than the prescribed limit of this medication. In case of overdose, do not panic and contact with your doctor or emergency room immediately.
- It has been observed in animal studies that intravenous Flunisolide did not show any marked effect at doses up to 4 mg/kg. A spray bottle of drug usually contain 6.25mg of Flunisolide, therefore cannot cause acute over dosage.
- Do not share the medication with other person suffering from a similar problem.
- Do not use the medication for a longer period of time.
What should I do in case of missed a dose?
- In case of missed dosage, take it as soon as you remember and maintain a regular dosing schedule.
- Keep in mind to not use a double dose to make up a missed dose
Does Flunisolide has any interaction with food, drugs and diseases?
- No significant food interactions have been reported for Flunisolide.
- Flunisolide may interact with other corticosteroid drugs such as prednisone and increase the risk of their side effects.
- Drug interaction studies of Flunisolide revealed that it interacts with 59 drugs (174 brand and generic names). Therefore, it is mandatory to inform your doctor about any medicines, vitamins, and herbal supplements you take.
- It has been observed that some medical conditions (disease) may also interact with Flunisolide such as ……
The intense use of inhaled and nasal corticosteroids such as Flunisolide may aggravate conditions of hyperadrenocorticism. The key symptoms are development of acneiform lesions, cataract, menstrual irregularities, and cushingoid features .
The corticosteroids work through suppression of immune system thus may likely to reduce the ability to localize infections, mask the symptoms of infection.
Ocular Herpes Simplex
Higher dosage of Flunisolide can cause corneal perforation in patients with ocular herpes.
The most common side effect of prolonged usage of corticosteroids is associated with a reduction in bone density.
Prolonged use of corticosteroids may cause cataract and elevated intraocular pressure thus can cause glaucoma and/or damage to the optic nerves.
Clinical research and current scenario of the drug
Clinical human Trials of Flunisolide nasal solution (Flunisolide nasal spray .025%, for up to 6 weeks at doses up to 300 mcg per day) have shown to be effective in treating the symptoms of allergic rhinitis, nasal congestion and sneezing.
- A pivotal, 3-center trial with 196 patients with seasonal allergic rhinitis showed statistically significant results following Flunisolide treatments.
- Animal studies with Flunisolide have shown teratogenic nature of the drug (an agent that can harm foetus and can generate birth defects). However, control human studies are not available.
- Animal studies have shown that Flunisolide acts as a potent glucocorticoid and weak mineralocorticoid. It has been observed that Flunisolide is ~180 times more potent a glucocorticoid than the cortisol standard.
- Controlled clinical trials of Flunisolide nasal solution (Flunisolide nasal spray .025%) effect on hypothalamic-pituitary-adrenal (HPA) axis function have suggested no significant effect on endogenous cortisol production in adult volunteers.
References from chemical, biological and toxicological databases.
Flunisolide:Pubchem open chemistry database. http://pubchem.ncbi.nlm.nih.gov/compound/flunisolide#section=Toxicity.Flunisolide:Drug bank database. http://www.drugbank.ca/drugs/DB00180.
FDA: Information by drug class. http://www.fda.gov/Drugs/DrugSafety/InformationbyDrugClass/ucm193896.html.
Flunisolide: Medline plus drug information. http://www.nlm.nih.gov/medlineplus/druginfo/meds/a601054.html.
US National Library of Medicine, NIH. Retrieved6 March 2014. http://www.nlm.nih.gov/medlineplus/druginfo/meds/a601054.html#how
Pharmacokinetics of intranasal corticosteroids. http://www.ncbi.nlm.nih.gov/pubmed/11449203
Systemic effects of intranasal steroids: an endocrinologist’s perspective. http://www.ncbi.nlm.nih.gov/pubmed/11032642
Topical glucocorticosteroids in rhinitis: clinical aspects. http://www.ncbi.nlm.nih.gov/pubmed/16923704
Drug therapy: inhaled glucocorticoids for asthma. http://www.nejm.org/doi/full/10.1056/NEJM199503303321307