Due to the low bioavailability by the intranasal route, the majority of the pharmacokinetic data was obtained via other routes of administration. Studies using oral dosing of radiolabeled drug have demonstrated that fluticasone propionate is highly extracted from plasma and absorption is low.
Oral bioavailability is negligible, and the majority of the circulating radioactivity is due to an inactive metabolite. Following intravenous administration, the initial disposition phase for fluticasone propionate was rapid and consistent with its high lipid solubility and tissue binding. The volume of distribution averaged 4. Fluticasone propionate is weakly and reversibly bound to erythrocytes and freely equilibrates between erythrocytes and plasma.
Fluticasone propionate is not significantly bound to human transcortin. Other metabolites detected in vitro using cultured human hepatoma cells have not been detected in man.
Following intravenous dosing, fluticasone propionate showed polyexponential kinetics and had a terminal elimination half-life of approximately 7. Fluticasone Propionate Nasal Spray, USP, was not studied in any special populations, and no gender-specific pharmacokinetic data have been obtained.
Fluticasone propionate is a substrate of cytochrome P 3A4. Coadministration of fluticasone propionate and the highly potent cytochrome P 3A4 inhibitor ritonavir is not recommended based upon a multiple- dose, crossover drug interaction study in 18 healthy subjects. Fluticasone propionate aqueous nasal spray mcg once daily was coadministered for 7 days with ritonavir mg twice daily.
Caution should be exercised when other potent cytochrome P 3A4 inhibitors are coadministered with fluticasone propionate. In a drug interaction study, coadministration of orally inhaled fluticasone propionate 1, mcg and ketoconazole mg once daily resulted in increased fluticasone propionate exposure and reduced plasma cortisol AUC, but had no effect on urinary excretion of cortisol.
In another multiple-dose drug interaction study, coadministration of orally inhaled fluticasone propionate mcg twice daily and erythromycin mg 3 times daily did not affect fluticasone propionate pharmacokinetics. In a trial to evaluate the potential systemic and topical effects of Fluticasone Propionate Nasal Spray, USP, on allergic rhinitis symptoms, the benefits of comparable drug blood levels produced by Fluticasone Propionate Nasal Spray, USP, and oral fluticasone propionate were compared.
The dosages used were mcg of Fluticasone Propionate Nasal Spray, USP, the nasal spray vehicle plus oral placebo , and 5 and 10 mg of oral fluticasone propionate plus nasal spray vehicle per day for 14 days.
Plasma levels were undetectable in the majority of patients after intranasal dosing, but present at low levels in the majority after oral dosing.
Fluticasone Propionate Nasal Spray, USP, was significantly more effective in reducing symptoms of allergic rhinitis than either the oral fluticasone propionate or the nasal vehicle. This trial demonstrated that the therapeutic effect of Fluticasone Propionate Nasal Spray, USP, can be attributed to the topical effects of fluticasone propionate.
Fluticasone Propionate Nasal Spray, USP, given as mcg once daily or mcg twice daily was compared with placebo or oral prednisone 7. Fluticasone Propionate Nasal Spray, USP, at either dosage for 4 weeks did not affect the adrenal response to 6-hour cosyntropin stimulation, while both dosages of oral prednisone significantly reduced the response to cosyntropin.
A total of 13 randomized, double-blind, parallel-group, multicenter, vehicle placebo-controlled clinical trials were conducted in the United States in adults and pediatric patients 4 years of age and older to investigate regular use of Fluticasone Propionate Nasal Spray, USP, in patients with seasonal or perennial allergic rhinitis. The trials included 2, adults 1, men and 1, women with a mean age of 37 range, 18 to 79 years.
A total of adolescents boys and 35 girls , mean age of 14 range, 12 to 17 years , and children boys and girls , mean age of 9 range, 4 to 11 years were also studied. These trials evaluated the total nasal symptom scores TNSS that included rhinorrhea, nasal obstruction, sneezing, and nasal itching in known allergic patients who were treated for 2 to 24 weeks. Nasal mucosal basophils and eosinophils were also reduced at the end of treatment in adult studies; however, the clinical significance of this decrease is not known.
There were no significant differences between fluticasone propionate regimens whether administered as a single daily dose of mcg two mcg sprays in each nostril or as mcg one mcg spray in each nostril twice daily in 6 clinical trials. A clear dose response could not be identified in clinical trials. Patients were instructed to take the study medication only on days when they thought they needed the medication for symptom control, not to exceed 2 sprays per nostril on any day, and not more than once daily.
The studies demonstrated significantly greater reduction in TNSS sum of nasal congestion, rhinorrhea, sneezing, and nasal itching with Fluticasone Propionate Nasal Spray, USP, mcg compared to placebo.
The relative difference in efficacy with as-needed use as compared to regularly administered doses was not studied.
Three randomized, double-blind, parallel- group, vehicle placebo-controlled trials were conducted in 1, patients to investigate regular use of Fluticasone Propionate Nasal Spray, USP, in patients with perennial nonallergic rhinitis.
These trials evaluated the patient-rated TNSS nasal obstruction, postnasal drip, rhinorrhea in patients treated for 28 days of doubleblind therapy and in 1 of the 3 trials for 6 months of open-label treatment. Two of these trials demonstrated that patients treated with Fluticasone Propionate Nasal Spray, USP, at a dosage of mcg twice daily exhibited statistically significant decreases in TNSS compared with patients treated with vehicle.
Adult patients may be started on a mcg once-daily regimen two mcg sprays in each nostril once daily. Individual patients will experience a variable time to onset and different degree of symptom relief. Maximum effect may take several days. Greater symptom control may be achieved with scheduled regular use. Efficacy of asneeded use of Fluticasone Propionate Nasal Spray, USP, has not been studied in pediatric patients under 12 years of age with seasonal allergic rhinitis, or patients with perennial allergic or nonallergic rhinitis.
Pediatric patients 4 years of age and older should be started with mcg 1 spray in each nostril once daily. Treatment with mcg 2 sprays in each nostril once daily or 1 spray in each nostril twice daily should be reserved for pediatric patients not adequately responding to mcg daily.
Once adequate control is achieved, the dosage should be decreased to mcg 1 spray in each nostril daily. There is no evidence that exceeding the recommended dose is more effective.
Fluticasone Propionate Nasal Spray, USP, is indicated for the management of the nasal symptoms of seasonal and perennial allergic and nonallergic rhinitis in adults and pediatric patients 4 years of age and older. Safety and effectiveness of Fluticasone Propionate Nasal Spray, USP, in children below 4 years of age have not been adequately established. Fluticasone Propionate Nasal Spray, USP, is contraindicated in patients with a hypersensitivity to any of its ingredients.
The replacement of a systemic corticosteroid with a topical corticosteroid can be accompanied by signs of adrenal insufficiency, and in addition some patients may experience symptoms of withdrawal, e. Patients previously treated for prolonged periods with systemic corticosteroids and transferred to topical corticosteroids should be carefully monitored for acute adrenal insufficiency in response to stress. In those patients who have asthma or other clinical conditions requiring long-term systemic corticosteroid treatment, too rapid a decrease in systemic corticosteroids may cause a severe exacerbation of their symptoms.
During postmarketing use, there have been reports of clinically significant drug interactions in patients receiving fluticasone propionate and ritonavir, resulting in systemic corticosteroid effects including Cushing syndrome and adrenal suppression. It's important that your child only uses the spray prescribed for them.
Some nasal sprays contain fluticasone mixed with an antihistamine. Brand names include Dymista. Most adults can use fluticasone nasal spray. To make sure the nasal spray or drops are safe for you, tell your doctor or pharmacist if you: are allergic to fluticasone or any other medicines are taking or have recently taken other corticosteroid medicines have had nose surgery have an infection in your nose are pregnant or trying to get pregnant.
How to use the spray Fluticasone nasal spray needs to be used regularly for it to work. Remove the cap and gently shake the bottle. Blow your nose gently, then close 1 nostril with your finger. Bend your head forward slightly and carefully put the nozzle into your other nostril.
Slowly breathe in through your nose and with your fingers press down on the widest part of the nozzle to squirt the spray once into your nostril.
Breathe out through your mouth. Follow steps 3 and 4 again to squirt a second spray if you need it into the same nostril. Repeat the process with the other nostril if you need it. How to use the drops Fluticasone drops come in small plastic containers called "nasules".
Follow the instructions that come with your nasal drops. Blow your nose gently. Follow the pictures in the manufacturer's leaflet to get your head into the right position.
Carefully put the container into 1 nostril and gently squeeze. Keep squeezing until the sides of the container touch each other, then release.
This will mean that you've had about half of the dose about 6 drops. Follow steps 3 and 4 again to use the rest of the drops in your other nostril. Do not keep the container. Only use it once. Will my dose go up or down? What if I forget to use it? Do not take a double dose to make up for a forgotten one.
What if I take too much? Common side effect These common side effects can happen in more than 1 in people. Keep taking the medicine but talk to your doctor if these side effects bother you or do not go away: an unpleasant taste or smell a dry or sore nose, or nosebleeds a dry or sore throat, or hoarse voice headache Serious side effects Serious side effects are rare. Tell a doctor immediately if you get: problems with your breathing damage to your nose or sores inside your nose changes in your eyesight, such as blurred vision or a cloudy lens in the eye — these can be signs of increased pressure in your eyes glaucoma or a cataract Serious allergic reaction It happens rarely, but it is possible to have a serious allergic reaction anaphylaxis to fluticasone.
Information: You can report any suspected side effect to the UK safety scheme. What to do about: unpleasant taste or smell — rinse your mouth with water or have a drink of water. Speak to your doctor or a pharmacist if these side effects do not go away. Do not drink too much alcohol. Talk to your doctor if the headache does not go away or is severe.
Fluticasone and pregnancy If you are pregnant, speak to your doctor or a pharmacist before buying fluticasone nasal spray at a pharmacy or supermarket. Fluticasone and breastfeeding It's generally OK to use your fluticasone nasal spray or drops as normal while you're breastfeeding.
Non-urgent advice: Talk to your doctor if you're:. Check with a pharmacist or your doctor if you're taking: medicines used to treat HIV, such as ritonavir or cobicistat medicines used to treat fungal infections, such as ketoconazole or itraconazole other medicines that contain steroids, such as eczema creams, asthma inhalers, tablets, injections, other nasal sprays and drops, or eye drops Mixing fluticasone with herbal remedies or supplement There's very little information about taking herbal remedies and supplements together with fluticasone.
Important Tell your doctor or a pharmacist if you're taking any other medicines, including herbal remedies, vitamins or supplements. How does fluticasone work?
Fluticasone is a corticosteroid steroid medicine. Maintain regular regimen. Respiratory tract tuberculosis. Infections eg, ocular herpes simplex. If exposed to measles or chickenpox, consider anti-infective prophylactic therapy. If adrenal insufficiency exists following systemic corticosteroid therapy, replacement with topical corticosteroids may exacerbate symptoms of adrenal insufficiency eg, depression.
Drug information provided by: IBM Micromedex. This medicine comes with patient instructions. Read and follow these instructions carefully. Ask your doctor or pharmacist if you have any questions.
This medicine is for use only in the nose. Do not get any of it in your eyes or on your skin. If it does get on these areas, rinse it off right away. The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine.
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